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Block 1 - GI > Pharm > Flashcards

Pharm Flashcards

1
Q

Primary neurotransmitter of the excitatory motor neurons simulating the gut?
Inhibitory?

A

ACh

NO

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2
Q

Modulation of motility, secretions, and emesis involves ___ released by enterochromaffin cells in response to mucosal sensor activity

A

Serotonin (5-HT)

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3
Q

Reversible ACh inhibitors

A
  1. Mono and bis-quaternary ammonium of alcohols (DOA minutes)
    - edrophonium
  2. Carbamates (DOA hours)
    - neostigmine
    - physostigmine
    - pyridostigmine
    - donepezil
    - tacrine
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4
Q

Irreversible ACh inhibitors

A
  • Organophosphorus inhibitors (DOA hundreds of hours)
    • echothioohate
    • parathion
    • malathion
    • Sarin
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5
Q

Absorption and distribution of Cholinergic drugs are based on

A

Structure

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6
Q

Most cholinergic drugs are metabolized to ___ with excretion usually ___

A

Inactive proteins

Renal

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7
Q

Adverse effects of cholinergic drugs

A
  1. Overstimulating cholinergic receptors:
    - Bradycardia
    - Increased salivation
    - Respiratory distress
  2. Blocking cholinergic receptors:
    - Dry mouth
    - Visual disturbances
    - Urinary retention
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8
Q

Atropine blockade

A

Competitive

Reversible

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9
Q

Effects of cholinergic stimulates

A

Increase smooth muscle contraction
Relax sphincters
Stimulates secretion

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10
Q

Mechanism by which ACh effect is terminated

A

Hydrolysis by cholinesterase in the synaptic cleft

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11
Q

Treatment of hyperactivity of the gut

A

Antimuscarinic drugs: Atropine

-decrease motility and secretions

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12
Q

Salivary glands are ____ to atropine (antimuscarinic drugs) while GI secretory cells are ___.
Perspiration is ___
Tearing and nasal secretions are ___

A

Very sensitive
Very insensitive
Very sensitive
Sensitive

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13
Q

Direct acting cholinomimetics

A 
ACh
Bethanechol
Carbachol
Pilocarpine
Cevimeline
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14
Q

Indirect acting cholinomimetics

A

Neostigmine
Pyridostigmine
Echothiophate

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15
Q

Adrenergic agonists

A

NE
Epinephrine
Dopamine
Terbutaline

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16
Q

Adrenergic antagonists

A 
Prazosin
Phentolamine
Tamulosin
Doxazosin
Terazosin
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17
Q

Muscarinic antagonists

A

Atropine
Oxybutynin
Darifenacin

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18
Q

The first line drugs to treat peptic ulcer and severe GERD

A

PPIs
-prazoles

Ex: omeprazole, etc.

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19
Q

Drugs indicated for H. pylori infection-induced peptic ulcers

A

Antibiotics

  • clarithromyocin
  • amoxicillin
  • metronidazole
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20
Q

MOA of PPI

A

Inhibit H+/K+ ATPase on parietal cells thus reducing acid secretion

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21
Q

MOA of H2 antagonists

A

Block H2 receptors on parietal cells to reduce acid secretion

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22
Q

H2 antagonists

A
  • tidines

* same uses as PPIs but less potent with rapid onset of action

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23
Q

Antacids

A

Sodium bicarbonate
Calcium carbonate
Aluminum hydroxide
Magnesium hydroxide

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24
Q

Drugs that promote mucosal defense

A

Sucralfate
Misoprostol
Bismuth subsalicylate

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25
Q

___ are weak bases that provide short term relief of peptic ulcer symptoms by neutralizing gastric acid

A

Antacids

26
Q

MOA:
coat GI wall
Stimulate secretion of PGs, mucus, and bicarbonate
Antimicrobial action

A

Bismuth subsalicylate

27
Q

MOA:
Coat GI wall
Inhibit pepsin
Stimulate secretion of PGs and bicarbonate

A

Sucralfate

28
Q

This drug is used in combo with antibiotics and H2 blocker or PPI to treat H. pylori peptic ulcer or to prevent travelers diarrhea

A

Bismuth subsalicylate

29
Q

This drug is a send to prevent stress gastritis and treat bile reflux gastropathy and oral mucositis

A

Sucralfate

30
Q

MOA:

Block both central and peripheral 5-HT3 receptors

A

5-HT3 receptor antagonists

-setrons

31
Q

MOA:

block central D2 or D2 and M receptors

A

D2 receptor blockers

  • metoclopramide
  • prochlorperazine
  • droperidol
32
Q

MOA:

Enhance GABAs effect on Cl ion conductance

A

Benzodiazepines

-Lorazepam

33
Q

MOA:

Block central and vestibular H1 receptors

A

H1 antagonists

  • diphenhydrazine
  • meclizine
  • doxylamine
34
Q

MOA:

Block vestibular M1 receptors

A

M1 receptor antagonist

-scopolamine

35
Q

MOA:
Not clear
Maybe blocking CB1 and 5-HT3 receptors?

A

Synthetic Cannabinoids

36
Q

This drug is used in combo with corticosteroids.

