Fluconazole Capsule a triazole antifungal-Hyperdrug

This medicine contains the active ingredient FLUCONAZOLE, which is a type of medicine called a triazole antifungal. It is used to treat infections with fungi and yeasts. FLUCONAZOLE works by preventing fungi from producing a substance called ergosterol, which is a component of fungal cell membranes. The cell membranes of fungi are vital for their survival. They keep unwanted substances from entering the cells and stop the contents of the cells from leaking out. Without ergosterol as part of the cell membrane, the membrane is weakened and damaged, and essential constituents of the fungal cells can leak out. This kills the fungi. FLUCONAZOLE is used to treat a number of different types of fungal and yeast infections, particularly those caused by Candida or Cryptococcus species of fungi. Fluconazole can be bought over-the-counter from pharmacies as a single 150mg dose. This single dose is an effective treatment for vaginal thrush (vaginal candidiasis). The single dose can also be used to treat male partners who are infected (candidal balanitis).

Product information leaflet:

http://emc.medicines.org.uk/medicine/12630/SPC/Fluconazole Capsules (Pliva Pharma Ltd)/

Fluconazole may be administered either orally or by intravenous infusion at a rate of approximately 5-10ml/min, the route being dependent on the clinical state of the patient. On transferring from the intravenous route to the oral route or vice versa, there is no need to change the daily dose. The daily dose of fluconazole should be based on the nature and severity of the fungal infection. Most cases of vaginal candidiasis respond to single dose therapy. Therapy for those types of infections requiring multiple dose treatment should be continued until clinical parameters or laboratory tests indicate that active fungal infection has subsided. An inadequate period of treatment may lead to the recurrence of active infection. Patients with AIDS and cryptococcal meningitis usually require maintenance therapy to prevent relapse. Adults 1. Candidal vaginitis or balanitis – 150 mg single oral dose. 2. Mucosal candidiasis – the usual dose is 50 mg once daily for 7 – 14 days. Treatment should not normally exceed 14 days except in severely immunocompromised patients. Atrophic oral candidiasis associated with dentures – the usual dose is 50 mg once daily for 14 days administered concurrently with local antiseptic measures to the denture. For other candidal infections of mucosa (except genital candidiasis see above), e.g. oesophagitis, non-invasive bronchopulmonary infections, candiduria, mucocutaneous candidiasis etc., the usual effective dose is 50 mg daily, given for 14 – 30 days. In unusually difficult cases of mucosal candidal infections the dose may be increased to 100 mg daily. 3. For tinea pedis, corporis, cruris, versicolor and dermal Candidal infections the recommended dosage is 50 mg once daily. Duration of treatment is normally 2 to 4 weeks but tinea pedis may require treatment for up to 6 weeks. Duration of treatment should not exceed 6 weeks. 4. For candidaemia, disseminated candidiasis and other invasive candidal infections the usual dose is 400 mg on the first day followed by 200 mg daily. Depending on the clinical response the dose may be increased to 400 mg daily. Duration of treatment is based upon the clinical response. 5a For cryptococcal meningitis and cryptococcal infections at other sites, the usual dose is 400 mg on the first day followed by 200 – 400 mg once daily. Duration of treatment for cryptococcal infections will depend on the clinical and mycological response, but is usually at least 6 – 8 weeks for cryptococcal meningitis. 5b For the prevention of relapse of cryptococcal meningitis in patients with AIDS, after the patient receives a full course of primary therapy, fluconazole may be administered indefinately at a daily dose of 100 – 200 mg. 6 For the prevention of fungal infections in immunocompromised patients considered at risk as a consequence of neutropenia following cytotoxic chemotherapy or radiotherapy, the dose should be 50 to 400 mg once daily, based on the patient's risk for developing fungal infection. For patients at high risk of systemic infection e.g. patients who are anticipated to have profound or prolonged neutropenia such as during bone marrow transplantation, the recommended dose is 400 mg once daily. Fluconazole administration should start several days before the anticipated onset of neutropenia, and continue for 7 days after the neutrophil count rises above 1000 cells per mm3. Children As with similar infections in adults, the duration of treatment is based on the clinical and mycological response. Fluconazole is administered as a single daily dose each day. Children over four weeks of age The recommended dose of fluconazole for mucosal candidiasis is 3 mg/kg daily. A loading dose of 6 mg/kg may be used on the first day to achieve steady state levels more rapidly. For the treatment of systemic candidiasis and cryptococcal infection, the recommended dosage is 6 – 12 mg/kg daily, depending on the severity of the disease. For the prevention of fungal infections in immunocompromised patients considered at risk as a consequence of neutropenia following cytotoxic chemotherapy or radiotherapy, the dose should be 3 – 12 mg/kg daily, depending on the extent and duration of the induced neutropenia (see adult dosing). A maximum dosage of 400 mg daily should not be exceeded in children. Despite extensive data supporting the use of fluconazole in children there are limited data available on the use of fluconazole for genital candidiasis in children below 16 years. Use at present is not recommended unless antifungal treatment is imperative and no suitable alternative agent exists. Children below 4 weeks of age Neonates excrete fluconazole slowly. In the first two weeks of life the same mg/kg dosing as in older children should be used but administered every 72 hours. During weeks 2 – 4 of life the same dose should be given every 48 hours. A maximum dosage of 12 mg/kg every 72 hours should not be exceeded in children below two weeks of life. For children between 2 – 4 weeks of life 12 mg/kg every 48 hours should not be exceeded. For children with impaired renal function the daily dose should be reduced in accordance with the guidelines given for adults. To facilitate accurate measurement of doses less than 10 mg, fluconazole should only be administered to children in hospital using preparations available as oral suspension or intravenous infusion, depending on the clinical condition of the child. Elderly The normal dose should be used if there is no evidence of renal impairment. In patients with renal impairment (creatinine clearance less than 50 ml/min) the dosage schedule should be adjusted as described below. Use in renal impairment Fluconazole is excreted predominantly in the urine as unchanged drug. No adjustments in single dose therapy are required. In patients with impaired renal function who will receive multiple doses of fluconazole, the normal recommended dose (according to indication) should be given on day 1, followed by a daily dose based on the following table:

