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SULFONAMIDES OR SULFA DRUGS
GROUP OF MEDICINES USED IN TREATING BACTERIAL INFECTIONS
Short acting
(4-8 hrs)
• sulfadiazine
Intermediate acitng
(8-12 hrs)
• Sulfamethoxazole
Long acting (7 days)
• sulfadoxine
• sulfamethopyrazine
Special purpose
sulfonamides
• sulfacetamide
• Sulfadiazine
• Sulfasalazine
SULFONAMIDES ARE BACTERIOSTATIC
AGAINST GRAM POSITIVE AND GRAM
NEGATIVE BACTERIA
ABSORPTION: Rapidly absorbed orally
EXCRETION: Through Urine
PLASMA PROTEIN BINDING: 50%
USES: meningitis (it have a good
penetrability in brain and CSF)
DOSE: 500mg
ABSORPTION: slowly absorbed orally
EXCRETION: Through Urine
PLASMA PROTEIN BINDING: 50%
PLASMA HALF LIFE: 10hours in adults
USES: Malaria
DOSE: 500mg
ABSORPTION: ultra long acting absorbed
orally
EXCRETION: Through Urine
PLASMA PROTEIN BINDING: high
PLASMA HALF LIFE: 5-9days in adults
USES: Malaria
DOSE: 500mg
ABSORPTION: highly soluble, topical use
EXCRETION: -----
PLASMA PROTEIN BINDING:-----
PLASMA HALF LIFE: ----
USES: Ocular infection
DOSE: 10%, 20%, 30% eye drops, 6% eye oint
Hepatitis
Hypersensitive reactions
Bone marrow depression
Acute renal failure
Cyanosis
Nausea and Vomitting
Headache
Mental depression
Fixed drug combination of sulfonamides
(sulfomethoxazole) and trimethoprim is
Cotrimoxazole
Trimethoprim is a diaminopyrimidine
related to the antimalarial drug
pyrimethamine
It is a selective dihydrofolate
reductase inhibitor
ABSORPTION: Well absorbed orally and
distributed through out the tissues
EXCRETION: Urine
PLASMA HALF LIFE: 24 hrs
USES: Brain Meningitis (high concentration at
CSF)
DOSE: 200 mg, 500 mg
Nalidixic acid
1960’s
Urinary and GI
infections only
Low potency, restrcited
spectrum, high
frequency to bacterial
resistance
Fluoroquinolones
1980’s
Flourination at Position
6 and piperazine at
position 7 changes
made fluoroquinolones
High potency, expanded
spectrum, slow
development of
resistance, better tissue
penetration, and
tolerability
Classification of
fluoroquinolones
First
generation
(one fluoro
substitutions)
Second
generation
(two fluoro
substitutions)
ABSORPTION:rapidly absorbed orally, food
delays
DISTRIBUTION: good tissue penetration
EXCRETION: Urine
USES: UTI, Gonorrhoea, Bacterial
gastroenteritis, typhoid
DOSE: 250 mg, 500 mg
ADVERSE EFFECTS:
CNS: Dizziness, Headache, restlessness,
anxiety, insomnia etc.
