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Product Name
:
CEPROZ
Chemical Name
:
Ciprofloxacin (HCl)
Therapeutic Category
:
Antimicrobial
Pharmacologic Category
:
Antibiotic, Quinolone
Pharmaceutical Form
:
Tablets
Composition
:
Ciprofloxacin (HCl) 500mg / 750mg
Monitoring Parameters
Dosing
 
Dosing: Adult

Anthrax:
Inhalational (postexposure prophylaxis):
Oral: 500 mg every 12 hours for 60 days
Cutaneous (treatment, CDC guidelines): Oral: Immediate release formulation: 500 mg every 12 hours for 60 days. Note: In the presence of systemic involvement, extensive edema, lesions on head/neck, refer to I.V. dosing for treatment of inhalational/gastrointestinal/oropharyngeal anthrax.
Bone/joint infections:
Oral: 500-750 mg twice daily for 4-6 weeks
Chancroid (unlabeled use): Oral: 500 mg twice daily for 3 days (CDC, 2010)
Endocarditis due to HACEK organisms (AHA guidelines, unlabeled use): Note: Not first-line option; use only if intolerant of beta-lactam therapy:
Oral: 500 mg every 12 hours for 4 weeks
Gonococcal infections:
Urethral/cervical gonococcal infections: Oral: 250-500 mg as a single dose (CDC recommends concomitant doxycycline or azithromycin due to possible coinfection with Chlamydia; Note: As of April 2007, the CDC no longer recommends the use of fluoroquinolones for the treatment of uncomplicated gonococcal disease.
Disseminated gonococcal infection (CDC guidelines): Oral: 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); Note: As of April 2007, the CDC no longer recommends the use of fluoroquinolones for the treatment of more serious gonococcal disease, unless no other options exist and susceptibility can be confirmed via culture.
Granuloma inguinale (donovanosis) (unlabeled use): Oral: 750 mg twice daily for at least 3 weeks (and until lesions have healed) (CDC, 2010)
Infectious diarrhea: Oral:
Salmonella: 500 mg twice daily for 5-7 days
Shigella: 500 mg twice daily for 3 days
Traveler's diarrhea: Mild: 750 mg for one dose; Severe: 500 mg twice daily for 3 days
Vibrio cholerae: 1 g for one dose
Intra-abdominal, complicated, community-acquired (in combination with metronidazole): Note: Avoid using in settings where E. coli susceptibility to fluoroquinolones is <90%:
Oral: 500 mg every 12 hours for 7-14 days
Lower respiratory tract, skin/skin structure infections:
Oral: 500-750 mg twice daily for 7-14 days
Periodontitis (unlabeled use): Oral: 500 mg every 12 hours for 8-10 days
Prostatitis (chronic, bacterial): Oral: 500 mg every 12 hours for 28 days
Sinusitis (acute): Oral: 500 mg every 12 hours for 10 days
Typhoid fever: Oral: 500 mg every 12 hours for 10 days
Urinary tract infection:
Acute uncomplicated, cystitis:
Oral:
Immediate release formulation: 250 mg every 12 hours for 3 days
Complicated (including pyelonephritis):
Oral:
Immediate release formulation: 500 mg every 12 hours for 7-14 days

Dosing: Pediatric

See Warnings/Precautions. Note: Extended release tablets and immediate release formulations are not interchangeable. Unless otherwise specified, oral dosing reflects the use of immediate release formulations.
Anthrax:
Inhalational (postexposure prophylaxis):
Oral: 15 mg/kg/dose every 12 hours for 60 days; maximum: 500 mg/dose
Cutaneous (treatment, CDC guidelines): Oral: 10-15 mg/kg every 12 hours for 60 days (maximum: 1 g/day); amoxicillin 80 mg/kg/day divided every 8 hours is an option for completion of treatment after clinical improvement. Note: In the presence of systemic involvement, extensive edema, lesions on head/neck, refer to I.V. dosing for treatment of inhalational/gastrointestinal/oropharyngeal anthrax.
Cystic fibrosis (unlabeled use): Children 5-17 years:
Oral: 40 mg/kg/day divided every 12 hours administered following 1 week of I.V. therapy has been reported in a clinical trial; total duration of therapy: 10-21 days
Urinary tract infection (complicated) or pyelonephritis: Children 1-17 years:
Oral: 20-30 mg/kg/day in 2 divided doses (every 12 hours) for 10-21 days; maximum: 1.5 g/day
Dosing: Geriatric
Refer to adult dosing. Adjust dose carefully based on renal function.

