GI drugs Flashcards

1
Q

Antacids drugs

A

Al (OH)3
Mg (OH)2
CaCO3

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2
Q

Antacids description

A

Weak bases increase the pH of the stomach

->pepsin inactivation

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3
Q

Antacids Mechanism

A

Forms a salt and H2O

Very fast effect

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4
Q

Antacids Indication

A

GERD
GASTRITIS
PUD

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5
Q

Antacids PK

A

AL(OH)3 may decrease bioavailability of tetracyclines, digoxin, and antimuscarinics

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6
Q

Antacids contraindications

A

Al(OH)3 -> constipation
Mg(OH)2 -> diarrhea

CaCO3 -> Nephrolithiasis and constipation -> fecal impaction

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7
Q

H2 blockers

A
Cimetidine (1st gen)
2nd gen:
Famotidine
Ranitidine
Nizatidine
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8
Q

H2 blockers description for peptic ulcer disease

A

90% reduction of HCl** secretion after a single dose

Promote healing of ulcers

Recurrence is common when monotherapy is stopped

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9
Q

H2 blockers mechanism for PUD

A

Block the Gs mediated increase in cAMP that activatges the H+/K+ pump

2nd gen do not inhibit CYP450 and are longer actring than cimetidine

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10
Q

H2 PUD Indication

A

Acute stress ulcer

Prevent aspiration PNA preoperatively

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11
Q

H2 PUD PK

A

Cimetidine inhibits CYP450 ->many drug interactions

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12
Q

H2 PUD adverse/contraindications

A

**Cimetidine crosses the BBB and is prolactin simulating and anti-androgenic -> gynecomastia*

Nausea, HA & dizziness

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13
Q

Proton pump inhibitor PUD drugs

A
Omeprazole
Esomeprazole
Lansoprazole
Rabeprazole
Pantoprazole
...basically prazoles
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14
Q

Proton pump inhibitor PUD description

A

Nearly 100% reduction in HCl

Activated after transport into parietal cell (prodrug)

Also support platelet aggregation and maintain clot integrity -> hemorrhagic ulcers

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15
Q

Proton pump inhibitor PUD mechanism

A

Covalent bond formation with cysteine residue on H+/K+ ATPase within the parietal cell canaliculi -> irreversible inactivation

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16
Q

Proton pump inhibitor PUD Indication

A
GERD
Gastric ulcers
MEN I
ZE syndrome
H pylori (with antibiotics)
NSAID induced ulcers
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17
Q

Proton pump inhibitors PUD PK

A

Omeprazole inhibits Warfarin, phenytoin, diazepam and cyclosporine

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18
Q

Proton pump inhibitor PUD Adverse/Contraindications

A

Nausea and diarrhea are possible, but they are generally well tolerated

Prolonged use of PPI and H2 -> decrease bioavailability and B12, disgoxin and ketoconazole (acid required for absorption)

GI and respiratory infections
Pancreatitis
Hepatotoxicity
Interstitial nephritis

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19
Q

Antimicrobials used against H pylori

A

Clarithromycin
Amoxicillin
Metronidazole
Tetracycline

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20
Q

Clarithromycin, Amoxicillin, Metronidazole, Tetracycline PUD description

A

Eradication of H pylori -> rapid healing (infection documented with endoscopy, serology or urea breath test)

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21
Q

Clarithromycin, Amoxicillin, Metronidazole, Tetracycline PUD Mechanism

A

Used as part of triple therapy regimen for 2 weeks -> 2 antibiotics + PPI

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22
Q

Clarithromycin, Amoxicillin, Metronidazole, Tetracycline PUD Indication

A

H pylori infection

Other combo: bismuth, + 2 antibiotics + PPI or ranitidine

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23
Q

Mucosal protective agents PUD drugs

A

Sucralfate
Bismuth subsalicylate
Misoprostol

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24
Q

Sucralfate PUD description

A

Disaccharide; Requires acid to be activated … do not give with PPI’s or H2 blockers

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25
Q

Misoprostol PUD description

A
  • *PGE1 analogue**

* *decrease HCl secretion** and increase mucin & bicarb production via activation of Gi -> decrease cAMP

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26
Q

Sucralfate, Bismuth subsalicylate, Misoprostol PUD mechanism

A

Polymerization and selective binding to necrotic tissue forms a physical barrier to acid

Stimulates PG synthesis

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27
Q

Sucralfate, Bismuth subsalicylate, Misoprostol Indication

A

Ulcers

Bismuth may also be helpful in H pylori infections (antimicrobial)

Misoprostol is approved for NSAID induced ulcers but has been replaced by H2 blockers and PPI’s

