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GI Pharmacology > GI Pharm 1 > Flashcards

GI Pharm 1 Flashcards

1
Q

PPI’s (Proton Pump Inhibitors):

List

A
  1. Omeprazole
  2. Esomeprazole
  3. Lansoprazole
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2
Q

PPI:

Mechanism, Metabolism, Side Effect

A

Mechanism: PRODRUG

  1. Absorbed into systemic circulation
  2. Diffuse into parietal cells
  3. Catalyzed into a sulfonamide
  4. Binds IRREVERSIBLY to K/H-ATPase and inhibits => prodrug short t1/2, but therapeutic effect is long.

Metabolism: P450’s

Side Effects:

  1. Bone fractures (chronic use)
  2. Infections (chronic use)
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3
Q

Histamine (H_2) Blockers:

List, Side Effect

A
  1. Cimetidine (inhibits liver P450’s!)
  2. Ranitidine

Side Effects:
1. Tolerance (due to increased histamine production)

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4
Q

Misoprostol:

Mechanism, Use, Side Effects

A

Mechanism:

  1. PGE_1 analog
  2. Binds EP_3
    (a) Blocks cAMP => H/K ATPase in parietal cell
    (b) Activates foveolar cell to make Mucus, Bicarb

Use:
1. Prevent NSAID-induced mucosal injury

Side Effects:

  1. Abortificaient (increases uterine contractions)
  2. Abdominal cramping
  3. Diarrhea
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5
Q

Sucralfate:

Mechanism, Use, Side Effects

A

Mechanism:

  1. =Sucrose sulfate + Al(OH)_3
  2. In acid, forms gel
  3. Gel adheres to epithelial cells/ ulcer craters

Use:
1. Protect ulcers from pepsin

Side Effect:

  1. Constipation
  2. Inhibits drug absorption (at time of admin.)
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6
Q

Antacids:

List, Mechanism, Side Effects

A
  1. Al(OH)_3
  2. Mg(OH)2
  3. CaCO_3
  4. Combo Mg+Al
    (a) To offset diarrhea/constipation

Mechanism:
1. Neutralize acid

Side Effects:

  1. Mg + Al can bind some drugs
  2. Block drug absorption (=> take +/-2 hours)
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7
Q

CaCO_3 (calcium carbonate, Tums):

Mechanism, Side Effect

A

Mechanism:
1. Fast acting

Side Effect:
1. CO_2 gas (burps)

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8
Q

AL(OH)_3 (aluminum hydroxide):

Side Effect

A

Side Effect:

1. Constipation

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9
Q

Mg(OH)_2 (magnesium hydroxide)

Side Effect

A

Side Effect:

1. Diarrhea

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10
Q

Bismuth subsalicylate:

Mechanism, Use, Side Effect

A

Mechanism:

  1. Binds Ulcer
  2. Promotes Mucin
  3. Promotes Bicarbonate
  4. Anti-Bacterial

Use:
1. Traveler’s Diarrhea

Side Effect:

  1. Black stool/tongue
  2. Reye’s syndrome (salicylate can be absorbed)
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11
Q

Antibiotics for H. Pylori

A
  1. Metronidazole
  2. Clarithromycin
  3. Amoxicillin
  4. Tetracycline
  • Triple Tx: 2-3 ABx + PPI 10-14 days
  • *Quadruple Tx: 2-3 ABx + PPI + Bismuth subsalicylate 10-14 days
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12
Q

Ulcer: H. Pylori Tx

A

Reduce acid + erradicate H. Pylori

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13
Q

Ulcer: NSAID Tx

A

Reduce acid, replace prostaglandins

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14
Q

Ulcer: Non- H. Pylori/ Non- NSAID Tx

A

Reduce acid

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15
Q

GERD Tx

A

PPI/H_2 blocker (related to severity)

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16
Q

Zollinger-Ellison Tx

A

PPI (+surgery/resection of gastroma) (+octreonam if systemic spread)

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17
Q

Simethicone

Mechanism, Use

A

Mechanism:
1. Surfactant (additive in antacids)

Use:
1. Additive in antacid => Decrease gas bubbles

18
Q

Scopolamine

Mechanism, Use

A

Mechanism:
1. Muscarinic Receptor Antagonist (cerebellum)

Use:
1. Motion sickness

19
Q

Dimenhydrinate

Mechanism, Use

A

Mechanism:

  1. H_1 blocker (antihistamine) (Brainstem)
  2. Muscarinic receptor antagonist

Use:
1. Motion sickness

20
Q

Ondansetron

Mechanism, Use

A

Mechanism:
1. 5-HT_3 receptor antagonist (CNS/PNS)

Use:
1. Chemotherapy/Radiation induced nausea (NOT motion sickness)

21
Q

Granisetron

Mechanism, Use

A

Mechanism:
1. 5-HT_3 receptor antagonist (CNS/PNS)

Use:
1. Chemotherapy/Radiation induced nausea (NOT motion sickness)

22
Q

Prochlorperazine

Mechanism, Use, Side Effect

A

Mechanism:
1. D_2 antagonist (CTZ)

Use:
1. General nausea

Side Effect:
1. Restlessness

23
Q

Dronabinol

Mechanism, Use, Side Effect

A

Mechanism:
1. CB_1 Receptor Agonist

Use:
1. Prophylaxis of refractory, chemotherapy-induced vomiting

Side Effects:

