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Anti-emetics
B. Dian Novita, dr., MKed.
diannovitakrisdianto@yahoo.co.id

General Classification of
Anti-emetic Agents

Receptor Specificity of
Anti-emetic Agents

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Serotonin 5 HT3 Antagonist 1

Serotonin 5 HT3 Antagonist 2

Potent antiemetics
Even though 5 HT3 receptors are present in

vomiting centre & CTZ, the antiemetic action is

restricted to emesis caused by vagal stimulation.
High first pass metabolism
Excreted by liver & kidney

can be administrated once a day

No dose reduction in renal insufficiency but needed

absorbed well from the GI tract.

Ondansetron is extensively liver metabolized by
CYP1A2, CYP2D6, and CYP3A4, followed by
glucuronide or sulfate conjugation

in hepatic insufficiency
Given once or twice daily orally or intravenously.

Granisetron is liver metabolized predominantly,

Indications

involve the CYP3A family, as it is inhibited by

ketoconazole.
Dolasetron is converted rapidly by plasma
carbonyl reductase to its active metabolite,
hydrodolasetron.

Chemotherapy induced nausea & vomiting given

Drugs Available

Excellent safety profile

Ondansetron

32 mg / day

Granisetron

10 mg / kg / day

Dolasetron

1.8 mg / kg / day

30 min. before chemotherapy.

Postoperative & postradiation nausea & vomiting

Adverse Effects
Headache & constipation
All three drugs cause prolongation of QT interval,

but more pronounced with dolasetron.

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Dopamine D2 Antagonist
Antagonise D2 receptors in CTZ.

Phenothiazines & Butyrophenones

Phenothiazines :

Prochlorperazine

Drugs available

Metoclopramide

Promethazine
Phenothiazines are antipsychotics with potent

Domperidone
Both drugs are also prokinetic agents due to their 5

HT4 agonist activity.

Domperidone oral ; Metoclopramide oral & i.v
Metoclopramide crosses BBB (w/extra pyramidal

effect)

antiemetic property due to D2 antagonism.

Butyrophenone :

Droperidol
Droperidol used for post-op. nausea & vomiting,

but cause QT prolongation.

H1 Antihistaminics
Most effective drugs for motion sickness
Drugs available

Anticholinergics
Scopolamine used as transdermal patch for

motion sickness

Dimenhydrinate

Cannabinoids

Diphenydramine
Promethazine Used in pregnancy, used by
NASA for space motion sickness

Dronabinol used as adjuvant in chemotherapy

induced vomiting.It is a psychoactive substance

Nabilone

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