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Griseofulvin 250 mg Tablets (Grifulvin)

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Griseofulvin is authorised in the world under the following brand names: Amudane, Biogrisin-fp, Curling factor, Delmofulvina, Fulcin, Fulcine, Fulvican grisactin, Fulvicin, Fulvicin P/G, Fulvicin U/F, Fulvina, Fulvinil, Fulvistatin, Fungivin, Greosin, Gresfeed, Gricin, Grifulin, Grifulvin, Grifulvin V, Gris-PEG, Grisactin, Grisactin Ultra, Griscofulvin, Grisefuline, Griseo, Griseofulvin forte, Griseomix, Grisetin, Grisofulvin, Grisovin, Grisovin FP, Grizeofulvin, Grysio, Guservin, Lamoryl, Likuden, Likunden, Murfulvin, Neo-Fulcin, Neocid, Poncyl, Spirofulvin, Sporostatin, Sporostatin xan, Xuanjing.

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Griseofulvin is an antifungal antibiotic derived from a number of Penicillium species. It was the first oral drug for treatment of dermatophytosis.

Mechanism of action

Griseofulvin is a fungistatic drug which binds to microtubular proteins and inhibits fungal cell mitosis. It also acts as an inhibitor of nucleic acid synthesis.

Griseofulvin: Spectrum of action

Griseofulvin has a limited spectrum of action which is almost restricted to the dermatophytes (Epidermophyton floccosum, Microsporum species and Trichophyton species). Its clinical use is limited to these infections. It is ineffective in cutaneous candidosis and pityriasis versicolor.

Acquired resistance

Treatment failure attributable to the development of griseofulvin resistance is an uncommon problem in patients with dermatophytoses.

Pharmacokinetics of Griseofulvin 250 mg (Grifulvin 250 mg)

Absorption of griseofulvin from the gastrointestinal tract is dependent on drug formulation. Administration of the drug with a high fat meal will increase the rate and extent of absorption, but individual patients tend to achieve consistently high or low serum concentrations. Four hours after a single 1000-mg dose, blood levels in the region of 0-3.75 mg/1 can be anticipated.

Griseofulvin appears in the stratum corneum within 4-8 h of oral administration, as a result of drug secretion in perspiration. However, levels begin to fall soon after the drug is discontinued and within 48-72 h it can no longer be detected. The mechanisms by which griseofulvin is delivered to the hair and nails are not well understood: deposition in newly formed cells is thought to be the major factor.

Metabolism of Griseofulvin 250 mg (Grifulvin 250 mg)

Griseofulvin is metabolized by the liver to 6-desmethyl griseofulvin which is excreted in the urine. The drug has an elimination half-life from 9 to 21 h. Less than 1% of a given dose appears in the urine in unchanged form.

Pharmaceutics of Griseofulvin 250 mg

Griseofulvin is available as oral tablets and oral suspension.

Therapeutic use of Griseofulvin 250 mg

Griseofulvin is indicated in moderate to severe dermatophytoses of the skin, scalp hair, or nails where topical treatment is considered inappropriate or has failed.

Griseofulvin: Mode of administration

It is important to adjust the dose to the weight of the patient. The adult dose can range from 500 to 1000 mg either as a single or divided doses; not less than 10 mg/kg should be given. The dose for children under 25kg is 10 mg/kg and 250-500 mg for children over 25 kg. It should be taken after meals.

The duration of treatment will differ from patient to patient and depend upon the nature and extent of the infection. For hair or skin at least 4 weeks of treatment is required. Long courses (usually 6-12 months) and high doses may be needed for nail infections. Long-term relapse rates are high; between 40 and 70% for toenails, but somewhat lower for fingernails.

Adverse reactions of Griseofulvin 250 mg (Grifulvin 250 mg)

In most cases, prolonged courses and high doses are well tolerated. Patients have complained of headaches, nausea, vomiting and abdominal discomfort. Urticarial reactions and erythematous rashes occur in occasional patients.

The drug is contraindicated in patients with liver disease as hepatic function may deteriorate and the risk of other side-effects is increased.

Drug interactions of Griseofulvin 250 mg

Griseofulvin has been shown to stimulate the metabolism of warfarin, thus reducing its anticoagulant effect. Absorption is reduced in patients receiving concomitant treatment with phenobarbitone, but the effect can be reduced by administration of griseofulvin with food. Failure of contraception has been reported in patients taking griseofulvin and oral contraceptive steroids.

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Dosage forms of Griseofulvin:
Griseofulvin powder Gris-peg 125 mg tablet Gris-peg 250 mg tablet Grifulvin v 500 mg tablet
Griseofulvin Microsize 125 mg/5ml Suspension 120ml Bottle

Synonyms of Griseofulvin:

Griseofulvina [INN-Spanish], Griseofulvine [INN-French], Griseofulvinum [INN-Latin]

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Therapeutic classes of Griseofulvin:

Antibacterial Agents, Antibiotics, Antifungal

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