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Best Practice & Research Clinical Endocrinology & Metabolism Use Of Cannabinoid CB1 Receptor Antagonists For The Treatment Of Metabolic Disorders
Cannabinoids are naturally occurring chemical compounds that are found in the cannabis plant (cannabis sativa). Cannabidiol (CBD) is one of these chemicals and studies have shown it has anti-inflammatory effects when induced on animal cells. People have smoked the marijuana plant for thousands of years and it has said have an anti-inflammatory role in the body. Tetrahydrocannabinol (THC) is another one of these chemicals. It contains psychoactive effects which are associated with cannabis users becoming “high”. Major cannabinoid receptors (CB1 and CB2) are found in the endocannabinoid system and allow exogenous and endogenous cannabinoids to thrive in the body.
The specific CB1 receptor antagonist rimonabant has been seen to decrease body size, waist diameter, insulin battle, triglycerides, dense LDL, CRP and blood pressure, and to better HDL and adiponectin doses in both non-diabetic and diabetic overweight/obese subjects. Abdominal obesity is related to several metabolic disfigurements including:
Part of these metabolic syndromes may be connected to greater endocannabinoid activity.
Besides an advancement of glucose ableness in non-diabetic people, a 0.5-0.7% decrease in HbA1c levels was continuously seen in various groups of people with type 2 diabetes. Almost half of the metabolic alterations could not be described by weight loss, supporting direct peripheral impacts of rimonabant. Ongoing research should show whether improved metabolic syndromes with CB1 receptor antagonists (rimonabant, taranabant) would translate into less cardiovascular complications among high-risk subjects.
More and more reports indicate that CB1 receptor inducing is a novel therapeutic plan that targets most of the metabolic syndromes related to abdominal obesity, including type 2 diabetes and atherogenic dyslipidaemia. Clinical tests are already at the ready for rimonabant at a daily dosage of 20 mg but still remain to be published for taranabant.
Despite the fact that the initial advancement of the first available CB1 receptor antagonist rimonabant was produced as an anti-obesity drug (weight loss as the main endpoint in the RIO programme), available data displayed that metabolic improvements, especially the decreasing in HbA1c, the triglyceride decrease and the increase in HDL cholesterol levels, were almost twice that expected from the weight loss alone.
These results are consistent with the direct peripheral metabolic impacts of the drug seen in various animal models and open a new perspective for the regulation of overweight/obese patients whose residual cardiovascular risk remains high despite the use of other substances such as statin and antiplatelet therapies.CB1-antagonists-Metabolism-2008