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28
Q

Misoprostol adverse/contraindications

A

Diarrhea
Abortion (contraindicated in pregnancy)
Exacerbation of IBD

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29
Q

Prokinetic GI drugs

A

Neostigmine, Bethanechol
Metoclopramide
Cisapride
Erythromycin

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30
Q

Neostigmine GI description and indication

A

Cholinomimetic agent

indication- Pseudoobstruction in hospitalized patients

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31
Q

Bethanechol GI Description and indication

A

Cholinomimetic agent
M receptor only
indication- Gastroparesis

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32
Q

Metoclopramide Prokinetic GI Description/Mechanism

A

Accelerates gastric emptying and intestinal motility

5-HT and D2 blocker
5HT4=prokinetic

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33
Q

Metoclopramide GI indication

A
Gastroparesis
Emesis (in higher doses) associated with chemo
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34
Q

Metoclopramide GI ae/contraindication

A

Sedation, Diarrhea
Galactorrhea
EXTRAPYRAMIDAL SYMPTOMS

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35
Q

Cisapride prokinetic GI description/mechanism

A

Stimulates ACh secretion

5-HT agonist

36
Q

Cisapride GI indication

A

GERD, constipation

Gastroparesis

37
Q

Cisapride ae/contraindications GI

A

Can cause arrhythmia

Avoid in patients with long QT*******

38
Q

Erythromycin GI description/mechanism

A

Marcolide antibiotic

Motilin receptor agonist

39
Q

Erythromycin GI indication

A

Gastric emptying before endoscopy

Prokinetic agent

40
Q

Erythromycin GI PK

A

give IV

Short term use

41
Q

Erythromycin GI ae/contraindication

A

May develop tolerance in gastroparesis

42
Q

Opioid agonist anti diarrheals drugs

A

Loperamide

Diphenoxylate

43
Q

Opioid agonist anti diarrheal description/mech.

A

Decrease gut motility

Inhibit ACh release

Atropine is added to diphenoxylate to reduce abuse potential

44
Q

Bile acid Binding resins

A

Cholestyramine
Colestipol
Colesevelam

45
Q

Cholestyramine, Colestipol, Colesevelam GI description/mech

A

Used in lower cholesterol
Also prevent secretory diarrhea

Bile salts stimulate Cl- secretion in the colon (cAMP)
Resins form insoluble complexes with bile acids that are no longer able to stimulate this excess secretion

46
Q

Octreotide description/mech/indication

A

Somatostatin analog, anti diarrheal
Carcinoid syndrome: wheeze, flushing, diarrhea, and right side heart murmurs
VIPoma -> copious diarrhea

Long acting

Indication- Carcinoid tumor, VIPoma, Acute variceal bleed

47
Q

Octreotide GI ae/contraind.

A

Reduces both endocrine and exocrine pancreatic activity -> nausea, cramps, steatorrhea

48
Q

Bismuth subsalicylate GI

A

can be used as an anti diarrheal

49
Q

Opioid laxatives

A

Alvimopan

Methylnaltrexone

50
Q

Alvimopan, Methylnaltrexone GI description/mech

A

Laxatives
Block GI mu-receptors without entering CNS

Increase ACh and Peristalsis**

51
Q

Lubiprostone GI description and indication

A

Laxative
Increase fluid content by stimulating Cl- secretion

Indication -> constipation and IBS

52
Q

Cl- channel activator laxative

A

Lubiprostone

53
Q

Stimulant laxatives

A

Senna
Bisacodyl
Castor Oil

54
Q

Senna indication GI

A

Laxative

Used with docusate for opioid inducted constipation **

55
Q

Stimulant laxative ae

A

Cramping

Prolonged use -> perceived need

56
Q

Osmotic laxatives

A

Mg2+ salts
Mg(OH)3

Lactulose
Polyethylene Glycol

57
Q

Osmotic laxative descrip

A

Osmotic action draws water into the lumen which stimulates motility

58
Q

Mg2+ salt GI mechanism

A

laxative

Saline cathartics

59
Q

Lactulose GI mechanism

A

Synthetic disaccharide degraded by bacteria

60
Q

Polyethylene glycol GI mech

A

Radiology and endo

61
Q

Osmotic laxative indication

A

Simple constipation

Prep for endoscopy

62
Q

Lactulose indication

A

Hepatic encephalopathy -> draws out NH3 preventing hyperammonemia
Acidification of gut lumen traps NH4+
*

63
Q

Softener laxatives

A

Docusate
Mineral oil
Glycerine

64
Q

Docusate, Mineral oil, Glycerine description and indication GI

A

Emulsify and soften stool making it easier to pass
Laxatives

Combined with stimulant in opioid induced constipation

65
Q

Methylcellulose, Psyllium, Bran description/mech

A

Bulk forming laxatives
Insoluble, indigestible derivatives from fruits and vegetables

Increased H2O retention to increase stool bulk
Distension of the bowel -> stimulation of peristalsis