Dosing: Renal Impairment

Adults:
Clcr 30-50 mL/minute: Oral: Administer 250-500 mg every 12 hours.
Clcr <30 mL/minute: Acute uncomplicated pyelonephritis or complicated UTI: Oral: Extended release formulation: 500 mg every 24 hours
Clcr 5-29 mL/minute:
Oral: Administer 250-500 mg every 18 hours.
I.V.: Administer 200-400 mg every 18-24 hours.
Use
 
Children: Complicated urinary tract infections and pyelonephritis due to E. coli. Note: Although effective, ciprofloxacin is not the drug of first choice in children.
Children and Adults: To reduce incidence or progression of disease following exposure to aerolized Bacillus anthracis.
Adults: Treatment of the following infections when caused by susceptible bacteria: Urinary tract infections; acute uncomplicated cystitis in females; chronic bacterial prostatitis; lower respiratory tract infections (including acute exacerbations of chronic bronchitis); acute sinusitis; skin and skin structure infections; bone and joint infections; complicated intra-abdominal infections (in combination with metronidazole); infectious diarrhea; typhoid fever due to Salmonella typhi (eradication of chronic typhoid carrier state has not been proven); uncomplicated cervical and urethra gonorrhea (due to N. gonorrhoeae); nosocomial pneumonia; empirical therapy for febrile neutropenic patients (in combination with piperacillin)
Note: As of April 2007, the CDC no longer recommends the use of fluoroquinolones for the treatment of gonococcal disease.
Use - Unlabeled/Investigational
Acute pulmonary exacerbations in cystic fibrosis (children); cutaneous/gastrointestinal/oropharyngeal anthrax (treatment, children and adults); disseminated gonococcal infection (adults); chancroid (adults); prophylaxis to Neisseria meningitidis following close contact with an infected person; empirical therapy (oral) for febrile neutropenia in low-risk cancer patients; HACEK group endocarditis; infectious diarrhea (children); periodontitis
Adverse Reactions
 
1% to 10%:
Central nervous system: Neurologic events (children 2%, includes dizziness, insomnia, nervousness, somnolence); fever (children 2%); headache (I.V. administration); restlessness (I.V. administration)
Dermatologic: Rash (children 2%, adults 1%)
Gastrointestinal: Nausea (3%); diarrhea (children 5%, adults 2%); vomiting (children 5%, adults 1%); abdominal pain (children 3%, adults <1%); dyspepsia (children 3%)
Hepatic: ALT increased, AST increased (adults 1%)
Local: Injection site reactions (I.V. administration)
Respiratory: Rhinitis (children 3%)
<1% (Limited to important or life-threatening): Abnormal gait, acute renal failure, agitation, agranulocytosis, albuminuria, allergic reactions, anaphylactic shock, anaphylaxis, anemia, angina pectoris, angioedema, anorexia, anosmia, arthralgia, ataxia, atrial flutter, bone marrow depression (life-threatening), breast pain, bronchospasm, candidiasis, candiduria, cardiopulmonary arrest, cerebral thrombosis, chills, cholestatic jaundice, chromatopsia, confusion, constipation, crystalluria (particularly in alkaline urine), cylindruria, delirium, depersonalization, depression, dizziness, drowsiness, dyspepsia (adults), dysphagia, dyspnea, edema, eosinophilia, erythema multiforme, erythema nodosum, exfoliative dermatitis, fever (adults), fixed eruption, flatulence, gastrointestinal bleeding, hallucinations, headache (oral), hematuria, hemolytic anemia, hepatic failure (some fatal), hepatic necrosis, hyperesthesia, hyperglycemia, hyperpigmentation, hyper-/hypotension, hypertonia, insomnia, interstitial nephritis, intestinal perforation, irritability, jaundice, joint pain, laryngeal edema, lightheadedness, lymphadenopathy, malaise, manic reaction, methemoglobinemia, MI, migraine, moniliasis, myalgia, myasthenia gravis exacerbation, myoclonus, nephritis, nightmares, nystagmus, orthostatic hypotension, palpitation, pancreatitis, pancytopenia (life-threatening or fatal), paranoia, paresthesia, peripheral neuropathy, petechia, photosensitivity, pneumonitis, prolongation of PT/INR, pseudomembranous colitis, psychosis, pulmonary edema, renal calculi, seizure; serum cholesterol, glucose, triglycerides increased; serum sickness-like reactions, Stevens-Johnson syndrome, syncope, tachycardia, taste loss, tendon rupture, tendonitis, thrombophlebitis, tinnitus, torsade de pointes, toxic epidermal necrolysis (Lyell’s syndrome), tremor, twitching, urethral bleeding, vaginal candidiasis, vaginitis, vasculitis, ventricular ectopy, visual disturbance, weakness
Contraindications
 
