GI meds Flashcards

1
Q

Gastric antacids

A
  • Magnesium hydroxide produce Mg salt, which is very poorly absorbed and cause diarrhea.
  • Aluminum hydroxide reacts with HCl to form Aluminum chloride, which is insoluble and cause constipation and hypophosphatemia
  • Calcium carbonate: Hypercalcemia, nephrolithiasis, and constipation –fecal compaction
  • Ca, Mg, Al molecules can chelate tetracyline.
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2
Q

H2 antagonists

A
  • Ranitidine, Famotidine and Nizatidine are longer acting and more potent than older cimetidine.
  • Unlike cimetidine, newer drugs does not produce the antiandrogenic or prolactin stimulating effects.
  • They do not inhibit the mixed function oxygenase system in the liver (CYP450 enzymes).
  • Most common side effects are nausea, headache, and dizziness.
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3
Q

Cimetidine

A
  • Cimetidine SE’s - gynecomastia, elevated serum PRL, and confusion in elderly people
  • Strong inhibitor of CYP450 system -> slow metab of warfarin, procainamide, phenytoin, BZOs, theophylline, imipramine, and quinidine
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4
Q

Omeprazole

A
  • In animals, is associated w/gastric carcinoid tumors
  • Inhibs the metabolism of warfarin, phenytoin, diazepam, and cyclosporine
  • Small increase in resp and GI infxns. Decrease in sr. Mg2+ and hip fx’s w/LT use
  • Rarely pancreatitis, hepatotoxicity, and interstitial nephritis
  • Prolonged use of PPI and H2 blockers -> decreased bioavailability of B12, digoxin, and ketoconazole bc acid is required for absorption
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5
Q

Sucralfate

A
  • Sulfated disacch used in PUD
  • MOA - drug undergoes polymerization and selective binding to necrotic tissue -> barrir to acid Also stimulates endogenous PG synth
  • Sucralfate is INEFFECTIVE w/action of H2 rec blockers or PPI -> needs acidic pH to be activated. Do NOT administer w/antacids
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6
Q

Bismuth

A
  • Selectively binds ulcer and forms coating, protects from acid and pepsin
  • Some anti microbe effect on H. pylori
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7
Q

Misoprostol

A
  • PGE1. Decreases acid secretion, stimulates mucin and bicarbonate production
  • For gastric ulcers induced by NSAIDs
  • SE’s: diarrhea, abortions (d/t induction of uterine contractions during pregnancy), exacerbations of BID
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8
Q

Metoclopramide

A
  • Prokinetic via 5-HT4 agonist activity -> increased gastric emptying and intestinal motility
  • Higher doses - anti 5-HT3 and anti-D2 - anti-emetic
  • Uses: diabetic, post op gastroparessis, anti-emetic
  • Especially useful at high doses against highly emetogenic cisplatin
  • SE’s: anti-dopaminergic -> sedation, diarrhea, Parkinson’s
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9
Q

Cisapride

A
  • Gastroparesis, GERD, and constipation

* SE’s: arrhythmias

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10
Q

Cholinomimetics

A
  • Neostigmine - used for colonic pseudo-obstruction

* Bethanechol - used in GI and bladder atony. Opposite is atropine

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11
Q

Erythromycin

A
  • Macrolide. Acts on motilin recs of GIT
  • Used for gastric emptying before upper GI endoscopic procedures
  • Tolerance develops in gastroparesis
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12
Q

Substances that act on area postrema

A

• D2, 5-HT3, opioid/ACh, substance P

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13
Q

Aprepitant, Fosaprepitant

A
  • NK-1 rec blocker in CNS
  • Decreases early and delayed emesis in CA chemotherapy
  • Fosaprepitant is used IV
  • SE’s: dizziness, fatigue, diarrhea, CYP interaction
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14
Q

Prochlorperazine

A
  • Blocks D2 recs and muscarinic recs

* SE’s: extrapyramidal sx’s, hypotension, etc

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15
Q

BZOs

A
  • Antiemetic potency of lorazepam, alprazolam, and diazepam is low
  • Beneficial d/t sedative, anxiolytic, and amnesic properties
  • Useful in anticipatory vomiting
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16
Q