66
Q

Methylcellulose, Psyllium, Bran GI PK

A

Bulk forming laxatives

Require high fluid intake

67
Q

Methylcellulose, Psyllium, Bran contraindication

A

Do not use with opioid induced constipation

68
Q

Ondansetron (Zofran), Granisetron description/indication

A

Anti emetics
5HT3 blockers
Autocoid with action in the gut and CNS

Indication- moderate to severe emesis associated with chemotherapy
Post op nausea/vomiting

69
Q

Aprepitant GI

A

Anti emetic NK1 blocker
Description- **CNS action at neurokinin 1 receptors (substance P)
Indication - early and delayed emesis in chemo

ae/contra - dizziness, fatigue, diarrhea, CYP interactions

70
Q

Dexamethasone, Methylprednisolone GI

A

Anti emetic corticosteroids
Combined with Odansetron to provide greater anti emesis
Indication - chemotherapy induced nausea/vomiting

71
Q

Diphenhydramine, Meclinzine, Cyclizine GI

A

Anti emetic H1 blockers

Indicaton - Motion sickness, chemotherapy induced nausea/vomiting

72
Q

Scopolamine GI

A

Anti emetic anti-muscarinic

DOC for emesis associated with motion sickness

73
Q

Prochlorperazine, Promethazine, Droperidol GI

A

Anti emetic D2 blockers
D2 and M blocker
Indication - emesis
AE- extrapyramidal symptoms & hypotension

74
Q

Lorazepam, Alprazolam, Diazepam GI

A

Anti emetic Benzos
Beneficial effect may be due to sedative, anxiolytic, and amnesic properties
Indication - anticipatory N/V

75
Q

Dronabinol GI

A

Anti emetic cannabinoids
Central acting anti emetic
Mechanism-THC
Indication - Chemoinduced nausea/vomit

76
Q

Sulfasalazine, Balsalzide, Mesalamine GI

A

Drugs for IBD, aminosalicylates

Sulfa derivative prodrug
Releases sulfapyridine and 5-ASA (aminosalicylic acid)

Mesalamine = 5-ASA

Mech- 5-ASA inhibits IL-1 & TNF alpha**

Use: Crohn’s, Ulcerative colitis

AE:
Avoid in patients with sulfa allergy
Due to sulfapyridine:
N/V/D, hypersensativity reactions, BM suppression

77
Q

Methotrexate, Mercaptopurine, Azathioprine GI

A

Drugs for IBD, immuno-modulators
Description-inhibits purine synthesis-> specific for S phase; generalized immune suppression

MTX inhibits DHF reductase**
6-MP promotes apoptosis**

Use: Crohn’s, Ulcerative Colitis

Aziothioprine converts to 6-MP

AE:
MTX -> toxicity rare
6MP->can cause GI mucositis, hepatotoxicity and myelosuppression

78
Q

Infliximab, Adalimumab GI

A

Drugs for IBD
Anti TNF alpha
Blocks the action of TNF alpha, a principle mediator of Crohn’s

Used in acute flare ups of Crohn’s and fistulas**
RA
Given IV

AE/contraindication->Reactivation of latent TB
Fever, chills, urticaria, hypotension
Development of Ab’s

79
Q

Natalizumab GI

A

Drug for IBD, Anti-integrin

Blocks leukocyte integrins

Used in acute flare ups of Crohn’s and fistulas
RA

AE/Contraindication-> Progressive multifocal leukoencephalopathy

80
Q

Hydrocortisone, Prednisone, Prednisolone, Budesonide GI

A

Drugs for IBD, glucocorticoids

General anti-inflammatories
Budesonide->controlled release in the distal ileum and colon

Inhibit TNF alpha, IL-1, IL-8

Used for acute cases of IBD

81
Q

Alosetron GI

A

Drug for IBS, 5-HT3 blocker
Long acting->IBS-D
Decreases smooth muscle activity

Indication-> IBS-diarrhea and/or constipation
Chronic symptoms with no structural abnormality

Treatment: symptomatic

AE/contraindications-. Ischemic colitis

82
Q

DIcyclomine, Glycopyrrolate, Methscopolamine, Hyoscyamine GI

A

Drugs for IBS; Anticholinergics
Non-selective IBS-D

Indication-
IBS-diarrhea and/or constipation
Chronic symptoms with no structural abnormality
Treatment:symptomatic

83
Q

Loperamide GI

A

Drug for IBS; Opioid agonist
Decrease gut motility -> IBS-D
Inhibits ACh release

Indication-
IBS-diarrhea and/or constipation
Chronic symptoms with no structural abnormality
Treatment: symptomatic

AE-> negligible CNS effects

84
Q

Lubiprostone GI

A

Drug for IBS; Cl- Channel Activator
IBS-C
Increase fluid content by Stimulating Cl- secretion

Indication -
IBS - diarrhea and or constipation
Chronic symptoms with no structural abnormality
Treatment: symptomatic

85
Q

Pancrelipase GI

A

Pancreas enzyme; drug for IBS
Replacement enzyme
Increases absorption
Indication -> chronic pancreatitis, etc.