Griseofulvin (Grisovin) is an antifungal medication that is used to treat infections of the scalp, skin, or nails caused by different fungi.

Griseofulvin (Grisovin) Uses:

• Dermatophyte infections:

  • Treatment of the following dermatophyte infections of the skin, hair, and nails not adequately treated by topical therapy:
    • Tinea corporis,
    • tinea pedis,
    • tinea cruris,
    • tinea barbae,
    • tinea capitis,
    • tinea unguium (onychomycosis) when developed by one or more of the following species of fungi:
      • Trichophyton rubrum,
      • Trichophyton tonsurans,
      • Trichophyton mentagrophytes,
      • Trichophyton interdigitalis,
      • Trichophyton verrucosum,
      • Trichophyton megnini,
      • Trichophyton gallinae,
      • Trichophyton crateriform,
      • Trichophyton sulphureum,
      • Trichophyton schoenleini,
      • Microsporum audouini,
      • Microsporum canis,
      • Microsporum gypseum, and
      • Epidermophyton floccosum.
  • Limitations of use:
    • Use for the prophylaxis of fungal infections has not been established; though it is not effective for the treatment of tinea versicolor.

Griseofulvin (Grisovin) Dose in Adults

Griseofulvin (Grisovin) Dose in the treatment of Dermatophyte infections: 

• Microsize:
  • 500 mg per day in single or divided doses;
  • for more widespread lesions initial doses of 750 to 1,000 mg per day in single or divided doses may be required;
  • it may decrease gradually to 500 mg/day or less in case the patient responds to a higher dose.
• Ultra micro size:
  • 375 mg per day in single or divided doses;
  • doses up to 750 mg per day in divided doses have been utilized for infections more difficult to eliminate such as tinea unguium and tinea pedis

• Duration of therapy depends on the site of infection:

  • Tinea corporis: 2 to 4 weeks
  • Tinea cruris: In the manufacturer’s labeling duration is not specified; in pediatric patients, 6 weeks has been suggested (Red Book, 2015)
  • Tinea capitis: 4 to 6 weeks
  • Tinea pedis: 4 to 8 weeks
  • Tinea unguium: 4 to 6 months or longer

Griseofulvin (Grisovin) Dose in Childrens

Griseofulvin (Grisovin) General Dosing Guidelines for Susceptible Infections:

• Children >2 years and Adolescents:

  • Microsize: Oral:
    • 20 to 25 mg/kg/day in single or 2 divided doses; maximum dose per day: 1,000 mg
  • Ultra micro size: Oral:
    • 10 to 15 mg/kg/day once on a daily basis;
    • The maximum per day dose: 750 mg

Griseofulvin (Grisovin) Dose in the treatment of Tinea capitis:

Note:

• It is the preferred therapy for Microsporum canis infection;
• It may be used in an amalgam with adjunctive topical therapy (e.g. selenium or antifungal shampoo).
• Patients who are receiving doses on the lower end of the dose range may need a longer duration of treatment for fungal eradication.

• Infants >1 month to Children ≤2 years:

  • Oral: Microsize:
    • 15 to 25 mg/kg/day in single or 2 divided doses (maximum daily dose: 1,000 mg/day) until resolution;
    • Usually, 6 to 8 weeks duration, although resistant cases may need longer duration.

• Children >2 years and Adolescents:

  • Microsize:
    • Oral: 20 to 25 mg/kg/day in single daily dose or in 2 divided doses for 6 to 8 weeks or until fungal cultures clear, while in some cases, treatment up to 12 to 18 weeks may be necessary
    • Maximum per day dose: 1,000 mg/day.
    • However,  lower doses (10 to 15 mg/kg/day) have been suggested priorly by experts, and by the manufacturer, they are linked with extended treatment durations and/or potentially lower cure rates and have fallen out of favor.
  • Ultra micro size:
    • Oral: 10 to 15 mg/kg/day once a day (maximum daily dose: 750 mg/day) for 6 to 8 weeks or until fungal cultures clear; while in some cases, treatment up to 12 to 18 weeks may be compulsory.

Pregnancy Risk Factor X

• Teratogenic effects in animal reproduction have been documented.
• Griseofulvin crosses over the placenta
• Pregnancy is not recommended as adverse events have been reported in humans (two cases where conjoined twins were observed).
• Women with reproductive potential should use effective contraception during treatment and after one month.
• Men should refrain from having children for six months after therapy.

Griseofulvin use during breastfeeding:

• It is not known if griseofulvin can be found in breast milk.
• Because of the risk of serious adverse reactions in nursing infants, breast-feeding is not recommended.