GASTROINTESTINAL: Nausea and vomitting,
Diarrhoea
SKIN/HYPERSENSITIVITY: rash, urticaria,
swelling of lips, cutaneaous reactions
INTERACTIONS
• Plasma concentration of theophylline,
warfarin, caffiene is increased dur to
ciprofloxacin
• NSAIDS: seizures are reported
• Antacids, iron salts will reduce the absorption
rate of FQ’s
ABSORPTION: oral bioavailability is high,
higher plasma conc,
DISTRIBUTION: good tissue penetration
EXCRETION: unchanged in Urine (dose
reduced in renal failure )
USES: cervicitis, urethritis, pneumonia caused
by chlamydia trachomatis, TB,
DOSE: 100, 200, 400mg tab, 200mg/100ml inj
It is a active levo isomer of ofloxacin of first
generation
ABSORPTION: 100% oral bioavailability and
IV dose also, higher potency
DISTRIBUTION: good tissue penetration
EXCRETION: Urine unchanged
USES: sinusitis, prostatitis, UTI
DOSE: 500 mg, 750mg/ 100ml inj
It is a tissue amaebicidic category, it lies under the both
intestinal and extraintestinal amaebiasis
Examples:
• Metronidazole
• Tinidazole
• Secnidazole
• Ornidazole
• Satranidazole
It is a synthetic antiprotozoal and anti
bacterial agent
It belongs to the nitroimidazole class of drugs
MECHANISM OF ACTION:
Metronidazole acts by inhibiting nucleic acid synthesis by
disrupting the DNA of microbial cells
This function only occurs when metrondazole is partially
reduced and because this reduction usually happens only in
anaerobic cells, it has relatively little effect upon human
cells or aerobic cells
PHARMCOKINETICS
ABSORPTION: Bioavailability is 80% absorbed from GI tract
PLASMA PROTEIN BINDING: < 20%
PLASMA HALF LIFE: 1-2 HRS
DISTRIBUTION: Well distributed, similar pattern for IV
METABOLISM: lliver enzymes inhibited
EXCRETION: unchanged in Urine (77% and faeces 14%)
USES: Anaerobe infections, H pylori, Bacterial vaginosis,
amebiasis,giardiasis
DOSE: 250mg and 500 mg (also in the form of gels creams
capsules suspensions etc)
SIDE EFFECTS
Epigastric disorder
Seizures
Metallic taste
Darkening of urine
Peripheral neuropathy
Pancreatitis
Hepatitis
Fever
Reversible neutropenia
DRUG INTERACTION
ALCOHOL: nausea vomitting abdominal
cramps
ANTICOAGULANTS (WARFARIN): Prolonged PT
CIMETIDINE: Prolong half life and decreased
clearance of metronidazole
PHENYTOIN and
PHENOBARBITONE:
decreased serum conc and
increased metabolism of
metronidazole
Long plasma half life,
slower in metabolism
Higher cure rates in amoebiasis
Lower side effects
USES:
Tricho,
giardiasis,
Anaerobic infection
H pylori
Longest plasma half life i.e., 17-29 hrs
2 grams of single dose but for hepatic amoebiasis 1.5 gram
twice X5 days
Long plasma half life, similar to TInidazole
Better tolerability
No disulfiram raaction
No acetamide metabolite (weak carcinogen)
It contains Beta lactam ring in thier molecular structure so
called beta lactam antibiotics
Nitrogen is attached to the beta carbon relative to the
carbonyl ring and hence the name is called
CLASSIFICATION
 Penicillins
 Cephalosporins
 Other Beta lactam drugs:
• Cephamycins
•Carbapenems
•Oxacephalosporins
•Beta lactamase inhibitors
•Monolactams
CLASSIFICATION:
NATURAL: Penicillin G
SEMISYNTHETIc:
Acid Resistant: Penicillin V
Penicillinase-resistant: methicillin, cloxacillin
Aminopenicillin: Ampicillin, Amoxicillin, Bacampicillin
Antipseudomonal penicillin:
Carboxypenicillin: cerbenicillin, ticarcillin
Ureidopenicillins: piperacillin, mezlocillin
Beta lactumase inhibitors: clavulanic acid, sulbactam,
tazobactam
It is Penicillin G
Narrow spectrum antibiotic
Primarily is it for gram positive cocci, bacilli and few gram
negative
Absorption: good but food delays hence given after 2 hrs of
food
Cant cross BBB
Plasma half life is 30 min
Uses: meningococci
Enterococcci
Actinomyces
Effective against: gram positive+ less effective against
gram negative bacteria
• Narrow spectrum
•Should be given orally
USES:
Tonsillitis
Anthrax
Rheumatic fever
Streptococcal skin infections
Effective against gram positive + gram negative bacteria
It is broad spectrum and can be given orally and
parenterally
USES:
Ear infection
Sinusitis
UTI
Meningitis
Effective against gram postitive and negative
It has a broad spectrum
Orally and paranterally administrated
USES:
Skin infection
Sinusitis
UTI
Streptococcal pharyngitis
SIDE EFFECTS:
Rash, Vomitting and Nausea, edema, stomatitis, Diarrhea
Septicaemia
Pneumonia
Meningitis
Billiary tract infection
UTI
Sinusitis
Administered: orally but mostly prefered is IV and IM
Distribution: well distributed in the tissues
Only few like cefotaxime, cefuroxime, ceftriaxome will cross
the BBB,
Elimination: thorugh urine few like ceftraixome is eliminated
through bile
Hypersensitivity reactions
Diarrhea
Antibacterials- sulphonamides, cotrimoxazole, Quinolones and fluoroquinolones, nitroimidazoles, Beta lactam antibiotics

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Antibacterials- sulphonamides, cotrimoxazole, Quinolones and fluoroquinolones, nitroimidazoles, Beta lactam antibiotics

  • 1.
