Griseofulvin

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Indications

  • Dermatophyte infections of the skin, scalp, and nails.
  • Tinea pedis (moccasin type)/tinea manuum(adults): 750–1000 mg/day (microsize) or 500–750 mg/day (ultramicrosize) × 4 weeks.
  • Tinea pedis (moccasin type)/tinea manuum(children):15–20 mg/kg/day (microsize suspension) × 4 weeks.
  • Tinea unguium (adults):1–2 g/day (microsize) or 750 mg/day (ultramicrosize) until nails are normal.
  • Tinea unguium (children) :20 mg/kg/day (microsize suspension) until nails are normal.
  • Tinea corporis (extensive, adults) :500–1000 mg/day (microsize) or 375–500 mg/day (ultramicrosize) × 2–4 weeks.
  • Tinea corporis (extensive, children):15–20 mg/kg/day (microsize suspension) × 2–4 weeks.
  • Tinea capitis (adults):10–15 mg/kg/day (ultramicrosize; usually maximum 750 mg/day) ×6–8 weeks.
  • Tinea capitis (children):20–25 mg/kg/day (microsize suspension) × 6–8 weeks.
  • Tinea imbricata :500 mg twice daily for 4–6 weeks.
  • Tinea barbae :Micronized or ultramicronized griseofulvin,500–1000 mg/day or 500–750 mg/day po,respectively, for 4–6 weeks.
  • Majocchi granuloma.

others

  • Lichen planus : 3 to 6 months.
  • Erythema dyschromicum perstans.
  • WELLS syndrome.

Follow Up Monitoring

With prolonged use :

  • Complete blood count.
  • Liver functions.

Side effects

  • COMMON
    • Urticaria.
    • Nausea, headache, confusion, vomiting, diarrhea, flatulence, increased thirst.
    • Candidiasis.
    • Photosensitivity.
    • Lupus-like reaction.
    • Estrogenic effects.
    • Paresthesias.
    • Dizziness, fatigue, insomnia,proteinuria.
  • RARE
    • Fixed drug eruptions.
    • Granulocytopenia.
    • Hepatotoxicity.
    • Neutropenia.
    • Nephrotoxicity.
    • Erythema multiforme.
    • Angioedema.
    • Mental confusion.

Contraindications

  • Hypersensitivity to drug/class.
  • Porphyria.
  • Pregnancy.
  • Penicillin allergy.
  • Impaired liver function.
  • Lupus erythematosus.

Mechanism of action

  • Fungistatic and anti-inflammatory agent that deposits in the keratinocytes, which are gradually exfoliated and replaced by new, uninfected cells.
  • It disrupts mitotic spindle by interacting with microtubules, thereby inhibiting mitosis in dermatophytes.

Interactions

  • Decreased levels of: alfentanil, amiodarone, aprepitant, aripiprazole, bortezomib, bosentan, buprenorphine, benzodiazepines, carbamazepine, calcium channel blockers, clarithromycin, oral contraceptives, cyclosporin, delavirdine, disopyramide, efavirenz, erythromycins, fentanyl, geftinib, itraconazole, ketoconazole, levonorgestrel, paclitaxel, protease inhibitors, repaglinide, sirolimus, statins, tacrolimus, voriconazole, warfarin,salicylates, zonisamide.
  • Decreased levels of griseofulvin: barbiturates.
  • Disulfiram reaction: ethanol.

Pregnancy &Lactation

  • Pregnancy category x.
  • Rare cases of conjoined twins have been reported in women taking griseofulvin in the frst trimester of pregnancy.
  • Excretion in milk is unknown, avoid use because of potential tumorigenicity.

Precautions

  • Patients should avoid pregnancy for at least 1 month after discontinuing griseofulvin.
  • Severe skin reactions (eg, Stevens-Johnson syndrome, toxic epidermal necrolysis) and erythema multiforme reported, some resulting in hospitalization or death; discontinue if severe skin reaction occurs.
  • Elevations in AST, ALT, bilirubin, and jaundice reported, some resulting in hospitalization or death; discontinue if jaundice occurs.
  • During prolonged griseofulvin therapy, periodic assessment of renal, hepatic, and hematopoietic functions should be performed.
  • It may increase estrogen metabolizing liver enzymes, which may make oral contraceptives less effective or cause menstrual irregularities.

Drug Info

  • The duration of therapy depends on the organism (e.g., T. tonsurans infections may require prolonged treatment schedules) but varies between 8 and 10 weeks.
  • Shorter courses may lead to higher relapse rates.
  • Griseofulvin is not effective in the treatment of pityriasis (tinea) versicolor, bacterial infections, candidiasis (moniliasis), or deep mycotic infections.
  • Resistance to griseofulvin among dermatophytes is rare.
  • Absorption of griseofulvin is improved when given with whole milk or ice cream.
  • Drug particle size reduction through micronization and ultra-micronization has signifcantly enhanced oral absorption.


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