Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antihypertensive agent, angiotensin II receptor antagonist. It blocks AT 1 -receptors, which leads to a decrease in the biological effects of angiotensin II (mediated by receptors of this type), incl. vasoconstrictive action, stimulating effect on the release of aldosterone, regulation of salt and water homeostasis, and stimulation of cell growth. Antihypertensive effect is due to a decrease in OPSS without a reflex increase in heart rate.
Does not inhibit ACE. It does not interact and does not block the receptors of other hormones or ion channels, which are important for the regulation of the functions of the cardiovascular system.
PHARMACOKINETICS
C max in blood plasma is achieved within 3-4 hours. The concentration in the plasma increases linearly with increasing dose in the therapeutic interval (up to 32 mg).V d - 0.13 l / kg. Binding to plasma proteins - 99.8%. It is slightly metabolized in the liver (20-30%) with the participation of CYP2C with the formation of an inactive metabolite.
The final T 1/2 - 9 hours. Does not cumulate. The total clearance is 0.37 ml / min / kg, with a kidney clearance of about 0.19 ml / min / kg. Candesartan is excreted by the kidneys (by glomerular filtration and active tubular secretion): 26% in the form of candesartan and 7% in the form of an inactive metabolite; with bile - 56% and 10%, respectively. After a single dose of 72 hours, more than 90% of the dose is withdrawn.
In elderly patients (over 65 years) C max and AUC increase by 50% and 80%, respectively, compared with young patients.
In patients with mild to moderate renal impairment, Cmax and AUC increase by 50% and 70%, respectively, whereas T 1/2 of the drug does not change as compared to patients with normal renal function.
In patients with severe renal dysfunction, C max and AUC increase by 50% and 110%, respectively, and T 1/2 increases by a factor of 2.
In patients with mild to moderate liver function abnormalities, AUC increased by 23%.
INDICATIONS
Arterial hypertension.
DOSING MODE
Take 1 time / day. The initial dose is 4 mg, the maintenance dose is 8 mg, the maximum dose is 16 mg.
For patients with impaired liver and / or kidney function, the initial dose is 2 mg.
SIDE EFFECT
From the side of the central nervous system: dizziness.
On the part of the respiratory system: cough, flu-like symptoms, rhinitis, pharyngitis, an increased incidence of respiratory infections.
From the digestive system: pain in the abdomen.
From the cardiovascular system: peripheral edema.
Other: back pain is possible.
CONTRAINDICATIONS
Severe hepatic insufficiency and / or cholestasis, pregnancy, lactation (breastfeeding), hypersensitivity to candesartan.
PREGNANCY AND LACTATION
Candesartan is contraindicated in pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
It is not recommended for patients with severe renal failure (QC less than 15 ml / min), with primary hyperaldosteronism.
When used in patients with renal insufficiency should periodically monitor the level of potassium and creatinine in the blood plasma.
For patients with impaired renal function, the initial dose is 2 mg.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe hepatic insufficiency.
For patients with impaired liver function, the initial dose is 2 mg.
SPECIAL INSTRUCTIONS
It is not recommended for patients with severe renal failure (QC less than 15 ml / min), with primary hyperaldosteronism.
Before starting treatment candesartan should be corrected violations of water-electrolyte balance.
When used in patients with renal insufficiency should periodically monitor the level of potassium and creatinine in the blood plasma.
Use with caution in patients with hemodynamic disorders due to aortic or mitral stenosis, with obstructive hypertrophic cardiomyopathy.
It should be borne in mind that in patients with ischemic cardiopathy, ischemic cerebrovascular diseases, severe arterial hypotension can lead to the development of myocardial infarction or stroke.
Impact on the ability to drive vehicles and manage mechanisms
If it is necessary to use in patients engaged in potentially hazardous activities (including driving), it should be borne in mind that candesartan can cause dizziness and weakness.
DRUG INTERACTION
With simultaneous use with potassium preparations, potassium-sparing diuretics, dietary supplements to food containing potassium, or potassium salt substitutes, it is possible to develop hyperkalemia.
Drugs that affect RAAS can increase the concentration of urea and creatinine in the blood in patients with bilateral renal artery stenosis or the artery of a single kidney. Simultaneous reception of diuretics and other antihypertensive drugs increases the risk of developing arterial hypotension.
Candesartan increases the concentration of lithium in the serum and increases the risk of developing toxic reactions.
