19.2 Gastrointestinal drugs Flashcards
Which first line medication is used to treat gastro-oesophageal reflux disease?
Proton pump inhibitors e.g. omperazole, lansoprazole
Give examples of drugs used to treat GORD, dyspepsia, peptic ulcers and upper gastrointestinal haemorrhages.
- Alkali alginate mixtures e.g. gaviscon
- H2 receptor antagonists e.g. ranitidine, cimetidine
- PPIs e.g. omeprazole
Describe the action of H2 receptor antagonists.
- Antagonise (block) the H2 receptor on the gastric parietal cells
- Reduces gastric acid secretion
- Less effective than PPIs
- Preferable for long term use
Do H2 receptor inhibitors interact with other drugs?
Yes, they interfere with a range of drugs.
E.g. Cimetidine interacts with warfarin, erythromycin, antifungals, carbamazepine
Give examples of proton pump inhibitors.
- Esomeprazole
- Lansoprazole
- Omperazole
- Pantoprazole
- Rabeprazole
How do H2 receptor antagonists act on the gastric parietal cells?
They block histamine 2 from binding to the H2 receptor of the parietal cell, thus preventing the production of cAMP and therefore preventing the function of the proton pump.
How do proton pump inhibitors act on gastric parietal cells?
Irreversibly inhibit the proton pump H/K-ATPase thus preventing acid secretion.
Describe the main features of PPIs.
- Prodrugs which require gastric acid for their conversion
- Good oral bioavailability
- Short plasma half life, approx.1 hour
- Duration of action is longer than 1 hour as they covalently bond causing irreversible inhibition of the proton pump - duration of acid suppression = 48 hours
Which enzymes metabolise PPIs?
- CYP2C19
- 3A4
What are the possible adverse side effects of PPIs?
- Hyponatraemia (low sodium)
- Fractures
- C.difficile infection
- Hypomagnesaemia
- Gastric cancers
- B12 deficiency
- Acute intestinal nephritis
- Pneumonia
- Cardiovascular disease
Which drug does omeprazole interact with?
Omeprazole interacts with clopidogrel, reducing its antiplatelet effects
What is H. pylori?
Helicobacter Pylori is a bacteria which infects the stomach, it is a major risk factor for peptic ulcers and stomach cancer.
How can we test for H. pylori?
- Carbon-13 urea breath test
- Stool antigen test
How is H. pylori treated?
- 7 day, twice daily course of treatment with: a PPI, amoxicillin and clarithomycin or metronidazole
- Pencillin allergy: 7-day, twice daily course of treatment with a PPI and clarithromycin and metronidazole
How should patients take PPIs?
- Prescribe the lowest effective dose for the minimum period of time
- Advise patients to take them 30-60 minutes before breakfast
- Risk of rebound hypersecretion on discontinuation for possibly 2-4 weeks after