pharmacology Acid suppression therapy H2 blockers Proton pump inhibitors Bismuth, sucralfate Misoprostol Octreotide Antacid use Osmotic laxatives Sulfasalazine Ondansetron Metoclopramide Orlistat Flashcards

1
Q

Proton pump inhibitors work on pumps that exchange which two ions?

A

Hydrogen and potassium

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2
Q

H2 blockers work on which stomach cell type?

A

Parietal cells

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3
Q

Muscarinic antagonists work on which two cell types in the stomach?

A

Enterochromaffin-like cells (with M1 receptors) and parietal cells (with M3 receptors)

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4
Q

Why are misoprostol, sucralfate, and bismuth useful in treating gastric ulcers?

A

These drugs have a protective effect on the mucosa underlying the ulcers

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5
Q

Where does somatostatin act?

A

Somatostatin acts on enterochromaffin-like cells via ST2 receptors

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6
Q

A surgeon damages the vagus nerve while operating. What type of GI therapy would be directly impacted?

A

Muscarinic antagonists, because the vagus nerve stimulates the M1 and M3 receptors

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7
Q

A man has been taking an antacid for GERD pain. What is the mechanism for this drug and where does it target?

A

Antacids work in the stomach lumen and block the secretion of acid, or H+

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8
Q

What type of cell in the antrum is stimulated by food? What hormone is stimulated by food to promote gastric acid secretion?

A

G cell; gastrin

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9
Q

If a patient is deficient in gastrin, which cells and receptors will be understimulated in the fundus?

A

Parietal cells and ECLs (both have G [CCK-B] receptors that are stimulated by gastrin)

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10
Q

A patient has a gastric ulcer causing severe pain. Name at least two medications can be given to help with ulcer healing?

A

Misoprostol, sucralfate, bismuth

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11
Q

You study stomach gastrin activity. You administer food to rats and take several biopsies. Which stomach area will show the most activity?

A

The antrum

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12
Q

Most gastric acid secretion (and the actions of medications that inhibit it) can be found in which area of the stomach?

A

The fundus

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13
Q

Give at least two examples of H2 blockers.

A

Cimetidine, ranitidine, famotidine, nizatidine (take H2 blockers before you dine, & table for 2 to remember H2)

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14
Q

What substance is the endogenous agonist of the H2 receptor?

A

Histamine

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15
Q

What is the effect of H2 blockers on parietal cells?

A

Reversible decrease of hydrogen ion secretion

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16
Q

Name at least two clinical uses of H2 blockers.

A

Peptic ulcers, gastritis, mild esophageal reflux

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17
Q

A patient takes over 10 medications for various reasons. You are worried about drug interactions. Which H2 blocker should you avoid?

A

Cimetidine, as it causes inhibition of cytochrome P-450 and may alter the metabolism of other drugs

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18
Q

Which two H2 blockers can decrease the renal excretion of creatinine?

A

Ranitidine and cimetidine

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19
Q

A 50-y/o man starts a gastritis medication that inhibits cytochrome P-450. What adverse effects for this drug are seen specifically in men?

A

Prolactin release, gynecomastia, impotence, decreased libido (cimetidine is a P-450 inhibitor and has antiandrogenic effects)

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20
Q

A 47-year-old woman has developed confusion, dizziness, and headaches since starting an H2 blocker. What is happening?

A

Cimetidine (able to cross the blood-brain barrier, unlike other H2 blockers) can cause confusion, dizziness, and headaches

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21
Q

A woman on a specific H2 blocker tells her doctor that she wants to get pregnant. The doctor says she needs to stop the H2 blocker. Why?

A

Cimetidine, the H2 blocker she is likely taking, is dangerous to the fetus, because it can cross the placenta

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22
Q

A woman has unexpected galactorrhea. Her medications include sertraline, pantoprazole, cimetidine, aspirin, simvastatin. Is a drug to blame?

