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NURS8024 Pharm Exam 1: Latest 2024 Update with complete correct Solutions ALL 66 Pages COVERED!!
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NURS8024 Pharm Exam 1: Latest 2024 Update with complete correct Solutions ALL 66 Pages COVERED!!
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NURS8024 Pharm Exam 1: Latest 2024 Updatewith complete correct Solutions
B
Gastric acid secretion by parietal cells of the gastric mucosa are stimulated by - ANSWER
*acetycholine, histamine, gastrin
LU
Receptor-mediated binding of acetylcholine, histamine, or gastrin results in - ANSWER *the
activation of protein kinases, which in
turn stimulates the H+/K+-adenosine triphosphatase (ATPase) proton pump
YC
Gastrin and acetylcholine stimulate release of - ANSWER
receptor binding of prostaglandin E2 and
somatostatin diminish - ANSWER gastric acid production
histamine
D
Antacids - ANSWER weak bases that react with gastric acid to
TU
form water and a salt → diminishing gastric acidity
Reduce pepsin activity - pepsin inactive at a pH >4
Wide variety* in chemical composition, acid-neutralizing capacity, sodium content, palatability,
ES
and price
Acid neutralizing ability* of an antacid depends on its capacity to neutralize gastric HCl and on
whether the stomach is full or empty
C
• food delays stomach emptying, allowing more time for the antacid to react
A
Therapeutic uses of antacids - ANSWER • Symptomatic relief of peptic ulcer disease (PUD)
and gastroesophageal reflux (GERD)
• May promote healing of duodenal ulcers, but not
robust evidence for efficacy in Tx of acute gastric
ulcers
• Calcium carbonate preparations
• also used as calcium supplements for the treatment of osteoporosis
,Commonly used antacid drugs - ANSWER Classes
• Calcium salts: calcium carbonate: Tums/Rolaids
• Sodium bicarbonate: Alka-Seltzer
• Aluminum salts - Aluminum hydroxide: Amphojel; Aluminum carbonate: Basaljel
• Magnesium salts/ magnesium oxide: Milk of Magnesia
• Combination products
• Aluminum hydroxide and magnesium hydroxide (Maalox, Mylanta)
• Alginic acid, magnesium trisilicate, calcium stearate
(Gaviscon)
B
Adverse effects of antacids - ANSWER • Aluminum hydroxide tends to be constipating
LU
• Magnesium hydroxide tends to cause diarrhea
• Binding of phosphate by aluminum-containing antacids → hypophosphatemia
• Sodium bicarbonate → belching and flatulence, potential for systemic alkalosis
• Sodium content of antacids → can be important in pts w/ HTN or CHF
• Excessive intake of calcium carbonate along w/ calcium foods → hypercalcemia
YC
Mucosal Protective Agents - ANSWER
Sucralfate
Bismuth Compounds
Cytoprotective compounds
D
Cytoprotective Compounds - ANSWER enhance mucosal protection
TU
mechanisms → preventing mucosal injury, ↓ inflammation, promotes healing of existing ulcers
Sucralfate - ANSWER complex of aluminum hydroxide and sulfated sucrose
• Small, poorly soluble molecule
ES
• Polymerizes in stomach acid → binds to injured tissue, forms physical barrier coating over
ulcer bed- impairs diffusion of HCl and prevents degradation of mucus by pepsin and acid
• Accelerates healing of peptic ulcers and ↓ recurrence rate
• Stimulates prostaglandin release, mucus and bicarbonate output
C
• *BIG drawback.... Must be taken qid• used in long-term maintenance therapy to prevent
recurrence
• Requires an acidic pH for activation -should not be administered with H2 antagonists or
A
antacids
• Little of the drug is absorbed systemically, very well tolerated
• Can interfere w/ absorption of other drugs by binding to them
• Does not prevent NSAID-induced ulcers
Bismuth Compounds - ANSWER • Coats ulcers → protective layer against acid and pepsin
• May stimulate prostaglandin, mucus, and bicarbonate secretion
,• Antimicrobial effect- binds enterotoxins
• reduces stool frequency & liquidity in acute infectious diarrhea
• Causes black stools- harmless
• Avoid in renal insufficiency
In geriatric patients avoid use of - ANSWER - antacids that contain magnesium in patients
with renal failure
- sodium-containing antacids because of fluid
retention
B
Antacids in Pediatrics - ANSWER Safety not established in children
LU
Antacids during pregnancy and lactation - ANSWER No FDA category established, although
antacids
generally are considered safe for use in pregnancy
YC
Antisecretory agents - ANSWER
Proton pump inhibitors
Histamine-2 receptor antagonists
Examples of Histamine-2 receptor antagonists - ANSWER ranitidine, *cimetidine,
D
famotidine, nizatidine
TU
Examples of Proton pump inhibitors - ANSWER • omeprazole, esomeprazole
• Lansoprazole, pantoprazole
• rabeprazole
ES
H2 Receptor antagonists - ANSWER • MOA
• Acts selectively on H2 receptors in the stomach, blood vessels, and other sites (no effect on H1
receptors)
• Competitively blocks binding of histamine to H2 receptors
C
• less effective than PPIs against stimulated secretion
• Four drugs: cimetidine*. ranitidine, famotidine, and nizatidine
• Can inhibit > 90% basal, food-stimulated and nocturnal secretion of gastric acid after a single
A
dose
• Main clinical use is to inhibit gastric acid secretion
• particularly effective against nocturnal acid secretion
H2 Receptor antagonist ADEs - ANSWER • H2 antagonists very safe
• ADE < 3% of patients - diarrhea, h/a, fatigue, myalgias, constipation
, • Drugs such as ketoconazole, which depend on an acidic medium for gastric absorption, may not
be efficiently absorbed if taken w/ H2 blocker
• Not used for NSAID-induced ulcers
• Better healing and prevention with PPIs
Cimetidine - ANSWER • Inhibits cytochrome P450 and can slow metabolism -potentiating
the action of other drugs
• warfarin, diazepam, phenytoin, quinidine,
carbamazepine, theophylline, and imipramine
B
• Cimetidine can have endocrine effects, acts as a
nonsteroidal antiandrogen. (effects include gynecomastia, galactorrhea, and reduced sperm
LU
count)
Proton pump inhibitors inhibit - ANSWER H+/K+ ATPase proton pump
Omeprazole - ANSWER PPI, the first of a class of drugs that bind to the H+/K+- ATPase
YC
enzyme system (proton pump) of the parietal cell
• Suppresses secretion of hydrogen ions into the gastric lumen (membrane-bound proton pump is
the final step in the secretion of gastric acid)
D
lansoprazole, rabeprazole, pantoprazole,
esomeprazole, dexlansoprazole - ANSWER PPIs
TU
• Agents are pro-drugs w/ acid-resistant enteric coating to protect them from premature
degradation by gastric acid
Absorption/Action of PPIs - ANSWER *Coating is removed* in the alkaline duodenum, and
ES
the prodrug, a weak base, is absorbed and transported to the parietal cell canaliculus →
Converted to the active form
All PPIs inhibit both basal and stimulated gastric acid secretion by > 90%
C
• Onset of gastric acid suppression w/i 1 to 2 hrs post first dose of lansoprazole and slightly
earlier with omeprazole
A
Metabolism/Actions of PPIs - ANSWER
Therapeutic uses of PPIs - ANSWER • Superiority of PPIs over H2 antagonists for gastric
acid suppression and healing peptic ulcers - preferred therapy
• Preferred drugs for treating erosive esophagitis, active duodenal ulcer, long-term tx of
pathologic hypersecretory conditions
• Approved for the treatment of GERD.
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