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Grizeofulvin

Grizeofulvin - General Information

An antifungal antibiotic. Grizeofulvin may be given by mouth in the treatment of tinea infections. [PubChem]

 

Pharmacology of Grizeofulvin

Grizeofulvin is a mycotoxic metabolic product of Penicillium spp. It was the first available oral agent for the treatment of dermatophytoses and has now been used for more than forty years. Grizeofulvin is fungistatic with in vitro activity against various species of Microsporum Epidermophyton, and Trichophyton. It has no effect on bacteria or on other genera of fungi. Following oral administration, griseofulvin is deposited in the keratin precursor cells and has a greater affinity for diseased tissue. The drug is tightly bound to the new keratin which becomes highly resistant to fungal invasions.

 

Grizeofulvin for patients

 

Grizeofulvin Interactions

Patients on warfarin-type anticoagulant therapy may require dosage adjustment of the anticoagulant during and after griseofulvin therapy. Concomitant use of barbiturates usually depresses griseofulvin activity and may necessitate raising the dosage.

The concomitant administration of griseofulvin has been reported to reduce the efficacy of oral contraceptives and to increase the incidence of breakthrough bleeding.

 

Grizeofulvin Contraindications

This drug is contraindicated in patients with porphyria, hepatocellular failure, and in individuals with a history of hypersensitivity to griseofulvin.

 

Additional information about Grizeofulvin

Grizeofulvin Indication: For the treatment of ringworm infections of the skin, hair, and nails, namely: tinea corporis, tinea pedis, tinea cruris, tinea barbae, cradle cap or other conditions caused by Trichophyton or Microsporum fungi.
Mechanism Of Action: Grizeofulvin is fungistatic, however the exact mechanism by which it inhibits the growth of dermatophytes is not clear. It is thought to inhibit fungal cell mitosis and nuclear acid synthesis. It also binds to and interferes with the function of spindle and cytoplasmic microtubules by binding to alpha and beta tubulin.
Drug Interactions: Amobarbital The barbiturate decreases the effect of griseofulvin
Aprobarbital The barbiturate decreases the effect of griseofulvin
Butalbital The barbiturate decreases the effect of griseofulvin
Butabarbital The barbiturate decreases the effect of griseofulvin
Butethal The barbiturate decreases the effect of griseofulvin
Dihydroquinidine barbiturate The barbiturate decreases the effect of griseofulvin
Heptabarbital The barbiturate decreases the effect of griseofulvin
Hexobarbital The barbiturate decreases the effect of griseofulvin
Methohexital The barbiturate decreases the effect of griseofulvin
Methylphenobarbital The barbiturate decreases the effect of griseofulvin
Talbutal The barbiturate decreases the effect of griseofulvin
Secobarbital The barbiturate decreases the effect of griseofulvin
Quinidine barbiturate The barbiturate decreases the effect of griseofulvin
Primidone The barbiturate decreases the effect of griseofulvin
Phenobarbital The barbiturate decreases the effect of griseofulvin
Pentobarbital The barbiturate decreases the effect of griseofulvin
Warfarin Grizeofulvin decreases the anticoagulant effect
Acenocoumarol Grizeofulvin decreases the anticoagulant effect
Dicumarol Grizeofulvin decreases the anticoagulant effect
Anisindione Grizeofulvin decreases the anticoagulant effect
Aspirin Anticipate decrease of ASA efficiency in presence of griseofulvin
Chlorotrianisene The enzyme inducer decreases the effect of the hormones
Clomifene The enzyme inducer decreases the effect of the hormones
Cyclosporine Grizeofulvin decreases the effect of cyclosporine
Diethylstilbestrol The enzyme inducer decreases the effect of the hormones
Estradiol The enzyme inducer decreases the effect of the hormones
Estriol The enzyme inducer decreases the effect of the hormones
Conjugated Estrogens The enzyme inducer decreases the effect of the hormones
Estrone The enzyme inducer decreases the effect of the hormones
Estropipate The enzyme inducer decreases the effect of the hormones
Medroxyprogesterone The enzyme inducer decreases the effect of the hormones
Megestrol The enzyme inducer decreases the effect of the hormones
Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
Quinestrol The enzyme inducer decreases the effect of the hormones
Mestranol This product may cause a slight decrease of contraceptive effect
Norethindrone This product may cause a slight decrease of contraceptive effect
Food Interactions: Take this medication with a high fat meal, fatty foods increase bioavailability.
Avoid alcohol.
Generic Name: Griseofulvin
Synonyms: Griseofulvina [INN-Spanish]; Griseofulvine [INN-French]; Griseofulvinum [INN-Latin]
Drug Category: Antibiotics, Antifungal; Antibacterial Agents
Drug Type: Small Molecule; Approved

Other Brand Names containing Griseofulvin: Amudane; Biogrisin-fp; Curling factor; Delmofulvina; Fulcin; Fulcine; Fulvican grisactin; Fulvicin; Fulvicin P/G; Fulvicin U/F; Fulvicin-P/G; Fulvicin-U/F; Fulvina; Fulvinil; Fulvistatin; Fungivin; Greosin; Gresfeed; Gricin; Grifulin; Grifulvin; Grifulvin V; Gris-PEG; Grisactin; Grisactin Ultra; Griscofulvin; Grisefuline; Griseo; Griseofulvin forte; Griseofulvin-forte; Griseomix; Grisetin; Grisofulvin; Grisovin; Grisovin FP; Grizeofulvin; Grysio; Guservin; Lamoryl; Likuden; Likunden; Murfulvin; Neo-Fulcin; Neocid; Poncyl; Spirofulvin; Sporostatin; Sporostatin xan; Xuanjing;
Absorption: Poorly absorbed from GI ranging from 25 to 70% of an oral dose. Absorption is significantly enhanced by administration with or after a fatty meal.
Toxicity (Overdose): Side effects are minor: headaches, gastrointestinal reactions and cutaneous eruptions
Protein Binding: Not Available
Biotransformation: Primarily hepatic with major metabolites being 6-methyl-griseofulvin and its glucuronide conjugate.
Half Life: 9-21 hours
Dosage Forms of Grizeofulvin: Tablet Oral
Suspension Oral
Chemical IUPAC Name: (2S,5'R)-7-chloro-3',4,6-trimethoxy-5'-methylspiro[1-benzofuran-2,4'-cyclohex-2-ene]-1',3-dione
Chemical Formula: C17H17ClO6
Griseofulvin on Wikipedia: https://en.wikipedia.org/wiki/Griseofulvin
Organisms Affected: Yeast and other Trichophyton or Microsporum fungi