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Medical Pharmacology > GI Drugs > Flashcards

GI Drugs Flashcards

1
Q

Esomeprazole

A

Proton Pump Inhibitor

  • Produg modified by acidic environment. Covalently (irreversible) modify active site of H+/K+ ATPase. Short duration (2 h) but effective due to slow turnover of H+/K+ ATPase pump. Treatment takes several days. Reduce acid by 90%
  • Effective treatment for GERD, erosive esophagitis, PUD, Zolllinger-Ellison syndrome, NSAID-induced gastric ulcer, H. pylori treatment.
  • Clearance through liver. Increases Warfarin concentration, decreases activation of clopidogrel. Hepatic failure reduces clearance!
  • Few side effects. Nausea, abdominal pain, constipation, flatulence, diarrhea. Rare: myopathy, arthralgias, headaches and rashes. Rebound hypergastrinemia and increased gastrin secretion.
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2
Q

Lansoprazole

A

Proton Pump Inhibitor

  • Produg modified by acidic environment. Covalently (irreversible) modify active site of H+/K+ ATPase. Short duration (2 h) but effective due to slow turnover of H+/K+ ATPase pump. Treatment takes several days. Reduce acid by 90%.
  • Effective treatment for GERD, erosive esophagitis, PUD, Zolllinger-Ellison syndrome, NSAID-induced gastric ulcer, H. pylori treatment.
  • Clearance through liver. Increases Warfarin concentration, decreases activation of clopidogrel. Hepatic failure reduces clearance!
  • Few side effects. Nausea, abdominal pain, constipation, flatulence, diarrhea. Rare: myopathy, arthralgias, headaches and rashes. Rebound hypergastrinemia and increased gastrin secretion.
  • Can be given parenterally
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3
Q

Omeprazole

A

Proton Pump Inhibitor

  • Produg modified by acidic environment. Covalently (irreversible) modify active site of H+/K+ ATPase. Short duration (2 h) but effective due to slow turnover of H+/K+ ATPase pump. Treatment takes several days. Reduce acid by 90%.
  • Effective treatment for GERD, erosive esophagitis, PUD, Zolllinger-Ellison syndrome, NSAID-induced gastric ulcer, H. pylori treatment.
  • Clearance through liver. Increases Warfarin concentration, decreases activation of clopidogrel. Hepatic failure reduces clearance.
  • Few side effects. Nausea, abdominal pain, constipation, flatulence, diarrhea. Rare: myopathy, arthralgias, headaches and rashes. Rebound hypergastrinemia and increased gastrin secretion.
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4
Q

Cimetidine

A

H2 Receptor Antagonist

  • Block base level of acid secretion by ECL cells. Reduce acid by 70%. 4-5 h duration.
  • Useful for Zollinger-Ellison syndrome (excessive gastrin secretion), nocturnal acid secretion, duodenal ulcers
  • Side effects: diarrhea, headache, drowsiness, fatigue, muscle pain. Rare CNS effects in elderly and following parenteral administration. Rebound gastritis. Tolerance can develop in 3 days. Decreased pepsin and intrinsic factor.
  • Long term use of Cimetidine at high doses can decrease testosterone binding to androgen receptor and hydroxylation of estradiol causing galactorrhea in women and feminization of men
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5
Q

Famotidine

A

H2 Receptor Antagonist

  • Block base level of acid secretion by ECL cells. Reduce acid by 70%. 10-12 h duration.
  • Useful for Zollinger-Ellison syndrome (excessive gastrin secretion), nocturnal acid secretion, duodenal ulcers
  • Side effects: diarrhea, headache, drowsiness, fatigue, muscle pain. Rare CNS effects in elderly and following parenteral administration. Rebound gastritis. Tolerance can develop in 3 days. Decreased pepsin and intrinsic factor.
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6
Q

Ranitidine

A

H2 Receptor Antagonist

  • Block base level of acid secretion by ECL cells. Reduce acid by 70%. 6-8 h duration.
  • Useful for Zollinger-Ellison syndrome (excessive gastrin secretion), nocturnal acid secretion, duodenal ulcers
  • Side effects: diarrhea, headache, drowsiness, fatigue, muscle pain. Rare CNS effects in elderly and following parenteral administration. Rebound gastritis. Tolerance can develop in 3 days. Decreased pepsin and intrinsic factor.
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7
Q