A

Yes, as cimetidine can increase prolactin levels, which may cause galactorrhea

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23
Q

A 34-y/o woman has continued GERD pain despite ranitidine & is negative for Helicobacter pylori antigens. Specific drugs to try next?

A

Omeprazole, esomeprazole, pantoprazole, lansoprazole, dexlansoprazole (proton pump inhibitors)

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24
Q

Proton pump inhibitors work by irreversibly inhibiting this protein in stomach parietal cells.

A

H+/K+ ATPase

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25
Name at least two conditions that are treated with proton pump inhibitors.
Peptic ulcers, gastritis, esophageal reflux, Zollinger-Ellison syndrome
26
A patient has been using proton pump inhibitors for a long time. His level of which divalent electrolyte is likely decreased?
Magnesium
27
Before starting a man on an H+/K+ ATPase inhibitor, you explain to him that there are some associated risks. What are some of these?
C. difficile infection, pneumonia, hip fractures, hypomagnesemia (with long-term use) (these are proton pump inhibitor side effects)
28
A man presents with traveler's diarrhea. What two drugs might you choose to help reestablish the pH gradient in the mucous layer?
Bismuth and sucralfate
29
Misoprostol is a ____ analog.
Prostaglandin E1
30
Misoprostol increases the production and secretion of the ____ barrier and decreases the production of ____.
Gastric mucous; acid
31
A patient with rheumatoid arthritis starts misoprostol after being intolerant to her prior treatment. What was the complication?
Peptic ulcers induced by NSAIDs (misoprostol increases gastric mucous production and decreases acid production)
32
A neonate is noted to be cyanotic on the third day of life. What medication should be ordered immediately?
Misoprostol, which maintains a patent ductus arteriosus, allowing pulmonary and systemic circulations to mix in cases of heart disease
33
A woman is given misoprostol at 42 weeks' gestation. Why?
To induce labor
34
Within what population is misoprostol contraindicated?
Women of childbearing potential (it is an abortifacient)
35
A 22-year-old woman requests a chemical abortion of her pregnancy. She receives a PGE1 analog. What side effect should she expect?
Diarrhea (she has likely been given misoprostol for her chemical abortion)
36
A patient presents with bleeding esophageal varices. What is the mechanism of action of a drug that can acutely help abort the bleeding?
Octreotide is a long-acting somatostatin analog that inhibits actions of many splanchnic vasodilatory hormones
37
A patient on pharmacologic treatment for a VIPoma experiences nausea, cramps, and steatorrhea. What medication is she likely taking?
Octreotide
38
• A man with recent onset of excessive growth hormone secretion and a woman with a carcinoid tumor both could both benefit from what drug
Octreotide
39
A 54-y/o woman being managed for CHF and hypothyroidism has started taking daily antacids. How might this affect her other medications?
Interference with absorption, bioavailability, and urinary excretion by altering gastric and urinary pH and delaying gastric emptying
40
Name at least two compounds commonly used as antacids.
Aluminum hydroxide, calcium carbonate, magnesium hydroxide
41
Diarrhea, hyporeflexia, hypotension, cardiac arrest, and hypokalemia are side effects of which antacid?
Magnesium hydroxide (Mg = must go to the bathroom)
42
A young patient is overusing antacid calcium carbonate. What toxicities does this cause?
Hypercalcemia, rebound acid increase
43
All antacids cause what electrolyte abnormality if overused?
Hypokalemia
44
A patient who heavily self-medicates her GERD complains of dizziness and diarrhea. Which antacid is she likely overusing?
Magnesium hydroxide (can cause diarrhea and hypotension)
45
A patient has hypophosphatemia and osteodystrophy. What medication is he likely chronically overusing to treat his GERD?
Aluminum hydroxide
46
A patient with GERD needs to start tetracycline for an infection. Why is it important for you to check the medication list before starting?
