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Pharmacology > Upper GI Drugs > Flashcards

Upper GI Drugs Flashcards

1
Q

Peptic Ulcer Disease (PUD) is ____ erosions d/t corroding factors overwhelming protective factors

A

Peptic Ulcer Disease (PUD) is mucosal erosions d/t corroding factors overwhelming protective factors

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2
Q

Gastric ulcers from NSAID use and epigastric pain is _____ by eating

whereas

Duodenal ulcers from H. pylori infection, epigastric pain ____ by eating

A

Gastric ulcers from NSAID use and epigastric pain is worsened by eating

whereas

Duodenal ulcers from H. pylori infection, epigastric pain relieved by eating

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3
Q

Describe the image

A

2 physiological states of gastric acid production: Basal & Meal stimulated

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4
Q

Antacids are weak ____ obtained without prescription → causes ____ of low gastric pH → protects esophageal mucosa from ____

A

Antacids are weak bases obtained without prescription → causes neutralization of low gastric pH → protects esophageal mucosa from reflux corrosion

Antacid + HCl → salt + H2O

Time of onset: 5 minutes
Duration of action: 30 mins – 1 hour

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5
Q

Antacids can affect other drugs by ____ gastric and urinary pH or by _____ gastric emptying.

All can cause ____.

A

Antacids can affect other drugs by increasing gastric and urinary pH or by delaying gastric emptying.

All can cause hypokalemia.

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6
Q

(Antacids)

Aluminum Hydroxide causes ____

Magnesium Hydroxide causes ____

therefore, combined to produce _____

A

(Antacids)

Aluminum Hydroxide causes constipation
“Aluminimum amount of feces”

Magnesium Hydroxide causes osmotic diarrhea
“Must _g_o 2 the washroom (Mg2+)”

Al and Mg combined to produce no change in bowel movements

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7
Q

Calcium Carbonate is an ____, CO2 causes _____, can lead to metabolic _____, aka ____ syndrome.

A

Calcium Carbonate is an antacid, CO2 causes belching, can lead to metabolic alkalosis, aka milk alkali syndrome.

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8
Q

describe antacid drug interactions

A
  • Binding/chelation of many drugs
  • Increased gastric pH alters dissolution of weakly charged drugs
  • Decreased absorption of co-administered:
    • Tetracyclines, Fluoroquinolones, Itraconazole, Iron
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9
Q

H2 receptor antagonists suppress ___-induced gastric acid secretion, and reduce signal transduction for ____ and ____-induced gastric acid production

A

H2 receptor antagonists suppress histamine-induced gastric acid secretion, and reduce signal transduction for ACh and Gastrin-induced gastric acid production

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10
Q

H2 receptor antagonists are selective _____ inhibitors at the ____ cell H2 Gs protein coupled receptor

Time of onset: 2.5 hours
Duration of action: 4- 10 hours
_____ develops in 2- 6 weeks

A

H2 receptor antagonists are selective competitive inhibitors at the parietal cell H2 Gs protein coupled receptor

Time of onset: 2.5 hours
Duration of action: 4- 10 hours
Tachyphylaxis develops in 2- 6 weeks

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11
Q

list the H2 Receptor Antagonists

A
  • Cimetidine – prototype with many adverse effects
  • Ranitidine, Famotidine, Nizatidine – 2nd generation with no anti-androgenic or CNS adverse effects
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12
Q

describe the effect of H2RAs on Gastric Acid Secretion

A

H2RAs strongly suppress basal gastric acid secretion

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13
Q

list the H2 receptor antagonist indications

A
  • GERD
  • PUD
  • Nonulcer dyspepsia
  • Prophylaxis against stress-related gastritis
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14
Q

what is the only H2 receptor antagonist with adverse effects

A

CIMETIDINE

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15
Q

AEs of Cimitidine

A
  • acts as nonsteroidal anti-androgen and prolactin stimulant → gynecomastia, galactorrhea, and male impotence
  • Crosses BBB → confusion, dizziness and headaches
  • Increases gastric pH → B12 deficiency and myelosuppression (long term use)
  • Potent CYP450 inhibitor increasing serum [] of:
    • Warfarin, Diazepam, Phenytoin
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16
Q