Sucralfate

A

Misc. Acid Blocker

  • An octosulfate of sucrose with aluminum hydroxide. Forms a sticky neutral pH polymer that coats gastric epithelium.
  • Used for stress ulcers
  • Acid-activated so avoid acid-reducing drugs
  • Side effect is constipation, can block gastric absorption of some drugs
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8
Q

Aluminum Hydroxide

A

Antacid

  • Neutralize pH of gastric contents. Mg fast acting and stimulates gastric emptying, Al is slower acting and delays emptying and slows motility.
  • Side effects include rebound acid secretion. For AlOH: constipation, nausea, possible phosphate loss, binds tetracyclines. Any Mg-containing antacid contraindicated in renal disease.
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9
Q

Calcium Carbonate

A

Antacid

  • Neutralize pH of gastric contents. Mg fast acting and stimulates gastric emptying, Al is slower acting and delays emptying and slows motility.
  • Side effects include rebound acid secretion. For AlOH: constipation, nausea, possible phosphate loss, binds tetracyclines. Any Mg-containing antacid contraindicated in renal disease.
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10
Q

Magnesium Hydroxide

A

Antacid

  • Neutralize pH of gastric contents. Mg fast acting and stimulates gastric emptying, Al is slower acting and delays emptying and slows motility.
  • Side effects include rebound acid secretion. For AlOH: constipation, nausea, possible phosphate loss, binds tetracyclines. Any Mg-containing antacid contraindicated in renal disease.
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11
Q

Magnesium Trisilicate

A

Antacid

  • Neutralize pH of gastric contents. Mg fast acting and stimulates gastric emptying, Al is slower acting and delays emptying and slows motility.
  • Side effects include rebound acid secretion. For AlOH: constipation, nausea, possible phosphate loss, binds tetracyclines. Any Mg-containing antacid contraindicated in renal disease.
  • Silica is absorbed and may cause renal stones
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12
Q

Misoprostol

A

Prostaglandin Analogue

  • Synthetic analogue of PGE1. Reduces basal or food-induced acid production by 80-90%. Short acting.
  • Generally only used to prevent NSAID-induced gastric injury
  • Side effects: diarrhea, can exacerbate IBD, will induce contractions in pregnant women and abortion
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13
Q

Pirenzepine

A

Muscarinic Antagonist

  • Selective for M1 receptors. Blocks upstream neurotransmission at the intramural ganglia resulting in less stimulation of parietal and ECL cells. Reduces basal acid production by 40-50%.
  • Used to decrease acid production
  • Significant anticholinergic side effects
  • Rarely used
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14
Q

Bethanechol

A

Prokinetic Agent, Muscarinic Agonist

  • Cholinergic derivative used to activate M2 and M3 receptors.
  • Used to stimulate urination in post-surgical patients
  • Side effects include bradycardia, flushing, diarrhea, crams, salivation, blurred vision
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15
Q

Cisapride

A

Prokinetic Agent, Serotonin Receptor Partial Agonist, adenylate cyclase stimulant

  • Serotonin increases gastric motility
  • Used to treat GERD
  • Side effects include fatal arrhythmias. Need FDA permission
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16
Q

Erythomycin

A

Prokinetic Agent, Motilin analogue

  • Motilin is a 22 aa peptide that increases motility and is secreted by enterochromaffic cells and M cells in upper small bowel. Erythromycin is a macrolide antibiotic that mimics motilin. Causes dramatic gastric dumping.
  • Used to move bezoars and treatment of ileus, scleroderma and pseudo-obstructions
  • Not for chronic use, fast dumps can be painful
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17
Q

Metoclopramide

A

Prokinetic Agent, Dopamine Receptor Antagonist

  • Dopamine decreases ACh release, so this drug enhances normal ACh responses. Increases upper GI motility and lower esophageal sphincter tone.
  • Used to treat GERD (will not promote healing), antiemetic, laxative.
  • Side effects include extrapyramidal side effects, dystonias, Parkinson-like symptoms, tardive dyskenesia
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18
Q

Neostigmine

A

Prokinetic Agent, Acetylcholinesterase Inhibitor

*Used in acute treatment of an ileus

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19
Q

Tegaserod

A

Prokinetic Agent, Serotonin Receptor Partial Agonist

  • Serotonin increases gastric motility
  • Used to treat women with IBD. Can improve lower bowel motility in cases with chronic constipation and bloating. Only mildly effective.
  • Side effects include fatal arrhythmias. Need FDA permission
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20
Q

