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GI II > Drugs for abdominal pain, diarrhea, and constipation > Flashcards

Drugs for abdominal pain, diarrhea, and constipation Flashcards

1
Q

what are the Prostaglandin inhibitors? and use?

A

Bismuth and used for diarrhea

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2
Q

What are the opioid agonists and their general use

A

Loperamide
Diphenoxylate
Eluxadoline

diarrhea

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3
Q

what are the Serotonin 5Ht-3 antagonists and their general use

A

Alosetron

diarrhea

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4
Q

what are the Chloride Channel Inhibitors and their general use?

A

Crofelemer

diarrhea

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5
Q

Mechanism of Action and side effects of Loperamide?

A

Interferes with peristalsis (slows transit time)

Direct action on circular and longitudinal muscles of intestinal wall, slowing motility
–Slowed motility allows for fluid/electrolyte reabsorption and increasing bulk/density of feces

Side effect:
classic anticholinergic
does not exhibit opiate like effects or addiction but can cause Cardiac toxicities

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6
Q

Mechanism of action and side effects of Diphenoxylate

A

Mechanism of Action:
Believed to exert effect locally & centrally on GI smooth muscle cells; inhibits GI motility and slows excess GI propulsion

•Side effects:
Classic anticholinergic; atropine

is a synthetic opiate agonist and can cause opioid effects at high dosages so atropine is added to discourage over dosage

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7
Q

Indication and mechanism of action of Eluxadoline

A

•Mechanism of Action:
Agonist at opioid mu& kappa receptors in GI (slows peristalsis/delays digestion)

Antagonist at delta opioid receptors in GI
stomach, pancreas, biliary secretions decreased

•Indication:
Irritable Bowel Syndrome, Diarrhea-predominant subtype (IBS-D)

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8
Q

what are major side effects of Eluxadione and its contraindictions

A

Side effects:
Hepatic/Pancreatic toxicity (increased enzymes)
Pancreatitis high-risk in pts. w/o a gallbladder
–Deaths have occurred (FDA warning)

CNS-related:
sedation/euphoria/impaired cognition

Contraindications:
biliary duct obstruction
alcoholism
history of pancreatitis
severe hepatic impairment
•Stop therapy if severe constipation develops and lasts 4+ days
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9
Q

Mechanism of action and indication for Alosetron

A

Selectively blocks GI-based 5HT3 receptors
Antagonism (receptor blocking) modulates regulation of visceral pain, colonic transit & GI secretions

Indications: Chronic, severe IBS-D not responsive to other conventional therapies (women)

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10
Q

what are the side effects and contraindications of Alosetron

A

Ischemic Colitis (Black Box Warning)
Physicians must enroll in prescribing program
Patients and physicians must sign a risk-benefit statement and agree to adhere to therapy plans
Additional self-training and testing by physicians to learn to appropriately diagnose IBS required
No refills without a follow-up exam by the prescriber

Contraindications:
History or Current:
GI obstruction, perforation, stricture/adhesions, toxic megacolon
Diverticulitis, Crohn’s disease, or Ulcerative colitis
Impaired intestinal circulation, thrombophlebitis or a hypercoagulable state
Severe constipation

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11
Q

Description and Mechanism of action of Cl- Channel Inhibitor

A

Description:
derived from dark red sap of Croton lechleri tree (botanical pharmaceutical)

•Mechanism of Action:
Inhibits chloride ion secretion by blocking cAMP-stimulated CFTR (cystic fibrosis transmembrane regulator) & calcium-activated (CaCC) chloride channels
channels regulate fluid secretion by intestinal epithelial cells

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12
Q

Indication and side effects of Crofelemer

A

Indication:
Non-infectious diarrhea in HIV/AIDS (for pts. on anti-retroviral therapy)

•Side Effects:
GI-related
Abdominal distention, elevated AST/ALT/Bilirubin
Infections
Respiratory/Urinary
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13
Q

what are the type and drug names used for abdominal pain

A

Antimuscarinic Agents
Hyoscyamine
Dicyclomine

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14
Q

what are Antimuscarinics MOA, Indication and side effects

A

Mechanisms of Action:
Competitively-inhibit autonomic, post-ganglionic cholinergic receptors (multiple sites)

•Indication:
Abdominal pain/spasms

•Side Effects:
Classic Anticholinergic-based

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15
Q

What are the Peripheral Opioid antagonists and what are their general function?

A

Methylnaltrexone
Naloxegol
Alvimopan

Constipation

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16
Q

What are the Guanylate Cyclase-C agonists and what are their general function?

