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OSD_GI > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Histamine is released in the stomach by __(a)__ cells in response to __(b)__?

A

a) Enterochromaffin-like Cells (ECLs)

b) ACh released by the Vagus nerve

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2
Q

Gastrin is released by G cells in the _____.

A

antrum (of stomach).

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3
Q

Effect of Histamine release in the stomach?

A

Histamine triggers the release of acid by the Parietal Cells via H2 receptors

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4
Q

ACh, from the Vagus nerve has what effects on stomach cells?

A
  1. Release of HCl from Parietal cells
    (directly via M3 receptors & indirectly via Histamine release on H2 receptors)
  2. Release of Mucus & Bicarbonate from Superficial Epithelial cells
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5
Q

Gastrin effect on stomach cells?

A

Causes the release of HCl from Parietal cells

via CCK2 receptors

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6
Q

Prostaglandins effect on stomach cells?

A

PGE2 inhibits release of HCl from Parietal cells
(via EP3 receptors)

PGI2 causes release of Mucous & Bicarbonate from Superficial Epithelial Cells
(via EP3 or EP? receptors)

(they also increase blood flow to stomach)

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7
Q

NO effect on stomach?

A

Increases blood flow to stomach

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8
Q

H2-blockers: side effects?

A

Very rare - mostly seen w/ Cimetidine

• Headache, dizziness, myalgia
• CNS AEs possible in elderly with impaired renal or hepatic function
• Confusion, hallucinations, etc.
• Drug Interactions – cimetidine inhibits CYP1A2, CYP2C19, CYP2D6, CYP3A4
• Antiandrogenic – cimetidine inhibits DHT binding to androgen receptor → impotence, loss of libido, gynecomastia
– Inhibit estradiol metabolism & increases prolactin levels
• All - ↓doses in mod. to severe renal dysfunction

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9
Q

H2-receptor Antagonist: effects?

A
  • ↓ Volume & [H+] of gastric secretion
  • ↓ Basal acid secretion
  • ↓ Gastrin & ACh stimulated secretion

• ↓ Food stimulated acid secretion – Modest

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10
Q

4 H2-receptor antagonists?

A

Cimetidine, Ranitidine, Famotidine, Nizatidine

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11
Q

Most potent H2-receptor Antagonist?

A

Famotidine

also longest effect
*available PO & IV

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12
Q

H2-Receptor Antagonists - Indications?

A
  • Rx for gastric & duodenal ulcers
  • Zollinger-Ellison syndrome
  • GERD
  • Erosive esophagitis
  • OTC – heartburn, acid indigestion, etc.
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13
Q

PPI - inhibition is reversible or irreversible?

A

Irreversible

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14
Q

PPIs - effects?

A
  • ↓↓ Acid secretion (basal & stimulated)
  • N/C in volume of secretion
  • ↑↑Gastrin secretion – hyperplasia of ECL cells
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15
Q

IV formulations available for which of the PPIs?

A

esomeprazole, pantoprazole, & lansoprazole

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16
Q

PPIs - Indications?

A

• GERD – erosive esophagitis treat/prevention

• PUD
– H pylori associated ulcers healing/ treatment
– NSAID-induced ulcers
– Prevention of rebleeding from peptic ulcers

• Dyspepsia – OTC – omeprazole, lansoprazole
– Limited to 14 day Tx no more than 3 times/yr

  • Prevention of stress ulcers in ICU patients – IV
  • Hypersecretory conditions – Zollinger- Ellison
17
Q

PPIs- adverse effects?

A

Very safe drugs! AEs in small % of patients

  • GI (nausea, diarrhea, colic, constipation)
  • CNS (headache, dizziness, somnolence)
  • Skin rash
  • ↑↑ Liver enzymes

• Potential DDI
– CYP2C19 & CYP3A4 – Clopidogrel, warfarin, methotrexate, tacrolimus
– Drugs with pH dependent absorption

18
Q

PPIs - safety warnings?

A
  • PPI Symptom relief does not rule out gastric Ca
  • PPI use may increase risk of C. difficile infection
  • Prolong use of high does may be associated with ↑ risk of osteoporosis-related bone fracture of the hip, wrist or spine.
  • Rare cases of life threatening hypomagnesemia have been reported in after prolonged use.
  • Cases of vitamin B12 deficiency have been reported with prolonged use.
19
Q

Misoprostol - MOA?

A
  • ↑ Secretion of Mucus & Bicarbonate from superficial epithelial cells
  • ↓ Acid secretion
20
Q

Misoprostol - contraindications?

A

Pregnancy

21
Q

Misoprostol - Uses?

A
  • Used to prevent of NSAID-induced ulcers

* Available in combination with NSAIDs

22
Q

Misoprostol - adverse effects?

A

Diarrhea, colic

23
Q

Sucralfate - Effect

A

sadf

OSD_GI (13 decks)

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