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Look Up > Drugs > Ciprofloxacin
Ciprofloxacin
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Monitoring Parameters
Reference Range
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(sip roe FLOKS a sin)

U.S. Brand Names
Ciloxan™ Ophthalmic; Cipro® Injection; Cipro® Oral

Generic Available

No


Synonyms
Ciprofloxacin Hydrochloride

Pharmacological Index

Antibiotic, Ophthalmic; Antibiotic, Quinolone


Use

Dental: Useful as a single agent or in combination with metronidazole in the treatment of periodontitis associated with the presence of Actinobacillus actinomycetemcomitans (AA), as well as enteric rods/pseudomonads

Medical: Treatment of documented or suspected infections of the lower respiratory tract, sinuses, skin and skin structure, bone/joints, and urinary tract including prostatitis, due to susceptible bacterial strains; especially indicated for Pseudomonal infections and those due to multidrug resistant gram-negative organisms, chronic bacterial prostatitis, infectious diarrhea, complicated gram-negative and anaerobic intra-abdominal infections (with metronidazole) due to E. coli (enteropathic strains), B. fragilis, P. mirabilis, K. pneumoniae, P. aeruginosa, Campylobacter jejuni or Shigella; approved for acute sinusitis caused by H. influenzae or M. catarrhalis; also used to treat typhoid fever due to Salmonella typhi (although eradication of the chronic typhoid carrier state has not been proven), osteomyelitis when parenteral therapy is not feasible, and sexually transmitted diseases such as uncomplicated cervical and urethral gonorrhea due to Neisseria gonorrhoeae; used ophthalmologically for superficial ocular infections (corneal ulcers, conjunctivitis) due to susceptible strains


Pregnancy Risk Factor

C


Contraindications

Hypersensitivity to ciprofloxacin, any component or other quinolones


Warnings/Precautions

Not recommended in children <18 years of age; has caused transient arthropathy in children; CNS stimulation may occur (tremor, restlessness, confusion, and very rarely hallucinations or seizures); use with caution in patients with known or suspected CNS disorder; green discoloration of teeth in newborns has been reported; prolonged use may result in superinfection; may rarely cause inflamed or ruptured tendons (discontinue use immediately with signs of inflammation or tendon pain)


Adverse Reactions

1% to 10%:

Central nervous system: Headache, restlessness

Gastrointestinal: Nausea, diarrhea, vomiting, abdominal pain

Dermatologic: Rash

<1%: Dizziness, confusion, seizures, anemia, increased liver enzymes, tremor, arthralgia, ruptured tendons, acute renal failure


Overdosage/Toxicology

Symptoms of overdose include acute renal failure, seizures

GI decontamination and supportive care; not removed by peritoneal or hemodialysis


Drug Interactions

CYP1A2 enzyme inhibitor

Enteral feedings may decrease plasma concentrations of ciprofloxacin probably by >30% inhibition of absorption. Ciprofloxacin should not be administered with enteral feedings. The feeding would need to be discontinued for 1-2 hours prior to and after ciprofloxacin administration. Nasogastric administration produces a greater loss of ciprofloxacin bioavailability than does nasoduodenal administration.

Aluminum/magnesium products, didanosine, and sucralfate may decrease absorption of ciprofloxacin by greater than or equal to 90% if administered concurrently

RECOMMENDATION: Administer ciprofloxacin 2 hours before dose OR administer ciprofloxacin at least 4 hours and preferably 6 hours after the dose of these agents OR change to an H2-antagonist or omeprazole

Calcium, iron, zinc, and multivitamins with minerals products may decrease absorption of ciprofloxacin significantly if administered concurrently

RECOMMENDATION: Administer ciprofloxacin 2 hours before dose OR administer ciprofloxacin at least 2 hours after the dose of these agents

Increased toxicity:

Caffeine and theophylline CNS stimulation when concurrent with ciprofloxacin

Cyclosporine may increase serum creatinine levels


Stability

Refrigeration and room temperature: Prepared bags: 14 days; Premixed bags: Manufacturer expiration dating


