Quercetin

Pharmacological properties

quercetin, which is part of the drug, exhibits the properties of a modulator of the activity of various enzymes involved in the degradation of phospholipids (phospholipases, phosphogenases, cogs), which affect free radical processes and are responsible for the biosynthesis of nitric oxide, proteinases, and other inhibitory effects of quercetin on membranotropic enzymes and above all, 5-lipoxygenase affects the inhibition of the synthesis of leukotrienes ltc4 and ltb4. Along with this, quercetin dose-dependently increases the level of nitric oxide in endothelial cells, which explains its cardioprotective effect in ischemic and reperfusion myocardial lesions. Corvitin also exhibits antioxidant and immunomodulating properties, reduces the production of cytotoxic superoxidanion, normalizes the activation of the subpopulation composition of lymphocytes and reduces their activation level. inhibiting the production of anti-inflammatory cytokines of interleukins (sludge) -1β and -8, helps to reduce the volume of necrotic myocardium and enhance reparative processes.

The mechanism of protective action is also associated with the prevention of an increase in the concentration of intracellular calcium in platelets and the activation of aggregation with inhibition of thrombogenesis.

The drug restores regional blood circulation and microcirculation without noticeable changes in vascular tone, increasing the reactivity of microvessels.

Corvitin normalizes cerebral hemodynamics in ischemic lesions, reduces the coefficient of asymmetry of cerebral blood flow in ischemic stroke.

Pharmacokinetics Clinical studies involving healthy volunteers. The therapeutic efficacy of Corvitin is due to the pharmacological effects of quercetin (free, total, conjugated) and its active metabolites (free, total and conjugated isoramnetin). Free quercetin is conjugated by 32.5% within 20 minutes after administration. Isoramnetin undergoes conjugation by 70% for 25-30 minutes. T_max total and free quercetin - 0.25 h, T_max free isoramnetin - 0.27 hours

T_½ free quercetin is 1.08 hours, free isoramnetin - 0.18 hours, T_½ total quercetin, conjugated quercetin, total isoramnetin, conjugated isoramnetin and the total concentration of quercetin and isoramnetin are significantly higher (6.92; 6.90; 4.39; 4.40; 5.80 h, respectively). Moreover, K_el quercetin and its metabolites show inversely proportional values. Highest C_max registered in the total concentration of quercetin and isoramnetin and amounted to 3870.9 ng / ml, the lowest indicator C_max observed in free isoramnetin (251.6 ng / ml). After parenteral administration, Corvitin is excreted in the urine in the form of conjugates of quercetin and isoramnetin.

Thus, the following can be considered as pharmacokinetic parameters of the drug:

Indications

• Combined therapy for acute violation of coronary circulation and myocardial infarction; complex therapy for decompensation of chronic heart failure; complex therapy for acute ischemic cerebrovascular accident (ischemic stroke, transient ischemic attack) and chronic ischemic diseases of the brain; treatment and prevention of reperfusion syndrome in the surgical treatment of patients with obliterating atherosclerosis of the abdominal aorta and peripheral arteries. ●

Application

Cooking solution

The solution is prepared in two stages:

Stage 1 - for the initial dilution of the drug, 0.9% sodium chloride solution in the amount of 15 ml is injected with a syringe into the vial with Corvitin, shake the vial until the lyophilized powder is completely dissolved.

2nd stage - transfer the resulting solution to a container with 0.9% sodium chloride solution, the total volume of the finished solution is 50-100 ml, depending on the indications.

If it is necessary to introduce 1 g of Corvitin, the initially diluted preparation of two vials should be transferred to a container with 0.9% sodium chloride solution; the total volume of the prepared solution is 50-100 ml.

Do not mix with other solutions and the drug