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Antibiotics
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Ciprofloxacin
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Ciprofloxacin
Doxycycline
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Ciprofloxacin (Cipro) 500 mg, 750 mg


  • Generic name: Ciprofloxacin hydrochloride
  • Trade names: Cipro, Ciprobay, Ciproxin, Ciproxine, Ciflox, Proquin
  • Dosages:
    Tablets 250 mg, 500 mg, 750 mg
    Powder for oral suspension 250 mg/5 mL (5%) (when reconstituted); 500 mg/5 mL (10%) (when reconstituted)
    Tablets, extended-release 500 mg, 1000 mg
    Injection (premixed) 200 mg, 400 mg; Injection (concentrate) 10 mg/mL
  • Pharmacologic category: Fluoroquinolone antibiotic, RX only
  • FDA approved: October 22, 1987
  • Pregnancy risk factor: C

Medical uses

Ciprofloxacin is a a fluoroquinolone antibiotic active against a broad range of bacteria. It is marketed by Bayer under the brand name Cipro®.

Ciprofloxacin indicated uses include:

  • Urinary tract infections: urethritis, cystitis, pyelonephritis.
  • Acute uncomplicated cystitis in women.
  • Chronic bacterial prostatitis.
  • Lower respiratory infections (but not pneumococcal): pneumonia, bronchitis, tracheobronchitis.
  • Acute sinusitis.
  • Skin, soft tissue and wound infections.
  • Bone and joint infections.
  • Complicated intra-abdominal infections (used in combination with metronidazole).
  • Foodborne diseases and iInfectious diarrhea: Escherichia coli infection, campylobacteriosis, salmonellosis, shigellosis, cystoisosporiasis (off-label).
  • Typhoid fever (enteric fever).
  • STDs: gonorrhea, chancroid
  • Complicated UTIs and pyelonephritis in children (1 to 17 years of age).
  • Post-exposure prophylaxis of anthrax (in adults and children).

Pharmacological characteristics

  • Absorption: Rapid (50% to 85%).
  • Metabolism: Partially hepatic; forms 4 metabolites.
  • Elimination half-life: 3-5 hours.
  • Excretion: Urine (30% to 50% as unchanged drug); feces (15% to 43%).

Ciprofloxacin for Urinary Tract Infections

Antibiotics are the mainstay treatment for complicated and uncomplicated urinary tract infections (UTIs). The choice of antibiotic and length of treatment depend on the patient's history and the urine tests that identify the offending bacteria. The sensitivity test is especially useful in helping select the most effective medication.

Escherichia coli is the leading cause of UTIs, followed by Staphylococcus saprophyticus, Proteus spp., and Klebsiella spp.

Fluoroquinolones are the standard alternatives to Sulfonamides (TMP-SMX), and sometimes are preferred antibacterials for UTI.

Ciprofloxacin is frequently used to treat urinary infections because of its excellent activity against majority of urinary tract pathogenic bacteria, and particularly E. coli. In fact, ciprofloxacin urinary concentrations are 10-50 fold higher than plasma. Ciprofloxacin is widely used in the areas with the high rates of bacterial resistance to TMP-SMX.

Effectiveness:
Ciprofloxacin has a success rate of about 90-96% in eradicating bacteriuria16.

Dosage for Urinary Tract Infections:

Acute uncomplicated cystitis (simple bladder infection): the recommended dosage is 250 mg twice daily for 3 days. In severe condition the duration of therapy is extended up to 7-10 days. Seven-day regimen is recommended for older women4.

Prophylaxis regimen for women with recurrent UTIs: 125 mg taken after intercourse10.

Uncomplicated pyelonephritis (kidney infection) in adults: the recommended ciprofloxacin dosage is 500-750 mg twice daily for 7-14 days.

Benefits

  • Convenient twice daily dosing regimen.
  • Rapid bactericidal activity.
  • Broad spectrum of antimicrobial activity.
  • Does not cause a significant QT interval prolongation 14.
  • Very effective antibiotic against aerobic gram-negative bacteria, particularly against P. aeruginosa (bacteria that causes infections of the pulmonary tract, external ear, urinary tract, burns, and wounds)
  • Low cost due to generic availability.

Concerns

  • Tendon rupture, tendonitis and arthropathies. Tendon injury may occur several months after antibiotic has been discontinued. About 95% of cases of fluoroquinolone-associated tendinitis/rupture involve the Achilles tendon 17. Damage of quadriceps, peroneus brevis, and rotator cuff has also been reported.
  • Peripheral neuropathy (nerve damage)18. The symptoms of neuropathy include pain, numbness, burning, tingling, weakness, impaired muscle coordination. If a person develops symptoms of nerve damage ciprofloxacin should be stopped immediately in order to prevent the irreversible damage.
  • Poor activity against Streptococcus pneumoniae - a major cause of pneumonia and meningitis.
  • Ciprofloxacin absorption may be greatly reduced by dairy products. Ciprofloxacin should not be taken with milk or calcium-fortified juices alone. However, it may be taken with a meal that contains dairy products (eg. cereal with milk).
  • Serious drug interactions with theophylline, propranolol, warfarin, tizanidine and some antipsychotic medications.
  • Overuse and inappropriate prescribing of Ciprofloxacin has lead to increasing rates of bacterial resistance.
  • May retard the fracture healing 1.