Magnesium Citrate

A

Osmotic Laxative, Salt

  • Non-absorbable, causes water retention in bowel and laxative effect (low dose) or cathartic effect (high dose)
  • Mg may stimulate CCK receptors and increase motility
  • Not for use in patients with renal insufficiency, cardiac disease, electrolyte abnormalities or with diuretic use.
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21
Q

Magnesium Sulfate

A

Osmotic Laxative, Salt

  • Non-absorbable, causes water retention in bowel and laxative effect (low dose) or cathartic effect (high dose)
  • Mg may stimulate CCK receptors and increase motility
  • Not for use in patients with renal insufficiency, cardiac disease, electrolyte abnormalities or with diuretic use.
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22
Q

Polyethylene Glycol

A

Osmotic Laxative, Alcohol

*Non-absorbable, causes water retention in bowel, laxative at low doses, cathartic agent (super pooper) at high doses

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23
Q

Lactulose

A

Osmotic Laxative, Sugar

  • Non-absorbable, causes water retention in bowel and laxative effect
  • Used for constipation associated with opioid use and vincristine
  • Bacterial fermentation can drop luminal pH and trap NH4 (increased in colon of Pts with severe hepatic disease)
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24
Q

Mannitol

A

Osmotic Laxative, Sugar

  • Non-absorbable, causes water retention in bowel and laxative effect
  • Used for constipation associated with opioid use and vincristine
25
Q

Sorbitol

A

Osmotic Laxative, Sugar

  • Non-absorbable, causes water retention in bowel and laxative effect
  • Used for constipation associated with opioid use and vincristine
26
Q

Docusate

A

Stool-Softening Laxative, Salt

  • Surfactant that allows mixing of fatty substances and water in stool.
  • Does not increase frequency of defecation
27
Q

Bisacodyl

A

Irritant Laxative

  • Oral or rectal admin.
  • High doses result in catharsis. Warn pts not to take antacids or milk or chew tablets to ensure activation in small intestine
28
Q

Castor Oil

A

Irritant Laxative
*General smooth muscle stimulant. A ricinoleic acid speeds motility in the small bowel. Low dose laxative, high dose cathartic.

29
Q

Glycerine

A

Irritant Laxative

  • Suppository that acts as hydroscopic agent and lubricant. Increases water retention and stimulates peristalsis and produces an evacuation reflex
  • Rectal admin produces bowel movement within 1 h
30
Q

Methylcellulose

A

Bulk Forming Laxative

*may exacerbate intestinal obstruction, may absorb other drugs

31
Q

Polycarbophil

A

Bulk Forming Laxative

*may exacerbate intestinal obstruction, may absorb other drugs

32
Q

Psyllium

A

Bulk Forming Laxative

*may exacerbate intestinal obstruction, may absorb other drugs

33
Q

Bismuth Subsalicylate

A

Antidiarrheal Agent

*Complex of bismuth and salicylate. salicylate is released in stomach and absorbed systemically.

34
Q

Diphenoxylate

A

Opioid Antidiarrheal

  • Piperidine derivative
  • Can have CNS effects, packaged with Atropine to discourage abuse
35
Q

Loperamide

A

Opioid Antidiarrheal

  • u-opioid receptor agonist that stops bowel motility
  • 40-50X more potent than morphine
  • Doesn’t enter the CNS
36
Q

Octreotide

A

Antidiarrheal Agent, somatostatin analogue

  • Parenterally administered octapeptide used to combat secretory diarrhea of hormone secreting tumors.
  • Used for post-surgical gastric dumping syndrome and diarrhea associated with chemotherapy. Also used to rest the pancreas in pancreatitis.
  • Side effects include nausea, bloating, injection site pain
  • Long term use may result in gall stones
37
Q

Chlorpromazine

A

Dopamine Receptor Antagonist, Antiemetic

  • Targets D2 receptors in CTZ and H1 receptors
  • General antinauseant and antiemetic, also treats motion sickness (H1)
  • Used to treat chemotherapy induced nausea but not as effective as serotonin receptor antagonists or metoclopramide
  • Can cause Parkinson-like symptoms and dysphoria
38
Q

Cyclizine

A

Antihistamine Antiemetic

  • H1 receptor antagonist, works on brainstem and vestibular apparatus. Anticholinergic effects used to treat abdominal cancer
  • Treats motion sickness, post-operative emesis
39
Q

Diphenhydramine

A

Antihistamine Antiemetic

  • H1 receptor antagonist, works on brainstem and vestibular apparatus.
  • Treats motion sickness, post-operative emesis
40
Q

