GI Drugs Flashcards

1
Q

Acute Gastroesophageal reflux causes…

A

heartburn

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2
Q

Chronic Gastroesophageal reflux causes

A

GERD

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3
Q

What happens when the diaphragm is displaced by peptic acid diseases?

A

Hiatal hernia (lowering of the diaphragm)

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4
Q

Three factors that protect from peptic acid

A

mucus, bicarb, pgE

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5
Q

H2 receptor antagonist

A

Ranitidine, Famotidine

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6
Q

H2 receptor antagonist function

A

directly block histamine stimulated gastric acid secretion

blocks 90% of nocturnal gastric acid secretion so better at NIGHT (over PPI)

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7
Q

Reduce dose of ranitidine/famotidine in what type of patients

A

Those with renal dysfunction (even though toxicity is low)

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8
Q

Coadmin of what drug markedly reduces ulcers caused by long-term NSAID use?

A

Famotidine

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9
Q

What is ranitidine/famotidine indicated for

A

Gastric and duodenal ulcers
GERD
Prophylactically after acute event to precent recurrence

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10
Q

Proton Pump Inhibitors

A

Omeprazole

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11
Q

Mech of PPIs

A

Administered as Prodrug
Irreversible inhibition of parietal cell proton pump (H/K ATPase)
The weak base accumulates in canaliculus of acidic parietal cells, becomes protonated and binds covalently to PP enzyme (PPIs are acid labile, so need enteric coating to get past stomach)
Result is that they have no effect unless stomach is secreting acid actively.

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12
Q

If the PPI irreversible inhibits proton pumps, how does the body recover proton pump activity?

A

Has to synthesize new enzymes

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13
Q

Indication for PPI

A

DAYtime (over H2)
Zollinger-Ellison syndrome, ulcers and GERD
(poor choice for occasional heartburn)

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14
Q

PPI AE

A

Pneumonia (50% increase)
nausea, diarrhea, dizziness
Generally well tolerated

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15
Q

Antacids

A

Mg(OH)2, Al(OH)3, CaCO3

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16
Q

Mg(OH)2 causes ______ while Al(OH)3 and CaCO3 cause ______

A

Mg(OH)2 - diarrhea

Al(OH)3, CaCO3 - constipation

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17
Q

Antacids mech

A

Weak bases that are poorly absorbed and directly neutralizes stomach acid
Can increase or decrease the absorption of many drug classes (Increase in urinary pH alters elimination of acidic (inc.) and basic drugs (dec.))

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18
Q

Antacids Indication

A

Occasional heartburn

19
Q

H. Pylori treatment

A

PPI + several antibiotics (clarithromycin with amoxicillin or metronidazole)

20
Q

Mucosal protective agents

A

Sucralfate and Bismuth subsalicylate

21
Q

Sucralfate mech

A

Forms paste-like gel at LOW pH that adheres to positively charged proteins of epithelial cells and ulcer craters
Coating action protects against acid

22
Q

Sucralfate AE

A

Can adsorb other drugs (so wait 2 hours after admin)

Do not co-admin with antacids (won’t form the gel, no positive charged proteins)

23
Q

Bismuth subsalicylate mech

A

Binds selectively to ulcers to protect against acid and pepsin but it blackens stool and tongue (active ingredient in pep to-bismol)

24
Q

Anti-emetic

A

Metoclopramide, ondansetron

25
Q

Metoclopramide mech of action

A

Agonist at 5-HT4 receptor and antagonist at 5-HT3 and D2 receptors (vagal/CNS); enhances Ach release in myenteric plexus, improves intestinal smooth muscle response to Ach

26
Q

Metoclopramide Indication

A

Increases esophageal clearance, improved tone LES, increase in intestinal motility, anti-emetic
Used for chemo-induced nausea and vomiting

27
Q

Metoclopramide AE

A

D2 antagonist: parkinson-like symptoms and irreversible muscle spasms (dyskinesia)

28
Q

Ondansetron

A

Selective (different from metoclopramide) 5-HT3 antagonist; given IV/orally prior to chemo or surgery and has no effects on muscarinic/dopaminergic receptors

29
Q

Contsipation occurs because of…

A

Reduced colonic motility and/or increased hardness of intestinal contents

30
Q

Lubiprostone

A

Stimulant laxative, increases intestinal fluid secretion by activating Cl channels = increased # of bowel movements
Approved for chronic use

31
Q

Mg(OH)2

A

Saline Laxatine AND antacid
Administered as a hypotonic sln, osmotic pressure leads to accumulation of fluids in GI tract and stimulation of peristalsis
Cathartic dose leads to complete evacuation in less than 3 hours (for colonoscopy prep)

32
Q

Loperamide

A

Anti-diarrhea, opioid, slows intestinal transit time due to stimulation of mu opioid receptors in intestinal smooth muscle

33
Q

Loperamide AE

A

Constipation, toxic megacolon, avoid in patients with ulcerative colitis or acute bacillary/amoebic dysentery
(CNS toxicity less of a problem)

34
Q

Drugs for IBS with constipation

A

Mg(OH)2 (1st option) and tegaserod (restricted use only)

35
Q

Drugs for IBS with diarrhea

A

Loperamide (1st option), anticholinergics (2nd option) and Alosetron (last resort)

36
Q

Alosteron

A

Last-resort for IBS-D, 5-HT3 antagonist = decrease in colonic motility via enteric and CNS blockade of 5-HT3 receptors
Only for women with IBS-D

37
Q

Alosteron AE

A

Constipation, ischemic colitis (rare but can be fatal)

38
Q

Prednisone

A

For IBD treatment; decreases inflammatory response to rapidly reduce ulceration and cause initial remission (not long term)

39
Q

Azathioprine

A

For IBD treatment long-term use (2nd line), works as an immunosuppressive but can also suppress bone marrow (Other AE includes rashes, fever and nausea). Purine analogue.
Need to do genetic testing prior because is is metabolized by TPMT

40
Q

Sulfasalazine

A

For first-line tx for ulcerative colitis; interferes with intermediates in inflammatory pathway
Topical over systemic (5-ASA onto intestinal wall= needs to be released at site of lesion)
Pro-drug that is converted by bacteria
Most effective at delivering 5-ASA to small or large intestine

41
Q

Sulfasalazine AE

A

Adverse: 40% of patients can’t tolerate

Nausea, headaches, hypersensitivity, bone marrow suppression

42
Q

Infliximab

A

Approved for ulcerative colitis and Crohn’s disease
Antibody to TNF-alpha; blocks inflammatory effects
Adverse: increased infections

43
Q

Describe the treatment approach to IBD, including management of acute, mild, moderate, and severe disease.

A

Acute episode: control with oral or IV prednisone
Mild/1st line: Sulfasalazine (topical 5-ASA)
Moderate/2nd line: Azathioprine (purine analogue)
Severe/Refractory: Inflixamab (TNF antagonist)