L 27-28 GI Flashcards
Name some antacids and their common side effects
Sodium bicarbonate: produces CO2 which can be harmful, metabolic alkalosis, sodium dangerous in CHF Calcium carbonate: alkalosis, milk alkali from too much Ca, acid rebound Magnesium hydroxide: poorly absorbed, diarrhea, Mg++ may accumulate if kidney function low Aluminum hydroxide: constipation, combined with Mg, low renal function may cause problems
What are the benefits and downsides to antacids?
Antacids are useful for immediate relief of heartburn and gastritis. However, it is a temporary fix and can result in a rebound effect. Must be careful with high Na levels. They also have an effect on drug absorption by changing the pH of the stomach.
Describe the production of acid in the stomach including signaling molecules, receptors, and pathways
Describe the mechanism of action for H2 antagonists as well as general characteristics of these drugs
H2 signals parietal cells to produce H+ by increasing cAMP through Gs coupled receptor.
This increases the presence of kinases that activate the H+/K+ ATPase
Blocking this receptor blocks a signal to produce H+
These are best at reducing nocturnal acid production
Few side-effects: headache, dizziness, rash, itch, nausea
Cimetidine is unique in that it is anti-testosterone causing gynecomastia, loss of libido, and impotence. It also inhibits P-450 system causing numerous drug interactions.
Describe the four cells involved in acid production in the stomach and the signaling molecules used between them
Name the H2 blockers
Cimetidine
Ranitidine
Famotidine
Nizatidine
What drig interactions are possible with Cimetidine?
Cimetidine affects the P-450 system and therefore has an effect on many drugs.
Effect most commmonly on drugs with narrow therapeutic window such as: warfarin, phenytoin, theophylline, propranolol, benzos, tca, nifedipine, digoxin, quinidine
Other H2 blockers do not inhibit metabolism!
Mechanism of action for PPI’s
Bind irreversibly to H+/K+ ATPase completely blocking production of H+
Irreversible binding allows a longer duration of action and fewer doses needed
Prodrug that must be activated and therefore is taken 30 min before meals
Name the PPI’s
Omeprazole
Esomeprazole
Lansoprazole
Rabeprazole
Pantoprazole
Side effects of PPI’s
N/D, colic weight gain
Osteoporosis from decreased Ca++ absorption
Hypomagnesia causing muscle spasms
Increased risk of pneumonia from bacterial overgrowth
Possible that Omeprazole inhibits P-450
Sucralfate (Carafate)
Provides a protective barrier for the stomach
Causes constipation
Rarely used
Misoprostol (cytotec)
Prostaglandin E1 analogue
Prevent damage from NSAID use
Causes diarrhea like all PG’s
Must not be used in pregnancy
Metoclopramide
D2 antagonist increasing Ach release which increases parasympathetic tone to increase motion of the bowels
Also acts as anti-emetic
Cramping and diarrhea common
High doses cause parkinson-like symptoms
Bethanechol
Prokinetic agent
Muscarinic agonist
Erythromycin
Acts on motilin receptors as a prokinetic agent
Sometimes used for diabetic gastroparesis