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ANTIBIOTICSANTIBIOTICS
IN DENTISTRYIN DENTISTRY
 INDIAN DENTAL ACADEMYINDIAN DENTAL ACADEMY
 Leader in continuing Dental EducationLeader in continuing Dental Education
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CONTENTSCONTENTS
IntroductionIntroduction
DefinitionDefinition
HistoryHistory
ClassificationClassification
PropertiesProperties
AntibioticsAntibiotics
Combination antibiotic therapyCombination antibiotic therapy
Local delivery of antibioticsLocal delivery of antibiotics
ConclusionConclusion
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 Pulpal and Periapical PathogensPulpal and Periapical Pathogens ––
V G SV G S ,, Beta – hemolytic streptococci, ProvetellaBeta – hemolytic streptococci, Provetella
Fusobacteria, Actinomyces, Porphyromonas gingivalisFusobacteria, Actinomyces, Porphyromonas gingivalis
Candida albicans ,Staphylococcus, Entero coccus.Candida albicans ,Staphylococcus, Entero coccus.
 Periodontal Diseases -Periodontal Diseases -
Porphyromonas gingivalis,Porphyromonas gingivalis, Provetella, FusobacteriaProvetella, Fusobacteria ,,
Actinobacillus actinomycetemcomitansActinobacillus actinomycetemcomitans,,
Campylobacter , Trepanoma Denticola , Bacteroids .Campylobacter , Trepanoma Denticola , Bacteroids .
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Indian Dental academy
• www.indiandentalacademy.com
• Leader continuing dental education
• Offer both online and offline dental courses
 Acute necrotizing ulcerative gingivitis –Acute necrotizing ulcerative gingivitis –
Treponema, FusobacteriaTreponema, Fusobacteria ,, Provetella, Veillonella ,Provetella, Veillonella ,
Neisseria , Bacteroids , Actinomyces, CapnocytophagaNeisseria , Bacteroids , Actinomyces, Capnocytophaga ..
 Pericoronitis –Pericoronitis –
V G S , Actinomyces israeliiV G S , Actinomyces israelii ,, Provetella, Neisseria ,Provetella, Neisseria ,
Bacteroids , Actinomyces, Capnocytophaga ,Bacteroids , Actinomyces, Capnocytophaga ,
Staphylococci, Lactobacilli, Fusobacteria ,Staphylococci, Lactobacilli, Fusobacteria ,
Porphyromonas .Porphyromonas .
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 Periimplantitis -Periimplantitis -
Bacteroids , FusobacteriaBacteroids , Fusobacteria ,, PorphyromonasPorphyromonas
gingivalis, Provetella, Campylobacter ,gingivalis, Provetella, Campylobacter ,
Trepanoma, V G S , Actinomyces.Trepanoma, V G S , Actinomyces.
 Osteomyelitis –Osteomyelitis –
Staphylococcus aureusStaphylococcus aureus ,,
VGS , Actinomyces, Fusobacteria , Provetella,VGS , Actinomyces, Fusobacteria , Provetella,
Eubacterium , Eikenella.Eubacterium , Eikenella.
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 Ludwig’s angina –Ludwig’s angina –
VGS ,VGS ,
Staphylococci , Porphyromonas gingivalis, Provetella,Staphylococci , Porphyromonas gingivalis, Provetella,
Pseudomonas aeruginosa , Klebsiella Haemophilus .Pseudomonas aeruginosa , Klebsiella Haemophilus .
 Mediastinal infections –Mediastinal infections –
VGS ,VGS ,
PorphyromonasPorphyromonas, Provetella, Fusobacteria ,, Provetella, Fusobacteria ,
Staphylococci .Staphylococci .
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DEFINITIONDEFINITION
 AntibioticAntibiotic --
Are substances produced by various speciesAre substances produced by various species
of microorganisms (bacterial, fungi, andof microorganisms (bacterial, fungi, and
actinomycetes) that suppress the growth ofactinomycetes) that suppress the growth of
or kill other microorganisms at very lowor kill other microorganisms at very low
concentrationconcentrations.s.
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 Antimicrobial agentAntimicrobial agent --
Synthetic as well as a naturally obtained drug thatSynthetic as well as a naturally obtained drug that
attenuate the microorganisms.attenuate the microorganisms.
They inhibit or kill the infecting organisms andThey inhibit or kill the infecting organisms and
has no or minimal effect on the recipienthas no or minimal effect on the recipient..
DEFINITIONDEFINITION
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 ChemotherapyChemotherapy ––
Treatment of systemic infections with specificTreatment of systemic infections with specific
drugs that selectively suppress the infectingdrugs that selectively suppress the infecting
microorganisms without significantly affectingmicroorganisms without significantly affecting
the host .the host .
Treatment of neoplastic diseases with drugs isTreatment of neoplastic diseases with drugs is
also called Chemotherapy.also called Chemotherapy.
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HISTORYHISTORY
Three phasesThree phases
Period of empirical phasePeriod of empirical phase ::
E.g.E.g. Chaulmoogra oil - LeprosyChaulmoogra oil - Leprosy
Mouldy curd - BoilsMouldy curd - Boils
Mercury - SyphilisMercury - Syphilis
Cinchona bark – FeverCinchona bark – Fever
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 Ehrlich’s phase : (1890-1935)Ehrlich’s phase : (1890-1935)
 Selectively stain microbes-Selectively stain microbes- DyesDyes(methylene blue)(methylene blue)
 Selectively toxic to the organisms .Selectively toxic to the organisms .
 Arsenicals-atoxyl - Sleeping sickness (1906)Arsenicals-atoxyl - Sleeping sickness (1906)
Norarsephenamine -Norarsephenamine -
Syphilis ( 1909)Syphilis ( 1909)
 He coined the termHe coined the term ‘chemotherapy’‘chemotherapy’
 ‘‘Father of modern chemotherapyFather of modern chemotherapy’’
 Awarded theAwarded the Nobel Prize in 1909.Nobel Prize in 1909.
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 Pasteur (1877)
Antibiosis
Growth of Anthrax Bacilli in urine was
inhibited by air born bacteria
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 The modern era of chemotherapy.
 Domagk (1935)
Therapeutic effect of Prontosil, Sulfonamide
dye, in pyogenic infection.
The active moiety was Para-amino benzene
sulfonamide, and the dye part was not essential.
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 Sir Alexander Fleming (1929)Sir Alexander Fleming (1929)
 Culture plates contaminated by aCulture plates contaminated by a
fungusfungus (Penicillium notatum)(Penicillium notatum)
 Prevented the growth ofPrevented the growth of
surrounding bacterial colonies.surrounding bacterial colonies.
 The fungal filtrate, which he namedThe fungal filtrate, which he named
PenicillinPenicillin
 FloreyFlorey and Chain (1941)and Chain (1941)
 Purified this fungal growth andPurified this fungal growth and
clinically used for treating theclinically used for treating the
wounds and diseases.wounds and diseases.
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ClassificationClassification
 Based on mechanism of action.Based on mechanism of action.
Inhibits cell wall synthesisInhibits cell wall synthesis
E.g. Penicillin's, Cephalosporin's, Vancomycin ,E.g. Penicillin's, Cephalosporin's, Vancomycin ,
Bacitracin.Bacitracin.
Act on the cell wall membraneAct on the cell wall membrane
E.g. Nystatin and Amphotericin - BE.g. Nystatin and Amphotericin - B..
Affect the function of 30s and 50s RibosomalAffect the function of 30s and 50s Ribosomal
subunitssubunits
E.g.E.g. Chloramphenicol, Tetracycline's andChloramphenicol, Tetracycline's and
Clindamycin, Erythromycin.Clindamycin, Erythromycin.
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Misreading of m- RNA codeMisreading of m- RNA code
E.g. AminoglycosidesE.g. Aminoglycosides
Inhibit DNA gyraseInhibit DNA gyrase
E.g. FluroquinolonesE.g. Fluroquinolones
Interfere with DNA functionInterfere with DNA function
E.g. Rifampin , MetronidazoleE.g. Rifampin , Metronidazole
Interfere with DNA synthesisInterfere with DNA synthesis
E.g.E.g.
Idoxuridine , Acyclovir , ZidovudineIdoxuridine , Acyclovir , Zidovudine
Interfere with intermediary metabolismInterfere with intermediary metabolism
E.g. Sulfonamides, Trimethoprim , EthambutolE.g. Sulfonamides, Trimethoprim , Ethambutolwww.indiandentalacademy.com
Based on Type of action:Based on Type of action:
Bacteriostatic antibioticsBacteriostatic antibiotics ––
Inhibits the growth and multiplicationInhibits the growth and multiplication
e.g.e.g. Sulfonamides,Sulfonamides, Chloramphenicol, Tetracycline'sChloramphenicol, Tetracycline's
and Erythromycinand Erythromycin
Bactericidal antibioticsBactericidal antibiotics ––
kill micro-organisms by interfering with the synthesis orkill micro-organisms by interfering with the synthesis or
function of either the cell wall, cell membrane or both.function of either the cell wall, cell membrane or both.
e.g.e.g. Penicillin's, cephalosporins, VancomycinPenicillin's, cephalosporins, Vancomycin
Aminoglycosides, Rifampin .Aminoglycosides, Rifampin .
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Based on Spectrum of activityBased on Spectrum of activity
Narrow spectrum.Narrow spectrum.
Penicillins, Erythromycin, Streptomycin.Penicillins, Erythromycin, Streptomycin.
Broad spectrum.Broad spectrum.
Tetracycline's , ChloramphenicolTetracycline's , Chloramphenicol
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 Based on chemical structureBased on chemical structure
Beta – lactam antibioticsBeta – lactam antibiotics
Penicillins, Cephalosporins, MonobactemsPenicillins, Cephalosporins, Monobactems ..
QuinolonesQuinolones
Nalidixic acid, Norfloxacin, CiprofloxacinNalidixic acid, Norfloxacin, Ciprofloxacin
Tetracycline'sTetracycline's
Oxytetracycline, DoxycyclineOxytetracycline, Doxycycline
SulfonamidesSulfonamides
Sulfadiazine, Sulfones – DapsonesSulfadiazine, Sulfones – Dapsones
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AminoglycosidesAminoglycosides
Streptomycin, Gentamicin, NeomycinStreptomycin, Gentamicin, Neomycin
Nitrobenzene derivativesNitrobenzene derivatives
ChloramphenicolChloramphenicol
DiaminopyrimidinesDiaminopyrimidines
Trimethoprim, PyrimethamineTrimethoprim, Pyrimethamine
Macrolide antibioticsMacrolide antibiotics
Erythromycin, Roxithromycin, AzithromycinErythromycin, Roxithromycin, Azithromycin
NitroimidazolesNitroimidazoles
Metronidazole, TinidazoleMetronidazole, Tinidazole
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Polyene antibioticsPolyene antibiotics
Nystatin, Amphotericine – B .Nystatin, Amphotericine – B .
Nicotinic acid derivativesNicotinic acid derivatives
Isoniazid, Pyrazinamide, EthionamideIsoniazid, Pyrazinamide, Ethionamide
Polypeptide antibioticsPolypeptide antibiotics
Polymyxin – B , Colistin , BacitracinPolymyxin – B , Colistin , Bacitracin
Imidazole derivativesImidazole derivatives
Miconazole, Clotrimazole, Ketoconazole, FluconazoleMiconazole, Clotrimazole, Ketoconazole, Fluconazole
OthersOthers
Rifampin, Lincomycin, Clindamycin, VancomycinRifampin, Lincomycin, Clindamycin, Vancomycin
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Properties of an ideal antibiotic:Properties of an ideal antibiotic:
 SSelective and effective against micro-organismselective and effective against micro-organisms
 Destroy micro-organismsDestroy micro-organisms ((Bactericidal action)Bactericidal action)
Retard their growthRetard their growth (Bacteriostatic action).(Bacteriostatic action).
 Not be ineffective as a result of bacterial resistance.Not be ineffective as a result of bacterial resistance.
 Not be inactivated by enzymes, plasma proteins or body fluids.Not be inactivated by enzymes, plasma proteins or body fluids.
 Quickly reach bactericidal levels throughout the body and beQuickly reach bactericidal levels throughout the body and be
maintained for long periods.maintained for long periods.
 Minimal adverse effects.Minimal adverse effects.
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Choice of an antimicrobial agentChoice of an antimicrobial agent
Patient FactorPatient Factor
AgeAge
 Chloramphenicol – Gray Baby SyndromeChloramphenicol – Gray Baby Syndrome
 Amino glycosides – VIII nerve toxicityAmino glycosides – VIII nerve toxicity
 Tetracycline – Discolor teeth , Weaken BoneTetracycline – Discolor teeth , Weaken Bone
Renal and Hepatic FunctionRenal and Hepatic Function
 Drugs to be avoided in Renal FailureDrugs to be avoided in Renal Failure
- Cephalosporin's, Amino glycosides , Tetracycline ,- Cephalosporin's, Amino glycosides , Tetracycline ,
Amphotericin BAmphotericin B
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 Drugs to be avoided in Liver diseasesDrugs to be avoided in Liver diseases
- Erythromycin , Tetracycline , Nilidixic acid- Erythromycin , Tetracycline , Nilidixic acid
Local FactorsLocal Factors
 Pus and SecretionsPus and Secretions
 HematomasHematomas
 Foreign materialsForeign materials
Drug allergyDrug allergy
 History of Previous exposures to AMAsHistory of Previous exposures to AMAs
Impaired Host DefenseImpaired Host Defense
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PregnancyPregnancy
 Safe –Safe –
Penicillin's , Cephalosporin's , ErythromycinPenicillin's , Cephalosporin's , Erythromycin
 Unsafe –Unsafe –
Tetracycline - Acute Yellow Atrophy – MotherTetracycline - Acute Yellow Atrophy – Mother
Teeth & Bone deformities – OffspringTeeth & Bone deformities – Offspring
Aminoglycosides – Fetal ear damageAminoglycosides – Fetal ear damage
Clotrimoxazole , Chloramphenicol , SulfonamidesClotrimoxazole , Chloramphenicol , Sulfonamides
Genetic Factor –Genetic Factor –
Primaquine , Sulfonamides , Chloramphenicol –Primaquine , Sulfonamides , Chloramphenicol –
Haemolycis in G – 6 PD deficiency patientHaemolycis in G – 6 PD deficiency patient
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Organism Related ConsiderationsOrganism Related Considerations
 Clinical DiagnosisClinical Diagnosis
 Bacteriological ExaminationBacteriological Examination
Drug FactorsDrug Factors
 Spectrum of activitySpectrum of activity
 Type of ActivityType of Activity
 Sensitivity of the organismSensitivity of the organism
 Relative ToxicityRelative Toxicity
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 Route of AdministrationsRoute of Administrations
Penicillin G, Carbenicillin ,Vancomycin,Penicillin G, Carbenicillin ,Vancomycin,
Aminoglycosides.Aminoglycosides.
