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GI Week 2 & 3 > Drugs for Diarrhea, Abdominal Pain, and Constipation > Flashcards

Drugs for Diarrhea, Abdominal Pain, and Constipation Flashcards

1
Q

What classes of drugs are used to treat diarrhea?

A

1) Prostaglandin inhibitors
2) Opioid agonists
3) Serotonin (5HT3) Antagonists
4) Chloride channel inhibitors

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2
Q

Bismuth which is used to treat diarrhea belongs to what class of drugs?

A

Prostaglandin inhibitors

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3
Q

Loperamide, Diphenoxylate, and Eluxadoline belong to what class of drugs?

A

Opioid agonists

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4
Q

Alosetron belongs to what class of drugs?

A

Serotonin (5HT3) Antagonists

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5
Q

Crofelemer belongs to what class of drugs?

A

Chloride channel inhibitors

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6
Q

What is the MOA of the opioid agonist loperamide?

It has direct action on what muscles of the intestinal wall that causes the above answer?

A

1) Interfere with peristalsis and slows motility

2) Circular and longitudinal muscles

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7
Q

What toxicity does loperamide cause that can lead to death?

A

Cardiac toxicities

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8
Q

Because diphenoxylate is a synthetic opiate agonist, what was added to the drug to discourage deliberate abuse?

A

Atropine

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9
Q

Diphenoxylate exerts its effect on?

This causes?

A

1) GI smooth muscles cells

2) Inhibits GI motility and slows excess GI propulsion

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10
Q

What is the classic side effect of diphenoxylate and loperamide?

A

Anticholinergic

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11
Q

Eluxadoline is an agonist at what opioid receptors in GI?

This causes what effect?

A

1) Mu and kappa

2) Slows peristalsis/delay digestion

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12
Q

Eluxadoline is an antagonist at what opioid receptor in GI?

What does it cause?

A

1) Delta

2) Stomach, pancreas, biliary secretions decreased

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13
Q

What is the specific indication for eluxadoline?

A

Irritable Bowel Syndrome, Diarrhea-predominant subtype (IBS-D)

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14
Q

When should you discontinue eluxadoline?

What side effect of eluxadoline has caused death to occur?

A

1) Hepatic/pancreatic enzymes dramatically increase and/or severe constipation develops and lasts 4+ days
2) Pancreatitis in patients without a gallbladder

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15
Q

What are some contraindications for eleuxadoline?

A

1) Biliary duct obstruction
2) Alcoholism
3) History of pancreatitis
4) Severe hepatic impairment

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16
Q

What selectively blocks GI-based 5HT3 receptors?

A

Alosetron

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17
Q

What is alosetron indicated for?

A

Women with chronic, severe IBS-D not responsive to other conventional therapies

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18
Q

What black box warning does alosetron have?

A

Ischemic colitis

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19
Q

What drug is derived from dark red sap of Croton lechleri tree?

A

Crofelemer

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20
Q

What is the MOA of crofelemer?

A

Inhibits chloride ion secretion by blocking cAMP stimulated CFTR and calcium activated chloride channels

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21
Q

What is the indication for crofelemer?

A

Non-infectious diarrhea in HIV/AIDS patients

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22
Q

What are potential side effects of crofelemer?

A

1) Abdominal distention
2) Elevated AST/ALT/Bilirubin
3) Respiratory/Urinary infections

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23
Q

What prostaglandin inhibitor is used to treat diarrhea?

A

Bismuth

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24
Q

What opioid agonists are used to treat diarrhea?

A

1) Loperamide
2) Diphenoxylate
3) Eluxadoline

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25
Q

What serotonin (5HT3) antagonist is used to treat diarrhea?

A

Alosetron

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26
Q

What Chloride channel inhibitor is used to treat diarrhea?

A

Crofelemer

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27
Q

Hyoscyamine and dicyclomine which are used for abdominal pain belong to what class of drugs?

A

Antimuscarinic agents

28
Q

What is the MOA of the antimuscarinc agents?

A

Competitively-inhibits autonomic, postganglionic cholinergic receptors

29
Q

What are the indications for the antimuscarinic agents?

A

Abdominal pain/spasms and IBS

30
Q

What side effects are seen with the antimuscarinic agents?

A

Anticholinergic

31
Q

What classes of drugs are used to treat constipation?

A

1) Laxative and cathartic agents
2) Peripheral opioid antagonists
3) Guanylate Cyclase-C agonists
4) Selective Chloride (C2) Channel Activators

32
Q

Methylnaltrexone, Naloxegol, and Alvimopan make up what class of drugs?

A

Peripheral opioid antagonists

33
Q

Linaclotide makes up what class of drugs?

A

Guanylate Cyclase-C agonists

34
Q

Lubiprostone makes up what class of drugs?

A

Selective Chloride (C2) Channel Activators

35
Q

The peripheral opioid antagonist have actions on what receptor?

