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
what drug is indicated in IBS-C, and chronic idiopathic constipation (CIC)?
linaclotide
26
what are the side effects of linaclotide?
- GI: diarrhea (dehydration, electrolyte imbalance) | - GERD, dyspepsia, N/V
27
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
lubiprostone
28
what drug is indicated for women with IBS-C, chronic idiopathic constipation (CIC), and **opioid-induced constipation (OIC)**?
lubiprostone This med is a great choice for cancer pts and people with chronic pain who can't stop opioids!
29
what are the side effects of lubiprostone?
nausea, dyspepsia, dizziness
30
what drug is a peripheral mu-opioid receptor antagonist? | - no common, significant CNS penetrations/actions or induction of withdrawal/pain symptoms
methylnaltrexone (alvimopan)
31
what drug is used only for accelerating time to GI recovery following bowel resection surgery with primary anastomosis (prevention of post-op ileus)
alvimopan | -**hospital use ONLY**
32
what are the side effects of methylnaltrexone?
abd pain, diarrhea, nausea, vomiting
33
why does alvimopan have a black box warning?
it carries a risk of MI with use | -REMS program requires use only in approved institutions, for max of 15 doses!
34
what are the 5 classes of laxatives and cathartic agents?
- stimulants - osmotics - salines - bulk forming - stool softeners
35
``` bisacodyl castor oil glycerin senna Na picosulfate ```
stimulants
36
lactulose Mg citrate polyethylene glycol (PEG) sorbitol (glycerin)
osmotics
37
Mg hydroxide | Na phosphate
salines
38
``` dietary fiber psyllium methylcellulose carboxymethylcellulose calcium polycarbophil ```
bulk forming - **efficacy seen in 2-4 days** - LOTs of drug interactions (mainly with psyllium and the celluloses) - cause bloating/obstruction
39
docusate "salts" | mineral oil -> penetrates stool
stool softeners - aka surfactant or emollient - **efficacy seen in 1-3 days**
40
these agents soften/lubricate feces by: - increasing fluid secretion into GI tract - inhibit water reabsorption from GI tract
stool softeners
41
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)
**sodium picosulfate**
42
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
stimulants (irritants) | - **efficacy seen in 12-36 hours** (sooner with glycerin)
43
what is castor oil hydrolyzed to?
ricinoleic acid
44
what are the adverse effects of stimulants?
- 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
what are the contraindications for stimulants?
GI obstruction/ileus/impaction
46
Mg sulfate Mg hydroxide Na phosphate
saline agents - Mg/Phos ions are poorly absorbed - osmotically retain wter in GI tract
47
what is the main drug interaction of saline agents?
electrolyte balance (diuretics)
48
what are cautions to be aware of while using saline agents?
- renal disease (electrolytes) | - CHF/HTN (sodium)
49
lactulose Mg citrate Sorbitol **Polyethylene glycol* -> large quantities can have sam rxn as Na picosulfate
osmotic agents
50
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
osmotic agents
51
what is lactulose also used to treat?
severe liver disease (*hyperammonemia*) | - change in pH traps ammonia in GI
52
what are the adverse effects of osmotic agents?
- electrolyte disturbances -> watch closely! | - GI-related
53
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)
polyethylene glycol