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Gastrointestinal Flashcards

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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
Hydroxide antacids ADME
A: oral, 1-3 hrs after meals and before bedtime D M: HCL reaction E: 30 min from stomach, 2-3 hrs from food
26
Difference of treatment between hemorrhagic ulcers and NSAID induced ulcers.
Hemorrhagic: IV PPI NSAID induced: PPI, then H2 antagonist and misoprostol if needed
27
Stress ulcer treatment of choice
Sucralfate IV H2 antagonists NOT PPI
28
Zollinger-Ellison treatment of choice
High PPI dose, then octreotide if needed
29
First line GERD treatment in general population and pregnant population
PPI, then H2 antagonists if failed Pregnancy: antacids and sucralfate, PPI only if severe
30
Metoclopramide mechanism of action
D2 receptor antagonist and serotonin antagonist —> Antiemetic —> Prokinetic ONLY UPPER GI
31
Uses of prokinetics (3)
- Gastroparesia - Nausea - Vomiting
32
Metoclopramide side effects (4)
- Extrapyramidal symptoms - Neurological - Hyperprolactinemia - Diarrhea, pain
33
Metoclopramide ADME
A: oral, IV, IM D M: sulfate and glucuronide conjugation E: urine
34
Prokinetics contraindications (5)
- Digoxin or antidiabetic drugs - Small bowel obstruction - Parkinson’s - Seizures - Antipsychotics
35
Domperidone mechanism of action
D2 receptor antagonist —> antiemetic —> prokinetic UPPER GI
36
Main differences between metoclopramide and domperidone side effects
Metoclopramide: neurological symptoms Domperidone: poor BBB crossing, cardiac arrythmia
37
Domperidone ADME
A: oral, IV, IM D M: CYP3A4 E: feces and urine
38
Psyllium husk mechanism of action
Bulk-forming laxative
39
Glycerin type of medication
Osmotic laxative
40
Castor oil type of medication
Stimulant laxative Induce inflammation of mucosa —> epithelial electrolyte secretion
41
Main difference between osmotic and stimulant laxative indications
Osmotic: chronic use Stimulant: short-term use ONLY, otherwise dependence
42
Loperamide is used for these types of diarrhea: (3)
- Traveler’s - Chronic - Chemotherapy-induced
43
Loperamide side effects (4)
- Constipation - CNS depression - Ileus - In IBD: toxic megacolon DON’T GIVE IN DYSENTERIC DIARRHEA
44
Loperamide ADME
A: oral D: poor BBB crossing M: hepatic E
45
Octeotride mechanism of action
Inhibit serotonin and peptide secretion (Insulin, glucagon, secretin, motilin, etc.) = antidiarrheal + splanchnic vasoconstriction
46
Preferred medication for secretory diarrhea
Octeotride (Can also be used for variceal bleeding)
47
Octeotride ADME
A: SC, IV, IM D M: hepatic E: urine
48
Ondansetron mechanism of action
5-HT3 antagonist —> antiemetic —> central: area postrema —> peripheral: vagus inhibition
49
Ondansetron main uses (2)
- Chemotherapy vomiting - Post op nausa and vomiting
50
Ondansetron side effects (4)
- Constipation or diarrhea - QT prolongation - Serotonin sx - Increase liver enzymes
51
Ondansetron ADME
A: oral, IV, IM D M: CYP1A2, CYP2D6, CYP3A4 E: urine
52
Characteristics of the serotonin syndrome
- Shivering - Diarrhea - Muscle rigidity - Fever - Seizures
53
Aprepitant mechanism of action
NK1 (neurokinin) antagonist —> central antiemetic Only used for chemotherapy induced with 5HT3 antagonist and dexamethasone
54
Aprepitant ADME
A: oral, IV D: 95% protein bound M: CYP3A4 E: feces
55
Aprepitant contraindications (2)
- Cisapride or pimozide - Prolonged QT interval
56
Cyproheptadine type of medication
Antihistamine —> antiemetic
57
Antihistamines main side effect
Anticholinergic side effect = dry mouth, mydriasis, tachycardia, urinary retention —> give physostigmine (cholinesterase inhibitor(
58
Dopamine antagonist vs antihistamine uses
Antihistamines are used more for motion sickness and post op emesis
59
Dronabinol mechanism of action
Cannabinoid CB1 agonist —> prophylaxis for chemotherapy-induced nausea —> stimulate appetite
60
Dronabinol ADME
A: D: lipid soluble, 95% protein bound M: —> 11-OH-delta-9-THC E
61
Cinitiaprida mechanism of action and 3 uses
5-HT1 and 5-HT4 agonist 5-HT2 antagonist —> increase serotonergic activity —> GERD, dyspepsia, gastroparesia
62
Cinnarizine mechanism of action and use
Antihistamine Ca2+ channel blocker —> treat nausea and vomiting due to motion sickness, vertigo or Meniere’s disease
63
Flunarazine mechanism of action and use
Ca2+ channel blocker —> treat vertigo and migraine
64
Pinaverium mechanism of action and use
Ca2+ channel blocker selective to GI = ANTISPASMODIC —> treat pain and intestinal dysfunction —> ex. IBS
65
Butylhyoscine mechanism of action and use
Antispasmodic and anticholinergic —> prevent pain and fecal urgency —> ex. IBS
66
Mesalamine mechanism of action
Also known as 5-ASA (5-aminosalicyclic acid) —> antiinflammatory —> immunosuppressive
67
Mesalamine main use
Induction and maintenance of remission in CUCI In combination with glucocorticoids
68
Mesalamine side effects (5)
- Headache - Nephrotoxicity (rare) - Dyspepsia - Cutaneous eruption
69
Mesalamine ADME
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
Medications that are commonly used in IBD (7) PAMIA56
- Prednisone - 5-ASA - Azathioprine - 6-MCP - Methotrexate - Infliximab - Adalimumab
71
Rimonabant mechanism of action
CB1 antagonist —> appetite suppression Treat obesity but with high neurologic risks, not used anymore
72
Phentermine mechanism of action
Methamphetamine isomer —> stimulate catecholamine release —> appetite suppresion *Possible addiction
73
Sibutramine mechanism of action
Inhibit 5-HT reuptake and norepinephrine —> satiety (central) —> increased metabolic rate (peripheral) **not used, CV effects
74
Sodium and phosphate citrate mechanism of action
Osmotic laxative
75
Cholestyramine mechanism of action and use
Bind to bile acids and absorbs them —> osmotically inactive —> relieves diarrhea symptoms
76
Pentoxifylline mechanism of action and uses
Decrease blood viscosity —> improve blood blow —> less aching, cramping (ex. IBS)
77
Sennosides A and B or Senna mechanism of action
Stimulant laxative Weaker than castor oil

Pharmacology (13 decks)

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