PGE1 analog - Incr production/secretion of gastric mucous barrier - Decr acid production

- Acute variceal bleeds - Acromegaly (blocks GH release from pituitary) - VIPoma - carcinoid tumors - helpful for 'secretory' diarrhea

GI Pharm from FA Flashcards by Jullet Han

what class?

Cimetidine

Ranitidine

Famotidine

Nizatidine

H2 blockers

Take H2 blockers before you dine: “Table for 2”

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H2 blockers: mech?

Reversible block of histamine H2 receptors

-> decr H+ secr by parietal cells

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H2 blockers: use?

peptic ulcers, gastritis, mild esophageal reflux

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Which H2 blockers have the most toxicity?

what is that tox?

Cimetidine: inhibits cytochrome P-450 -> multiple drug interactions.

Also is an anti-androgen -> prolactin release, gynecomastia, impotence, decr libido in males

Crosses BBB -> confusion, dizziness, headaches

crosses placenta.

Both Cimetidine and Ranitidine decrease renal excr of creatinine (could be a reason for elevated creatinine without another cause)

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Name the H2 blockers that have no toxic effects listed in FA? (2)

Famotidine

Nizatidine

(Ranitidine has only one tox effect: decr renal excr of creatinine. Cimetidine has a boatload.)

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What class?

Omeprazole, Lansoprazole, Esomeprazole, Pantoprazole, Dexlansoprazole

Proton Pump Inhibitors

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Mechanism?

Omeprazole, Lansoprazole, Esomeprazole, Pantoprazole, Dexlansoprazole

Irreversibly inhibit H/K ATPase in stomach parietal cells

(receptors on LUMEN side of the stomach)

(Proton Pump Inhibitors: inhibit “primary active transport”)

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Clinical Use?

Omeprazole, Lansoprazole, Esomeprazole, Pantoprazole, Dexlansoprazole

Peptic ulcer, gastritis, esophageal reflux, Zollinger-Ellison syndrome

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Toxocity?

Omeprazole, Lansoprazole, Esomeprazole, Pantoprazole, Dexlansoprazole

Incr risk of C Diff infection

Pneumonia

With long term use: hip fractures, decr serum Mg2+

(I’m sure this all has something to do with acid.)

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Bismuth, Sucralfate: Mech?

Binds to ulcer base –> physical protection, allows Bicarb secretion to re-establish pH gradient in the mucous layer.

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Bismuth, Sucralfate: Use?

Allows ulcer healing

Traveler’s diarrhea

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Misoprostol

Mech?

PGE₁ analog

Incr production/secretion of gastric mucous barrier
Decr acid production

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Misoprostol

Use?

Prevents peptic ulcers from NSAID use (NSAIDs block PGE₁ production)
Maintains PDA
Ripens cervix -> induces labor

(miso soup steams things open (PDA, cervix). Also is Jen’s hangover cure: aspirin + miso soup)

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Octreotide

Mech?

Long-acting somatostatin analog

Acts on ECL cell, not parietal cell

(Endocrine connection: somatostatin from hypothal decr GH and TSH release. If hypothalamus is destroyed, Octreotide can replace somatostatin)

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Octreotide

Use?

Acute variceal bleeds
Acromegaly (blocks GH release from pituitary)
VIPoma
carcinoid tumors
helpful for ‘secretory’ diarrhea

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Octreotide

Tox?

nausea, cramps, steatorrhea

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What class?

Aluminum hydroxide

Calcium carbonate

Magnesium hydroxide

Antacids

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Antacids: general tox?

affect absorption, bioavailability, or urinary excr of other drugs by altering gastric and urinary pH or by delaying gastric emptying
Hypokalemia

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Aluminum hydroxide: tox?

Antacid general tox = alter gastric/urinary pH or delay gastric emptying -> affect other drugs; hypokalemia

Specific to Al hydroxide: constipation, hypophosphatemia, prox muscle weakness, osteodystrophy, seizures

“Aluminimum amount of feces”

Calcium carbonate: tox?