 Evidence of Clinical EfficacyEvidence of Clinical Efficacy
Reliable clinical trail data – Final guideReliable clinical trail data – Final guide
 CostCost
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DRUG RESISTANCEDRUG RESISTANCE
Unresponsiveness of a microorganism toUnresponsiveness of a microorganism to
Antimicrobial agentsAntimicrobial agents
A bacteria ,which as sensitive originally becomesA bacteria ,which as sensitive originally becomes
Insensitive on further exposure easily be seen withInsensitive on further exposure easily be seen with
Staphylococcus AureusStaphylococcus Aureus
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 Reasons for antibiotic resistanceReasons for antibiotic resistance
Irrational antibiotic use – Wrong indicationIrrational antibiotic use – Wrong indication
- Wrong doses- Wrong doses
- Wrong duration- Wrong duration
Self medicationSelf medication
Local resistance patterns unavailable to physicianLocal resistance patterns unavailable to physician
Patient emphasize on Expensive and Newer drugsPatient emphasize on Expensive and Newer drugs
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MechanismMechanism
 BiochemicalBiochemical
 Inactivation of the antibiotics by enzymesInactivation of the antibiotics by enzymes
Produced by bacteriaProduced by bacteria
e.g. Penicillinasee.g. Penicillinase
 Beta- lactamase are produced by staphylococci,Beta- lactamase are produced by staphylococci,
Haemophilus, GonococciHaemophilus, Gonococci
 Chloramphenicol – Acetyl transferase -Chloramphenicol – Acetyl transferase -
Resistant E.Coli , H. Influenzae , S. TyphiResistant E.Coli , H. Influenzae , S. Typhi
 Aminoglycoside - Adenylate , Acetylate ,Aminoglycoside - Adenylate , Acetylate ,
PhosphorylatePhosphorylate
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DRUG TOLERANTDRUG TOLERANT
 Loss of affinity of the target biomolecule of theLoss of affinity of the target biomolecule of the
microorganismmicroorganism
 Streptomycin, Rifampin, Macrolids,Streptomycin, Rifampin, Macrolids,
Beta – lactam antibioticsBeta – lactam antibiotics
Alternate pathway of metabolismAlternate pathway of metabolism
 SulphonamidesSulphonamides
 CycloserineCycloserine
 TrimethoprimTrimethoprim
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Change in the permeability caused byChange in the permeability caused by
antibioticsantibiotics
 Tetracycline'sTetracycline's
 Beta – lactam antibioticsBeta – lactam antibiotics
 ChoramphenicolChoramphenicol
 QuinolonesQuinolones
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Genetic MechanismGenetic Mechanism
Natural ResistanceNatural Resistance
 Lack of metabolic ProcessLack of metabolic Process
 Lack of Target siteLack of Target site
e.g. Gram negative bacillie.g. Gram negative bacilli
- Unaffected by Penicillin- Unaffected by Penicillin
M. Tuberculosis - Is insensitive to TetracyclineM. Tuberculosis - Is insensitive to Tetracycline
Acquired ResistanceAcquired Resistance
 Use of an AMAs over a period of timeUse of an AMAs over a period of time
 Dependent on the - Micro organism ,Dependent on the - Micro organism ,
- Drug- Drug
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Two typesTwo types
 MutationMutation
 Stable and Heritable genetic changesStable and Heritable genetic changes
 Single StepSingle Step
e.g. Enterococci - Streptomycine.g. Enterococci - Streptomycin
E. Coli , Staphylococci – RifampinE. Coli , Staphylococci – Rifampin
 Multi StepMulti Step
Erythromycin , Tetracycline , ChloramphenicolErythromycin , Tetracycline , Chloramphenicol
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Gene transferGene transfer
 Conjugation –Conjugation –
 That gene carrying the Resistance or R factorThat gene carrying the Resistance or R factor
Gram Negative BacilliGram Negative Bacilli
Chloramphenicol - Typhoid bacilliChloramphenicol - Typhoid bacilli
Streptomycin - E . ColiStreptomycin - E . Coli
Penicillin – Haemophilus , GonococciPenicillin – Haemophilus , Gonococci
 TransductionTransduction
Penicillin's , Erythromycins , ChloramphenicolPenicillin's , Erythromycins , Chloramphenicol
 TransformationTransformation
 Passage of Naked DNAPassage of Naked DNA
 Pneumococcal – Penicillin GPneumococcal – Penicillin G
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 Cross ResistanceCross Resistance
 Resistance to One AMAs confirming resistanceResistance to One AMAs confirming resistance
to another AMAs .to another AMAs .
 Chemically or Mechanically related drugsChemically or Mechanically related drugs
Sulfonamides - All other same groupSulfonamides - All other same group
Tetracycline – ChloramphenicolTetracycline – Chloramphenicol
Erythromycin - LincomycinErythromycin - Lincomycin
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PreventionPrevention
 No inadequate , 0r Prolonged useNo inadequate , 0r Prolonged use
 Rapidly acting and selective drugsRapidly acting and selective drugs
 Broad spectrum – Specific one cannot beBroad spectrum – Specific one cannot be
determineddetermined
 Prolonged therapy – Combination therapyProlonged therapy – Combination therapy
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Beta- Lactam antibioticsBeta- Lactam antibiotics
Penicillin'sPenicillin's
 First antibiotic to be used clinically in 1941First antibiotic to be used clinically in 1941
 Penicillium notatumPenicillium notatum
 Present source – Mutant of P. chrysogenumPresent source – Mutant of P. chrysogenum
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Mechanism of actionMechanism of action
 Interfere with the synthesis of bacterial cell wallInterfere with the synthesis of bacterial cell wall
 Inhibit the transpeptidasesInhibit the transpeptidases
 Peptidoglycan cell wall is unique to bacteria.Peptidoglycan cell wall is unique to bacteria.
 Gram positive bacteria - PeptidoglycanGram positive bacteria - Peptidoglycan
 Gram negative bacteria -Lipoprotein ,Gram negative bacteria -Lipoprotein ,
Peptidoglycan.Peptidoglycan.
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 Bactericidal actionBactericidal action
Bacteria divide in the presence of aBacteria divide in the presence of a
beta – lactam antibioticbeta – lactam antibiotic
Cell wall deficient forms are producedCell wall deficient forms are produced
Normally bacterium interior is hyper osmoticNormally bacterium interior is hyper osmotic
DiffusionDiffusion
Bacterium swell and burstBacterium swell and burst
Bacterial lysisBacterial lysis
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PinicillinasePinicillinase
 Staphylococci, some strains of Gonococci , E.Coli,Staphylococci, some strains of Gonococci , E.Coli,
H. Influenzae.H. Influenzae.
 Opens the Beta- lactam ring and inactivates PnGOpens the Beta- lactam ring and inactivates PnG
Penicillin GPenicillin G
 Narrow spectrumNarrow spectrum
 Acid labileAcid labile
 t ½ - 30 mint ½ - 30 min
 Distributed extracellularlyDistributed extracellularly
 Very rapid renal excretionVery rapid renal excretion
 Tubular secretion of PnG blocked by – ProbenecidTubular secretion of PnG blocked by – Probenecid
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DoseDose
CrystallineCrystalline
PenicillinPenicillin
0.5 – 5 MU0.5 – 5 MU
i.m / i.v 6- 12 hi.m / i.v 6- 12 h
CrystapenCrystapen 0.2, 0.5,0.2, 0.5,
1 MU inj1 MU inj
ProcaineProcaine
Penicillin GPenicillin G
0.5 – 1 MU i.m0.5 – 1 MU i.m
12- 24 h12- 24 h
ProcaineProcaine
PenicillinPenicillin
G 0.5 – 1 MUG 0.5 – 1 MU
BenzathineBenzathine
PenicillinPenicillin
0.6 – 2.4 MU i.m0.6 – 2.4 MU i.m
2-4 w2-4 w
LONGACILLINLONGACILLIN
PENCOMPENCOM
0.6, 1.2, 2.4 MU0.6, 1.2, 2.4 MU
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Adverse effectsAdverse effects
 Local irritancy and Direct toxicityLocal irritancy and Direct toxicity
 Pain , Nausea, Thrombophlebitis,Pain , Nausea, Thrombophlebitis,
 HypersensitivityHypersensitivity
More commonMore common –– Rash , Itching , Urticaria, FeverRash , Itching , Urticaria, Fever
Less commonLess common –– Angioneurotic edema, Serum sickness,Angioneurotic edema, Serum sickness,
Bronchospasm, Exfoliative dermatitisBronchospasm, Exfoliative dermatitis
Rare-Rare- AnaphylaxisAnaphylaxis
More commonly seen – ParenteralMore commonly seen – Parenteral
- Procaine penicillin G- Procaine penicillin G
Scratch test, Intradermal testScratch test, Intradermal test -Performed first-Performed first
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 Super infectionsSuper infections
Bowel, respiratory, cutaneous micro flora changesBowel, respiratory, cutaneous micro flora changes
 Jarisch – Herxheimer reactionJarisch – Herxheimer reaction
 Injected in a syphilitic patientInjected in a syphilitic patient
 Shivering, fever , myalgia, exacerbation ofShivering, fever , myalgia, exacerbation of
lesionslesions
 Due to sudden release of spirochetal lyticDue to sudden release of spirochetal lytic
productsproducts
 Lasts 12- 72 hLasts 12- 72 h
 Aspirin and sedation afford relief of symptomsAspirin and sedation afford relief of symptoms
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UsesUses
 Streptococcal, Pneumococcal, MeningococcalStreptococcal, Pneumococcal, Meningococcal
 Syphilis, Gonorrhoea, DiphtheriaSyphilis, Gonorrhoea, Diphtheria
 Tetanus , Gas gangreneTetanus , Gas gangrene
 Prophylactic useProphylactic use
 Rheumatic fever – 1.2 MU every 4wRheumatic fever – 1.2 MU every 4w
till 18y of age ( or ) 5 years after antill 18y of age ( or ) 5 years after an
attackattack
 Gonorrhoea or syphilis – P.P (or ) Pn G –Gonorrhoea or syphilis – P.P (or ) Pn G –
2.4 MU single dose before or within 12 h of contact2.4 MU single dose before or within 12 h of contact
affordsaffords
 Bacterial endocarditisBacterial endocarditis
 AgranulocytosisAgranulocytosis
 Surgical infectionsSurgical infections – PP - 1MU+ Aminoglycosides– PP - 1MU+ Aminoglycosideswww.indiandentalacademy.com
Semisynthetic Penicillin'sSemisynthetic Penicillin's
 Chemically combining specific side chainsChemically combining specific side chains
 Aim –Aim –
 Overcome the shortcoming of PnGOvercome the shortcoming of PnG
 Poor oral efficacyPoor oral efficacy
 Susceptibility to PenicillinaseSusceptibility to Penicillinase
 Narrow spectrum of activityNarrow spectrum of activity
 HypersensitivityHypersensitivity
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ClassificationClassification
 Acid resistant alternative to Penicillin GAcid resistant alternative to Penicillin G
Phenoxy methyl Penicillin( Penicillin V )Phenoxy methyl Penicillin( Penicillin V )
 Penicillinase resistant Penicillin'sPenicillinase resistant Penicillin's
Methicillin , Oxacillin , Cloxacillin , NafcillinMethicillin , Oxacillin , Cloxacillin , Nafcillin
 Extended spectrum PenicillinsExtended spectrum Penicillins
Aminopenicillins – Ampicillin , amoxicillinAminopenicillins – Ampicillin , amoxicillin
Carboxy Penicillins – Carbenicillin, TicarcillinCarboxy Penicillins – Carbenicillin, Ticarcillin
UreidoPenicillins – Piperacillin , MezlocillinUreidoPenicillins – Piperacillin , Mezlocillin
Mecillinam – AmdinocillinMecillinam – Amdinocillin
 Beta- Lactamase inhibitors-Beta- Lactamase inhibitors-
Clavulonic acid , SulbactamClavulonic acid , Sulbactamwww.indiandentalacademy.com
Acid resistant alternative to Penicillin GAcid resistant alternative to Penicillin G
 Phenoxy methyl Penicillin( Penicillin V )Phenoxy methyl Penicillin( Penicillin V )
 Acid stableAcid stable
 Active against – Neisseria, Other GramActive against – Neisseria, Other Gram
negative bacteria , Anaerobes .negative bacteria , Anaerobes .
 Used in –Streptococcal Pharyngitis , Sinusitis ,Used in –Streptococcal Pharyngitis , Sinusitis ,
Otitis media, Prophylaxis of rheumatic fever ,Otitis media, Prophylaxis of rheumatic fever ,
Trench mouthTrench mouth
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Penicillinase Resistant Penicillin's (Cloxacillin)Penicillinase Resistant Penicillin's (Cloxacillin)
 Isoxazolyl side chainIsoxazolyl side chain
 Highly Penicillinase as well as acid resistantHighly Penicillinase as well as acid resistant
 t ½ - 1 ht ½ - 1 h
 Elimination primarily by KidneyElimination primarily by Kidney
Aminopenicillins –Aminopenicillins – AmpicillinAmpicillin
Active against – all microorganisms sensitive to PnG ,Active against – all microorganisms sensitive to PnG ,
and Gram negative bacilliand Gram negative bacilli
e.g.. H. Influenzae, E. coli , Proteus , Salmonella , Shigella .e.g.. H. Influenzae, E. coli , Proteus , Salmonella , Shigella .
