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Pharmacology > GI: Diarrhea, Abdominal Pain, and Constipation > Flashcards

GI: Diarrhea, Abdominal Pain, and Constipation Flashcards

1
Q

What 5 drug classes can be sed for diarrhea?

A
  1. Prostaglandin Inhibitors
    - Bismuth
  2. Opioid Agonists
    - loperamide, diphenoxylate, eluxadoline
  3. 5HT3 antagonists
    - alosetron
  4. Cl Channel Inhibitors
    - Crofelemer
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2
Q

Does loperamide cross the BBB?

A

No, so no need to worry about addiction as much

-watch for cardiac toxicities though!

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3
Q

MOA for loperamide and diphenoxylate?

A

Interferes with peristalsis, so it slows transit time

-increases segmental peristalsis, so increases bulk

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4
Q

Side effects for Mu Opioids (loperamide and diphenoxylate)?

A

Anticholinergic (Dry as a cracker, hot as a hare, mad as a hatter, red as a beet.. you get it)

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5
Q

What is given with diphenoxylate to prevent addiction?

A

Can cross BBB, so give with small dose of atropine to avoid overdose

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6
Q

MOA for Eluxadoline?

A

Mu and Kappa agonist
-slows peristalsis

Antagonist at Delta opioid receptors
-stomach, pancreas, biliary secretions decreased

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7
Q

When would you prescribe eluxadoline?

A

IBS, diarrhea predominant

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8
Q

Side effects for Eluxadoline?

A

Hepato/pancreatotoxicity
-pancreatitis is especially high risk in those without gallbladder

CNS related
-sedation, euphoria, impaired cognition

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9
Q

If a patient doesnt have a gallbladder, what do you need to watch out for in a patient taking eluxadoline?

A

Pancreatitis

-deaths have occurred due to this

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10
Q

What are some contraindications to taking eluxadoline?

A
  1. Biliary obstruction
  2. alcoholism
  3. pancreatitis
  4. Severe hepatic impairment (liver disease, cirrhosis)
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11
Q

If a patient is taking eluxadoline and has constipation for more than 4 days, what should you do?

A

Stop the therapy!

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12
Q

What is the indication for alosetron?

A

Chronic, severe IBS-D that is unresponsive to other therapies (especially in women)

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13
Q

Say a patient has IBS-D, and has tried all other conventions to stop it and all have failed.. what would you presribe?

A

Alosetron

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14
Q

Side effects for Alosetron?

A
  1. Ischemic Colitis
    - pts must have follow up to get again, patients at significant risk!
  2. GI related
    - constipation, dyspepsia
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15
Q

Contraindications for alosetron?

A

History or current:

  • GI obstruction, perf, toxic megacolon
  • diverticulitis, Chrons, UC
  • Severe constipation
  • -STOP IMMEDIATELY
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16
Q

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

A

Crofelemer

-Cl- channel blocker

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17
Q

MOA of Crofelemer?

A

Inhibits Cl- secretion by blocking cAMP stimulated CFTR

-less Cl- means less water.. so bulks up the stool

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18
Q

If an HIV/AIDs patient comes in with diarrhea that is caused by their antiretroviral therapy what should you prescribe?

A

Crofelemer

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19
Q

Side effects for crofelemer?

A

GI issues
-abdominal distention, elevated AST/ALT

Infections
-respiratory/urinary

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20
Q

Agents used for Abdominal pain, mainly IBS related?

A

Antimuscarinic agents

  1. Hyoscamine
  2. Dicyclomine
21
Q

MOA of hyoscamine and Dicyclomine?

A

they are antimuscarinic agents, so competitively inhibit post ganglionic cholinergic receptors

22
Q

Side effects of hyoscamine and Dicyclomine?

A

They are antimuscarinic agents, so Dry as a cracker, hot as a hare, mad as a hatter, red as a beet.. you get it

23
Q

Drugs used for constipation

A
  1. Laxatives
  2. Peripheral Opioids
    - methylnaltrexone, naloxegol, alvimopan
  3. Guanylate Cyclase Agonists
    - Linaclotide
  4. Selective Cl (C2) channel activators
    - lubiprostone
24
Q

MOA of Methylnaltrexone, naloxegol, and alvimopan?

