Gastrointestinal Pharmacology II: Therapeutic Management of Diarrhea and Constip
Terms
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Antidiarrheal Angents include:
a)
b)
c)
d)
e)
f) -
Antidiarrheal Angents include:
a)Antimotility Agents -Opiates, Opioid Derivatives
b)Anticholinergic Agents/Antispasmodics- atropine sulftate, atropine/hyoscyamine/phenobarbital/scopolamine (Donnatal), dicyclomine hydrochloride (Bentyl)
c)Adsorbents - Kaolin and pectin and attalpulgite mixtures (Kaodene, Kapectolin, Kaopectate), Bismuth subsalicylate (Pepto-Bismol)
d)Absorbents - Polycarbophil (Mitrolan, FiberCon)
e)Lactobacillus Acidophilus (Bacid, Lactinex)
f)Octreotide (Sandostatin) -
Antimotility Agents
Opiates include: -
Antimotility Agents
Opiates include:
1. Opium Tincture, Deodorized
2. Opium Tincture, Camphorated (Paregoric)
3. Paregoric combination products (Kaodene, Parepectolin) -
Antimotility Agents
Opioid Derivatives include: -
Antimotility Agents
Opioid Derivatives include:
1. diphenoxylate HCL with atropine sulfate (Lomotil)
2. difenoxin HCL with atropine sulfate (Motofen)
3. loperamide HCL (Imodium) -
Antimotility Agents
mechanism of action: -
Antimotility Agents
mechanism of action:
a. reduces intestinal motility and peristalsis in small and large intestine thereby slowing the transit of intestinal contents and increase contact time for gut absorption
b. Imodium slows intestinal motility via direct effect on nerve endings and on smooth muscles in intestines -
Antimotility Agents
clinical indications: -
Antimotility Agents
clinical indications:
a. OPIATES: acute, short-term, uncomplicated diarrhea
b. OPIOID DERIVATIVES: acute or chronic diarrhea -
Antimotility Agents
adverse effects: -
Antimotility Agents
adverse effects:
a. CNS: sedation, dizziness, fatigue, RESPIRATORY DEPRESSION, EUPHORIA
* only IMODIUM does NOT produce respiratory depression or euphoria -
Antimotility Agents
cautions and considerations: -
Antimotility Agents
cautions and considerations:
a. contraindications:
1)diarrhea associated with:
-invasive organisms (infectious)
-pseudomembranous colitis (antibiotic-associated)
-poisoning
2)ACUTE RESPIRATORY DEPRESSION - Anticholinergic Agents/Antispasmodics include:
-
Anticholinergic Agents/Antispasmodics include:
1. atropine sulfate
2. atropine/hyoscyamine/pheobarbital/scopolamine (Donnatal)
3. dicyclomine hydrochloride (Bentyl) -
Anticholinergic Agents/Antispasmodics
mechanism of action: -
Anticholinergic Agents/Antispasmodics
mechanism of action: decreases GI HYPERmotility; relieves cramping by decreasing vagal GI tone; prolongs gut transit time -
Anticholinergic Agents/Antispasmodics
adverse effects: -
Anticholinergic Agents/Antispasmodics
adverse effects:
a. anticholinergic: dry mouth, blurred vision, urinary hesitancy, tachycardia, constipation
b. CNS: headache, nervousness, drowsiness, dizziness - Adsorbents include:
-
Adsorbents include:
1. Kaolin and pectin and attalpulgite mixtures (Kaodene, Kapectolin, Kaopectate)
2. Bismuth subsalicylate (Pepto-Bismol) -
Adsorbents
mechanism of action: -
Adsorbents
mechanism of action:
a. no systemic ABsorption; minimal adverse effects
b. binds and removes bacteria, toxins and other irritants from the intestine; also act as protectants
c. bismuth subsalicylate - also inhibits intestinal secretions -
Adsorbents
clinical indications: -
Adsorbents