  • It is the most effective treatment for prevention of acute severe vomiting caused by chemotherapy
  • Also used for radiation and post-op nausea and vomiting
A

5-HT3 receptor antagonists

-setrons

37
Q

This drug is used in combo with corticosteroids for delayed chemotherapy-induced vomiting
-Also used in combo with 5-HT3 blockers and corticosteroids to prevent acute delayed chemotherapy-induced vomiting

A

NK1 receptor blocker

-pitant

38
Q

MOA:

Block central NK1 receptors

A

NK1 receptor blocker

-pitant

39
Q

This drug is used for:

  1. radiation, chemo, and infection-induced nausea and vomiting
  2. general emesis
  3. post-op nausea and vomiting, sedation
A

D2 receptor blockers

  1. metoclopramide
  2. Prochlorperazine
  3. droperidol
40
Q

This drug is used for anticipatory emesis

A

Benzodiazepines

-lorazepam

41
Q

This drug is used for:

  1. chemo induced vomiting
  2. Motion sickness
  3. With pyridoxine for pregnancy related emesis
A

H1 antagonists:

  1. diphenhydrazine
  2. meclizine
  3. doxylamine
42
Q

This drug is used as a transdermal patch to prevent motion sickness

A

M1 receptor antagonist

-Scopolamine

43
Q

This drug is used for chemo induced emesis

A

Synthetic cannabinoids

44
Q

MOA:

  1. Stimulate “mu” receptors in enteric neurons
  2. Inhibit presynaptic cholinergic action

Used for ___

A

Opioids

All forms of chronic diarrhea

45
Q

MOA:

  1. Bind to bacteria, toxin, and fluid
  2. Binds to bile acid

Side effects?

A

Adsorbents

  1. Kaolin and Pectin
    - also bismuth subsalicylate
  2. Bile-salt binding resins

*may affect absorption of other drugs

46
Q

This drug is used to treat:

  1. Acute diarrhea in children
  2. Travelers diarrhea
  3. Bile malabsorption-caused diarrhea
A

Adsorbents

  1. Kaolin and Pectin
  2. bismuth subsalicylate
  3. Bile-salt binding resins
47
Q

MOA:
Inhibits the secretion of numerous hormones and transmitters leading to reduced intestinal fluid secretion and decreased GI motility

*used for

A

Synthetic somatostatin

  • diarrhea caused by endocrine tumor, vagotomy or dumping syndrome
  • short bowel syndrome
  • AIDS
48
Q

MOA:
Inhibit Cl secretion to intestinal lumen

*used to treat ___

A

Chloride channel inhibitor

*diarrhea caused by antiretroviral therapy

49
Q

Treatment of mild IBS

  1. Pain/bloating
  2. Constipation predominant
  3. Diarrhea predominant
A
  1. Diet
  2. Diet, fiber
  3. Diet, loperamide
50
Q

Treatment of moderate to severe IBS

  1. Pain/bloating
  2. Constipation predominant
  3. Diarrhea predominant
A
  1. Anticholinergics, rifaximin, antidepressants
  2. Laxatives, lubiprostone, antidepressants
  3. Loperamide, antidepressants, rifaximin, alosetron
51
Q

Drugs used for IBD

A
  1. Inflammatory suppressors
  2. Immunomodulators
  3. Biologicals
52
Q

Drugs used for IBD:
Inflammatory suppressors

*specific uses

A
  1. 5-ASA: mesalamine, sulfasalazine
    * mild to moderate UC, induce and maintain remission, RA
  2. Oral corticosteroids: budesonide, prednisone
    * only used short term to induce remission
    * more potent than 5-ASAs
53
Q

This drug, used for IBD, is also used in Crohn disease

A

Budesonide

54
Q

Drugs used for IBD:
Immunomodulators

*specific uses

A
  1. 6-mercaptopurine
    * used to maintain remission of UC and CD
  2. Methotrexate
  3. Cyclosporine
  4. Tacrolimus
55
Q

Drugs used for IBD:

Biologicals

A
  1. Infliximab (anti TNF-alpha)
    * moderate to severe UC or CD
  2. Natalizumab (anti alpha4 integrin)
  3. Ustekinumab (interleukin 12/23 inhibitor)
56
Q

MOA:
Peripheral-increase gastro-esophageal peristalsis and LES pressure
Central-block D2 receptors in CTZ

*Uses?

A

Prokinetic agents (D2 receptor antagonists)

*gastroparesis, nausea, and vomiting

57
Q

MOA:
Absorb water into fiber leading to increased fecal volume, thus promoting peristalsis and bowel evacuation

*uses?

A

Bulk-forming laxatives

*prevent constipation

58
Q

MOA:
Permit water and lipids to penetrate feces or lubricate stool

*uses?

A

Stool surfactant agents

*prevent constipation in patients who should avoid strain

59
Q

MOA:
Draw water into intestine and colon, increase fecal fluid, and stimulate colonic peristalsis

*uses?

A

Osmotic laxatives

  • treat acute constipation or prevent chronic constipation
  • bowel prep
60
Q

MOA:
Stimulate smooth muscle contraction, increase colonic electrolyte and fluid secretion

*uses?

A

Stimulant laxatives

  • same as osmotic lax. but more potent:
  • treat acute constipation or prevent chronic constipation
  • bowel prep
61
Q

MOA:
Stimulate type 2 chloride channel in small intestine thus increasing chloride-rich fluid secretion

*uses?

A

Chloride channel activator

*chronic constipation

62
Q

MOA:
Block intestinal “mu” receptors leading to increased intestinal motility

*uses?

A

Opioid receptor antagonists

*opioid-induced constipation

Block 1 - GI (15 decks)

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