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26 Cards in this Set

  • Front
  • Back

MOA of H2 antagonists

Competitive inhibitors of all histamine type 2 receptors. Inhibit histamine and gastrin stimulated gastric acid secretion by their action on parietal cells in the stomach

Indications for H2 antagonists

Gastric and duodenal ulcers


Gastro - oesophageal reflux


Treatment and prophylaxis of NSAID associated ulcers

Contraindications of H2 antagonists

Hypersensitiviy


If red flag features of malignancy, need to investigate prior to initiating treatment

Side effects of H2 antagonists

GI disturbances, especially diarrhoea


Gynaecomastia (cimetidine)

Metabolism and half life of H2 antagonists

Excreted largely unchanged in urine


T1/2 2-3hrs

Monitoring needed for H2 antagonists

None

Drug interactions of H2 antagonists

Cimetidine inhibits cytochrome P450 activity in liver and therefore potentiates the action of drugs such as warfarin, phenytoin and theophylline

Special uses of H2 antagonists

Rantidine can be used prior to anaesthesia in patients at high risk of aspiration particularly in obstetric practice (Mendelson's Syndrome)

MOA of laxatives

Bulk laxatives (ispaghula husk) - polysaccharide polymers that are not broken down by digestion and therefore increase stool volume. This stimulates intestinal peristalsis (due to the stretch reflex) a well as softening faeces



Osmotic laxatives (lactulose, Movicol) - these poorly absorbed salts increase the volume of water in the bowel lumen by osmosis thus increasing transit



Stimulant laxatives (senna, docusate sodium) - the primary effect is via direct stimulation of the myenteric plexus resulting in smooth muscle contrition and increased peristalsis



Faecal softeners (arachis oil) - these are surfactants that reduce surface tension and allow water to penetrate and soften faeces

Indications for laxatives

Constipation


Hepatic encephalopathy (lactulose - reduces ammonia producing organisms)

Side effects of laxatives

Flatulence


Diarrhoea


Abdominal cramps


Electrolyte disturbances

Drug interactions of laxatives

Lactulose may enhance warfarin effects in severe liver disease

Contraindications of laxatives

Bowel obstruction (risk of perforation)


Galactacaemia (lactulose only)


Acute inflammatory bowl disease


Severe dehydration

Monitoring needed for laxatives

None

Metabolism and half life of laxatives

Variable - most are broken down in the GIT tract with minimal absorption

Can laxatives cause tolerence

Yes, stimulant laxatives cause tolerance in chronic use

Metabolism and half life of PPIs

Extensively metabolised by the liver and excreted by both renal and biliary routes


T1/2 varies from 40 min to 2 hrs

Side effects of PPIs

GI disturbances (abdominal pain, nausea, vomiting, diarrhoea)


Increased risk of gastric infections due to hypochlorhydria

MOA of PPIs

Inhibit H/K ATPase on luminal surface of gastric parietal cells and therefore reduce gastric acid secretion

Monitoring needed for PPIs

None

Drug interactions of PPIs

PPIs are inducers of cytochrome P450 with some variation in potency between individual drugs and therefore may enhance effects of drugs metabolised in the liver

How long does it take for laxatives to take effect

2-3 days for bulking of osmotic laxatives

Indications for PPIs

Gastric/duodenal ulcers


As part of the triple therapy for eradication of H pylori


Gastro - oesophageal reflux disease


Acid - related dyspepsia


Hyper - secretory conditions, including Zollinger-Ellison syndrome


Prevention and treatment of NSAID associated ulcers

Contraindications of PPIs

Hypersensitiviy


If red flag features of malignancy, need to investigate prior to initiating treatment

PPIS vs H2 antagonists

PPIs reduce gastric acid secretion by >90% and H2 antagonists reduce by 50-60% making PPIs more effective at healing peptic ulcers

Special used of PPIs

IV PPIs can be used in the management of acute upper GI bleeds