PHAR 100 Lecture Notes - Lecture 10: Opioid Receptor, Active Metabolite, Naloxone
12 Nov 2016
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Lecture 10 summary narcotic analgesics (opiates and opioids) Opioids are natural or synthetic drugs that exhibit effects on the body similar to morphine. Natural opioids are usually derivatives from the poppy plant morpheine and codeine. Synthetic opioids include heroin (morphine with 2 acetyl groups highly lipid soluble and very addictive). Other synthetic examples include: meperidine (similar to morphine but shorter acting), methadone and laam and mptp (gave people early onset parkinsons!). Antagonists include nalaxone (blocks opioid receptor activity) and mixed agonist antagonists. The active metabolite of morphine is morphine -6- glucuronide (10 -12 x more potent analgesic than morpheine). The active metabolite of heroin is morphine and monoacetylmorphine. Heroin is 10 x more lipid soluble that morphine. It has 2 acetyl groups on it which makes it more non polar. Thus like dissolved like so its effects would be much faster and probably more potent. Because heroin is so lipid soluble it concentrates itself in the brain faster the morphine.