Antacid general tox = alter gastric/urinary pH or delay gastric emptying -> affect other drugs; hypokalemia

Specific to Ca carbonate: hypercalcemia, rebound acid increase.

Can chelate and decr effectiveness of other drugs (ex tetracycline)

Magnesium hydroxide: tox?

Antacid general tox = alter gastric/urinary pH or delay gastric emptying -> affect other drugs; hypokalemia

Specific to Mg hydroxide: diarrhea, hyporeflexia, hypotension, cardiac arrest

“Mg = Must Go to the bathroom”

Class?

Magnesium hydroxide

Magnesium citrate

Polyethylene glycol

Lactulose

Osmotic laxatives

Osmotic laxatives: mech?

(Magnesium hydroxide

Magnesium citrate

Polyethylene glycol

Lactulose)

Provide osmotic load to drive water out

Lactulose treats hepatic encephalophy (gut flora degrade it into lactic acide and acetic acid -> promotes nitrogen excretion as NH4+

Osmotic laxatives: use?

(Magnesium hydroxide

Magnesium citrate

Polyethylene glycol

Lactulose)

Constipation

Lactulose: hepatic encephalopathy

Osmotic laxatives: tox? (Magnesium hydroxide Magnesium citrate Polyethylene glycol Lactulose)

diarrhea dehydration abuse by bulimics

Infliximab: mech?

Monoclonal antibody to TNF-a

Infliximab: use?

Crohn's Ulcerative colitis rheumatoid arthritis ank spondylitis psoriasis

Infliximab: tox?

Infection (possible reactivation of latent TB) fever hypotension

sulfazalazine: mech?

combination of sulfapyridine (antibacterial) + 5-aminosalicylic acid (anti-inflammatory) Activated by colonic bacteria

Sulfasalazine: use?

Ulcerative colitis Crohn's

Sulfasalazine: tox?

Malaise nausea sulfonamide tox decr sperm count (reversible)

metoclopramide: mech?

D2 receptor antagonist. decr resting tone, contractility, LES tone, motility does not change colon transport time

metoclopramide: use?

diabetic and post-surg gastroparesis (paralysis) Anti-emetic

metoclopramide: tox?

incr parkinsonian effects restlessness, drowsiness, fatigue, depression, nausea, diarrhea. Interacts with digoxin and diabetic agents

metoclopramide: CI in what patients?

pts with small bowel obstruction Parkinson dz patients (D1-receptor blockade)

Odansetron: mech?

5-HT₃ antagonist; decr vagal stimulation Powerful central-acting antiemetic "Keep on dancing with odansetron!"

Odansetron: use?

control vomiting post-op patients undergoing cancer chemo

Odansetron: tox?

headache constipation

Diphenoxylate: mech?

binds mu receptors in GI; slows motility

Diphenoxylate: use?

opiate anti-diarrheal (similar to meperidine - opioid agonist) in low doses, can slow gut motility with no euphoric effects packaged with atropine to discourage abuse!

Treatment for Crohn's disease? (5)

Corticosteroids Azathioprine Methotrexate Infliximab Adalimumab

Treatment for Ulcerative Colitis? (4)

ASA preparations (sulfasalazine) 6-mercaptopurine infliximab Colectomy

Treatment for hepatic encephalopathy?

Lactulose (bacterial action -\> acid produced -\> NH3 becomes NH4, ammonium trap) Low protein diet (less nitrogen intake) Rifaximin (kills intestinal bacteria)

Treatment for Crigler-Najjar syndrome? | (type I, Type II)

Type I: plasmapheresis, phototherapy Type II (less severe): phenobarbital (incr liver enzyme synthesis)

Treatment for Wilson disease?

Penicillamine or Trientine

Treatment of hereditary hemochromatosis?

- repeated phlebotomy - Iron chelation (deferasirox, deferoxamine)