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GI II - Weeks 2/3 > Drugs for Diarrhea, Abdominal Pain, & Constipation (Segars) > Flashcards

Drugs for Diarrhea, Abdominal Pain, & Constipation (Segars) Flashcards

1
Q

What are the main families of drugs for treatment of diarrhea?

A
    • Prostaglandin Inhibitors
    • Opioid Agonists
    • Serotonin (5-HT3) Antagonists
    • Chloride Channel Inhibitors
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2
Q

What drugs are Opioid Agonists (Anti-propulsives)?

A
    • Loperamide
    • Diphenoxylate
    • Eluxadoline
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3
Q

This Opioid Agonist is chemically-related to opioids but does NOT exhibit analgesic/opiate-like effects, or appear to produce physical dependence.

A

Loperamide

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4
Q

Loperamide does have an FDA-issued drug safety communication, which is it can cause ________ toxicities leading to death.

A

Cardiac

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5
Q

What is the mechanism of action for Loperamide?

A

Directly acts on circular and longitudinal muscles of intestinal wall, which interferes with peristalsis and slows motility

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6
Q

What are the side effects of Loperamide?

A

Classic anticholinergic effects

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7
Q

This Opioid Agonist is a synthetic opiate agonist, and is much more closely related to them. Opioid effects are only seen at very high doses.

A

Diphenoxylate

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8
Q

For Diphenoxylate, a small quantity of ________ is added to discourage deliberate abuse or over-dosage.

A

Atropine

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9
Q

What is the mechanism of action for Diphenoxylate?

A

– Exerts effects locally and centrally on GI smooth muscle cells.

– Inhibits GI motility and slows excess GI propulsion.

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10
Q

What are the side effects of Diphenoxylate?

A

Classic anticholinergic effects

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11
Q

This Opioid Agonist acts as an agonist at mu and kappa receptors in GI, resulting in slowed peristalsis and delays digestion.

A

Eluxadoline

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12
Q

This Opioid Agonist acts as an antagonist at delta opioid receptors in GI, resulting in decreased secretions in the stomach, pancreas, and biliary tract.

A

Eluxadoline

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13
Q

Eluxadoline is not for any and all patients with diarrhea, it’s specific for…

A

IBS-D

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14
Q

What is it very important to watch while a patient is on Eluxadoline?

A

Watch hepatic and liver enzymes!

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15
Q

Eluxadoline can cause hepatic and pancreatic toxicity due to increased enzymes. Pancreatitis is also a high-risk in patients without a _________. Deaths have occurred due to this (FDA warning).

A

Gallbladder

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16
Q

What are the CNS side effects related to Eluxadoline?

A
    • Sedation
    • Euphoria
    • Impaired cognition
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17
Q

What are the contraindications for use of Eluxadoline?

A
    • Biliary duct obstruction
    • Alcoholism
    • Hx of pancreatitis
    • Severe hepatic impairment
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18
Q

Eluxadoline therapy should be stopped if severe __________ develops and lasts 4+ days.

A

Constipation

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19
Q

What is the Serotonin (5-HT3) Antagonist specific for the use of diarrhea?

A

Alosetron

***Remember, Serotonin Antagonists end in -setron!

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20
Q

Alosetron is not very commonly used on the market, but it works by selectively blocking GI-based _______ receptors. This antagonism modulates regulation of visceral pain, colonic transit, and GI secretions.

A

5-HT3

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21
Q

This medication is used for chronic, severe IBS-D that is not responsive to other conventional therapies. Commonly used in women.

A

Alosetron

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22
Q

Severe Diarrhea-predominant IBS includes diarrhea, and one or more of the following…

A
    • Frequent/severe abdominal pain
    • Frequent bowel urgency or fecal incontinence
    • Restriction of daily activities due to IBS

***Anatomical or biochemical GI abnormalities must be excluded before prescribing!

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23
Q

The major side effect of Alosetron is a black box warning for…

A

Ischemic Colitis

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24
Q

Due to the black box warning of ischemic colitis for the medication Alosetron, what are the requirements for its use?

A

– 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 is required

– No refills without a follow-up exam by the prescriber

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25
Q

While on Alosetron, if a patient develops severe _________ the physician must D/C its use immediately.

