Ciprofloxacin Overview Summary of Information from Provided Images
Ciprofloxacin Overview - Most potent first-generation fluoroquinolone (FQ) - Active against a broad range of bacteria - MIC: < 0.1 µg/ml for highly susceptible bacteria - Inhibits bacterial DNA gyrase, introducing negative supercoils
Highly Susceptible Bacteria Gram-negative: - E. coli - K. pneumoniae - Enterobacter - H. influenzae - Neisseria gonorrhoeae - N. meningitidis Gram-positive: - Inhibited at relatively higher concentrations
Mechanism of Action - Inhibits bacterial DNA gyrase - Consists of two A and two B subunits - A subunit: nicking of DNA and introducing negative supercoils - B subunit: reseals the strands - Prevents excessive positive supercoiling - In gram-positive bacteria: targets enzyme topoisomerase IV
Pharmacokinetics - Rapidly absorbed orally, food delays absorption - Good tissue penetration - Excreted primarily in urine - Urinary and biliary concentrations are 10-50 fold higher than plasma
Adverse Effects - Occur in ~10% of patients, generally mild - Withdrawal needed only in 1.5% of cases - Gastrointestinal: nausea, vomiting, bad taste, anorexia - CNS: dizziness, headache, restlessness, anxiety, insomnia - Skin/Hypersensitivity: rash, pruritus, photosensitivity, urticaria - Musculoskeletal: tendonitis and tendon rupture - Contraindicated in children and during pregnancy
Interactions - Inhibition of metabolism: can lead to CNS toxicity with theophylline - NSAIDs: may enhance CNS toxicity - Antacids, sucralfate, iron salts: reduce absorption
Uses - Effective against a wide range of infections - Used for empirical therapy - Reserved for serious infections Specific Infections: - UTIs: high cure rates - Gonorrhea: initially effective, now less reliable - Chancroid: effective in some cases - Bacterial Gastroenteritis: for moderate-to-severe cases - Typhoid Fever: recommended for resistant S. typhi strains