GI DRUGS Flashcards
Antacids
Mg(OH)2-
Al(OH)2
CaCO3
USES: GERD
Gastritis
PUD
MOA:Weak bases that react with HCL to form salt
AE: MG- diarrhea
AL- Constipation
CaCO3- hypercalcemia, nehprolithitas and constipation
H2 Receptor Blocker
Cimetidine
Ranitidine
Famotidine
Nizatidine
Uses:GERD
Promote healing of
duodenal/gastric ulcers
MOA:Reversibly blocks Gsà
¯cAMPà inhibition of
H+/K+ ATPase
AE:Cimetidine:gynecomastia, prolactin levels, ¯libido, confusion in elderly
PPIs
Omeprazole Esomeprazole Lansoprazole Rabeprazole Pantoprazole
Inhibits nearly 100% HCL secretions
USES:GERD Duodenal/gastric ulcers H. pylori with ABx MEN-1 neoplasia ZE Syndrome NSAID induced ulcers
MOA:Covalent bond formation
with cysteine residue of H+/K+ ATPase inside parietal cell canaliculi à irreversible inactivation
AE:Nausea and diarrhea (rare) Small resp/ GI infections Long term use: ¯serum Mg2+ and hip fractures Pancreatitis, hepatotoxicity and interstitial nephritis
Clarithromycin
Class: Antimicrobials used in H.pylori, Macrolide
USES: H.Pylori
MOA:Bacteriostatic Binds to 23S rRNA of the 50S subunit prevents translocation and inhibits protein synthesis
AE:Bind to motilin receptors & GI upset
QT intervalà arrhythmia
hepatitis, rash, eosinophilia
Amoxiclin
Class: B-lactams
USES: H. Pylori ( gram + and some gram -)
MOA:Bacteriostatic
Binds to PBP prevent
cross linking of peptidoglycan in cell wall activate autolytic
enzymes
AE:Rash
HSN reactions
Pseudomembranous colitis
Metronidazole
Class: Antiprotozoal
Uses: H. pylori, Anaerobes ( C. difficile, Bacteroides)
MOA:Bactericidal agent
Produces toxic
metaboliteàdamage DNA and inhibits electron transport
AE:Severe flushing, tachycardia, hypotension
Tetracycline
Class: Broad Spectrum antibiotic
Uses:H. pylori
MOA:Binds to 30S subunità
prevent attachment of
aminoacyl-tRNA
AE:GI upset discoloration of teeth and inhibition of bone growth in children superinfection photosensitivity Contraindicated in pregnancy
Sucralfate
Class: sulfated disaccharide, mucosal protective
USES:PUD
MOA:Undergoes polymerization
and selective binding to
necrotic tissueàbarrier to
acid Stimulates PG synthesis
AE:
Bismuth Subsalicylate
Class: Pepto, Mucosal Protective
USES: H.pylori, heals ulcers
MOA:Selectively binds to ulcer and forms protective
coating against acid/pepsin
AE:
Misoprostol
Class: PGE1, mucosal protective
USES: Prevention of NSAID induced ulcers
MOA:Activates EP receptors
(Gi)à ¯acid secretion,
mucin and bicarb
Causes uterine contraction
AE:Diarrhea
Uterine cramping
Abortifacient
Exacerbation of IBD
Metoclopramide
Class: antiemetic agent, 5HT3 antagonist, D2 antagonist 5HT4
USES:Diabetic/ post-op gastroparesis Relief of GERD
MOA:Mediated by muscarinic activity via 5HT4 agonist activityà gastric emptying and intestinal motility High dosesà5HT3 antagonist activity
AE:Parkinsonian effects
Cisapride
Class:5HT4 agonist
Uses: Gastroparesis , relief of GERD
MOA:stims. ACh
AE:Arrhythmias
Neostigmine
Class: Muscarinic agonist
Use: Colonic pseudo obstruction
Bethanechol
Class: Muscarinic agonist
Uses:Post-op bladder atony
Erythromycin
Class:Macrolide
Use: GI emptying before endoscopy
MOA: Motilin receptor agonist
AE: tolerance
Ondasetron
Class:5HT3 inhibitor
USES:Chemotherapy and post-op vomiting
MOA:Autacoid that blocks chemoreceptor trigger zone and enteric nervous system of 5HT3 receptors
