GI drugs Flashcards
Antacids drugs
Al (OH)3
Mg (OH)2
CaCO3
Antacids description
Weak bases increase the pH of the stomach
->pepsin inactivation
Antacids Mechanism
Forms a salt and H2O
Very fast effect
Antacids Indication
GERD
GASTRITIS
PUD
Antacids PK
AL(OH)3 may decrease bioavailability of tetracyclines, digoxin, and antimuscarinics
Antacids contraindications
Al(OH)3 -> constipation
Mg(OH)2 -> diarrhea
CaCO3 -> Nephrolithiasis and constipation -> fecal impaction
H2 blockers
Cimetidine (1st gen) 2nd gen: Famotidine Ranitidine Nizatidine
H2 blockers description for peptic ulcer disease
90% reduction of HCl** secretion after a single dose
Promote healing of ulcers
Recurrence is common when monotherapy is stopped
H2 blockers mechanism for PUD
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
H2 PUD Indication
Acute stress ulcer
Prevent aspiration PNA preoperatively
H2 PUD PK
Cimetidine inhibits CYP450 ->many drug interactions
H2 PUD adverse/contraindications
**Cimetidine crosses the BBB and is prolactin simulating and anti-androgenic -> gynecomastia*
Nausea, HA & dizziness
Proton pump inhibitor PUD drugs
Omeprazole Esomeprazole Lansoprazole Rabeprazole Pantoprazole ...basically prazoles
Proton pump inhibitor PUD description
Nearly 100% reduction in HCl
Activated after transport into parietal cell (prodrug)
Also support platelet aggregation and maintain clot integrity -> hemorrhagic ulcers
Proton pump inhibitor PUD mechanism
Covalent bond formation with cysteine residue on H+/K+ ATPase within the parietal cell canaliculi -> irreversible inactivation
Proton pump inhibitor PUD Indication
GERD Gastric ulcers MEN I ZE syndrome H pylori (with antibiotics) NSAID induced ulcers
Proton pump inhibitors PUD PK
Omeprazole inhibits Warfarin, phenytoin, diazepam and cyclosporine
Proton pump inhibitor PUD Adverse/Contraindications
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
Antimicrobials used against H pylori
Clarithromycin
Amoxicillin
Metronidazole
Tetracycline
Clarithromycin, Amoxicillin, Metronidazole, Tetracycline PUD description
Eradication of H pylori -> rapid healing (infection documented with endoscopy, serology or urea breath test)
Clarithromycin, Amoxicillin, Metronidazole, Tetracycline PUD Mechanism
Used as part of triple therapy regimen for 2 weeks -> 2 antibiotics + PPI
Clarithromycin, Amoxicillin, Metronidazole, Tetracycline PUD Indication
H pylori infection
Other combo: bismuth, + 2 antibiotics + PPI or ranitidine
Mucosal protective agents PUD drugs
Sucralfate
Bismuth subsalicylate
Misoprostol
Sucralfate PUD description
Disaccharide; Requires acid to be activated … do not give with PPI’s or H2 blockers
Misoprostol PUD description
- *PGE1 analogue**
* *decrease HCl secretion** and increase mucin & bicarb production via activation of Gi -> decrease cAMP
Sucralfate, Bismuth subsalicylate, Misoprostol PUD mechanism
Polymerization and selective binding to necrotic tissue forms a physical barrier to acid
Stimulates PG synthesis
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
Misoprostol adverse/contraindications
Diarrhea
Abortion (contraindicated in pregnancy)
Exacerbation of IBD
Prokinetic GI drugs
Neostigmine, Bethanechol
Metoclopramide
Cisapride
Erythromycin
Neostigmine GI description and indication
Cholinomimetic agent
indication- Pseudoobstruction in hospitalized patients
Bethanechol GI Description and indication
Cholinomimetic agent
M receptor only
indication- Gastroparesis
Metoclopramide Prokinetic GI Description/Mechanism
Accelerates gastric emptying and intestinal motility
5-HT and D2 blocker
5HT4=prokinetic
Metoclopramide GI indication
Gastroparesis Emesis (in higher doses) associated with chemo
Metoclopramide GI ae/contraindication
Sedation, Diarrhea
Galactorrhea
EXTRAPYRAMIDAL SYMPTOMS
Cisapride prokinetic GI description/mechanism
Stimulates ACh secretion
5-HT agonist
Cisapride GI indication
GERD, constipation
Gastroparesis
Cisapride ae/contraindications GI
Can cause arrhythmia
Avoid in patients with long QT*******
Erythromycin GI description/mechanism
Marcolide antibiotic
Motilin receptor agonist
Erythromycin GI indication
Gastric emptying before endoscopy
Prokinetic agent
Erythromycin GI PK
give IV
Short term use
Erythromycin GI ae/contraindication
May develop tolerance in gastroparesis
Opioid agonist anti diarrheals drugs
Loperamide
Diphenoxylate
Opioid agonist anti diarrheal description/mech.
