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GI > Drugs for D, AP, C > Flashcards

Drugs for D, AP, C Flashcards

1
Q

What are Loperamide, Diphenoxylate and Eluxadoline?

A

opioid agonists

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2
Q

What are Loperamide, Diphenoxylate and Eluxadoline used to treat?

A

diarrhea

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3
Q

What is Alosetron?

A

Serotonin (5HT3) antagonist

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4
Q

What is Alosetron used for?

A

IBS-D in women

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5
Q

What is Crofelemer?

A

Chloride channel inhibitor

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6
Q

What is Crofelemer used for?

A

HIV/AIDS diarrhea

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7
Q

What is Bismuth?

A

Prostaglandin inhibitor

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8
Q

What is Bismuth used for?

A

diarrhea

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9
Q

What are Hyoscyamine and Dicyclomine?

A

antimuscarinic agents

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10
Q

What are Methylnaltrexone, Naloxegol and Alvimopan?

A

Peripheral opioid antagonists

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11
Q

What is Linaclotide?

A

Guanylate Cyclase-C Agonist

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12
Q

What is Lubiprostone?

A

Selective chloride (C2) channel activator

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13
Q

Describe uses for bismuth

A

AKA pepto-bismol

  • heartburn/indigestion
  • H pylori (quadruple regimen) - -diarrhea via inhibiting prostaglandins–> decreases secretions in GI tract
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14
Q

What opioid agonist does not exhibit analgesic effects, physical dependence and is an anti-propulsive?

A

Loperamide (imodium)

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15
Q

Describe MOA of loperamide

A

slows transit time (interferes with peristalsis)
–> gives time to absorb fluid and electrolytes

direct action on circular and longitudinal muscles

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16
Q

What can occur with abuse of Loperamide?

A

cardiac toxicity

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17
Q

Side effect of Loepramide

A

anticholinergic

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18
Q

What is a synthetic opioid agoinst used for diarrhea?

A

Diphenoxylate (lomotil)

–>more readily abused c/t loperamide

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19
Q

What is added to Diphenoxylate to discourage abuse?

A

atropine

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20
Q

Side effect of diphenoxylate

A

anticholinergic (atropine)

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21
Q

MOA of diphenoxylate

A

local and central effects of GI smooth muscle cells

inhibits GI motility, slows excess propulsion

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22
Q

What drug is an agonist at mu and kappa receptors in GI and antagonist at delta receptors in GI?

A

eluxadoline

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23
Q

MOA of Eluxadoline

A

mu and kappa agonist: slows peristalsis and delays digestion

antagonist at delta receptor: decreased secretions from stomach, pancreas, biliary

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24
Q

When to use Eluxadoline (specifically)?

A

IBS-D

diarrhea-predominant subtype

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25
Q

Side effects of Eluxadoline

A

Hepatic/Pancreatic toxicity
–> high risk for pancreatitis in patients without gallbladder (can cause deaths)

some CNS

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26
Q

Eluxadoline Contradindications

A

biliary duct obstruction
alcoholism
Hx pancreatitis
severe hepatic impairment

STOP if severe constipation develops and last more than 4 days

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27
Q

MOA of Alosetron

A

selectively blocks GI-based serotonin (3) receptors

–>modulates visceral pain, colonic transit, GI secretions

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28
Q

Indications for Alosetron

A

chronic IBS-D not responsive to other therapy (only in women)

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29
Q

Side effects of Alosetron

A

GI-related
Ischemic Colitis
–> need enroll, sign, self-training, no refills w/o f/u

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30
Q

Contraindications of Alosetron

A

History or Current:
-GI obstruction, perf, stricture, adhesion, toxic megacolon

  • diverticulitis, crohn disease, ulcerative colitis
  • impaired circulation in intestines
  • severe constipation (d/c immediately)
31
Q

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

A

Crofelemer (chloride inhibitor)

32
Q

MOA of Crofelemer

A

inhibits choride ion secretion via blocking cAMP CFTR and CaCC channels

(normal fxn is to regulate fluid secretion by intestinal epithelial cells)

33
Q

Indication for Crofelemer

A

non-infectious diarrhea in HIV/AIDS

34
Q

Side effects of Crofelemer

A

GI (elevated AST, ALT, bili)

Infections (Resp/Urinary)

35
Q

When to use Hyoscyamine and Dicyclomine?

A

abdominal pain/spasms (as in IBS)

–>antimuscarinics

36
Q

MOA of antimuscarinics

A

competitively inhibits post-gang cholinergic receptors at multiple sites

37
Q

Side effects of antimuscarinics

A

classic anticholinergic

38
Q

What to use Lubiprostone for

A

constipation

selective chloride (c2) activator

39
Q

What to use Linaclotide for

A

Constipation

guanylate cyclase-c agonist

40
Q

What to use peripheral opioid antagonists for

A

constipation

41
Q

What to use laxative and cathartic agents for

A

constipation

42
Q

What is the only class that is used exclusively for abdominal pain?

