Products
Cannabinoid receptor antagonists are no longer on the market in many countries. Rimonabant (Acomplia) was withdrawn from the market in 2008 because it can cause psychiatric disorders, particularly depression.
Effects
Cannabinoid receptor antagonists have appetite suppressant, lipid-lowering, antidiabetic, analgesic (antiallodynic, antinociceptive), and anti-inflammatory properties. The effects of cannabinoid receptor antagonists are largely opposite to those of cannabis. In clinical studies, the effects of cannabis could be antagonized with rimonabant.
| Cannabis | Rimonabant |
| Antiemetic | emetic, nausea is a common adverse effect |
| appetizing | appetite suppressant |
| analgesic | analgesic |
| muscle relaxant | Muscle cramps are an undesirable effect |
| Antispasmodic | Use with caution in patients prone to seizures |
| Antianxiety | Anxiety is a common adverse effect |
| mood elevating | Depressed mood is a common adverse effect |
Mechanism of action
Cannabinoid receptor antagonists abolish the effects of the endogenous endocannabinoids anandamide and 2-arachidonylglycerol at the cannabinoid receptor (CB). In the endocannabinoid system, two receptors exist CB
1
and CB
2
. The endocannabinoid system is a physiological system that, in neurons of the mesolimbic system, stimulates, among other things, the intake of highly palatable, sweet, or fatty foods. The system is localized in the central nervous system and peripheral tissues including adipocytes and influences energy balance, glucose and lipid metabolism, and body weight.
Indications
Rimonabant was approved for the treatment of overweight and obesity. Cannabinoid receptor antagonists have also been studied in smoking cessation, alcohol dependence, opioid dependence, and cocaine dependence, among others.
