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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.