Podcast
Questions and Answers
What is the primary indication for the use of Nalidixic acid?
What is the primary indication for the use of Nalidixic acid?
- Bone infections
- Skin infections
- Pneumonia
- Urinary tract infections (correct)
Why are quinolones not recommended for use during pregnancy?
Why are quinolones not recommended for use during pregnancy?
- Unknown reasons
- Increased risk of allergy
- Risk of fetal toxicity (correct)
- Inefficient in placental barrier
What is the primary mechanism of action of Sulphonamide and Trimethoprim combination?
What is the primary mechanism of action of Sulphonamide and Trimethoprim combination?
- Inhibiting cell wall synthesis
- Inhibiting DNA synthesis
- Inhibiting protein synthesis
- Inhibiting folic acid synthesis (correct)
Which of the following is NOT a 3rd generation fluoroquinolone?
Which of the following is NOT a 3rd generation fluoroquinolone?
What is the primary indication for the use of Rifampicin?
What is the primary indication for the use of Rifampicin?
Why are some antibiotics restricted in pregnancy and specific ages?
Why are some antibiotics restricted in pregnancy and specific ages?
What is the primary mechanism of action of Moxifloxacin?
What is the primary mechanism of action of Moxifloxacin?
Which of the following is an anaerobic antibiotic?
Which of the following is an anaerobic antibiotic?
What is the primary mechanism by which sulfa drugs are eliminated?
What is the primary mechanism by which sulfa drugs are eliminated?
What is the cause of crystalluria in patients taking sulfa drugs?
What is the cause of crystalluria in patients taking sulfa drugs?
What is the risk of kernicterus in newborns associated with?
What is the risk of kernicterus in newborns associated with?
What is the mechanism of enzyme induction caused by rifampicin?
What is the mechanism of enzyme induction caused by rifampicin?
What is the common adverse effect of metronidazole?
What is the common adverse effect of metronidazole?
What is the primary use of cotrimoxazole?
What is the primary use of cotrimoxazole?
What is the consequence of sulfonamide use in infants < 2 months of age?
What is the consequence of sulfonamide use in infants < 2 months of age?
What is the adverse effect of trimethoprim that is related to folic acid?
What is the adverse effect of trimethoprim that is related to folic acid?
What is the primary mechanism by which fluoroquinolones are absorbed?
What is the primary mechanism by which fluoroquinolones are absorbed?
Which of the following organisms is sensitive to levofloxacin?
Which of the following organisms is sensitive to levofloxacin?
What is the primary route of elimination for most fluoroquinolones?
What is the primary route of elimination for most fluoroquinolones?
What is a contraindication for the use of Moxifloxacin?
What is a contraindication for the use of Moxifloxacin?
What is the primary adverse effect of fluoroquinolones on the central nervous system?
What is the primary adverse effect of fluoroquinolones on the central nervous system?
What is the primary indication for the use of sulfonamides in inflammatory bowel disease?
What is the primary indication for the use of sulfonamides in inflammatory bowel disease?
What is a characteristic of fluoroquinolones that makes them effective against intracellular organisms?
What is a characteristic of fluoroquinolones that makes them effective against intracellular organisms?
What is the primary reason why fluoroquinolones are avoided in children under 18 years of age?
What is the primary reason why fluoroquinolones are avoided in children under 18 years of age?
Study Notes
Pharmacokinetics of Sulfonamides
- Well absorbed
- Penetrate well into cerebrospinal fluid and placental barrier, entering fetal tissues
- Metabolized in the liver through acetylation (metabolites are insoluble in acidic urine → Crystalluria)
- Eliminated by glomerular filtration
Adverse Effects of Sulfonamides
- Crystalluria and nephrotoxicity (↓ by adequate hydration and alkalinization of urine)
- Hypersensitivity: rashes, angioedema, and Stevens-Johnson syndrome
- Hemopoietic disturbances: Hemolytic anemia in patients with G6PD deficiency, leucopenia, and thrombocytopenia
- Kernicterus in newborns: displace bilirubin from binding sites on serum albumin
Contraindications of Sulfonamides
- Infants < 2 months of age
- Pregnant women
Trimethoprim
- Adverse effects: Folic acid deficiency, megaloblastic anemia, and leukopenia
Cotrimoxazole
- Combination of sulfamethoxazole and Trimethoprim (ratio 5:1)
- Bactericidal and broad-spectrum
- Antibacterial spectrum: Urinary and Respiratory Tract Infections, Systemic salmonella infections (Typhoid fever)
- Adverse effects: Sulfa and TMP
- Drug interactions: Sulfonamide ↑ free level of warfarin and Methotrexate (Transistent potentiation)
Rifampicin (Rifampin)
- Antimicrobial spectrum and uses: T.B. prophylaxis against meningitis
- Adverse effects: Red discoloration of urine, tears, and contact lenses, enzyme induction (serious drug interactions), flu-like syndrome, and hepatotoxicity
Metronidazole (Flagyl)
- Uses: Anaerobic protozoal infections (Amebiasis, Giardiasis, Trichomoniasis), Anaerobic bacterial infections (Pseudomembranous colitis due to clostridium difficile), and dental infections
- Adverse effects:
- GIT: unpleasant metallic taste, stomatitis, nausea, and vomiting
- BMS161:
Quinolones
- 1st generation: Nalidixic acid (used as urinary antiseptic)
- 2nd generation: Norfloxacin (UTI)
- 3rd generation: Levofloxacin (Respiratory FQ, Gram +ve Cocci, Staph)
- 4th generation: Moxifloxacin (Anaerobic, Clinafloxacin)
- Pharmacokinetics:
- Absorption: ↓ Absorption with antacids (Al, Mg) or dietary supplements (Zn & Ca)
- Distribution: High levels in bone, urine, kidney, prostatic tissue, and lung; penetrate into cerebrospinal fluid (except for ofloxacin); accumulate in macrophages
- Elimination: Excreted by renal route (except Moxifloxacin, which is excreted by liver)
- Adverse reactions:
- GIT: nausea, vomiting, and diarrhea
- CNS: Headache, dizziness (use cautiously in epilepsy)
- Phototoxicity, Connective tissue problems: Arthropathy and ruptured tendon in adults
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Description
This quiz covers the absorption, distribution, metabolism, and excretion of sulfa drugs, as well as their adverse effects, including crystalluria and hypersensitivity reactions.