Adverse effects – Diarrhoea , Rashes , HypersensitivityAdverse effects – Diarrhoea , Rashes , Hypersensitivity
Extended spectrum PenicillinsExtended spectrum Penicillins
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 Beta- Lactamase inhibitors-Beta- Lactamase inhibitors-
 Clavulonic acidClavulonic acid
 Streptomyces ClavuligerusStreptomyces Clavuligerus
 Inhibition increase with timeInhibition increase with time
IndicationsIndications
 Skin & Soft tissue infectionsSkin & Soft tissue infections
 Urinary ,Respiratory , Bilary tract infectionsUrinary ,Respiratory , Bilary tract infections
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NAMENAME DOSEDOSE DRUG NAMEDRUG NAME
PenicillinVPenicillinV 250- 500 mg - Adults,250- 500 mg - Adults,
125 - 250 mg - Children125 - 250 mg - Children
60 mg - Infants60 mg - Infants
CRYSTAPEN – VCRYSTAPEN – V ,,
KAYPENKAYPEN - 125, 250 mg- 125, 250 mg
TabTab
CloxacillinCloxacillin 0.25 – 0.5 gm orally every 6 h0.25 – 0.5 gm orally every 6 h
severe infections 0.25 – 1 gmsevere infections 0.25 – 1 gm
i.m / i.vi.m / i.v
KLOXKLOX 0.25,0.5 gm cap, inj0.25,0.5 gm cap, inj
BIOCLOX , CLOCILINBIOCLOX , CLOCILIN
0.25 , 0.5 gm cap0.25 , 0.5 gm cap
AmpicillinAmpicillin 250- 500 mg - Adults250- 500 mg - Adults
100 mg / ml - Children100 mg / ml - Children
AMPILIN,AMPILIN,
ROSCILLIN,ROSCILLIN,
BIOCILLINBIOCILLIN
250, 500 mg Cap250, 500 mg Cap
AmoxicillinAmoxicillin 0.25 – 1 gm TDS oral0.25 – 1 gm TDS oral
AMOXIL , MOXAMOXIL , MOX
250, 500 mg cap250, 500 mg cap
AMOXYLIN ,AMOXYLIN ,
NOVAMOX,NOVAMOX,
SYNAMOXSYNAMOX 250, 500 mg250, 500 mg
cap .cap .
125 mg /5ml dry syrup125 mg /5ml dry syrup
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CarbenicillinCarbenicillin 1 gm ,5gm i. v1 gm ,5gm i. v CARBBLINCARBBLIN
1gm, 5gm inj1gm, 5gm inj
PiperacillinPiperacillin PIPRAPENPIPRAPEN 1gm, 2gm1gm, 2gm
PIPRACILPIPRACIL 2gm , 4gm2gm , 4gm
vials for injvials for inj
Clavulonic acidClavulonic acid AUGMENTIN ,AUGMENTIN ,
ENHANCIN,ENHANCIN,
AMONATEAMONATE ,,
Amoxicillin 250 mg +Amoxicillin 250 mg +
Clavulonic acid 125 mgClavulonic acid 125 mg
TDSTDS
severe infections – 6 hsevere infections – 6 h
SulbactamSulbactam Ampicillin 1 gmAmpicillin 1 gm
+Sulbactam 0.5 gm per+Sulbactam 0.5 gm per
vial inj 6-8 hvial inj 6-8 h
SULBACINSULBACIN
AMPITUMAMPITUM
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CEPHALOSPORINSCEPHALOSPORINS
 Cephalosporium – Fungus ,Bactericidal .Cephalosporium – Fungus ,Bactericidal .
 Chronological sequences of developmentChronological sequences of development
ParenteralParenteral
CephalothinCephalothin
CefazolinCefazolin
CephaloridineCephaloridine
OralOral
CephalexinCephalexin
CefadroxilCefadroxil
ParenteralParenteral
CefuroximeCefuroxime
CefoxitinCefoxitin
OralOral
CefaclorCefaclor
CefuroximeCefuroxime
ParenteralParenteral
CefotaximeCefotaxime
CeftriaxoneCeftriaxone
CefoperazoneCefoperazone
OralOral
CefiximeCefixime
ParenteralParenteral
CefepimeCefepime
CefpiromeCefpirome
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CephalexinCephalexin 0.25 – 1 gm 6-8 h Adult0.25 – 1 gm 6-8 h Adult
ChildrenChildren
25 – 100 mg / kg / day25 – 100 mg / kg / day
SPORIDEX, ALCEPHIN,SPORIDEX, ALCEPHIN,
CEPHAXIN ,CEPHAXIN ,
250- 500 mg Cap250- 500 mg Cap
CefadroxilCefadroxil DROXYL-DROXYL- 0.5 ,1 gm tab0.5 ,1 gm tab
CEFADROXCEFADROX 0.5 mg Cap0.5 mg Cap
KEFLOXINKEFLOXIN 0.5 mg Cap0.5 mg Cap
250 mg kid tab250 mg kid tab
BDBD
CefotaximeCefotaxime 1-2 gm i.m /iv 6-12h1-2 gm i.m /iv 6-12h
Children 50 -100Children 50 -100
mg/kg/daymg/kg/day
CLAFORANCLAFORAN
0.25 &1 gm /vial inj0.25 &1 gm /vial inj
CefazolinCefazolin Mild cases – 0.25 gm 8hMild cases – 0.25 gm 8h
Severe cases – 1 gm 6hSevere cases – 1 gm 6h
i/m ,i/vi/m ,i/v
ALCIZONALCIZON
ORIZOLINORIZOLIN
0.25,0.5 gm per vial inj0.25,0.5 gm per vial inj
CeftazidimeCeftazidime FORTUM , CEFAZIDFORTUM , CEFAZID
0.25,0.5,1 gm per vial inj0.25,0.5,1 gm per vial inj
every 8hevery 8h
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 Adverse effectsAdverse effects
 Pain - CephalothinPain - Cephalothin
 Diarrhoea- OralDiarrhoea- Oral
 Hypersensitivity reactions – Coomb’s testHypersensitivity reactions – Coomb’s test
 Nephro toxicity – Cephalothin,Nephro toxicity – Cephalothin,
CephaloridineCephaloridine
 Bleeding - Ceftriaxone , CefoperazoneBleeding - Ceftriaxone , Cefoperazone
 Neutropenia - CeftazidimeNeutropenia - Ceftazidime
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Tetracycline'sTetracycline's
 Broad-spectrum antibioticsBroad-spectrum antibiotics
 Obtained from ActinomycetesObtained from Actinomycetes
 First – Chlortetracycline – In 1948 - AureomycinFirst – Chlortetracycline – In 1948 - Aureomycin
Group I Group II Group IIIGroup I Group II Group III
ChlortetracyclineChlortetracycline DemoclocyclineDemoclocycline DoxycyclineDoxycycline
OxytetracyclineOxytetracycline MethacyclineMethacycline MinocyclineMinocycline
TetracyclineTetracycline LymecyclineLymecycline
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 BacteriostaticBacteriostatic
 Inhibits protein synthesis by binding to 30 SInhibits protein synthesis by binding to 30 S
Ribosome's in susceptible organismRibosome's in susceptible organism
 Inhibited – All typesInhibited – All types
 Except – Fungi , VirusesExcept – Fungi , Viruses
 Absorbed from G.I.TAbsorbed from G.I.T
 Chelating Property - Calcium , Some metalsChelating Property - Calcium , Some metals
 Milk , Iron Preparations, Nonsystemic AntacidsMilk , Iron Preparations, Nonsystemic Antacids
Sucralfate .Sucralfate .
 Secreted in milkSecreted in milk
 Oral administration – Should be taken ½ beforeOral administration – Should be taken ½ before
(or ) 2 h after food .(or ) 2 h after food .
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ChlorChlor
tetracyclinetetracycline
AureomycinAureomycin 250 , 500 mg Cap250 , 500 mg Cap
OxyOxy
tetracyclinetetracycline
Terramycin -Terramycin -
Oxysteclin -Oxysteclin -
3% Skin ,1% eye3% Skin ,1% eye
ointmentointment
250 , 500 mg Cap250 , 500 mg Cap
50 mg /ml inj in 2 ml amp50 mg /ml inj in 2 ml amp
and 20 ml vialand 20 ml vial
TetracyclineTetracycline AchromycinAchromycin
HostacyclinHostacyclin
250 , 500 mg Cap250 , 500 mg Cap
100mg vial for i.m100mg vial for i.m
250-500 mg vial for i. v250-500 mg vial for i. v
DoxycyclineDoxycycline Tetradox,Biodoxi,Tetradox,Biodoxi,
Duracyclin , DoxyDuracyclin , Doxy
Cap 100 mg capCap 100 mg cap
2cap 12cap 1stst
day, 1cap 2day, 1cap 2ndnd
dayday
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IndicationsIndications
 Aggressive PeriodontitisAggressive Periodontitis
 Refractory Periodontitis.Refractory Periodontitis.
 Debridement and even surgery have failed-Debridement and even surgery have failed-
Indicating that chemotherapyIndicating that chemotherapy
Contraindications:Contraindications:
• Permanent discoloration of teeth.Permanent discoloration of teeth.
• Pregnancy and lactation.Pregnancy and lactation.
• Oral contraceptives - less effective.Oral contraceptives - less effective.
• Depress serum prothrombin activityDepress serum prothrombin activity
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Adverse effectAdverse effect
Irritative effectIrritative effect – Epigastric pain ,Nausea– Epigastric pain ,Nausea
Vomiting , Diarrhoea, esophageal UlcerationVomiting , Diarrhoea, esophageal Ulceration
Liver damageLiver damage --
Safer – Tetracycline , OxytetracyclineSafer – Tetracycline , Oxytetracycline
Tetracycline – Acute hepatic necrosis –Tetracycline – Acute hepatic necrosis –
Pregnant womenPregnant women
Kidney damageKidney damage - except Doxycycline- except Doxycycline
Photo toxicityPhoto toxicity -Doxycycline ,Democlocycline-Doxycycline ,Democlocycline
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 Teeth and BoneTeeth and Bone
 Calcium – Tetracycline Chelate DepositionCalcium – Tetracycline Chelate Deposition
 Brown discoloration ill formed teethBrown discoloration ill formed teeth
 Mid pregnancy to 5 months – Deciduous teethMid pregnancy to 5 months – Deciduous teeth
 5 months to 5 years - Permanent anterior teeth5 months to 5 years - Permanent anterior teeth
 More susceptible to cariesMore susceptible to caries
 Temporary suppression of bone growthTemporary suppression of bone growth
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 HypersensitivityHypersensitivity
 Vestibular toxicityVestibular toxicity
 Super infectionSuper infection
 Diabetes insipidus –Diabetes insipidus –
 Democlocycline antagonizes A.D.H actionDemoclocycline antagonizes A.D.H action
 Ant anabolic effect – Reduce ProteinAnt anabolic effect – Reduce Protein
SynthesisSynthesis
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METRONIDAZOLE:
 Nitroimidazole compound.
 Bactericidal to anaerobic organisms
( P . Gingivalis , P. Intermedia ).
 cytotoxic metabolites of metronidazole directly
interact with bacterial DNA - cell death.
Clinical UseClinical Use
 Gingivitis, ANUG, Chronic Periodontitis, AggressiveGingivitis, ANUG, Chronic Periodontitis, Aggressive
Periodontitis, and Refractory Periodontitis.Periodontitis, and Refractory Periodontitis.
 Not the drug of choice to treat A.actinomycetemNot the drug of choice to treat A.actinomycetem
comitans infections. Effective when used incomitans infections. Effective when used in
combination with other antibiotics.combination with other antibiotics.
 A single dose of metronidazole (A single dose of metronidazole (250 mg orally250 mg orally))
appears in both serum and gingival fluid in sufficientappears in both serum and gingival fluid in sufficient
quantity to inhibit periodontal pathogens.quantity to inhibit periodontal pathogens.
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 SSynergistically with amoxicillinynergistically with amoxicillin
 Useful in many mixed periodontal infections.Useful in many mixed periodontal infections.
 Commonly prescribed regimen isCommonly prescribed regimen is 250 mg t.i.d for 7250 mg t.i.d for 7
days.days.
Contraindications:Contraindications:
• An ant abuse effectAn ant abuse effect
• Alcohol ingestion, since abdominal distress, nausea,Alcohol ingestion, since abdominal distress, nausea,
vomiting and / or headache may occurvomiting and / or headache may occur
• TumorigenicityTumorigenicity
• Pregnant women and nursing mothersPregnant women and nursing mothers
• An anti-abuse drugAn anti-abuse drug
• Patients receiving anticoagulants, lithium or disulfuranPatients receiving anticoagulants, lithium or disulfuran
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MacrolidsMacrolids
 ErythromycinErythromycin
 Isolated from Streptomyces erythreus in 1952Isolated from Streptomyces erythreus in 1952
 Bacteriostatic at low concentrationsBacteriostatic at low concentrations
 Bactericidal at high concentrationsBactericidal at high concentrations
 Acts by inhibiting bacterial protein synthesis .Acts by inhibiting bacterial protein synthesis .
