Pharm - Tx for Diarrhea, Abd Pain & Constipation Flashcards

1
Q

what are the 4 drug families used for diarrhea?

A

prostaglandin inhibitors
opioid agonists
5HT3 antagonists
chloride channel inhibitors

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2
Q

loperamine
diphenoxylate
eluxadoline

A

opioid agonists

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3
Q

alosetron

A

5HT3 antagonist

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4
Q

crofelemer

A

chloride channel inhibitor

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5
Q

this drug interferes with peristalsis (slows transit time)
- direct action on circular and longitudinal muscles of intestinal wall, slowing motility -> allowing for fluid/electrolyte reabsorption and increasing bulk/density of feces

A

loperamide (anti-propulsive)

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6
Q

what are the side effects of loperamide?

A

dizziness, fatigue, drowsiness and urinary retention

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7
Q

this synthetic opiate agonist, has a small quantity of atropine added to discourage deliberate abuse/over-dosage
- believed to exert effect locally & centrally on GI smooth muscle cells, inhibits GI motility and slows excess GI propulsion

A

diphenoxylate

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8
Q

the drug is an AGONIST at mu & kappa opioid receptors in GI tract
- also an ANTAGONIST at delta opioid receptors in GI (decreases stomach, pancreas & biliary tract secretions)

A

eluxadoline

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9
Q

what drug is indicated for IBS-D (diarrhea-predominant subtype)

A

eluxadoline

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10
Q

what are the side effects of eluxadoline?

A
  • GI: N/V/abd pain
  • hepatic/pancreatic toxicity -> pancreatitis high-risk in patients without a gallbladder!!
  • CNS: dizziness, sedation, euphoria, impaired cognition
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11
Q

what are the contraindications for eluxadoline?

A
  • biliary duct obstruction
  • alcoholism
  • history of pancreatitis
  • severe hepatic impairment

NOTE: stop therapy iF severe constipation develops and lasts >4 days

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12
Q

this drug selectively blocks GI-based 5HT3 receptors, but is NOT indicated for N/V
- antagonism in GI modulates the regulation of pain, colonic transit and GI secretions

A

alosetron

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13
Q

what drug is indicated for chronic, severe IBS-D in women, who are not responsive to conventional therapies

A

alosetron

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14
Q

what constitutes chronic, severe IBS-D?

A

diarrhea, and one or more of the following:

  • frequent/severe abdominal pain
  • frequent bowel urgency or fecal incontinence
  • restriction of daily activities due to IBS
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15
Q

what are the side effects of alosetron?

A
  • constipation, dyspepsia, GERD, N/V

* *ischemic colitis** -> black box warning!!

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16
Q

this drug is derived from dark red sap of Croton lechleri tree
- it inhibits chloride ion secretion by blocking cAMP-stimulated CFTR and calcium-activated chloride channels

A

crofelemer

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17
Q

what drug is ONLY indicated for HIV/AIDS patients, who are on retroviral therapy, and have chronic diarrhea that has been confirmed as non-infectious

A

crofelemer

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18
Q

what are the side effects of crofelemer?

A
  • GI: abdominal distention, elevated AST/ALT/bilirubin

- respiratory/urinary tract infections

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19
Q

what drug family is used to treat abdominal pain/spasms?

A

antimuscarinic agents

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20
Q

hyoscyamine
dicyclomine
clidinium/chlordiazepoxide

A

antimuscarinic agents

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21
Q

these drugs competitively inhibit autonomic, post-ganglionic cholinergic receptors
- causes decreased GI motility and spasms

A

antimuscarinics

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22
Q

what are the side effects of antimuscarinics?

A

classic anticholinergic effects!

  • dry mouth
  • urinary retention
  • constipation
  • drowsiness
  • mental confusion
  • blurred vision
23
Q

what drug families are used to treat constipation?

A
  • peripheral opioid antagonists
  • Guanylate Cyclase-c (GC-c) agonists
  • selective chloride (C2) channel activators
  • laxative and cathartic agents
24
Q
  • *this drug binds GC-c on luminal surface of intestinal epithelium and increases intracellular/extracellular concentrations of cGMP**
  • stimulates secretion of chloride/bicarb into intestinal lumen via activation of CFTR ion channel (trying to bring moisture into lumen -> accelerating transit)
A

linaclotide

25
Q

what drug is indicated in IBS-C, and chronic idiopathic constipation (CIC)?

A

linaclotide

26
Q

what are the side effects of linaclotide?

