Rimonabant (Zimulti, Akomplia)

Rimonabant is a drug for treatment of obesity, antagonist of cannabinoid receptors. Rimonabant is issued under trademarks of Akomplia and Zimulti. In Russia, Ukraine, EU countries and the USA permission to use of rimonabant either isn't received, or is withdrawn.

Effects

According to the world association of dietarians the weight of patients of patients with obesity for a year of systematic administration of drug was lost for 5%.

Much attention is paid to the endocannabinoidsystem taking the main part in a pathogenesis of a morbidly obesity now. Close dependence of receptors of endocanabioid with biologically active agents of visceral fatty tissue is taped. The regulating role of endocannabinoid system in formation of appetite and types of alimentary behavior is proved.

At the use of nutrition tasty, high-caloric and rich with fats in a hypothalamus there is a hyper activation of endocannabinoid system that conducts to augmentation of appetite and intensifying of fat appearance, and saturation and wasting of energy respectively decrease. Greasy food enlarges availability of polyunsaturated fatty acids to a biosynthesis of endocannabinoid that also leads to a hyperactivity of endocannabinoid system. Please pay attention to Tiramin.

At an obesity of endocannabinoid system becomes excessively active. It stimulates alimentary behavior, operating on the CNS level, and induces adiposity, operating on the level of adiposities.

Receptors of endokannabinoid system of the first type (CB1) receptors of the second type (CB2) in the 1993rd were open in 1990. CB1-receptors are located in a brain (in a hypothalamus, bark of big hemispheres, basal ganglia, a cerebellum, a brain trunk) and on the periphery (in adiposities, digestive tract), they are also found in a myocardium, an endothelia of tanks and the sympathetic nervous terminations. CB2-receptors are located in lymphoid fabric and macrophages and play an important role in regulation of immune system of an organism. Endocannabinoidn system is activated "on demand" in response to irritation, upon termination of effect of an endocannabinoid quickly fail .

Endokannabinoid system plays a role of one of key regulators of arrival and digestion of food. At patients with obesity the endocannabinoid system is over stimulated by excess of food that carries to constant framing of endocannabinoid: at the level of TsNS (a hypothalamus and the arc kernel) there is a pathological activation of appetite, on the periphery — stimulation of processes of lipogenez .

Application and doses

Accept rimonabant 20 mg of 1 times a day not later than an hour to food and not earlier than through 3 later

Researches

Now seven multicenter clinical trials devoted to the medicine influence study rimonobant locking endocannabinoid receptors are abroad conducted. These receptors are located at hypothalamic centers of hunger, kernel and on the surface of adiposities. They are activated under the influence of an arakhidonilglitserol, anandamid and other derivatives of arakhidon acid that is followed by increase in appetite, gain of synthesis of triglycerides and lowering of synthesis of adiponectin in adipocytes. Stimulation the endocannabinoid receptors in the sub tentorialnykh acumbicheskikh kernels leads to formation of nicotine addiction at is long the smoking patients. Rimonobant applied in a daily dose from 5 to 20 mg a day.

Results

For 1 year of treatment this drug lost weight on average on 6,6 kg (RIO-Europa), reduced waist volume by 8,5 cm (RIO-North America), authentically reduced the level of triglycerides and lipoproteins of low density in plasma (RIO-Lipid), allowed to overcome nicotine addiction and to stop smoking without ricochet increase of the weight (STRATUS-US). Due to adiponectin synthesis stimulation the rimonobant lowered an index of insulin resistance by 41% and led to normalization of carbohydrate metabolism at patients with a high glycemia on an empty stomach and with the broken tolerance to a glucose (RIO-Diabetes). Considering the listed above results of clinical trials of rimonobant, it is possible to assume that this drug will be included in the list of the medicines recommended for treatment of an obesity in the nearest future.

After carrying out repeated clinical tests it became clear that more than 70% experimental had signs of suicidal thoughts, and two committed suicide. Also were observed apoplectic seizures, multiple sclerosis, violence cases in families of some patients.