 Highly active againstHighly active against
–– Streptococcus pyogensStreptococcus pyogens
- Streptococcus Pnuemoniae- Streptococcus Pnuemoniae
- Clostridia , N. gonorrhoeae- Clostridia , N. gonorrhoeae
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PharmacokineticsPharmacokinetics
 Acid labileAcid labile
 Enteric coated tabletsEnteric coated tablets
 Crosses Placenta , but not blood – brain barrierCrosses Placenta , but not blood – brain barrier
 Plasma t ½ - 1.5 hPlasma t ½ - 1.5 h
 Excreted primarily - in the Bile in the activeExcreted primarily - in the Bile in the active
formform
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ErythromycinErythromycin 250-500mg 6h250-500mg 6h
Max 8gm/ dayMax 8gm/ day
Children 30-Children 30-
60mg/kg/day60mg/kg/day
ERYSAFEERYSAFE
125,250,500 mg tab125,250,500 mg tab
EROMEDEROMED 333mg333mg
E. StearateE. Stearate ERYTHROCINERYTHROCIN 100,250,500mg tab100,250,500mg tab
E. EstolateE. Estolate
(Acid stable )(Acid stable )
ALTHROCINALTHROCIN 250,500mg tab250,500mg tab
100mg /ml100mg /ml
Pedo dropsPedo drops
E. EthylE. Ethyl
SuccinateSuccinate
ERYNATEERYNATE
ERYTHROCINERYTHROCIN
100mg /5ml dry syr100mg /5ml dry syr
100mg /ml drops100mg /ml drops
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Adverse effectsAdverse effects
 Remarkably safe drugRemarkably safe drug
 Gastro intestinalGastro intestinal
 Epigastric pain , DiarrhoeaEpigastric pain , Diarrhoea
 HypersensitivityHypersensitivity
USESUSES
 Alternative to penicillin in allergic patientsAlternative to penicillin in allergic patients
 First choice drug forFirst choice drug for
 Atypical pneumonia - 3 w treatmentAtypical pneumonia - 3 w treatment
 Whooping cough - 2w TreatmentWhooping cough - 2w Treatment
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Newer MacrolidsNewer Macrolids
 Overcome the limitations of erythromycinsOvercome the limitations of erythromycins
 Narrow spectrum gastric intoleranceNarrow spectrum gastric intolerance
 Gastric acid LiabilityGastric acid Liability
 Low oral bioavailabilityLow oral bioavailability
 Poor tissue penetrationPoor tissue penetration
 Short half lifeShort half life
 Semi synthetic MacrolidsSemi synthetic Macrolids
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RoxithroRoxithro
mycinmycin
t ½t ½
-12h-12h
15 mg BD 30 min15 mg BD 30 min
before mealsbefore meals
ChildrenChildren
2.5 -5 mg /kg BD2.5 -5 mg /kg BD
ROXID,ROXID,
ROXEM,ROXEM,
ROXIBIDROXIBID
150 mg tab150 mg tab
ClarithroClarithro
mycinmycin
3-6 h3-6 h 250mg BD for 7days250mg BD for 7days
Severe cases 500mgSevere cases 500mg
BDBD
up to 14 daysup to 14 days
CLARBIDCLARBID
CELEXCELEX
250 ,500mg250 ,500mg
tabtab
AZITHROAZITHRO
MYCINMYCIN
>50h>50h ZITHROMACZITHROMAC
AZITHRALAZITHRAL
AZIWOKAZIWOK
250 mg cap250 mg cap
250mg cap250mg cap
250mg cap250mg cap
100 mg KID tab100 mg KID tab
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FluoroquinolonesFluoroquinolones
Primarily against gram negative bacteriaPrimarily against gram negative bacteria
First generation second generationFirst generation second generation
Norfloxacin LomefloxacinNorfloxacin Lomefloxacin
Ciprofloxacin SparfloxacinCiprofloxacin Sparfloxacin
Ofloxacin FleroxacinOfloxacin Fleroxacin
Pefloxacin AmifloxacinPefloxacin Amifloxacin
 Inhibits the enzyme bacterial DNA gyraseInhibits the enzyme bacterial DNA gyrase
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CIPROFLOXACINCIPROFLOXACIN
 Most susceptible toMost susceptible to
Aerobic gram negative bacilliAerobic gram negative bacilli
Enterobacteriaceae , NeisseriaEnterobacteriaceae , Neisseria
 Rapidly absorbed OrallyRapidly absorbed Orally
 High tissue penitrationHigh tissue penitration
 Excreted primarily in urineExcreted primarily in urine
 t ½ 35 ht ½ 35 h
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 CIFRANCIFRAN 250 , 500 , 750 mg tab250 , 500 , 750 mg tab
 CIPLOXCIPLOX 250 , 500 , 750 mg tab250 , 500 , 750 mg tab
200 mg / 100 ml i/v infusion200 mg / 100 ml i/v infusion
 CIPROFLOX , QUINTORCIPROFLOX , QUINTOR
250 , 500 mg tab250 , 500 mg tab
 CIPROBIDCIPROBID 250 , 500 , 750 mg tab250 , 500 , 750 mg tab
3mg /ml eye drops3mg /ml eye drops
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 Wide spectrum bactericidal activityWide spectrum bactericidal activity
 UTIUTI
 GonorrheaGonorrhea
 Typhoid 500-750 mg BD for 10 daysTyphoid 500-750 mg BD for 10 days
 Bone , Soft tissue wound infections along withBone , Soft tissue wound infections along with
metronidazolemetronidazole
 MeningitisMeningitis
OFLOXACINOFLOXACIN
 More potent than ciprofloxacin for gram positiveMore potent than ciprofloxacin for gram positive
organismsorganisms
 ZANOCIN , TARIVIDZANOCIN , TARIVID -- 100, 200 mg tab100, 200 mg tab
200mg / 100ml i.v infusion200mg / 100ml i.v infusion
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ClindamycinClindamycin
 BacteriostaticBacteriostatic
 Inhibits bacterial protein synthesis, by bindingInhibits bacterial protein synthesis, by binding
irreversibly to 50S ribosomal subunit.irreversibly to 50S ribosomal subunit.
 Active against - gram-positive bacteria,Active against - gram-positive bacteria,
( both facultative and anaerobic species. )( both facultative and anaerobic species. )
gram negative anaerobes.gram negative anaerobes.
 Inherently resistant to - Eikenella corrodens,Inherently resistant to - Eikenella corrodens,
- A. actinomycetemcomitans- A. actinomycetemcomitans
 Effective in - Allergic to penicillin.Effective in - Allergic to penicillin.
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 Refractory patients.- 150 mg q.i.d for 10 days.Refractory patients.- 150 mg q.i.d for 10 days.
300 mg twice daily for 8 days.300 mg twice daily for 8 days.
 Efficacy in - Periodontitis refractory toEfficacy in - Periodontitis refractory to
tetracycline therapy.tetracycline therapy.
Side EffectsSide Effects
 Pseudo membranous colitisPseudo membranous colitis
 Watery diarrhea, fever, leucocytosis and crampyWatery diarrhea, fever, leucocytosis and crampy
abdominal pain beginning on 4abdominal pain beginning on 4thth
to 9to 9thth
day ofday of
antibiotic therapy suggestive ofantibiotic therapy suggestive of
Pseudo membranous colitis.Pseudo membranous colitis.
 EnterotoxinEnterotoxin
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Local delivery of antibioticsLocal delivery of antibiotics
 Targeting an antimicrobial to infection sites andTargeting an antimicrobial to infection sites and
sustaining its localized concentration at effectivesustaining its localized concentration at effective
levels for a sufficient time .levels for a sufficient time .
 Minimal or no side effects.Minimal or no side effects.
 Antibiotic concentrations are releasedAntibiotic concentrations are released
continuously.continuously.
 Recent advances - Resulted in the controlledRecent advances - Resulted in the controlled
Release of drugs.Release of drugs.
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 Local subgingival delivery devices (antibiotic) for up to 24 hoursLocal subgingival delivery devices (antibiotic) for up to 24 hours
 Active ingredients are incorporated into an agent (fibers, gels,Active ingredients are incorporated into an agent (fibers, gels,
chips, collagen film, acrylic strips, and a polymer). The activechips, collagen film, acrylic strips, and a polymer). The active
ingredient is then released over a period of daysingredient is then released over a period of days
Aims at three targets:Aims at three targets:
 Support of non-surgical mechanical anti-infective therapy.Support of non-surgical mechanical anti-infective therapy.
 Support of re-instrumentation during supportive periodontalSupport of re-instrumentation during supportive periodontal
therapy.therapy.
 As alternative to subgingival re-instrumentation duringAs alternative to subgingival re-instrumentation during
supportive periodontal therapy.supportive periodontal therapy.
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 Goodson and co workers (1979). – first to testGoodson and co workers (1979). – first to test
 Using Permeable hollow Cellulose Acetate fibers filledUsing Permeable hollow Cellulose Acetate fibers filled
with 20%solution of tetracycline.with 20%solution of tetracycline.
Tetracycline-Containing FibersTetracycline-Containing Fibers (Actisite)(Actisite)
 Ethylene/vinyl acetate copolymer fiber, diameterEthylene/vinyl acetate copolymer fiber, diameter
0.5 mm, containing tetracycline, 12.7 mg/9 inches.0.5 mm, containing tetracycline, 12.7 mg/9 inches.
 Sustains tetracycline concentrations for 10 daysSustains tetracycline concentrations for 10 days
exceeding 1300 µg/ml.exceeding 1300 µg/ml.
 Well beyond the 32 to 64 µg/ml required to inhibit theWell beyond the 32 to 64 µg/ml required to inhibit the
growth of Periodontal Pathogens.growth of Periodontal Pathogens.
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Placement of ActisitePlacement of Actisite
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Disadvantages of the fiberDisadvantages of the fiber
 The length of time required for placementThe length of time required for placement
(10 minutes or more per tooth).(10 minutes or more per tooth).
 The considerable learning curve required to gainThe considerable learning curve required to gain
proficiency at placement.proficiency at placement.
 The need for a second patient appointment 10The need for a second patient appointment 10
days after placement for removal of the fiber.days after placement for removal of the fiber.
 Also, placement of fibers around 12 or moreAlso, placement of fibers around 12 or more
teeth has resulted in oral candidiasis in a fewteeth has resulted in oral candidiasis in a few
cases.cases.
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Subgingival Delivery of DoxycyclineSubgingival Delivery of Doxycycline::
(Atridox)(Atridox)
 Doxycycline (10%) - Syringeable gel system.Doxycycline (10%) - Syringeable gel system.
 Controlled-release product.Controlled-release product.
 Two-syringe mixing system.Two-syringe mixing system.
 Stored at 2°– 8°CStored at 2°– 8°C
 Syringe A - 450 mg of the Atrigel Delivery System,Syringe A - 450 mg of the Atrigel Delivery System,
(36.7% poly actide dissolved in 63.3% N methyl-2-pyrrolidone)(36.7% poly actide dissolved in 63.3% N methyl-2-pyrrolidone)
 Syringe B - Doxycycline hyclate equivalent to 42.5 mg ofSyringe B - Doxycycline hyclate equivalent to 42.5 mg of
Doxycycline. .Doxycycline. .
 Upon contact with crevicular fluid it solidifiesUpon contact with crevicular fluid it solidifies
 Allowing drug release for seven days.Allowing drug release for seven days.
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Subgingival Delivery System of MinocyclineSubgingival Delivery System of Minocycline
(Arestin):(Arestin):
 2% Minocycline Hydrochloride.2% Minocycline Hydrochloride.
 Syringeable gel suspension formulation.Syringeable gel suspension formulation.
 Arestin “microspheres” (minocycline HCL 1mg)Arestin “microspheres” (minocycline HCL 1mg)
 Availability - Box with 2 trays, each containing 12 cartridges.Availability - Box with 2 trays, each containing 12 cartridges.
 Each cartridge contains 1 mg of minocycline microencapsulatedEach cartridge contains 1 mg of minocycline microencapsulated
in 3 mg of poly (glycolide-lactide) dry powder.in 3 mg of poly (glycolide-lactide) dry powder.
 Cartridge is inserted into an autoclavable cartridge handle toCartridge is inserted into an autoclavable cartridge handle to
administer.administer.
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Subgingival Delivery of Metronidazole:Subgingival Delivery of Metronidazole:
 Oil-based metronidazole 25% dental gelOil-based metronidazole 25% dental gel
 It is liquidized by the body heat and thenIt is liquidized by the body heat and then
hardens again forming crystals in contacthardens again forming crystals in contact
with water.with water.
 Two 25% gel applications at a 1-weekTwo 25% gel applications at a 1-week
interval have been used in cinterval have been used in c
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Combination antibiotic therapyCombination antibiotic therapy
 Oral infections is a ‘mixed’ infections.Oral infections is a ‘mixed’ infections.
 no single antibiotic is effective against all pathogens.no single antibiotic is effective against all pathogens.
 use more than one antibiotic, either serially or in combination.use more than one antibiotic, either serially or in combination.
 when Bacteriostatic and bactericidal antibiotic drugs are requiredwhen Bacteriostatic and bactericidal antibiotic drugs are required
they are best given serially, not in combination.they are best given serially, not in combination.
 Combination therapy:Combination therapy:
 Should exhibit synergy or additive effects in vitro.Should exhibit synergy or additive effects in vitro.
 E.g., Metronidazole-amoxicillin,E.g., Metronidazole-amoxicillin,
 metronidazole-Augmentinmetronidazole-Augmentin
 metronidazole-ciprofloxacin.metronidazole-ciprofloxacin.
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 IndicationsIndications
 Oral infections involving variety of pathogenicOral infections involving variety of pathogenic
species with differing antimicrobialspecies with differing antimicrobial
susceptibility.susceptibility.
 To overcome the drug-protective effectsTo overcome the drug-protective effects
 Development of resistant strains.Development of resistant strains.
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Common Antibiotic Therapies
AntibioticAntibiotic Adult dosageAdult dosage
MetronidazoleMetronidazole 500 mg/t.i.d/8 days500 mg/t.i.d/8 days
ClindamycinClindamycin 300 mg/t.i.d/8 days300 mg/t.i.d/8 days
Doxycycline or MinocyclineDoxycycline or Minocycline 100-200 mg/q.d/7 days100-200 mg/q.d/7 days
CiprofloxacinCiprofloxacin 500 mg/b.i.d/8 days500 mg/b.i.d/8 days
AzithromycinAzithromycin 500 mg q.d/4-7 days500 mg q.d/4-7 days
Metronidazole +AmoxicillinMetronidazole +Amoxicillin 250 mg/t.i.d/8 days each drug250 mg/t.i.d/8 days each drug
Metronidazole + CiprofloxacinMetronidazole + Ciprofloxacin 500 mg/b.i.d/8 days each drug500 mg/b.i.d/8 days each drug
www.indiandentalacademy.com
ConclusionConclusion
 Although over 300 species of bacteria areAlthough over 300 species of bacteria are
currently recognized in the oral cavity.currently recognized in the oral cavity.
