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Unit 6 pharm - GI drugs
GI drugs
50
Pharmacology
Professional
02/27/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
What are the treatment objectives for ulcers? (3)
Definition

1) Neutralize acid.

2) Decrease acid production.

3) Increase mucosal resistance.

Term
Calcium Carbonate
Definition

Antacid.

MECH: Reacts with HCl forming calcium chloride and carbonic acid, raising pH. High pH reduces proteolysis of pepsin and reduces damaging effect of acid.

USE: Relieves pain. Heals ulcer faster than placebo. Requires high dosage; best taken 1 hr. after meal.

TOX: Constipating. Milk-alkali syndrome, nephrocalcinosis, rebound acidity, digitalis antagonism.

Term
Sodium bicarbonate
Definition

Antacid.

MECH: Raises pH. High pH reduces proteolysis of pepsin and reduces damaging effect of acid.

USE: Relieves pain. Heals ulcer faster than placebo. Requires high dosage; best taken 1 hr. after meal.

TOX: Rarely used due to systemic alkalosis. Enhances effect of amphetamine, quinidine and cinchophen.

Term

Magnesium Hydroxide and Magnesium Carbonate

(Maalox, Mylanta, Gelusil, Riopan)

Definition

Antacid.

MECH: Reacts with HCl forming calcium chloride and carbonic acid, raising pH. High pH reduces proteolysis of pepsin and reduces damaging effect of acid.

USE: Relieves pain. Heals ulcer faster than placebo. Requires high dosage; best taken 1 hr. after meal.

TOX: May cause Magnesium toxicity in the presence of renal disease. Diarrhea, hypokalemia, iron deficiency due to complexing in gut.

Term

Aluminum hydroxide

(Alternagel, Amphoijel)

Definition

Antacid.

MECH: Reacts with HCl forming aluminum chloride and water, raising pH. High pH reduces proteolysis of pepsin and reduces damaging effect of acid. Aluminun chloride forms aluminum phosphate in intestines which is non-absorbable, therefore it's not likely to disturb the serum electrolytes or serum pH.

USE: Relieves pain. Heals ulcer faster than placebo. Also exerts a protective effect on mucosa. Requires high dosage; best taken 1 hr. after meal. Good for renal failure patients (unload phos).

TOX: Constipation, phosphate depletion, weakness, anemia, tetany, apnea; delayed gastric emptying; concretions--fecaloma, colonic perforation and stercoral peritonitis; encephalopathy; impaired absorption of many drugs--tetracycline, digoxin, INH.

Term
Atropine
Definition

Anticholinergic.

MECH: Vagotomy-effect. Reduces hydrochloric acid secretion.

AE: Dry mouth, blurred vision, atony of bladder, constipation, drowsiness and mental confusion.

CONTRA: Pyloric obstruction, hiatal hernia, peptic esophagitis.

Term
Propantheline
Definition

Anticholinergic.

MECH: Vagotomy-effect. Reduces hydrochloric acid secretion.

AE: Dry mouth, blurred vision, atony of bladder, constipation, drowsiness and mental confusion.

CONTRA: Pyloric obstruction, hiatal hernia, peptic esophagitis.

Term
Metantheline bromide
Definition

Anticholinergic.

MECH: Vagotomy-effect. Reduces hydrochloric acid secretion.

AE: Dry mouth, blurred vision, atony of bladder, constipation, drowsiness and mental confusion.

CONTRA: Pyloric obstruction, hiatal hernia, peptic esophagitis.

Term
Cimetidine (Tagamet)
Definition

MECH: Blockage of Histamine H2 receptor on parietal cells lowering acid secretion. Inhibit 50-80% of acid secretion.

USE: Healing of ulcers. Prophylaxis of stress ulcers (in patients).

AE: Headache, lethargy, confusion, depression, hallucinations. Binds CYT P450 interfering with metabolism of theophylline, warfarin, dilantin or lidocaine.

Term
Ranitidine (Zantac)
Definition

MECH: Blockage of Histamine H2 receptor on parietal cells lowering acid secretion. Inhibit 50-80% of acid secretion.

USE: Healing of ulcers. Prophylaxis of stress ulcers (in patients).

AE: Headache, lethargy, confusion, depression, hallucinations. Binds CYT P450 interfering with metabolism of theophylline, warfarin, dilantin or lidocaine.

Term
Famitodine (Pepsid)
Definition

MECH: Blockage of Histamine H2 receptor on parietal cells lowering acid secretion. Inhibit 50-80% of acid secretion.

USE: Healing of ulcers. Prophylaxis of stress ulcers (in patients).

AE: Headache, lethargy, confusion, depression, hallucinations.

