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.

1domperidone: does not normally cross the blood-brain barrier; minimal risk of extrapyramidal effects, watch for interactions.

2metoclopramide: 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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