Hypersensitivity to ciprofloxacin, any component of the formulation, or other quinolones; concurrent administration of tizanidine
Warnings / Precautions Drug
 
Boxed Warnings:
• Myasthenia gravis: See “Disease-related concerns” below.
• Tendon inflammation/rupture: See “Concerns related to adverse effects” below.
Concerns related to adverse effects:
• Altered cardiac conduction: Fluoroquinolones may prolong QTc interval; avoid use in patients with a history of QTc prolongation, uncorrected hypokalemia, hypomagnesemia, or concurrent administration of other medications known to prolong the QT interval (including Class Ia and Class III antiarrhythmics, cisapride, erythromycin, antipsychotics, and tricyclic antidepressants).
• CNS stimulation: Tremor, restlessness, confusion, and very rarely hallucinations or seizures may occur; use with caution in patients with known or suspected CNS disorder. Discontinue in patients who experience significant CNS adverse effects (eg, dizziness, hallucinations, suicidal ideations or actions).
• Crystalluria: Rarely, crystalluria has occurred; urine alkalinity may increase the risk. Ensure adequate hydration during therapy.
• Glucose regulation: Fluoroquinolones have been associated with the development of serious, and sometimes fatal, hypoglycemia. These events have occurred most often in elderly patients with diabetes, but have also been reported in patients without a prior history of diabetes. Prompt identification and treatment of hypoglycemia is essential. Individual quinolones may differ in their potential to cause this effect. It was most evident with gatifloxacin (no longer marketed as s systemic formulation). Hyperglycemia has also been associated with the use of fluoroquinolones. Patients should be monitored closely for signs/symptoms of disordered glucose regulation.
• Hypersensitivity reactions: Severe hypersensitivity reactions, including anaphylaxis, have occurred with quinolone therapy. The spectrum of these reactions can vary widely; reactions may present as typical allergic symptoms (eg, itching, urticaria, rash, edema) after a single dose, or may manifest as severe idiosyncratic dermatologic (eg, Stevens-Johnson, toxic epidermal necrolysis), vascular (eg, vasculitis), pulmonary (eg, pneumonitis), renal (eg, nephritis), hepatic (eg, hepatic failure or necrosis), and/or hematologic (eg, anemia, cytopenias) events, usually after multiple doses. Prompt discontinuation of drug should occur if skin rash or other symptoms arise.
• Peripheral neuropathy: The use of quinolones has been linked to peripheral neuropathy (rare); discontinue if symptoms of sensory or sensorimotor neuropathy occur.
• Phototoxicity: Avoid excessive sunlight and take precautions to limit exposure (eg, loose fitting clothing, sunscreen); may cause moderate-to-severe phototoxicity reactions. Discontinue use if photosensitivity occurs.
• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.
• Tendon inflammation/rupture: [U.S. Boxed Warning]: There have been reports of tendon inflammation and/or rupture with quinolone antibiotics; risk may be increased with concurrent corticosteroids, organ transplant recipients, and in patients >60 years of age. Rupture of the Achilles tendon sometimes requiring surgical repair has been reported most frequently; but other tendon sites (eg, rotator cuff, biceps) have also been reported. Strenuous physical activity may be an independent risk factor for tendonitis. Discontinue at first sign of tendon inflammation or pain. May occur even after discontinuation of therapy.
Disease-related concerns:
• Myasthenia gravis: [U.S. Boxed Warning]: May exacerbate muscle weakness related to myasthenia gravis. Cases of severe exacerbations, including the need for ventilatory support and deaths have been reported; avoid use in patients with myasthenia gravis.
• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment required. May increase risk of tendon rupture.
• Rheumatoid arthritis: Use with caution in patients with rheumatoid arthritis; may increase risk of tendon rupture.
• Seizures: Use with caution in individuals at risk of seizures (CNS disorders or concurrent therapy with medications which may lower seizure threshold). Potential for seizures, although very rare, may be increased with concomitant NSAID therapy.
• Syphilis: Since ciprofloxacin is ineffective in the treatment of syphilis and may mask symptoms, all patients should be tested for syphilis at the time of gonorrheal diagnosis and 3 months later.
Concurrent drug therapy issues:
• CYP1A2 substrates: Ciprofloxacin is a potent inhibitor of CYP1A2. Coadministration of drugs which depend on this pathway may lead to substantial increases in serum concentrations and adverse effects.
Special populations:
• Elderly: Adverse effects (eg, tendon rupture, QT changes) may be increased in the elderly.
• G6PD deficiency: Hemolytic reactions may (rarely) occur with quinolone use in patients with latent or actual G6PD deficiency.
• Pediatrics: Adverse effects, including those related to joints and/or surrounding tissues, are increased in pediatric patients and therefore, ciprofloxacin should not be considered as drug of choice in children (exception is anthrax treatment).
Metabolism/Transport Effects
Substrate of P-glycoprotein; Inhibits CYP1A2 (strong), 3A4 (weak)
Interactions
 
