Gastrointestinal Drugs Flashcards
Describe how to reduce acid secretion in the stomach. (5)
Target the parietal cell: M3 ACh receptors H2 histamine receptor (key) CCKB Gastrin receptor Direct cavalry stimulation
Describe H2 receptor antagonists.
MoA (2)
Pharmacokinetics. (2)
ADRs (1)
Inhibits histaminergic stimulation of parietal cells to reduce acid output.
t1/2 of 6-8 hours, so needs to be given bd.
Loose stools.
Give an example of a H2 antagonist. (1)
Ranitidine.
Describe proton pump inhibitors.
MoA (4)
Reversal (2)
Health concerns. (5)
Binds in its active state to active pumps (pumps only active after eating, so needs to be taken before food) to prevent secretion of H+. Takes 3-5 cycles to reduce acid production.
Once ceased, acid secretion returns in 2-3 days.
High Gastrin seen here (trying to prompt the parietal cells) was though to be harmful like in Zollinger-Ellison, but it’s not. Also associated with osteoporosis in long term use (affects calcium absorption).
Describe Zollinger-Ellison Syndrome. (2)
A gastrinoma (Gastrin secreting tumour) leading to high gastrin, and so high acid secretion.
Name three PPIs. (3)
Give the common feature of the names of PPIs. (1)
Lansoprazole, omeprazole, esomeprazole.
-prazole
Describe the initial treatments for peptic disease that are available OTC. (6)
Antacids - bicarbonate Lifestyle changes - weight loss, diet Alginates - gaviscon - forms a viscous layer over the exposed mucosa to stop irritation. H2 receptor antagonists PPIs
Describe the treatment plan of a patient with peptic ulceration. (4)
Explain the low compliance of this plan. (1)
Stop NSAIDs Begin H. Pylori eradication: Clarithromycin Amoxicillin Lansoprazole Over 100 tablets in a day.
Explain the differences between regurgitation and vomiting. (4)
Vomiting is Involuntary, and forceful expulsion of gastric contents, regurgitation is effortless and relating to a problem of the LOS closing.
Describe the stages in vomiting (8)
CTZ in the medulla signals to vomit Nausea, sweating, salivation occur during intestinal reverse peristalsis. Deep inspiration Closure of glottis Abdominal muscles contract Lower oesophageal sphincter relaxes Vomiting occurs.
Describe the types of things that can trigger the chemoreceptor trigger zone (CTZ) and give an example of each type. ((8)
Sensory afferent via the midbrain eg a bad smell
Direct triggers eg drugs, hormones, toxins
Visceral afferent from gut eg stretch in obstruction
Vestibular nuclei eg in motion sickness.
Name two drugs acting primarily on the vestibular nuclei. (2)
Hyoscine hydrobromide
Cyclizine
Describe Hyosine Hydrobromide.
MoA (2)
Uses (3)
Side effects (4)
Muscarinic receptor competitive antagonist - blocks body wide ACh.
Used in motion sickness and bowel obstruction (reduced GI secretions is good)
Side effects: sedation, dry mouth, constipation, glaucoma.
Describe Cyclizine.
MoA (2)
Uses (3)
Side effects (4)
H1 receptor antagonists - antihistamines
Used to reduce motion sickness, help you sleep (drowsiness), reduce allergic reactions.
Side effects: drowsiness, antimuscarinic effects (dry mouth, constipation, urinary retention), and long QT syndrome.
Name three drugs that act primarily on the visceral gut afferents. (3)
Ondansetron
Metaclopramide
Domperidone
Describe Ondansetron.
MoA (3)
Side effects (4)
5HT3 (seratonin) receptor antagonist that reduces GI motility and GI secretions
Side effects are rare but can include constipation, headache, long QT syndrome, deranged LFTs, Parkinsonism.
Describe metaclopramide.
MoA (4)
Uses (2)
Side effects (3)
D2 receptor antagonists - increased ACh at muscarinic receptors - promotes gastric emptying and increases peristalsis.
Good in GORD or ileus.
Side effects include galactorrhoea, dystonia and Parkinsonism.
Describe domperidone.
MoA (1)
Uses (1)
Side effects (2)
D2 receptor antagonist used to improve lactation in breastfeeding mothers.
Side effects include sudden cardiac death (long QT and VT) and severe galactorrhoea.