______ are the most potent inhibitors of gastric acid secretion → inhibit 90–98% of 24-hour acid secretion

A

Proton pump inhibitors are the most potent inhibitors of gastric acid secretion → inhibit 90–98% of 24-hour acid secretion

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17
Q

PPIs ____ bind and inhibit the ____ ATPase pump of gastric ____ cells

suppressing the final ____ pathway of gastric acid secretion

A

PPIs irreversibily bind and inhibit the H+-K+ ATPase pump of gastric parietal cells

suppressing the final common pathway of gastric acid secretion

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18
Q

describe the image

A

PPIs strongly suppress basal & meal stimulated gastric acid production

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19
Q

list PPIs

A
  • Omeprazole
  • Esomeprazole
  • Lansoprazole
  • Rabeprazole
  • Pantoprazole
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20
Q

list the indications for PPIs

A
  • Patients who fail twice-daily H2RA therapy
  • Severe symptoms of GERD that impair quality of life
  • PUD
    • H. pylori eradication
    • NSAID associated ulcers
    • Prevention of peptic ulcer rebleeding
  • Gastrinoma
  • Nonulcer dyspepsia
  • Prophylaxis against stress-related gastritis
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21
Q

PPI adverse effects

A
  • Vitamin B12 deficiency – d/t reduced pepsin function
  • Increased risk of CAP and C. difficile colitis
  • Hypomagnesemia
  • Osteopenia – possibly via reduced Ca2+ absorption or osteoclast inhibition
    • FDA-mandated warning of possible increased risk of fractures
  • Diarrhea, abdominal pain and headache reported in less than 5% of patients
22
Q

____ and ____ inhibit CYP450 decreasing metabolism of which drugs?

A

Omeprazole and Cimitidine inhibit CYP450 decreasing metabolism of Warfarin, Diazepam, Phenytoin

23
Q

Clopidogrel (prodrug) requires activation by hepatic P450 _____ isoenzyme

drugs that affect this isoenzyme are (3) - what is their effect on clopidogrel?

A

Clopidogrel (prodrug) requires activation by hepatic P450 CYP2C19 isoenzyme

(LEO) Lansoprazole, Esomeprazole, Omeprazole inhibit CYP2C19 reducing Clopidogrel activation

24
Q

____ or ____ are preferred in persons taking clopidogrel

A

pantoprazole or rabeprazole are preferred in persons taking clopidogrel

25
Q

H. Pylori is gram ____, contains ____ and H +/-?

causes inflammatory response, with increased risk of:

A

H. Pylori is gram negative, contains urease and H+

causes inflammatory response, with increased risk of:

  • Peptic ulcer disease (esp. duodenal)
  • Gastritis
  • Gastric MALToma
  • Gastric adenocarcinoma
26
Q

H. Pylori eradication triple therapy combines two ____ with a ____, resulting in <15% recurrence

A

H. Pylori eradication triple therapy combines two antibiotics with a PPI, resulting in <15% recurrence

27
Q

describe how PPIs promote eradication of H. pylori

A
  1. Direct antimicrobial properties
  2. Increased gastric pH → lowers minimal inhibitory concentrations of antibiotics needed to clear the organism
28
Q

Triple therapy for ____ days - which drugs?

A

Triple therapy for 10-14 days - which drugs?

Clarithromycin + Amoxicillin + PPI

Clarithromycin + Metronidazole + PPI

29
Q

Quadruple therapy for ___ days - which drugs?

