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Lecture 4 Antiemetics Nov 5 (1)

The document discusses the physiological causes of nausea and vomiting, detailing various classes of antiemetic agents and their mechanisms of action. It highlights specific drug examples such as Ondansetron, Metoclopramide, and Prochlorperazine, along with their indications and side effects. Additionally, it addresses the use of antiemetics in pregnancy, recommending non-pharmacological methods and safe pharmacological options like Pyridoxine.

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6 views11 pages

Lecture 4 Antiemetics Nov 5 (1)

The document discusses the physiological causes of nausea and vomiting, detailing various classes of antiemetic agents and their mechanisms of action. It highlights specific drug examples such as Ondansetron, Metoclopramide, and Prochlorperazine, along with their indications and side effects. Additionally, it addresses the use of antiemetics in pregnancy, recommending non-pharmacological methods and safe pharmacological options like Pyridoxine.

Uploaded by

sandynicolegella
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Drug affecting the nervous system

Sara Wong
BPharm; MSc Clinical Pharm Drug action and use of medicines II
Registered Pharmacist (H.K.)
OVERV
IEW
 Physiological cause of nausea and vomiting

 Antiemetic agents : Drug classes, Indications

 Drug examples of antiemetic agents : Ondansedron (most potent)

 Metoclopramide (commonly used in HK)

 Dimenhydrinate, Cinnarizine (for travel sickness)

 Prochlorperazine (associated with more SE :


drowsiness, tremor)

 Nausea and vomiting in pregnancy


Vomiting centre (VC) in medulla 3
(lower part of the brainstem)

2
Four pathways stimulate VC to trigger vomiting:
1) Vestibular nerves (inner ear)
Vomiting centre
2) Visceral nerves ( GIT )
3) Cerebral cortex ( smell, sight, thought )
4) Chemoreceptor trigger zone (CTZ) : to detect toxic substances in
blood
(4)
1) Vestibular nerves (inner ear) NAUSEA & VOMIT
2) Visceral nerves (GIT ) (3)
3) Cerebral cortex (smell, sight, thought)
4) Chemoreceptor trigger zone (CTZ)(1)

vomiting centre

In these 4 pathways:
(2)
Dopamine-2 receptors
5-HT3 receptors
Opioid receptors
It is the stimulation of these receptors that
Cholinergic receptors activate the vomiting centre and trigger
vomiting
Histamine H1 receptors

•Antiemetic agents stop vomiting by blocking these receptors


 Antiemetics drug classes: (act by blocking receptors in the pathways)
ANTIEMETI
CS
 5-HT3 receptor antagonists : most potent

 Dopamine D2 Antagonist

 Prokinetic agent

 Corticosteroids

 Antihistamines

 Anticholinergics

 Indications :

 Postoperative N & V

 Chemotherapy induced vomiting

 Radiotherapy induced vomiting

 Motion sickness (or travel sickness)


ANTIEMETIC AGENTS
5-HT3 SEROTONIN RECEPTOR
ANTAGONISTS

 most potent antiemetics eg. Ondansetron

MOA:
1- Peripheral 5-HT3 receptor blockade in GIT
2- Central 5-HT3 receptor blockade in the vomiting center and chemoreceptor trigger
zone

Indication:
Chemotherapy induced nausea & vomiting – given 30 min. before chemotherapy.
Postoperative & post-radiation nausea & vomiting

administration route : oral, IV


SE: Headache, constipation

Expensive !!
PROKINETIC
AGENT

Prokinetic means to enhance GI motility

Drug examples: Metoclopramide (very commonly used in HK)

 Domperidone

MOA:

1) Prokinetic action: enhances GIT motility by increasing the frequency of contractions
in small intestine
2) Blockage of D2 receptor in the CTZ in CNS

Domperidone – oral ; Metoclopramide – oral & IV

Metoclopramide SE: tremor, drowsiness


DOPAMINE D2
ANTAGONIST

 Drug examples : Prochlorperazine (commonly used in H.K.)

 MOA: the blockage of D2 receptors in the CNS

 SE: tremor, sedation, dizziness, blurred vision

 Not recommended as first–line agent for treating vomiting


ANTIHISTAMINE
S

 Drug examples : Dimenhydrinate, Diphenhydramine, Cinnarizine, Cyclizine,

 MOA: they block H1 histamine receptors (they also block cholinergic receptors)

 most effective for motion (or travel) sickness

 SE: drowsiness, anticholinergic effects


USE OF ANTIEMETIC IN PREGNANCY

 Non–pharmacological methods (often recommended):

 Rest

 Emotional support & acupressure.

 Frequent small meals with avoidance of spicy or fatty foods

 Increasing high-protein snacks are recommended

 Pharmacological management :

 Pyridoxine (vit B6) has been shown to be safe and effective treatment in reducing
severe vomiting

 Ginger may be considered in mild vomiting.

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