  • 2.
  • 3. SULFONAMIDES OR SULFA DRUGS GROUP OF MEDICINES USED IN TREATING BACTERIAL INFECTIONS
  • 4. Short acting (4-8 hrs) • sulfadiazine Intermediate acitng (8-12 hrs) • Sulfamethoxazole Long acting (7 days) • sulfadoxine • sulfamethopyrazine Special purpose sulfonamides • sulfacetamide • Sulfadiazine • Sulfasalazine
  • 5. SULFONAMIDES ARE BACTERIOSTATIC AGAINST GRAM POSITIVE AND GRAM NEGATIVE BACTERIA
  • 6.
  • 7. ABSORPTION: Rapidly absorbed orally EXCRETION: Through Urine PLASMA PROTEIN BINDING: 50% USES: meningitis (it have a good penetrability in brain and CSF) DOSE: 500mg
  • 8. ABSORPTION: slowly absorbed orally EXCRETION: Through Urine PLASMA PROTEIN BINDING: 50% PLASMA HALF LIFE: 10hours in adults USES: Malaria DOSE: 500mg
  • 9. ABSORPTION: ultra long acting absorbed orally EXCRETION: Through Urine PLASMA PROTEIN BINDING: high PLASMA HALF LIFE: 5-9days in adults USES: Malaria DOSE: 500mg
  • 10. ABSORPTION: highly soluble, topical use EXCRETION: ----- PLASMA PROTEIN BINDING:----- PLASMA HALF LIFE: ---- USES: Ocular infection DOSE: 10%, 20%, 30% eye drops, 6% eye oint
  • 11. Hepatitis Hypersensitive reactions Bone marrow depression Acute renal failure Cyanosis Nausea and Vomitting Headache Mental depression
  • 12.
  • 13. Fixed drug combination of sulfonamides (sulfomethoxazole) and trimethoprim is Cotrimoxazole
  • 14. Trimethoprim is a diaminopyrimidine related to the antimalarial drug pyrimethamine It is a selective dihydrofolate reductase inhibitor
  • 15. ABSORPTION: Well absorbed orally and distributed through out the tissues EXCRETION: Urine PLASMA HALF LIFE: 24 hrs USES: Brain Meningitis (high concentration at CSF) DOSE: 200 mg, 500 mg
  • 16.
  • 17.
  • 18. Nalidixic acid 1960’s Urinary and GI infections only Low potency, restrcited spectrum, high frequency to bacterial resistance Fluoroquinolones 1980’s Flourination at Position 6 and piperazine at position 7 changes made fluoroquinolones High potency, expanded spectrum, slow development of resistance, better tissue penetration, and tolerability
  • 20.
  • 21.
  • 22. ABSORPTION:rapidly absorbed orally, food delays DISTRIBUTION: good tissue penetration EXCRETION: Urine USES: UTI, Gonorrhoea, Bacterial gastroenteritis, typhoid DOSE: 250 mg, 500 mg
  • 23. ADVERSE EFFECTS: CNS: Dizziness, Headache, restlessness, anxiety, insomnia etc. GASTROINTESTINAL: Nausea and vomitting, Diarrhoea SKIN/HYPERSENSITIVITY: rash, urticaria, swelling of lips, cutaneaous reactions INTERACTIONS • Plasma concentration of theophylline, warfarin, caffiene is increased dur to ciprofloxacin • NSAIDS: seizures are reported • Antacids, iron salts will reduce the absorption rate of FQ’s
  • 24. ABSORPTION: oral bioavailability is high, higher plasma conc, DISTRIBUTION: good tissue penetration EXCRETION: unchanged in Urine (dose reduced in renal failure ) USES: cervicitis, urethritis, pneumonia caused by chlamydia trachomatis, TB, DOSE: 100, 200, 400mg tab, 200mg/100ml inj
  • 25. It is a active levo isomer of ofloxacin of first generation ABSORPTION: 100% oral bioavailability and IV dose also, higher potency DISTRIBUTION: good tissue penetration EXCRETION: Urine unchanged USES: sinusitis, prostatitis, UTI DOSE: 500 mg, 750mg/ 100ml inj
  • 26. It is a tissue amaebicidic category, it lies under the both intestinal and extraintestinal amaebiasis Examples: • Metronidazole • Tinidazole • Secnidazole • Ornidazole • Satranidazole
  • 27. It is a synthetic antiprotozoal and anti bacterial agent It belongs to the nitroimidazole class of drugs MECHANISM OF ACTION: Metronidazole acts by inhibiting nucleic acid synthesis by disrupting the DNA of microbial cells This function only occurs when metrondazole is partially reduced and because this reduction usually happens only in anaerobic cells, it has relatively little effect upon human cells or aerobic cells
  • 28.
