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Pharmacology > Gastrointestinal > Flashcards

Gastrointestinal Flashcards

1
Q

PPIs decrease acid production by around ____%

A

80-95%

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2
Q

PPI effect duration

A

24-48 hours

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3
Q

PPI ADME

A

A: 30 min before meal or IV
D: 95% protein binding
M: CYP2C19, CYP3A4
E: urine

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4
Q

PPI uses

A
  • PUD or stress ulcers
  • GERD
  • Gastritis
  • H.pylori or NSAID gastropathies
  • Zollinger-Ellison sx
  • MALT lymphoma
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5
Q

PPI mechanism of action

A

PRODRUG
Irreversible H+/K+ ATPase inhibition in parietal cells
= higher pH

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6
Q

PPI possible side effects

A
  • C.difficile infection
  • Decreased iron and B12 absorption
  • Osteoporosis
  • Pneumonia risk
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7
Q

PPI interactions (6)

A
  • Clopidogrel
  • Warfarin
  • Diazepam
  • Phenytoin
  • Carbamazepine
  • Nifedipine
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8
Q

H2 receptor antagonists (3)

A
  • Ranitidine
  • Famotidine
  • Cimetidine
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9
Q

Ranitidine mechanism of action

A

H2 receptor antagonist on parietal cells
—> less cAMP —> less gastric acid secretion

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10
Q

Ranitidine and famotidine uses (5)

A
  • Peptic ulcer healing
  • Anaphylactic shock
  • GERD
  • Gastritis
  • Zollinger-Ellison sx
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11
Q

Which are more effective: PPIs or ranitidine?

A

PPIs

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12
Q

Ranitidine and famotidine ADME

A

A: oral, IV, IM
D: low protein binding, cross placenta, cross BBB
M: hepatic
E: urine

Note: inhibits CYP2C19

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13
Q

Misoprostol mechanism of action

A

PGE2 analog —> mucus secretion + blood flow + inhibit acid secretion (up to 3 hours)

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14
Q

Which medication can be used as prophylaxis for NSAID-induced gastric ulcers?

A

Misoprostol

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15
Q

Misoprostol side effects (2) + biggest contraindication

A
  • Diarrhea
  • IBD symptom exacerbation

PREGNANCY —> contractions = abortion

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16
Q

Sucralfate mechanism of action

A

Inhibit hydrolysis of mucosal proteins by sticking to epithelial cells —> less erosion and ulcers for 6 hours

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17
Q

Sucralfate should not be taken with: (3 )

A

PPIs
H2 blocker
Aluminum containing antacids

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18
Q

Sucralfate ADME

A

A: oral minimal absorption, 1 hr before meal
D: minimal
M: HCL reaction —> sucrose sulfate
E: feces

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19
Q

Bismuth mechanism of action

A

Binds to ulcer affected mucosa —> physical protection

Stimulates gastric HCO3

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20
Q

Which antiulcer agent is used for H.pylori eradication and traveler’s diarrhea?

A

Bismuth

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21
Q

Bismuth most relevant side effect

A

Stool darkening

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22
Q

Bismuth ADME

A

A: oral
D:
M: hydrolyzed to bismuth and salicylic acid
E: urine

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23
Q

Mg hydroxide and Al hydroxide mechanism of action, and their difference

A

ANTACIDS
React with HCL —> produce low acidity salts

Mg: fast acting
Al: slow acting

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24
Q

Side effects of hydroxide antacids (3)

A
  • Hypokalemia
  • Bloating
  • Belching

Mg: diarrhea, hyporeflexia, hypotension, cardiac arrest
Al: constipation, hypophosphatemia, osteodystrophy, proximal muscle weakness, seizures

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25
Q

Hydroxide antacids ADME

A

A: oral, 1-3 hrs after meals and before bedtime
D
M: HCL reaction
E: 30 min from stomach, 2-3 hrs from food

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26
Q

Difference of treatment between hemorrhagic ulcers and NSAID induced ulcers.

