GI DRUGS Flashcards by Sarah Zarzeczny

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

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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

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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

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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

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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

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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

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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

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Sucralfate

Class: sulfated disaccharide, mucosal protective

USES:PUD

MOA:Undergoes polymerization
and selective binding to
necrotic tissueàbarrier to
acid Stimulates PG synthesis

AE:

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Bismuth Subsalicylate

Class: Pepto, Mucosal Protective

USES: H.pylori, heals ulcers

MOA:Selectively binds to ulcer and forms protective
coating against acid/pepsin

AE:

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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

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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

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Cisapride

Class:5HT4 agonist

Uses: Gastroparesis , relief of GERD

MOA:stims. ACh

AE:Arrhythmias

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Neostigmine

Class: Muscarinic agonist

Use: Colonic pseudo obstruction

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Bethanechol

Class: Muscarinic agonist

Uses:Post-op bladder atony

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Erythromycin

Class:Macrolide

Use: GI emptying before endoscopy

MOA: Motilin receptor agonist

AE: tolerance

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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

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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)

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Scoplamine

Class:Antimuscarinic

USES:DOC for motion sickness

MOA: depolarizing blocker, crosses BBB

AE:

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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

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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

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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

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Phenothiazine

(Prochlorperazine

Class:D2 blocker

MOA:D2 and muscarinic antagonist

AE:Extrapyramidal SXS
Hypotension
Sedation

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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

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