Receptor site affinities

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Receptor site affinities of selected anti-emetics

 

D2 antagonist

H1 antagonist

Muscarinic antagonist

5HT2 antagonist

5HT3 antagonist

NK1 antagonist

5HT4 agonist

CB1 agonist

GABA mimetic

Domperidone1

**

 

 

 

 

 

 

 

 

Haloperidol

***

 

 

*/-

 

 

 

 

 

Metoclopramide2

**

 

 

 

*

 

**

 

 

 

Cyclizine

 

**

**

 

 

 

 

 

 

Hyoscine
Hydrobromide

 

 

***

 

 

 

 

 

 

 

Chlorpromazine

***

***

**

**

 

 

 

 

 

Levomepromazine

**

***

**

***

 

 

 

 

 

Olanzapine

**

*

**

**

*

 

 

 

 

Prochlorperazine

***

**

*

*/**

 

 

 

 

 

Promethazine

*/**

**

**

 

 

 

 

 

 

 

Lorazepam

 

 

 

 

 

 

 

 

***

Nabilone

 

 

 

 

 

 

 

***

 

Aprepitant

 

 

 

 

 

***

 

 

 

Ondansetron/

Granisetron3

 

 

 

 

***

 

 

 

 

Pharmacological activity: blank = none or insignificant; * = slight; ** = moderate; *** = marked. 

domperidone:  does not normally cross the blood-brain barrier; minimal risk of extrapyramidal effects, watch for interactions.

metoclopramide: caution in use of prolonged higher doses, monitor for extrapyramidal side effects. 
3ondansetron/granisetron: consider interactions


Adapted from Twycross, R, Wilcock, A and Howard, P (eds) Palliative Care Formulary 5th Edition 2014.

 

Receptor site chart

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