Griseofulvin

Pronunciation

(gri see oh FUL vin)

U.S. Brand Names

Grifulvin® V; Gris-PEG®

Synonyms

Griseofulvin Microsize; Griseofulvin Ultramicrosize

Generic Available

Yes: Ultramicrosized product

Canadian Brand Names

Fulvicin® U/F

Use

Treatment of susceptible tinea infections of the skin, hair, and nails

Pregnancy Risk Factor

Lactation

Excretion in breast milk unknown

Contraindications

Hypersensitivity to griseofulvin or any component of the formulation; severe liver disease; porphyria (interferes with porphyrin metabolism)

Warnings/Precautions

Safe use in children

2 years of age has not been established; during long-term therapy, periodic assessment of hepatic, renal, and hematopoietic functions should be performed; may cause fetal harm when administered to pregnant women; avoid exposure to intense sunlight to prevent photosensitivity reactions; hypersensitivity cross reaction between penicillins and griseofulvin is possible

Adverse Reactions

Frequency not defined.

Central nervous system: Headache, fatigue, dizziness, insomnia, mental confusion

Dermatologic: Rash (most common), urticaria (most common), photosensitivity, erythema multiforme, angioneurotic edema (rare)

Gastrointestinal: Nausea, vomiting, epigastric distress, diarrhea, GI bleeding

Genitourinary: Menstrual irregularities (rare)

Hematologic: Leukopenia, granulocytopenia

Neuromuscular & skeletal: Paresthesia (rare)

Renal: Hepatotoxicity, proteinuria, nephrosis

Miscellaneous: Oral thrush, drug-induced lupus-like syndrome (rare)

Overdosage/Toxicology

Symptoms of overdose include lethargy, vertigo, blurred vision, nausea, vomiting, and diarrhea. Treatment is supportive.

Drug Interactions

Induces CYP1A2 (weak), 2C8/9 (weak), 3A4 (weak)

Decreased effect:

Barbiturates may decrease levels of griseofulvin

Decreased warfarin, cyclosporine, and salicylate activity with griseofulvin

Griseofulvin decreases oral contraceptive effectiveness

Increased toxicity: With ethanol, may cause tachycardia and flushing

Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (may increase CNS depression). Ethanol will cause "disulfiram"-type reaction consisting of flushing, headache, nausea, and in some patients, vomiting and chest and/or abdominal pain.

Food: Griseofulvin concentrations may be increased if taken with food, especially with high-fat meals.

Mechanism of Action

Inhibits fungal cell mitosis at metaphase; binds to human keratin making it resistant to fungal invasion

Pharmacodynamics/Kinetics

Absorption: 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)

Distribution: Crosses placenta

Metabolism: Extensively hepatic

Half-life elimination: 9-22 hours

Excretion: Urine (<1% as unchanged drug); feces; perspiration

Dosage

Oral:

Children >2 years:

Microsize: 10-20 mg/kg/day in single or 2 divided doses

Ultramicrosize: >2 years: 5-10 mg/kg/day in single or 2 divided doses

Adults:

Microsize: 500-1000 mg/day in single or divided doses

Ultramicrosize: 330-375 mg/day in single or divided doses; doses up to 750 mg/day have been used for infections more difficult to eradicate such as tinea unguium

Duration of therapy depends on the site of infection:

Tinea corporis: 2-4 weeks

Tinea capitis: 4-6 weeks or longer

Tinea pedis: 4-8 weeks

Tinea unguium: 3-6 months or longer

Administration

Oral: Administer with a fatty meal (peanuts or ice cream) to increase absorption, or with food or milk to avoid GI upset

Monitoring Parameters

Periodic renal, hepatic, and hematopoietic function tests

Test Interactions

False-positive urinary VMA levels

Patient Education

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Take as directed, around-the-clock with food. Take full course of medication; do not discontinue without consulting prescriber. Avoid alcohol while taking this drug (disulfiram reactions). Practice good hygiene measures to prevent reinfection. Frequent blood tests may be required with prolonged therapy. You may experience nausea and vomiting (small, frequent meals may help); confusion, dizziness, drowsiness (use caution when driving or engaging in tasks that require alertness until response to drug is known); nausea, vomiting, or diarrhea (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); or increased sensitivity to sun (use sunscreen, wear protective clothing and eyewear, and avoid excessive exposure to direct sunlight). Report skin rash; respiratory difficulty; CNS changes (confusion, dizziness, acute headache); changes in color of stool or urine; white plaques in mouth; or worsening of condition. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.

