Griseofulviin (Microsize)

Uses

Major indications for griseofulvin are:

• Tinea capitis (ringworm of the scalp)
• Tinea corporis (ringworm of the body)
• Tinea pedis (athlete's foot)
• Tinea unguium (onychomycosis; ringworm of the nails)
• Tinea cruris (ringworm of the thigh)
• Tinea barbae (barber's itch)

Griseofulviin (Microsize) inhibits the growth of those genera of fungi that commonly cause ringworm infections of the hair, skin, and nails, such as:

• Trichophyton rubrum
• Trichophyton tonsurans
• Trichophyton mentagrophytes
• Trichophyton interdigitalis
• Trichophyton verrucosum
• Trichophyton sulphureum
• Trichophyton schoenleini
• Microsporum audouini
• Microsporum canis
• Microsporum gypseum
• Epidermophyton floccosum
• Trichophyton megnini
• Trichophyton gallinae
• Trichophyton crateriform

Note: Prior to therapy, the type of fungi responsible for the infection should be identified. The use of the drug is not justified in minor or trivial infections which will respond to topical anti-fungal agents alone.

Griseofulviin (Microsize) is also used to associated treatment for these conditions: Tinea Capitis, Tinea Corporis, Tinea Cruris, Tinea Pedis, Tinea Unguium, Tinea barbae

How Griseofulviin (Microsize) works

Griseofulviin (Microsize) is fungistatic, however the exact mechanism by which it inhibits the growth of dermatophytes is not clear. It is thought to inhibit fungal cell mitosis and nuclear acid synthesis. It also binds to and interferes with the function of spindle and cytoplasmic microtubules by binding to alpha and beta tubulin. It binds to keratin in human cells, then once it reaches the fungal site of action, it binds to fungal microtubes thus altering the fungal process of mitosis.

Dosage

Griseofulviin (Microsize) dosage

Accurate diagnosis of the infecting organism is essential. Identification should be made either by direct microscopic examination of a mounting of infected tissue in a solution of potassium hydroxide or by culture on an appropriate medium.

Medication must be continued until the infecting organism is completely eradicated as indicated by appropriate clinical or laboratory examination. Representative treatment periods are tinea capitis, 4 to 6 weeks; tinea corporis, 2 to 4 weeks; tinea pedis, 4 to 8 weeks; tinea unguium- depending on rate of growth- fingernails, at least 4 months; toenails, at least 6months.

General measures in regard to hygiene should be observed to control sources of infection or reinfection. Concomitant use of appropriate topical agents is usually required, particularly in treatment of tinea pedis since in some forms ofathlete's foot, yeasts and bacteria may be involved. Griseofulviin (Microsize) will not eradicate the bacterial or monilial infection.

Adults:A daily dose of 500 mg will give a satisfactory response in most patients with tinea corporis, tinea cruris, and tinea capitis. For those fungus infections more difficult to eradicate such as tinea pedis and tinea unguium, a daily dose of 1.0gmis recommended.

Children: Approximately 5 mg per pound of body weight per day is aneffective dosefor most children. On this basis the following dosage schedule for children is suggested:

• Children weighing 30 to 50 pounds:125 mg to 250 mg daily.
• Children weighing over 50 pounds:250 mg to 500 mg daily.

Should be taken with food. Take immediately after meals.

Side Effects

When adverse reactions occur, they are most commonly of the hypersensitivity type such as skin rashes, urticaria and rarely, angioneurotic edema or erythemamultiforme-like drug reaction, and may necessitate withdrawal of therapy and appropriate countermeasures. Paresthesias of the hands and feet have been reported rarely after extended therapy. Other side effects reported occasionally are oral thrush, nausea, vomiting, epigastric distress, diarrhea, headache, fatigue, dizziness, insomnia, mental confusion and impairment of performance of routine activities.

Proteinuria and leukopenia have been reported rarely. Administration of the drug should be discontinued if granulocytopenia occurs. When rare, serious reactions occur with griseofulvin, they are usually associated with high dosages, long periods of therapy, or both.

Toxicity

Side effects are minor: headaches, gastrointestinal reactions and cutaneous eruptions

Precaution

Patients on prolonged therapy with any potent medication should be under close observation. Periodic monitoring of organ system function, including renal, hepaticand hemopoietic, should be done.

Since griseofulvin is derived from species of penicillin, the possibility of cross sensitivity with penicillin exists; however, known penicillin-sensitive patients have been treated without difficulty.

Since a photosensitivity reaction is occasionally associated with griseofulvin therapy, patients should be warned to avoid exposure to intense natural or artificial sunlight. Should a photosensitivity reaction occur, lupus erythematosus may be aggravated.

Interaction

Patients on warfarin-type anticoagulant therapy may require dosage adjustment of the anticoagulant during and after griseofulvin therapy. Concomitant use of barbiturates usually depresses griseofulvin activity and may necessitate raising the dosage.

The concomitant administration of griseofulvin has been reported to reduce the efficacy of oral contraceptives and to increase the incidence of breakthrough bleeding.

Food Interaction

• Avoid alcohol.
• Take with a high fat meal.

[Moderate] MONITOR: Isolated case reports have suggested that the ingestion of alcohol during griseofulvin therapy may rarely cause disulfiram-like reactions, flushing, tachycardia, or increased effects of alcohol.

The mechanism is unknown.

MANAGEMENT: Patients should be advised of the possibility of increased adverse effects or a disulfiram-like reaction.

Griseofulviin (Microsize) Drug Interaction

Moderate: montelukast, montelukastMinor: aspirin, aspirinUnknown: ginkgo, ginkgo, acetaminophen, acetaminophen, valproic acid, valproic acid, thiamine, thiamine, pyridoxine, pyridoxine, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, cetirizine, cetirizine

Griseofulviin (Microsize) Disease Interaction

Major: hepatic dysfunction, porphyriaModerate: lupus erythematosus

Elimination Route

Poorly absorbed from GI ranging from 25 to 70% of an oral dose. Absorption is significantly enhanced by administration with or after a fatty meal.

Half Life

9-21 hours

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Contraindication

This drug is contraindicated in patients with porphyria, hepatocellular failure, and in individuals with a history of hypersensitivity to griseofulvin.

Two cases of conjoined twins have been reported in patients taking griseofulvin during the first trimester of pregnancy. Griseofulviin (Microsize) should not be prescribed to pregnant patients.

Storage Condition

Store between 15-30° C.

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