Mechanism and clinical effects of thalidomide in the blood of rheumatic diseases.doc

 PAGE \* MERGEFORMAT 18 Mechanism and clinical effects of thalidomide in the blood of rheumatic diseases [Keywords:] thalidomide, mechanism, applications Thalidomide (thalidomide, Thd is a synthetic glutamic acid derivative, in 1953, first synthesized in West Germany, as a sedative to enter the European market and found to alleviate morning sickness symptoms are particularly effective, then its induced abnormal function in the world is disabled. but the reaction stop continuing. and is used to treat leprosy, skin lesions, nodular erythema, such as graft-versus-host disease In 1998 the U.S. FDA approval of thalidomide in the United States formally listed for the treatment of nodular erythema like leprosy (ENL, through the mechanism of its therapeutic study found that thalidomide not only has sedative and hypnotic effects, but also has strong anti-angiogenic and immunomodulatory effects, has been in the blood and tumor rheumatic diseases has been more widely used. 1 Chemical Properties and Pharmacokinetics The chemical name for thalidomide N-(2,6 - dioxo -3-- piperidinyl - phthalimide, is a glutamic acid derivative, is a racemic, in the physiological pH conditions, There are two isomers S and R, S-type and related teratogenic effects, R-type and sedative effect on the body the two isomers can be quickly transformed into each other, because it has a glutamic acid and an aromatic ring, pHgt; 6 in the aqueous solution is very unstable and can spontaneously hydrolyze, for two different breaking point on the ring, so the hydrolysis products of up to 100, thalidomide is a light yellow crystalline powder, odorless and tasteless, slightly soluble in water, methanol, ethanol or acetone, soluble in dimethylformamide, or pyridine (DMSO), insoluble in ether, chloroform or benzene. melting point of 269 ~ 274 ℃ .1.2 pharmacokinetics in healthy volunteers and by the Hansen Disease patients [1] After a single oral dose of 200mg, the peak time for the 2.9-5.7h, an a