Nursing Implications

Monitor periodic renal, hepatic, and hematopoietic function tests

Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: May cause soreness or irritation of mouth or tongue.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause dizziness, confusion, or insomnia

Mental Health: Effects on Psychiatric Treatment

May rarely cause leukopenia; use caution with clozapine and carbamazepine; barbiturates may decrease levels of griseofulvin

Dosage Forms

Suspension, oral, microsize (Grifulvin® V): 125 mg/5 mL (120 mL) [contains alcohol 0.2%]

Tablet, microsize (Grifulvin® V): 500 mg

Tablet, ultramicrosize: 125 mg, 250 mg, 330 mg

Gris-PEG®: 125 mg, 250 mg

References

Ginsburg CM, McCracken GH Jr, Petruska M, et al, "Effect of Feeding on Bioavailability of Griseofulvin in Children," J Pediatr , 1983, 102(2):309-11.

Kawabe Y, Mizuno N, Miwa N, et al, "Photosensitivity Induced by Griseofulvin," Photodermatol , 1988, 5(6):272-4.

Lecky BR, "Griseofulvin-Induced Neuropathy," Lancet , 1990, 335(8683):230-1.

Mion G, Verdon R, Le Gulluche Y, et al, "Fatal Toxic Epidermal Necrolysis After Griseofulvin," Lancet , 1989, 2(8675):1331.

Trepanier EF and Amsden GW, "Current Issues in Onchomycosis," Ann Pharmacother , 1998, 32(2):204-14.

Yang DJ and Rankin GO, "Nephrotoxicity of Antifungal Agents," Adverse Drug React Acute Poisoning Rev , 1985, 4(1):37-49.

International Brand Names

Afuvin® (BD); Aofen® (TH); Biogrisin® (ID, RO); Erlivin® (SG); Fulcin® (AU, BG, BR, CY, EG, ES, HK, ID, IE, IT, JO, KW, LB, MT, RO, SY, ZA); Fulcinex® (BD); Fulcin S® (DE); Fulkain® (DO); Fulvicin® U/F (CA); Fulvin-G® (BD); Fulvistatin P/G® (CL); Fulvistatin U/F® (CL); Fungistop® (ID); Gefulvin® (TR); G-G. Vin® (BD); Greosin® (CL, ES); Gricin® (CZ, DE, PL); Grifulin® (IL); Grifulvin® (TH); Grisactin® (IN); Griséfuline® (FR); Griseoderm® (HK); Griseofort® (ID); Griseofulvina L.CH.® (CL); Griseofulvin® (BE, CY, ID, PL, RO); Griseofulvin Chemist Lab® (BD); Griseofulvin Hovid® (SG); Griseofulvin Leo® (LU); Griseomed® (AT); Griseostatin® (AU, HK); griseo von ct® (DE); Grisflavin® (TH); Grisol® (CH); Griso-T (BD); Grisovina FP® (IT); Grisovin® (AT, AU, GB, HK, KW, MX, NZ, TR); Grisovin-FP® (BD); Grivin® (ID, SG, TH); H.G. Griseofulvin® (EC); Japcin® (BD); Krisovin® (SG); Likuden® (DE); Medofluvin® (SG); Microcidal® (ZA); Microfulvin® (ID); Mycostop® (ID); Neofulvin® (TH); Nidovin® (BD); Opsovin® (BD); Orgavin® (BD); Seovin® (BD); Sporostatin® (BR); Trivanex®1 (TH); Walavin® (IN)

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