Agents for Nausea & Vomiting Flashcards

1
Q

Name a major chemosensory area for emesis.

A

Chemoreceptor Trigger Zone (CTZ)

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2
Q

Where is the CTZ found?

A

Area postrema of the fourth ventricle of the brain

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3
Q

Name drug classes with examples of specific drugs that are effective in the treatment of nausea & vomiting.

A
  • Antihistamine-anticholinergics
  • Benzodiazepines
  • Butyrophenones
  • Cannabinoids
  • Corticosteroids
  • Phenothiazines
  • Substituted Benzamides-Metoclopramide
  • 5-HT3 receptor blockers
  • Neurokinin receptor blockers
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4
Q

How does metoclopramide work as an antiemetic?

A

Blocks D2 receptors centrally in the CTZ

  • Prokinetic
  • Increases resting tone, contactility, LES tone, & motility

Does NOT influence colon transport time

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5
Q

What are the DOC for treating emesis during pregnancy?

A

(Antihistamine-Anticholinergics Meclizine Cyclizine Promethazine

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6
Q

What antihistamine is often used to treat motion sickness?

A

Meclizine

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7
Q

What anticholinergic is often used to treat motion sickness? How is it normally administered?

A

Scopolamine Transdermal patch to prevent systemic anticholinergic effects

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8
Q

What medication is often used in combo regimens to enhance antiemetic activity?

A

Dexamethasone

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9
Q

What are the s/e of phenothiazine antiemetics?

A

Extrapyramidal symptoms Sedation Hypotension

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10
Q

Why doesn’t ondansetron cause extrapyramidal s/e?

A

Blocks 5-HT3 instead of dopamine receptors in the CTZ

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11
Q

What chemotherapy agent has one of the highest emetogenic potentials?

A

Cisplatin

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12
Q

What antibiotic has prokinetic properties for the GI tract?

A

Erythromycin, though tolerance to this effect develops rapidly, it’s usefulness is limited by its nausea & vomitting s/e

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13
Q

Give examples of Antihistamine-Anticholinergics used to treat nausea & vomiting

A
  • Diphenhydramine
  • Hydoxyzine
  • Meclizine
  • Cyclizine
  • Promethazine
  • Pyrilamine
  • Scopolamine
  • Trimethobenzamide
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14
Q

Give examples of Benzodiazepines used in the treatment of nausea & vomiting

A
  • Alprozolam
  • Diazepam
  • Lorazepam
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15
Q

Give examples of Butyrophenones used in the treatment of nausea & vomiting

A
  • Haloperidol
  • Droperidol
  • Domperidone
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16
Q

Give examples of cannabinoids used for the treatment of nausea & vomiting

A
  • Dronabinol
  • Nabilone
17
Q

What are the corticosteroids used to treat nausea & vomiting?

A
  • Dexamethasone
  • Methylprednisolone
18
Q

What phenothiazines are used to treat nausea & vomiting?

A
  • Prochlorperazine
  • Chlorpromazine
  • Perphenazine
19
Q

What substituted Benzamides are used for the treatment of nausea & vomiting?

A
  • Metoclopramide
20
Q

What 5-HT3 Receptor Blockers are POWERFUL CENTRAL-ACTING antiemetics?

What are some of their clinical uses?

A

”-setron

  • Ondansetron
    • At a party but feeling queasy? Keep ON DANCing with ONDANSetron!
  • Dolasetron
  • Granisetron

Clinical Use:

  • Control N&V postoperatively
  • pts undergoing chemotherapy
21
Q

What Neurokinin Receptor Blockers are used for the treament of nausea & vomiting?

A
  • Aprepitant (oral)
  • Fosaprepitant (IV formulation converted to aprepitant)
22
Q

Do synthetic cannabinoids have psychotropic activity?

A

No

23
Q

What is intractable emesis leading to dehydration & hypotension during pregnancy called?

A

Hyperemesis Gravidarum

24
Q

What are the s/e of cannabinoids?

A
  • Anxiety
  • Memory Loss
  • Confusion
  • Motor incoordination
  • Hallucinations
  • Euphoria
  • Relaxation
  • Hunger
  • Gynecomastia
25
Q

What OTC medication can be given in combo w metoclopramide to reduce its extrapyramidal s/e?

A

Metoclopramide is a D2 receptor blocker similar to typical anti-psychotics- EPS symptoms are due to central dopamine receptor blockade

Diphenhydramine can be used for its anticholinergic properties

Tardive Dyskinesia if it develops may be irreversible- therefore, metoclopramide should only be used for short-term therapy if possible

26
Q

What are the side effects associated with 5-H3 antagonists “-setron”?

A
  • Headache
  • Constipation
27
Q

What are the clinical uses of Metoclopramide?

A
  • Diabetic gastroparesis
  • Post-surgery gastroparesis
  • Anti-emetic
28
Q

What are the toxicities associated w Metoclopramide?

What are its contraindications?

A
  • increased Parkinsonian effects
  • Restlessness
  • Drowsiness, fatigue, Depression
  • Nausea & Diarrhea
  • Drug interaction w DIGOXIN & DIABETIC agents

Contraindications:

  • pts w SMALL BOWEL OBSTRUCTION
  • Parkingson’s Disease