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AD-Fluconazole

Adpharm Pharmaceuticals Limited
60, Ajao Road, Surulere, Lagos State, Nigeria
Email: adpharm2010@yahoo.com; info@adpharmltd.com
Tel: +234(0)818-839-0519, +234(0)807-408-4334. Mobile: 08033481022
Website: http://adpharmltd.com/

Brand Name

AD-Fluconazole

Manufacturer

Globela Pharma Pvt. Ltd

Therapeutic Class

Antifungals, Systemic

Dosage Form, Composition & NAFDAC Registration Number (NRN)

Tablet (NRN:B4-1543): Each uncoated tablet contains Fluconazole USP 150 mg. Excipients q.s

Pack size: AD-FLUCONAZOLE (FLUCONAZOLE TABLETS 150 mg) White color, caplet shape, uncoated tablets having breakline on one side and other side plain, and pack in Alu-Alu blister of 10 tablets.

AD Fluconazole Tablet

Pharmacology

Fluconazole is a triazole antifungal drug which in sensitive fungi inhibits cytochrome P-450 dependent enzymes resulting in impairment of ergosterol synthesis in fungal cell membranes. Fluconazole is well absorbed following oral administration, bioavailability from the oral route being 90% or more of that from the intravenous route. Peak plasma concentrations are reached within 1 to 2 hours of oral administration.

Plasma concentrations are proportional to the dose over a range of 50 mg to 400 mg. Multiple dosing leads to increases in peak plasma concentrations; steady-state concentrations are reached in 6 to 10 days but may be attained on day 2 if a loading dose is given.

The elimination half life of fluconazole is about 30 hours and is increased in patients with impaired renal function. Plasma protein binding is only about 12%. It has been shown in pharmacokinetic studies performed in children that fluconazole is cleared faster in children than in adults, with a half life of 23 hours.

In children under the age of 1, the volume of distribution of fluconazole (950 mL/kg) is higher than in adults (700 mL/kg). Accumulation on multiple daily dosing is therefore less and steady state plasma levels are achieved faster than in adults. The half lives of fluconazole, in neonates, determined over the first 2 weeks of life are considerably longer than adult values with a mean of 74 hours at Day 1 and 47 hours at Day 13 of life. The volume of distribution is about 1200 mL/kg in neonates.

There is no evidence of circulating metabolites, but accumulation is significant over 15 days and concentrations may rise 2-3 fold. The long plasma elimination half-life (approximately 30 hours) provides the basis for once daily dosing in the treatment of systemic conditions, single dose therapy for vaginal candidiasis and once weekly dosing for other indications.

Indications

Fluconazole is administered by mouth or by intravenous infusion in similar doses. Fluconazole is indicated for the treatment of the following conditions in adults and children:

Cryptococcal meningitis and maintenance therapy to prevent relapse of cryptococcal disease in patients with AIDS.

Systemic candidiasis, Oropharyngeal and oesophageal candidiasis.

Prevention of fungal infections in patients with malignancy who are predisposed to such infections as a result of cytotoxic chemotherapy and radiotherapy.

When systemic treatment is indicated and appropriate, fluconazole is used in the following conditions: vaginal candidiasis, acute or recurrent and prophylaxis to reduce the incidence of recurrent vaginal candidiasis.

Contra-indications

Hypersensitivity to fluconazole or any of the ingredients of the preparation.

Concomitant administration of cisapride is contraindicated in patients receiving fluconazole.

Concomitant administration of terfenadine is contra-indicated in patients receiving fluconazole at multiple doses of 400 mg per day or higher based upon results of a multiple dose interaction study. (See Interactions section)

Pregnancy.

Fluconazole should not be given to breast-feeding women, as fluconazole is found in breast milk at concentrations similar to plasma.

Precautions/Warnings

WARNINGS
Use during pregnancy and lactation
Safety in pregnancy and lactation has not been established.

There are no adequate and well controlled studies which assessed the safety of fluconazole treatment in pregnant women, congenital abnormalities in infants whose mothers were treated with fluconazole have been reported. The relationship between fluconazole use and these events are unclear.

DOSAGE AND ADMINISTRATION
Creatinine clearance (mL/min) Percent of Recommended Dose
>50 100%

Regular haemodialysis 100% after each dialysis
These are suggested dose adjustments based on pharmacokinetics following administration of multiple doses. Depending on clinical condition, further adjustment may be required.

