Pefloxacin - Contraindications

Contraindications

• Hypersensitivity (allergy) to pefloxacin or to one of its components or to another member of the quinolones.

• Known deficiency in glucose-6 phosphate dehydogenase (a blood red cells enzyme).

• Due to growing prevalence of antibiotic resistance to the fluoroquinolones in Southeast Asia, the use of pefloxacin in patients who have been to Southeast Asia is increasingly being contraindicated.

• Pefloxacin is also considered to be contraindicated within the pediatric population (due to the risk of arthropathies), pregnancy, nursing mothers, and in patients with epilepsy or other seizure disorders.

• Precautions:

Coadministration of Pefloxacin with other drugs primarily metabolized by CYP1A2 results in increased plasma concentrations of these drugs and could lead to clinically significant adverse events of the coadministered drug.

Patients should be warned to avoid exposure to direct sunlight or UV light during treatment and until 36 hours after the discontinuation of treatment, because of the risk of phototoxicity reactions (allergic skin rashes).

Tendinitis (inflammation of tendon) may occur and can lead to tendon rupture, particularly in the Achilles tendon and more frequently in elderly patients. Age, past history of tendinitis, vigorous physical exercise and long-term corticoid treatment may predispose a patient to tendinitis and tendon rupture. Therefore, as soon as the treatment with pefloxacin is initiated, it is recommended to look for pain or edema at the level of Achilles tendon, particularly in patients at risk. If such signs are identified therapy should be discontinued immediately.

In patients with a past history of convulsions or with risk factors of convulsions pefloxacin should be used with caution.

In case of myasthenia pefloxacin should be used with caution in these patients.

• Pregnancy

The fluoroquinolones rapidly cross the blood-placenta and blood-milk barrier, and are extensively distributed into the fetal tissues. For this reason the Fluroquinolones are contraindicated during pregnancy due to the risk of spontaneous abortions and birth defects. The Flouroquinolones have also been reported as being present in the mother’s milk and are passed on to the nursing child, which may increases the risk of the child suffering from this syndrome as well, even though the child had never been prescribed or taken any of the drugs found within this class.

• Pediatric population

Fluoroquinolones are not licensed for use in children due to the risk of fatalities as well as permanent injury to the musculoskeletal system, with two exceptions. Ciprofloxacin is being licensed in the United States for the treatment of Complicated Urinary Tract Infections and Pyelonephritis due to Escherichia coli and Inhalational Anthrax (post-exposure) and Levofloxacin was recently licensed for the treatment of Inhalational Anthrax (post-exposure). However, the Fluoroquinolones are licensed to treat lower respiratory infections in children with cystic fibrosis in the UK.

At least ten cases of arthropathy occurred in pediatric patients receiving fluoroquinolones; seven of these cases involved pefloxacin. Clinical features included joint swelling or pain in one or more joints. Usually the knees were most oftentimes reported. One patient had evidence of significant joint damage to the right hip and both knees. One study that calculated the risk of such injury had stated that such injury occurred more often with Pefloxacin. Within another study it was stated that the pediatric patient has a 3.8% chance of experiencing a serious musculoskeletal adverse event. Within the studies submitted in response to a Pediatric Written Request (Ciprofloxacin, circa 2004) the rate of athropy was reported to be 9.3%.

Pefloxacin is well known to be associated with high incidence of arthropathy in humans because the drug affects articular cartilage and the epiphyseal growth plate. The importance of this toxicity is that it is irreversible and manifest later after the drug is discontinued. Musculoskeletal events tended to be more frequent with pefloxacin.