 There is evidence that suppression orThere is evidence that suppression or
eradication of these organisms results ineradication of these organisms results in
an improvement in oral health and evenan improvement in oral health and even
perhaps systemic health.perhaps systemic health.
www.indiandentalacademy.com

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Antibiotics in Dentistry: Classification, Properties and Uses

  • 1. ANTIBIOTICSANTIBIOTICS IN DENTISTRYIN DENTISTRY  INDIAN DENTAL ACADEMYINDIAN DENTAL ACADEMY  Leader in continuing Dental EducationLeader in continuing Dental Education www.indiandentalacademy.com
  • 2. CONTENTSCONTENTS IntroductionIntroduction DefinitionDefinition HistoryHistory ClassificationClassification PropertiesProperties AntibioticsAntibiotics Combination antibiotic therapyCombination antibiotic therapy Local delivery of antibioticsLocal delivery of antibiotics ConclusionConclusion www.indiandentalacademy.com
  • 3.  Pulpal and Periapical PathogensPulpal and Periapical Pathogens –– V G SV G S ,, Beta – hemolytic streptococci, ProvetellaBeta – hemolytic streptococci, Provetella Fusobacteria, Actinomyces, Porphyromonas gingivalisFusobacteria, Actinomyces, Porphyromonas gingivalis Candida albicans ,Staphylococcus, Entero coccus.Candida albicans ,Staphylococcus, Entero coccus.  Periodontal Diseases -Periodontal Diseases - Porphyromonas gingivalis,Porphyromonas gingivalis, Provetella, FusobacteriaProvetella, Fusobacteria ,, Actinobacillus actinomycetemcomitansActinobacillus actinomycetemcomitans,, Campylobacter , Trepanoma Denticola , Bacteroids .Campylobacter , Trepanoma Denticola , Bacteroids . www.indiandentalacademy.com
  • 4. www.indiandentalacademy.com Indian Dental academy • www.indiandentalacademy.com • Leader continuing dental education • Offer both online and offline dental courses
  • 5.  Acute necrotizing ulcerative gingivitis –Acute necrotizing ulcerative gingivitis – Treponema, FusobacteriaTreponema, Fusobacteria ,, Provetella, Veillonella ,Provetella, Veillonella , Neisseria , Bacteroids , Actinomyces, CapnocytophagaNeisseria , Bacteroids , Actinomyces, Capnocytophaga ..  Pericoronitis –Pericoronitis – V G S , Actinomyces israeliiV G S , Actinomyces israelii ,, Provetella, Neisseria ,Provetella, Neisseria , Bacteroids , Actinomyces, Capnocytophaga ,Bacteroids , Actinomyces, Capnocytophaga , Staphylococci, Lactobacilli, Fusobacteria ,Staphylococci, Lactobacilli, Fusobacteria , Porphyromonas .Porphyromonas . www.indiandentalacademy.com
  • 6.  Periimplantitis -Periimplantitis - Bacteroids , FusobacteriaBacteroids , Fusobacteria ,, PorphyromonasPorphyromonas gingivalis, Provetella, Campylobacter ,gingivalis, Provetella, Campylobacter , Trepanoma, V G S , Actinomyces.Trepanoma, V G S , Actinomyces.  Osteomyelitis –Osteomyelitis – Staphylococcus aureusStaphylococcus aureus ,, VGS , Actinomyces, Fusobacteria , Provetella,VGS , Actinomyces, Fusobacteria , Provetella, Eubacterium , Eikenella.Eubacterium , Eikenella. www.indiandentalacademy.com
  • 7.  Ludwig’s angina –Ludwig’s angina – VGS ,VGS , Staphylococci , Porphyromonas gingivalis, Provetella,Staphylococci , Porphyromonas gingivalis, Provetella, Pseudomonas aeruginosa , Klebsiella Haemophilus .Pseudomonas aeruginosa , Klebsiella Haemophilus .  Mediastinal infections –Mediastinal infections – VGS ,VGS , PorphyromonasPorphyromonas, Provetella, Fusobacteria ,, Provetella, Fusobacteria , Staphylococci .Staphylococci . www.indiandentalacademy.com
  • 8. DEFINITIONDEFINITION  AntibioticAntibiotic -- Are substances produced by various speciesAre substances produced by various species of microorganisms (bacterial, fungi, andof microorganisms (bacterial, fungi, and actinomycetes) that suppress the growth ofactinomycetes) that suppress the growth of or kill other microorganisms at very lowor kill other microorganisms at very low concentrationconcentrations.s. www.indiandentalacademy.com
  • 9.  Antimicrobial agentAntimicrobial agent -- Synthetic as well as a naturally obtained drug thatSynthetic as well as a naturally obtained drug that attenuate the microorganisms.attenuate the microorganisms. They inhibit or kill the infecting organisms andThey inhibit or kill the infecting organisms and has no or minimal effect on the recipienthas no or minimal effect on the recipient.. DEFINITIONDEFINITION www.indiandentalacademy.com
  • 10.  ChemotherapyChemotherapy –– Treatment of systemic infections with specificTreatment of systemic infections with specific drugs that selectively suppress the infectingdrugs that selectively suppress the infecting microorganisms without significantly affectingmicroorganisms without significantly affecting the host .the host . Treatment of neoplastic diseases with drugs isTreatment of neoplastic diseases with drugs is also called Chemotherapy.also called Chemotherapy. www.indiandentalacademy.com
  • 11. HISTORYHISTORY Three phasesThree phases Period of empirical phasePeriod of empirical phase :: E.g.E.g. Chaulmoogra oil - LeprosyChaulmoogra oil - Leprosy Mouldy curd - BoilsMouldy curd - Boils Mercury - SyphilisMercury - Syphilis Cinchona bark – FeverCinchona bark – Fever www.indiandentalacademy.com
  • 12.  Ehrlich’s phase : (1890-1935)Ehrlich’s phase : (1890-1935)  Selectively stain microbes-Selectively stain microbes- DyesDyes(methylene blue)(methylene blue)  Selectively toxic to the organisms .Selectively toxic to the organisms .  Arsenicals-atoxyl - Sleeping sickness (1906)Arsenicals-atoxyl - Sleeping sickness (1906) Norarsephenamine -Norarsephenamine - Syphilis ( 1909)Syphilis ( 1909)  He coined the termHe coined the term ‘chemotherapy’‘chemotherapy’  ‘‘Father of modern chemotherapyFather of modern chemotherapy’’  Awarded theAwarded the Nobel Prize in 1909.Nobel Prize in 1909. www.indiandentalacademy.com
  • 13.  Pasteur (1877) Antibiosis Growth of Anthrax Bacilli in urine was inhibited by air born bacteria www.indiandentalacademy.com
  • 14.  The modern era of chemotherapy.  Domagk (1935) Therapeutic effect of Prontosil, Sulfonamide dye, in pyogenic infection. The active moiety was Para-amino benzene sulfonamide, and the dye part was not essential. www.indiandentalacademy.com
  • 15.  Sir Alexander Fleming (1929)Sir Alexander Fleming (1929)  Culture plates contaminated by aCulture plates contaminated by a fungusfungus (Penicillium notatum)(Penicillium notatum)  Prevented the growth ofPrevented the growth of surrounding bacterial colonies.surrounding bacterial colonies.  The fungal filtrate, which he namedThe fungal filtrate, which he named PenicillinPenicillin  FloreyFlorey and Chain (1941)and Chain (1941)  Purified this fungal growth andPurified this fungal growth and clinically used for treating theclinically used for treating the wounds and diseases.wounds and diseases. www.indiandentalacademy.com
  • 16. ClassificationClassification  Based on mechanism of action.Based on mechanism of action. Inhibits cell wall synthesisInhibits cell wall synthesis E.g. Penicillin's, Cephalosporin's, Vancomycin ,E.g. Penicillin's, Cephalosporin's, Vancomycin , Bacitracin.Bacitracin. Act on the cell wall membraneAct on the cell wall membrane E.g. Nystatin and Amphotericin - BE.g. Nystatin and Amphotericin - B.. Affect the function of 30s and 50s RibosomalAffect the function of 30s and 50s Ribosomal subunitssubunits E.g.E.g. Chloramphenicol, Tetracycline's andChloramphenicol, Tetracycline's and Clindamycin, Erythromycin.Clindamycin, Erythromycin. www.indiandentalacademy.com
  • 17. Misreading of m- RNA codeMisreading of m- RNA code E.g. AminoglycosidesE.g. Aminoglycosides Inhibit DNA gyraseInhibit DNA gyrase E.g. FluroquinolonesE.g. Fluroquinolones Interfere with DNA functionInterfere with DNA function E.g. Rifampin , MetronidazoleE.g. Rifampin , Metronidazole Interfere with DNA synthesisInterfere with DNA synthesis E.g.E.g. Idoxuridine , Acyclovir , ZidovudineIdoxuridine , Acyclovir , Zidovudine Interfere with intermediary metabolismInterfere with intermediary metabolism E.g. Sulfonamides, Trimethoprim , EthambutolE.g. Sulfonamides, Trimethoprim , Ethambutolwww.indiandentalacademy.com
  • 18. Based on Type of action:Based on Type of action: Bacteriostatic antibioticsBacteriostatic antibiotics –– Inhibits the growth and multiplicationInhibits the growth and multiplication e.g.e.g. Sulfonamides,Sulfonamides, Chloramphenicol, Tetracycline'sChloramphenicol, Tetracycline's and Erythromycinand Erythromycin Bactericidal antibioticsBactericidal antibiotics –– kill micro-organisms by interfering with the synthesis orkill micro-organisms by interfering with the synthesis or function of either the cell wall, cell membrane or both.function of either the cell wall, cell membrane or both. e.g.e.g. Penicillin's, cephalosporins, VancomycinPenicillin's, cephalosporins, Vancomycin Aminoglycosides, Rifampin .Aminoglycosides, Rifampin . www.indiandentalacademy.com
  • 19. Based on Spectrum of activityBased on Spectrum of activity Narrow spectrum.Narrow spectrum. Penicillins, Erythromycin, Streptomycin.Penicillins, Erythromycin, Streptomycin. Broad spectrum.Broad spectrum. Tetracycline's , ChloramphenicolTetracycline's , Chloramphenicol www.indiandentalacademy.com
  • 20.  Based on chemical structureBased on chemical structure Beta – lactam antibioticsBeta – lactam antibiotics Penicillins, Cephalosporins, MonobactemsPenicillins, Cephalosporins, Monobactems .. QuinolonesQuinolones Nalidixic acid, Norfloxacin, CiprofloxacinNalidixic acid, Norfloxacin, Ciprofloxacin Tetracycline'sTetracycline's Oxytetracycline, DoxycyclineOxytetracycline, Doxycycline SulfonamidesSulfonamides Sulfadiazine, Sulfones – DapsonesSulfadiazine, Sulfones – Dapsones www.indiandentalacademy.com
  • 21. AminoglycosidesAminoglycosides Streptomycin, Gentamicin, NeomycinStreptomycin, Gentamicin, Neomycin Nitrobenzene derivativesNitrobenzene derivatives ChloramphenicolChloramphenicol DiaminopyrimidinesDiaminopyrimidines Trimethoprim, PyrimethamineTrimethoprim, Pyrimethamine Macrolide antibioticsMacrolide antibiotics Erythromycin, Roxithromycin, AzithromycinErythromycin, Roxithromycin, Azithromycin NitroimidazolesNitroimidazoles Metronidazole, TinidazoleMetronidazole, Tinidazole www.indiandentalacademy.com
  • 22. Polyene antibioticsPolyene antibiotics Nystatin, Amphotericine – B .Nystatin, Amphotericine – B . Nicotinic acid derivativesNicotinic acid derivatives Isoniazid, Pyrazinamide, EthionamideIsoniazid, Pyrazinamide, Ethionamide Polypeptide antibioticsPolypeptide antibiotics Polymyxin – B , Colistin , BacitracinPolymyxin – B , Colistin , Bacitracin Imidazole derivativesImidazole derivatives Miconazole, Clotrimazole, Ketoconazole, FluconazoleMiconazole, Clotrimazole, Ketoconazole, Fluconazole OthersOthers Rifampin, Lincomycin, Clindamycin, VancomycinRifampin, Lincomycin, Clindamycin, Vancomycin www.indiandentalacademy.com
  • 23. Properties of an ideal antibiotic:Properties of an ideal antibiotic:  SSelective and effective against micro-organismselective and effective against micro-organisms  Destroy micro-organismsDestroy micro-organisms ((Bactericidal action)Bactericidal action) Retard their growthRetard their growth (Bacteriostatic action).(Bacteriostatic action).  Not be ineffective as a result of bacterial resistance.Not be ineffective as a result of bacterial resistance.  Not be inactivated by enzymes, plasma proteins or body fluids.Not be inactivated by enzymes, plasma proteins or body fluids.  Quickly reach bactericidal levels throughout the body and beQuickly reach bactericidal levels throughout the body and be maintained for long periods.maintained for long periods.  Minimal adverse effects.Minimal adverse effects. www.indiandentalacademy.com
  • 24. Choice of an antimicrobial agentChoice of an antimicrobial agent Patient FactorPatient Factor AgeAge  Chloramphenicol – Gray Baby SyndromeChloramphenicol – Gray Baby Syndrome  Amino glycosides – VIII nerve toxicityAmino glycosides – VIII nerve toxicity  Tetracycline – Discolor teeth , Weaken BoneTetracycline – Discolor teeth , Weaken Bone Renal and Hepatic FunctionRenal and Hepatic Function  Drugs to be avoided in Renal FailureDrugs to be avoided in Renal Failure - Cephalosporin's, Amino glycosides , Tetracycline ,- Cephalosporin's, Amino glycosides , Tetracycline , Amphotericin BAmphotericin B www.indiandentalacademy.com
  • 25.  Drugs to be avoided in Liver diseasesDrugs to be avoided in Liver diseases - Erythromycin , Tetracycline , Nilidixic acid- Erythromycin , Tetracycline , Nilidixic acid Local FactorsLocal Factors  Pus and SecretionsPus and Secretions  HematomasHematomas  Foreign materialsForeign materials Drug allergyDrug allergy  History of Previous exposures to AMAsHistory of Previous exposures to AMAs Impaired Host DefenseImpaired Host Defense www.indiandentalacademy.com
