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ciprofloxacin (Cipro, Ciloxan)

Tradename: Cipro. (ciprofloxacin HCl) Indications: - adjunctive treatment of moderate to severe bacterial infections caused by susceptible gram positive & gram negative organisms - as a single agent in urinary tract infections for adults & children [9] - single dose treatment of gonorrhea - chancroid [11] - lower respiratory tract infections - pneumonia - nosocomial pneumonia - ventilator-associated pneumonia - inhalation anthrax [9] - intra-abdominal infections - gastrointestinal infections - gastroenteritis, diverticulitis, abdominal abscess - traveler's diarrhea, infectious diarrhea, typhoid fever - bacterial peritonitis - skin or soft tissue infection - diabetic foot infection - cutaneous anthrax [11] - infectious arthritis, osteomyelitis [11] - otitis externa (otic) - eye infection due to corneal ulcer (ophthalmic) - ciprofloxacin & ofloxacin are used in multidrug regimens for treatment of drug-resistant Mycobacterium tuberculosis - empiric treatment of febrile neutropenia Contraindications: - anaerobic & Streptococcal infections - poor coverage Dosage: 200-400 mg IV every 12 hours - 250-750 mg PO BID. - Gonorrhea: 250-500 mg PO single dose. Tabs: 250, 500, 750 mg. Ophthalmic agent: Tradename: Ciloxan 1) bacterial keratitis 2) bacterial conjunctivitis 1 drop every 1-6 hours, 0.35% Pharmacokinetics: 1) oral route achieves similar concentration to parenteral route 2) highly concentrated in urine, prostate & lungs 3) most of drug is eliminated in the urine 4) 1/2life is 4-5 hours (6-9 hours with ESRD) Dosage adjustment in renal failure: Creatinine clearance dose > 50 mL/min 500-750 mg every 12 hours 30-49 mL/min 500 mg every 12 hours 10-29 mL/min 500-750 mg every 24 hours < 10 mL/min 500 mg every 24 hours hemodialysis 200 mg every 12 hours Antimicrobial activity: Gram positive - Streptococcus pneumonia (+/-) - Staphylococcus aureus (MSSA) - Staphylococcus epidermidis - Listeria monocytogenes Gram negative - Neisseria gonorrhoeae - Neisseria meningitidis - Moraxella catarrhalis - Haemophilus influenzae - Haemophilus parainfluenzae - Escherichia coli# - Klebsiella species - Enterobacter species - Serratia species - Salmonella species - Shigella species - Proteus mirabilis - Proteus vulgaris - Providencia species - Morganella species - Morganella morganii - Citrobacter species - Aeromonas species - Acinetobacter species - Pseudomonas aeruginosa* - Yersinia enterocolitica - Legionella species - Pasteurella multocida - Campylobacter [11] Atypical bacteria - Mycoplasma pneumonia Anaerobes - Clostridium species (+/-) - Peptostreptococcus species (+/-) - Bacterioides [11] *Among the quinolones, ciprofloxacin has the best activity against Pseudomonas aeruginosa. # 20% of healthy women delivering twins are colonized with ciprofloxacin resistant E coli - antibiotic exposure not identified as risk factor for colonization [12] Adverse effects: 1) most common (1-10%) - nausea/vomiting - diarrhea - abdominal pain - headache - restlessness - rash 2) uncommon (< 1%) - tremor, dizziness, confusion, seizures, anemia, increased serum transaminases, arthralgia, acute renal failure, photosensitivity, allergic reactions (rare) 3) Do not use in children & pregnant women because of effects on cartilage 4) dose-related neurotoxicity in elderly, especially parenteral administration 5) ophthalmic agent - white granular or crystalline precipitate superficially on corneal defect (17% of patients with bacterial keratitis) does NOT warrant discontinuation of therapy - ocular irritation (10%) - taste abnormality (5%) 6) crystal nephropathy, especially in the elderly [9] 6) QT prolongation [] Drug interactions: 1) absorption decreased 30-60% when administered concurrently with antacids, sucralfate, Mg+2, Ca+2, Fe+2, Zn+2 or Al+3-containing products, including enteral & vitamin/mineral formulas; - administer ciprofloxacin 2 hours before or afterwards 2) ciprofloxacin decreases metabolism of theophylline 3) didanosine (ddI) reduces ciprofloxacin levels; administer ciprofloxacin 2 hours before or afterwards 4) probenecid decreases renal clearance of ciprofloxacin 5) ciprofloxacin may increase prothrombin time in patients receiving warfarin 6) ciprofloxacin inhibits cyt P450 1A2 - may increase levels of drugs metabolized by cyt P450 1A2 7) see fluoroquinolone Laboratory: 1) specimen: a) serum, urine b) stable for 20 weeks at -20 degrees C 2) methods: HPLC, bioassay 3) interferences: - presence of other antimicrobial agents may interfere with bioassay Mechanism of action: concentration-dependent, bactericidal, inhibitor of DNA gyrase

Interactions

drug interactions drug adverse effects of fluoroquinolones

Related

cytochrome p450 1A2 (cytochrome P3-450, phenacetin deethylase, cytochrome p450-4, CYP1A2)

Specific

Ciprofloxacin Ophthalmic

General

fluoroquinolone

Properties

INHIBITS: DNA gyrase MISC-INFO: elimination route KIDNEY LIVER 1/2life 3-5 HOURS protein-binding 30% elimination by hemodialysis - peritoneal dialysis - pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Harrison's Principles of Internal Medicine, 13th ed. Companion Handbook. Isselbacher et al (eds), McGraw-Hill Inc. NY, 1995, pg 165
  3. Sanford Guide to antimicrobial therapy 1997, 2001
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  6. Medical Knowledge Self Assessment Program (MKSAP) 11, 19. American College of Physicians, Philadelphia 1998, 2021
  7. Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
  8. Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: 220233 (subscription needed) http://www.prescribersletter.com
  9. Prescriber's Letter 11(5):29 2004 Detail-Document#: 200506 (subscription needed) http://www.prescribersletter.com
  10. Stratta P et al, Ciprofloxcin crystal nephropathy. Am J Kidney Dis 2007, 50:330 PMID: 17660035
  11. Deprecated Reference
  12. Gurnee EA et al. Gut colonization of healthy children and their mothers with pathogenic ciprofloxacin-resistant Escherichia coli. J Infect Dis 2015 Dec 15; 212:1862 PMID: 25969564 http://jid.oxfordjournals.org/content/212/12/1862 - Spellberg B, Doi Y. The rise of fluoroquinolone-resistant Escherichia coli in the community: Scarier than we thought. J Infect Dis 2015 Dec 15; 212:1853 PMID: 25969562 http://jid.oxfordjournals.org/content/212/12/1853

Component-of

ciprofloxacin/cortisol (Cipro HC) ciprofloxacin/dexamethasone