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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
While on Alosetron, if a patient develops severe _________ the physician must D/C its use immediately.
Constipation
26
What is the drug that is a Prostaglandin Inhibitor and used to treat diarrhea?
Bismuth
27
What is the drug that is a Chloride Channel Inhibitor and used for treatment of diarrhea?
Crofelemer
28
This drug is derived from the dark red sap of the Croton lechleri tree (botanical pharmaceutical).
Crofelemer
29
What is the mechanism of action for Crofelemer?
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!
30
This medication is used for non-infectious diarrhea in HIV/AIDS pts (for pts on anti-retroviral therapy).
Crofelemer
31
What are the side effects for Crofelemer?
-- GI-related = Abdominal distention, elevated AST/ALT/Bilirubin -- Infections = Respiratory/Urinary
32
What is the drug family and drugs used for abdominal pain/spasms?
Antimuscarinic Agents -- - - Hyoscyamine - - Dicyclomine
33
What is the mechanism of action for Antimuscarinics?
Competitively-inhibit autonomic, post-ganglionic cholinergic receptors
34
What are the side effects of Antimuscarinics?
Classic anticholinergic effects
35
What are the drug families used to treat constipation?
- - Laxative and Cathartic Agents - - Peripheral Opioid Antagonists - - Guanylate Cyclase-C Agonists - - Selective Chloride (C2) Channel Activators
36
What drugs are Peripheral Opioid Antagonists?
- - Methylnaltrexone - - Naloxegol - - Alvimopan
37
What is the mechanism of action for Peripheral Opioid Antagonists?
Peripheral mu-opioid receptor antagonists ***No common, significant CNS actions nor induction of withdrawal/pain symptoms!
38
These drugs are used only for Opioid-Induced Constipation (OIC).
Methylnaltrexone | Naloxegol
39
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).
Alvimopan
40
Alvimopan carries a risk of _______ with use, so ______ program requires use only in approved institutions for a maximum of 15 doses.
MI | REMS
41
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.
Linaclotide
42
Via its mechanism of action, Linaclotide stimulates secretion of ________ and ________ into the intestinal lumen via activation of the CFTR ion channel.
Chloride | Bicarbonate
43
For what types of constipation is Linaclotide used?
- - IBS-C | - - CIC (Chronic Idiopathic Constipation)
44
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.
Lubiprostone
45
For what types of constipation is Lubiprostone used?
- - IBS-C in women - - CIC (Chronic Idiopathic Constipation) - - OIC (Opioid-Induced Constipation)
46
This is the only drug for constipation that has CNS-related side effects.
Lubiprostone
47
What are the categories for Laxative and Cathartic Agents?
- - Stimulants - - Osmotics - - Salines - - Bulk Forming - - Stool Softeners
48
What are the bulk forming/hydrophilic colloidal agents?
- - Fiber/Bran (dietary) - - Psyllium - - Methylcellulose/Carboxymethylcellulose - - Calcium Polycarbophil
49
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.
Fiber
50
Bulk-forming/Hydrophilic colloidal agents can have adverse effects of bloating and obstruction, so it is important to...
Drink fluids -- but have caution in renal failure!
51
Stool softeners are also known as _________ or ________ laxatives.
Surfactant | Emollient
52
What are the types of Stool softeners?
- - Docusate 'salts' - - Mineral Oil - - Anionic surfactants
53
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.
Increases | Decreases
54
Mineral Oil ________ stool to soften.
Penetrates
55
Stool softeners are effective in 1-3+ days and have a ________ laxative effect.
Minimal
56
What are Stimulants (Irritants)?
- - Senna - - Bisacodyl - - Castor Oil - - Glycerin - - Sodium Picosulfate
57
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.
Sodium Picosulfate
58
How do Stimulants (Irritants) work?
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
T/F. Stimulants (Irritants) promote water and electrolyte accumulation in the GI.
True
60
This Stimulant (Irritant) is hydrolyzed to Ricinoleic Acid.
Castor Oil
61
This Stimulant (Irritant) is a tri-hydroxyl alcohol and functions as an irritant, osmotic, and lubricant agent.
Glycerin
62
The efficacy of Stimulants (Irritants) from usual laxative doses is usually seen in 12-36 hours. Its adverse effects include...
- - Abdominal cramping - - Urine discoloration - - Fluid/electrolyte disturbances (from long use)
63
This is a particular Stimulant that causes the urine discoloration.
Senna
64
What are contraindications for the use of Stimulants (Irritants)?
- - GI Obstruction - - Ileus - - Impaction
65
What are the Saline Agents that are used as laxatives?
- - Magnesium salts (Mag. Sulfate, Mag. Hydroxide) | - - Sodium phosphate
66
How do Saline Agents work?
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
(SMALLER/GREATER) volume of Saline Agents shortens the transit time.
Greater ***ie, this is why you take a full bottle of mag. citrate!
68
What drug interactions do you have to be careful with for Saline Agents?
Diuretics (electrolyte imbalance)
69
What things do you have to take caution of when giving Saline Agents?
- - Renal disease (electrolytes) | - - CHF/HTN (sodium)
70
What are the Osmotic Agents used as laxatives?
- - Lactulose - - Magnesium Citrate - - Sorbitol - - Polyethylene glycol (PEG-3350)
71
What is the difference in effect between a small and large dose of Polyethylene glycol?
Small doses = Used for constipation Large doses = Used for bowel prep prior to GI scopes, radiological procedures, or surgery
72
How do Osmotic Agents work?
Osmotically attract and retain increased water in colon, increasing moisture, softness, and volume/bulk.
73
In general, _______ _______ provide effects in 1-2+ days with laxative doses, while larger doses may provide catharsis sooner (hours).
Osmotic Agents
74
This Osmotic Agent is used for severe liver disease patients with hyperammonemia. The change in pH traps the ammonia in the GI.
Lactulose
75
An adverse effect of Lactulose is _______ _______ and must be closely watched in at-risk patient populations.
Electrolyte disturbances

GI II - Weeks 2/3 (6 decks)

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