Composition

Forcan-50 Capsules

Each capsule contains Fluconazole 50 mg.

Forcan-150 Capsules

Each capsule contains Fluconazole 150mg.

Forcan-200 Capsules

Each capsule contains Fluconazole 200 mg.

Description

Fluconazole is a bis-triazole antifungal structurally related to imidazole derivative antifungals. The nitrogen of the azole ring of the triazole binds to the haem moiety of the fungal cytochrome P-450 enzyme lanosterol 14 alpha demethylase which halts conversion of lanosterol to ergosterol that leads to a cascade of abnormalities in membrane permeability, membrane bound enzyme activity and coordination of chitin synthesis.

Indications

Forcan is indicated for:

• Mucosal candidiasis: e.g. oropharyngeal, oesophageal, mucocutaneous and chronic oral atrophic candidiasis, vaginal candidiasis etc.
• Systemic candidiasis: Candidaemia, disseminated candidiasis, infection of peritoneum, endocardium, pulmonary and urinary tract.
• Cryptococcosis: Cryptococcal meningitis, primary as well as maintenance therapy.
• Prevention of fungal infection in patients with malignancy, AIDS, in intensive care units and patients on immunosuppressive drugs.

Dosage and Administration

Forcan may be administered either orally or by intravenous infusion at a rate of approximately 5-10 ml/min. On transferring the patient from the intravenous to oral route or vice versa, there is no need to change the daily dose.

Adults

Vaginal candidiasis

150 mg single dose.

Mucosal candidiasis

50-100 mg daily for 14-30 days.

Systemic candidiasis

400 mg on first day, then 200-400 mg once daily.

Cryptococcal meningitis

400 mg loading dose, followed by 200 mg daily for 1012 weeks after CSF becomes culture negative.

Maintenance to prevent relapse of cryptococcal meningitis

100-200 mg daily.

Prophylaxis in immunocompromised

50-400 mg once daily started several days before onset of neutropenia and continued for 7 days after neutrophil count > 1000 cells/mm³.

Children

Mucosal candidiasis

Neonates: 3 mg/kg every 72 hrs

2-4 weeks: 3 mg/kg every 48 hrs

over 4 weeks: 3 mg/kg daily

Systemic candidiasis

Neonates: 6-12 mg/kg every 72 hrs

2-4 weeks: 6-12 mg/kg every 48 hrs

over 4 weeks: 6-12 mg/kg daily

Prophylaxis in immunocompromised

Neonates: 3-12 mg/kg every 72 hrs

2-4 weeks: 3-12 mg/kg daily every 48 hrs

over 4 weeks: 3-12 mg/kg daily

In impaired renal function

Fluconazole is excreted predominantly in urine as unchanged drug. Hence in patients with impaired renal function, dosage of fluconazole must be modified in response to the degree of impairment and should be based on the patient's measured or estimated creatinine clearance.

The recommended dosages are:

Creatinine Clearance	Dosage Interval / (ml/min) Daily Dose
>50	24 hrs / 100%
21 - 50	48 hrs / 50%
10 - 20	72 hrs / 25%

Patients receiving 100 per cent dose regular after haemodialysis every dialysis.

Compatibility of intravenous infusion: Although further dilution is unnecessary, Forcan intravenous infusion is compatible with the following administration fluids:

• Dextrose 20 per cent
• Ringer's solution
• Hartmann's solution
• Potassium chloride in dextrose
• Sodium bicarbonate
• Normal saline (0.9 per cent)

Mixing with any other drug prior to infusion is not recommended.

Contraindications

Hypersensitivity to Forcan or any of its excipients or related azole compounds.

Warnings and Precautions

Drug Interactions

Anticoagulants

Fluconazole has been shown to prolong prothrombin times of coumarin drugs, hence requires careful monitoring.

Cyclosporin

Concomitant administration of fluconazole and cyclosporin may result in increase in cyclosporin level.

Phenytoin

Fluconazole significantly increases phenytoin levels and AUC resulting in phenytoin toxicity.

Oral hypoglycaemics

Concomitant administration of fluconazole and oral hypoglycaemics such as sulphonylurea in diabetic patients results in increased plasma concentration and reduced metabolism of antidiabetic agents.

Rifampicin

Concomitant administration of fluconazole and rifampicin decrease AUC for fluconazole by 20 per cent.

Theophylline

Fluconazole may increase serum concentrations of theophylline. Careful monitoring is recommended if the two drugs are coadministered.

Pregnancy

There are no adequate and wellcontrolled studies in pregnant women. Forcan should be used in pregnancy only if the benefits outweigh the risks.

Nursing Mothers

Since the drug is secreted in breast milk, it should not be used in lactating women.

Paediatric Use

See Dosage and Administration.

In impaired renal function

See Dosage and Administration.

In impaired hepatic function

Patients who develop abnormal liver function should be monitored. Immunocompromised patients who develop rash during fluconazole therapy should be monitored and the drug discontinued if lesions progress.

Side Effects

Fluconazole is generally well tolerated. Commonly reported side effects are nausea, vomiting, abdominal pain, headache, skin rash and diarrhoea. Mild transient, reversible increase in liver enzymes like ALT, AST, alkaline phosphatase and serum bilirubin, etc. may be seen. Serious hepatotoxicity is rarely seen. Clinical adverse reactions have been more frequently reported in HIV infected patients than in nonHIV infected patients, however, the patterns were similar. In rare cases, anaphylaxis has been reported.

Overdosage

In the event of overdosage, supportive measures and symptomatic treatment with gastric lavage if necessary, may be adequate.

Fluconazole is excreted largely in the urine, forced diuresis would probably increase the elimination rate. A three hour session of haemodialysis decreases plasma levels by approximately 50 per cent.

Storage

Intravenous infusion

Do not freeze. It is for single use only. Discard any remaining solution.

Presentation

Forcan-50 Strip of 4 capsules

Forcan-150 Strip of 1 capsule

Forcan-200 Strip of 4 capsules