Afluzole Capsule, Oral Suspension
Afluzole is the first of a new subclass of synthetic triazole antifungal agent which acts by inhibition of the ergosterol component of the fungal cell membrane. It is active against a broad spectrum of fungal pathogens and is available for oral use.
Afluzole is used for
- Superficial candidal infections such as oral or vaginal thrush
- Esophagitis caused by Candida or other susceptible species
- Maintenance therapy of cryptococcal meningitis
- Disseminated candidiasis
- Prophylaxis for fungal infection in neutropenic cancer patients
- Acute treatment of other systemic fungal infections
- Dermatophyte and Candida skin infections
- Fungal UTIs
Afluzole is also used to associated treatment for these conditions: Candida intertrigo, Candida pneumonia, Candida urinary tract infection, Candidemia, Candidiasis, Coccidioidomycosis, Esophageal Candidiasis, Fungal peritonitis caused by Candida, Infections, Fungal, Meningitis, Cryptococcal, Oropharyngeal Candidiasis, Peritoneal candidiasis, Pneumonia cryptococcal, Pruritus, Skin Irritation, Systemic Candida Infections caused by Candida, Vaginal Candidiasis, Disseminated Candidiasis
|Other Names||Diflucan, Difluconazole, Fluconazol, Fluconazole, Fluconazolum, Triflucan|
|Weight||50mg, 150mg, 50mg/5ml|
|Type||Capsule, Oral Suspension|
The protein binding of fluconazole is low and estimated to be 11 to 12%.
|Therapeutic Class||Drugs for cutaneous mycoses, Drugs for subcutaneous and systemic mycoses|
|Manufacturer||Ambee Pharmaceuticals Ltd|
|Last Updated:||June 23, 2021 at 11:21 am|
Table Of contents
- Oropharyngeal Candidiasis: 200 mg on the first day, followed by 100 mg once daily for 7-14 days.
- Esophageal Candidiasis: 200 mg on the first day, followed by 100 mg once daily for 2-3 weeks.
- Systemic Candidiasis and Cryptococcal Meningitis: 400 mg daily followed by 200 mg once daily. The recommended duration of treatment for initial therapy of cryptococcal meningitis is 10 to 12 weeks.
- Acute or recurrent vaginal candidiasis: Single dose of 150 mg.
- Urinary Tract Infections and Peritonitis: 50 to 200 mg once daily. Prophylaxis in Patients Undergoing Bone Marrow Transplantation: 400 mg once daily.
- Oropharyngeal Candidiasis: 6 mg/kg on the first day, followed by 3 mg/kg once daily. Treatment should be administered for at least 2 weeks to decrease the likelihood of relapse.
- Esophageal Candidiasis: 6 mg/kg on the first day, followed by 3 mg/kg once daily.
- Cryptococcal meningitis: Initial therapy should be started with 6 to 12 mg/kg daily. Doses up to 12 mg/kg/day may be used for three weeks and treatment for initial therapy of cryptococcal meningitis is 10 to 12 weeks.
Adult & child:
Invasive candidal infections including candidaemia and disseminated candidiasis and cryptococcal infections including meningitis, by IV, 400 mg initially then 200 mg daily, increased if necessary to 400 mg daily, treatment continued according to response (at least 6-8 weeks for cryptococcal meningitis); Child 6-12 mg/kg daily (every 72 hours in neonate up to 2 weeks old, every 48 hours in neonate 2-4 weeks old); maximum 400 mg daily.Prevention of relapse of cryptococcal meningitis, by IV, 100-200 mg daily.
Since oral absorption is rapid and almost complete, the daily dose of Afluzole is the same for oral and intravenous administration.
Therapy with Afluzole is well tolerated. The common adverse effects are nausea. abdominal pain, vomiting, diarrhoea, headache and skin rash.
Caution should be taken in renal impairment, pregnancy and breast feeding and in raised liver enzymes. The use of Afluzolein lactating mothers is not recommended.
Rifampicin reduces plasma concentration of Afluzole. Afluzole enhances the effect of nicoumalone, warfarin and phenytoin. It also increases the plasma concentration of sulphonylureas & theophlline.
- Take with or without food. The absorption is unaffected by food.
Volume of Distribution
The apparent volume of distribution is said to be similar to the volume of distribution of total body water. One clinical study of healthy volunteers administered 50 mg/kg of fluconazole was 39L, based on a body weight of 60kg.
Afluzole shows substantial penetration in many body fluids, which is a property that renders it an ideal treatment for systemic fungal infections, especially when administered over a longer time. Afluzole is found in high concentrations in the stratum corneum and dermis-epidermis of skin, in addition to eccrine sweat. Afluzole is found to accumulate especially well in the stratum corneum, which is beneficial in superficial fungal infections.[L6496] Saliva and sputum concentrations of fluconazole are found to be similar to the plasma concentrations. In patients diagnosed with fungal meningitis, fluconazole CSF (cerebrospinal fluid) levels are measured to be about 80% of the corresponding plasma levels. Therefore, fluconazole crosses the blood-brain barrier[L6496]. The meninges are increasingly permeable to fluconazole in states of inflammation, facilitating treatment in meningitis.
The terminal elimination half-life in the plasma is approximately 30 hours (range: 20-50 hours) after oral administration. The long plasma elimination half-life supports a single dose therapy for vaginal candidiasis, once daily and once weekly dosing for other indications.[L6496]. Patients with renal failure may require dosage adjustment, and half-life can be significantly increased in these patients.
This drug is mainly eliminated by the kidneys and the mean body clearance in adults is reported to be 0.23 mL/min/kg. One clinical study of healthy subjects showed total clearance of 19.5 ± 4.7 mL/min and renal clearance of 14.7 ± 3.7 mL/min (1.17 ± 0.28 and 0.88 ± 0.22 L/h).
Clearance in the pediatric population varies according to age, as does clearance in patients with renal failure.
Pregnancy & Breastfeeding use
Use in pregnancy: Afluzole should be used in pregnancy only if the potential benefit justifies the possible risk to the foetus.Use in lactation: Afluzole is secreted in human milk at concentrations similar to plasma. Therefore, the use of Flouconazole in nursing mother is not recommended.
Afluzole is contraindicated to patients hypersensitive to this drug and in advanced liver disease.
Store below 30° C. Protect from light & moisture. Remaining reconstituted suspension should not be used after 7 days. If it is kept under freezing temperature (2- 8° C) , it can be used for 14 days. Keep out of the reach of children.
In the case of an overdose, supportive measures should be instituted.