GI DRUGS Flashcards

1
Q

Antacids

A

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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2
Q

H2 Receptor Blocker

A

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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3
Q

PPIs

A
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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4
Q

Clarithromycin

A

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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5
Q

Amoxiclin

A

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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6
Q

Metronidazole

A

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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7
Q

Tetracycline

A

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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8
Q

Sucralfate

A

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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9
Q

Bismuth Subsalicylate

A

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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10
Q

Misoprostol

A

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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11
Q

Metoclopramide

A

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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12
Q

Cisapride

A

Class:5HT4 agonist

Uses: Gastroparesis , relief of GERD

MOA:stims. ACh

AE:Arrhythmias

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13
Q

Neostigmine

A

Class: Muscarinic agonist

Use: Colonic pseudo obstruction

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14
Q

Bethanechol

A

Class: Muscarinic agonist

Uses:Post-op bladder atony

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15
Q

Erythromycin

A

Class:Macrolide

Use: GI emptying before endoscopy

MOA: Motilin receptor agonist

AE: tolerance

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16
Q

Ondasetron

A

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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17
Q

Diphenhydramine,Cyclizine,Meclizine

A

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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18
Q

Scoplamine

A

Class:Antimuscarinic

USES:DOC for motion sickness

MOA: depolarizing blocker, crosses BBB

AE:

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19
Q

Aprepitant

A

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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20
Q

Fosaprepitant

A

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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21
Q

Dexamethasone

Methylprednisolone

A

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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22
Q

Phenothiazine

(Prochlorperazine

A

Class:D2 blocker

MOA:D2 and muscarinic antagonist

AE:Extrapyramidal SXS
Hypotension
Sedation

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23
Q

Promethazine

A

Class: D2 Blocker,

MOA: Anti-dopaminergic and anticholinergic

USES:Motion sickness
Antipsychotic effects
Sedative

24
Q

Droperidol

A

Class: D2 blocker

MOA:Antidopaminergic, antiemetic, antipsychotic and
neuroleptic analgesic agent

25
Q

Dronabinol

A

Class: Cannabinoids

USES:CINV

MOA:CB1 receptor antagonist (central acting)

26
Q

Lorazepam
Alprazolam
Diazepam

A

Class:CB1 receptor antagonist (central acting)

USES:Anticipatory vomiting

MOA:Beneficial effects d/t their sedative, anxiolytic, and
amnesic properties

27
Q

Loperamide

A

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

28
Q

Diphenoxylate

A

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

29
Q

Octreotide

A

Class:Somatostatin Analog

USES:Carcinoid syndrome, bleeding of EO varices, Acromegaly

MOA:Somatostatin receptor agonist

AE: GI disturbances
Gallstones
Bradycardia
Cardiac conduction anomalies

30
Q

Bismuth

Subsalicylate

A

Class:Bismuth Compound

USES:Antacid and antidiarrheal

MOA:Binds with toxins from E.colià decreases inflammation

31
Q

Senna

Bisacodyl

A

Class: Stimulant

USES: Laxative

AE:Cramping

32
Q

Methylcellulose
Psyllium
Bran

A

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

33
Q

Mg(OH)2

MgO

A

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

34
Q

Lactulose

A

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

35
Q

Polyethylene Glycol

PEG

A

Class:Osmotic agents

USES:Colonic lavage for endoscopic/ radiologic procedures

MOA:Draw water into the lumen of GIT increasing motility

36
Q

Glycerin

A

Class:Stool Softeners

USES:Laxative

AE:Irritation of anal mucosa

37
Q

Docusate (Colace)

Mineral Oil

A

Class:Stool Softeners

USES:Laxative

MOA:Emulsify and soften stool leading to lubrication (makes easier to pass)

38
Q

Lupiprostone

A

Class: Chloride Channel Activators

USES:Constipation associated IBS

MOA: increases Cl
secretion into GI leading to increase fluid content

39
Q

Alvimopan

Methylnaltrexone

A

Class: Opioid Antagonist

USES:Opioid induced constipation

MOA:Block Gi mu-opioid receptors leading to increase in ACh and peristalsis, DOES NOT ENTER CNS

40
Q

Sulfasalazine

A

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,

41
Q

Mesalamine

A

Class:Aminosalicylates

USES:Mild- Mod Crohn’s

MOA:Inhibits eicosanoids, Various formulations designed to deliver drug to distal ileum and colon

42
Q

Balsalazie

A

Class:Aminosalicylates

USES:UC

MOA:Releases Mesalamine in the large intestine @ site of UC

43
Q

Hydrocortisone
Prednisone
Prednisolone
Budesonide

A

Class:Glucocorticoids

USES: UC and Crohns’

MOA:Activation of glucocorticoid receptor alters gene transcription

AE:Adrenal suppression, Osteoporosis, GLucose intolerance

44
Q

Methotrexate

MTX

A

Class:Immunosuppressants

USES:Anticancer
Rheumatic disorders
UC and Crohn’s

MOA:Inhibit dihydrofolate reductase

AE: Nausea, Mucosal Ulcer, Hepatotoxicity, Teratogenic

45
Q

6-mercaptopurine
(6-MP)
Azathioprine

A

Class:Immunosuppressants

USES:AML, UC and Crohn’s

MOA:Promotes apoptosis

AE:Nausea and vomiting
Myelosuppression
Hepatotoxicity

46
Q

Infliximab

A

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

47
Q

Adalimumab

A

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

48
Q

Natalizumab

A

Class: Anti-integrins

USES:UC and Crohn’s

MOA:Blocks leukocyte integrins

AE:Progressive Multifocal
leukoencephalopathy (PML)

49
Q

Hyoscyamine
Dicyclomine
Glycopyrrolate
Methscopolamine

A

Class:Anticholinergic

USES:IBS

AE: Delirium, hallucinations, HTN, urinary retention

50
Q

Alosetron

A

Class:5HT3 Antagonists

USES:severe IBS

MOA:Reduced smooth mm. activity in the gut

AE:Serious constipation(Rare)
Ischemic colitis
Infarction

51
Q

Loperamide

A

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

52
Q

Lubiprostone

A

Class:Chloride Channel
Activators

USES:IBS

MOA: increases Cl
secretion into GI leading to increase fluid content

53
Q

Ursodiol

A

Class:Bile acid derivative

USES:Gallstones in pts refusing/not eligible for surgery

MOA:inhibits cholesterol gallstones

54
Q

Pancrelipase

A

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

55
Q

Orlistat

A

Class: Lipases inhibitor

USES:Weights Loss

MOA:decreases absorption of Vit. ADEK