Ethionamide


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Tuberculosis
Adult: In combination w/ 1 or 2 anti-TB agents: 15-20 mg/kg daily as single dose or in divided doses. Usually given at an initial dose of 250 mg daily for 1-2 days, increased to 250 mg bid for 1-2 days, then gradually increased to highest tolerated dose. Max: 1 g daily in 3-4 divided doses.
Child: 10-20 mg/kg daily in 2-3 divided doses, or alternatively, 15 mg/kg daily as a single dose. Max: 1 g daily.
Hepatic Impairment
Severe: Contraindicated.
Cách dùng
Should be taken with food. Take at mealtimes.
Chống chỉ định
Hypersensitivity to ethionamide. Severe hepatic impairment.
Thận trọng
Patient w/ depression or other psychiatric illness, DM, porphyria, thyroid dysfunction. Hepatic or renal impairment. Pregnancy and lactation.
Phản ứng phụ
Nervous: Psychotic disturbances, mental depression, anxiety, drowsiness, dizziness, restlessness, headache, peripheral neuritis, paraesthesia, seizures, tremors, pellagra-like syndrome, hallucination, asthenia.
CV: Orthostatic hypotension.
GI: Nausea, vomiting, diarrhoea, abdominal pain, excessive salivation, metallic taste, stomatitis, anorexia, wt loss.
Resp: Olfactory disturbances.
Hepatic: Hepatitis, transient increase in serum bilirubin, AST, ALT.
Endocrine: Hypothyroidism, hypoglycaemia, gynaecomastia, impotence, menorrhagia.
Haematologic: Thrombocytopenia.
Musculoskeletal: Joint pain, acute rheumatic symptoms.
Ophthalmologic: Diplopia, optic neuritis, blurred vision.
Dermatologic: Rash, photosensitivity, purpura, acne, dermatitis, alopecia.
MonitoringParameters
Monitor serum ALT and AST at baseline and mthly; blood glucose and TSH periodically. Perform ophthalmologic exams prior to and during therapy. Evaluate CNS changes, ocular changes, and neuritis during therapy.
Tương tác
May potentiate AR of other anti-TB drugs. Additive CNS effect w/ isoniazid and cycloserine. May cause seizures w/ cycloserine.
Food Interaction
May cause psychotic reaction w/ excessive alcohol ingestion.
Tác dụng
Description: Ethionamide’s exact mechanism of action has not been fully elucidated, however, the drug appears to inhibit peptide synthesis. It may be bacteriostatic or bactericidal in action, depending on the concentration of drug attained at the site of infection and susceptibility of organism.
Pharmacokinetics:
Absorption: Readily absorbed from the GI tract. Time to peak serum concentration: Approx 1 hr.
Distribution: Widely distributed throughout body tissues and fluids. Crosses placenta and CSF. Volume of distribution: 93.5 L. Plasma protein binding: 30%.
Metabolism: Extensively metabolised in the liver to the active metabolite sulfoxide and some inactive metabolites.
Excretion: Via urine (<1% as unchanged drug). Elimination half-life: Approx 2 hr.
Đặc tính

Chemical Structure Image
Ethionamide

Source: National Center for Biotechnology Information. PubChem Database. Ethionamide, CID=2761171, https://pubchem.ncbi.nlm.nih.gov/compound/Ethionamide (accessed on Jan. 23, 2020)

Bảo quản
Store between 20-25°C.
Phân loại MIMS
Phân loại ATC
J04AD03 - ethionamide ; Belongs to the class of thiocarbamide derivatives. Used in the systemic treatment of tuberculosis.
References
Anon. Ethionamide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/03/2017.

Buckingham R (ed). Ethionamide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/03/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Ethionamide. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 07/03/2017.

Trecator Tablet (Wyeth Pharmaceuticals Inc.). U.S. FDA. https://www.fda.gov/. Accessed 07/03/2017.

Trecator Tablet, Film Coated (Wyeth Pharmaceuticals Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 07/03/2017.

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