Cetraxal

DESCRIPTION

CETRAXAL (ciprofloxacin otic solution) 0.2% contains the synthetic antimicrobial agent ciprofloxacin hydrochloride. CETRAXAL (ciprofloxacin otic solution) is a sterile, preservative-free solution for otic use. Each single use container of CETRAXAL delivers 0.25 mL of solution equivalent to 0.5 mg of ciprofloxacin. The inactive ingredients are povidone, glycerin, and water for injection. Sodium hydroxide and/or lactic acid may be added to adjust pH.

Ciprofloxacin, a fluroquinolone is available as the monohydrochloride, monohydrate salt of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid. Its molecular formula is C₁₇H₁₈FN₃O₃•HCl•H₂O, and molecular weight is 385.82.

The chemical structure of ciprofloxacin hydrochloride is:

SIDE EFFECTS

Because clinical studies are conducted under widely varying conditions, adverse drug reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in clinical practice.

In a randomized, active-controlled clinical trial, approximately 300 patients with clinical signs and symptoms of otitis externa were treated with CETRAXAL. The most frequently reported adverse reactions were application site pain, ear pruritus, fungal ear superinfection, and headache, each reported in approximately 2-3% of patients.

DRUG INTERACTIONS

No Information Provided

WARNINGS

Included as part of the "PRECAUTIONS" Section

PRECAUTIONS

Otic Use Only

CETRAXAL is for otic use only. It should not be used for injection, for inhalation or for topical ophthalmic use.

Hypersensitivity

CETRAXAL should be discontinued at the first appearance of a skin rash or any other sign of hypersensitivity.

Growth Of Resistant Organisms With Prolonged Use

As with other anti-infectives, use of CETRAXAL may result in overgrowth of nonsusceptible organisms, including yeast and fungi. If super-infection occurs, discontinue use and institute alternative therapy.

Lack Of Clinical Response

If the infection is not improved after one week of therapy, cultures may help guide further treatment.

Use In Specific Populations

Pregnancy

Pregnancy Category C

Reproduction studies have been performed in rats and mice using oral doses of up to 100 mg/kg and intravenous (IV) doses up to 30 mg/kg and have revealed no evidence of harm to the fetus as a result of ciprofloxacin. In rabbits, ciprofloxacin (30 and 100 mg/kg orally) produced gastrointestinal disturbances resulting in maternal weight loss and an increased incidence of abortion, but no teratogenicity was observed at either dose. After intravenous administration of doses up to 20 mg/kg, no maternal toxicity was produced in the rabbit, and no embryotoxicity or teratogenicity was observed.

Animal reproduction studies have not been conducted with CETRAXAL. No adequate and well-controlled studies have been performed in pregnant women. Caution should be exercised when CETRAXAL is used by a pregnant woman.

Nursing Mothers

Ciprofloxacin is excreted in human milk with systemic use. It is not known whether ciprofloxacin is excreted in human milk following otic use. Because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

The safety and effectiveness of CETRAXAL in infants below one year of age have not been established. The efficacy of CETRAXAL in treating otitis externa in pediatric patients one year or older has been demonstrated in controlled clinical trials (see Clinical Studies).

There is no evidence that the otic administration of quinolones has any effect on weight bearing joints, even though systemic administration of some quinolones has been shown to cause arthropathy in immature animals.

Geriatric Use

No overall differences in safety and effectiveness have been observed between elderly and younger

OVERDOSE

No Information Provided

CONTRAINDICATIONS

CETRAXAL is contraindicated in persons with a history of hypersensitivity to ciprofloxacin.

CLINICAL PHARMACOLOGY

Mechanism Of Action

Ciprofloxacin is a fluoroquinolone antimicrobial (see CLINICAL PHARMACOLOGY, Microbiology).

Pharmacokinetics

The plasma concentrations of ciprofloxacin were not measured following administration of 0.25 mL CETRAXAL (total dose: 0.5 mg ciprofloxacin). However, the maximum plasma concentration of ciprofloxacin is anticipated to be less than 5 ng/mL.

Microbiology

The bactericidal action of ciprofloxacin results from interference with the enzyme DNA gyrase, which is needed for the synthesis of bacterial DNA.

Bacterial resistance to quinolones can develop through chromosomally- or plasmid-mediated mechanisms.

The mechanism of action of fluoroquinolones, including ciprofloxacin, is different from that of macrolides. Therefore, ciprofloxacin may be active against pathogens that are resistant to these antibiotics, and these antibiotics may be active against pathogens that are resistant to ciprofloxacin. In vitro studies demonstrated cross-resistance between ciprofloxacin and some fluoroquinolones.

Ciprofloxacin has been shown to be active against most isolates of the following bacteria, both in vitro and in clinical infections of acute otitis externa as described in Section INDICATIONS AND USAGE.

Staphylococcus aureus
Pseudomonas aeruginosa.

Clinical Studies

In a randomized, multi-center, evaluator-blinded study of patients with acute otitis externa, patients were treated with either CETRAXAL twice daily or neomycin and polymyxin B sulfates and hydrocortisone otic solution (PNH) three times daily for 7 days.

In the per protocol population, clinical cure was achieved at the end of a 7-day treatment in 70% (173/247) for the CETRAXAL treated group versus 60% (147/243) for the control treated group.

PATIENT INFORMATION

Directions For Use

Patients should be advised that CETRAXAL is for otic use only. It is not for ophthalmic or inhalation use. It is not for injection.

CETRAXAL should be given 2 times each day (about 12 hours apart) in each infected ear.

CETRAXAL should be used for as long as it is prescribed, even if the symptoms improve. The patient should be advised to follow these directions while on CETRAXAL:

Wash their hands before use.

Warm the container in their hands for at least one minute prior to use to minimize dizziness that may result from the instillation of a cold solution into the ear canal. Twist off and discard top of container.

Lie with the affected ear upward and then instill the contents of one container into the ear. Maintain this position for at least one minute to facilitate penetration of the drops into the ear.

Repeat, if necessary, for the opposite ear.

Discard used container.

Store unused containers in pouch to protect from light.

Hypersensitivity

Patients should be advised to immediately discontinue CETRAXAL at the first appearance of a skin rash or any other sign of hypersensitivity [see WARNINGS AND PRECAUTIONS].