  • 29. PHARMCOKINETICS ABSORPTION: Bioavailability is 80% absorbed from GI tract PLASMA PROTEIN BINDING: < 20% PLASMA HALF LIFE: 1-2 HRS DISTRIBUTION: Well distributed, similar pattern for IV METABOLISM: lliver enzymes inhibited EXCRETION: unchanged in Urine (77% and faeces 14%) USES: Anaerobe infections, H pylori, Bacterial vaginosis, amebiasis,giardiasis DOSE: 250mg and 500 mg (also in the form of gels creams capsules suspensions etc)
  • 30. SIDE EFFECTS Epigastric disorder Seizures Metallic taste Darkening of urine Peripheral neuropathy Pancreatitis Hepatitis Fever Reversible neutropenia
  • 31. DRUG INTERACTION ALCOHOL: nausea vomitting abdominal cramps ANTICOAGULANTS (WARFARIN): Prolonged PT CIMETIDINE: Prolong half life and decreased clearance of metronidazole PHENYTOIN and PHENOBARBITONE: decreased serum conc and increased metabolism of metronidazole
  • 32. Long plasma half life, slower in metabolism Higher cure rates in amoebiasis Lower side effects USES: Tricho, giardiasis, Anaerobic infection H pylori
  • 33. Longest plasma half life i.e., 17-29 hrs 2 grams of single dose but for hepatic amoebiasis 1.5 gram twice X5 days Long plasma half life, similar to TInidazole Better tolerability No disulfiram raaction No acetamide metabolite (weak carcinogen)
  • 34.
  • 35.
  • 36. It contains Beta lactam ring in thier molecular structure so called beta lactam antibiotics Nitrogen is attached to the beta carbon relative to the carbonyl ring and hence the name is called
  • 37. CLASSIFICATION  Penicillins  Cephalosporins  Other Beta lactam drugs: • Cephamycins •Carbapenems •Oxacephalosporins •Beta lactamase inhibitors •Monolactams
  • 38.
  • 39. CLASSIFICATION: NATURAL: Penicillin G SEMISYNTHETIc: Acid Resistant: Penicillin V Penicillinase-resistant: methicillin, cloxacillin Aminopenicillin: Ampicillin, Amoxicillin, Bacampicillin Antipseudomonal penicillin: Carboxypenicillin: cerbenicillin, ticarcillin Ureidopenicillins: piperacillin, mezlocillin Beta lactumase inhibitors: clavulanic acid, sulbactam, tazobactam
  • 40. It is Penicillin G Narrow spectrum antibiotic Primarily is it for gram positive cocci, bacilli and few gram negative Absorption: good but food delays hence given after 2 hrs of food Cant cross BBB Plasma half life is 30 min Uses: meningococci Enterococcci Actinomyces
  • 41. Effective against: gram positive+ less effective against gram negative bacteria • Narrow spectrum •Should be given orally USES: Tonsillitis Anthrax Rheumatic fever Streptococcal skin infections
  • 42. Effective against gram positive + gram negative bacteria It is broad spectrum and can be given orally and parenterally USES: Ear infection Sinusitis UTI Meningitis
  • 43. Effective against gram postitive and negative It has a broad spectrum Orally and paranterally administrated USES: Skin infection Sinusitis UTI Streptococcal pharyngitis SIDE EFFECTS: Rash, Vomitting and Nausea, edema, stomatitis, Diarrhea
  • 44.
  • 46. Administered: orally but mostly prefered is IV and IM Distribution: well distributed in the tissues Only few like cefotaxime, cefuroxime, ceftriaxome will cross the BBB, Elimination: thorugh urine few like ceftraixome is eliminated through bile