Gastointestinal Pharmacology Flashcards

1
Q

What is the pathogenesis of gastroduodenal ulcers?

A

Excess gastric acid secretion, breakdown of mucosal cytoprotection, Helicobacter pylori infection

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are the goals of ulcer treatment?

A

reduce ulcerogenic factors, enhance defensive factors, or eradicate any infectious causes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What are pro-ulcerogenic factors?

A

Acids (HCl, VFA, bile acids), pepsin, infections

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are antiulcerogenic factors?

A

mucosal cytoprotection, epithelial renewal, external protection

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

How does one increase the gastric pH to greater than 4 to promote healing?

A

H2-Histamine receptor blockade, stimulation of gastric PGE receptors, gastric H+-K+-ATPase inhibition (proton pump inhibitors)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Famotidine

A

H2-Histamine antagonist, decreases acid secretion which decreases pepsin. As treatment continues effectiveness decreases due to an increased secretion of gastrin. Low oral biovalibility and renal clearance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are examples of H2-histamine antagonists?

A

famotidine, ranitidine, cimetidine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What are the side effects and indications of H2-histamine antagonist?

A

Renal disease patients need lower dose, treatment of ulcers due to gastritis, stress, NSAID terapies, gastrinomas

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Misoprostil

A

PGE analogue, po administration, needs frequent administration due to rapid hepatic metabolism. Decreases acid secretion stimulated by histamine or gastrin. Less effective than H2-HR antagonists or PPI, increases gastric cytoprotection

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

How do PGE and PGI promote cytoprotection?

A

Mucus production (coats surface of the gastric mucosa), bicarb production (neutralizes HCl), intrinsic mucosal barrier (resist back-diffusion of acid), and gastric blood flow (flushes away acid, prevents buildup, maintains tissue pH in normal range)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Indications/side effects/contraindications of misoprostil?

A

NSAIDs-induced ulcers, increased mast cell influx. Side effects include diarrhea due to prokinetic action. Contraindications include IBD, pregnancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is an example of a proton pump inhibitor?

A

Omeprazole

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is the action of proton pump inhibitors?

A

Irreversibly inactivate H+/K+ ATPase, so effects extend longer than the drug’s presence in the body. Reduce acid secretions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Omeprazole

A

Proton pump inhibitor. Oral paste that is a weak base that decreases the release of HCl

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Sucralfate

A

Binds to ulcerated tissue to form a seal after oral administration, heals existing ulcers not prevent new ones. Short duration of action. Binds and inactivates bile acids, increases local prostanoid formation.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Antacids

A

Either systemic or non-systemic, non-systemic only affects stomach. Maalox and Mylanta examples. Relieve clinical signs, no healing.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Na or Ca carbonate antacids onset

A

rapid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Mg salts (sulfate, hydroxide) onset

A

intermediate with laxative effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

all hydroxide antacids onset

A

slow

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What is the best type of drug to use to treat an ulcer: PPIs, H2-histamine antagonists, or cytoprotectants?

A

PPIs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What are examples of locally-acting emetic agents?

A

warm water, sodium chloride, 3% hydrogen peroxide, syrup of ipecac (emetine akaloid substance)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Apomorphine

A

centrally acts on D2 dopamine receptors, produces vomiting in 2-10 minutes

23
Q

Xylazine

A

simulates alpha2-adrenergic receptors to produce emesis in cats

24
Q

Indications of anti-emetic drugs

A

motion sickness, uremia, liver disease, cancer chemo, parvo, trauma

25
Q

Famotidine

A

H2-histamine antagonist that lessens irritating effects of acid on the stomach

26
Q

muscarinic acetylcholine antagonist anti-emetic effects

A

decrease vagal afferent transmission to vomiting center to decrease vomiting

27
Q

kaolin-pectin and other coating agents anti-emetic efficacy

A

not very effective

28
Q

Metoclopramide

A

Simulate gastric motility, block CNS dopamine receptors and 5-HT3 receptors

29
Q

Action of diphenhydramine, meclizine

A

may reduce motion sickness by blocking histamine and muscarinic cholinergic receptors

30
Q

Ondanestron

A

blocks type three serotonin receptors on gastric vagal fibers and are effective at inhibiting emesis in dogs associated with chemo or parvo

31
Q

Maropitant

A

Blocks type 1 neurokinin (substance P) receptors present in vomiting center, broad spectrum anti-emetic

32
Q

What effect do mAChR antagonists have on the GI tract?

A

increased peristalsis

33
Q

What affect do opiods have on the GI tract?

A

increased segmentation

34
Q

What affect do opiod antagonists or mAChR antagonists have on the GI tract?

A

inhibit increased segmentation

35
Q

Bethanechol

A

mAChR agonist that is a cholinomimetric that increases GI motility

36
Q

Neostigmine

A

anticholinesterase drug that increases GI motility

37
Q

Ranitidine and Nizatidine

A

weak cholinesterase inhibitors that can increase upper GI motility

38
Q

Metoclopramide

A

Acts on upper GI tract to increase smooth muscle contractions, blocks D2 dopamine receptors and is an agonist at the 5-HT4 serotonin receptors

39
Q

Cisapride

A

Partial agonist at 5-HT4 receptors, increase acetylcholine release from enteric neurons to stimulate motility, indicated by chronic constipation, ileus in dogs

40
Q

Erythromycin

A

agonist at receptors in smooth muscle and gastroenteric nerves for motilin, stimulates motility of stomach and upper SI (not colon). Metabolized by CYP450 and eliminated in bile

41
Q

Lidocaine

A

Blocks voltage-gated Na+ channels in enteric nerves, stimulates intestinal motility although mechanism unclear

42
Q

What are contraindications of prokinetic drugs?

A

GI tract obstructions and post-surgical anastomoses

43
Q

What are the major types of laxatives and cathartics?

A

Osmotic, bulk, lubricants/surfactants, and irritants

44
Q

What are examples of osmotic laxatives?

A

Mannitol, sorbitol (draws water into intestinal tract)

45
Q

What is an example of a irritant laxative?

A

Bisacodyl- stimulates enteric sensory nerves to increase intestinal motility and decrease water absorption

46
Q

What is an example of a bulk laxative drug?

A

Canned pumpkin- increase mass of non-digestible matter

47
Q

What is an example of a lubricant/surfactant laxative drug?

A

Mineral oil, docusate sodium- coat fecal surface with hydrophobic film

48
Q

Bismuth subsalicylate

A

breaks down to salicylic acid (NSAID) and bismuth oxychloride (bacteriocide?), bismuth salts absorb enterotoxins

49
Q

Kaolin-Pectin

A

Aluminum silicate, changes fecal consistency (maybe??) but clinical efficacy questionable

50
Q

Propantheline, Isopropramide, N-butylscopolammonium bromine

A

Types of quarternary ammonium anticholinergic drugs (act through intestinal mAChR) that do not enter CNS and inhibit intestinal motility and secretion as antidiarrheal drugs

51
Q

Naloxone

A

antagonize opiod actions in GI tract (opiods inhibit GI propulsion)

52
Q

What are examples of opiate antidiarrheal drugs?

A

Loperamide (no abuse) and codine (acts at perif and CNS cites too)

53
Q

What are examples of opiod antagonists that are peripherally-specific?

A

Alvimopan and methynaltrexone