GI meds Flashcards

1
Q

What are the three cells in the stomach glands?

A

Mucous neck cells
Chief cells
Parietal cells

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2
Q

What do the three main cells secrete in the stomach?

A

Mucous neck cells- Mucin
Chief cells- Pepsinogen and gastric lipase
Parietal cells- HCl

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3
Q

What receptors do parietal cells contain?

A

Gastrin, Histamin, and Ach

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4
Q

Explain the events of acid secretion.

A

Ach/gastrin bind to parietal cells, causing increase in cytosolic Ca, stimulating protein kinases. This stimulates acid secretion from H/K ATPase

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5
Q

What is the function of carbonic anhydrase?

A

Converts H2CO3 into H+ from water

Forms H2O3 from water and CO2

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6
Q

What is one way to treat hyperacidity through inhibition of production? The med that can do this is?

A

Inhibiting formation of HCl through carbonic anhydrase inhibition (So H2CO3 hydrolysis is inhibited)

Acetazolamide

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7
Q

What drugs inhibit secretion of H+ ions into the lumen? How do these inhibit HCl?

A

Antimuscarinic, histamine blockers, and PPI

Inhibit H+ release prevents HCl from being formed

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8
Q

What is the definition of antacids? What is their MOA?

A

Weak bases that react with gastric hydrochloric acid to form salt and water.

Neutralization of acid. Causing reduction of intra gastric acidity

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9
Q

What is the ANC?

A

Acid neutralizing capacity. Number of milliquivalents of 1N HCL that brought to pH to 3.5 by a unit dose of antacid.

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10
Q

What drug category is baking soda and alka seltzer?

A

Antacid-Sodium bicarbonate

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11
Q

What drug category is tums and Os-cal?

A

Antacid- Calcium carbonate

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12
Q

What are the ADE’s for excessive calcium carbonate with Ca containing dairy products?

A

Hypercalcemia, renal insufficiency, and metabolic alkalosis (Milk alkali syndrome)

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13
Q

What is a benefit of the magnesium hydroxide or aluminum hydroxide compared to other antacids?

A

No gas is generated, so no belching

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14
Q

How are magnesium hydroxide or aluminum hydroxide normally administered?

A

Proprietary formulations

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15
Q

How should not take magnesium/aluminum hydroxide?

A

Patients with renal insufficiency because Mag and Al are excreted by kidneys

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16
Q

What are the general ADEs of antacids?

A

Rebound hyperacidity-Transient and mild
Milk-alkali syndrome
Drug specific toxicities

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17
Q

What are the drug specific toxicities for antacids?

A

Mg containing antacids-Laxatives
Al containing antacids-constipation
Al containing antacids-inhibit absorption of some drugs like digoxin and indomethacin

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18
Q

What are the MOAs of cytoprotective/mucosal protective agents

A

DO NOT interfere with HCL, but protect interior of stomach against acidity by establishing a pH gradient within the mucous layer. Also somehow helps repair injured epithelium through restitution

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19
Q

What are some example of cytoprotective agents?

A

Sucralfate, bismuth salts, and prostaglandins

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20
Q

What is sucralfates main use? Why?

A

Prevention of stress related bleeding because there are concerns that antacids, H2 blockers, and PPIs increase risk of nosocomial pneumonia

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21
Q

What is bismith salts used for?

A

Dyspepsia and acute diarrhea

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22
Q

What is the provided prostoglandin prototype?

A

Misoprostol

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23
Q

What are the side effects of bulk forming laxatives?

A

Minimal….

24
Q

What is a beneficial part to bulk forming laxative?

A

May be beneficial to heart

25
Q

What are stool surfactant agent (softeners) examples?

A

Docusate and glycerin suppository

26
Q

What is the MOA of osmotic laxatives?

A

They are soluble but not absorbable compounds, so they increase stool liquidity by allowing more water to be in the GI tract

27
Q

What are examples of osmotic laxatives?

A

Magnesium hydroxide, sorbitol, and lactulose

Polyethelene glycol

28
Q

What does polyethylene glycol contain?

A

Inert, nonabsorbable, osmotically active sugar

29
Q

What is a drug to drug concern with PEG?

A

Tartaric acid, some heart concerns I guess

30
Q

What are the two different stimulant laxatives?

A

Anthraquinone and diphenylmethane derivatives

31
Q

How do stimulant laxatives work?

A

Induce BMs by direct stimulation of enteric nervous system, and colonic electrolyte and fluid secretion

32
Q

What are the chloride channel activators?

A

Lubiprostone, linaclotide

33
Q

What is the MOA of lubiprostone?

A

Stimulates type 2 chloride channel in small intestine

34
Q

What is lubiprostone/linaclotide used for?

A

IBS

Chronic constipation-Only linaclotide

35
Q

What is the MOA of opioid receptor antagonists as a laxative?

A

Inhibit u-opiod receptors… IDK

36
Q

What are the listed opioid receptor antagonists?

A

Alvimopan and naloxigel

37
Q

Do the opioid receptor antagonists cross the BBB?

A

No

38
Q

What are some ADEs of alvimopan?

A

CV toxicity, only for short tem use

39
Q

What is naloxigel contraindicated in?

A

Suspected GI obstruction
Patients on strong CYP 3A4 inhibitors because they may worsen opioid withdrawal
Also patients on CYP3A4 INDUCERS

Strong CYP3A4 inhibitors listed were clarithromycin and ketoconazole, diltiazem, and verapamil

40
Q

What is naloxigels ADEs?

A

May cause opiod withdrawal in fetus

41
Q

Does Loperamide cross the BBB?

A

No

42
Q

What are the opioid antidiarrheal agents?

A

Loperamide and diphenoxylate

43
Q

What are the three drug classes that can inhibit secretion of H+ into the lumen of the stomach?

A

Antimuscarinic, histamine blockers, PPI

44
Q

What are the antimuscarinic drugs mentioned?

A

Atropine, scopolamine

45
Q

What are the ADEs of atropine?

A

Dry mouth, constipation

46
Q

What is a better antimuscarinic drug to use than atropine for acid reduction?

A

M1 selective drugs to avoid atropine like side effects

Atropine is an M2 receptor antagonist

47
Q

What are the H2 blockers? aka histamine blockers

A

Cimetidine, ranitadine, famotadine, nizatadine

48
Q

How do H2 blockers reduce gastric acid secretion?

A

Blocks binding histamine from binding to parietal cell H2 receptor
Direct stimulation of parietal cell by gastrin or Ach and causes the cell to have a DIMINISED EFFECT on acid secretion in presence of H2 receptor blockade

49
Q

What are H2 antagonists specifically effective at inhibiting?

A

Nocturnal acid secretion

50
Q

What are the uses of H2 blockers?

A

GERD, PUD, nonucler dyspepsia, prevention of bleeding from stress related gastritis

51
Q

What are drug interactions with cimetadine?

A

Binds to CYP450

Ranitadine does as well, but to a lesser extent

52
Q

What are the common PPIs?

A

Omeprazole, esomeprazole, lansoprazole, dexlansoprazole, rabeprazole, pantoprazolw

53
Q

What is PPIs MOA?

A

Gets into the parietal cells, accumulates in parietal cells, covalently bind H/K ATPase

This is IRREVERSIBLE

Inhibits this proton pump… which is a H pump

54
Q

PPI are administered as a ____

A

Prodrug

55
Q

What is the treatment for Zollinger Ellison syndrome?

A

PPIs

56
Q

What are the ADEs of PPIs?

A

Omeprazole and esomeprazole inhibit CYP2C19

This CYP also is used for plavix

Subnormal B12 levels