医学ppt课件消化系统药DigestiveSystem .ppt

timoprazole * Amphoteric stability stabilization capsule granule tablet pellet 注射剂 * Derivate sulfenic 双硫键 * Development of PP Inhibitor Hepatotoxicity (肝毒性) An antiviral drug originally Benzimidazole derivative Subsequently converted to sulfoxide, exhibiting highly potent, irreversible inhibition. PP Inhibitor----continued Trifluoroalkoxylation Omeprazole(奥美拉唑) Lansoprazole(兰索拉唑) Pantoprazole(泮托拉唑) 　Omeprazole (奥美拉唑) (R,S)-5-methoxy-2-(4-methoxy-3,5-dimethyl-2-pyridylmethylsulfinyl)benzimidazole A white to off-white crystalline powder with very slight solubility in water 1 2 3 4 5 Physico-chemical property Racemic mixture in clinic. S-isomer is more active. Esomeprazole( pure S-isomer) is launched in 2000. pyridine N, pKa 4.13 imidazole N-H, pKa 1.68 acid labile Formulated as delayed-release drug with enteric-coating. Mechanism of action Pharmacologic action Substantial first-pass biotransformation, oral administration is 30-40%. about 1 hour Its antisecretory actions persist for 24-72 hrs, which is consistent with its suggested mechanism of action involving irreversible inhibition of the proton pump. Approved for the treatment and reduction of risk of recurrence of DU, GERD(胃食管反流病), GU and pathological hypersecretory conditions. Chemical synthesis Section 2 Antiemetic (止吐药) Vomit A instinct, removing endogastric harmful substance. But maybe lead to water depletion, electrolyte chaos, disproportion of acid-base equilibrium, nutrition obstacle, etc. Some disease, pregnancy, radiotherapy and drug treatment for cancer can cause nausea and vomiting. Mechanism to stop vomitting The activity of vomit nervous reflex circellus(环) determined by many neurotransmitter (NT, 神经递质) antiemetic block this reflex Dopamine (多巴胺) 5-HT3 (5-羟色胺) Histamine (组胺) Acetylcholine (乙酰胆碱) Classification Nausea and vomit related to motion Caused by chemotherapy 　 Difenidol(地芬尼多) Thiethylperazine(硫乙拉嗪) Ondansetron(昂丹司琼) Caused by chemo and radiot