ILE I U5 D2 Flashcards

1
Q

Laxatives work by generally

A

increasing stool amount and/or changing consistency

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2
Q

How do saline, hyper osmotic, and chlorine channel laxatives work?

A

Creating osmotic gradient resulting in water being drawn into the lumen creating pressure and stimulating peristalsis

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3
Q

How do lubricant (mineral oil), and emollient agent laxatives work?

A

Soften fecal material and prevent colonic resorption of fecal water

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4
Q

How do stimulant laxatives work?

A

Stimulate motility of small and large intestine, and rectum

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5
Q

Bulk forming laxatives MoA

A

Increased fiber intake, increases stool volume and may make stools softer

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6
Q

Bulk forming laxatives (products)

A
Methylcellulose (caplets, powder to mix in water)
Calcium Polycarbophil(caplets)
Pysillium husk (capsules, powdered formulations to mix in water)
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7
Q

Bulk forming laxatives onset? Suitable for chronic use?

A

12-72 hours, suitable - just adding fiber. SYSTEMIC

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8
Q

Bulk forming laxatives ADRs

A

abdominal cramping, flatulence, some have high sugar content

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9
Q

Hyperosmotic agents MoA

A

Creates an osmotic gradient resulting in water being drawn into the lumen of the intestines and rectume, creating increased intraluminal pressure and stimulating peristalsis

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10
Q

Hyperosmotic laxative products

A

PEG (polyethylene glycol), glycerin suppositories

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11
Q

Hyperosmotic laxative duration?

A

12-72 hours (PEG) NON-SYSTEMIC, 15-30 min (suppositories)

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12
Q

Hyperosmotic laxative ADR

A

bloating, cramping, discomfort, diarrhea, dehydration,

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13
Q

Saline laxatives MoA

A

Create an osmotic gradient resulting in water being drawn into the lumen of the intestines and rectum, creating increased intraluminal pressure and stimulating peristalsis

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14
Q

Saline laxatives products

A

Magnesium Hydroxide (Milk of Magnesia)
Magnesium Sulfate (Epsom salts)
Magnesium Citrate
Sodium Phosphate salts –Enemas (Fleet® Enema)

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15
Q

Saline laxatives onset

A

oral; 30 min - 6 hours

enema; 2-15 min

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16
Q

Saline laxative ADR

A

Bloating, cramping, abdominal discomfort, and flatulence.•Diarrhea, dehydration, and related complications may occur, particularly with excessive use.•Elevated magnesium levels, particularly in patients with kidney failure, infants and children, and elderly

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17
Q

Emollient agent MoA

A

Anionic surfactants that increase wetting efficiency (promote mixing of aqueous and fatty substances) so that intestinal fluid mixes with fecal material to create a softer fecal mass. These are not true laxatives, but are recommended to prevent stool straining and prevent painful defecation.

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18
Q

Emollient agent products

A

Docusate Sodium (Colace® and others) –capsules and liquid•Docusate Calcium –capsules

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19
Q

Emollient agents onset

A

12-72 hours, up to 5 days

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20
Q

Emollient agents ADRs

A

diarrhea and mild cramping

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21
Q

Emollient agent interactions

A

Don’t use with mineral oil

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22
Q

Lubricant product MoA

A

Coats the stool and prevents reabsorption of fecal water. This results in a softer stool, that is more easily eliminated.

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23
Q

Lubricant products available

A

Mineral Oil oral liquid•Mineral Oil oral liquid emulsion•Mineral Oil liquid enema

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24
Q

Lubricant products onset

A

6-8 hours oral, 5-15 min enema

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25
Q

Lubricant product ADRs

A

Lipid Pneumonia –if aspirated•Leakage of Oil through anal sphincter•Absorption into intestinal mucosa, liver and spleen –foreign body reactions

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26
Q

Lubricant product interactions

A

Reduced absorption of drugs and fat soluble vitamins (A, D, E, and K)

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27
Q

Stimulant laxatives MoA

A

Since these are old drugs, their mechanisms of action are not well understood. Act locally by irritating the mucosa or stimulating the nerve plexus of the intestinal smooth muscle. May also simulate secretion of water and electrolytes into the intestine. The idealstimulant agent would act only on the colon, and not on the small intestine.

28
Q

Stimulant laxatives onset

A

generally, 6 to 10 hours after oral use, but may be up to 24 hours.

29
Q

Bisacodyl dosafge

A

must be delivered to site of action in colon; suppositories and ENTERIC COATED tabs

30
Q

ENTERIC COATED TABS funtion

A

Coat allows drug to not be released until in basic pH

31
Q

Where do drugs normally dissolve?

A

Stomach

32
Q

Why wouldn’t you want bisacodyl to dissolve in stomach?