A

antimuscarinics

–> Hyoscyamine
Dicyclomine

43
Q

MOA of peripheral opidoid antagonists

A

antagonize mu receptors without CNS action or induction of withdrawal sx

44
Q

Which peripheral opioid antagonist is hospital use only?

A

alvimopan

45
Q

When to use peripheral opioid antagonists

A

opioid-induced constipation

46
Q

What drug is used only for accelerating time to GI recovery following bowel resection surgery (essentially to prevent post-op ileus)?

A

alvimopam

–>peripheral opioid antagonist

47
Q

What is risk a/w Alvimopan?

A

MI

REMS program requires hosp use with max 15 doses

48
Q

MOA of Linaclotide

A

selective guanylate cyclase-C agonist

–> binds luminal surface of intestinal epithelium, increases cGMP

–> + secretion of chloride/bicarb into lumen via +CFTR ion channel

49
Q

Indications for Linaclotide use

A

IBS-C (consipation predom subtype)

Chronic idiopathic constipation (CIC)

50
Q

MOA of Lubiprostone

A

prostaglandin-E1 derivative

–> increases intestinal secretion of fluid by + CIC-2(GI specific chloride channels)

51
Q

Indications for Lubiprostone

A

IBS-C in WOMEN
–> no pregnancy

CIC (chronic idiopathic c)

Opioid-induced constipation

52
Q

Give examples of Bulk-forming or Hydrophilic colloidal agents used in treating constipation

A

Fiber/bran

Psyllium

Methylcellulose/ Carboxymethylcellulose

Polycarbophil

53
Q

MOA of bulk-forming/ hydrophilic colloidal agents

A

increase bulk volume and water content–> increases GI motility

fiber supports colonic bacteria, fermentation, digestion

efficacy in 2-4 days

54
Q

Adverse effects of bulk-forming/hydrophilic colloidal agents

A

bloating/obstruction
–> drink fluids w/ caution in renal failure

LOTS of drug-drug interactions

55
Q

Examples of stool softeners

A

AKA surfactant/emollient laxatives

docusate salts

mineral oid

56
Q

MOA of stool softeners

A

anionic surfactants–> soften and lubricate feces

–> increase fluid secretion in GI tract

–> decrease fluid reabsorption from GI tract

efficacy 1-3 days

57
Q

Adverse effects of stool softeners

A

GI related

58
Q

What is used for pre-colonoscopy bowel prep?

A

sodium picosulfate

–>osmotic

59
Q

Give examples of stimulants/irritants used to treat constipation

A

senna

bisacodyl

castor oil

glycerin

sodium picosulfate (bowl prep)

60
Q

MOA of stimulants/irritants to treat constipation

A
  • irritant to enterocytes and GI smooth muscle–> inflammation
  • —>increases prostaglandin secretion and inhibits Na/K ATPase
  • promotes water/electrolyte accumulation in GI
  • –>castor oil

efficacy 12-36 hours

61
Q

What is castor oil hydrolyzed to

A

ricinoleic acid

62
Q

What is the function of glycerin?

A

treat constipation as;

irritant
osmotic
lubricant

63
Q

Adverse effects of stimulants/irritants

A

abdominal cramping

urine discoloration (senna)

fluid/electrolyte disturbaces with long use

64
Q

What is an effect of senna?

A

urine discoloration (yellow-brown or red-pink)

65
Q

Examples of saline agents used in treating constipation

A

Magnesium salts

Sodium phosphate

66
Q

MOA of saline agents

A

poorly absorbed–> hyperosmolar solutions, osmotically retain water in GI tract

67
Q

Drug interactions with saline agents

A

diuretics–> electrolyte balance

68
Q

Cautions with saline agent use

A

renal disease (d/t electrolyte)

CHF/HTN (d/t sodium)

69
Q

Give examples of osmotic agents

A

lactulose

magnesium citrate

sorbitol

polyethylene glycol (PED-3350)

70
Q

MOA of osmotic agents

A

attract and retain increased water in colon–> increase moisture, softness, bulk

efficacy 1-2 days but larger doses can occur sooner (1-3 hrs)

71
Q

What osmotic agent is used for severe liver disease patients with hyperammonemia?

A

lactulose

72
Q

Adverse effects of osmotic agents

A

electrolyte disturbances

GI

73
Q

What drug is given in large doses during bowel prep prior to scopes and surgery?

A

Polyethylene glycol

often given with mag citrate

GI (4 decks)

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