A

Hemorrhagic: IV PPI
NSAID induced: PPI, then H2 antagonist and misoprostol if needed

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27
Q

Stress ulcer treatment of choice

A

Sucralfate

IV H2 antagonists
NOT PPI

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28
Q

Zollinger-Ellison treatment of choice

A

High PPI dose, then octreotide if needed

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29
Q

First line GERD treatment in general population and pregnant population

A

PPI, then H2 antagonists if failed

Pregnancy: antacids and sucralfate, PPI only if severe

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30
Q

Metoclopramide mechanism of action

A

D2 receptor antagonist and serotonin antagonist
—> Antiemetic
—> Prokinetic ONLY UPPER GI

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31
Q

Uses of prokinetics (3)

A
  • Gastroparesia
  • Nausea
  • Vomiting
32
Q

Metoclopramide side effects (4)

A
  • Extrapyramidal symptoms
  • Neurological
  • Hyperprolactinemia
  • Diarrhea, pain
33
Q

Metoclopramide ADME

A

A: oral, IV, IM
D
M: sulfate and glucuronide conjugation
E: urine

34
Q

Prokinetics contraindications (5)

A
  • Digoxin or antidiabetic drugs
  • Small bowel obstruction
  • Parkinson’s
  • Seizures
  • Antipsychotics
35
Q

Domperidone mechanism of action

A

D2 receptor antagonist
—> antiemetic
—> prokinetic UPPER GI

36
Q

Main differences between metoclopramide and domperidone side effects

A

Metoclopramide: neurological symptoms

Domperidone: poor BBB crossing, cardiac arrythmia

37
Q

Domperidone ADME

A

A: oral, IV, IM
D
M: CYP3A4
E: feces and urine

38
Q

Psyllium husk mechanism of action

A

Bulk-forming laxative

39
Q

Glycerin type of medication

A

Osmotic laxative

40
Q

Castor oil type of medication

A

Stimulant laxative
Induce inflammation of mucosa —> epithelial electrolyte secretion

41
Q

Main difference between osmotic and stimulant laxative indications

A

Osmotic: chronic use
Stimulant: short-term use ONLY, otherwise dependence

42
Q

Loperamide is used for these types of diarrhea: (3)

A
  • Traveler’s
  • Chronic
  • Chemotherapy-induced
43
Q

Loperamide side effects (4)

A
  • Constipation
  • CNS depression
  • Ileus
  • In IBD: toxic megacolon

DON’T GIVE IN DYSENTERIC DIARRHEA

44
Q

Loperamide ADME

A

A: oral
D: poor BBB crossing
M: hepatic
E

45
Q

Octeotride mechanism of action

A

Inhibit serotonin and peptide secretion
(Insulin, glucagon, secretin, motilin, etc.)
= antidiarrheal

+ splanchnic vasoconstriction

46
Q

Preferred medication for secretory diarrhea

A

Octeotride

(Can also be used for variceal bleeding)

47
Q

Octeotride ADME

A

A: SC, IV, IM
D
M: hepatic
E: urine

48
Q

Ondansetron mechanism of action

A

5-HT3 antagonist —> antiemetic
—> central: area postrema
—> peripheral: vagus inhibition

49
Q

Ondansetron main uses (2)

A
  • Chemotherapy vomiting
  • Post op nausa and vomiting
50
Q

Ondansetron side effects (4)

A
  • Constipation or diarrhea
  • QT prolongation
  • Serotonin sx
  • Increase liver enzymes
51
Q

Ondansetron ADME

A

A: oral, IV, IM
D
M: CYP1A2, CYP2D6, CYP3A4
E: urine

52
Q

Characteristics of the serotonin syndrome

A
  • Shivering
  • Diarrhea
  • Muscle rigidity
  • Fever
  • Seizures
53
Q

Aprepitant mechanism of action

A

NK1 (neurokinin) antagonist —> central antiemetic

Only used for chemotherapy induced with 5HT3 antagonist and dexamethasone

54
Q

Aprepitant ADME

A

A: oral, IV
D: 95% protein bound
M: CYP3A4
E: feces

55
Q

Aprepitant contraindications (2)

