Griseofulvin


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Dermatophytosis
Adult: For treatment of refractory cases or when topical treatment is inappropriate: 0.5-1 g as single or in divided doses. Duration of treatment: 2-4 weeks (tinea corporis); 4-8 weeks (tinea capitis, pedis); 8-12 weeks (refractory cases of tinea capitis); 4-6 months (tinea unguium).
Child: >2 years As tab or oral suspension: 10 mg/kg daily in divided doses.

Topical/Cutaneous
Tinea pedis
Adult: As 1% spray: 1 spray (0.4 mg) once daily, may be increased to 3 sprays (1.2 mg) once daily, if necessary, depending on the severity of the condition. Continue treatment for 10 days after all lesions have disappeared. Max duration of treatment: 4 weeks.
Hepatic Impairment
Oral
Severe: Contraindicated.
Cách dùng
Should be taken with food. Take immediately after meals.
Chống chỉ định
Hypersensitivity to griseofulvin and penicillin. Systemic lupus erythematosus (SLE), porphyria. Severe hepatic impairment. Pregnancy.
Thận trọng
Mild to moderate hepatic impairment. Children. Lactation. Men should not father a child during and for 6 months after treatment.
Phản ứng phụ
Significant: Onset or exacerbation of SLE, photosensitivity reaction, rarely, leucopenia, granulocytopenia.
Gastrointestinal disorders: Diarrhoea, dry mouth, vomiting, nausea, gastric discomfort, epigastric distress, oral candidiasis. Rarely, gastrointestinal haemorrhage.
General disorders and administration site conditions: Fatigue.
Nervous system disorders: Headache, dizziness, paraesthesia, impaired coordination, peripheral neuropathy.
Psychiatric disorders: Confusion, insomnia.
Renal and urinary disorders: Rarely, nephrosis, proteinuria.
Skin and subcutaneous tissue disorders: Rash, urticaria, irritation (e.g. stinging, burning).
Potentially Fatal: Severe skin reactions (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme), photosensitivity, hepatotoxicity (e.g. jaundice, elevated LFT or bilirubin).
Thông tin tư vấn bệnh nhân
This drug may cause drowsiness, confusion, dizziness and impaired coordination, if affected, do not drive or operate machinery. Avoid exposure to sunlight or UV sources. Spray: Avoid exposure to open flame or other source of ignition during or after application.
MonitoringParameters
Monitor CBC (long-term treatment), liver and renal function. Assess for signs of severe skin reaction.
Tương tác
Decreased serum concentrations of coumarin anticoagulants, oral contraceptives, ciclosporin and salicylates. Decreased serum concentrations of griseofulvin with phenylbutazone, barbiturates (e.g. phenobarbital) and other sedative and hypnotic drugs.
Food Interaction
Increased absorption and plasma concentration with food, particularly high-fat meals. Enhanced effects (e.g. nausea, vomiting, flushing, tachycardia, severe hypotension) of alcohol.
Lab Interference
False-positive urinary vanillylmandelic acid (VMA) levels.
Tác dụng
Description: Griseofulvin inhibits fungal cell division at metaphase by disrupting the mitotic spindle structure of the cell. It binds to human keratin and make it resistant to fungal infections; may also interfere with deoxyribonucleic acid (DNA) production.
Pharmacokinetics:
Absorption: Almost completely absorbed primarily from the duodenum and to a lesser extent from jejunum and ileum. Food enhances absorption, particularly high-fat meal. Time to peak plasma concentration: Approx 4 hours (microsize griseofulvin).
Distribution: Distributed in the keratin layer of the skin, hair, and nails, and concentrates in the liver, fat and skeletal muscles. Crosses the placenta. Volume of distribution: Approx 1.5 L.
Metabolism: Extensively metabolised in the liver to 6-desmethylgriseofulvin and glucuronide conjugate.
Excretion: Via urine (<1% as unchanged drug); faeces (approx 33%); perspiration. Elimination half-life: 9-24 hours.
Đặc tính

Chemical Structure Image
Griseofulvin

Source: National Center for Biotechnology Information. PubChem Database. Griseofulvin, CID=441140, https://pubchem.ncbi.nlm.nih.gov/compound/Griseofulvin (accessed on Jan. 23, 2020)

Bảo quản
Store between 20-25°C. Protect from light. Spray: Protect from direct light and heat.
Phân loại MIMS
Phân loại ATC
D01AA08 - griseofulvin ; Belongs to the class of antibiotics. Used in the topical treatment of fungal infection.
D01BA01 - griseofulvin ; Belongs to the class of antifungals for systemic use.
References
Anon. Griseofulvin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 19/12/2019.

Buckingham R (ed). Griseofulvin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 19/12/201919/12/2019.

Griseofulvin 125 mg Tablets (Chemidex Pharma Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 19/12/2019.

Griseofulvin 500 mg Tablets (Chemidex Pharma Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 19/12/2019.

Griseofulvin Suspension (Actavis Pharma, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 19/12/2019.

Griseofulvin Tablet (Sigmapharma Laboratories, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 19/12/2019.

Joint Formulary Committee. Griseofulvin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 19/12/2019.

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