Agents for GERD Flashcards

1
Q

What are the drug therapy goals in treating GERD?

A
  1. Eliminate Symptoms 2. Heal Esophagitis 3. Prevent the relapse of esophagitis 4. Prevent the development of complications
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2
Q

What types of medications are useful in the treatment of GERD?

A

Antacids H2- Receptor Blockers PPIs Prokinetic Agents (Cisapride, Metoclopramide, Bethanechol) Mucosal Protectants (Sucralfate)

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3
Q

MOA of Antacids

What electrolyte imbalance do ALL antacids cause?

A

Weak bases that increase gastric pH through acid-neutralizing ability to form a salt & water

  • Can affect absorption, bioavailability, or urinary excretion of other drugs by altering gastric & urinary pH or by delaying gastric emptying

*****ALL antacids cause HYPOKALEMIA****

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4
Q

H2-Blockers MOA

A

Competitively block H2 receptors on gastric parietal cells, thereby decreasing acid production (Reverible)

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5
Q

PPIs MOA

A

Irreversibly inhibit gastric parietal cell H/K-ATPase inhibiting gastric acid secretion

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6
Q

Cisapride MOA

A

increases LES pressure accelerates gastric emptying time increases amplitude of esophageal contractions 5-HT4 agonist 5-HT3 antagonist

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7
Q

Metoclopramide

A

D2 receptor blocker increases LES pressure accelerates gastric emptying time

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8
Q

Sucralfate

A

complexes with positively charges proteins to form a viscous coat when exposed to acid- thereby protecting gastric lining from gastric acid secretions

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9
Q

What are adverse s/e caused by metoclopramide?

A

Anxiety Insomnia Extrapyramidal Symptoms Increased Prolactin levels

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10
Q

What are the adverse effects cause by sucralfate?

A

Constipation Nausea Abdominal Discomfort

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11
Q

Which antacids can produce a metabolic alkalosis?

A

Sodium Bicarbonate Calcium Carbonate

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12
Q

What are the possible adverse effects of Aluminum Hydroxide antacids?

A
  • aluMINIMUM amount of feces=Constipation
  • Hypophosphatemia
  • Proximal muscle weakness
  • Osteodystrophy- bone damage via binding phosphate in the gut
  • Seizures
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13
Q

What are the possible adverse effects of Magnesium Hydroxide antacids?

A
  • Mg= Must Go to the bathroom! Diarrhea
  • Hyporeflexia
  • Hypotension
  • Cardiac Arrest
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14
Q

What are the possible adverse effects off Calcium Carbonate antacids?

A
  • Hypercalcemia
  • Rebound increase in acid when use is halted
  • Can chelate & decrease the effectivenesss of other drugs (eg tetracycline)
  • belching
  • Constipation
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15
Q

What causes the milk-alkali syndrome?

A

Ingestion of excessive amounts of calcium & absorbable alkali such as sodium bicarbonate or calcium carbonate

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16
Q

What is a potential complication after d/c chronic antacid use?

A

Acid rebound

17
Q

List the H2-Blockers

A

“-TIDINE” CimeTIDINE FamoTIDINE RaniTIDINE NizaTIDINE

18
Q

Which H2-Blocker inhibits hepatic cyt P-450 metabolizing enzymes?

A

Cimetidine

19
Q

Which H2-Blocker can cause gynecomastia?

A

Cimetidine (prolactin-stimulating activity)

20
Q

Which H2-Blocker has antiandrogenic activity?

A

Cimetidine

21
Q

What are the common s/e of PPIs?

A
  • Prolonged use–> bacterial overgrowth in the GI tract= increased risk for C.Diff infxn
  • Pneumonia
  • decreased serum Mg w long-term use
  • pts>50 yo taking chronic high doses of PPIs have increased risk of hip fractures
22
Q

What is the most serious s/e of Cisapride?

A

Prolongation of QT interval

23
Q

What arrhythmia can be caused by prolongation of the QT interval?

A

Torsades de points (polymorphic ventricular tachycardia)

50
Q

Cisapride should be avoided in which type of pts?

A
  • Pts with prolonged QT intervals
  • Pts taking medications that inhibit cyt P-ESO 34A
    • Fluconazole
    • Ketoconazole
    • Itraconazole
    • Erythromycin
    • Clarithromycin
    • Ritonavir
51
Q

Which drugs increase Cisapride blood levels by inhibiting the cyt P-450 34A enzymes that metabolize Cisapride?

A
52
Q

What is the class of drugs that ends in “-dine”?

A

H2 Blockers

  • Cimetidine
  • Ranitidine
  • Famotidine
  • Nizatidine

Take H2 Blockers before you DINE- think “table for 2” to remember H2

53
Q

What are the clinical uses for H2 Blockers?

A
  • Peptic Ulcer
  • Gastritis
  • Mild Esphagel Reflux
54
Q

What are the toxicities associated with Cimetidine?

Do other H2 blockers share these same effects?

A
  • Potent inhibit of cyt P-450 (multiple drug interactions)
  • Antiandrogenic effects
    • PL release
    • Gynecomastia
    • Impotence
    • Decreased Libido in males
  • Can cross BBB & Placenta
    • Confusion
    • Headaches
    • Dizziness
  • Decreases renal excretion of Creatinine (ALSO RANITIDINE)

Other H2 blockers are relatively free of these effects

55
Q

What are the clinical uses for PPIs?

A
  • Peptic Ulcer
  • Gastritis
  • GERD
  • Zollinger-Ellison Syndrome