Chemical constitution Structural features
➢ 17position R is －CH3……agonists ➢ 17 position R is －CH2CH＝CH2……antagonists ➢ 7 position NCH2CH－……inreversible compound
During the 1950s, a series of morphine-like potent analgesics were synthesized,such as pethidine,methadone,etorphine,fentanyl.
镇痛药Analgesics
Pain is a complex subjective sensation ，and a kind of protective response when organism suffer the nociceptive stimulus;
镇痛药 阿片生物碱类 罂粟(poppy） 阿片生物碱类
Fresh capsule of opium poppy
Hale Waihona Puke Cut capsule showing latex exuding from cut
镇痛药 阿片生物碱类 罂粟(poppy）
镇痛药 阿片生物碱类
含阿片生物碱类植物： 罂粟
吗啡 morphine
Types and effects
μ(mu) δ(delta)
κ(kappa)
Analgesia above spinal cord level spinal cord level spinal cord level
Respiratory depression ＋＋
＋＋
＋
Pupil
myosis
myosis
Morphine (1806，10% of opium total base） 吗啡 morphine Codeine （1832,methyl-morphine）
Heroin （1874, acetomorphine ，powerful addictive drugs
）
Isoquinoline
Papaverine
take orally, injection→pass through the blood brain barrier→hepatic metabolism→renal excretion
阿片(opium)生物碱类(opiate alkaloids) HO
Phenanthrene
O N CH3
HO
use analgesics immediately; But it is inadvisable to use narcotic analgesics when a pain
hasn`t be certified ，in order to avoid misdiagnosis.
阿片类药物Opium
Mechanisms and Effects
阿片受体 opioid receptor
In 1973,three American labs dicovered the receptor at the same time. Exist on cell membrane, glycoprotein。 High affinity Saturability Stereospecificity Distribution of definite area Specificity antagonists
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
Classification：
chemical constitution affinity and intrinsic activity
➢ Agonists：morphine,Pethidine,adanton…… ➢ Antagonists：Naloxone,Naltrexone ➢ Partial agonist：Pentazocine，Nalorphine Physiological disposition：
－
Stomach intestine decrease
decrease
－
SM spasm
＋＋
＋＋
－
Psychoactivity euphoria＋＋ euphoria＋＋ restlessness ＋
镇痛药 Analgesics
北京协和医学院基础医学院药理学系 叶菜英
镇痛药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.
镇痛药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；