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:
    • Although its effectiveness in treating tinea versicolor has not been demonstrated, it may be used as a preventative measure for fungal infections.

Griseofulvin (Grisovin) Dose in Adults

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

• Microsize:
  • Initial dosages of 750 to 1,000 mg per day in single or divided doses may be needed for more widespread lesions; if the patient responds to a larger dose, the amount may be gradually decreased to 500 mg/day or less.
• Ultra micro size:
  • Dosages up to 750 mg per day in divided doses have been used for infections that are harder to treat, like tinea unguium and tinea pedis. 375 mg per day in single or divided doses

• 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 recommended treatment for Microsporum canis infection and can be used with further topical treatments (e.g. selenium or antifungal shampoo).
• Patients who are receiving dosages at the lower end of the dosing range could require more time in treatment to completely eradicate the fungal infection.

• Infants >1 month to Children ≤2 years:

  • Oral: Microsize:
    • The typical length is 6 to 8 weeks, while resistant cases may require a longer term. The highest daily dose is 1,000 mg/day.

• Children >2 years and Adolescents:

  • Microsize:
    • Oral: 20 to 25 mg/kg/day given as a single dose or in two divided doses for six to eight weeks, or until the fungal cultures are clean, though in some situations 12 to 18 weeks of treatment may be required.
    • The daily dose cap is set at 1,000 mg.
    • Poorer doses (10 to 15 mg/kg/day) have been recommended in the past by specialists and the manufacturer, but they have lost favour because they are associated with longer treatment times and/or potentially lower cure rates.
  • Ultra micro size:
    • Oral: For 6 to 8 weeks or until fungal cultures clear, administer 10 to 15 mg/kg/day once daily (maximum daily dose: 750 mg/day); in some circumstances, treatment for up to 12 to 18 weeks may be required.

Pregnancy Risk Factor X

• Teratogenic effects in animal reproduction have been documented.
• Griseofulvin crosses over the placenta
• Given the human reports of negative outcomes, pregnancy is not advised (two cases where conjoined twins were observed).
• Effective contraception should be used both throughout therapy and after one month for women who are sexually active.
• Men should wait six months after therapy before starting a family.

Griseofulvin use during breastfeeding:

• If griseofulvin is present in breast milk is unknown.
• Breastfeeding is not advised due to the possibility of major adverse effects in breastfeeding infants.

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 reported (rarely); if granulocytopenia appears, stop treatment.

• Hepatic effects

  • It may result in bilirubin, liver function test elevations, or jaundice (can be fatal or serious).
  • However, if necessary, stop therapy. keep an eye on liver health.

• Penicillin allergy

  • Despite the possibility of hypersensitivity reactions between penicillins, griseofulvin, and penicillins, it has been reported that penicillin-sensitive patients have successfully undergone treatment without any issues.

• Photosensitivity

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

• Reactions to skin:

  • Stevens-Johnson syndrome and toxic epidermal nécrolysis are two examples of severe skin responses that can be lethal. However, stop using if you have serious skin repercussions.

• 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
• Hematopoietic function 

How to administer Griseofulvin (Grisovin)?

Administer orally with a fatty meal to boast up absorption.

Gris-PEG tablets:

• You can fast and without chewing consume it whole or crush it and sprinkle it over 1 tablespoon of applesauce.

Suspension:

• Shake well before use.

Mechanism of action of Griseofulvin (Grisovin):

• Metaphase inhibits fungal cell mitosis; it inhibits fungal invasion by attaching to human keratin.

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.
• The keratin layers of the skin, hair, and nails contain it.
• 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: