(gri see oh FUL vin)
- Griseofulvin Microsize
- Griseofulvin Ultramicrosize
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Generic: 125 mg/5 mL (118 mL, 120 mL)
Grifulvin V: 500 mg [DSC] [scored]
Gris-PEG: 125 mg, 250 mg [scored]
Generic: 125 mg, 250 mg, 500 mg
Brand Names: U.S.
- Grifulvin V [DSC]
- Antifungal Agent, Oral
Inhibits fungal cell mitosis at metaphase; binds to human keratin making it resistant to fungal invasion
Ultramicrosize griseofulvin absorption is almost complete; absorption of microsize griseofulvin is variable (25% to 70% of an oral dose); enhanced by ingestion of a fatty meal (GI absorption of ultramicrosize is ~1.5 times that of microsize); absorbed from the duodenum
Deposited in the keratin layer of skin, hair, and nails; concentrates in liver, fat, and skeletal muscles; Vd: ~1.5 L (Vozeh 1988)
Urine (<1% as unchanged drug); feces; perspiration
Time to Peak
Serum: 4 hours
Use: Labeled Indications
Treatment of tinea infections of the skin, hair, and nails caused by susceptible species of Microsporum, Epidermophyton, or Trichophyton
Hypersensitivity to griseofulvin or any component of the formulation; liver failure; porphyria; pregnancy
Children >2 years:
Microsize: 10-20 mg/kg/day in single or 2 divided doses (maximum: 1000 mg daily) (Red Book, 2012)
Tinea capitis: Higher dosages (20-25 mg/kg/day) have been recommended (Ali, 2007; Lipozenic, 2002; Sethi, 2006)
Ultramicrosize: 5-15 mg/kg/day in single dose or 2 divided doses (maximum: 750 mg daily) (Red Book, 2012)
Tinea corporis, tinea cruris, tinea capitis: 500 mg daily in single or divided doses
Tinea pedis, tinea unguium: 1000 mg daily in single or divided doses
Ultramicrosize: 375 mg daily in single or divided doses; doses up to 750 mg daily in divided doses have been used for infections more difficult to eradicate such as tinea unguium and tinea pedis
Duration of therapy depends on the site of infection: Children and Adults:
Tinea corporis: 2-4 weeks
Tinea cruris: 2-6 weeks (Red Book, 2012)
Manufacturer's labeling: 4-6 weeks
Alternate recommendations: Children: 6-12 weeks; use up to 16 weeks may be required (AAP Red Book® recommends continuing treatment for 2 weeks after clinical resolution of symptoms) (Ali, 2007; Lipozenic, 2002; Sethi, 2006)
Tinea pedis: 4-8 weeks
Tinea unguium: 4-6 months or longer
Oral: Administer with a fatty meal (peanut butter or ice cream) to increase absorption, or with food or milk to avoid GI upset (Red Book, 2012)
Gris-PEG® tablets: May be swallowed whole or crushed and sprinkled onto 1 tablespoonful of applesauce and swallowed immediately without chewing.
Suspension: Shake well before use.
Suspension: Store at 20°C to 25°C (68°F to 77°F).
Ultramicrosize tablets: Store at 15°C to 30°C (59°F to 86°F)
Alcohol (Ethyl): Griseofulvin may enhance the adverse/toxic effect of Alcohol (Ethyl). A disulfiram-like reaction may occur. Monitor therapy
Barbiturates: May decrease the serum concentration of Griseofulvin. Exceptions: Methohexital; Thiopental. Monitor therapy
Carbocisteine: Griseofulvin may enhance the adverse/toxic effect of Carbocisteine. Specifically, griseofulvin may enhance adverse effects of alcohol that is present in liquid formulations of carbocisteine-containing products. Monitor therapy
Contraceptives (Estrogens): Griseofulvin may increase the metabolism of Contraceptives (Estrogens). Contraceptive failure is possible. Management: Use an alternative, nonhormonal form of contraception, or use an alternative to griseofulvin. Consider therapy modification
Contraceptives (Progestins): Griseofulvin may diminish the therapeutic effect of Contraceptives (Progestins). Contraceptive failure is possible. Avoid combination
CycloSPORINE (Systemic): Griseofulvin may decrease the serum concentration of CycloSPORINE (Systemic). Monitor therapy
Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Monitor therapy
Saccharomyces boulardii: Antifungal Agents (Systemic, Oral) may diminish the therapeutic effect of Saccharomyces boulardii. Avoid combination
Ulipristal: Griseofulvin may decrease the serum concentration of Ulipristal. Avoid combination
Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Monitor therapy
Vitamin K Antagonists (eg, warfarin): Griseofulvin may decrease the serum concentration of Vitamin K Antagonists. Monitor therapy
False-positive urinary VMA levels
Frequency not defined.
Central nervous system: Dizziness, fatigue, headache, insomnia, mental confusion
Dermatologic: Angioneurotic edema (rare), erythema multiforme-like drug reaction, photosensitivity, rash (most common), urticaria (most common),
Gastrointestinal: Diarrhea, epigastric distress, GI bleeding, nausea, vomiting
Hematologic: Granulocytopenia, leukopenia (rare)
Neuromuscular & skeletal: Paresthesia (rare)
Renal: Nephrosis, proteinuria (rare)
Miscellaneous: Drug-induced lupus-like syndrome (rare), oral thrush
Postmarketing and/or case reports: Bilirubin increased, liver transaminases increased, Stevens-Johnson syndrome, toxic epidermal necrolysis
Concerns related to adverse effects:
• Hematologic effects: Discontinue therapy if granulocytopenia occurs.
• Hepatic effects: May cause jaundice and elevated liver function tests or bilirubin (may be serious or even fatal); discontinue therapy if necessary.
• Penicillin allergy: Hypersensitivity cross reaction between penicillins and griseofulvin is possible.
• Photosensitivity: Avoid exposure to intense sunlight to prevent photosensitivity reactions.
• Skin reactions: Severe skin reactions (eg, Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme) have been reported (may be serious or even fatal); discontinue use if severe skin reactions occur.
• Appropriate use: Use for the prophylaxis of fungal infections has not been established; not effective for the treatment of tinea versicolor.
Periodic renal, hepatic, and hematopoietic function tests especially with long-term use
Pregnancy Risk Factor
Teratogenic effects have been observed in animal reproduction studies. Griseofulvin crosses the placenta (Pacifici, 2006). Because adverse events have also been observed in humans (two cases of conjoined twins), use during pregnancy is contraindicated. Effective contraception should be used during therapy and for 1 month after therapy is discontinued in women of reproductive potential. Men should avoid fathering a child for at least 6 months after therapy.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience headache, dizziness, nausea, asthenia, insomnia, or diarrhea. Have patient report immediately to prescriber signs of hepatic impairment, illogical thinking, paresthesia, stomatitis, or signs of Stevens-Johnson syndrome/toxic epidermal necrolysis (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.
More about griseofulvin
- Griseofulvin (AHFS Monograph)
- Griseofulvin (FDA)
- Griseofulvin Tablets (FDA)
- Griseofulvin Ultramicrosize Tablets (FDA)