Antacids: May decrease the absorption of Quinolone Antibiotics. Of concern only with oral administration of quinolones. Exceptions: Sodium Bicarbonate. Risk D: Consider therapy modification
BCG: Antibiotics may diminish the therapeutic effect of BCG. Risk X: Avoid combination
Bendamustine: CYP1A2 Inhibitors (Strong) may increase the serum concentration of Bendamustine. Concentrations of the active metabolites of bendamustine may be decreased. Risk C: Monitor therapy
Caffeine: Quinolone Antibiotics may decrease the metabolism of Caffeine. Risk C: Monitor therapy
Calcium Salts: May decrease the absorption of Quinolone Antibiotics. Of concern only with oral administration of both agents. Exceptions: Calcium Chloride. Risk D: Consider therapy modification
Corticosteroids (Systemic): Quinolone Antibiotics may enhance the adverse/toxic effect of Corticosteroids (Systemic). Risk of tendon-related side effects, including tendonitis and rupture, may be enhanced. Risk C: Monitor therapy
CYP1A2 Substrates: CYP1A2 Inhibitors (Strong) may decrease the metabolism of CYP1A2 Substrates. Risk D: Consider therapy modification
Didanosine: May decrease the serum concentration of Quinolone Antibiotics. Management: Administer oral quinolones at least 2 hours before or 6 hours after didanosine. Monitor for decreased therapeutic effects of quinolones, particularly if doses cannot be separated as recommended. This does not apply to unbuffered enteric coated didanosine. Risk D: Consider therapy modification
Erlotinib: Ciprofloxacin (Systemic) may increase the serum concentration of Erlotinib. Risk C: Monitor therapy
Fosphenytoin: Ciprofloxacin (Systemic) may decrease the serum concentration of Fosphenytoin. Risk C: Monitor therapy
Insulin: May enhance the hyperglycemic effect of Quinolone Antibiotics. Insulin may enhance the hypoglycemic effect of Quinolone Antibiotics. Risk C: Monitor therapy
Iron Salts: May decrease the absorption of Quinolone Antibiotics. Of concern only with oral administration of both agents. Exceptions: Ferric Gluconate; Ferumoxytol; Iron Dextran Complex; Iron Sucrose. Risk D: Consider therapy modification
Lanthanum: May decrease the serum concentration of Quinolone Antibiotics. Management: Administer oral quinolone antibiotics at least two hours before or after lanthanum. Risk D: Consider therapy modification
Magnesium Salts: May decrease the absorption of Quinolone Antibiotics. Of concern only with oral administration of both agents. Risk D: Consider therapy modification
Methotrexate: Ciprofloxacin (Systemic) may increase the serum concentration of Methotrexate. Risk C: Monitor therapy
Mycophenolate: Quinolone Antibiotics may decrease the serum concentration of Mycophenolate. Specifically, quinolones may decrease concentrations of the active metabolite of mycophenolate. Risk C: Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May enhance the neuroexcitatory and/or seizure-potentiating effect of Quinolone Antibiotics. Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Quinolone Antibiotics. Risk C: Monitor therapy
Pentoxifylline: Ciprofloxacin (Systemic) may enhance the adverse/toxic effect of Pentoxifylline. Risk C: Monitor therapy
P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
P-glycoprotein/ABCB1 Inhibitors: P-glycoprotein/ABCB1 Substrates may increase the serum concentration of P-glycoprotein/ABCB1 Inhibitors. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
Phenytoin: Ciprofloxacin (Systemic) may decrease the serum concentration of Phenytoin. Risk C: Monitor therapy
Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Risk C: Monitor therapy
Probenecid: May increase the serum concentration of Quinolone Antibiotics. Risk C: Monitor therapy
QTc-Prolonging Agents: Ciprofloxacin (Systemic) may enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk C: Monitor therapy
Quinapril: May decrease the serum concentration of Quinolone Antibiotics. Management: Separate doses of quinapril and oral quinolones by at least 2 hours in order to reduce the risk of interaction. Monitor for reduced efficacy of the quinolone if these products are used concomitantly. Risk D: Consider therapy modification
ROPINIRole: Ciprofloxacin (Systemic) may decrease the metabolism of ROPINIRole. Risk C: Monitor therapy
Ropivacaine: Ciprofloxacin (Systemic) may decrease the metabolism of Ropivacaine. Risk C: Monitor therapy
Sevelamer: May decrease the absorption of Quinolone Antibiotics. Risk D: Consider therapy modification
Sucralfate: May decrease the serum concentration of Quinolone Antibiotics. Management: Administer oral quinolones at least 2 hours before or 6 hours after the sucralfate dose. Greater separation of doses may further lessen the risk for a significant interaction. Risk D: Consider therapy modification
Sulfonylureas: Quinolone Antibiotics may enhance the hypoglycemic effect of Sulfonylureas. This appears to be particularly concerning early in the course of combination therapy. Quinolone Antibiotics may diminish the hypoglycemic effect of Sulfonylureas. With longer-term combination, there is a greater risk of hyperglycemia. Risk C: Monitor therapy
Theophylline Derivatives: Quinolone Antibiotics may decrease the metabolism of Theophylline Derivatives. Ciprofloxacin and enoxacin are of greatest concern. Theophylline/quinolone therapy might augment the seizure-producing potential of each of the individual agents. Exceptions: Dyphylline. Risk D: Consider therapy modification
TiZANidine: Ciprofloxacin (Systemic) may decrease the metabolism of TiZANidine. Risk X: Avoid combination
Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 24 hours after cessation of antibacterial agents. Risk D: Consider therapy modification
Varenicline: Quinolone Antibiotics may increase the serum concentration of Varenicline. Management: Monitor for increased varenicline adverse effects with concomitant use of levofloxacin or other quinolone antibiotics, particulary in patients with severe renal impairment. International product labeling recommendations vary. Consult appropriate labeling. Risk C: Monitor therapy
Vitamin K Antagonists (eg, warfarin): Quinolone Antibiotics may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
Zinc Salts: May decrease the absorption of Quinolone Antibiotics. Of concern only with oral administration of both agents. Risk D: Consider therapy modification
Pregnancy
 