A
  • GI: diarrhea (dehydration, electrolyte imbalance)

- GERD, dyspepsia, N/V

27
Q

the drug is a PGR-1 derivative
- it increases intestinal fliud secretion by activating GI-specific cloride channels (CIC-2) in luminal cells of intestinal epithelium

A

lubiprostone

28
Q

what drug is indicated for women with IBS-C, chronic idiopathic constipation (CIC), and opioid-induced constipation (OIC)?

A

lubiprostone

This med is a great choice for cancer pts and people with chronic pain who can’t stop opioids!

29
Q

what are the side effects of lubiprostone?

A

nausea, dyspepsia, dizziness

30
Q

what drug is a peripheral mu-opioid receptor antagonist?

- no common, significant CNS penetrations/actions or induction of withdrawal/pain symptoms

A

methylnaltrexone (alvimopan)

31
Q

what drug is used only for accelerating time to GI recovery following bowel resection surgery with primary anastomosis (prevention of post-op ileus)

A

alvimopan

-hospital use ONLY

32
Q

what are the side effects of methylnaltrexone?

A

abd pain, diarrhea, nausea, vomiting

33
Q

why does alvimopan have a black box warning?

A

it carries a risk of MI with use

-REMS program requires use only in approved institutions, for max of 15 doses!

34
Q

what are the 5 classes of laxatives and cathartic agents?

A
  • stimulants
  • osmotics
  • salines
  • bulk forming
  • stool softeners
35
Q
bisacodyl
castor oil
glycerin
senna
Na picosulfate
A

stimulants

36
Q

lactulose
Mg citrate
polyethylene glycol (PEG)
sorbitol (glycerin)

A

osmotics

37
Q

Mg hydroxide

Na phosphate

A

salines

38
Q
dietary fiber
psyllium
methylcellulose
carboxymethylcellulose
calcium polycarbophil
A

bulk forming

  • efficacy seen in 2-4 days
  • LOTs of drug interactions (mainly with psyllium and the celluloses)
  • cause bloating/obstruction
39
Q

docusate “salts”

mineral oil -> penetrates stool

A

stool softeners

  • aka surfactant or emollient
  • efficacy seen in 1-3 days
40
Q

these agents soften/lubricate feces by:

  • increasing fluid secretion into GI tract
  • inhibit water reabsorption from GI tract
A

stool softeners

41
Q

what drug is given for pre-colonoscopy bowel prep?

  • aggressive, works very well!
  • has magnesium oxide/anhydrous citric acid -> metabolically converted to magnesium citrate (osmotic)
A

sodium picosulfate

42
Q

these agents are irritating to enterocytes, GI smooth muscle leading to inflammation

  • Na/K-ATPase inhibition and/or increase in PGE synthesis via cAMP/GMP
  • promote water/electrolyte accumulation in GI
A

stimulants (irritants)

- efficacy seen in 12-36 hours (sooner with glycerin)

43
Q

what is castor oil hydrolyzed to?

A

ricinoleic acid

44
Q

what are the adverse effects of stimulants?

A
  • abd cramping
  • urine discoloration -> yellow-brown/red-pink (senna)
  • fluid electrolyte disturbances

NOTE: make sure pt has ACTIVE bowels (is not constipated/impacted) before giving stimulant! can make the obstruction worse

45
Q

what are the contraindications for stimulants?

A

GI obstruction/ileus/impaction

46
Q

Mg sulfate
Mg hydroxide
Na phosphate

A

saline agents

  • Mg/Phos ions are poorly absorbed
  • osmotically retain wter in GI tract
47
Q

what is the main drug interaction of saline agents?

A

electrolyte balance (diuretics)

48
Q

what are cautions to be aware of while using saline agents?

A
  • renal disease (electrolytes)

- CHF/HTN (sodium)

49
Q

lactulose
Mg citrate
Sorbitol
**Polyethylene glycol* -> large quantities can have sam rxn as Na picosulfate

A

osmotic agents

50
Q

these agents work to osmotically attract and retain increased water in the colon, thereby increasin moisture, softness and volume/bulk
- provide effects in 1-2 days with laxative doses (larger doses may provide catharsis sooner

A

osmotic agents

51
Q

what is lactulose also used to treat?

A

severe liver disease (hyperammonemia)

- change in pH traps ammonia in GI

52
Q

what are the adverse effects of osmotic agents?

A
  • electrolyte disturbances -> watch closely!

- GI-related

53
Q

large doses of this osmotic agent are used for bowel prep prior to GI scopes, radiological procedures, or surgery (fast acting 1-3 hours!)
- smaller doses can be used for constipation (can take a few days)

A

polyethylene glycol