Term
Nizatidine
Definition

MECH: Blockage of Histamine H2 receptor on parietal cells lowering acid secretion. Inhibit 50-80% of acid secretion.

USE: Healing of ulcers. Prophylaxis of stress ulcers (in patients).

AE: Headache, lethargy, confusion, depression, hallucinations. Binds CYT P450 interfering with metabolism of theophylline, warfarin, dilantin or lidocaine.

Term
Omeprazole (prilosec)
Definition

MECH: Inhibition of H+/K+ ATPase on activated parietal cells.

USE: Administer on empty stomach 30mins prior to meal so that parietal cells are in active state. Better pain relief and faster healing thatn with H2 antagonists.

TOX: Headache, gynecomastia. Strong inhibitor of P450 delaying metabolism of diazepam, warfarin, and dilantin. Gastric hyperplasia--not good for long-term usage.

Term
Lansoprazole (prevacid)
Definition

MECH: Inhibition of H+/K+ ATPase on activated parietal cells.

USE: Administer on empty stomach 30mins prior to meal so that parietal cells are in active state. Better pain relief and faster healing thatn with H2 antagonists.

TOX: Headache, gynecomastia. Inhibitor of P450 delaying metabolism of diazepam, warfarin, and dilantin. Gastric hyperplasia--not good for long-term usage.

Term
Rabeprazole
Definition

MECH: Inhibition of H+/K+ ATPase on activated parietal cells.

USE: Administer on empty stomach 30mins prior to meal so that parietal cells are in active state. Better pain relief and faster healing thatn with H2 antagonists.

TOX: Headache, gynecomastia. Moderate inhibitor of P450 delaying metabolism of diazepam, warfarin, and dilantin. Gastric hyperplasia--not good for long-term usage.

Term
Esomeprazole (Nexium)
Definition

MECH: Inhibition of H+/K+ ATPase on activated parietal cells.

USE: Administer on empty stomach 30mins prior to meal so that parietal cells are in active state. Better pain relief and faster healing thatn with H2 antagonists.

TOX: Headache, gynecomastia. Inhibitor of P450 delaying metabolism of diazepam, warfarin, and dilantin. Gastric hyperplasia--not good for long-term usage.

Term
Pantoprazole (Protonix)
Definition

MECH: Inhibition of H+/K+ ATPase on activated parietal cells.

USE: Administer on empty stomach 30mins prior to meal so that parietal cells are in active state. Better pain relief and faster healing thatn with H2 antagonists.

TOX: Headache, gynecomastia. Does NOT inhibit P450 delaying metabolism of diazepam, warfarin, and dilantin--good for polypharmacy patients. Gastric hyperplasia--not good for long-term usage.

Term
Dexlansoprazole
Definition

MECH: Inhibition of H+/K+ ATPase on activated parietal cells.

USE: Administer on empty stomach 30mins prior to meal so that parietal cells are in active state. Better pain relief and faster healing thatn with H2 antagonists.

TOX: Headache, gynecomastia.  Inhibitor of P450 delaying metabolism of diazepam, warfarin, and dilantin. Gastric hyperplasia--not good for long-term usage.

Term
What are causes of peptic ulcers? (3)
Definition

1) NSAID use.

2) Helicobacter pylori.

3) Zollinger-Ellison Syndrome (gastrinoma).

Term
Bismuth Salts (PeptoBismul)
Definition

MECH: Crystals formed in acidic environment coat ulcer crater.

USE: Lowers recurrence rate of ulcer better than H2 antagonists.

TOX: Causes black discoloration of tongue or stool (can be confused with hemorrhage).

Term
Sucralfate
Definition

MECH: An aluminum hydroxide complex of sucrose binds to ulcerated tissue when activated by acid environment.

USE: As effective as H2 antagonist for healing and prevention of relapse.

TOX: Constipation, aluminum toxicity in renal failure.

Term
Misoprostol
Definition

MECH: Prostaglandin agonist increasing mucosal secretions, bicarbonate secretion, decreasing acid production--protecting surface of stomach.

USE: Prevention of NSAID-related gastric ulcers.

Term
How is H. pylori treated?
Definition

Triple therapy:

1) PPI or ranitidine bismuth citrate.

2) Metronidazole.

3) Tetracycline or Amoxicillin.

Term
What is the pathogenesis of GERD?
Definition

1) Impaired lower esophageal sphincter.

2) Hypersecretion of acid.

3) Decreased acid clearance (impaired peristalsis; abnormal saliva production).

4) Delayed gastric emptying/duodenogastric reflux.

Term
Metochlopramide
Definition

MECH: Peripheral dopamine antagonist increases gastric motility. CNS dopamine antagonism is anti-emetic.

USE: GERD--decreases acid in stomach. Outlet obstruction - stimulates upper GI motility without stimulating gastric, biliary or pancreatic secretions. Anti-emetic.