A

Mu-opioid

36
Q

Which peripheral opioid antagonist is used in the hospital only?

A

Alvimopan

37
Q

What is the indication for peripheral opioid antagonist use?

What is the specific indication for alvimopan only?

A

1) Opioid-Induced Constipation (OIC)

2) Prevention of postoperative ileus after bowel resection surgery

38
Q

What does alvimopan carry a risk for?

A

MI

39
Q

What drug increases cGMP which stimulates secretion of chloride/bicarbonate into intestinal lumen via activation of CFTR ion channel?

A

Linaclotide

40
Q

What are the indication for linaclotide?

A

1) IBS-Constipation (IBS-C)

2) Chronic Idiopathic Constipation (CIC)

41
Q

What drug is a prostaglandin-E1 (PGE-1) derivative?

A

Lubiprostone

42
Q

What are the indications for lubiprostone?

A

1) IBS-C for women
2) CIC
3) OIC

43
Q

What is the MOA of lubiprostone?

A

Increases intestinal fluid secretion by activating GI specific chloride channels (CIC-2)

44
Q

What are the peripheral Opioid Antagonists used to treat constipation?

A

1) Methylnaltrexone
2) Naloxegol
3) Alvimopan

45
Q

What is the guanylate cyclase-C agonists used to treat constipation?

A

Linaclotide

46
Q

What is the selective chloride (C2) channel activator used to treat constipation?

A

Lubiprostone

47
Q

Bisacodyl, Castor Oil, Glycerin, Senna, and sodium picosulfate make up what category of laxative and cathartic agents?

A

Stimulants

48
Q

Lactulose, Magnesium citrate, polyethylene glycol (PEG), and Sorbitol make up what category of laxative and cathartic agents?

A

Osmotics

49
Q

Magnesium hydroxide and sodium phosphate make up what category of laxative and cathartic agents?

A

Salines

50
Q

Dietary (Fiber/Bran/Fruits), Psyllium, Methylcellulose, and Calcium polycarbophil make up what category of laxative and cathartic agents?

A

Bulk forming

51
Q

Docusate and Mineral oil make up what category of laxative and cathartic agents?

A

Stool softeners

52
Q

What is the MOA of the bulk-forming/Hydrophilic colloidal agents?

What can fiber also provide support for?

How long does it usually take to take effect?

A

1) Increase bulk-volume and water content, thereby increasing GI motility
2) Supports colonic bacteria, fermentation, and digestion
3) Fast, 2-4 days

53
Q

What adverse effects are seen with Bulk-forming agents?

What is the recommendation for this?

A

1) Bloating/Obstruction

2) Drink fluids

54
Q

What are stool softeners also known as?

When is efficacy seen?

A

1) Surfactant or Emollient laxatives

2) 1-3 days

55
Q

What is the MOA of anionic surfactants?

A

Soften/lubricate feces by increasing fluid secretion into GI tract and decreasing fluid reabsorption from GI tract

56
Q

What stimulant is used for pre-colonoscopy bowel prep?

What is it metabolically converted to?

A

1) Sodium picosulfate

2) magnesium citrate

57
Q

The stimulants are irritants to enterocytes, GI smooth muscle leading to
inflammation by?

A

Na+/K+-ATPase inhibition and/or increase in prostaglandin synthesis/secretion (via cAMP/GMP)

58
Q

What do the stimulates promote?

A

Water/electrolyte accumulation in GI

59
Q

What stimulant is hydrolyzed to ricinoleic acid?

Which is a tri-hydroxyl alcohol and functions as an irritant and an osmotic lubricant agent?

A

1) Castor oil

2) Glycerin

60
Q

What is the efficacy of stimulants?

What are the contraindications?

A

1) 12-36 hours

2) GI obstruction/Ileus

61
Q

What adverse effect can stimulants cause?

Which stimulant causes urine discoloration (yellow-brown/red-pink)?

A

1) Abdominal cramping

2) Senna

62
Q

What is the MOA of the saline agents magnesium hydroxide and sodium phosphate?

A

They are hyperosmolar solutions that retain water in GI tract

63
Q

What drug interactions do saline agents have?

What should be watched carefully with these interactions?

A

1) Diuretics

2) Electrolyte balance

64
Q

When conditions should bring caution when giving saline agents?

A

1) Renal disease

2) CHF/HTN

65
Q

What osmotic agent in large doses can be used for pre-colonoscopy bowel prep?

A

Polyethylene glycol

66
Q

In general, osmotic agents provide effects in how many days with laxative doses?

What effect do larger doses have on catharsis?

A

1) 1-2 days

2) Effect occurs in hours

67
Q

Which osmotic agent can also be used for severe liver disease patients such as hyperammonemia?

A

Lactulose

GI Week 2 & 3 (9 decks)

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