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Morphine

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

C
an 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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