Decrease gut motility
Inhibit ACh release
Atropine is added to diphenoxylate to reduce abuse potential
Bile acid Binding resins
Cholestyramine
Colestipol
Colesevelam
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
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
Octreotide GI ae/contraind.
Reduces both endocrine and exocrine pancreatic activity -> nausea, cramps, steatorrhea
Bismuth subsalicylate GI
can be used as an anti diarrheal
Opioid laxatives
Alvimopan
Methylnaltrexone
Alvimopan, Methylnaltrexone GI description/mech
Laxatives
Block GI mu-receptors without entering CNS
Increase ACh and Peristalsis**
Lubiprostone GI description and indication
Laxative
Increase fluid content by stimulating Cl- secretion
Indication -> constipation and IBS
Cl- channel activator laxative
Lubiprostone
Stimulant laxatives
Senna
Bisacodyl
Castor Oil
Senna indication GI
Laxative
Used with docusate for opioid inducted constipation **
Stimulant laxative ae
Cramping
Prolonged use -> perceived need
Osmotic laxatives
Mg2+ salts
Mg(OH)3
Lactulose
Polyethylene Glycol
Osmotic laxative descrip
Osmotic action draws water into the lumen which stimulates motility
Mg2+ salt GI mechanism
laxative
Saline cathartics
Lactulose GI mechanism
Synthetic disaccharide degraded by bacteria
Polyethylene glycol GI mech
Radiology and endo
Osmotic laxative indication
Simple constipation
Prep for endoscopy
Lactulose indication
Hepatic encephalopathy -> draws out NH3 preventing hyperammonemia
Acidification of gut lumen traps NH4+*
Softener laxatives
Docusate
Mineral oil
Glycerine
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
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
Methylcellulose, Psyllium, Bran GI PK
Bulk forming laxatives
Require high fluid intake
Methylcellulose, Psyllium, Bran contraindication
Do not use with opioid induced constipation
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
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
Dexamethasone, Methylprednisolone GI
Anti emetic corticosteroids
Combined with Odansetron to provide greater anti emesis
Indication - chemotherapy induced nausea/vomiting
Diphenhydramine, Meclinzine, Cyclizine GI
Anti emetic H1 blockers
Indicaton - Motion sickness, chemotherapy induced nausea/vomiting
Scopolamine GI
Anti emetic anti-muscarinic
DOC for emesis associated with motion sickness
Prochlorperazine, Promethazine, Droperidol GI
Anti emetic D2 blockers
D2 and M blocker
Indication - emesis
AE- extrapyramidal symptoms & hypotension
Lorazepam, Alprazolam, Diazepam GI
Anti emetic Benzos
Beneficial effect may be due to sedative, anxiolytic, and amnesic properties
Indication - anticipatory N/V
Dronabinol GI
Anti emetic cannabinoids
Central acting anti emetic
Mechanism-THC
Indication - Chemoinduced nausea/vomit
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
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
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
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
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
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
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
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
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
Pancrelipase GI
Pancreas enzyme; drug for IBS
Replacement enzyme
Increases absorption
Indication -> chronic pancreatitis, etc.