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Organic Name Reactions for the students and aspirants of Chemistry12th.pptx
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
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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.
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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
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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.
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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.
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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.
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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.
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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.
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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 .
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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
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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
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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.
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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
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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
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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
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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
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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
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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
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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
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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
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33. 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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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
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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
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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
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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
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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
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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
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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.
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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 .
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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
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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
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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
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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.
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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.
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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
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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.
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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.
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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.
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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.
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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.
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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.
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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
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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.
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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.
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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
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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.
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