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Pharmacology Of Gi System Notes

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Lecture 5 Pharmacology of GI system LECTURE 1

• Nausea and vomiting o

 General

Act centrally to inhibit or prevent emesis Include antagonists of o D2 receptor (chemical trigger zone) o 5-HT receptor (chemical trigger zone) o H1-receptor (NTS) o AChM receptor (vomiting centre)


D2 Dopamine receptor antagonists o Phenothiazines- CHLORPROMAZINE & ACEPROMAZINE
 General

• Good at preventing vomiting agents directly stimulating CTZ

• Sedative action= more useful for motion sickness

• Also antagonises H1 and AChM receptors (dirty)
 Side effects

• Hypotension, platelet dysfunction, ataxia

• Not recommended for pregnant, affects babies (+500mg) o METACLOPRAMIDE
 General

• Blocks 5-HT3 receptors= large part of effect

• Peripheral actions- increased muscle tone in lower oesophageal sphincter (near stomach) to prevent vomiting
 Side effects

• As chlorpromazine, Diarrhoea 5-HT receptor antagonists o ONDANSETRON
 Particularly useful in chemo/radiotherapy
 Side effects: drowsiness & dizziness o NABILONE
 Synthetic cannabinoid (not first choice- addiction)
 Used in cytotoxic-induced vomiting
 Side effect: drowsiness & dizziness 5-HT4 receptor agonists o CISAPRIDE
 General

• Peripherally, increasing gastro-oesophageal sphincter contraction & GI motility

• Withdrawn= long QT-syndrome (death)
 Side effects (high dosage)

• Diarrhoea, abdominal cramp

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