A

They are peripheral mu-opioid receptor antagonists

-so block the effects to relieve constipation

25
Q

If a patient is taking and opioid and are constipated.. what should you prescribe?

A

A mu opioid antangonist
-Methylnaltrexone, naloxegol, or alvimopan

or

Lubiprostone

26
Q

If you are wanting to accelerate GI recovery for a patient following bowel resection surgery with an anastomosis.. what would you prescribe?

A

Alvimopan

27
Q

What is a warning when taking alvimopan?

A

can cause MI

-Max of 15 doses according to REMS program

28
Q

MOA for LIncaclotide?

A

Activates guanylate cyclase-c for constipation

-stimulates CFTR ion channel, more Cl- in lumen, water will follow to relieve constipation

29
Q

When would you prescribe lincaclotide?

A
  1. IBS-C

2. Chronic Idiopathic Constipation

30
Q

MOA of lubiprostone?

A

A prostaglindin E derivative for constipation
-activates ClC-2 channels, Cl- out and water will follow to relieve constipation

First three letters are Lub(e), so it helps things slide out

31
Q

Indications for Lubiprostone?

A
  1. IBS-C (women)
  2. Chronic Idiopathic Constipation
  3. Opoid induced constipation
32
Q

What are the bulk forming agents used in diarrhea?

A

Fiber/Bran
Psyllium
Cellulose agents
Calcium Polcarbophil

33
Q

Adverse effects of bulk forming agents?

A

Bloating and obstruction
-must drink lots of water

Also interactions with drugs!

34
Q

What agents are used as stool softeners? how do they work?

A
  1. Docusate salts
  2. Mineral Oil

Work to lubricate feces and decrease fluid resorption from GI tract

35
Q

Which agents are used as stimulants (irritants) for laxatives?

A 
Senna
Bisacodyl
Castor Oil
Glycerin
Sodium Picosulfate
36
Q

Which stimulate is used for pre-colonoscopy bowel prep?

A

Sodium picosulfate

37
Q

MOA of stimulants?

A
  1. Irritate the enterocytes, leads to inflammation
    - causes Na/K inhibition and can increase prostaglindin synthesis
  2. Promote water/electorlyte accumulation in GI
38
Q

What is castor oil hydrolyzed to?

A

ricinoleic acid

39
Q

Which of the stimulates acts as a tri-hydroxyl alcohol and functions as an irritant, osmotic agent, and lubricant?

A

Glycerin

40
Q

When is the effect of stimulants noticed?

A

12-36 hours

41
Q

Which stimulant can cause red/brown urine?

A

Senna

42
Q

What are the two saline agents used as laxatives?

A
  1. Magnesium salts (mag. sulfate, mag. hydroxide)

2. Sodium Phosphate

43
Q

How do the saline agents work?

A

Magnesium/phosphate is poorly absorbed, so created a hyperosmolar solution to retain water in GI tract

44
Q

What drugs do saline agents interact with?

A

diuretics

45
Q

What are the contraindications in someone taking a saline agent as a laxative?

A 
Renal Disease (electrolytes)
CHF/HTN
46
Q

What are the osmotic agents used as a laxative?

A

lactulose
Magnesium Citrate
Sorbitol
Polyethylene Glycol

Effects seen in 1-3 hours in large doses

47
Q

What can lactulose be used for besides as a laxative?

A

Severe liver disease (Hepatic Encephalopathy) causing hyperammonemia, as it changes pH to trap ammonia in GI

48
Q

What are the adverse effects of osmotic agents?

A

Can cause severe dehydration fro electrolyte disturbances

-so watch at risk populations!

49
Q

Which osmotic agents is used in large doses for bowel prep?

A

Polyethylene glycol

-smaller doses for constipation

Pharmacology (50 decks)

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