C
Pregnancy Implications
Adverse events have been observed in some animal studies; therefore, the manufacturer classifies ciprofloxacin as pregnancy category C. Ciprofloxacin crosses the placenta and produces measurable concentrations in the amniotic fluid and cord serum. An increased risk of teratogenic effects has not been observed in animals or humans following ciprofloxacin use during pregnancy; however, because of concerns of cartilage damage in immature animals, ciprofloxacin should only be used during pregnancy if a safer option is not available. Ciprofloxacin is recommended for prophylaxis and treatment of pregnant women exposed to anthrax. Serum concentrations of ciprofloxacin may be lower during pregnancy than in nonpregnant patients.
Lactation
 
Enters breast milk/not recommended (AAP rates "compatible"; AAP 2001 update pending)
Breast-Feeding Considerations
Ciprofloxacin is excreted in breast milk. Breast-feeding is not recommended by the manufacturer. Due to the low concentrations in human milk, minimal toxicity would be expected in the nursing infant and infant serum levels were undetectable in one report. Nondose-related effects could include modification of bowel flora. There has been a single case report of perforated pseudomembranous colitis in a breast-feeding infant whose mother was taking ciprofloxacin.
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: Immediate release tablet: Rapid (~50% to 85%)
Distribution: Vd: 2.1-2.7 L/kg; tissue concentrations often exceed serum concentrations especially in kidneys, gallbladder, liver, lungs, gynecological tissue, and prostatic tissue; CSF concentrations: 10% of serum concentrations (noninflamed meninges), 14% to 37% (inflamed meninges)
Protein binding: 20% to 40%
Metabolism: Partially hepatic; forms 4 metabolites (limited activity)
Half-life elimination: Children: 2.5 hours; Adults: Normal renal function: 3-5 hours
Time to peak: Oral:
Immediate release tablet: 0.5-2 hours
Excretion: Urine (30% to 50% as unchanged drug); feces (15% to 43%)
 
   
 
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