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Gastroenterology4 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What are the pharmacokinetic properties and mechanisms of action of drugs used in bowel motility disorders?

A

They vary by class and subclass but share a common thread in their clinical applications.

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2
Q

What should students be able to do after completing the preparation materials?

A

Describe pharmacokinetic properties, relate clinical applications, and correlate adverse effects of bowel motility drugs.

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3
Q

Name the types of disorders related to gut motility.

A
  • Impaired gastric emptying / Ileus
  • Diarrhea
  • Constipation
  • Irritable bowel syndrome (IBS)
  • IBS-C
  • IBS-D
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4
Q

What are the classes of drugs for disorders of gut motility?

A
  • Prokinetic agents
  • Antidiarrheals
  • Laxatives
  • Antispasmodics
  • Antibiotics
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5
Q

What is the mechanism of action of prokinetic agents like Metoclopramide?

A

Antagonism of dopamine’s inhibitory effect on myenteric motor neurons.

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6
Q

List some uses of Metoclopramide.

A
  • Diabetic gastroparesis
  • Post-pyloric enteral tube placement
  • Radiologic exam of stomach
  • Chronic intestinal pseudo-obstruction
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7
Q

What are the adverse effects of Metoclopramide?

A
  • Depression
  • Dizziness
  • Sedation
  • Extrapyramidal side effects
  • Tardive dyskinesia
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8
Q

True or False: Domperidone crosses the blood-brain barrier.

A

False

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9
Q

What are the effects of Erythromycin as a motilin receptor agonist?

A
  • Stimulates motilin receptors
  • Induces high amplitude propulsive contractions
  • Effective in gastroparesis
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10
Q

What are the possible adverse effects of Erythromycin?

A
  • Small bowel spasms
  • Vomiting
  • QT interval prolongation
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11
Q

Fill in the blank: _______ is a cholinesterase inhibitor that enhances contractile effects of ACh.

A

Neostigmine

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12
Q

What is the mechanism of action of mu Opioid Receptor (MOR) agonists in treating diarrhea?

A

Stimulate peripheral MORs on enteric nerves and GI epithelial cells.

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13
Q

List the therapeutic uses of Bismuth subsalicylate.

A
  • Nausea and vomiting
  • Mild, nonspecific diarrhea
  • Traveler’s diarrhea
  • H. pylori eradication
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14
Q

What are some risk factors for serious adverse drug effects in bowel motility treatments?

A

Specific risk factors vary by drug class and mechanism of action.

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15
Q

What are the main dopaminergic pathways of the brain?

A
  • Mesocortical pathway
  • Mesolimbic pathway
  • Nigrostriatal pathway
  • Tuberoinfundibular pathway
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16
Q

What is a potential adverse effect of high doses of Loperamide?

A

QTc prolongation leading to ventricular arrhythmia.

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17
Q

What is the role of serotonin in the mechanism of bowel motility?

A

Mucosal stimulation leads to release of serotonin which excites intrinsic primary afferent neurons.

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18
Q

Fill in the blank: The chemoreceptor trigger zone is located at the caudal end of the _______.

A

fourth ventricle

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19
Q

What is the primary action of bismuth subsalicylate?

A

Antisecretory effects, anti-inflammatory effects, antimicrobial action, coats and protects intestinal mucosa, adsorbs intestinal toxins or microorganisms

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20
Q

List the therapeutic uses of bismuth subsalicylate.

A
  • Nausea and vomiting
  • Mild, nonspecific diarrhea
  • Traveler’s diarrhea
  • H. pylori eradication
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21
Q

What are common side effects of bismuth subsalicylate?

A
  • Impaction
  • Dark stools (harmless)
  • Black tongue (harmless)
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22
Q

True or False: Bile acid sequestrants form a nonabsorbable complex that is excreted in the urine.

A

False

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23
Q

What conditions are treated with bile acid sequestrants?

A
  • Bile salt-induced diarrhea
  • Inflammatory bowel disease
  • Irritable bowel syndrome-diarrhea
  • Post-colectomy
  • Radiation therapy of abdomen
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24
Q

What are the potential adverse effects of bile acid sequestrants?

A
  • Bloating
  • Flatulence
  • Constipation
  • Fecal impaction
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25
Q

What is the mechanism of action of octreotide?

A

Inhibits secretion of GI hormones such as serotonin, gastrin, VIP, insulin, glucagon, secretin, motilin, and pancreatic polypeptide

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26
Q

What are the therapeutic uses of octreotide?

A
  • Severe secretory diarrhea caused by carcinoid tumors
  • Gastroenteropancreatic tumors
  • VIP-secreting tumors (VIPomas)
  • Acromegaly
  • Variceal and upper GI bleeding
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27
Q

What is the onset time for bulk-forming laxatives?

A

12-72 hours

28
Q

Fill in the blank: Docusate salts are classified as _______.

A

Stool softeners

29
Q

What is the primary action of osmotic agents like PEG 3350?

A

Osmotically draws water into the lumen

30
Q

What is the mechanism of lactulose in the management of hepatic encephalopathy?

A

Acidifies pH in colon, shifts NH3 to NH4+, inhibits diffusion of NH3 from colon to circulation

31
Q

What are the cautions associated with saline laxatives?

A
  • Magnesium toxicity
  • Renal impairment
  • Neuromuscular disease (Myasthenia gravis)
  • Acute phosphate nephropathy
32
Q

What are the main classes of laxatives?