  • 26. PregnancyPregnancy  Safe –Safe – Penicillin's , Cephalosporin's , ErythromycinPenicillin's , Cephalosporin's , Erythromycin  Unsafe –Unsafe – Tetracycline - Acute Yellow Atrophy – MotherTetracycline - Acute Yellow Atrophy – Mother Teeth & Bone deformities – OffspringTeeth & Bone deformities – Offspring Aminoglycosides – Fetal ear damageAminoglycosides – Fetal ear damage Clotrimoxazole , Chloramphenicol , SulfonamidesClotrimoxazole , Chloramphenicol , Sulfonamides Genetic Factor –Genetic Factor – Primaquine , Sulfonamides , Chloramphenicol –Primaquine , Sulfonamides , Chloramphenicol – Haemolycis in G – 6 PD deficiency patientHaemolycis in G – 6 PD deficiency patient www.indiandentalacademy.com
  • 27. Organism Related ConsiderationsOrganism Related Considerations  Clinical DiagnosisClinical Diagnosis  Bacteriological ExaminationBacteriological Examination Drug FactorsDrug Factors  Spectrum of activitySpectrum of activity  Type of ActivityType of Activity  Sensitivity of the organismSensitivity of the organism  Relative ToxicityRelative Toxicity www.indiandentalacademy.com
  • 28.  Route of AdministrationsRoute of Administrations Penicillin G, Carbenicillin ,Vancomycin,Penicillin G, Carbenicillin ,Vancomycin, Aminoglycosides.Aminoglycosides.  Evidence of Clinical EfficacyEvidence of Clinical Efficacy Reliable clinical trail data – Final guideReliable clinical trail data – Final guide  CostCost www.indiandentalacademy.com
  • 29. DRUG RESISTANCEDRUG RESISTANCE Unresponsiveness of a microorganism toUnresponsiveness of a microorganism to Antimicrobial agentsAntimicrobial agents A bacteria ,which as sensitive originally becomesA bacteria ,which as sensitive originally becomes Insensitive on further exposure easily be seen withInsensitive on further exposure easily be seen with Staphylococcus AureusStaphylococcus Aureus www.indiandentalacademy.com
  • 30.  Reasons for antibiotic resistanceReasons for antibiotic resistance Irrational antibiotic use – Wrong indicationIrrational antibiotic use – Wrong indication - Wrong doses- Wrong doses - Wrong duration- Wrong duration Self medicationSelf medication Local resistance patterns unavailable to physicianLocal resistance patterns unavailable to physician Patient emphasize on Expensive and Newer drugsPatient emphasize on Expensive and Newer drugs www.indiandentalacademy.com
  • 31. MechanismMechanism  BiochemicalBiochemical  Inactivation of the antibiotics by enzymesInactivation of the antibiotics by enzymes Produced by bacteriaProduced by bacteria e.g. Penicillinasee.g. Penicillinase  Beta- lactamase are produced by staphylococci,Beta- lactamase are produced by staphylococci, Haemophilus, GonococciHaemophilus, Gonococci  Chloramphenicol – Acetyl transferase -Chloramphenicol – Acetyl transferase - Resistant E.Coli , H. Influenzae , S. TyphiResistant E.Coli , H. Influenzae , S. Typhi  Aminoglycoside - Adenylate , Acetylate ,Aminoglycoside - Adenylate , Acetylate , PhosphorylatePhosphorylate www.indiandentalacademy.com
  • 32. DRUG TOLERANTDRUG TOLERANT  Loss of affinity of the target biomolecule of theLoss of affinity of the target biomolecule of the microorganismmicroorganism  Streptomycin, Rifampin, Macrolids,Streptomycin, Rifampin, Macrolids, Beta – lactam antibioticsBeta – lactam antibiotics Alternate pathway of metabolismAlternate pathway of metabolism  SulphonamidesSulphonamides  CycloserineCycloserine  TrimethoprimTrimethoprim www.indiandentalacademy.com
  • 33. Change in the permeability caused byChange in the permeability caused by antibioticsantibiotics  Tetracycline'sTetracycline's  Beta – lactam antibioticsBeta – lactam antibiotics  ChoramphenicolChoramphenicol  QuinolonesQuinolones www.indiandentalacademy.com
  • 34. Genetic MechanismGenetic Mechanism Natural ResistanceNatural Resistance  Lack of metabolic ProcessLack of metabolic Process  Lack of Target siteLack of Target site e.g. Gram negative bacillie.g. Gram negative bacilli - Unaffected by Penicillin- Unaffected by Penicillin M. Tuberculosis - Is insensitive to TetracyclineM. Tuberculosis - Is insensitive to Tetracycline Acquired ResistanceAcquired Resistance  Use of an AMAs over a period of timeUse of an AMAs over a period of time  Dependent on the - Micro organism ,Dependent on the - Micro organism , - Drug- Drug www.indiandentalacademy.com
  • 35. Two typesTwo types  MutationMutation  Stable and Heritable genetic changesStable and Heritable genetic changes  Single StepSingle Step e.g. Enterococci - Streptomycine.g. Enterococci - Streptomycin E. Coli , Staphylococci – RifampinE. Coli , Staphylococci – Rifampin  Multi StepMulti Step Erythromycin , Tetracycline , ChloramphenicolErythromycin , Tetracycline , Chloramphenicol www.indiandentalacademy.com
  • 36. Gene transferGene transfer  Conjugation –Conjugation –  That gene carrying the Resistance or R factorThat gene carrying the Resistance or R factor Gram Negative BacilliGram Negative Bacilli Chloramphenicol - Typhoid bacilliChloramphenicol - Typhoid bacilli Streptomycin - E . ColiStreptomycin - E . Coli Penicillin – Haemophilus , GonococciPenicillin – Haemophilus , Gonococci  TransductionTransduction Penicillin's , Erythromycins , ChloramphenicolPenicillin's , Erythromycins , Chloramphenicol  TransformationTransformation  Passage of Naked DNAPassage of Naked DNA  Pneumococcal – Penicillin GPneumococcal – Penicillin G www.indiandentalacademy.com
  • 37.  Cross ResistanceCross Resistance  Resistance to One AMAs confirming resistanceResistance to One AMAs confirming resistance to another AMAs .to another AMAs .  Chemically or Mechanically related drugsChemically or Mechanically related drugs Sulfonamides - All other same groupSulfonamides - All other same group Tetracycline – ChloramphenicolTetracycline – Chloramphenicol Erythromycin - LincomycinErythromycin - Lincomycin www.indiandentalacademy.com
  • 38. PreventionPrevention  No inadequate , 0r Prolonged useNo inadequate , 0r Prolonged use  Rapidly acting and selective drugsRapidly acting and selective drugs  Broad spectrum – Specific one cannot beBroad spectrum – Specific one cannot be determineddetermined  Prolonged therapy – Combination therapyProlonged therapy – Combination therapy www.indiandentalacademy.com
  • 39. Beta- Lactam antibioticsBeta- Lactam antibiotics Penicillin'sPenicillin's  First antibiotic to be used clinically in 1941First antibiotic to be used clinically in 1941  Penicillium notatumPenicillium notatum  Present source – Mutant of P. chrysogenumPresent source – Mutant of P. chrysogenum www.indiandentalacademy.com
  • 40. Mechanism of actionMechanism of action  Interfere with the synthesis of bacterial cell wallInterfere with the synthesis of bacterial cell wall  Inhibit the transpeptidasesInhibit the transpeptidases  Peptidoglycan cell wall is unique to bacteria.Peptidoglycan cell wall is unique to bacteria.  Gram positive bacteria - PeptidoglycanGram positive bacteria - Peptidoglycan  Gram negative bacteria -Lipoprotein ,Gram negative bacteria -Lipoprotein , Peptidoglycan.Peptidoglycan. www.indiandentalacademy.com
  • 41.  Bactericidal actionBactericidal action Bacteria divide in the presence of aBacteria divide in the presence of a beta – lactam antibioticbeta – lactam antibiotic Cell wall deficient forms are producedCell wall deficient forms are produced Normally bacterium interior is hyper osmoticNormally bacterium interior is hyper osmotic DiffusionDiffusion Bacterium swell and burstBacterium swell and burst Bacterial lysisBacterial lysis www.indiandentalacademy.com
  • 42. PinicillinasePinicillinase  Staphylococci, some strains of Gonococci , E.Coli,Staphylococci, some strains of Gonococci , E.Coli, H. Influenzae.H. Influenzae.  Opens the Beta- lactam ring and inactivates PnGOpens the Beta- lactam ring and inactivates PnG Penicillin GPenicillin G  Narrow spectrumNarrow spectrum  Acid labileAcid labile  t ½ - 30 mint ½ - 30 min  Distributed extracellularlyDistributed extracellularly  Very rapid renal excretionVery rapid renal excretion  Tubular secretion of PnG blocked by – ProbenecidTubular secretion of PnG blocked by – Probenecid www.indiandentalacademy.com
  • 43. DoseDose CrystallineCrystalline PenicillinPenicillin 0.5 – 5 MU0.5 – 5 MU i.m / i.v 6- 12 hi.m / i.v 6- 12 h CrystapenCrystapen 0.2, 0.5,0.2, 0.5, 1 MU inj1 MU inj ProcaineProcaine Penicillin GPenicillin G 0.5 – 1 MU i.m0.5 – 1 MU i.m 12- 24 h12- 24 h ProcaineProcaine PenicillinPenicillin G 0.5 – 1 MUG 0.5 – 1 MU BenzathineBenzathine PenicillinPenicillin 0.6 – 2.4 MU i.m0.6 – 2.4 MU i.m 2-4 w2-4 w LONGACILLINLONGACILLIN PENCOMPENCOM 0.6, 1.2, 2.4 MU0.6, 1.2, 2.4 MU www.indiandentalacademy.com
  • 44. Adverse effectsAdverse effects  Local irritancy and Direct toxicityLocal irritancy and Direct toxicity  Pain , Nausea, Thrombophlebitis,Pain , Nausea, Thrombophlebitis,  HypersensitivityHypersensitivity More commonMore common –– Rash , Itching , Urticaria, FeverRash , Itching , Urticaria, Fever Less commonLess common –– Angioneurotic edema, Serum sickness,Angioneurotic edema, Serum sickness, Bronchospasm, Exfoliative dermatitisBronchospasm, Exfoliative dermatitis Rare-Rare- AnaphylaxisAnaphylaxis More commonly seen – ParenteralMore commonly seen – Parenteral - Procaine penicillin G- Procaine penicillin G Scratch test, Intradermal testScratch test, Intradermal test -Performed first-Performed first www.indiandentalacademy.com
  • 45.  Super infectionsSuper infections Bowel, respiratory, cutaneous micro flora changesBowel, respiratory, cutaneous micro flora changes  Jarisch – Herxheimer reactionJarisch – Herxheimer reaction  Injected in a syphilitic patientInjected in a syphilitic patient  Shivering, fever , myalgia, exacerbation ofShivering, fever , myalgia, exacerbation of lesionslesions  Due to sudden release of spirochetal lyticDue to sudden release of spirochetal lytic productsproducts  Lasts 12- 72 hLasts 12- 72 h  Aspirin and sedation afford relief of symptomsAspirin and sedation afford relief of symptoms www.indiandentalacademy.com
  • 46. UsesUses  Streptococcal, Pneumococcal, MeningococcalStreptococcal, Pneumococcal, Meningococcal  Syphilis, Gonorrhoea, DiphtheriaSyphilis, Gonorrhoea, Diphtheria  Tetanus , Gas gangreneTetanus , Gas gangrene  Prophylactic useProphylactic use  Rheumatic fever – 1.2 MU every 4wRheumatic fever – 1.2 MU every 4w till 18y of age ( or ) 5 years after antill 18y of age ( or ) 5 years after an attackattack  Gonorrhoea or syphilis – P.P (or ) Pn G –Gonorrhoea or syphilis – P.P (or ) Pn G – 2.4 MU single dose before or within 12 h of contact2.4 MU single dose before or within 12 h of contact affordsaffords  Bacterial endocarditisBacterial endocarditis  AgranulocytosisAgranulocytosis  Surgical infectionsSurgical infections – PP - 1MU+ Aminoglycosides– PP - 1MU+ Aminoglycosideswww.indiandentalacademy.com
  • 47. Semisynthetic Penicillin'sSemisynthetic Penicillin's  Chemically combining specific side chainsChemically combining specific side chains  Aim –Aim –  Overcome the shortcoming of PnGOvercome the shortcoming of PnG  Poor oral efficacyPoor oral efficacy  Susceptibility to PenicillinaseSusceptibility to Penicillinase  Narrow spectrum of activityNarrow spectrum of activity  HypersensitivityHypersensitivity www.indiandentalacademy.com
  • 48. ClassificationClassification  Acid resistant alternative to Penicillin GAcid resistant alternative to Penicillin G Phenoxy methyl Penicillin( Penicillin V )Phenoxy methyl Penicillin( Penicillin V )  Penicillinase resistant Penicillin'sPenicillinase resistant Penicillin's Methicillin , Oxacillin , Cloxacillin , NafcillinMethicillin , Oxacillin , Cloxacillin , Nafcillin  Extended spectrum PenicillinsExtended spectrum Penicillins Aminopenicillins – Ampicillin , amoxicillinAminopenicillins – Ampicillin , amoxicillin Carboxy Penicillins – Carbenicillin, TicarcillinCarboxy Penicillins – Carbenicillin, Ticarcillin UreidoPenicillins – Piperacillin , MezlocillinUreidoPenicillins – Piperacillin , Mezlocillin Mecillinam – AmdinocillinMecillinam – Amdinocillin  Beta- Lactamase inhibitors-Beta- Lactamase inhibitors- Clavulonic acid , SulbactamClavulonic acid , Sulbactamwww.indiandentalacademy.com
  • 49. Acid resistant alternative to Penicillin GAcid resistant alternative to Penicillin G  Phenoxy methyl Penicillin( Penicillin V )Phenoxy methyl Penicillin( Penicillin V )  Acid stableAcid stable  Active against – Neisseria, Other GramActive against – Neisseria, Other Gram negative bacteria , Anaerobes .negative bacteria , Anaerobes .  Used in –Streptococcal Pharyngitis , Sinusitis ,Used in –Streptococcal Pharyngitis , Sinusitis , Otitis media, Prophylaxis of rheumatic fever ,Otitis media, Prophylaxis of rheumatic fever , Trench mouthTrench mouth www.indiandentalacademy.com
