General A potent opioid analgesic. The "gold standard" of pain relief. High potential for tolerance and addiction. Mimics natural 'pain relief' chemicals - endorphins and cephalins Action Morphine is a phenanthrene phenanthrene opioid receptor agonist – its main effect is binding to and activating the μ-opioid receptors in the central nervous system.Blocks calcium and potassium flux via GPCRs and protein kinase cascade. Binds very strongly. Antitussive. Blocks peristalsis - therefore anti-diarrhoea Administration Can be taken orally, rectally, subcutaneously, intravenously, intrathecally or epidurally. Pharmacokinetics Extensive first-pass metabolism by liver (only 40 - 50 % of an oral dose reaches CNS). Elimination half-life 120 mins. Structure  |
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