When serum creatinine is the only measure of renal function available, the following formula (based on sex, weight, and age of the patient) should be used to estimate the creatinine clearance: Males:
Weight (kg) x (140 minus age)

72 x serum creatinine (mg/dL) Conversion of serum creatinine units to SI (i.e., micro mol/L):
Weight (kg) x (140 minus age)
88.4 x 72 x serum creatinine (mg/dL)
Females: 0.85 x above value

SIDE-EFFECTS AND SPECIAL PRECAUTIONS

The most common side-effects associated with fluconazole are:

Gastrointestinal: Abdominal pain, diarrhoea, nausea, vomiting, and flatulence.

Central and Peripheral Nervous System: Headache

Dermatologic: Rash. If a rash develops which is considered attributable to fluconazole, further treatment with this agent should be stopped.

Liver/Biliary: Serious hepatic toxicity has been reported in patients with severe underlying disease. Rare cases of fatalities, elevated alkaline phosphatase, elevated bilirubin, elevated SGOT, elevated SGPT have been observed.

Interactions

In subjects receiving warfarin, fluconazole has been shown to prolong prothrombin times. In patients receiving concomitant fluconazole and warfarin therapy, bleeding events (haematuria, bruising, epistasis, gastrointestinal bleeding, and melaena), in association with increases in prothrombin time have been reported.

The dose of anticoagulant should be carefully titrated and the prothrombin time carefully monitored in patients who are being treated concomitantly with fluconazole and coumarin medicines.
Such patients requiring minor oral surgery and dental procedures should be carefully monitored.

Adverse Effects

The most common side-effects associated with fluconazole are:

Gastrointestinal: Abdominal pain, diarrhoea, nausea, vomiting, and flatulence.

Central and Peripheral Nervous System: Headache.

Dermatologic: Rash. If a rash develops which is considered attributable to fluconazole, further treatment with this agent should be stopped.

Liver/Biliary: Serious hepatic toxicity has been reported in patients with severe underlying disease. Rare cases of fatalities, elevated alkaline phosphatase, elevated bilirubin, elevated SGOT, elevated SGPT have been observed.

Dosage & Administration

Therapy for infections requiring multiple dose treatment should be continued untiI laboratory tests and clinical parameters indicate that active fungal infection has subsided. An insufficient duration of fluconazole therapy may lead to the recurrence of active infection.
Maintenance therapy in patients with AIDS and cryptococcal meningitis or recurrent oropharyngeal candidiasis is usually necessary to prevent relapse.

Use in Adult
1. Cryptococcal meningitis may be treated with an initial dose of fluconazole 400 mg on the first day followed by 200 mg once daily. This dose may be increased to 400 mg daily, depending on the clinical response of the patient. The duration of therapy for cryptococcal meningitis is based on clinical and mycological response, but is usually 6- 8 weeks. Fluconazole may also be used in daily doses of 100 to 200 mg to prevent relapse following a primary course of antifungal therapy for acute cryptococcal meningitis in patients with AIDS.

2. Systemic candidiasis may be treated with an initial dose of fluconazole 400 mg on the first day followed by 200 mg daily. The dose may be increased to 400 mg daily, depending on the clinical response of the patient. Duration of therapy for systemic candidiasis treatment is based on the clinical response of the patient.

3. Fluconazole 150 mg should be administered as a single oral dose for vaginal candidiasis. A 150 mg once monthly dose may be used to reduce the incidence of recurrent vaginal candidiasis. Individualisation of the duration of therapy is necessary but ranges from 4-12 months. Some patients may require more frequent dosing. Fluconazole 150 mg should be administered as a single oral dose, for the treatment of candida balanitis.

Use in Elderly
Normal dosage recommendations should be adopted where there is no evidence of renal impairment.

Use in Children
Fluconazole is administered as a single daily dose. Fluconazole is excreted slowly in neonates. In the first two weeks of life the same mg/kg dosing as in older children should be used but administered every 72 hours. The same dose should be given every 48 hours, during weeks 3 and 4 of life.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT 
Overdosage with fluconazole has been reported.
In one case a 42 year-old patient infected with HIV developed hallucinations and exhibited paranoid behaviour after reportedly ingesting 8200 mg of fluconazole.
The patient was admitted to hospital and his condition resolved within 48 hours.

Storage/Handling Recommendations

Store in a cool, dry & dark place. Protect from direct sunlight.

Do not use in pregnancy. Keep all medicines out of reach of children.

Review Date

2017-08-21 01:57:50