  • 50. Penicillinase Resistant Penicillin's (Cloxacillin)Penicillinase Resistant Penicillin's (Cloxacillin)  Isoxazolyl side chainIsoxazolyl side chain  Highly Penicillinase as well as acid resistantHighly Penicillinase as well as acid resistant  t ½ - 1 ht ½ - 1 h  Elimination primarily by KidneyElimination primarily by Kidney Aminopenicillins –Aminopenicillins – AmpicillinAmpicillin Active against – all microorganisms sensitive to PnG ,Active against – all microorganisms sensitive to PnG , and Gram negative bacilliand Gram negative bacilli e.g.. H. Influenzae, E. coli , Proteus , Salmonella , Shigella .e.g.. H. Influenzae, E. coli , Proteus , Salmonella , Shigella . Adverse effects – Diarrhoea , Rashes , HypersensitivityAdverse effects – Diarrhoea , Rashes , Hypersensitivity Extended spectrum PenicillinsExtended spectrum Penicillins www.indiandentalacademy.com
  • 51.  Beta- Lactamase inhibitors-Beta- Lactamase inhibitors-  Clavulonic acidClavulonic acid  Streptomyces ClavuligerusStreptomyces Clavuligerus  Inhibition increase with timeInhibition increase with time IndicationsIndications  Skin & Soft tissue infectionsSkin & Soft tissue infections  Urinary ,Respiratory , Bilary tract infectionsUrinary ,Respiratory , Bilary tract infections www.indiandentalacademy.com
  • 52. NAMENAME DOSEDOSE DRUG NAMEDRUG NAME PenicillinVPenicillinV 250- 500 mg - Adults,250- 500 mg - Adults, 125 - 250 mg - Children125 - 250 mg - Children 60 mg - Infants60 mg - Infants CRYSTAPEN – VCRYSTAPEN – V ,, KAYPENKAYPEN - 125, 250 mg- 125, 250 mg TabTab CloxacillinCloxacillin 0.25 – 0.5 gm orally every 6 h0.25 – 0.5 gm orally every 6 h severe infections 0.25 – 1 gmsevere infections 0.25 – 1 gm i.m / i.vi.m / i.v KLOXKLOX 0.25,0.5 gm cap, inj0.25,0.5 gm cap, inj BIOCLOX , CLOCILINBIOCLOX , CLOCILIN 0.25 , 0.5 gm cap0.25 , 0.5 gm cap AmpicillinAmpicillin 250- 500 mg - Adults250- 500 mg - Adults 100 mg / ml - Children100 mg / ml - Children AMPILIN,AMPILIN, ROSCILLIN,ROSCILLIN, BIOCILLINBIOCILLIN 250, 500 mg Cap250, 500 mg Cap AmoxicillinAmoxicillin 0.25 – 1 gm TDS oral0.25 – 1 gm TDS oral AMOXIL , MOXAMOXIL , MOX 250, 500 mg cap250, 500 mg cap AMOXYLIN ,AMOXYLIN , NOVAMOX,NOVAMOX, SYNAMOXSYNAMOX 250, 500 mg250, 500 mg cap .cap . 125 mg /5ml dry syrup125 mg /5ml dry syrup www.indiandentalacademy.com
  • 53. CarbenicillinCarbenicillin 1 gm ,5gm i. v1 gm ,5gm i. v CARBBLINCARBBLIN 1gm, 5gm inj1gm, 5gm inj PiperacillinPiperacillin PIPRAPENPIPRAPEN 1gm, 2gm1gm, 2gm PIPRACILPIPRACIL 2gm , 4gm2gm , 4gm vials for injvials for inj Clavulonic acidClavulonic acid AUGMENTIN ,AUGMENTIN , ENHANCIN,ENHANCIN, AMONATEAMONATE ,, Amoxicillin 250 mg +Amoxicillin 250 mg + Clavulonic acid 125 mgClavulonic acid 125 mg TDSTDS severe infections – 6 hsevere infections – 6 h SulbactamSulbactam Ampicillin 1 gmAmpicillin 1 gm +Sulbactam 0.5 gm per+Sulbactam 0.5 gm per vial inj 6-8 hvial inj 6-8 h SULBACINSULBACIN AMPITUMAMPITUM www.indiandentalacademy.com
  • 54. CEPHALOSPORINSCEPHALOSPORINS  Cephalosporium – Fungus ,Bactericidal .Cephalosporium – Fungus ,Bactericidal .  Chronological sequences of developmentChronological sequences of development ParenteralParenteral CephalothinCephalothin CefazolinCefazolin CephaloridineCephaloridine OralOral CephalexinCephalexin CefadroxilCefadroxil ParenteralParenteral CefuroximeCefuroxime CefoxitinCefoxitin OralOral CefaclorCefaclor CefuroximeCefuroxime ParenteralParenteral CefotaximeCefotaxime CeftriaxoneCeftriaxone CefoperazoneCefoperazone OralOral CefiximeCefixime ParenteralParenteral CefepimeCefepime CefpiromeCefpirome www.indiandentalacademy.com
  • 55. CephalexinCephalexin 0.25 – 1 gm 6-8 h Adult0.25 – 1 gm 6-8 h Adult ChildrenChildren 25 – 100 mg / kg / day25 – 100 mg / kg / day SPORIDEX, ALCEPHIN,SPORIDEX, ALCEPHIN, CEPHAXIN ,CEPHAXIN , 250- 500 mg Cap250- 500 mg Cap CefadroxilCefadroxil DROXYL-DROXYL- 0.5 ,1 gm tab0.5 ,1 gm tab CEFADROXCEFADROX 0.5 mg Cap0.5 mg Cap KEFLOXINKEFLOXIN 0.5 mg Cap0.5 mg Cap 250 mg kid tab250 mg kid tab BDBD CefotaximeCefotaxime 1-2 gm i.m /iv 6-12h1-2 gm i.m /iv 6-12h Children 50 -100Children 50 -100 mg/kg/daymg/kg/day CLAFORANCLAFORAN 0.25 &1 gm /vial inj0.25 &1 gm /vial inj CefazolinCefazolin Mild cases – 0.25 gm 8hMild cases – 0.25 gm 8h Severe cases – 1 gm 6hSevere cases – 1 gm 6h i/m ,i/vi/m ,i/v ALCIZONALCIZON ORIZOLINORIZOLIN 0.25,0.5 gm per vial inj0.25,0.5 gm per vial inj CeftazidimeCeftazidime FORTUM , CEFAZIDFORTUM , CEFAZID 0.25,0.5,1 gm per vial inj0.25,0.5,1 gm per vial inj every 8hevery 8h www.indiandentalacademy.com
  • 56.  Adverse effectsAdverse effects  Pain - CephalothinPain - Cephalothin  Diarrhoea- OralDiarrhoea- Oral  Hypersensitivity reactions – Coomb’s testHypersensitivity reactions – Coomb’s test  Nephro toxicity – Cephalothin,Nephro toxicity – Cephalothin, CephaloridineCephaloridine  Bleeding - Ceftriaxone , CefoperazoneBleeding - Ceftriaxone , Cefoperazone  Neutropenia - CeftazidimeNeutropenia - Ceftazidime www.indiandentalacademy.com
  • 57. Tetracycline'sTetracycline's  Broad-spectrum antibioticsBroad-spectrum antibiotics  Obtained from ActinomycetesObtained from Actinomycetes  First – Chlortetracycline – In 1948 - AureomycinFirst – Chlortetracycline – In 1948 - Aureomycin Group I Group II Group IIIGroup I Group II Group III ChlortetracyclineChlortetracycline DemoclocyclineDemoclocycline DoxycyclineDoxycycline OxytetracyclineOxytetracycline MethacyclineMethacycline MinocyclineMinocycline TetracyclineTetracycline LymecyclineLymecycline www.indiandentalacademy.com
  • 58.  BacteriostaticBacteriostatic  Inhibits protein synthesis by binding to 30 SInhibits protein synthesis by binding to 30 S Ribosome's in susceptible organismRibosome's in susceptible organism  Inhibited – All typesInhibited – All types  Except – Fungi , VirusesExcept – Fungi , Viruses  Absorbed from G.I.TAbsorbed from G.I.T  Chelating Property - Calcium , Some metalsChelating Property - Calcium , Some metals  Milk , Iron Preparations, Nonsystemic AntacidsMilk , Iron Preparations, Nonsystemic Antacids Sucralfate .Sucralfate .  Secreted in milkSecreted in milk  Oral administration – Should be taken ½ beforeOral administration – Should be taken ½ before (or ) 2 h after food .(or ) 2 h after food . www.indiandentalacademy.com
  • 59. ChlorChlor tetracyclinetetracycline AureomycinAureomycin 250 , 500 mg Cap250 , 500 mg Cap OxyOxy tetracyclinetetracycline Terramycin -Terramycin - Oxysteclin -Oxysteclin - 3% Skin ,1% eye3% Skin ,1% eye ointmentointment 250 , 500 mg Cap250 , 500 mg Cap 50 mg /ml inj in 2 ml amp50 mg /ml inj in 2 ml amp and 20 ml vialand 20 ml vial TetracyclineTetracycline AchromycinAchromycin HostacyclinHostacyclin 250 , 500 mg Cap250 , 500 mg Cap 100mg vial for i.m100mg vial for i.m 250-500 mg vial for i. v250-500 mg vial for i. v DoxycyclineDoxycycline Tetradox,Biodoxi,Tetradox,Biodoxi, Duracyclin , DoxyDuracyclin , Doxy Cap 100 mg capCap 100 mg cap 2cap 12cap 1stst day, 1cap 2day, 1cap 2ndnd dayday www.indiandentalacademy.com
  • 60. IndicationsIndications  Aggressive PeriodontitisAggressive Periodontitis  Refractory Periodontitis.Refractory Periodontitis.  Debridement and even surgery have failed-Debridement and even surgery have failed- Indicating that chemotherapyIndicating that chemotherapy Contraindications:Contraindications: • Permanent discoloration of teeth.Permanent discoloration of teeth. • Pregnancy and lactation.Pregnancy and lactation. • Oral contraceptives - less effective.Oral contraceptives - less effective. • Depress serum prothrombin activityDepress serum prothrombin activity www.indiandentalacademy.com
  • 61. Adverse effectAdverse effect Irritative effectIrritative effect – Epigastric pain ,Nausea– Epigastric pain ,Nausea Vomiting , Diarrhoea, esophageal UlcerationVomiting , Diarrhoea, esophageal Ulceration Liver damageLiver damage -- Safer – Tetracycline , OxytetracyclineSafer – Tetracycline , Oxytetracycline Tetracycline – Acute hepatic necrosis –Tetracycline – Acute hepatic necrosis – Pregnant womenPregnant women Kidney damageKidney damage - except Doxycycline- except Doxycycline Photo toxicityPhoto toxicity -Doxycycline ,Democlocycline-Doxycycline ,Democlocycline www.indiandentalacademy.com
  • 62.  Teeth and BoneTeeth and Bone  Calcium – Tetracycline Chelate DepositionCalcium – Tetracycline Chelate Deposition  Brown discoloration ill formed teethBrown discoloration ill formed teeth  Mid pregnancy to 5 months – Deciduous teethMid pregnancy to 5 months – Deciduous teeth  5 months to 5 years - Permanent anterior teeth5 months to 5 years - Permanent anterior teeth  More susceptible to cariesMore susceptible to caries  Temporary suppression of bone growthTemporary suppression of bone growth www.indiandentalacademy.com
  • 63.  HypersensitivityHypersensitivity  Vestibular toxicityVestibular toxicity  Super infectionSuper infection  Diabetes insipidus –Diabetes insipidus –  Democlocycline antagonizes A.D.H actionDemoclocycline antagonizes A.D.H action  Ant anabolic effect – Reduce ProteinAnt anabolic effect – Reduce Protein SynthesisSynthesis www.indiandentalacademy.com
  • 64. METRONIDAZOLE:  Nitroimidazole compound.  Bactericidal to anaerobic organisms ( P . Gingivalis , P. Intermedia ).  cytotoxic metabolites of metronidazole directly interact with bacterial DNA - cell death. Clinical UseClinical Use  Gingivitis, ANUG, Chronic Periodontitis, AggressiveGingivitis, ANUG, Chronic Periodontitis, Aggressive Periodontitis, and Refractory Periodontitis.Periodontitis, and Refractory Periodontitis.  Not the drug of choice to treat A.actinomycetemNot the drug of choice to treat A.actinomycetem comitans infections. Effective when used incomitans infections. Effective when used in combination with other antibiotics.combination with other antibiotics.  A single dose of metronidazole (A single dose of metronidazole (250 mg orally250 mg orally)) appears in both serum and gingival fluid in sufficientappears in both serum and gingival fluid in sufficient quantity to inhibit periodontal pathogens.quantity to inhibit periodontal pathogens. www.indiandentalacademy.com
  • 65.  SSynergistically with amoxicillinynergistically with amoxicillin  Useful in many mixed periodontal infections.Useful in many mixed periodontal infections.  Commonly prescribed regimen isCommonly prescribed regimen is 250 mg t.i.d for 7250 mg t.i.d for 7 days.days. Contraindications:Contraindications: • An ant abuse effectAn ant abuse effect • Alcohol ingestion, since abdominal distress, nausea,Alcohol ingestion, since abdominal distress, nausea, vomiting and / or headache may occurvomiting and / or headache may occur • TumorigenicityTumorigenicity • Pregnant women and nursing mothersPregnant women and nursing mothers • An anti-abuse drugAn anti-abuse drug • Patients receiving anticoagulants, lithium or disulfuranPatients receiving anticoagulants, lithium or disulfuran www.indiandentalacademy.com
  • 66. MacrolidsMacrolids  ErythromycinErythromycin  Isolated from Streptomyces erythreus in 1952Isolated from Streptomyces erythreus in 1952  Bacteriostatic at low concentrationsBacteriostatic at low concentrations  Bactericidal at high concentrationsBactericidal at high concentrations  Acts by inhibiting bacterial protein synthesis .Acts by inhibiting bacterial protein synthesis .  Highly active againstHighly active against –– Streptococcus pyogensStreptococcus pyogens - Streptococcus Pnuemoniae- Streptococcus Pnuemoniae - Clostridia , N. gonorrhoeae- Clostridia , N. gonorrhoeae www.indiandentalacademy.com
  • 67. PharmacokineticsPharmacokinetics  Acid labileAcid labile  Enteric coated tabletsEnteric coated tablets  Crosses Placenta , but not blood – brain barrierCrosses Placenta , but not blood – brain barrier  Plasma t ½ - 1.5 hPlasma t ½ - 1.5 h  Excreted primarily - in the Bile in the activeExcreted primarily - in the Bile in the active formform www.indiandentalacademy.com
  • 68. ErythromycinErythromycin 250-500mg 6h250-500mg 6h Max 8gm/ dayMax 8gm/ day Children 30-Children 30- 60mg/kg/day60mg/kg/day ERYSAFEERYSAFE 125,250,500 mg tab125,250,500 mg tab EROMEDEROMED 333mg333mg E. StearateE. Stearate ERYTHROCINERYTHROCIN 100,250,500mg tab100,250,500mg tab E. EstolateE. Estolate (Acid stable )(Acid stable ) ALTHROCINALTHROCIN 250,500mg tab250,500mg tab 100mg /ml100mg /ml Pedo dropsPedo drops E. EthylE. Ethyl SuccinateSuccinate ERYNATEERYNATE ERYTHROCINERYTHROCIN 100mg /5ml dry syr100mg /5ml dry syr 100mg /ml drops100mg /ml drops www.indiandentalacademy.com
  • 69. Adverse effectsAdverse effects  Remarkably safe drugRemarkably safe drug  Gastro intestinalGastro intestinal  Epigastric pain , DiarrhoeaEpigastric pain , Diarrhoea  HypersensitivityHypersensitivity USESUSES  Alternative to penicillin in allergic patientsAlternative to penicillin in allergic patients  First choice drug forFirst choice drug for  Atypical pneumonia - 3 w treatmentAtypical pneumonia - 3 w treatment  Whooping cough - 2w TreatmentWhooping cough - 2w Treatment www.indiandentalacademy.com
