Agents for Diarrhea & Constipation Flashcards
3 Classes of drugs & examples of specific drugs that are effective in the treatment of diarrhea?
- ADSORBENTS
- Kaolin
- Pectin
- Polycarbophil
- Attapulgite
- ANTIMOTILITY AGENTS
- Diphenoxylate
- Loperamide
- Morphine
- ANTISECRETORY AGENTS
- Bismuth Subsalicylate
MOA of Adsorbents (Kaolin, Pectin, Polycarbophil, Attapulgite)
Adsorbs (adheres to) drugs, nutrients, toxins, & digestive juices
MOA of Antimotility Agents (Diphenoxylate, Loperamide, & Morphine)
Decrease peristalsis by activating mu presynaptic opiod receptors in the enteric nervous system
MOA of Antisecretory Agents Bismuth Subsalicylate
Decrease fluid secretion in the bowel
What adsorbent can adsorb 60x its weight in water & treat BOTH diarrhea AND constipation
Polycarbophil
What are the potential s/e of bismuth subsalicylate?
- Salicylism (tinnitus, nausea, vomiting)
- Darkening of tongue & stools
- Induce gout attacks in susceptible pts
What antidiarrheal can decrease tetracycline absorption if given cocomitantly?
Bismuth Subsalicyclate
What antidiarrheal is often formulated in combination with atropine?
DIPHENOXYLATE= low therapeutic dose with potent anti-diarrheal effects w/out significant opiate effects
- combined w/ small dosese of atropine= LOMOTIL
- dry mouth, blurry vision, & nausea discourage abuse
Which class of antidiarrheals can cause paralytic ileus?
Antimotility agents
- Diphenoxylate
- Loperamide
- Morphine)
What medication is often used to treat flushing & diarrhea seen in carcinoid syndrome and VIPomas?
Octreotide
Non-antidiarrheal uses include treatment for esophageal varices & acromegaly
What is Octreotide’s MOA?
- Synthetic somatostatin analog that blocks release of serotonin & other Vasoactive peptides
- Direct inhibitory effects on intestinal secretion
- Direct stimulatory effects on intestinal absorption
What medication can be used in combo with antibiotics to bulk stools & absorb C. diff toxins A & B in C. Difficile colitis?
Cholestyramine= nonabsorbable binding agent
What types of medications cause constipation?
- Opioid analgesics
- Anticholinergics
- Calcium-containing antacids
- Aluminum containing antacids
- CCBs
- Clonidine
- Iron
- Sodium
- Polystyrene Sulfonate
These are the drug classes effective in the treatment of constipation. What is each of their MOA?
1) Bulk forming agents
2) Osmotic Laxatives
3) Irritants & Stimulants
4) Stool Softeners
5) Cl Channel Activators
1) BULK FORMING AGENTS
* form gels in large intestine which causes water retention & intestinal distention, which increases peristaltic activity
2) OSMOTIC LAXATIVES
- nonabsorbable compounds which draw fluid into the colon to maintain osmotic neutrality
- disten intestinal wall & increase peristalsis
3) IRRITANTS & STIMULANTS
* Irritate gut lining which subsequently increases peristalsis
4) STOOL SOFTENERS
* Surfactants that become emulsified w stool, thereby softening feces
5) Cl CHANNEL ACTIVATORS
- Activate Cl channels in the apical membrane of intestinal cells increasing fluid & intestinal motility without altering serum Na or K levels
- effects are localized to the GI tract
- increase fluid secretion into the intestinal lumen
- accelerate fecal transit
Name the Bulk Forming Agents used to treat constipation.
- Methylcellulose
- Psyllium Bran
- Magnesium-containing salts
- Polyethylene Glycol
Name the Osmotic Laxatives
- Lactulose
- Magnesium Hydroxide (milk of magnesia)
- Magnesium Citrate
- Polyethylene Glycol
- Sorbitol
Name the Irritants & Stimulants used to treat constipation
- Cascara
- Senna
- Aloe
- Bisacodyl
Name the Stool Softeners
- Mineral Oil Docusate (oral or enema)
- Glycerin Suppository
Name the Cl channel activator used to treat constipation
Lubiprostone (Amitiza)
What are the potential s/e of bisacodyl?
- Abdominal cramping
- Atonic colon
What Osmostic Laxative is used to treat hepatic encephalopathy?
How does it work?
LACTULOSE
Gut flora degrade it into metabolites (lactic acid & acetic acid)–>metabolites promote Nitrogen excretion as NH4+
What are the adverse s/e associated with osmotic laxatives?
- Diarrhea
- Dehydration
- May be abused by bulemics
- Harmful electrolyte imbalances
What are the treatments used for secretory diarrhea?
- Bismuth Subsalicylate
- Probiotics
- Octreotide