AE:QT intervalàarrhythmias
Diphenhydramine,Cyclizine,Meclizine
Class:H1, a and M
antagonist
USES:Motion sickness Hay fever Angioedema Sleep aid (oral) Dystonia (parenteral)
MOA:Competitively block central and peripheral H1 receptors + a-receptors and M-receptors
AE:Sedation
Autonomic block
CNS excitation (Rare)
Scoplamine
Class:Antimuscarinic
USES:DOC for motion sickness
MOA: depolarizing blocker, crosses BBB
AE:
Aprepitant
Class:NK1 blocker,oral
USES:early and delayed emesis in cancer chemotherapy
MOA:Substance P antagonist
NK1(neurokinin 1) blocker in the CNS
AE:Dizziness, fatigue, diarrhea CYP interactions
Fosaprepitant
Class:NK1 blocker,oral
USES:early and delayed emesis in cancer chemotherapy
MOA:Substance P antagonist
NK1(neurokinin 1) blocker in the CNS
AE:Dizziness, fatigue, diarrhea CYP interactions
Dexamethasone
Methylprednisolone
Class:Glucocorticoid
agonist/ Corticosteroids
USES:Inflammatory conditions
Organ transplantation
Hematologic cancers
Choice of chemotherapy
induced nausea/vomiting
(CINV)
MOA:Activation of glucocorticoid receptor alters gene transcription
AE:Adrenal Suppression,Glucose intolerance, osteoporosis, growth and muscle wasting
Phenothiazine
(Prochlorperazine
Class:D2 blocker
MOA:D2 and muscarinic antagonist
AE:Extrapyramidal SXS
Hypotension
Sedation
Promethazine
Class: D2 Blocker,
MOA: Anti-dopaminergic and anticholinergic
USES:Motion sickness
Antipsychotic effects
Sedative
Droperidol
Class: D2 blocker
MOA:Antidopaminergic, antiemetic, antipsychotic and
neuroleptic analgesic agent
Dronabinol
Class: Cannabinoids
USES:CINV
MOA:CB1 receptor antagonist (central acting)
Lorazepam
Alprazolam
Diazepam
Class:CB1 receptor antagonist (central acting)
USES:Anticipatory vomiting
MOA:Beneficial effects d/t their sedative, anxiolytic, and
amnesic properties
Loperamide
Class: Opioid Agonist
USES:
MOA:Opioid derivatives that decreases gut motility with negligible
CNS effects
Act via Gi mu-opioid receptorsà inhibit ACh release and decreases peristalsis
Doesn’t cross BBB
AE:Toxic Megacolon
Diphenoxylate
Class: Opioid Agonist
USES:
MOA:Opioid derivatives that decreases gut motility with negligible
CNS effects
Act via Gi mu-opioid receptorsà inhibit ACh release and decreases peristalsis
Crosses BBB
AE:Toxic Megacolon
Octreotide
Class:Somatostatin Analog
USES:Carcinoid syndrome, bleeding of EO varices, Acromegaly
MOA:Somatostatin receptor agonist
AE: GI disturbances
Gallstones
Bradycardia
Cardiac conduction anomalies
Bismuth
Subsalicylate
Class:Bismuth Compound
USES:Antacid and antidiarrheal
MOA:Binds with toxins from E.colià decreases inflammation
Senna
Bisacodyl
Class: Stimulant
USES: Laxative
AE:Cramping
Methylcellulose
Psyllium
Bran
Class:Bulk forming agents
USES:Laxative
MOA: increases water
retention leading to stools
become bulky
Distention of bowel leading to peristaltic stimulation of gut
AE: Do not use with opioid induced constipation
Mg(OH)2
MgO
Class: Osmotic agent
USES:Simple constipation
Bowel prep for endoscopy
MOA:Draw water into the lumen of GITàmotility
AE:Mg may be absorbed leading to toxicity &
renal impairment
Lactulose
Class:Osmotic agents
USES:Laxative, Hepatic encephalopathy
MOA:Converted into lactic, formic and acetic acid by intestinal bacteria increases osmotic effect
Draws out NH3 from body preventing hyperammonia
Polyethylene Glycol
PEG
