Table 4. Receptor site affinity of available antiemetic drugs.
| Drug group | Dopamine
(D2) |
Muscarinic
cholinergic |
Histamine
(H2) |
Serotonin
(5-HT3) |
NK-1
antagonist |
CB-1
modulator |
MOR
antagonist |
Gaba
mimetic |
|---|---|---|---|---|---|---|---|---|
| Antiserotonin | ||||||||
| Ondansetron | - | - | - | ++++ | - | - | - | - |
| Granisetron | - | - | - | ++++ | - | - | - | - |
| Tropisetron | - | - | - | ++++ | - | - | - | - |
| Palonosetron | - | - | - | ++++ | - | - | - | - |
| Phenothiazines | ||||||||
| Fluphenazine | ++++ | + | ++ | - | - | - | - | - |
| Chlorpromazine | ++++ | ++ | ++++ | + | - | - | - | - |
| Butyrophenones | ||||||||
| Droperidol | ++++ | - | + | + | - | - | - | - |
| Haloperidol | ++++ | - | + | - | - | - | - | - |
| Domperidone | ++++ | - | - | - | - | - | - | - |
| Antihistamines | ||||||||
| Diphenhydramine | + | ++ | ++++ | - | - | - | - | - |
| Promethazine | ++ | ++ | ++++ | - | - | - | - | - |
| Anticholinergics | ||||||||
| Scopolamine | + | ++++ | + | - | - | - | - | - |
| Benzamides | ||||||||
| Metoclopramide | +++ | - | + | ++ | - | - | - | - |
| Tricyclic antidepressants | ||||||||
| Amitriptyline | +++ | +++ | ++++ | - | - | - | - | - |
| Nortriptyline | +++ | ++ | +++ | - | - | - | - | - |
| Neurokinin-1 | ||||||||
| Aprepitant | - | - | - | - | ++++ | - | - | - |
| Fosaprepitant | - | - | - | - | ++++ | - | - | - |
| Others | ||||||||
| Dronabinol | - | - | - | - | - | ++++ | - | - |
| Nabilone | - | - | - | - | - | +++ | - | - |
| Naloxone | - | - | - | - | - | - | ++++ | |
| Lorazepam | - | - | - | - | - | - | - | +++ |
The number of positive signs (+) indicates receptor activity.
This table was adapted with permission from White PF (ed). Ambulatory Anesthesia and Surgery. London, WB Saunders, 1997 Page 442 133