Sulfasalazine

A
  • Tx CD and UC. Inhibs pro-inflam IL1 and TNF-a
  • Sulfa derivative
  • Sulfapyridine (antibacterial) and 5-ASA (anti-inflam) released by colonic bacteria
  • SE’s: nausea, vomiting, diarrhea, hypersensitivity, reversible oligospermia, BM suppression d/t sulfapyrazine
17
Q

6-MP, MTX

A
  • Tx CD and UC. 6-MP may promote apoptosis of immune cells. MTX blocks DHF reductase
  • Cause generalized immune suppression
  • SEs: GI mucositis, myelopsuppression. Hepatotoxicity w/6-MP. Toxicities w/low dose MTX is rare
18
Q

Infliximab

A
  • Especially good for CD w/fistulas and acute flares. Also in RA
  • SEs: reactivate latent TB and other infxns. Given IV -> fever, chills, urticarial rxn, hypotension, Ab formation

• Adalimumab is similar

19
Q

Natalizumab

A

• Tx CD and UC. Blocks leukocyte integrins. Can produce multifocal leukoencephalopathy

20
Q

Corticosteroids in IBD

A
  • Hydrocortisone, prednisone, prednisolone used in acute cases
  • Inhibit TNF-a, IL-1, IL-8
  • Budesonide - ctrl-release formulaiton in distal ileum and colon
21
Q

Alosetron

A
  • Tx IBS- D. 5-HT3 antagonist w/long duration of action
  • Reduces smooth mm activity in the gut for IBS-D
  • Recommended for severe diarrhea
  • SEs: rare, serious constipation, ischemic colitis, infarction
22
Q

Anticholinergics used for IBS-D

A

• Hyoscyamine, dicyclomeine, glycopyrrolate, methscopolamine

23
Q

Lubiprostone

A

• Tx IBS-C. Chloride channel activator

24
Q

Loperamide, Diphenoxylate

A
  • Opiate derivatives. Antidiarrheals that slow motility w/negligible CNS effects
  • Acts via GI mu-opioid recs. Inhibs ACh release and decreases peristalsis
  • Diphenoxylate is formulated w/atropine to reduce abuse potential. High doses of diphenoxylate -> CNS effects
25
Q

Bile salt-binding resins

A
  • Cholestyramine, colestipol, colesevelam
  • Prevent diarrhea of IBS and IBD by blocking osmotic and irritating actions of bile salt
  • Form insoluble complexes w/bile in intestine
  • SEs: bad taste, GI discomfort, decreased fat-soluble vitamin absorption
26
Q

Stimulant laxatives

A
  • Castor oil, Senna, Bisacodyl, Cascara
  • May cause cramping
  • Chronic use -> habit of perceived need for laxatives
27
Q

Bulk forming agents

A
  • Agar, methylcellulose, psyllium, bran. Laxatives

* Increase water retention -> stools become bulky -> distention -> peristaltic stim of gut

28
Q

Osmotic laxatives

A
  • Mg citrate and MgOH (saline cathartics). Lactulose, sorbitol (non-digestible sugars)
  • Osmotically draw water into GIT -> stimulate motility
  • Used in simple constipation, bowel prep for endoscope
  • Lactulose -> lactic, formic, and acetic acid that also increase osmotic effect. Also used in hepatic encephalopathy to draw out ammonia (NH3), useful for preventing hyper ammonia
  • PEG - used for colonic lavage for endoscopic and radiological procedures
29
Q

Stool softeners

A
  • Mineral oil and docusate sodium. Emulsify stool. soften it, lubricate
  • Senna combined w/docusate for opioid constipation
30
Q

Opioid receptor antagonists

A

• Alvimopan, methylnaltrexone. Tx opioid-induced constipation -> block GI mu recs, do not enter CNS

31
Q

Ursodiol

A
  • Secondary bile acid, used to tx gallstones
  • Reduces chol absorption by breaking up micelles containing chop
  • Used in pt who refuses or not eligible for surgery
  • SE: diarrhea
32
Q

Octreotide

A
  • Long-acting SST
  • Uses: carcinoid tumors (appendix, ileum, rectum), VIPoma, acute variceal bleeding, and acromegaly
  • SEs: abdominal cramps, nausea, steatorrhea, gallstones, decreased endocrine and exocrine pancreatic activity

• Variceal hemorrhage - MOA uncertain. Alter portal blood flow and variceal pressure. Can also use propranolol and nadolol to reduce portal pressure