2009A07 Outline the subtypes of serotonin (5-hydroxytryptamine) receptors.
Discuss pharmacological agents that act at these sites.

 

List:

·      Intro

·      Serotonergic drugs

·      Serotonin syndrome

 

Intro:

·         Monoamine receptor in CNS, PNS, vascular smooth muscle (dilate and constrict), platelets

·         Multiple subtypes: 1ABCD, 2ABC, 3, others

·         Mostly metabotropic GPCR, except 5HT3 ligand-gated ion channel (activity -> depolarisation)

·         Both excitatory and inhibitory

 

Serotonergic drugs by class:

Anti-depressants

·   SSRI (e.g. fluoxetine)

·   SNRI (e.g. duloxetine)

·   TCA (e.g. amitryptiline)

·   MAOi (e.g. moclobemide)

Anti-emetics

·   5-HT3 antagonists (e.g. ondansetron)

·   Metoclopramide (central 5-HT3 antagonist, peripheral 5-HT4 agonist

Non-opioid analgesics

·   Paracetamol (5-HT1A)

·   Ketamine

Opioid analgesics

·   Tramadol

·   Methadone

·   Pethidine

Anaesthetic agents

·   Halogenated ether anaesthetics

·   Propofol

·   Ketamine

Other

·   5HT1D: sumatriptan

·   5HT2: ketanserin, methylsergide, pizotifen

·   5HT2A: ergometrine, phenoxybenzamine

·   LSD: ?

 

Serotonin syndrome:

Cause

·   Multiple drugs increasing serotonergic activity

·   Especially MAOi

Features

·   Autonomic: ↑HR, ↑BP, shivering, sweating, dilated pupils

·   Somatic NS: hyperreflexia, myoclonus

·   CNS: agitation

·   GIT: abdo pain, nausea/vomiting, diarrhoea

Treatment

·   Cyproheptadine

·   Supportive

 

 

 

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