A

Want it to dissolve in small intestine-colon, NOT stomach

33
Q

Bisacodyl ADRs

A

antacids, H2 agonists or PPIs; cramping, a nominal pain, diarrhea with fluid/electrolyte loss, intestinal protein loss

34
Q

Senna is a __ laxative

A

stimulant

35
Q

Bisacodyl is a __ laxative

A

stimulant

36
Q

Senna availability

A

natural, tablets/pills, chocolate pieces, liquids

37
Q

Senna ADRs

A

similar to others; black pigmentation in colon (totally benign), discoloration of urine

38
Q

Castor oil

A

NOT a laxative! Should not be used. Really old drug, no known MoA, but appears to stimulate small and large oil

39
Q

Castor oil ADRs

A

severe cramping, nutrient loss, excessive fluid and electrolyte loss

40
Q

“first-line” laxatives after diet changes

A
  1. Assess diet; if deficient in fiber, then recommend fiber product
  2. If diet is correct, bisacodyl
  3. If this doesn’t work, see physician
41
Q

Difference between OTC and Rx laxatives

A

OTC is much older, Rx is better understood and targets specific receptor sites, but Rx meds are much, much more expensive

42
Q

Lubiprostone (Amitiza) MoA

A

Chloride channel activator
Acts locally in gut to open Cl channels in LUMINAL EPITHELIUM, increased Cl and intra-luminal fluid secretion, softens stool, accelerates GI transit

43
Q

Lubiprostone (Amitiza) effectiveness

A

Typically increases number of spontaneous bowel movements by 1-2/week

44
Q

Lubiprostone (Amitiza) ADRs

A

nausea, headaches, diarrhea

45
Q

Lumiprostone (Amitiza) dosages

A

8 and 24 mg tabs; 24 mg BID is normal dose

46
Q

Linaclotide (linzess) MoA

A

Activates guanylate cyclase-C receptor on intestinal epithelium
Increases intestinal fluid secretion, increases motility

47
Q

Linaclotide (Linzess) effectiveness

A

similar to Amitiza

48
Q

Linaclotide (Linzess) dose

A

72, 145, 290 mcg; usual is 145 qd

49
Q

Plecanatide (trulance) MoA

A

Guanylate cyclase-C agonist, increases intra and extra cellular concentration of cyclic guanosine monophosphate (cGMP)

50
Q

Electation of cGMP does what?

A

stimulates secretion of chloride and bicarbonate into the intestinal lumen, resulting in increased intestinal fluid and accelerated transit.

51
Q

Plecanatide (trulance) dose

A

3 mcg qd

52
Q

“Best” Rx laxative

A

Plecanatide (trulance)

53
Q

mu-receptor antagonists MoA

A

inhibit PERIPHERAL mu-receptors (opioid primary receptor)

54
Q

Mu receptor agonists (peripheral and central)

A
  1. Peripheral -> slows GI motility, leads to constipation

2. Central -> pain releif

55
Q

Best opioid-induced constipation relief

A

mu-receptor

56
Q

mu[receptor drugs

A
  1. Alvimopan (Entereeg)
  2. Methylnaltrexone (Registro)
  3. Naloxegol (Movantik)
  4. Naldemedine (Symproic)
57
Q

Alvimopan (Entereg) MoA and dose

A

Recovery of bowel function after small/large resection, 12 mg

58
Q

Methylnaltrexone (Relistor) MoA and dose

A

Opioid-induced constipation in palliative care, 150 mg, 8 and 12 mg injections

59
Q

Naloxegol (Movantik) MoA and dose

A

Opioid-induceed constipation in non-cancer pain; 12.5 - 25 mg

60
Q

Naldemedine (Symproic) MoA and dose

A

Opioid-induced constipation in adult patients with chronic non-cancer pain, 0.2 mg tabs

61
Q

Best non-cancer pain drugs

A

Acetaminophen and ibuprofen

62
Q

Lactulose MoA

A

Lactulose is a sugar derivative of lactose; acts as OSMOTIC AGENT similar to PEG

63
Q

Lactulose products

A

powders and solution lactulose

64
Q

Large volume administrations of PEG products is used for preparation prior to bowel procedures. Goal is to

A

completely clean colon to facilitate high quality endoscopic examination - patients should continue to consume solution until they are evaluating clear liquid stool with no visible fecal matter

65
Q

PEG regimens

A

2-4 liters of solution; major ADR of concern is excessive fluid loss and dehydration

66
Q

Sodium-phosphate products (SPS)

A

used to be OTC, but now Rx only because of large ADRs. Available in liquid or tablets

67
Q

SPS ADRs

A

dehydration - serious complication, leads to hypotension or renal impairment, patients using these must carefully follow directions. May exacerbate congestive heart failure de to Na content along with need to consume significant amounts of fluids to prevent dehydration and renal complications