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