Dose in Kidney disease:

No dosage adjustments provided in the manufacturer's labeling.

Griseofulvin (Grisovin) Dose in Liver disease:

Its use is contraindicated in hepatic failure.

Side effects of Griseofulvin (Grisovin):

• Central Nervous System:

  • Confusion
  • Dizziness
  • Fatigue
  • Headache
  • Insomnia

• Dermatologic:

  • Dermatological Reaction (Erythema Multiforme-Like Drug Reaction)
  • Skin Photosensitivity
  • Skin Rash (Most Common)
  • Urticaria (Most Common)

• Gastrointestinal:

  • Diarrhea
  • Epigastric Distress
  • Gastrointestinal Hemorrhage
  • Nausea
  • Oral Candidiasis
  • Vomiting

• Genitourinary:

  • Nephrosis

• Hematologic & Oncologic:

  • Granulocytopenia

• Hepatic:

  • Hepatotoxicity

Contraindications to Griseofulvin (Grisovin):

• Hypersensitivity to griseofulvin or any component of the formulation
• hepatic failure
• porphyria
• pregnancy

Warnings and Precautions

• Hematologic effects

  • Leukopenia has been described (rare); discontinue therapy if granulocytopenia develops.

• Hepatic effects

  • It can cause jaundice, elevated liver function tests, or bilirubin (can be fatal or serious).
  • However, discontinue therapy if necessary. Monitor hepatic function.

• Penicillin allergy

  • Although hypersensitivity cross-reactions between penicillins, griseofulvin and penicillins is possible, it has been reported that patients who are penicillin-sensitive have been successfully treated without complications.

• Photosensitivity

  • To avoid photosensitivity reactions, it is important to avoid intense sunlight.

• Reactions to skin:

  • Severe skin reactions (e.g. Severe skin reactions (e.g. Stevens-Johnson syndrome and toxic epidermal nécrolysis) can be fatal. However, discontinue use if you experience severe skin reactions.

• Lupus erythematosus:

  • Reports have been made about lupus and lupus-like disorders, as well as exacerbation or development of existing lupus.

Griseofulvin: Drug Interaction

Monitoring parameters:

Periodic renal, hepatic, and hematopoietic function tests especially with long-term use.

How to administer Griseofulvin (Grisovin)?

Administer orally with a fatty meal to boast up absorption.

Gris-PEG tablets:

• It may be swallowed whole or crushed and sprinkled onto 1 tablespoonful of applesauce and swallowed quickly without chewing.

Suspension:

• Shake well before use.

Mechanism of action of Griseofulvin (Grisovin):

• Metaphase inhibition of fungal cell mitosis; binding to human keratin makes it resistive to fungal invasion.

Absorption: Distribution:

• The ultra-micro size griseofulvin absorption can be almost completely completed
• Although the microsize griseofulvin absorption rate is variable (27%-72% of an oral dose),
• Ingestion of fatty meals can increase GI absorption (GI absorption ultramicrosize is approximately 1.5 times greater than microsize);
• The duodenum absorbs it.
• It's found in the keratin layers of skin, hair, or nails.
• Concentrates in liver, fat, skeletal muscles

Metabolism:

• Extensively hepatic

Half-life elimination:

• 9 to 24 hours

Time to peak serum concentration:

• 4 hours

Excretion:

• Urine (<1% as unchanged drug);
• feces (~33%);
• perspiration

International Brand Names of Griseofulvin:

• Grifulvin V
• Gris-PEG
• Afuvin
• Asfulvin
• Biogrisin
• Delmofulvina
• Fulcin
• Fulcin Forte
• Fulcin S
• Fulcinex
• Fulsovin
• Fulvin G
• Fungistop
• Fungivin
• Fusovin
• Gricin
• Grifulin Forte
• Grifulvin
• Grisefuline
• Grisen
• Grisenova
• griseo von ct
• Griseofil
• Griseofulvin
• Griseofulvin Leo
• Griseofulvin Prafa
• Griseofulvina
• Griseomed
• Griseon
• Griseovin
• Griseovine
• Grisflavin
• Grisfulvin V
• Grisol
• Grisomicon
• Grisoral
• Grisovin
• Grisovin F.P.
• Grisovin-FP
• Grisovina FP
• Grisuven
• Grisuvin
• Grivin
• Grivin Forte
• Japcin
• Krisovin
• Likuden
• Microcidal
• Pongyl V
• Ponzyr V
• Rexavin
• Trivanex
• Ultrafulvin
• Ultragriseofulvin

Griseofulvin Brand Names in Pakistan: