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Pharmacology > GI Tract > Flashcards

GI Tract Flashcards

1
Q

Different types and uses of GI drugs

A

1- For peptic ulcer
2- For chemo-induced emesis control
3- Antidiarrheals
4- Laxatives
5- For IBDs

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2
Q

Peptic ulcer causes

A

1- NSAIDs
2- H. Pylori (70% of gastric, 90% of duodenal)
3- Increased acid
4- Inadequate mucosal defense

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3
Q

Peptic ulcer treatment approaches

A

1- Antimicrobial: For H. Pylori
2- Decrease acid secretion: H2 antagonists & proton pump inhibitors
3- Neutralize gastric acid: Non-absorbable antacids
4- Enhance mucosal defense: Misoprostol, sucralfate
5- Stop smoking

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4
Q

Decrease gastric acid secretion

A
  • H2 receptor antagonist (Inhibition of H/K-ATPase proton pump)
  • Prostaglandins
  • Antimuscarinic agents (Anticholinergics)
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5
Q

H2 receptor antagonist

Mechanism, Use time, Examples

A
  • Block binding of histamine to H2 receptor
  • So reduce cAMP concentration
  • So decrease secretion of acid
  • Basal, food stimulated & nocturnal secretion decrease after single dose
  • More acid at nights so used mostly at nights
  • -TIDINE:
  • Cimetidine
  • Ranitidine
  • Famotidine
  • Niatidine
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6
Q

Histamine effects

A
  • Adenylyl cyclase activation:
    • Increases cAMP
    • Activates PKA
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7
Q

What does PKA do?

A
  • Phosphorylation of skeletal proteins
  • Moves H-K ATPase from cytoplasm to membrane
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8
Q

Acetylcholine & Gastrin on calcium

A

Increases intracellular Ca2+

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9
Q

Muscarinic receptor (Acethylcholine)

A

Increases 4 things:
- Peristalsis
- Secretions
- Sphincter opening
- Smooth muscle contraction

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10
Q

Cimetidine

mechanism, side effects

A
  • Blocks H2 receptor, decreases acid
    Side effects:
  • Tachycardia
  • Cirrhosis (overdose with other drugs)
  • Gynecomastia (in men)
  • Galactorrhea (in women)
  • Bleeding w/ Warfarin
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11
Q

Nizatidine

First pass effect

A
  • Less affected by first pass effect
    First pass effect:
    Drug destroyed in liver before reaching circulation
    Therefore less oral form & more injection
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12
Q

Anti-acids

Example, mechanism

A
  • Al(OH)3 constipation
  • Mg(OH)2 diarrhea
  • Neutralize acid, increase pH
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13
Q

Protectants

Examples

A
  • Carbenoxolone
  • Sucralfate
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14
Q

Proton pump inhibitors
PPI

Examples, Mechanism, Clinical use, Half life

A
  • Omeprazol, Pantoprazol, Esomeprazol
  • Inhibit H-K ATPase pump in parietal cells
  • Bioavailability decreases by 50% with food (mornings 1h before breakfast)
    Clinical use:
  • Reflux
  • Peptic ulcers
  • Ulcer from H. pylori
  • NSAIDs ulcer
  • Peptic ulcer prevention
  • Before stomach tumor treatment
    Half life: 1-1.5h but 24h effect
  • Stronger than H2 blockers, almost 0 acid
  • Negative feedback causes histamin, gastrin & acethylcholine increase
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15
Q

PPI side effects

A
  • B12 decrease in long term
  • Decrease mineral absorption
  • Increase lung & GI infection (destroying acid wall)
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16
Q

Prostaglandins

Examples, mechanism

A
  • PGE 1 (Decrease acid secretion & strengthen stomach mucous)
  • Misoprostol (PGE 1 analog, Decreases NSAIDs, Increase bicarbonate, Induce miscarriage)
  • Bismuth subsalicylate
17
Q

Anti-cholinergics
(Anti-muscarinic, Atropinic)

Mechanism, example

A

Mechanism:
- Stimulates vagus nerve, then
- Acethylcholine secretion, then
- Muscarinic receptor stimulation, then
- Peristalsis
Vagus nerve:
1. Contractions
2. Increase peristalsis
3. Sphincter loosening
4. Increase secretions
Examples:
1. Atropine (not good for stoamch, good for salivary & sweat glands, lung, eyes)
2. Dicyclomine
3. Clidinium c (only M1 receptor block)

18
Q

Cholinergics

Overdose causes peptic ulcer

A
  • Carbachol
  • Bethanechol
  • Pilocarpin
  • Acethylcholine
  • Organophosphates
19
Q

Peptic ulcer approach

A
  1. Histamine: H2 blocker
  2. Vagus nerve: anti-muscarinic
  3. Bacteria: Ab (3 antibiotics, 1 won’t work)
  4. Weak mucosal layer: Protectants, honey, licorice, no smoking
20
Q

Diseases related to peptic ulcer

A
  • Zollinger-Ellison syndrome & Hypercalcemia: Increased gastrin
  • Diseases w/ severe vomitting: Hypochloremic metabolic alkalosis
21
Q

GERD

Risk factor, treatment

A
  • Asthmatics more susceptible
  • Some asthma drugs: theophylline
    Treatment:
    1. Histamin receptor inhibitors
    2. Antacids
    3. PPI
    4. Baclofen (Decreased sphincter loosening (GABA B agonist))
22
Q

Cholinomimetics

Example, Side effect

A
  • Neostigmine
  • Bethanechol & Carbachol
    Side effects: Menstruation problems, Gynecomastia, Prolactin increase
    NOT diarrhea
23
Q

D2 dopamine antagonists

A
  • Domperidone:
    1. Penetrates BBB
    2. Anti diarrhea & vomit
    3. Increases GI motility
    4. Drug resistant hiccups
  • Metoclopramide:
    FOR:
    GERD, Drug resistant hiccups, Gastric emptying problems, Indigestion, Vomit prevention
    Chronic use: Parkinsonism symptoms, Extrapyramidal problems, Hyperprolactinemia
24
Q

Laxatives

types

A
  1. Bulk-producing: methylcellulose, psyllium
  2. Stool surfactants: glycerin supp, docusate
  3. Osmotics: Mg citrate, Na phosphate
  4. Sorbitol, Lactose: Chronic (can cause flatulence)
  5. Polyethylene Glycol (PEG)
  6. Cl channel activators: Lubiprostone, Linaclotide
  7. 5HT3 antagonists & 5HT4 agonists
  8. Opioid receptor antagonists & 5HT4 antagonists (chronic constipation)
25
Q

Antidiarrheals

A
  1. Opioid agonists: loperamide, diphenoxylate
  2. Bile Acid Sequestrants: Cholestyramine, Colestipol
  3. Somatostatin: Gastrin, glucagon, GH & insulin inhibitor & Vasoactive peptid
  4. Clonidine
  5. Botax
  6. Cisapride
26
Q

Octreotide & somatostatin mimetic

Use, Side effects

A

Use:
- Intestine & pancreas secretion inhibitor
- Dumping syndrome
- Gastric carcinoid
- Hypophysis tumors (Acromegaly)
Side effects:
- Pancreas secretion problem
- Low DEKA vits
- Stomachache
- Flatulence & Diarrhea
- Bile stones
- Hyperglycemia
- Weak hypoglycemia

27
Q

Drugs for IBS

combination

A

Loperamide + Fiber supplements + MOM + Osmotic laxatives + TCAs

28
Q

Anti-spasms

A
  • Hyoscine
  • Dicyclomine
  • 5HT3 antagonists (-setron):
    Alosetron, ondansteron, graniseron, palonosetron
29
Q

Systems in vomitting

Receptors

A
  1. Cholinergic M1
  2. Histaminergic H1
  3. Serotonin 5HT3
  4. Neurokinin NK1

Pharmacology (6 decks)

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