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    Griseofulvin

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    Rhadezahara Patrisa
    Griseofulvin is a fungistatic drug used for the treatment of dermatophytes. It works by binding to tubulin and microtubule proteins, inhibiting cell division and causing apoptosis. It has low bioavailability and is absorbed in the duodenum, accumulating in keratin-producing tissues. The main indications are for tinea capitis and onychomycosis. Dosing is dependent on the condition and weight of the patient, and can cause side effects like hypersensitivity, photosensitivity, and neurological or liver issues. It should not be taken with phenobarbital due to interactions.

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    Griseofulvin

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    Rhadezahara Patrisa
    123 views1 page
    Griseofulvin is a fungistatic drug used for the treatment of dermatophytes. It works by binding to tubulin and microtubule proteins, inhibiting cell division and causing apoptosis. It has low bioavailability and is absorbed in the duodenum, accumulating in keratin-producing tissues. The main indications are for tinea capitis and onychomycosis. Dosing is dependent on the condition and weight of the patient, and can cause side effects like hypersensitivity, photosensitivity, and neurological or liver issues. It should not be taken with phenobarbital due to interactions.

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    Griseofulvin is a fungistatic drug used for the treatment of dermatophytes. It works by binding to tubulin and microtubule proteins, inhibiting cell division and causing apoptosis. It has low bioavailability and is absorbed in the duodenum, accumulating in keratin-producing tissues. The main indications are for tinea capitis and onychomycosis. Dosing is dependent on the condition and weight of the patient, and can cause side effects like hypersensitivity, photosensitivity, and neurological or liver issues. It should not be taken with phenobarbital due to interactions.

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    123 views1 page

    Griseofulvin

    Uploaded by

    Rhadezahara Patrisa
    Griseofulvin is a fungistatic drug used for the treatment of dermatophytes. It works by binding to tubulin and microtubule proteins, inhibiting cell division and causing apoptosis. It has low bioavailability and is absorbed in the duodenum, accumulating in keratin-producing tissues. The main indications are for tinea capitis and onychomycosis. Dosing is dependent on the condition and weight of the patient, and can cause side effects like hypersensitivity, photosensitivity, and neurological or liver issues. It should not be taken with phenobarbital due to interactions.

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    of 1

    Griseofulvin is a metabolic derivative of Penicillium griseofulvum, classically used for the treatment of

    dermatophytes. It has no activity against yeast and molds.8

    MECHANISM OF ACTION Griseofulvin is a fungistatic drug, blocking the growth and proliferation of the
    fungal cell. Griseofulvin binds tubulin- and microtubule-associated proteins (MAPs) along the
    polymerized microtubules, suppressing the formation of the mitotic spindle at the G2/M phase of the
    cell cycle. This inhibits cell division and forces the cell to undergo apoptosis.48

    PHARMACOKINETICS Griseofulvin is a water-insoluble drug, known for its low bioavailability profile.
    Most of the drug absorption occurs in the duodenum, and better absorption of griseofulvin can occur
    either when coated with polyethylene glycol or on coadministration with fatty meals.49,50 Griseofulvin
    is characterized by its accumulation in the keratin-producing tissues, where it is adherently bound to
    newly formed keratin, rendering it resistant to fungal penetration. The 6-desmethyl enzyme is
    responsible for the metabolism of griseofulvin in the liver. The cutaneous elimination of the drug is
    slower than its elimination from plasma, allowing for extended drug activity even after its
    discontinuation. Griseofulvin is eliminated from the body mainly through the kidney in the form of
    metabolites.

    INDICATIONS Griseofulvin remains the first line of treatment for tinea capitis caused by Microsporum
    species owing to its higher efficacy compared to terbinafine, and similar efficiency yet lower cost
    compared to itraconazole and fluconazole.19 It is also the only FDA-approved treatment for pediatric
    onychomycosis, though its efficacy is limited to dermatophytes only (Table 188-2).15

    DOSAGE AND FORMULATIONS Griseofulvin is available in the following formulations: 250- and 500-mg
    microsize and 125-, 165-, and 250-mg ultramicrosize tablets, and 125-mg/5-mL oral suspensions.8
    Griseofulvin is recommended at a daily dose of 1-g microsize, or 660- to 750-mg ultramicrosize for 4 to 8
    weeks in the treatment of tinea pedis and half of these doses for the treatment of tinea cruris and
    corporis. The recommended daily dosing of griseofulvin for the treatment of tinea capitis in children is
    dependent on their body weight and is as follows: ultramicrosize 10 to 15 mg/kg, oral suspension 15 to
    25 mg/kg, microsize 20 to 25 mg/kg, continued for 1 to 2 months (Table 188-2).3

    SIDE EFFECTS The main side effects associated with griseofulvin are related to hypersensitivity, which
    ranges from mild urticaria, serum sickness, acute generalized exanthematous pustulosis, subacute
    cutaneous lupus erythematous, Stevens–Johnson syndrome, and toxic epidermal necrolysis.
    Photosensitivity, including photo-toxic and photo-allergic reactions, also has been commonly reported
    with griseofulvin.51 Other cutaneous eruptions include lichenoid eruption, porphyria, and pityriasis
    rosea.12,13 Rare but serious side effects include hepatotoxicity, leukopenia, thrombocytopenia, and
    anemia.51 Neurologic problems such as peripheral neuritis, memory loss, confusion, and insomnia were
    uncommonly recorded in some patients (Table 188-3).52,53

    DRUG–DRUG INTERACTIONS Griseofulvin should not be prescribed concurrently with phenobarbitone


    because it decreases the absorption and increases the metabolism of griseofulvin.44 Interactions with
    alcohol, cyclosporine, oral contraceptives, aspirin, and warfarin also have been reported (Table 188-
    4).54-56

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