A

Constipation

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26
Q

What is the drug that is a Prostaglandin Inhibitor and used to treat diarrhea?

A

Bismuth

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27
Q

What is the drug that is a Chloride Channel Inhibitor and used for treatment of diarrhea?

A

Crofelemer

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28
Q

This drug is derived from the dark red sap of the Croton lechleri tree (botanical pharmaceutical).

A

Crofelemer

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29
Q

What is the mechanism of action for Crofelemer?

A

Inhibits chloride ion secretion by blocking cAMP-stimulated CFTR and calcium-activated chloride channels (CaCC).

***These channels regulate fluid secretion by intestinal epithelial cells. Can also be a treatment for cholera!

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30
Q

This medication is used for non-infectious diarrhea in HIV/AIDS pts (for pts on anti-retroviral therapy).

A

Crofelemer

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31
Q

What are the side effects for Crofelemer?

A

– GI-related = Abdominal distention, elevated AST/ALT/Bilirubin

– Infections = Respiratory/Urinary

32
Q

What is the drug family and drugs used for abdominal pain/spasms?

A

Antimuscarinic Agents –

    • Hyoscyamine
    • Dicyclomine
33
Q

What is the mechanism of action for Antimuscarinics?

A

Competitively-inhibit autonomic, post-ganglionic cholinergic receptors

34
Q

What are the side effects of Antimuscarinics?

A

Classic anticholinergic effects

35
Q

What are the drug families used to treat constipation?

A
    • Laxative and Cathartic Agents
    • Peripheral Opioid Antagonists
    • Guanylate Cyclase-C Agonists
    • Selective Chloride (C2) Channel Activators
36
Q

What drugs are Peripheral Opioid Antagonists?

A
    • Methylnaltrexone
    • Naloxegol
    • Alvimopan
37
Q

What is the mechanism of action for Peripheral Opioid Antagonists?

A

Peripheral mu-opioid receptor antagonists

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

38
Q

These drugs are used only for Opioid-Induced Constipation (OIC).

A

Methylnaltrexone

Naloxegol

39
Q

This drug is used for constipation only in a hospital setting. It is only for accelerating time to GI recovery following bowel resection surgery with primary anastomosis (prevention of postoperative ileus).

A

Alvimopan

40
Q

Alvimopan carries a risk of _______ with use, so ______ program requires use only in approved institutions for a maximum of 15 doses.

A

MI

REMS

41
Q

This drug works by binding to GC-C on luminal surface of intestinal epithelium and increases intracellular/extracellular concentrations of cGMP. It is a GC-C Agonist, used for constipation.

A

Linaclotide

42
Q

Via its mechanism of action, Linaclotide stimulates secretion of ________ and ________ into the intestinal lumen via activation of the CFTR ion channel.

A

Chloride

Bicarbonate

43
Q

For what types of constipation is Linaclotide used?

A
    • IBS-C

- - CIC (Chronic Idiopathic Constipation)

44
Q

This drug is a prostaglandin-E1 (PGE-1) derivative, and works by increasing intestinal fluid secretions by activating GI-specific chloride channels (ClC-2) in luminal cells of intestinal epithelium. Used for constipation.

A

Lubiprostone

45
Q

For what types of constipation is Lubiprostone used?

A
    • IBS-C in women
    • CIC (Chronic Idiopathic Constipation)
    • OIC (Opioid-Induced Constipation)
46
Q

This is the only drug for constipation that has CNS-related side effects.

A

Lubiprostone

47
Q

What are the categories for Laxative and Cathartic Agents?

A
    • Stimulants
    • Osmotics
    • Salines
    • Bulk Forming
    • Stool Softeners
48
Q

What are the bulk forming/hydrophilic colloidal agents?

A
    • Fiber/Bran (dietary)
    • Psyllium
    • Methylcellulose/Carboxymethylcellulose
    • Calcium Polycarbophil
49
Q

Bulk forming/hydrophilic colloidal agents work to increase bulk-volume and water content, thereby increasing GI motility. _______ can also support colonic bacteria, fermentation, and digestion. Efficacy is seen in 2-4+ days.

