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GI Final > Antiemetic Drugs > Flashcards

Antiemetic Drugs Flashcards

1
Q

What are the seven types of Antiemetic Drugs?

A

Serotonin (5HT3) Antagonists, Anticholinergics, Neurokinin Receptor 1 (NK1) Antagonists, Anithistamines (H1), Dopamine (D2) receptor antagonists, Cannabinoids, Corticosteroids

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2
Q

What are the four Serotonin (5HT3) drugs?

A

Dolasetron, Granisetron, Ondansetron, Palonosetron

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3
Q

What is the MOA of Serotonin (5HT3) Antagonists?

A

Blockage of peripheral 5HT3 receptors on primary afferent. Also acts in CTZ (chemoreceptive trigger zone) and VC (vomiting center)

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4
Q

What is the therapeutic use for Serotonin (5HT3) Antagonists?

A

Drugs of choice for preventing and inhibiting chemotherapy-induced N/V, Prevent acute phase (less than 24 hours after infusion) if given 30 min prior to chemo. Also used post op and post radiation.

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5
Q

What are the side effects of Serotonin (5HT3) Antagonists?

A

Well tolerated. Excellent safety profiles. Esp. compared to Alosetron. Most SE are transient (constipation, dizziness, HA). Small QT elongation.

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6
Q

What drug is truly effective for prevention of chemo emesis (esp. caused by Cisplatin)?

A

Ondansetron

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7
Q

What are Serotonin (5HT3) Antagonists NO effective for?

A

Not as effective at delayed (2-5 days) of chemo or for motion sickness.

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8
Q

What Anticholinergic should you know?

A

Scopolamine

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9
Q

What is the MOA of Anticholinergics?

A

Muscarinic and cholinergic receptor antagonists. Esp. at cerebellum. Widely distributed in CNS.

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10
Q

What is the therapeutic use of Scopolamine?

A

Motion sickness (most effective)

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11
Q

What are the side effects of Scopolamine?

A

Given as transdermal patch to dec. systemic side effects compared to oral.

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12
Q

What Neurokinin Receptor 1 (NK1) Antagonists should you know?

A

Aprepitant (oral), Fosaprepitant (IV)

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13
Q

What is the MOA for NK1 Antagonists?

A

Antagonize substance P receptor. Central higher order center - NK1 receptors.

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14
Q

What is the therapeutic use of NK1 Antagonists?

A

Chemotherapy induced N/V. Given in combo with 5HT3 receptor antagonists and dexamethasone.

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15
Q

What are the side effects of NK1 Antagonists?

A

Well tolerated. Fatigue, dizziness, diarrhea. Metabolized by CYP3A4 (chemo drugs also metabolized so increases bone marrow suppression)

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16
Q

What Antihistamines (H1) do you need to know?

A

Dimenhydrinate, Diphenhydramine, Meclizine

17
Q

What is the MOA for Antihistamines (H1)?

A

Sedation. H1 may not be the primary mechanism (might be antimuscarinic effects)

18
Q

What is the therapeutic use of Antihistamines (H1)?

A

Antiemetic

19
Q

What are the side effects of Antihistamines (H1)?

A

Anticholinergic –> confusion, dry mouth, etc. Interaction with antibiotics. Not to be used in pregnancy.

20
Q

What are the Dopamine (D2) receptor antagonists you need to know?

A

Droperidol, Metochlopramide, Prochlorperazine, Promethazine, Thiethylperazine

21
Q

What is the MOA for Dopamine (D2) Receptor Antagonists?

A

D2 receptors in CTZ (muscarinic?) antagonism. “Reset” GI motility. Sedation.

22
Q

What are the side effects for Dopamine (D2) Receptor Antagonists?

A

Sedation.

23
Q

What are the two Cannabinoids you need to know?

A

Dronabinol, Nabilone

24
Q

What is the MOA for Cannabinoids?

A

Mimics THC at central cannabinoid receptors. May be sedation.

25
Q

What are side effects of Cannabinoids?

A

Euphoria, sedation, hallucinations, dry mouth. Increased appetite (good for cancer patients)

26
Q

What are cannabinoids given with?

A

Phenothiazines

27
Q

Why aren’t cannabinoids used much?

A

There are better agents available now for cancer therapy.

28
Q

What two corticosteroids do you need to know?

A

Dexamethasone and Methylprednisolone

29
Q

What is the MOA for corticosteroids and antiemesis?

A

Mechanism in emesis is unknown.

30
Q

What are corticosteroids used with?

A

5HT3 antagonists

GI Final (9 decks)

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