Doksazozin Belupo

General characteristics. Structure:

Active agent: a doksazozina мезилат 2,425 mg (there correspond 2 mg of a doksazozin of the basis)  

Excipients: MKTs; lactose; sodium carboxymethylstarch; silicon dioxide colloid; sodium lauryl sulfate; magnesium stearate  

Active agent: a doksazozina мезилат 4,85 mg (there correspond 4 mg of a doksazozin of the basis)  

Excipients: MKTs; lactose; sodium carboxymethylstarch; silicon dioxide colloid; sodium lauryl sulfate; magnesium stearate.

Pharmacological properties:

The selection competitive blocker postsynaptic α1-адренорецепторов. Causes expansion of peripheral vessels that leads to reduction of OPSS and decrease in the ABP. Increase in coefficient of LPVP is promoted / by the general cholesterol, to decrease in total level of triglycerides and cholesterol.
At prolonged use regression of a hypertrophy of a left ventricle is observed, there is a suppression of aggregation of thrombocytes and increase in content in plasminogen activator fabrics. Blockade α1-адренорецепторов, located in a stroma and the capsule of a prostate, in a neck of a bladder leads to decrease in resistance and pressure in an urethra, to reduction of resistance in its internal opening. Improves urodynamic and reduces displays of a benign hyperplasia of a prostate.

Pharmacokinetics. After intake it is well absorbed from a GIT. Cmax in plasma is reached in 1.5-3.6 h. Linkng with proteins of plasma makes 98-99%. It is intensively metabolized in a liver. T1/2 makes 19-22 h. 5% - in not changed look are removed mainly through intestines in the form of metabolites; 9% are removed by kidneys.

Indications to use:

Arterial hypertension. Benign hyperplasia of a prostate (symptomatic treatment).

Route of administration and doses:

Inside, washing down with enough liquid. Drug can be used both in the morning, and in the evening, once a day. It is desirable to carry out the first reception before going to bed for the prevention of possible development of orthostatic hypotension.

Arterial hypertension. The usual dose makes from 1 to 8 mg/days. At insufficient expressiveness of hypotensive effect perhaps gradual increase in a dose up to the greatest possible daily dose — 16 mg or addition of other hypotensive HP (thiazide diuretics, beta adrenoblockers, BKK, APF inhibitors).

Initial dose — 1 mg once a day during 1–2 weeks. For the following 1–2 weeks the dose can be increased to 2 mg of 1 times a day. If necessary the daily dose can be increased to 4, 8 and 16 mg of 1 times a day depending on expressiveness of hypotensive effect of drug at regular intervals. As a rule, the effective supporting daily dose makes 2–4 mg/days.

Benign Hyperplasia of a Prostate (BHP). An initial dose — 1 mg of 1 times a day. If necessary the dose is increased with an interval of 1-2 weeks to 2–4 mg/days. The maximum daily dose — 8 mg/days. The recommended maintenance dose — 2–4 mg/days.

Features of use:

With care apply at abnormal liver functions.

After reception of a doksazozin in an initial dose development of orthostatic hypotension (a phenomenon of the first dose), especially in a standing position is possible. Such state is more often it is observed at patients with a hypovolemia, deficit of sodium, at elderly people. In this regard the initial dose is recommended to be accepted before going to bed.

Clinical experience of use of a doksazozin for children is absent.

Influence on ability to driving of motor transport and to control of mechanisms

During reception of a doksazozin, especially in an initiation of treatment, it is necessary to be careful when performing the work demanding the increased speed of psychomotor reactions in connection with possible development of drowsiness, dizziness.

Side effects:

From cardiovascular system: orthostatic reactions (including faints), tachycardia, arrhythmia, peripheral hypostases.
From the alimentary system: nausea.
From TsNS: dizziness, headache, feeling of fatigue, irritability, adynamy, drowsiness.
Others: rhinitis.

Interaction with other medicines:

At simultaneous use with anti-hypertensive drugs perhaps mutual strengthening of effects.

At simultaneous use with blockers of calcium channels there is some risk of development of the expressed arterial hypotension.

At simultaneous use with nitrates, means for the general anesthesia, tricyclic antidepressants, ethanol strengthening of hypotensive effect is possible.

At simultaneous use of the means influencing metabolism speed in a liver delay or acceleration of metabolism of a doksazozin is possible.

Contraindications:

Hypersensitivity to quinazoline derivatives.

Use at pregnancy and feeding by a breast
Adequate and strictly controlled researches of safety of use of a doksazozin at pregnancy and in the period of a lactation (breastfeeding) were not conducted. Use is possible only in cases when the potential advantage for mother exceeds potential risk for a fruit or the child.

Use at abnormal liver functions
With care apply at abnormal liver functions.

Use for elderly patients
After reception of a doksazozin in an initial dose at elderly people development of orthostatic hypotension (a phenomenon of the first dose), especially in a standing position is possible. In this regard the initial dose is recommended to be accepted before going to bed.

Use for children
Clinical experience of use of a doksazozin for children is absent.

Overdose:

There are no data.

Storage conditions:

At a temperature not above 30 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, 2 mg, 4 mg. According to 20 tab. in PVC/PVDH / the aluminum blister. One blister is placed in a cardboard pack.