镇痛药analgesics.ppt

镇痛药 Analgesics 北京协和医学院基础医学院药理学系 叶菜英 Analgesics Primary effect on CNS, eliminate or ease pain selectively, to lessen the nervous of patients, these agents relieve pain without producing a loss of consciousness. They are used primarily to relieve acute and chronicity pain of any origin. Analgesics It has been know for centuries that extracts of the opium poppy can be used to relieve pain and treat diarrhea. In 1806, Morphine was first isolated from the juice of the opium poppy by German pharmacist Friedrich Sertürner. During the 1950s, a series of morphine-like potent analgesics were synthesized, such as pethidine,methadone, etorphine,fentanyl. Analgesics Pain is a complex subjective sensation, and a kind of protective response when organism suffer the nociceptive stimulus. Pain is also the basis for the doctors diagnosing diseases. It usually accompany anxiety, dread, horror, discomfort and so on, to cause the patients disorder, even shock. Acute pain that has been made a definite diagnosis, should use analgesics immediately. But it is inadvisable to use narcotic analgesics when a pain hasn`t be certified, in order to avoid misdiagnosis. Opium (阿片类药物) 【Classification】 chemical constitution affinity and intrinsic activity Agonists: Morphine, Pethidine, adanton…… Antagonists: Naloxone, Naltrexone Partial agonist: Pentazocine, Nalorphine 【 Physiological disposition 】 take orally, injection→pass through the blood brain barrier→hepatic metabolism→renal excretion Morphine Chemical constitution Structural features 17position R is －CH3……agonists 17 position R is －CH2CH＝CH2……antagonists 7 position NCH2CH－……inreversible compound Mechanisms and Effects Opioid receptor In 1973, three American labs discovered the receptor at the same time. Exist on cell membrane, glycoprotein High affinity Saturability Stereospecificity Distribution of definite area Specificity antagonists Types and effects μ(mu) δ(delta) κ(kappa) Analgesia above spinal cord level spi