티아세타존

한글명:티아세타존

카스 번호104-06-3

상품명:THIACETAZONE

CBNumberCB8422936

분자식C10H12N4OS

포뮬러 무게236.29

MOL 파일104-06-3.mol

동의어(한글)

티아세타존

화학적 성질

녹는점	225-230 °C
밀도	1.2752 (rough estimate)
굴절률	1.6440 (estimate)
저장 조건	Store at -20°C
용해도	DMSO에 용해됨
산도 계수 (pKa)	11.35±0.70(Predicted)
물리적 상태	powder to crystal
색상	White to Orange to Green

위험 및 안전 성명

위험품 표기

위험 카페고리 넘버

안전지침서

WGK 독일

RTECS 번호

AE3850000

HS 번호

29309090

독성

LD50 s.c. in mice: 1-2 g/kg (Bavin)

NFPA 704:

	0
1		0

그림문자(GHS)

티아세타존 화학적 특성, 용도, 생산

화학적 성질
Solid
용도
Thiacetazone (cas# 104-06-3) is used in combination chemotherapy, in preparation of nucleosides as inhibitors of adenylate-forming enzyme MenE.
Indications
Thiacetazone is active against many strains of M. tuberculosis. It is not marketed in the United States. However, because of its low cost, it is used as a first-line agent in East Africa, especially in combination with compounds such as isoniazid. The most common side effects of thiacetazone include GI intolerance and development of rashes. It causes significant ototoxicity, especially when coadministered with streptomycin. Lifethreatening hypersensitivity reactions, such as hepatitis, transient marrow aplastic syndromes, neutropenia, and thrombocytopenia, have been reported.
Pharmaceutical Applications
Thioacetazone (USAN amithiozone) is a synthetic compound discovered during initial work on the sulfonamides, to which it is structurally related. It is only slightly soluble in water. It is a weak bacteristatic drug, with frequent serious side effects, particularly in HIV-positive persons to whom it must never knowingly be given. On the advice of the WHO it no longer has a place in the treatment of tuberculosis, except as a last resort in cases of extreme drug resistance.
In-vitro MICs vary considerably according to the medium used and bear little relation to in-vivo efficacy. Many strains of M. tuberculosis isolated in East Africa, India and Hong Kong are naturally more resistant than strains from Europe. Acquired resistance, as a result of monotherapy, is prevalent in the developing countries.
Thioacetazone is well absorbed, achieving a plasma concentration of 1–4 mg/L 2–4 h after a 100 mg oral dose. The plasma half-life is 8–12 h. Little is known about the distribution of the drug. Several metabolites are described. About 20% is eliminated in the urine; the fate of the remainder is unknown. Rashes are common, occurring in 2–4% of patients in Africa but much more frequently in those of Chinese ethnic origin. More severe skin reactions, exfoliative dermatitis and Stevens–Johnson syndrome occur in less than 0.5% of HIV-negative patients, but there is a 10-fold increase of these reactions in HIV-positive patients, proving fatal in up to 3% of such patients. Other common side effects include gastrointestinal reactions, vertigo and conjunctivitis. Less common reactions include hepatitis, erythema multiforme, hemolytic anemia and, rarely, agranulocytosis. Prolonged therapy may rarely lead to hypertrichosis, gynecomastia and osteoporosis. It is very rarely used, but may occasionally be considered (with other antituberculosis drugs) in extremely drug resistant tuberculosis.

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