  • 70. Newer MacrolidsNewer Macrolids  Overcome the limitations of erythromycinsOvercome the limitations of erythromycins  Narrow spectrum gastric intoleranceNarrow spectrum gastric intolerance  Gastric acid LiabilityGastric acid Liability  Low oral bioavailabilityLow oral bioavailability  Poor tissue penetrationPoor tissue penetration  Short half lifeShort half life  Semi synthetic MacrolidsSemi synthetic Macrolids www.indiandentalacademy.com
  • 71. RoxithroRoxithro mycinmycin t ½t ½ -12h-12h 15 mg BD 30 min15 mg BD 30 min before mealsbefore meals ChildrenChildren 2.5 -5 mg /kg BD2.5 -5 mg /kg BD ROXID,ROXID, ROXEM,ROXEM, ROXIBIDROXIBID 150 mg tab150 mg tab ClarithroClarithro mycinmycin 3-6 h3-6 h 250mg BD for 7days250mg BD for 7days Severe cases 500mgSevere cases 500mg BDBD up to 14 daysup to 14 days CLARBIDCLARBID CELEXCELEX 250 ,500mg250 ,500mg tabtab AZITHROAZITHRO MYCINMYCIN >50h>50h ZITHROMACZITHROMAC AZITHRALAZITHRAL AZIWOKAZIWOK 250 mg cap250 mg cap 250mg cap250mg cap 250mg cap250mg cap 100 mg KID tab100 mg KID tab www.indiandentalacademy.com
  • 72. FluoroquinolonesFluoroquinolones Primarily against gram negative bacteriaPrimarily against gram negative bacteria First generation second generationFirst generation second generation Norfloxacin LomefloxacinNorfloxacin Lomefloxacin Ciprofloxacin SparfloxacinCiprofloxacin Sparfloxacin Ofloxacin FleroxacinOfloxacin Fleroxacin Pefloxacin AmifloxacinPefloxacin Amifloxacin  Inhibits the enzyme bacterial DNA gyraseInhibits the enzyme bacterial DNA gyrase www.indiandentalacademy.com
  • 73. CIPROFLOXACINCIPROFLOXACIN  Most susceptible toMost susceptible to Aerobic gram negative bacilliAerobic gram negative bacilli Enterobacteriaceae , NeisseriaEnterobacteriaceae , Neisseria  Rapidly absorbed OrallyRapidly absorbed Orally  High tissue penitrationHigh tissue penitration  Excreted primarily in urineExcreted primarily in urine  t ½ 35 ht ½ 35 h www.indiandentalacademy.com
  • 74.  CIFRANCIFRAN 250 , 500 , 750 mg tab250 , 500 , 750 mg tab  CIPLOXCIPLOX 250 , 500 , 750 mg tab250 , 500 , 750 mg tab 200 mg / 100 ml i/v infusion200 mg / 100 ml i/v infusion  CIPROFLOX , QUINTORCIPROFLOX , QUINTOR 250 , 500 mg tab250 , 500 mg tab  CIPROBIDCIPROBID 250 , 500 , 750 mg tab250 , 500 , 750 mg tab 3mg /ml eye drops3mg /ml eye drops www.indiandentalacademy.com
  • 75.  Wide spectrum bactericidal activityWide spectrum bactericidal activity  UTIUTI  GonorrheaGonorrhea  Typhoid 500-750 mg BD for 10 daysTyphoid 500-750 mg BD for 10 days  Bone , Soft tissue wound infections along withBone , Soft tissue wound infections along with metronidazolemetronidazole  MeningitisMeningitis OFLOXACINOFLOXACIN  More potent than ciprofloxacin for gram positiveMore potent than ciprofloxacin for gram positive organismsorganisms  ZANOCIN , TARIVIDZANOCIN , TARIVID -- 100, 200 mg tab100, 200 mg tab 200mg / 100ml i.v infusion200mg / 100ml i.v infusion www.indiandentalacademy.com
  • 76. ClindamycinClindamycin  BacteriostaticBacteriostatic  Inhibits bacterial protein synthesis, by bindingInhibits bacterial protein synthesis, by binding irreversibly to 50S ribosomal subunit.irreversibly to 50S ribosomal subunit.  Active against - gram-positive bacteria,Active against - gram-positive bacteria, ( both facultative and anaerobic species. )( both facultative and anaerobic species. ) gram negative anaerobes.gram negative anaerobes.  Inherently resistant to - Eikenella corrodens,Inherently resistant to - Eikenella corrodens, - A. actinomycetemcomitans- A. actinomycetemcomitans  Effective in - Allergic to penicillin.Effective in - Allergic to penicillin. www.indiandentalacademy.com
  • 77.  Refractory patients.- 150 mg q.i.d for 10 days.Refractory patients.- 150 mg q.i.d for 10 days. 300 mg twice daily for 8 days.300 mg twice daily for 8 days.  Efficacy in - Periodontitis refractory toEfficacy in - Periodontitis refractory to tetracycline therapy.tetracycline therapy. Side EffectsSide Effects  Pseudo membranous colitisPseudo membranous colitis  Watery diarrhea, fever, leucocytosis and crampyWatery diarrhea, fever, leucocytosis and crampy abdominal pain beginning on 4abdominal pain beginning on 4thth to 9to 9thth day ofday of antibiotic therapy suggestive ofantibiotic therapy suggestive of Pseudo membranous colitis.Pseudo membranous colitis.  EnterotoxinEnterotoxin www.indiandentalacademy.com
  • 78. Local delivery of antibioticsLocal delivery of antibiotics  Targeting an antimicrobial to infection sites andTargeting an antimicrobial to infection sites and sustaining its localized concentration at effectivesustaining its localized concentration at effective levels for a sufficient time .levels for a sufficient time .  Minimal or no side effects.Minimal or no side effects.  Antibiotic concentrations are releasedAntibiotic concentrations are released continuously.continuously.  Recent advances - Resulted in the controlledRecent advances - Resulted in the controlled Release of drugs.Release of drugs. www.indiandentalacademy.com
  • 79.  Local subgingival delivery devices (antibiotic) for up to 24 hoursLocal subgingival delivery devices (antibiotic) for up to 24 hours  Active ingredients are incorporated into an agent (fibers, gels,Active ingredients are incorporated into an agent (fibers, gels, chips, collagen film, acrylic strips, and a polymer). The activechips, collagen film, acrylic strips, and a polymer). The active ingredient is then released over a period of daysingredient is then released over a period of days Aims at three targets:Aims at three targets:  Support of non-surgical mechanical anti-infective therapy.Support of non-surgical mechanical anti-infective therapy.  Support of re-instrumentation during supportive periodontalSupport of re-instrumentation during supportive periodontal therapy.therapy.  As alternative to subgingival re-instrumentation duringAs alternative to subgingival re-instrumentation during supportive periodontal therapy.supportive periodontal therapy. www.indiandentalacademy.com
  • 80.  Goodson and co workers (1979). – first to testGoodson and co workers (1979). – first to test  Using Permeable hollow Cellulose Acetate fibers filledUsing Permeable hollow Cellulose Acetate fibers filled with 20%solution of tetracycline.with 20%solution of tetracycline. Tetracycline-Containing FibersTetracycline-Containing Fibers (Actisite)(Actisite)  Ethylene/vinyl acetate copolymer fiber, diameterEthylene/vinyl acetate copolymer fiber, diameter 0.5 mm, containing tetracycline, 12.7 mg/9 inches.0.5 mm, containing tetracycline, 12.7 mg/9 inches.  Sustains tetracycline concentrations for 10 daysSustains tetracycline concentrations for 10 days exceeding 1300 µg/ml.exceeding 1300 µg/ml.  Well beyond the 32 to 64 µg/ml required to inhibit theWell beyond the 32 to 64 µg/ml required to inhibit the growth of Periodontal Pathogens.growth of Periodontal Pathogens. www.indiandentalacademy.com
  • 81. Placement of ActisitePlacement of Actisite www.indiandentalacademy.com
  • 82. Disadvantages of the fiberDisadvantages of the fiber  The length of time required for placementThe length of time required for placement (10 minutes or more per tooth).(10 minutes or more per tooth).  The considerable learning curve required to gainThe considerable learning curve required to gain proficiency at placement.proficiency at placement.  The need for a second patient appointment 10The need for a second patient appointment 10 days after placement for removal of the fiber.days after placement for removal of the fiber.  Also, placement of fibers around 12 or moreAlso, placement of fibers around 12 or more teeth has resulted in oral candidiasis in a fewteeth has resulted in oral candidiasis in a few cases.cases. www.indiandentalacademy.com
  • 83. Subgingival Delivery of DoxycyclineSubgingival Delivery of Doxycycline:: (Atridox)(Atridox)  Doxycycline (10%) - Syringeable gel system.Doxycycline (10%) - Syringeable gel system.  Controlled-release product.Controlled-release product.  Two-syringe mixing system.Two-syringe mixing system.  Stored at 2°– 8°CStored at 2°– 8°C  Syringe A - 450 mg of the Atrigel Delivery System,Syringe A - 450 mg of the Atrigel Delivery System, (36.7% poly actide dissolved in 63.3% N methyl-2-pyrrolidone)(36.7% poly actide dissolved in 63.3% N methyl-2-pyrrolidone)  Syringe B - Doxycycline hyclate equivalent to 42.5 mg ofSyringe B - Doxycycline hyclate equivalent to 42.5 mg of Doxycycline. .Doxycycline. .  Upon contact with crevicular fluid it solidifiesUpon contact with crevicular fluid it solidifies  Allowing drug release for seven days.Allowing drug release for seven days. www.indiandentalacademy.com
  • 85. Subgingival Delivery System of MinocyclineSubgingival Delivery System of Minocycline (Arestin):(Arestin):  2% Minocycline Hydrochloride.2% Minocycline Hydrochloride.  Syringeable gel suspension formulation.Syringeable gel suspension formulation.  Arestin “microspheres” (minocycline HCL 1mg)Arestin “microspheres” (minocycline HCL 1mg)  Availability - Box with 2 trays, each containing 12 cartridges.Availability - Box with 2 trays, each containing 12 cartridges.  Each cartridge contains 1 mg of minocycline microencapsulatedEach cartridge contains 1 mg of minocycline microencapsulated in 3 mg of poly (glycolide-lactide) dry powder.in 3 mg of poly (glycolide-lactide) dry powder.  Cartridge is inserted into an autoclavable cartridge handle toCartridge is inserted into an autoclavable cartridge handle to administer.administer. www.indiandentalacademy.com
  • 87. Subgingival Delivery of Metronidazole:Subgingival Delivery of Metronidazole:  Oil-based metronidazole 25% dental gelOil-based metronidazole 25% dental gel  It is liquidized by the body heat and thenIt is liquidized by the body heat and then hardens again forming crystals in contacthardens again forming crystals in contact with water.with water.  Two 25% gel applications at a 1-weekTwo 25% gel applications at a 1-week interval have been used in cinterval have been used in c www.indiandentalacademy.com
  • 88. Combination antibiotic therapyCombination antibiotic therapy  Oral infections is a ‘mixed’ infections.Oral infections is a ‘mixed’ infections.  no single antibiotic is effective against all pathogens.no single antibiotic is effective against all pathogens.  use more than one antibiotic, either serially or in combination.use more than one antibiotic, either serially or in combination.  when Bacteriostatic and bactericidal antibiotic drugs are requiredwhen Bacteriostatic and bactericidal antibiotic drugs are required they are best given serially, not in combination.they are best given serially, not in combination.  Combination therapy:Combination therapy:  Should exhibit synergy or additive effects in vitro.Should exhibit synergy or additive effects in vitro.  E.g., Metronidazole-amoxicillin,E.g., Metronidazole-amoxicillin,  metronidazole-Augmentinmetronidazole-Augmentin  metronidazole-ciprofloxacin.metronidazole-ciprofloxacin. www.indiandentalacademy.com
  • 89.  IndicationsIndications  Oral infections involving variety of pathogenicOral infections involving variety of pathogenic species with differing antimicrobialspecies with differing antimicrobial susceptibility.susceptibility.  To overcome the drug-protective effectsTo overcome the drug-protective effects  Development of resistant strains.Development of resistant strains. www.indiandentalacademy.com
  • 90. Common Antibiotic Therapies AntibioticAntibiotic Adult dosageAdult dosage MetronidazoleMetronidazole 500 mg/t.i.d/8 days500 mg/t.i.d/8 days ClindamycinClindamycin 300 mg/t.i.d/8 days300 mg/t.i.d/8 days Doxycycline or MinocyclineDoxycycline or Minocycline 100-200 mg/q.d/7 days100-200 mg/q.d/7 days CiprofloxacinCiprofloxacin 500 mg/b.i.d/8 days500 mg/b.i.d/8 days AzithromycinAzithromycin 500 mg q.d/4-7 days500 mg q.d/4-7 days Metronidazole +AmoxicillinMetronidazole +Amoxicillin 250 mg/t.i.d/8 days each drug250 mg/t.i.d/8 days each drug Metronidazole + CiprofloxacinMetronidazole + Ciprofloxacin 500 mg/b.i.d/8 days each drug500 mg/b.i.d/8 days each drug www.indiandentalacademy.com
  • 91. ConclusionConclusion  Although over 300 species of bacteria areAlthough over 300 species of bacteria are currently recognized in the oral cavity.currently recognized in the oral cavity.  There is evidence that suppression orThere is evidence that suppression or eradication of these organisms results ineradication of these organisms results in an improvement in oral health and evenan improvement in oral health and even perhaps systemic health.perhaps systemic health. www.indiandentalacademy.com