A
  • Cisapride or pimozide
  • Prolonged QT interval
56
Q

Cyproheptadine type of medication

A

Antihistamine —> antiemetic

57
Q

Antihistamines main side effect

A

Anticholinergic side effect = dry mouth, mydriasis, tachycardia, urinary retention
—> give physostigmine (cholinesterase inhibitor(

58
Q

Dopamine antagonist vs antihistamine uses

A

Antihistamines are used more for motion sickness and post op emesis

59
Q

Dronabinol mechanism of action

A

Cannabinoid
CB1 agonist —> prophylaxis for chemotherapy-induced nausea
—> stimulate appetite

60
Q

Dronabinol ADME

A

A:
D: lipid soluble, 95% protein bound
M: —> 11-OH-delta-9-THC
E

61
Q

Cinitiaprida mechanism of action and 3 uses

A

5-HT1 and 5-HT4 agonist
5-HT2 antagonist

—> increase serotonergic activity

—> GERD, dyspepsia, gastroparesia

62
Q

Cinnarizine mechanism of action and use

A

Antihistamine
Ca2+ channel blocker

—> treat nausea and vomiting due to motion sickness, vertigo or Meniere’s disease

63
Q

Flunarazine mechanism of action and use

A

Ca2+ channel blocker

—> treat vertigo and migraine

64
Q

Pinaverium mechanism of action and use

A

Ca2+ channel blocker selective to GI = ANTISPASMODIC
—> treat pain and intestinal dysfunction
—> ex. IBS

65
Q

Butylhyoscine mechanism of action and use

A

Antispasmodic and anticholinergic
—> prevent pain and fecal urgency
—> ex. IBS

66
Q

Mesalamine mechanism of action

A

Also known as 5-ASA (5-aminosalicyclic acid)
—> antiinflammatory
—> immunosuppressive

67
Q

Mesalamine main use

A

Induction and maintenance of remission in CUCI
In combination with glucocorticoids

68
Q

Mesalamine side effects (5)

A
  • Headache
  • Nephrotoxicity (rare)
  • Dyspepsia
  • Cutaneous eruption
69
Q

Mesalamine ADME

A

A: oral or rectal/topical
D: cross placenta but not teratogenic
M: from sulfasalazine by colonic bacteria, then into N-acetyl-5-ASA
E: feces and urine

70
Q

Medications that are commonly used in IBD (7)

PAMIA56

A
  • Prednisone
  • 5-ASA
  • Azathioprine
  • 6-MCP
  • Methotrexate
  • Infliximab
  • Adalimumab
71
Q

Rimonabant mechanism of action

A

CB1 antagonist —> appetite suppression

Treat obesity but with high neurologic risks, not used anymore

72
Q

Phentermine mechanism of action

A

Methamphetamine isomer —> stimulate catecholamine release
—> appetite suppresion

*Possible addiction

73
Q

Sibutramine mechanism of action

A

Inhibit 5-HT reuptake and norepinephrine
—> satiety (central)
—> increased metabolic rate (peripheral)

**not used, CV effects

74
Q

Sodium and phosphate citrate mechanism of action

A

Osmotic laxative

75
Q

Cholestyramine mechanism of action and use

A

Bind to bile acids and absorbs them —> osmotically inactive

—> relieves diarrhea symptoms

76
Q

Pentoxifylline mechanism of action and uses

A

Decrease blood viscosity
—> improve blood blow

—> less aching, cramping (ex. IBS)

77
Q

Sennosides A and B or Senna mechanism of action

A

Stimulant laxative
Weaker than castor oil

Pharmacology (13 decks)

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