Included in the formulation
АТХ:C.09.X.A.02 Aliskiren
Pharmacodynamics:Selective inhibitor of renin of non-peptide structure, blocks the conversion of angiotensin into angiotensin I, reducing the plasma renin level, angiotensin I and angiotensin II.
Renin is excreted by the kidneys with a decrease in renal perfusion and the volume of circulating blood. Once in the bloodstream, renin cleaves angiotensin to an inactive decapeptide of angiotensin I, which, in turn, with the help of an angiotensin-converting enzyme is converted into active octapeptide angiotensin II, which causes vasoconstriction and stimulates the release of adrenal catecholamines from the adrenal medulla, also enhances the reabsorption of sodium and aldosterone ions, which increases blood pressure. By increasing the level of angiotensin II there is an expression of markers and mediators of inflammation and fibrosis of the organ. In addition, angiotensin II inhibits the release of renin, adversely affecting the system. As a result, increased activity of renin leads to an increased risk of cardiovascular complications.
The action of inhibitors of renin leads to a compensatory increase in the concentration of renin in the blood plasma.The action of aliskiren neutralizes the feedback effect, which leads to a persistent decrease in plasma renin activity.
Pharmacokinetics:After oral ingestion, up to 2.5% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 1-3 hours. The equilibrium concentration in blood plasma is reached within 5-7 days after the start of the administration once a day, the equilibrium level is approximately 2 times higher than at the initial dose. The connection with plasma proteins is up to 50%.
Therapeutic effect develops after the reception. Metabolism in the liver.
The half-life is 40 hours. Elimination with feces, mostly unchanged.
Indications:It is used for the treatment of arterial hypertension.
IX.I10-I15.I15 Secondary Hypertension
IX.I10-I15.I10 Essential [primary] hypertension
Contraindications:Severe renal failure, hereditary angioedema, shock, individual intolerance, children under 18 years of age.
Carefully:Hypokalemia, hyponatremia, Renovascular hypertension, elderly age.
Pregnancy and lactation:Recommendations for FDA - Category C.Contraindicated in pregnancy and lactation.
Dosing and Administration:Inside, 150 mg once a day, regardless of food intake. With persistent arterial hypertension, it is possible to increase the dose to 300 mg per day.
The highest daily dose: 300 mg.
The highest single dose: 300 mg.
Side effects:Central and peripheral nervous system: dizziness.
The cardiovascular system: hypotension, peripheral edema.
Digestive system: diarrhea.
Dermatological reactions: hyperemia, toxic epidermal necrolysis, Stevens-Johnson syndrome, skin itching.
urinary system: impaired renal function.
Allergic reactions.
Overdose:Symptoms: marked reduction in blood pressure.Treatment is symptomatic.
Interaction:Clinically significant interactions are not described.
Special instructions:Monitoring of electrolyte composition of blood plasma and kidney function.