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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
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Harrison's Principles of Internal Medicine, 13th ed.
Companion Handbook. Isselbacher et al (eds),
McGraw-Hill Inc. NY, 1995, pg 165
- Sanford Guide to antimicrobial therapy 1997, 2001
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Medical Knowledge Self Assessment Program (MKSAP) 11, 19.
American College of Physicians, Philadelphia 1998, 2021
- Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed.,
W.B. Saunders, 1995
- Prescriber's Letter 13(3): 2006
Cytochrome P450 drug interactions
Detail-Document#: 220233
(subscription needed) http://www.prescribersletter.com
- Prescriber's Letter 11(5):29 2004
Detail-Document#: 200506
(subscription needed) http://www.prescribersletter.com
- Stratta P et al,
Ciprofloxcin crystal nephropathy.
Am J Kidney Dis 2007, 50:330
PMID: 17660035
- Deprecated Reference
- 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