Fluconazole should not be used in patients with known hypersensitivity to fluconazole or to related azole compounds or to any other ingredient within the formulation (see section 6.1.). Co-administration with terfenadine or cisapride is contra-indicated in patients receiving fluconazole. See 'Interactions with other medicinal products and other forms of interaction'.

Fluconazole is generally well tolerated. The most common side effects observed during clinical trials and associated with fluconazole are: Central and Peripheral Nervous System Headache. Dermatological Rash. Gastrointestinal Abdominal pain, diarrhoea, flatulence, nausea. In some patients, particularly those with serious underlying diseases such as AIDS and cancer, changes in renal and haematological function test results and hepatic abnormalities have been observed during treatment with fluconazole and comparative agents, but the clinical significance and relationship to treatment is uncertain. (See Section 4.4., 'Special warnings and special precautions for use'.) Liver/ Biliary Hepatic toxicity including rare cases of fatalities, elevated alkaline phosphatase, elevated bilirubin, elevated SGOT, elevated SGPT. In addition, the following adverse events have occurred during post-marketing: Central and Peripheral Nervous System Dizziness, seizures. Dermatological Alopecia, exfoliative skin disorders including Stevens-Johnson syndrome and toxic epidermal necrolysis. Gastrointestinal Dyspepsia, vomiting. Haematopoietic and Lymphatic Leukopenia including neutropenia and agranulocytosis, thrombocytopenia. Immunological Anaphylaxis (including angiodema, face oedema, pruritus). Liver/ Biliary Hepatic failure, hepatitis, hepatocellular necrosis, jaundice. Metabolic/ Nutritional Hypercholesterolaemia, hypertriglyceridaemia, hypokalaemia. Other senses Taste perversion.

Fluconazole Capsule 150mg