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Medication Safety Issues
Sound-alike/look-alike issues:
Fulvicin® may be confused with Furacin®
Pronunciation
(gri see oh FUL vin)
U.S. Brand Names
Index Terms
Generic Available
Yes: Suspension, ultramicrosized product
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Treatment of susceptible tinea infections of the skin, hair, and nails
Pregnancy Risk Factor
C
Pregnancy Considerations
Animal studies have shown decreased spermatogenesis, as well as embryotoxic and teratogenic effects with griseofulvin. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy is contraindicated.
Lactation
Excretion in breast milk unknown/use caution
Contraindications
Hypersensitivity to griseofulvin or any component of the formulation; severe liver disease; porphyria (interferes with porphyrin metabolism); pregnancy
Warnings/Precautions
Concerns related to adverse effects:
• Penicillin allergy: Hypersensitivity cross reaction between penicillins and griseofulvin is possible.
• Photosensitivity: Avoid exposure to intense sunlight to prevent photosensitivity reactions.
Special populations:
• Pediatrics: Safety and efficacy have not been established in children ?2 years of age.
• Pregnancy: May cause fetal harm when administered to pregnant women.
Other warnings/precautions:
• Monitoring: During long-term therapy, periodic assessment of hepatic, renal, and hematopoietic functions should be performed.
Adverse Reactions
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: Nausea, vomiting, epigastric distress, diarrhea, GI bleeding
Genitourinary: Menstrual irregularities (rare)
Hematologic: Granulocytopenia, leukopenia
Hepatic: Hepatotoxicity
Neuromuscular & skeletal: Paresthesia (rare)
Renal: Nephrosis, proteinuria
Miscellaneous: Drug-induced lupus-like syndrome (rare), oral thrush
Metabolism/Transport Effects
Induces CYP1A2 (weak), 2C8 (weak), 2C9 (weak), 3A4 (weak)
Drug Interactions
Alcohol (Ethyl): Griseofulvin may enhance the adverse/toxic effect of Alcohol (Ethyl). A disulfiram-like reaction may occur. Risk C: Monitor therapy
Barbiturates: May decrease the absorption of Griseofulvin. Exceptions: Methohexital; Thiopental. Risk D: Consider therapy modification
Contraceptive (Progestins): Griseofulvin may diminish the therapeutic effect of Contraceptive (Progestins). Contraceptive failure is possible. Risk X: Avoid combination
Coumarin Derivatives: Griseofulvin may increase the metabolism of Coumarin Derivatives. Risk C: Monitor therapy
CycloSPORINE: Griseofulvin may increase the metabolism of CycloSPORINE. Risk D: Consider therapy modification
Maraviroc: CYP3A4 Inducers may decrease the serum concentration of Maraviroc. Risk D: Consider therapy modification
Oral Contraceptive (Estrogens): Griseofulvin may increase the metabolism of Oral Contraceptive (Estrogens). Contraceptive failure is possible. Risk D: Consider therapy modification
Saccharomyces boulardii: Antifungal Agents may diminish the therapeutic effect of Saccharomyces boulardii. Risk D: Consider therapy modification
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid ethanol (may increase CNS depression). Concomitant use with ethanol will cause “disulfiram”-type reaction consisting of tachycardia, 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. In the treatment of tinea capitis, higher dosages (20-25 mg/kg/day for 8-12 weeks) have been recommended by some authors (unlabeled).
Ultramicrosize: Usual: 7.3 mg/kg/day in single dose or 2 divided doses; range: 5-15 mg/kg/day in single dose or 2 divided doses (maximum: 750 mg/day)
Adults:
Microsize: 500-1000 mg/day in single or divided doses
Ultramicrosize: 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 and tinea pedis
Duration of therapy depends on the site of infection:
Tinea corporis: 2-4 weeks
Tinea capitis: 4-6 weeks or longer (up to 8-12 weeks)
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
Gris-PEG® tablets: May be swallowed whole or crushed and sprinkled onto 1 tablespoonful of applesauce and swallowed immediately without chewing.
Monitoring Parameters
Periodic renal, hepatic, and hematopoietic function tests
Test Interactions
False-positive urinary VMA levels
Patient Education
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 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.
Geriatric Considerations
No specific changes in dosing are needed.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: May cause soreness or irritation of mouth or tongue. May cause oral thrush.
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
Nursing: Physical Assessment/Monitoring
Assess allergic history prior to beginning treatment (cross reaction with penicillin is possible). Assess potential for interactions with other pharmacological agents or herbal products patient may be taking (eg, decreased effectiveness of oral contraceptives). Assess results of laboratory tests, renal function, and hepatic function with long-term use, therapeutic effectiveness (resolution of viral infection), and adverse response (eg, CNS changes, gastrointestinal upset, rash, opportunistic infection) periodically during therapy. Teach patient proper use, possible side effects/appropriate interventions and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Suspension, oral [microsize]: 125 mg/5mL (120 mL)
Grifulvin® V: 125 mg/5 mL (120 mL) [contains alcohol 0.2%]
Tablet, oral [microsize]:
Grifulvin® V: 500 mg
Tablet, oral [ultramicrosize]:
Gris-PEG®: 125 mg, 250 mg
Pricing: U.S. (www.drugstore.com)
Suspension (Grifulvin V)
125 mg/5 mL (120): $68.14
Suspension (Griseofulvin Microsize)
125 mg/5 mL (120): $46.99
Tablets (Gris-PEG)
125 mg (90): $162.41
References
Fleece D, Gaughan JP, and Aronoff SC, “Griseofulvin Versus Terbinafine in the Treatment of Tinea Capitis: A Meta-Analysis of Randomized, Clinical Trials,” Pediatrics, 2004, 114(5):1312-5.
Fuller LC, Smith CH, Cerio R, et al, “A Randomized Comparison of 4 Weeks of Terbinafine vs 8 Weeks of Griseofulvin for the Treatment of Tinea Capitis,” Br J Dermatol, 2001, 144(2):321-7.
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.
Lipozencic J, Skerlev M, Orofino-Costa R, et al, “A Randomized, Double-Blind, Parallel-Group, Duration-Finding Study of Oral Terbinafine and Open-Label, High-Dose Griseofulvin in Children With Tinea Capitis due to Microsporum Species,” Br J Dermatol, 2002, 146(5):816-23.
Mion G, Verdon R, Le Gulluche Y, et al, “Fatal Toxic Epidermal Necrolysis After Griseofulvin,” Lancet, 1989, 2(8675):1331.
Pomeranz AJ and Sabnis SS, “Tinea Capitis: Epidemiology, Diagnosis and Management Strategies,” Paediatr Drugs, 2002, 4(12):779-83.
Sladden MJ and Johnston GA, “Common Skin Infections in Children,” BMJ, 2004, 329(7457):95-9.
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
Lexi-Comp.com
Last full review/revision August 2008
Content last modified August 2008
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