clinical indications: BISMUTH SUBSALICYLATE used for prevention or symptomatic treatment of SECRETORY diarrhea produced by ENTEROTOXIC E. coli and viral infections -
Adsorbents
cautions and considerations: -
Adsorbents
cautions and considerations:
a. pediatrics: avoid use of bismuth subsalicylate in presence of acute febrile illness (Reye's Syndrome)
b. pregnancy, breast-feeding: concern with high doses/chronic use of salicylates -
Adsorbents
drug interactions: -
Adsorbents
drug interactions:
a. bismuth subsalicylate: high does of ASPIRIN or other SALICYLATES; oral anticoagulants
b. oral medications: (i.e. tetracyclines) impaired absorption, therefore, administer adsorbents 2 hours before or 3-4 hours after medication - Absorbents include:
-
Absorbents include:
Polycarbophil (Mitrolan, FiberCon) -
Absorbents
mechanism of action: -
Absorbents
mechanism of action: absorb WATER thereby increasing fecal bulk; modify frequency and consistency of stools, but does NOT reduce fluid loss -
Lactobacillus Acidophilus (Bacid, Lactinex)
mechanism of action: -
Lactobacillus Acidophilus (Bacid, Lactinex)
mechanism of action: NATURAL INHABITANT of the GI tract which produces lactic acid thereby suppressing bacterial and fungal overgrwoth; reestablishes normal intestinal flora -
Lactobacillus Acidophilus (Bacid, Lactinex)
clinical indications: -
Lactobacillus Acidophilus (Bacid, Lactinex)
clinical indications: treatment of uncomplicated diarrhea, especially that associated with antibiotic therapy -
Octreotide (Sandostatin)
mechanism of action: -
Octreotide (Sandostatin)
mechanism of action:
a. suppresses secretion of SEROTONIN and GASTROENTEROPANCREATIC PEPTIDES
b. stimulates fluid and electrolyte absorption from GI tract
c. prolongs intestinal transit time -
Octreotide (Sandostatin)
clinical indications: -
Octreotide (Sandostatin)
clinical indications: to manage severe diarrhea associated with GI endocrine tumors (carcinoid, vasoactive intestinal peptide tumors) -
Octreotide (Sandostatin)
adverse effects: -
Octreotide (Sandostatin)
adverse effects:
a. metabolic: hyperglycemia or hypoglycemia
b. GI: abdominal pain, n/v/d
c. injection site: pain, burning, redness, swelling -
Octreotide (Sandostatin)
cautions and considerations: -
Octreotide (Sandostatin)
cautions and considerations:
a. diabetes mellitus: doses of antidiabetic agents may require adjustment
b. severe renal failure requiring dialysis; dosage reduction may be required
c. elderly: dose reduction due to decrease in clearance
d. pregnancy, breastfeeding: not recommended -
Octreotide (Sandostatin)
drug interactions: -
Octreotide (Sandostatin)
drug interactions:
a. oral antidiabetic agents; glucagon; growth hormone; insulin
b. cyclosporine serum levels may be decreased
c. dietary fat absorption may be altered
d. vitamin B12 levels depressed -
Therapeutic Management of Diarrhea -
General Approach to Treatment:
1.
2.
3.
4.
5. -
Therapeutic Management of Diarrhea -
General Approach to Treatment:
1. REST, including bowel rest (symptomatic relief)
2. DIET modifications
3. ADMINISTRATION OF FLUID AND ELECTROLYTES to prevent/correct imbalances
a)Rehydration: Pediatrics-Infalyte, Pedialyte
4. IDENTIFY AND TREAT the underlying cause/disease
a)Infectious diarrhea, "Traveler's"
b)Drug-induced
c)Disease-associated chronic diarrhea
5. ANTIDIARRHEALS ARE GENERALLY NOT REQUIRED FOR GREATER THAN 48 HOURS AND SHOULD NOT BE USED IN THE PRESENCE OF HIGH FEVER