A

Fiber

50
Q

Bulk-forming/Hydrophilic colloidal agents can have adverse effects of bloating and obstruction, so it is important to…

A

Drink fluids – but have caution in renal failure!

51
Q

Stool softeners are also known as _________ or ________ laxatives.

A

Surfactant

Emollient

52
Q

What are the types of Stool softeners?

A
    • Docusate ‘salts’
    • Mineral Oil
    • Anionic surfactants
53
Q

Anionic surfactants (stool softener) work by softening and lubricating the feces. It (INCREASES/DECREASES) fluid secretion into the GI tract and (INCREASES/DECREASES) fluid reabsorption from the GI tract.

A

Increases

Decreases

54
Q

Mineral Oil ________ stool to soften.

A

Penetrates

55
Q

Stool softeners are effective in 1-3+ days and have a ________ laxative effect.

A

Minimal

56
Q

What are Stimulants (Irritants)?

A
    • Senna
    • Bisacodyl
    • Castor Oil
    • Glycerin
    • Sodium Picosulfate
57
Q

This Stimulant (Irritant) contains magnesium oxide/anhydrous citric acid, which is metabolically converted to magnesium citrate (osmotic). It is used to clean out the GI tract for pre-colonoscopy bowel prep.

A

Sodium Picosulfate

58
Q

How do Stimulants (Irritants) work?

A

They stimulate peristalsis by irritating enterocytes and GI smooth muscle leading to inflammation. This causes Na/K-ATPase inhibition and/or increase in prostaglandin synthesis and secretion (via cAMP/GMP).

59
Q

T/F. Stimulants (Irritants) promote water and electrolyte accumulation in the GI.

A

True

60
Q

This Stimulant (Irritant) is hydrolyzed to Ricinoleic Acid.

A

Castor Oil

61
Q

This Stimulant (Irritant) is a tri-hydroxyl alcohol and functions as an irritant, osmotic, and lubricant agent.

A

Glycerin

62
Q

The efficacy of Stimulants (Irritants) from usual laxative doses is usually seen in 12-36 hours. Its adverse effects include…

A
    • Abdominal cramping
    • Urine discoloration
    • Fluid/electrolyte disturbances (from long use)
63
Q

This is a particular Stimulant that causes the urine discoloration.

A

Senna

64
Q

What are contraindications for the use of Stimulants (Irritants)?

A
    • GI Obstruction
    • Ileus
    • Impaction
65
Q

What are the Saline Agents that are used as laxatives?

A
    • Magnesium salts (Mag. Sulfate, Mag. Hydroxide)

- - Sodium phosphate

66
Q

How do Saline Agents work?

A

Magnesium and Phosphate ions are poorly absorbed, and because they are hyperosmolar solutions they will osmotically retain water in the GI tract, flushing it out.

67
Q

(SMALLER/GREATER) volume of Saline Agents shortens the transit time.

A

Greater

***ie, this is why you take a full bottle of mag. citrate!

68
Q

What drug interactions do you have to be careful with for Saline Agents?

A

Diuretics (electrolyte imbalance)

69
Q

What things do you have to take caution of when giving Saline Agents?

A
    • Renal disease (electrolytes)

- - CHF/HTN (sodium)

70
Q

What are the Osmotic Agents used as laxatives?

A
    • Lactulose
    • Magnesium Citrate
    • Sorbitol
    • Polyethylene glycol (PEG-3350)
71
Q

What is the difference in effect between a small and large dose of Polyethylene glycol?

A

Small doses = Used for constipation

Large doses = Used for bowel prep prior to GI scopes, radiological procedures, or surgery

72
Q

How do Osmotic Agents work?

A

Osmotically attract and retain increased water in colon, increasing moisture, softness, and volume/bulk.

73
Q

In general, _______ _______ provide effects in 1-2+ days with laxative doses, while larger doses may provide catharsis sooner (hours).

A

Osmotic Agents

74
Q

This Osmotic Agent is used for severe liver disease patients with hyperammonemia. The change in pH traps the ammonia in the GI.

A

Lactulose

75
Q

An adverse effect of Lactulose is _______ _______ and must be closely watched in at-risk patient populations.

A

Electrolyte disturbances

GI II - Weeks 2/3 (6 decks)

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