A
  • Bulk-forming laxatives
  • Stool softeners
  • Osmotic laxatives
  • Stimulant laxatives
  • Peripherally acting mu-opioid receptor antagonists
33
Q

What are the primary uses of peripherally acting mu-opioid receptor antagonists?

A
  • Opioid-induced constipation in cancer pain
  • Chronic non-cancer pain
  • Post-operative ileus
34
Q

What are the adverse effects of linaclotide and plecanatide?

A
  • Diarrhea
  • Dehydration
35
Q

True or False: Guanylate cyclase 2C agonists increase intestinal fluid and motility.

A

True

36
Q

What is Tenapanor’s mechanism of action?

A

Inhibits NHE3 on enterocytes, reduces dietary Na+ and water absorption

37
Q

What is the primary action of lubiprostone?

A

Activates chloride channel type 2 (ClC-2) to increase chloride-rich fluid secretions

38
Q

What are common adverse effects of lubiprostone?

A
  • Nausea
  • Abdominal pain
  • Diarrhea
  • Flatulence
  • Headache
  • Dyspnea
39
Q

What is the mechanism of action for Chloride channel activators?

A

Activates chloride channel type 2 (ClC-2) on apical aspect of GI epithelial cells

This activation leads to increased chloride-rich fluid secretions, softening stool, increasing motility, and promoting spontaneous bowel movements.

40
Q

List two adverse effects of Chloride channel activators.

A
  • Nausea
  • Abdominal pain
41
Q

What is Prucalopride classified as?

A

5-HT4 Receptor Agonist

It is indicated for severe, refractory cases.

42
Q

What is the elimination route for Prucalopride?

A

Excretion: Urine (unchanged mainly)

It has a half-life of approximately 24 hours.

43
Q

What conditions is Prucalopride used to treat?

A
  • Chronic Idiopathic Constipation (CIC)
  • Opioid-induced chronic constipation
44
Q

True or False: Tegaserod is currently available on the market.

A

False

Tegaserod was withdrawn from the market due to safety concerns.

45
Q

What neurotransmitter release is enhanced by the activation of 5-HT4 receptors?

A
  • Acetylcholine (ACh)
  • Calcitonin gene-related peptide (CGRP)
46
Q

What are the indications for Alosetron?

A

Used in adult females only with severe diarrhea and chronic IBS symptoms

Generally for patients who have failed to respond to other therapies.

47
Q

Fill in the blank: The mechanism of Eluxadoline involves mixed ______ receptor actions.

A

opioid

48
Q

List two key therapeutic uses of Octreotide.

A
  • Inhibit severe secretory diarrhea
  • Treatment of acromegaly
49
Q

What is the mechanism of action for Loperamide?

A

Activates mu opioid receptors in the enteric nervous system

This action slows motility.

50
Q

What type of laxative is PEG 3350 classified as?

A

Osmotic agent

It increases water content of stool.

51
Q

What is the primary action of bulk-forming laxatives?

A

Absorb water to increase volume and stimulate evacuation.

52
Q

What is the mechanism of action for Methylnaltrexone?

A

Blocks intestinal mu opioid receptors but does not enter CNS.

53
Q

What are the adverse effects of Eluxadoline?

A
  • Constipation
  • Nausea
54
Q

What is the role of serotonin (5-HT) in gastrointestinal function?

A

Stimulates submucosal intrinsic primary afferent neurons (IPANs) via 5-HT1P receptors.

55
Q

List two adverse effects associated with Alosetron.

A
  • Ischemic colitis
  • Complications of constipation
56
Q

What is the therapeutic use of Lubiprostone?

A
  • IBS-C
  • Chronic Idiopathic Constipation
  • Opioid-induced constipation
57
Q

What is the mechanism of action for Stimulant laxatives like bisacodyl?

A

Direct action on intestinal mucosa and nerve plexus to stimulate peristalsis.

58
Q

True or False: Octreotide is only administered orally.

A

False

It can be administered via I.V., subcutaneous, intramuscular long-acting release suspension, and oral delayed-release capsules.

59
Q

What is the primary use of Alosetron?

A

Severe diarrhea with chronic IBS symptoms in adult women who have failed to respond to other therapies

Alosetron is a 5-HT3 receptor antagonist that is potent and reduces gastrointestinal transit, secretions, and visceral pain.

60
Q

What are the serious adverse effects of Alosetron?

A

Ischemic colitis and complications of constipation

These serious adverse effects are rare but significant.

61
Q

What condition does the drug that reduces diarrhea and pain primarily treat?

A

IBS-D with severe diarrhea refractory to all other therapies

This indicates a specific type of Irritable Bowel Syndrome characterized by diarrhea.

62
Q

What are some adverse effects associated with the use of the drug that reduces diarrhea and pain?

A

Sphincter of Oddi spasm; pancreatitis; several contraindications

These adverse effects highlight the potential risks involved in using the medication.

63
Q

According to Sydney Smith, what contributes significantly to unhappiness in the world?

A

Little stoppages, a duct choked up, food pressing in the wrong place

This quote emphasizes the importance of gastrointestinal health in overall well-being.

64
Q

Who is AT Stills and what was his contribution to health?

A

Founder of osteopathy; believed correcting structural imbalances can alleviate health problems

His views highlight the interconnection between physical structure and health outcomes.

65
Q

Fill in the blank: Alosetron is a _______ receptor antagonist.

A

5-HT3

66
Q

True or False: Alosetron is indicated for use in adult men with IBS-D.

A

False

Alosetron is specifically indicated for adult women.

Gastroenterology4 (8 decks)

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