GI Drugs Flashcards
Antacids example
Gaviscon
Antacids MOA
- Compound containing alginate and 1+ antacid
- Alginate: increase viscosity of stomach contents to reduce reflux
- Antacids: buffer stomach acids
- After reacting with stomach contents, form a floating ‘raft’ which separates gastric contents from GOJ preventing mucosal damage
Antacids indications
- Ulcers
- Non-ulcer dyspepsia
- GORD
Antacids contraindications
- Aluminium / magnesium hydroxide should not be given to patients with hypophosphatemia
- Sodium bicarbonate avoided for patients on low salt diet
Antacids side effects
- constipation / diarrhoea
- flatulence
- stomach cramps
- nausea
Antacids interactions
Divalent cations in compound alginates bind to other drugs and reduce their absorption: ACEi, Abx, bisphosphonates, digoxin, levothyroxine, PPIs.
Doses should be taken at different times - 2 hour gap
Antacids patient info
Action prolonged if durg taken 1-3 hours after food
H2 receptor agonists examples
Ranitidine
H2 receptor agonists indications
- Peptic ulcer disease: treatment and prevention, although PPIs more effective
- GORD / dyspepsia: symptomatic relief
H2 receptor agonists MOA
Histamine from parietal cells binds to H2 receptor
Activates proton pump on parietal cell which secretes H+ into lumen (and draws K+ into cell)
Blockade of H2 = decreased acid
H2 receptor agonists contraindications
Dose reduction in renal impairment
H2 receptor agonists side effects
- Generally well tolerated
- Most common: bowel disturbance, headache, dizziness
PPIs examples
Lansoprazole, Omeprazole Patoprazole
PPIs indications
- Prevention and treatment of peptic ulcer disease including NSAID-associated ulcers
- Symptomatic relief of dyspepsia and GORD
- Eradication of H. Pylori in combination with antibiotics
PPIs MOA
- Irreversibly inhibit H+/K+ ATPase in gastric parietal cells.
- This reduces gastric acid secretion
- More effective than H2 receptor agonists
PPIs administration
Oral
Injectable
PPIs contraindications
-Risk of osteoporosis: can increase fracture risk
PPIs side effects
- GI upset
- Headache
- Reduce host defence against infection - increased risk of C. diff
- Prolonged treatment can cause hypomagnesia - can lead to ventricular arrhythmias
PPIs interactions
cP450 inhibitor
Reduce anti-platelet effect of clopidogrel by decreasing its activation by cP450
PPIs patient info
- Take with food or on empty stomach
- Best taken in morning
Anti-motility agents examples
Loperamide, codeine phosphate
Anti-motility agents indications
- Diarrhoea: symptomatic treatment - IBS or viral gastroenteritis
Anti-motility agents MOA
- Opioid which doesn’t penetrate the CNS so has no analgesic effects
- Agonist of the mu-opioid receptors in the GIT, which increases non-propulsive contractions of the gut smooth muscle
- Reduces peristaltic contractions
- Bowel content slowed . + sphincter tone increased
- Slower gut transit allows more time for water absorption which hardens stool
Anti-motility agents administration
Oral capsule, tablet, syrup
Anti-motility agents contraindications
- Acute ulcerative colitis: inhibition of peristalsis may increase of megacolon and perforation
- Clostridium difficile colitis: inc. diarrhoea associated with broad-spec antibiotic use
- Acute bloody diarrhoea: this may signify bacterial infection
Anti-motility agents side effects
- Constipation
- Abdominal cramping
- Flatulence
Laxatives examples
Senna, lactulose, macrogol
Laxatives indications
- Constipation and faecal impaction
- Bowel preparation prior to surgery
- Hepatic encephalopathy
Laxatives MOA
- Based on osmotically active substances are not digested / absorbed are left in lumen, and therefore hold water in the stool, maintaining its volume and stimulating peristalsis
- Lactulose increases gut transit rate and acidifies the stool which inhibits ammonia producing bacteria
Laxatives administration
Oral
Enema
Laxatives contraindications
- Intestinal obstruction: risk of perforation
2. Heart failure, ascites, electrolyte disturbance: enemas can cause significant fluid shift
Laxatives side effects
- Flatulence, nausea and abdominal cramps
- Diarrhoea
- Phosphate enemas can cause local irritation and electrolyte disturbance
Laxatives interactions
May enhance effects of warfarin
Aminosalicylates examples
Mesalazine, sulfasalazine
Aminosalicylates indications
- Ulcerative colitis: mesalazine 1st line
2. Rheumatoid arthritis: sulfasalazine acts as DMARD as part of combination therapy
Aminosalicylates MOA
Ulcerative colitis: Release 5-aminosalicylic acid, which is anti-inflammatory and immunosuppressive.
Aminosalicylates administration
Oral: coated in acid resistant substance so released further along gut
Foam enema
Suppository
Aminosalicylates contraindications
Aspirin hypersensitivity (aspirin is salicylate)
Aminosalicylates side effects
GI upset (nausea, dyspepsia)
Headache
Rare but serious blood abnormalities: leucopenia, thrombocytopenia
Renal impairment
Oligospermia
Hypersensitivity: rash, fever, liver damage
Aminosalicylates interactions
Drugs which alter gut pH e.g. PPIs - may cause premature breakdown
Anti-emetics examples
Metoclopramide, Domperidone
Anti-emetics indiactions
Prophylaxis and treatment of nausea and vomiting, particularly in context of reduced gut motility
Anti-emetics MOA
- D2-receptor antagonists
- D2 is main receptor in chemoreceptor trigger one of medulla, the area responsible for sensing emetogenic substances in blood e.g. drugs
- Dopamine is important NET in gut: promotes relaxation of stomach and lower oesophageal sphincter, inhibits gastroduodenal coordination
- D2 receptor agonists have prokinetic effect - promote gastric emptying
- Effective in nausea and vomiting due to chemoreceptor trigger zone stimulation and reduced gut motility
Anti-emetics adinistration
IV injections
Anti-emetics contraindications
- GI obstruction
2. Young - increased risk of extra-pyramidal side effects
Anti-emetics side effects:
- Diarrhoea
- Extra-pyramidal ssyndromes: dystonic reaction
Anti-emetics interactions
- Antipsychotics: increased risk of extra-pyramidal side effects
- Parkinson’s dopaminergic agents: antagonises