Unlabeled uses

  • Chlamydia 11. Ciprofloxacin is a poor choice for Chlamydia. Although ciprofloxacin has good activity against Chlamydia in test tubes, in practice it is insufficient for the treatment of chlamydia and often results in relapsing infection.
  • Gynecological infections (pelvic inflammatory disease, post-partum endometritis, cervicitis, salpingitis, tubo-ovarian abscess) 12, 13. Ciprofloxacin not always provides optimal effective treatment for pelvic inflammatory disease if used alone.
  • Cystic fibrosis 6. Ciprofloxacin is effective and well-tolerated maintenance antipseudomonal antibiotic in cystic fibrosis due to its high activity against P. aeruginosa infection.
  • Cat-scratch disease 2. This benign infectious disease caused by the intracellular parasite Bartonella usually resolves spontaneously and does not require antibiotic. In more serious cases treatment with ciprofloxacin is effective.
  • Brucellosis 3-5. Brucellosis is an infectious disease transmitted from animals to humans. Despite ciprofloxacin is highly active in test tube against Brucella, it does not provide optimal treatment for acute brucellosis and should be used in combination with other antibacterials.
  • Tuberculosis 7-8. Ciprofloxacin is a second-line choice for tuberculosis in persons who cannot use conventional anti-tuberculosis medications or for drug-resistant tuberculosis.
  • Chronic ear disease (chronic suppurative otitis media) 9.

Mode of action

Ciprofloxacin is a synthetic, broad-spectrum antibacterial that inhibits (prevents the activity) DNA gyrase and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription, and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division.

Discussion Boards & Forums

References

  • 1. Tuncay I, Ozbek H, Köşem M, Unal O. A comparison of effects of fluoroquinolones on fracture healing. Ulus Travma Acil Cerrahi Derg. 2005 Jan;11(1):17-22.
  • 2. Windsor JJ. Cat-scratch disease: epidemiology, aetiology and treatment. Br J Biomed Sci. 2001;58(2):101-10.
  • 3. Lopez-Merino A, Contreras-Rodri'guez A, Migranas-Ortiz R, et al. Susceptibility of Mexican brucella isolates to moxifloxacin, ciprofloxacin and other antimicrobials used in human brucellosis. Scand J Infect Dis. 2004;36(9):636-8.
  • 4. Warren JW, Abrutyn E, Hebel JR, Johnson JR, Schaeffer AJ, Stamm WE. IDSA. Guidelines for antimicrobial treatment of uncomplicated acute bacterial cystitis and acute pyelonephritis in women. Clin Infect Dis. 1999;29:745–58.
  • 5. Lang R, Raz R, Sacks T, Shapiro M. Ciprofloxacin failure in acute infections due to Brucella melitensis. J Antimicrob Chemother. 1990 Dec;26(6):841-6.
  • 6. Schaad UB, Wedgwood J, Ruedeberg A, Kraemer R, Hampel B. Ciprofloxacin as antipseudomonal quinolone in cystic fibrosis. Pediatr Infect Dis J. 1997 Jan;16(1):106-11; discussion 123-6. PubMed
  • 7. Kahana LM, Spino M. DICP. 1991 Sep;25(9):919-24.
  • 8. Yang CK, Lin HC, Lee KY, Lin SM, Yu CT, Kuo HP. The effects of ciprofloxacin on chest radiographic regression in patients with drug intolerance or resistant tuberculosis. Chang Gung Med J. 2004 Apr;27(4):292-9.
  • 9. Legent F, Bordure P, Beauvillain C, Berche P. Chemotherapy. 1994;40 Suppl 1:16-23.
  • 10. Melekos MD, Asbach HW, Gerharz E, et al. Post-intercourse versus daily ciprofloxacin prophylaxis for recurrent urinary tract infections in premenopausal women. J Urol. 1997 Mar;157(3):935-9.
  • 11. Fong IW, Linton W, Simbul M, Thorup R, McLaughlin B, Rahm, Quinn PA. Ciprofloxacin in nongonococcal urethritis. Am J Med. 1987 Apr 27;82(4A):311-6. PubMed
  • 12. Maccato ML, Faro S, Martens, Hammill HA. Ciprofloxacin versus gentamicin/clindamycin for postpartum endometritis. J Reprod Med. 1991 Dec;36(12):857-61.
  • 13. Crombleholme WR, Schachter J, Ohm-Smith M, Luft J, Whidden R, Sweet RL. Efficacy of ciprofloxacin for acute pelvic inflammatory disease. Am J Med. 1989 Nov 30;87(5A):142S-147S. PubMed
  • 14. Makaryus AN, Byrns K, Makaryus MN, Natarajan U, Singer C, Goldner B. South Med J. 2006 Jan;99(1):52-6.
  • 16. Hooton TM, Roberts PL, Stapleton AE. Cefpodoxime vs ciprofloxacin for short-course treatment of acute uncomplicated cystitis: a randomized trial. JAMA. 2012 Feb 8;307(6):583-9. PubMed
  • 17. Kim GK. The Risk of Fluoroquinolone-induced Tendinopathy and Tendon Rupture. J Clin Aesthet Dermatol. 2010 Apr;3(4):49-54.
  • 18. Ali AK. Peripheral neuropathy and Guillain-Barré syndrome risks associated with exposure to systemic fluoroquinolones. Ann Epidemiol. 2014 Apr;24(4):279-85.

Written by HealthyStock.net, October 2009.
Last updated: June, 2015

Interesting facts

Ciprofloxacin

  • Ciprofloxacin is the fluoroquinolone most studied in children, mostly when used to treat pulmonary exacerbations of cystic fibrosis (CF).

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