Calcium carbonate antacids can chelate and reduce the effectiveness of certain other oral medications, such as tetracycline
47
A patient suffering from both constipation and hepatic encephalopathy should be given which medication?
Lactulose, since this addresses both problems
48
A patient with a history of bulimia is found to be dehydrated. Abuse of what GI medication could contribute to this finding?
Osmotic laxatives
49
How does lactulose treat hepatic encephalopathy?
The gut flora degrades lactulose into lactic and acetic acid, promoting nitrogen excretion as NH4+ and reducing NH3 levels
50
For a 24-year-old man with ulcerative colitis, you prescribe a medication that is a combination of two drugs. What are these?
Sulfapyridine and 5-aminosalicylic acid (the medicine is sulfasalazine)
51
What is the function of sulfapyridine?
It is an antibiotic
52
What activates sulfasalazine in the gut? Be specific
Colonic bacteria activate sulfasalazine
53
A patient is on sulfasalazine. What two diseases is the drug typically used to treat?
Crohn disease (for the colitis component) and ulcerative colitis
54
A 30-year-old man starts on a drug composed of sulfapyridine and 5-aminosalicylic acid for Crohn disease. Side effects to be monitored for?
Reversible oligospermia, malaise, nausea, sulfonamide toxicity (this is sulfasalazine)
55
A patient is found to have Crohn ileitis and asks if he can be started on sulfasalazine. What is the appropriate response?
Sulfasalazine would be ineffective, because it is activated by colonic bacteria and thus has no effect proximal to the colon
56
What component of the sulfasalazine is known to be anti-inflammatory?
5-aminosalicylic acid
57
Ondansetron is an antagonist of what receptor type?
5-hydroxytryptamine3
58
Ondansetron is used to control vomiting primarily in which two settings?
After surgery and in conjunction with cancer chemotherapy (if you are feeling queasy at a party, keep on dancing with ondansetron)
59
You give a 47-year-old woman a 5-HT3 antagonist for her nausea while she gets chemotherapy. What two main toxicities should you look for?
Headache and constipation (this is ondansetron)
60
What is the mechanism of action for ondansetron?
It binds 5-HT3 receptors and antagonizes them, decreasing vagal stimulation
61
What is the mechanism of action of metoclopramide?
It is a dopamine receptor antagonist (specifically the D2 receptor)
62
A man with HF and diabetes is receiving a D2 receptor antagonist for gastroparesis. What two types of drugs may cause interactions?
Digoxin and diabetic agents (this is metoclopramide)
63
Metoclopramide is contraindicated in patients with what serious gastrointestinal disorder?
Small bowel obstruction; it is prokinetic and thus will worsen the discomfort of these patients
64
On what parts of the gastrointestinal tract does metoclopramide act?
Lower esophageal sphincter (increases tone and contractility), stomach, small bowel (increases motility) (no effect on colon)
65
Give at least two clinical uses of metoclopramide.
Diabetic gastroparesis, postsurgical gastroparesis, antiemesis
66
A Parkinson disease patient with profuse vomiting asks for metoclopramide. Why does the doctor disagree with this choice?
Metoclopramide, a D2 receptor antagonist, can cross-react with and block D1 receptors, exacerbating parkinsonian symptoms
67
A diabetic man is given a drug that causes restlessness, drowsiness, and nausea. Does this drug impact colon transit time?
No, as this is metoclopramide
68
A 74-y/o woman has hypovolemia due to gastroenteritis. As the resident, would you start with ondansetron or metoclopramide for her nausea?
Ondansetron (metoclopramide is useful in GI-based nausea but has a greater risk of adverse effects in the elderly)
69
A man wants a refill of a drug medication a previous doctor prescribed for weight loss. He says it gives him greasy stools. What drug is it?
Orlistat (inhibits gastric and pancreatic lipase)
70
A patient asks about a weight loss drug she saw on TV, with greasy stools and vitamin deficiencies as side effects. How does the drug work?
It inhibits gastric and pancreatic lipase (this is orlistat)