Mechanism of Action

Inhibits DNA-gyrase in susceptible organisms; inhibits relaxation of supercoiled DNA and promotes breakage of double-stranded DNA


Pharmacodynamics/Kinetics

Absorption: Oral: Rapid from GI tract (~50% to 85%)

Distribution: Crosses the placenta; appears in breast milk; distributes widely throughout body; tissue concentrations often exceed serum concentrations especially in the kidneys, gallbladder, liver, lungs, gynecological tissue, and prostatic tissue; CSF concentrations reach 10% with noninflamed meninges and 14% to 37% with inflamed meninges

Protein binding: 16% to 43%

Metabolism: Partially metabolized in the liver

Half-life: Children: 2.5 hours; Adults with normal renal function: 3-5 hours

Time to peak: Oral: Tmax: 0.5-2 hours

Elimination: 30% to 50% excreted as unchanged drug in urine; 20% to 40% of dose excreted in feces primarily from biliary excretion


Usual Dosage

Children (see Warnings/Precautions):

Oral: 20-30 mg/kg/day in 2 divided doses; maximum: 1.5 g/day

Cystic fibrosis: 20-40 mg/kg/day divided every 12 hours

I.V.: 15-20 mg/kg/day divided every 12 hours

Cystic fibrosis: 15-30 mg/kg/day divided every 8-12 hours

Adults: Oral:

Urinary tract infection: 250-500 mg every 12 hours for 7-10 days, depending on severity of infection and susceptibility; (3 investigations (n=975) indicate the minimum effective dose for women with acute, uncomplicated urinary tract infection may be 100 mg twice daily for 3 days)

Lower respiratory tract, skin/skin structure infections: 500-750 mg twice daily for 7-14 days depending on severity and susceptibility

Bone/joint infections: 500-750 mg twice daily for 4-6 weeks, depending on severity and susceptibility

Infectious diarrhea: 500 mg every 12 hours for 5-7 days

Typhoid fever: 500 mg every 12 hours for 10 days

Urethral/cervical gonococcal infections: 250-500 mg as a single dose (CDC recommends concomitant doxycycline or azithromycin due to developing resistance; avoid use in Asian or Western Pacific travelers)

Disseminated gonococcal infection: 500 mg twice daily to complete 7 days of therapy (initial treatment with ceftriaxone 1 g I.M./I.V. daily for 24-48 hours after improvement begins)

Chancroid: 500 mg twice daily for 3 days

Mild to moderate sinusitis: 500 mg every 12 hours for 10 days

Adults: I.V.

Urinary tract infection: 200-400 mg every 12 hours for 7-10 days

Lower respiratory tract, skin/skin structure infection (mild to moderate): 400 mg every 12 hours for 7-14 days

Ophthalmic: Instill 1-2 drops in eye(s) every 2 hours while awake for 2 days and 1-2 drops every 4 hours while awake for the next 5 days

Dosing adjustment in renal impairment:

Clcr <30 mL/minute:

500 mg every 24 hours or

750 mg every 24 hours

Dialysis: Only small amounts of ciprofloxacin are removed by hemo- or peritoneal dialysis (<10%); usual dose: 250-500 mg every 24 hours following dialysis

Continuous arteriovenous or venovenous hemodiafiltration (CAVH) effects: Administer 200-400 mg I.V. every 12 hours


Dietary Considerations

Food: Decreases rate, but not extent, of absorption. Drug may cause GI upset; take without regard to meals (manufacturer prefers that drug is taken 2 hours after meals)

Dairy products, oral multivitamins, and mineral supplements: Absorption decreased by divalent and trivalent cations. These cations bind to and form insoluble complexes with quinolones. Avoid taking these substrates with ciprofloxacin. The manufacturer states that the usual dietary intake of calcium has not been shown to interfere with ciprofloxacin absorption.

