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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
Misoprostol PUD description
* *PGE1 analogue** | * *decrease HCl secretion** and increase mucin & bicarb production via activation of Gi -> decrease cAMP
26
Sucralfate, Bismuth subsalicylate, Misoprostol PUD mechanism
Polymerization and selective binding to necrotic tissue *forms a physical barrier* to acid Stimulates PG synthesis
27
Sucralfate, Bismuth subsalicylate, Misoprostol Indication
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*
28
Misoprostol adverse/contraindications
Diarrhea **Abortion** (contraindicated in pregnancy) Exacerbation of IBD
29
Prokinetic GI drugs
Neostigmine, Bethanechol Metoclopramide Cisapride Erythromycin
30
Neostigmine GI description and indication
Cholinomimetic agent | indication- Pseudoobstruction in hospitalized patients
31
Bethanechol GI Description and indication
Cholinomimetic agent M receptor only indication- Gastroparesis
32
Metoclopramide Prokinetic GI Description/Mechanism
Accelerates gastric emptying and intestinal motility 5-HT and D2 blocker **5HT4=prokinetic**
33
Metoclopramide GI indication
``` Gastroparesis Emesis (in higher doses) associated with chemo ```
34
Metoclopramide GI ae/contraindication
Sedation, Diarrhea Galactorrhea **EXTRAPYRAMIDAL SYMPTOMS**
35
Cisapride prokinetic GI description/mechanism
Stimulates ACh secretion 5-HT agonist
36
Cisapride GI indication
GERD, constipation | Gastroparesis
37
Cisapride ae/contraindications GI
Can cause arrhythmia | Avoid in patients with long QT*********
38
Erythromycin GI description/mechanism
Marcolide antibiotic **Motilin receptor agonist**
39
Erythromycin GI indication
Gastric emptying before *endoscopy* | Prokinetic agent
40
Erythromycin GI PK
give IV | Short term use
41
Erythromycin GI ae/contraindication
May *develop tolerance* in gastroparesis
42
Opioid agonist anti diarrheals drugs
Loperamide | Diphenoxylate
43
Opioid agonist anti diarrheal description/mech.
Decrease gut motility Inhibit ACh release Atropine is added to diphenoxylate to reduce abuse potential
44
Bile acid Binding resins
Cholestyramine Colestipol Colesevelam
45
Cholestyramine, Colestipol, Colesevelam GI description/mech
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
Octreotide description/mech/indication
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
Octreotide GI ae/contraind.
Reduces both endocrine and exocrine pancreatic activity -> nausea, cramps, steatorrhea
48
Bismuth subsalicylate GI
can be used as an anti diarrheal
49
Opioid laxatives
Alvimopan | Methylnaltrexone
50
Alvimopan, Methylnaltrexone GI description/mech
Laxatives Block GI mu-receptors without entering CNS Increase ACh and Peristalsis**
51
Lubiprostone GI description and indication
Laxative Increase fluid content by stimulating Cl- secretion Indication -> constipation and IBS
52
Cl- channel activator laxative
Lubiprostone
53
Stimulant laxatives
Senna Bisacodyl Castor Oil
54
Senna indication GI
Laxative | Used with docusate for opioid inducted constipation **
55
Stimulant laxative ae
Cramping | Prolonged use -> perceived need
56
Osmotic laxatives
Mg2+ salts Mg(OH)3 Lactulose Polyethylene Glycol
57
Osmotic laxative descrip
Osmotic action draws water into the lumen which stimulates motility
58
Mg2+ salt GI mechanism
laxative | Saline cathartics
59
Lactulose GI mechanism
Synthetic disaccharide degraded by bacteria
60
Polyethylene glycol GI mech
Radiology and endo
61
Osmotic laxative indication
Simple constipation | Prep for endoscopy
62
Lactulose indication
**Hepatic encephalopathy -> draws out NH3 preventing hyperammonemia Acidification of gut lumen traps NH4+***
63
Softener laxatives
Docusate Mineral oil Glycerine
64
Docusate, Mineral oil, Glycerine description and indication GI
Emulsify and soften stool making it easier to pass Laxatives Combined with stimulant in opioid induced constipation
65
Methylcellulose, Psyllium, Bran description/mech
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
Methylcellulose, Psyllium, Bran GI PK
Bulk forming laxatives | Require high fluid intake
67
Methylcellulose, Psyllium, Bran contraindication
**Do not use with opioid induced constipation**
68
Ondansetron (Zofran), Granisetron description/indication
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
Aprepitant GI
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
Dexamethasone, Methylprednisolone GI
Anti emetic corticosteroids *Combined with Odansetron* to provide greater anti emesis Indication - chemotherapy induced nausea/vomiting
71
Diphenhydramine, Meclinzine, Cyclizine GI
Anti emetic H1 blockers Indicaton - Motion sickness, chemotherapy induced nausea/vomiting
72
Scopolamine GI
Anti emetic anti-muscarinic DOC for emesis associated with motion sickness
73
Prochlorperazine, Promethazine, Droperidol GI
Anti emetic D2 blockers D2 and M blocker Indication - emesis AE- **extrapyramidal symptoms** & hypotension
74
Lorazepam, Alprazolam, Diazepam GI
Anti emetic Benzos Beneficial effect may be due to *sedative, anxiolytic, and amnesic properties* Indication - *anticipatory N/V*
75
Dronabinol GI
Anti emetic cannabinoids Central acting anti emetic Mechanism-THC Indication - Chemoinduced nausea/vomit
76
Sulfasalazine, Balsalzide, Mesalamine GI
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
Methotrexate, Mercaptopurine, Azathioprine GI
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
Infliximab, Adalimumab GI
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
Natalizumab GI
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
Hydrocortisone, Prednisone, Prednisolone, Budesonide GI
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
Alosetron GI
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
DIcyclomine, Glycopyrrolate, Methscopolamine, Hyoscyamine GI
Drugs for IBS; Anticholinergics Non-selective IBS-D Indication- IBS-diarrhea and/or constipation Chronic symptoms with no structural abnormality Treatment:symptomatic
83
Loperamide GI
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
Lubiprostone GI
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
Pancrelipase GI
Pancreas enzyme; drug for IBS Replacement enzyme Increases absorption Indication -> chronic pancreatitis, etc.

Pharmacology (24 decks)

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