Beruflich Dokumente
Kultur Dokumente
Neutralizing and
Suppressive Medications
Stimulatory receptors:
- Catecholamine (β)
- Muscarinic (M3)
- Gastrin (CCKB)
Inhibitory receptors:
- Somatostatin (SSTR)
- Histamine (H3)
ECL cell
Epinephrine
β● cAMP
M3
Parietal Cell
Stimulatory receptors:
- Histamine (H2)
- Muscarinic (M3)
- Gastrin (CCKB)
Inhibitory receptor:
- Somatostatin
- Prostaglandin E2
The parietal cell
CCKB
Gastrin
Ach Histamine
Parietal Cell
Zuidema G: Shackelford’s Surgery of the Alimentary Tract, 4th ed. Philadelphia, WB Saunders, 1995
The H+/K+-ATPase pump
resting secreting
♦
CCKb
Mechanisms for Acid Secretion
Zuidema G: Shackelford’s Surgery of the Alimentary Tract, 4th ed. Philadelphia, WB Saunders, 1995
Mechanisms for stimulation of acid
secretion
Overview
M3
Proton Pump Inhibitors (PPIs)
• omeprazole, esomeprazole, lansoprazole,
rabeprazole, pantoprazole.
∀ α-benzimidazoles
• Prodrugs
• Unstable at low pH
• T1/2 = 1 hour
Feldman: Sleisenger & Fordtran's Gastrointestinal and Liver Disease, 8th ed. 2006
PPIs
•EP3
Prostaglandin analogs:
Misoprostol
• Rapidly absorbed
• First-pass metabolism to form
misoprostol acid (= active form)
• Acid suppression < 30 min; lasts ≈ 2
hrs
• T1/2 = 20- 40 minutes
• Excreted in the urine: renal dosing
not necessary
Misoprostol: Side-effects
• Contraindicated:
1 IBD
2 Pregnancy (class X)
Misoprostol: indications
• Constipation (2%)
• gelusil x x x
• maalox x x
• mylanta x x x
• riopan plus magaldrate x
• rolaids x
• tums ex x
• milk of magnesia x
Antacids: side-effects
• Hypercalcemia
∀ ↓ PTH secretion
∀ ↑ Phosphate
• Ca2+ precipitation in kidneys/ CRI
Overview
• Complications:
- esophagitis/stricture
- chest pain
- laryngitis/asthma/chronic cough
- Barrett’s
GERD
• “step-down” approach:
↓ PPI or switch to H2-blocker
NSAID related ulcers: treatment
Continued or
further bleeding 12/110 40/110 p<0.001
• Acute GI bleeding:
– Benefits of iv PPI therapy still under
investigation
– Used routinely if endoscopic therapy is
needed
– new studies are promising and suggest a
decreased rate of recurrent bleeding
Case 1