レバミソール 化學(xué)特性,用途語,生産方法
用途
レバミゾール（levamisole）とは線蟲駆蟲薬の1種。線蟲の體內(nèi)におけるフマル酸の還元およびコハク酸の酸化を遮斷することにより炭水化物代謝を抑制し、駆蟲効果を発揮する。
レバミゾールは小腸、胎盤型を除くほとんどのアルカリホスファターゼアイソフォームを可逆的?非競合的に阻害する。このため、in situ ハイブリダイゼーションやウェスタンブロッティングなどを用いたシグナル検出において、余分なアルカリホスファターゼ活性を減らすための抑制剤として使用される。
効能
駆蟲薬
使用
Levamisole is used for initial and secondary immunodeficient conditions, autoimmune
diseases, chronic and reoccurring infections, large intestine adenocarcinoma, helmintosis,
and rheumatoid arthritis. Synonyms of this drug are decaris, tetramizole, and others.
Levimasole is also a drug of choice for ascardiasis. Numerous investigations show that a
single dose of levamisole heals from 90 to 100% of patients with ascardiasis, in particular
those infected with A. duodenale. It is less effective against ancylostomiasis and strongyloidiasis. However, it is not effective against N. americanus. It seems likely that it has a
gangliostimulating effect on parasite tissues in both the parasympathetic and sympathetic
regions. Moreover, it is presumed that this drug has an immunomodulatory effect on the
host organism. Synonyms of this drug are decaris, solacil, ergamisol, tramisol, immunol,
and others.
定義
ChEBI: Levamisole is a 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole that has S configuration. It is used (generally as the monohydrochloride salt) to treat parasitic worm infections in pigs, sheep and cattle and was formerly used in humans as an adjuvant to chemotherapy for the treatment of various cancers. It is also widely used as an adulterant to coccaine. It has a role as an antinematodal drug, an antirheumatic drug, an immunomodulator, an immunological adjuvant and an EC 3.1.3.1 (alkaline phosphatase) inhibitor. It is an enantiomer of a dexamisole.
適応癥
Levamisole (Ergamisol) is an antiparasitic drug that has
been found to enhance T-cell function and cellular immunity.
The drug improves survival of patients with resected
colorectal cancers when combined with 5-fluorouracil;
the mechanism of this interaction is not
known. Levamisole does not have antitumor activity
against established or metastatic cancer and has not
been found useful in the adjuvant therapy of cancers
other than colorectal cancer.
The major adverse effects of levamisole are nausea
and anorexia. Skin rashes, itching, flulike symptoms, and
fevers also have been observed.
抗菌性
Its principal activity is against Asc. lumbricoides and hookworms. Worms are paralyzed and passed
out in the feces within a few hours.
応用例（製薬）
The l-isomer of tetramisole, available as the monohydrochloride.
The d-isomer has no anthelmintic activity. It is very soluble
in water and is stable in the dry state.
作用機(jī)序
Levamisole has immunomodulating activity. It is believed that it regulates cellular mechanisms of the immune system, and the mechanism of its action may be associated with
activation and proliferative growth of T-lymphocytes, increased numbers of monocytes and
activation of macrophages, and also with increased activity and hemotaxis of neutrophylic
granulocytes. Levamisole also exhibits anthelmint action. It also increases the body’s overall resistivity and restores altered T-lymphocyte and phagocyte function. It can also fulfill
an immunomodulatory function by strengthening the weak reaction of cellular immunity,
weakening strong reaction, and having no effect on normal reaction.
薬物動態(tài)學(xué)
Oral absorption: c. 90%
C
max 150 mg oral: 0.5 mg/L after c. 2 h
Plasma half-life: c. 4 h
Volume of distribution: 100–120 L
Levamisole is rapidly absorbed from the gut and extensively
metabolized in the liver. It is excreted chiefly in the urine.
臨床応用
Ascariasis
Hookworm infection
Levamisole has been used in rheumatoid arthritis and some
other conditions that are said to respond to its immunomodulatory
activity.
副作用
Nausea, gastrointestinal upsets and very mild neurological
problems have been reported.
レバミソール 上流と下流の製品情報
原材料
準(zhǔn)備製品