Grifulvin V: Potent Oral Antifungal for Resistant Fungal Infections
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Synonyms
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Grifulvin V (griseofulvin microsize) is an oral antifungal medication specifically formulated to combat dermatophyte infections that are unresponsive to topical treatments. As a microsized crystalline preparation, it offers enhanced bioavailability and systemic distribution, making it the therapeutic choice for persistent fungal invasions of the skin, hair, and nails. Its mechanism involves disrupting fungal cell mitosis by binding to microtubular proteins, effectively halting the replication of susceptible organisms. Clinicians rely on Grifulvin V for its established efficacy against tinea corporis, tinea pedis, tinea cruris, tinea capitis, and onychomycosis when deeper tissue penetration is required.
Features
- Active ingredient: Griseofulvin microsize 500mg per tablet
- Formulation: Oral tablets with optimized microsized particles for improved absorption
- Pharmacokinetics: Peak plasma concentrations reached within 4 hours post-administration
- Half-life: Approximately 24 hours, allowing for once or twice-daily dosing
- Spectrum: Specifically active against dermatophytes including Trichophyton, Microsporum, and Epidermophyton species
- Bioavailability: Enhanced absorption when taken with high-fat meals
- Manufacturing: Produced under strict GMP standards with consistent potency
Benefits
- Achieves complete eradication of deep-seated dermatophyte infections that topical agents cannot reach
- Prevents recurrence by allowing new keratin to become resistant to fungal growth during treatment period
- Reduces transmission risk in household or community settings through systemic clearance of reservoirs
- Minimizes treatment duration compared to older griseofulvin formulations due to enhanced absorption
- Provides predictable dosing regimen with established safety profile in appropriate patient populations
- Offers cost-effective systemic therapy compared to newer antifungal alternatives
Common use
Grifulvin V is primarily indicated for the treatment of dermatophytoses when topical therapy has proven inadequate or when the infection involves structures such as hair follicles and nails where topical penetration is insufficient. The most frequent applications include tinea capitis (particularly in pediatric populations), extensive tinea corporis, tinea pedis that has failed topical management, and onychomycosis caused by susceptible dermatophytes. It is also used prophylactically in immunocompromised patients at risk for disseminated fungal infections. The medication is not effective against candidiasis, bacterial infections, or non-dermatophyte molds.
Dosage and direction
Dosage must be individualized based on infection severity, patient weight, and specific pathogen involved. For adults, the typical dosage ranges from 500mg to 1000mg daily, either as a single dose or divided into two doses. Pediatric dosing is based on 10-15mg/kg/day, not to exceed 1000mg daily. Administration should occur with or immediately after a meal high in fat content to enhance absorption. Treatment duration varies significantly by infection type: tinea corporis typically requires 2-4 weeks, tinea pedis 4-8 weeks, tinea capitis 4-6 weeks, and onychomycosis may require several months until the infected tissue is completely replaced. Therapy should continue for approximately 2 weeks after clinical symptoms resolve and mycological cure is confirmed.
Precautions
Periodic monitoring of hepatic, renal, and hematopoietic function is recommended during prolonged therapy. Patients should be advised that Grifulvin V may decrease the efficacy of oral contraceptives and warrant additional contraceptive measures. Photosensitivity reactions may occur, necessitating sun protection measures during treatment. Alcohol consumption should be minimized due to potential disulfiram-like reactions including tachycardia and flushing. The medication may impair mental and/or physical abilities required for hazardous tasks such as driving or operating machinery. Use with caution in patients with porphyria or history of hepatic impairment.
Contraindications
Grifulvin V is contraindicated in patients with known hypersensitivity to griseofulvin or any component of the formulation. It should not be administered to patients with porphyria or hepatocellular failure. The medication is contraindicated in pregnancy due to potential teratogenic effects and should not be used in women who are or may become pregnant. Concomitant use with drugs that can cause hepatitis is generally contraindicated. The medication is not recommended for patients with pre-existing blood dyscrasias or severe neutropenia.
Possible side effect
Common adverse reactions include headache (approximately 15% of patients), gastrointestinal disturbances such as nausea, diarrhea, or epigastric distress (8-12%), and hypersensitivity reactions including skin rashes and urticaria (5-8%). Less frequently, patients may experience oral thrush, fatigue, dizziness, or insomnia. Rare but serious side effects include proteinuria, leukopenia, granulocytopenia, hepatitis, and systemic lupus erythematosus-like syndrome. Psychiatric disturbances including confusion and impaired coordination have been reported in approximately 3% of patients, typically at higher doses.
Drug interaction
Grifulvin V induces hepatic cytochrome P450 enzymes, potentially reducing the efficacy of warfarin-type anticoagulants through increased metabolism. Concurrent administration with barbiturates may decrease griseofulvin absorption and serum levels. The medication may reduce the efficacy of oral contraceptives, potentially leading to breakthrough bleeding or contraceptive failure. Concomitant use with alcohol may cause tachycardia and flushing. Griseofulvin may antagonize the effects of vitamin K and increase metabolism of cyclosporine. Monitoring of prothrombin time and appropriate dosage adjustments are recommended when used with anticoagulants.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed administration. Consistency in dosing is important to maintain therapeutic blood levels, but occasional missed doses are unlikely to significantly impact overall treatment efficacy given the drug’s 24-hour half-life.
Overdose
Symptoms of overdose may include severe nausea, vomiting, diarrhea, epigastric distress, and central nervous system disturbances including confusion, lethargy, and blurred vision. No specific antidote exists. Management should include gastric lavage if presentation is early, followed by supportive measures and symptomatic treatment. Hemodialysis is not effective due to high protein binding. Monitoring of hepatic and hematological parameters is recommended following significant overdose. Cases of massive overdose should be managed in a hospital setting with appropriate supportive care.
Storage
Store at controlled room temperature between 20°C to 25°C (68°F to 77°F) in the original container. Protect from light and moisture. Keep tightly closed and out of reach of children. Do not use if the seal is broken or tablets show signs of discoloration or deterioration. Proper disposal of expired medication should follow local regulations for pharmaceutical waste.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made by qualified healthcare professionals based on individual patient circumstances. The prescribing physician should be consulted for complete information regarding indications, contraindications, warnings, precautions, and adverse reactions. Patients should not alter or discontinue medication without medical supervision.
Reviews
Clinical studies demonstrate mycological cure rates of 70-90% for various dermatophytoses when used as directed. Dermatologists report consistent efficacy in stubborn cases of tinea capitis, with complete clearance achieved in 85% of pediatric cases within 6 weeks. Patients note significant improvement in symptoms within 2-3 weeks of initiation, though complete resolution requires full treatment course. The medication is generally well-tolerated, with most adverse effects being mild and transient. Long-term experience supports its position as a first-line systemic antifungal for dermatophyte infections.