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PDA 1 GI Drugs
GI Drugs Mechanisms of Action
| Question | Answer |
|---|---|
| inhibit the activation of the H2 receptor; results in parietal cell inability to release H+ into the lumen due to H+/K+ ATPase activity loss | H2 receptor antagonists |
| ENTERIC COATED - allow absorption through small intestine - accumulates in the parietal cells --> covalently binds to H/K ATPase (irreversible deactivates it) | proton pump inhibitors |
| upon entering stomach, cross-links/polymerizes and adheres to epithelial cells and ulcer "craters" ALSO binds bile salts | sucralfate |
| stimulate EP3 receptor on parietal cells - activate Gprotein coupled receptor - decrease cAMP levels in parietal cells (inhibit H/K ATPase) stimulate mucous production in epithelial cells | prostaglandin analogs |
| reacts with and neutralizes stomach H+ | antacids |
| inhibit the 5-HT3 receptor | serotonic antagonists |
| inhibit dopamine receptors (D2) in the CTZ | dopamine receptor antagonists |
| inhibit input from the inner ear to the vestibular nuclei - only certain H1 property are effective (1st gen) | anti-histamines |
| inhibit muscarinic receptors (acetylcholine activates both muscarinic and H1 receptors as part of the vestibular nerve) | anti-cholinergics |
| binds to the neurokinin 1 receptor (NK1; GPCR) | substance P receptor antagonists |
| exact mech unknown stimulations of the CB1 subtype of the cannabinoid receptor on neurons in and around the vomiting center in the medulla | cannabinoids |
| does not have antiemetic properties!!! has sedative/anti-anxiety effects (given for anxiety related nausea) | lorazepam |
| 1) inhibition of dopamine receptors - results in increased motility by increasing cholinergic transmission 2) antiemetic: dopamine receptor antagonism in the CTZ: 5-HT3 receptor ANTAGONISM and 5-HT4 AGONIST (stimulates coordinated release of ACh into GI) | dopamine receptor antagonists |
| mimic function of natural 5-HT (serotonin) stimulate the myenteric plexus (5-HT3 and 5-HT4 receptors) - increase in motor function stimulate submucosal afferent neurons (receptors; 5-HT4 increased epithelial secretion) | serotonin receptor agonists |
| 22-amino acid peptide found in enterochromaffin and M cells of GI tract - receptors for it are found on smooth muscle cells and myenteric neurons --> stimulation results in coordinated contraction | motilides |
| peptide of varying length found in I cells of GI epithelium - receptors on acinar cells in pancreas, gall bladder, and sphincter of ODdia (allows bile to be delievered to the duodenum), and the duodenum (can result in delayed gastric emptying) | cholecystokinin |
| opioid receptors located on the enteric nerves, epithelia cells, and smooth muscle cells (involved in intestinal motility & absorption) these anti-diarrheals target peripheral receptors! - cause contraction of GI muscle - increase time in small intestin | opioid receptor agonists |
| interruption of the normal hepatic circulation of bile salts - results in excessive concentrations reaching the colon - more fat absorption from the intestine and less water/electrolyte secretion into the lumen of the GI | bile acid sequestrants |
| inhibit hormone secreting tumors of the pancreas and GI tract inhibit secretino of 5-HT, gstrin, secretin, pancreatic polypeptide, GLP-2 --> inhibit severe secretory diarrhea | somatostatin analogs |
| exact mech not understood - believed to have anti-secretory, anti-inflammatory, and anti-microbial effects | bismuth |
| 1) containing a mucilloid that undergoes fermentation in the colon - increase in bacterial mass 2) semisynthetic celluoses, resin calcium polycarbophil, or polymeric carbs are poorly fermented - absorb water and increase fecal bulk | fiber supplements |
| either the cation and/or the anion are poorly absorbed - creation of an osmotic gradient - pulls water into the GI tract or retains water in GI tract | saline laxatives |
| resistant to intestinal disaccharidase activity (can't be absorbed) - hydrolyzed to fatty acid chains: stimulates colonic motility by drawing water into lumen | non-digestable sugars |
| retain water in the lumen, the added ions ensure little to no ionic shifts | glycerin |
| act as anionic surfactants that lower the surface tension of stool to allow mixing of aqueous and fatty substances - preventative medicine | emollients (stool softeners) |
| 1) stimulates the enteric nerves resulting in colonic mass movement 2) increases fluid and electrolyte excretion | diphenylmethanes (stimulant laxatives) |
| inactive glycoside form is ingested --> converted to monoanthrone (Active form) by colonic bacteria 1) produces colonic contractions resulting in migration 2) induces water and electrolyte secretion | anthraquinone (stimulant laxatives) |
Created by:
astephens5
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