Caffeine: Possible exaggerated or prolonged effects of caffeine. Ciprofloxacin reduces total body clearance of caffeine. Patients consuming regular large quantities of caffeinated beverages may need to restrict caffeine intake if excessive cardiac or CNS stimulation occurs.


Monitoring Parameters

Patients receiving concurrent ciprofloxacin, theophylline, or cyclosporine should have serum levels monitored


Reference Range

Therapeutic: 2.6-3 mg/mL; Toxic: >5 mg/mL


Mental Health: Effects on Mental Status

May cause dizziness, insomnia, or confusion; quinolones reported to cause restlessness, hallucinations, euphoria, depression, panic, and paranoia


Mental Health: Effects on Psychiatric Treatment

Inhibits CYP1A2 isoenzyme; use caution with clozapine and other psychotropics; monitor for adverse effects


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

<1% of patients experience painful oral mucosa, oral candidiasis, oral ulceration, or mouth dryness


Patient Information

Take as directed, preferably on an empty stomach (30 minutes before or 2 hours after meals). Take entire prescription even if feeling better. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake) to avoid concentrated urine and crystal formation. You may experience nausea, vomiting, or anorexia (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). Report immediately any signs of skin rash, joint or back pain, or difficulty breathing. Report unusual fever or chills; vaginal itching or foul-smelling vaginal discharge; easy bruising or bleeding; or pain, inflammation, or rupture of a tendon.


Nursing Implications

Hold antacids for 2 hours after giving


Dosage Forms

Infusion, as hydrochloride, in D5W: 400 mg (200 mL)

Infusion, as hydrochloride, in NS or D5W: 200 mg (100 mL)

Injection, as hydrochloride: 200 mg (20 mL); 400 mg (40 mL)

Solution, ophthalmic, as hydrochloride: 3.5 mg/mL (2.5 mL, 5 mL)

Suspension, oral, as hydrochloride: 250 mg/5 mL (100 mL); 500 mg/5 mL (100 mL)

Tablet, as hydrochloride: 100 mg, 250 mg, 500 mg, 750 mg


References

Bayer A, Gajewska A, Stephens M, et al, "Pharmacokinetics of Ciprofloxacin in the Elderly," Respiration, 1987, 51(4):292-5.

Campoli-Richards DM, Monk JP, Price A, et al, "Ciprofloxacin: A Review of Its Antibacterial Activity, Pharmacokinetic Properties and Therapeutic Use," Drugs, 1988, 35(4):373-447.

Cohen H and Francisco DH, "Twelve Gram Overdose of Ciprofloxacin With Mild Symptomatology," Ann Pharmacother, 1994, 28(6):805-6.

Davies SP, Azadian BS, Kox WJ, et al, "Pharmacokinetics of Ciprofloxacin and Vancomycin in Patients With Acute Renal Failure Treated by Continuous Haemodialysis," Nephrol Dial Transplant, 1992, 7(8):848-54.

Davis R, Markham A, and Balfour JA, "Ciprofloxacin. An Updated Review of Its Pharmacology, Therapeutic Efficacy and Tolerability," Drugs, 1996, 51(6):1019-74.

Fish DN, Bainbridge JL, and Peloquin CA, "Variable Disposition of Ciprofloxacin in Critically Ill Patients Undergoing Continuous Arteriovenous Hemodiafiltration," Pharmacotherapy, 1995, 15(2):236-45.

Gamboa F, Rivera JM, Gomez Mateos JM, et al, "Ciprofloxacin-Induced Henoch-Schönlein Purpura," Ann Pharmacother, 1995, 29(1):84.

Guay DRP, Awni WM, Peterson PK, et al, "Single and Multiple Dose Pharmacokinetics of Oral Ciprofloxacin in Elderly Patients," Int J Clin Pharmacol Ther Toxicol, 1988, 26(6):279-84.