Dimenhydrinate

A

Antihistamine Antiemetic, salt of diphenhydramine

  • H1 receptor antagonist, works on brainstem and vestibular apparatus.
  • Treats motion sickness, post-operative emesis
41
Q

Dolasetron

A

Serotonin Receptor Antagonist Antiemetic

  • Blocks serotonin receptor, acts on CTZ and STN (centrally) and in small intestine. 7-9 h
  • Used for chemotherapy-induced emesis and nausea
  • Liver excretion
42
Q

Hydroxyzine

A

Antihistamine Antiemetic

  • H1 receptor antagonist, works on brainstem and vestibular apparatus.
  • Treats motion sickness, post-operative emesis
43
Q

Granisetron

A

Serotonin Receptor Antagonist Antiemetic

  • Blocks serotonin receptor, acts on CTZ and STN (centrally) and in small intestine. 9-12 h
  • Used for chemotherapy-induced emesis and nausea
  • Liver excretion
44
Q

Palonosetron

A

Serotonin Receptor Antagonist Antiemetic

  • Blocks serotonin receptor, acts on CTZ and STN (centrally) and in small intestine. 40 h!
  • Used for chemotherapy-induced emesis and nausea
  • Highest affinity of all SRAAs, parenteral administration only!
  • Kidney and Liver excretion
45
Q

Ondansetron

A

Serotonin Receptor Antagonist Antiemetic

  • Blocks serotonin receptor, acts on CTZ and STN (centrally) and in small intestine. 4 h
  • Used for chemotherapy-induced emesis and nausea
  • Liver excretion
46
Q

Prochlorperazine

A

Dopamine Receptor Antagonist, Antiemetic

  • Targets D2 receptors in CTZ and H1 receptors
  • General antinauseant and antiemetic, also treats motion sickness (H1)
  • Used to treat chemotherapy induced nausea but not as effective as serotonin receptor antagonists or metoclopramide
  • Can cause Parkinson-like symptoms and dysphoria
47
Q

Promethazine

A

Antihistamine Antiemetic

  • H1 receptor antagonist, works on brainstem and vestibular apparatus.
  • Treats motion sickness, post-operative emesis
48
Q

Scopolamine

A

Anticholinergic, Muscarinic ACh Receptor Antagonist

  • Can be parenteral but often transdermal. Acts on vestibular apparatus.
  • Very effective for short or long-term motion sickness prevention. Post operative emesis.
  • Not effective for chemotherapy induced nausea, minimal CTZ effects.
  • Common side effects include dry mouth, blurred vision and uncontrolled behavior when used in the presence of pain or anxiety
49
Q

Apomorphine

A

Emetic

*Sub-Q administered. Acts locally and on CTZ

50
Q

Ipecac

A

Emetic

*Orally administered. Acts on CTZ

51
Q

6-mercaptopurine

A

Anti-tumor anti-metabolite used to treat IBD

52
Q

Adalimumab

A

Anti-TNF Ab human, less effective than infliximab

53
Q

Alosetron

A

Prokinetic Agent, Serotonin Receptor Partial Agonist, adenylate cyclase stimulant

  • Serotonin increases gastric motility
  • Used to treat GERD
  • Side effects include fatal arrhythmias. Need FDA permission
54
Q

Budesonide

A

Corticosteroid

55
Q

Infliximab

A

Anti-TNF Ab humanized mouse

56
Q

Mesalamine

A

5-ASA

  • Inhibits TNF activity
  • Delivered as enteric coated tablet that is delayed release in the small bowel
  • Treats flare ups and maintains remission in UC, Treats flare ups in Chrons but not remission
  • Side effects include nausea, fatigue, allergic reactions, contraindicated in pregnancy.
  • May cause interstitial nephritis
57
Q

Osalazine

A

5-ASA

  • Inhibits TNF activity
  • Delivered as pro-drug activated in colon by bacterial enzymes
  • Treats flare ups and maintains remission in UC, Treats flare ups in Chrons but not remission
  • Side effects include nausea, fatigue, allergic reactions, contraindicated in pregnancy.
58
Q

Prednisone

A

Glucocorticoid used to treat IBD

59
Q

Sulfasalazine

A

5-ASA

  • Inhibits TNF activity
  • Delivered as pro-drug activated in colon by bacterial enzymes
  • Treats flare ups and maintains remission in UC, Treats flare ups in Chrons but not remission
  • Side effects include nausea, fatigue, allergic reactions, contraindicated in pregnancy.
  • Most side effects of this class

Medical Pharmacology (26 decks)

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