Omeprazole - Prodrug activated by gastric acid environment - Enters the parietal cells via systemic circulation - Irreversibly binds to cystines in the H/K ATPase pump

Misoprostal Regulator of Gastric Acid MOA - Analogue of PEG2 - Activates the EP3 receptor on parietal cells. This decrease cAMP which inhibits the H/K ATPase pump Cytoprotective MOA - Analogue of PGE2 stimulates mucin and HCO3 production

Coating Agent - Combination of Sucrose and Aluminum hydroxide - Forms a paste which buffers acidic proteins in the ulcer (coats) - Stimulate PG synthesis and endothelial growth factors for repair

- Prostaglandins - Bismuth coating agents - Sucralfate coating agents

Pharm GI Flashcards by Mike Butler

Side effects of H2 receptor blockers

Ranitidine

Diarrhea
Headache
Fatigue

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MOA of PPI

Omeprazole

Prodrug activated by gastric acid environment
Enters the parietal cells via systemic circulation
Irreversibly binds to cystines in the
H/K ATPase pump

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Prostaglandins MOA

Misoprostal

Regulator of Gastric Acid MOA

Analogue of PEG2
Activates the EP3 receptor on parietal cells. This decrease cAMP which inhibits the H/K ATPase pump

Cytoprotective MOA
- Analogue of PGE2 stimulates mucin and HCO3 production

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Contraindications for Prostaglandins

Misoprostal

Pregnancy (stimulates uterine contraction)

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Side effects of prostaglandins

Misoprostal

Diarrhea
Abdominal Cramping
Uterine Contractions

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Cations used as antacids

Calcium Carbonate
Aluminum Hydroxide
Magnesium Hydroxide

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MOA of antacids

Binds with H+ to neutralize stomach acid

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Side effects of antacids

Mg = Diarrhea
- Mg has an osmotic effect

Ca = Hypercalcemia

Renal Calculi (Kidney stones)
Gas from CO2 release

Al = Hypophosphatemia
- Al binds phosphate

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MOA of Sucralfate

Coating Agent

Combination of Sucrose and Aluminum hydroxide
Forms a paste which buffers acidic proteins in the ulcer (coats)
Stimulate PG synthesis and endothelial growth factors for repair

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Contraindications of Sucralfate coating agents

Use caution with other aluminum containing drugs. Sucralfate is a combination of Sucrose and Aluminum hydroxide

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Side effects of Sucralfate coating agents

Constipation

- because of aluminum causing Hypophosphatemia

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MOA of Busmuth

Coating Agent
- Binds to the ulcer and releases PG 
      - PG releases HCO3 and mucin
- inhibits growth and adherence of 
H pilori

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Contraindications for Bismuth coating agents

Reyes Syndrome in kids

ASA administration with viral infection

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Side effects of Bismuth coating agents

Black tarry stools
Black tongue
Constipation
Tinnitus (ASA)

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Regulators of Gastric Acid Secretion

H2 Receptor Antagonists
PPI’s
Prostaglandins
Antacids

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Cytoprotective Drugs

Prostaglandins
Bismuth coating agents
Sucralfate coating agents

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MOA of H2 Receptor Antagonist

Ranitidine

Block histamine from binding H2 receptors. Decreased cAMP thus inhibits the H/K ATPase pump.

Also decreases gastrin and ACh induced secretion

MOA of bulk forming agents

Anti-diarrheal - Kaolin/pectin

Insoluble (hydrophilic) absorb H2O
Poorly fermentable colloids add gel to the stool
Bind to bacterial endotoxins

Laxative - Psyllium

Fermentable and Non-fermentable fibers add H2O and bacterial count to the stool
Fiber stimulates the gut

Contraindications of bulk forming agents

Kaolin/Pectin
- IBD

Psyllium

Obstructive symptoms
Megacolon

Side effects of bulk forming agents

Kaolin/ Pectin
- constipation

Psyllium
- Abdominal distention
(Fermentation leads to gas)

MOA of opiates

Loperamide

Mu receptors inhibit peristalsis of the colon
Delta receptors inhibit intestinal secretion

Contraindications of opiates

Loperamide

Severe Infectious Diarrhea
IBD

Side effects of opiates

Loperamide

Constipation

MOA if irritant/ laxatives

Sennosides

Irritate the intestinal wall through cAMP and cGMP which;
- Inhibit H/K ATPase pump
- NO release
- Increase platelet activating factor which is pro colonic secretions

Side effects of irritant/ laxatives

Sennosides Diarrhea

MOA of Osmotics

Polyethylene Glycol - Sugar and Alcohol - Salts and Electrolytes Both have osmotic forces which pull water into the stool - (think of mannitol) Mg also stimulates CCK

Contraindications of Osmotics

Polyethylene Glycol Sugar - None Salts - Renal dysfunction and diuretics

Side effects of Osmotics

Polyethylene Glycol Sugars - Abdominal distention and flatulence (sugar causes fermentation) Salts - Electrolyte imbalance (caution with renal disease)

MOA for stool softeners

Docusate and Mineral Oil - Surfactants which allow H2O into the stool - Stimulate intestinal secretion through cAMP

Side effects of stool softeners

Docusate and Mineral Oil - Limits vitamin absorption - Foreign body reactions - Lipid Pneumonitis

MOA for Prokinetics: Dopamine Amtagonists

Domperidone ``` Increase ACh from transmitting impulses in SI smooth muscle - by blocking dopamine from binding to D2 receptors - D2 inhibits ACh (Blocking D2 increases ACh) Almost exclusively acts on UGI - increases lower esophageal sphincter tone ``` Metoclopramide - Antiemetic - Block D2 in the CTZ

Contraindications for Prokinetics: Dopamine Antagonists

Dromperidone and Metoclopramide - Onstruction - Perforation

Side effects of Prokine: Dopamine Antagonists

Dromperidone and Metoclopramide Hyperprolactiemia - Galactorrhea - Gynecomastia - Dysmenorrhea

MOA of Cannaboids

THC Binds to Cannaboid receptors - CB1 - Brian - CB2 - Periphery These receptors inhibit cAMP and increase DA

Contraindications of Cannaboids

THC - Cardiovascular Disease - Pregnancy - Psychosis

Side effects of Cannaboids

THC - Euphoria - Drowsiness - Tachycardia - Hypertension

MOA of Serotonin Antagonist

Ondansetron Block 5-HT3 (serotonin) receptors in: - CTZ - Vagus - Mesenteric Plexus - Spinal sensory neurons

Side Effects of Serotonin Antagonist

Ondasetron - Headache - Lightheaded - Constipation Severe but rare * Ischemic Colitis * QT Prolongation

MOA for pancreatic enzymes

Pancrlipase ``` Adjunct for pancreatic enzymes Combination of - Amylase - Lipase - Protease ```

Side effects for pancreatic enzymes

Pancrelipase - Diarrhea - Abdominal Pain - Hyperuricosuria - Renal Stones