Class:Osmotic agents
USES:Colonic lavage for endoscopic/ radiologic procedures
MOA:Draw water into the lumen of GIT increasing motility
Glycerin
Class:Stool Softeners
USES:Laxative
AE:Irritation of anal mucosa
Docusate (Colace)
Mineral Oil
Class:Stool Softeners
USES:Laxative
MOA:Emulsify and soften stool leading to lubrication (makes easier to pass)
Lupiprostone
Class: Chloride Channel Activators
USES:Constipation associated IBS
MOA: increases Cl
secretion into GI leading to increase fluid content
Alvimopan
Methylnaltrexone
Class: Opioid Antagonist
USES:Opioid induced constipation
MOA:Block Gi mu-opioid receptors leading to increase in ACh and peristalsis, DOES NOT ENTER CNS
Sulfasalazine
Class:Aminosalicylates
USES:Mild- Mod Crohn’s
MOA: Inhibits eicosanoids, Converted to sulfapyridine (antibacterial) and 5- aminosalicylic acid (5-ASA) (anti-inflammatory)
AE:Nausea vomiting, Reversible oligospermia,
Mesalamine
Class:Aminosalicylates
USES:Mild- Mod Crohn’s
MOA:Inhibits eicosanoids, Various formulations designed to deliver drug to distal ileum and colon
Balsalazie
Class:Aminosalicylates
USES:UC
MOA:Releases Mesalamine in the large intestine @ site of UC
Hydrocortisone
Prednisone
Prednisolone
Budesonide
Class:Glucocorticoids
USES: UC and Crohns’
MOA:Activation of glucocorticoid receptor alters gene transcription
AE:Adrenal suppression, Osteoporosis, GLucose intolerance
Methotrexate
MTX
Class:Immunosuppressants
USES:Anticancer
Rheumatic disorders
UC and Crohn’s
MOA:Inhibit dihydrofolate reductase
AE: Nausea, Mucosal Ulcer, Hepatotoxicity, Teratogenic
6-mercaptopurine
(6-MP)
Azathioprine
Class:Immunosuppressants
USES:AML, UC and Crohn’s
MOA:Promotes apoptosis
AE:Nausea and vomiting
Myelosuppression
Hepatotoxicity
Infliximab
Class:Anti-TNFa Drugs
USES:UC and Crohn’s remission/ acute flare ups
MOA: Mouse ab, targets TNFa (principle
mediator in Crohn’s
AE:Infusion rxns and infections
Reactivation of latent TB
Adalimumab
Class:Anti-TNFa Drugs
USES:UC and Crohn’s remission/ acute flare ups
MOA: Human IgG Ab,targets TNFa (principle
mediator in Crohn’s
AE:Infusion rxns and infections
Reactivation of latent TB
Natalizumab
Class: Anti-integrins
USES:UC and Crohn’s
MOA:Blocks leukocyte integrins
AE:Progressive Multifocal
leukoencephalopathy (PML)
Hyoscyamine
Dicyclomine
Glycopyrrolate
Methscopolamine
Class:Anticholinergic
USES:IBS
AE: Delirium, hallucinations, HTN, urinary retention
Alosetron
Class:5HT3 Antagonists
USES:severe IBS
MOA:Reduced smooth mm. activity in the gut
AE:Serious constipation(Rare)
Ischemic colitis
Infarction
Loperamide
Class: Opioids Agonist
USES:IBS
MOA;Act via Gi mu-opioid
receptors leading to inhibit ACh release and decreases peristalsis
AE:Toxic megacolon , Contraindicated in severe IBS and children
Lubiprostone
Class:Chloride Channel
Activators
USES:IBS
MOA: increases Cl
secretion into GI leading to increase fluid content
Ursodiol
Class:Bile acid derivative
USES:Gallstones in pts refusing/not eligible for surgery
MOA:inhibits cholesterol gallstones
Pancrelipase
Class:Pancreatic enzyme
USES:Pancreatic insufficiency in pts with: Chronic pancreatitis Pancreatectomy Steatorrhea Cystic Fibrosis
MOA:Improves digestion of dietary
fat, protein, and carbs
increases absorption of Vit. ADEK
AE: Gout
Orlistat
Class: Lipases inhibitor
USES:Weights Loss
MOA:decreases absorption of Vit. ADEK