A

Quadruple therapy for 14 days

Bismuth Subsalicylate + Tetracycline + Metronidazole + PPI

30
Q

list the mucosal protective agents

A
  • Misoprostol
  • Sucralfate
  • Bismuth Subsalicylate
31
Q

Misoprostol is a ____ analog

A

Misoprostol is a PGE1 analog

32
Q

____ binds to EP3 receptor on ___ cells stimulating ___

pathway → decreasing gastric acid secretion

A

Misoprostol binds to EP3 receptor on parietal cells stimulating

Gi pathway (decreasing cAMP) → decreasing gastric acid secretion

33
Q

Misoprostol also stimulates ___ and ___ secretion,

and enhances mucosal ____

A

Misoprostol also stimulates mucus and bicarbonate secretion,

and enhances mucosal blood flow

34
Q

____ is used for preventing NSAID-induced ulcers in high-risk patients

A

Misoprostol is used for prevention of NSAID-induced ulcers

(NSAIDS block PGE1 production)

35
Q

Misoprostol AEs and contraindications

A
  • Diarrhea, abdominal pain, cramps (30%)
  • Contraindicated in pregnancy d/t abortifacient effects
36
Q

Sucralfate MOA

A
  • Sucralfate: sucrose salt + sulfated aluminum hydroxide
  • Forms viscous paste that binds selectively to ulcers
  • -ve sucrose sulfate binds +ve proteins forming a physical barrier → restricting further caustic damage
  • Stimulates mucosal PG and bicarbonate secretion
37
Q

Sucralfate clinical use

A

initial management of GERD in pregnancy

38
Q

Bismuth subsalicylate (BSS) suppresses ____

Does it have a neutralizing action on gastric acid?

A

Bismuth subsalicylate (BSS) suppresses H. pylori

NO neutralizing action on gastric acid

39
Q

Bismuth Subsalicylate clinical use

A
  • Quadruple antibiotic therapy of H. pylori-positive ulcers
  • Pepto-Bismol is widely used for dyspepsia and acute diarrhea
40
Q

Bismuth toxicity and contraindications

A
  • Rare
  • Metabolite bismuth sulfide causes harmless blackening of the stool → may be confused with gastrointestinal bleeding
  • BSS can cause salicylate toxicity in combination with other salicylate products
  • Contraindicated in renal failure
41
Q

Prokinetic agents enhance coordinated GI ___

Ideally should act ___ of ACh

A

Prokinetic agents enhance coordinated GI motility

Ideally should act upstream of ACh (at receptor sites on the enteric neuron itself or higher)

42
Q

Why are muscarinic (M1) receptor agonists not currently preferred for treating GI motility disorders?

A

Activated M1-receptors enhance contractions in an uncoordinated fashion, producing little/no net propulsive activity

Bethanechol (cholinomimetic agent) and Neostigmine (ACh esterase inhibitor) are not preferred for treating GI motility disorders

43
Q

Erythromycin (macrolide) has ____ effects at the ___ receptor

Rapid down-regulation of this receptor leads to ______→ use is limited to short courses

A

Erythromycin (macrolide) has agonistic effects at the motilin receptor

Rapid down-regulation of this receptor leads to early tolerance → use is limited to short courses

44
Q

Erythromycin is a CYP450 ____

A

Erythromycin is a CYP450 inhibitor

45
Q

best established indication for Erythromycin is

A

Diabetic gastroparesis

46
Q

Describe Cisapride

A
  • 5-HT4 agonist
    • increase cAMP, stimulates enteric neurons
  • 5-HT3 antagonist
    • smooth muscle stimulant
  • was used for GERD and Gastroparesis
  • no longer available in U.S. → can induce serious/fatal cardiac ventricular arrhythmias
47
Q

Metoclopramide:

____ agonist

vagal and central ___ antagonist

___ receptor antagonist

A

Metoclopramide:

5-HT4 receptor agonist

vagal and central 5-HT3 receptor antagonist

D2 receptor antagonist

48
Q

____ increases LES tone and stimulates antral & small intestinal contractions

A

Metoclopramide increases LES tone and stimulates antral & small intestinal contractions

49
Q

Metoclopramide clinical indications

A
  • Antiemetic (d/t central 5-HT3 block)
  • symptom relief in GERD (doesn’t heal)
  • Diabetic gastroparesis
  • acid suppression therapy is more efficacious/preferred
50
Q

Metoclopramide AEs

A
  • Extrapyramidal effects
    • ​d/t DA antagonism
    • mc in children/young adults at higher doses
  • Galactorrhea
    • blocks dopamine which normally inhibits prolactin release
  • QT prolongation → torsades
  • Depression

Pharmacology (19 decks)

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