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. Has a central and peripheral action. Blocks postsynaptic? 1- adrenoreceptors, which reduces the OPSS. Regulates the central mechanism of maintaining vascular tone by stimulating the serotonin 5-HT1A receptors of the vasomotor center (prevents reflex increase in the tone of the sympathetic nervous system). Heart rate, cardiac output does not change. Low cardiac output may be increased by lowering the OPSS. Orthostatic phenomena do not cause. Stimulates presynaptic? 2- adrenoreceptors.
Reduces systolic and diastolic blood pressure, reducing OPSS, does not cause reflex tachycardia. Reduces pre- and afterload on the heart, increases the efficiency of cardiac contraction, thus (in the absence of arrhythmia) increases the reduced minute volume of the heart.
Does not affect the parameters of carbohydrate metabolism, the exchange of uric acid and does not cause fluid retention in the body.
PHARMACOKINETICS
After intravenous administration of 25 mg, a two-phase decrease in concentration is observed: first, a rapid (? -phase), then a slow (? -phase) decrease. The period of distribution of urapidil is 35 min, V d - 0.8 l / kg (0.6-1.2 l / kg). Binding to plasma proteins - 80%. Metabolised in the liver. The main metabolite is the hydroxylated derivative (in the 4 position of the benzene ring), it does not have antihypertensive activity. O-demethylated metabolite is formed in very small amounts and is also active, like urapidil. T 1/2 (after IV bolus administration) - 2.7 h (1.8-3.9 h). It is excreted by the kidneys - 50-70% in the form of unchanged substance and 15% - in the form of metabolites; through the intestine - in the form of metabolites (mainly in the form of inactive n-hydroxylated urapidil). In elderly patients and with severe hepatic and / or renal failure, V d and clearance are reduced, and T 1/2 is increased. It penetrates the GEB and the placental barrier.
INDICATIONS
Hypertensive crisis, refractory arterial hypertension, arterial hypertension of the third degree, controlled arterial hypotension during and / or after a surgical operation.
DOSING MODE
Enter into / in a jet or drip (long, in a prone position).
With hypertensive crisis, grade III arterial hypertension, refractory arterial hypertension: intravenously slowly 10-50 mg (under the control of blood pressure, the expected decrease in blood pressure within 5 minutes), it is possible to re-introduce. IV infusion (by drip or continuous) with a perfusion pump. The maintenance dose (on average) is 9 mg / h, i.e. 250 mg of urapidil in 500 ml of solution for infusion (1 mg = 44 drops = 2.2 ml). The maximum allowable ratio is 4 mg of urapidil per 1 ml of solution for infusion. The maximum initial speed is 2 mg / min (depending on blood pressure).
With controlled arterial hypotension (during and / or after surgery): continuous infusion (using a perfusion pump) or drip to maintain blood pressure, achieved with IV injection. With iv administration of 25 mg: if blood pressure drops after 2 minutes - transferred to infusion (6 mg for 1-2 minutes, then reduce the dose); if the blood pressure does not change after 2 minutes - repeatedly iv in 25 mg and with a decrease in blood pressure after 2 minutes - transferred to infusion (6 mg for 1-2 minutes, then reduce the dose); if the BP after a second injection after 2 minutes does not change - I / O slowly 50 mg and then, with a decrease in blood pressure after 2 minutes, transferred to infusion (6 mg for 1-2 minutes, then reduce the dose). If previously used other antihypertensives, then urapidil is administered after the time during which the previously administered remedy should act. The dose of urapidil should be adjusted.
In elderly patients, the initial dose should be reduced, compared with the recommended dose. Introduction can be single or multiple. Injections can be combined with subsequent drip infusion. Therapy is repeated with a second increase in blood pressure.
SIDE EFFECT
From the cardiovascular system: sometimes - palpitation, tachycardia, bradycardia, a feeling of compression behind the sternum, shortness of breath, arrhythmias.
From the digestive system: often - nausea; sometimes - vomiting.
From the side of the central nervous system: often - dizziness, headache, fatigue; very rarely - worry.
Dermatological reactions: sometimes - increased sweating.
Allergic reactions: rarely - skin itching, redness of the skin, exanthema.
From the urinary system: often - proteinuria; rarely - nephropathy, nephrotic syndrome.
On the part of the reproductive system: rarely - priapism.
Laboratory indicators: very rarely - thrombocytopenia.
CONTRAINDICATIONS
Aortic stenosis, open arterial duct, pregnancy, lactation, children and adolescents under 18, hypersensitivity to urapidil.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be used in patients with impaired renal function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Caution should be used in patients with impaired liver function.
APPLICATION IN ELDERLY PATIENTS
Caution should be used in elderly patients.
SPECIAL INSTRUCTIONS
C caution should be used in patients with impaired liver and / or kidney function, with hypovolemia, the elderly.
A sharp drop in blood pressure disappears within a few minutes after the cessation of the administration of urapidil.
Possible simultaneous use with antihypertensive agents for oral administration.
With hypovolemia, the hypotensive effect of urapidil is enhanced.
DRUG INTERACTION
Other antihypertensives, incl. alpha-adrenoblockers, ethanol enhance the antihypertensive effect of urapidil.
With the simultaneous administration of cimetidine, an increase in C max of urapidil in blood plasma by 15% is possible.