TOX: Tremor (extrapyramidal symptoms).

Term
Cisapride
Definition

MECH: Seratonin receptor agonist increases gastric motility.

USE: GERD--decreases acid in stomach.

 

Term
Prochlorperazine
Definition

Phenothiazine - neuroleptic class.

MECH: Acts on Chemo Receptor Trigger Zone (CRTZ) in medulla (vomiting center). CNS interaction with dopaminergic receptor - antagonist.

USE: Antiemetic.

AE: Torticollis.

Term
Promethazine
Definition

Phenothiazine - neuroleptic class.

MECH: Antihistamineic (H1) receptor, anticholinergic.

USE: Antiemetic.

AE: Somnolence.

Term
Trimethobenzamide
Definition

Benzamide derivative.

MECH: Unknown but acts on CRTZ.

USE: Antiemetic.

AE: Extrapyramidal symptoms--not as severe.

Term
Tetrahydrocannabinol (THC, Nabilone)
Definition

MECH: Supress the CRTZ by probably anticholinergic mechanism.

USE: Anti-emetic.

 

Term
Ondansetron
Definition

Seratonin receptor antagonists.

MECH: 5-HT3 receptor blockade.

USE: Anti-emetic.

AE: Headache, dizziness, somnolence.

Term
Granesitron
Definition

Seratonin receptor antagonists.

MECH: 5-HT3 receptor blockade.

USE: Anti-emetic.

AE: Headache, dizziness, somnolence.

Term
Dolasetron
Definition

Seratonin receptor antagonists.

MECH: 5-HT3 receptor blockade.

USE: Anti-emetic.

AE: Headache, dizziness, somnolence.

Term
Domperidone
Definition

MECH: Promotilty drug.

USE: Outlet obstruction and/or loss of gastric tone (DM).

Term
Loperamide (immodium)
Definition

Opioid agonist.

MECH: Increase rectal tone and distrupt peristalsis via mu receptor.

USE: Anti-diarrheal.

 

Term
Diphenoxylate
Definition

Opioid agonist.

MECH: Increase rectal tone and distrupt peristalsis via mu receptor allowing gut time to absorb fluid.

USE: Anti-diarrheal.

 

Term
Codeine Sulfate
Definition

Opioid agonist.

MECH: Increase rectal tone and distrupt peristalsis via mu receptor allowing gut time to absorb fluid.

USE: Anti-diarrheal.

 

Term
Metamucil
Definition

Colloid.

MECH: Absorbs water in intestines.

USE: Anti-diarrheal.

AE: Doesn't prevent dehydration.

 

Term
Kaopectate
Definition

Pectin.

 MECH: Absorbs water in intestines.

USE: Anti-diarrheal.

AE: Doesn't prevent dehydration.

Term
REMINDER: STUDY CONSTIPATION CHART--pg. 12 GI lecture 2.
Definition
Term
Mesalamine
Definition

MECH: Works on lumenal side. Anti-inflammatory agent derivative of salicylic acid.

USE: Inflammatory bowel disease (Crohn's, ulcerative colitis, etc.)

Term
Sulfasalazine
Definition

MECH: Works on lumenal side. Anti-inflammatory agent derivative of salicylic acid. Cleaved to release salicylic acid.

USE: Inflammatory bowel disease (Crohn's, ulcerative colitis, etc.)

Term
Osalazine
Definition

MECH: Works on lumenal side. Anti-inflammatory agent derivative of salicylic acid. As good as sulfasalazine but with less toxicity.

USE: Inflammatory bowel disease (Crohn's, ulcerative colitis, etc.).

Term
Azathioprine
Definition

Immunosuppressive agent.

MECH: Anti-metabolite - interferes with DNA synthesis.

USE: Ulcerative colitis; Crohn's disease.

 

Term
Infliximab
Definition

Immunosuppressive agent.

MECH: Anti-TNF alpha antibody.

USE: Crohn's; ulcerative colitis.

Term
Cyclosporine
Definition

Immunosuppressant.

MECH: Supresses T helper and T suppressor lymphocytes.

USE: Crohn's; ulcerative colitis.

Term
Dicyclomine Hydrochloride
Definition

MECH: Anticholinergic drug prevents colon spasm.

USE: IBS.

 

Term
Hyoscyamine Sulfate
Definition

MECH: Anticholinergic drug prevents colon spasm.

USE: IBS.

 

Term
Alosetron
Definition

MECH: Seratonin antagonist at 5HT3 receptor.

USE: Diarrheal prominant IBS. (Also depression).

AE: Constipation; ischemic bowel.

Term
Tegaserod maleate
Definition

MECH: 5HT4 receptor agonist.

USE: Constipation predominant IBS.

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