  1. Increased eating
  2. Lethargy
24
Q

Dexamethasone

Mechanism, Use, Side Effect

A

Mechanism:
1. ??? Unknown

Use:
1. In conjunction with other anti-emetics(5 HT_3 antagonist) for chemo

Side Effects:

  1. Hiccups
  2. Fatigue
  3. Nausea
  4. Constipation
25
Q

Aprepitant

Mechanism, Use, Side Effects

A

Mechanism:
1. Substance P Mimic/ NK_1 receptor antagonist

Use:

  1. Acute and delayed chemotherapy nausea and vomiting
  2. Given with Dexamethasone
26
Q

Metoclopramide

Mechanism, Use, Side Effects

A

Mechanism:

  1. D_2 Antagonist
  2. Triggers ACh release in the myenteric plexus
  3. Enhanced gastric emptying

Use:

  1. Diabetic gastroparesis
  2. GERD

Side Effects:

  1. Dystonia (careful in parkinson’s patients)
  2. Drowsiness
27
Q

Erythromycin

Use, Side Effects

A

Use:
1. Enhanced gastric motility (off-label)

Side Effect:
Cramping

28
Q

Acute Diarrhea Tx

A
  1. Rehydration
  2. Electrolyte balance

*Want patients to flush out pathogen

29
Q

Loperamide

Mechanism, Use

A

Mechanism:
1. mu-Receptor Antagonist

Use:
1. Anti-diarrheal (Imodium)

*No CNS penetration

30
Q

Diphenoxylate

Mechanism, Use, Side Effects

A

Mechanism:

  1. Prodrug -> Difenoxin
  2. mu-Receptor Antagonist

Use:
1. Anti-diarrheal

Side Effects:

  1. CNS penetration -> abuse potential
    (a) give with Atropine (anti-muscarinic causes dry mouth and decreases high dose abuse)
31
Q

Fiber

Mechanism, Use

A

Mechanism:

  1. =Cellulose
  2. increases bulk
  3. binds toxins

Use:
1. Anti-diarrheal

32
Q

Octreotide

Mechanism, Use, Side Effects

A

Mechanism:

  1. =Somatostatin Analogue
  2. Blocks gastrin secretion (+other hormones)

Use:

  1. Inhibit secretory diarrhea due to gastroma (hormone-secreting tumors of the pancreas and GI tract)
  2. Post-op dumping syndrome
  3. Variceal bleeding
  4. Chemotherapy/AIDS diarrhea
33
Q

Prednisone

Mechanism, Use, Side Effects

A

Mechanism:
1. Corticosteroid

Use:

  1. Mod-Severe acute IBD attacks
    (a) Steroid-responsive patients (improve)
    (b) Steroid-dependent patients (relapse if dose tapered)
    (c) Steroid-unresponsive patients

Side Effects:
1. Systemic effects

34
Q

Budesonide

Mechanism, Use

A

Mechanism:
1. Steroid (enteric targeting)

Use:
1. Crohn’s Disease

35
Q

Mesalamine

Mechanism, Use, Side Effects

A

Mechanism:

  1. 5-ASA (aminosalicylate)
  2. Inhibits IL-1
  3. Inhibits TNF-a
  4. Inhibits lipoxygenase

Use:

  1. Mild-Mod ulcerative colitis
  2. Distal Stomach -> Colon (delayed release capsule)

Side Effects:

  1. HA
  2. Dyspepsia
  3. Skin Rash
  4. Salicylate allergy
36
Q

Olsalazine

Mechanism, Use, Side Effects

A

Mechanism:

  1. PRODRUG of mesalamine [5-ASA (aminosalicylate)]
  2. Inhibits IL-1
  3. Inhibits TNF-a
  4. Inhibits lipoxygenase

Use:

  1. Mild-Mod ulcerative colitis
  2. Colon only

Side Effect:

  1. Diarrhea
  2. Salicylate allergy
37
Q

Sulfasalazine

Mechanism, Use, Side Effects

A

Mechanism:

  1. PRODRUG of mesalamine [5-ASA (aminosalicylate)]
  2. Inhibits IL-1
  3. Inhibits TNF-a
  4. Inhibits lipoxygenase

Use:

  1. Mild-Mod ulcerative colitis
  2. Colon only

Side Effects: Sulfa-related

  1. Fever
  2. Malaise
  3. Vomiting
  4. HA
  5. Salicylate allergy
38
Q

Infliximab

Mechanism, Use, Side Effects

A

Mechanism:
1. Anti-TNF-a Antibody

Use:
1. Mod-Severe Crohn’s or UC

Side Effects:

  1. Lupus-like symptoms
  2. Delayed HS rxn
  3. Infection (URI’s - TB)
  4. NHL
39
Q

IBS (Irritable Bowel Syndrome)

Mechanism

A

Gut 5-HT release => increased gut motility and sensation

40
Q

IBD (Inflammatory Bowel Disease

List

A
  1. Ulcerative colitis - mucosal inflamation in the colon

2. Crohn’s Disease - transmural inflamation in any part of the GI tract

GI Pharmacology (1 decks)

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