Guharoy SR, "Serum Sickness Secondary to Ciprofloxacin Use," Vet Hum Toxicol, 1994, 36(6):540-1.

Hoogkamp-Korstanje JA, " In vitro Activities of Ciprofloxacin, Levofloxacin, Lomefloxacin, Ofloxacin, Pefloxacin, Sparfloxacin, and Trovafloxacin Against Gram-Positive and Gram-Negative Pathogens From Respiratory Tract Infections," J Antimicrob Chemother, 1997, 40(3):427-31.

Hooper DC and Wolfson JS, "Fluoroquinolone Antimicrobial Agents," N Engl J Med, 1991, 324(6):384-94.

Kapila K, Chysky V, Hullman R, et al, "Worldwide Clinical Experience on Safety of Ciprofloxacin in Children on Compassionate Use Basis," Proceedings of Third International Symposium on New Quinolones, Vancouver, Canada, 1990, 9.

Lomaestro BM and Bailie GR, "Quinolone-Cation Interactions: A Review," DICP, 1991, 25(11):1249-58.

Mackay AD and Mehta A, "Autoimmune Haemolytic Anemia Associated With Ciprofloxacin," Clin Lab Haematol, 1995, 17(1):97-8.

Mulhall JP and Bergmann LS, "Ciprofloxacin-Induced Acute Psychosis," Urology, 1995, 46(1):102-3.

Nilsson-Ehle I and Ljungberg B, "Quinolone Disposition in the Elderly: Practical Implications," Drugs Aging, 1991, 1(4):279-88.

Paul J and Brown NM, "Tinnitus and Ciprofloxacin," BMJ, 1995, 311(6999):232.

Rams TE and Slots J, "Antibiotics in Periodontal Therapy: An Update," Compendium, 1992, 13(12):1130, 1132, 1134.

Rfidah EI, Findlay CA, and Beattie TJ, "Reversible Encephalopathy After Intravenous Ciprofloxacin Therapy," Pediatr Nephrol, 1995, 9(2):250-1.

Rodriguez WJ, and Wiedermann BL, "The Role of Newer Oral Cephalosporins, Fluoroquinolones, and Macrolides in the Treatment of Pediatric Infections," Adv Pediatr Infect Dis, 1994, 9:125-59.

Rubio TT, Miles MV, Lettieri JT, et al, "Pharmacokinetic Disposition of Sequential Intravenous/Oral Ciprofloxacin in Pediatric Cystic Fibrosis Patients with Acute Pulmonary Exacerbation," Pediatr Infect Dis J, 1997, 16:112-7

Sanders CC, "Ciprofloxacin: In Vitro Activity, Mechanism of Action, and Resistance," Rev Infect Dis, 1988, 10(3):516-27.

Schaad UB, abdus Salam M, Aujard Y, et al, "Use of Fluoroquinolones in Pediatrics: Consensus Report of an International Society of Chemotherapy Commission," Pediatr Infect Dis J, 1995, 14(1):1-9.

Stein GE, "The 4-Quinolone Antibiotics: Past, Present, and Future," Pharmacotherapy, 1988, 8(6):301-14.

Sudip RG, "Serum Sickness Secondary to Ciprofloxacin Use," Vet Hum Toxicol, 36(6):540-1, 1994.

Szarfman A, Chen M, and Blum MD, "More on Fluoroquinolone Antibiotics and Tendon Rupture," N Engl J Med, 1995, 332(3):193.

Villenueve JP, Davies C, and Cote J, "Suspected Ciprofloxacin-Induced Hepatotoxicity," Ann Pharmacother, 1995, 29(3):257-9.

Walker RC and Wright AJ, "The Fluoroquinolones," Mayo Clin Proc, 1991, 66(12):1249-59.

Yew WW, Chau CH, Wong PC, et al, "Ciprofloxacin-Induced Renal Dysfunction in Patients With Mycobacterial Lung Infections," Tuber Lung Dis, 1995, 76(2):173-5.


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