A

Linaclotide

COnstipation

17
Q

what are the Selective Chloride C2 channel activators and what are their general function

A

Lubiprostone

Constipation

18
Q

Mechanism of action for Peripheral Opioid antagonists and which one is only used in the hospital

A

peripheral mu-opioid receptor antagonists

No common, significant CNS actions nor induction of withdrawal/pain symptoms

Alvimopan

19
Q

What are the Indications and side effects of Peripheral Opioid antagonists

A

Opioid-Induced Constipation (OIC)

Alvimopan–only for accelerating time to GI recovery following bowel resection surgery with primary anastomosis (prevention of postoperative ileus)

Side effects: GI related

Alvimopan carries a risk of MI with use;
REMS program requires use only in approved institutions for max. of 15 doses

20
Q

Linaclotide mechanism of action, indications and side effects

A

Selective guanylate cyclase-C (GC-C) Agonist

Binds to GC-C on luminal surface of intestinal epithelium & increases intracellular/extracellular concentrations of cGMP
Stimulates secretion of chloride/bicarbonate into intestinal lumenvia activation of cystic fibrosis transmembrane conductance regulator (CFTR) ion channel

•Indications:

  1. Irritable Bowel Syndrome-Constipation predominant subtype (IBS-C)
  2. Chronic Idiopathic Constipation (CIC)

•Side Effects:
GI-Related

21
Q

Mechanism of action for Lubiprostone

A

a prostaglandin-E1(PGE-1) derivative
increases intestinal fluid secretion by activatingGI-specific chloride channels (ClC-2) in luminal cells of intestinal epithelium

22
Q

Indications and side effects of Lubiprostone

A

Indications:

  1. Irritable Bowel Syndrome-Constipation predominant subtype (IBS-C) (women)
  2. Chronic Idiopathic Constipation (CIC)
  3. Opioid-Induced Constipation (OIC)

•Side Effects:
GI-related
CNS-related

23
Q

What are stimulant Laxative and Cathartic agents?

A 
Bisacodyl
Castor Oil
Glycerin
Senna
Na+Picosulfate
24
Q

what are osmotic Laxatives and Cathartic agents

A 
Lactulose
Mag. citrate
Polyethyleneglycol (PEG)
Sorbitol
(Glycerin)
25
Q

what are saline Laxative and Cathartic agents

A

Mag. hydroxide

Na+phosphate

26
Q

what are bulk forming Laxative and cathartic agents

A 
Dietary (Fiber/Bran
Fruits/Grains/Cereal)
Psyllium
Methylcellulose/
Carboxymethylcellulose
Calcium polycarbophil
27
Q

what are stool softners laxative and cathartic agents

A

Docusate
Mineral Oil

also known as Surfactant or emollient laxatives

28
Q

what is the mechanism of action and efficacy of Bulk forming/hydrophilic colloidal agents

A

Work to increase bulk-volume and water content, thereby increasing GI motility

  • Fiber can also support colonic bacteria, fermentation, and digestion
  • Efficacy is seen in 2-4+ days
29
Q

adverse and drug interactions of bulk forming/ hydrophilic colloidal agents

A

Adverse Effects:
Bloating/Obstruction
Drink fluids (caution in renal failure)

•Drug Interactions:
LOTS!(recommendation similar to that of the bile acid sequestrants, antacids, etc…)

30
Q

mechanism and efficacy of stool softners

A

Anionic surfactants–soften/lubricate feces:
Increases fluid secretion into GI tract
Decreases fluid reabsorption from GI tract
Mineral oil penetrates stool to soften

efficacy: seen in 1-3 days for minimal laxative effect

31
Q

what is the main purpose of Sodium Picosulfate

A

Pre-Colonoscopy bowel prep

also has magnesium oxide/anhydrous citric acid that metabolically converts to magnesium citrate (osmotic)

32
Q

what is the mechanism of action of the stimulants

A

Irritant to enterocytes, GI smooth muscle leading to inflammation
Na+/K+-ATPase inhibition and/or increase in prostaglandin synthesis/secretion (via cAMP/GMP)

Promote water/electrolyte accumulation in GI
Castor oil is hydrolyzed to ricinoleic acid

Glycerin is a tri-hydroxyl alcohol and functions as an irritant &an osmotic &lubricant agent

33
Q

what is the efficacy, adverse effects and contraindications of stumulant laxatives

A

Efficacy of usual laxative doses seen in 12-36 hours

•Adverse Effects:
Abdominal cramping
Urine discoloration (yellow-brown/red-pink) in Senna
Fluid/electrolyte disturbances (long use)

•Contraindications:
GI obstruction/Ileus/Impaction

34
Q

Mechanism of actio of Saline agents

A

Magnesium/Phosphate ions poorly absorbed
Hyperosmolar solutions
Osmotically retain water in GI tract

•Greater volume shortens transit time

35
Q

Drug interactions and Cautions of Saline agents

A 
•Drug Interactions:
Diuretics (electrolytebalance)
•Cautions:
Renal disease (electrolytes)
CHF/HTN (sodium)
36
Q

Mechanism of Osmotic agents and efficacy

A
  • Osmotically attract and retain increased water in colon increasing moisture, softness and volume/bulk
  • In general, these agents provide effects in 1-2+ days with laxative doses; larger doses may provide catharsis sooner (hrs)

Efficacy may be seen within 1-3 hour of large-volume administration
Smaller, daily doses provide effects in 0.5-3 days

37
Q

what is another use for Lactulose

A

•Lactulose also used for severe liver disease patients (hyperammonemia)

Change in pH traps ammonia in GI

38
Q

Adverse effects of osmotic agents

A

•Adverse Effects:
Electrolyte Disturbances; watch closely in at-risk patient populations!
GI-related

39
Q

what is the number one reason to use Polyethylene glycol

A

PEG 3350

Large doses (volume) used for bowel prep prior to GI scopes, radiological procedures or surgery

Smaller doses for constipation

GI II (5 decks)

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