international and chemical name: doxazosin; 1 – (4-amino –6, 7-dimetoksi-2-хиназолинил) – 4 – (1, 4-petroldioxane-2-илкарбонил) piperazin;
Main physical and chemical characteristics:
tablets of 1 mg – round, oboyevypukly tablets, white color, with slanted sides;
tablets of 2 mg and 4 mg – round, flat tablets, white color, with slanted sides and a notch on one party;
Structure. 1 tablet contains 1 mg, 2 mg or 4 mg of a doksazozin in the form of a doksazozin of a mezilat;
other components: cellulose microcrystallic, lactoses monohydrate, sodium starch glikolit, magnesium stearate, sodium a lauryl sulfate.
Form of production of medicine. Tablets.
Farmakoterapevtichesky group. Anti-adrenergic means with the peripheral mechanism of action.
Code of automatic telephone exchange C02C And 04.
Effect of the medicine.
Pharmacodynamics. Doksazozin is a blocker of alpha adrenoceptors.
It reduces arterial pressure, preventing reduction of unstriated muscles in walls of peripheral vessels thanks to what decrease in the general peripheric resistance results.
Influence on function of heart is insignificant and tranzitorny. Resistance to a doksazozin does not develop even after prolonged treatment.
Doksazozin reduces the level of the general cholesterol, cholesterol of lipoproteins low density, triglycerides and stimulates increase in level of cholesterol of lipoproteins of high density therefore it has protective action against development of atherosclerosis and coronary heart disease. Doksazozin patients on a non-insulin-dependent diabetes mellitus as it has neutral or even positive effect on the level of sugar and insulin in blood can apply. It slows down aggregation of thrombocytes. After long use decrease in mass of a left ventricle results. Doksazozin is safe drug for patients with a renal failure, chronic obstructive diseases of lungs, a peripheral arterial angiopatiya and gout.
Influence of a doksazozin continues within 24 hours and more. Lowered arterial pressure the most expressed in 2 – 6 hours after reception. The full stable effect lowering of blood pressure is observed in several weeks of regular reception. If effect unsatisfactory, the patient can accept other anti-hypertensive drugs at the same time: beta-blockers, diuretics, antagonists of calcium and inhibitors of an angiotensin-converting enzyme.
Doksazozin interferes with reduction of unstriated muscles of upper part of an urethra and muscles of a prostate which surround and squeeze an urethra. Owing to relaxation of muscles results simplification of an urination that promotes elimination of unpleasant symptoms which are observed at a benign hyperplasia of a prostate. Drug almost does not influence normal arterial pressure. The positive impact on the above-stated symptoms is observed after two weeks of treatment and increases at further treatment.
Pharmacokinetics. After intake doksazozin it is well soaked up. The concentration peak in plasma is observed in 1.5 – 3 hours after reception. Doksazozin almost completely contacts proteins of plasma. It is metabolized in a liver and removed with excrements, generally in the form of metabolites. Less than 10% of a dose are removed with urine. The elimination half-life of a doksazozin makes 16 – 22 hours.
Indications for use. Treatment of arterial hypertension (as monotherapy and in a combination with other antihypertensives); elimination of clinical symptoms of a benign hyperplasia of a prostate.
Way of use and dose. Drug Kamiren can be accepted to, during the period or after food.
Arterial hypertension. The initial dose of a doksazozin for adults makes 1 mg a day. The first dose should be accepted in the evening before going to bed. The doctor can gradually increase a drug dose in 1 – 2 weeks to 2 mg, 4 mg or 8 mg a day. Efficiency of a dose - 2 – 8 mg a day is finished. The maximum daily dose should not exceed 16 mg.
Benign hyperplasia of a prostate at a normotenziya. The initial dose of a doksazozin makes 1 mg a day. The first dose should be accepted in the evening before going to bed. The doctor can gradually increase a dose in 1 – 2 weeks to 2 mg, then to 4 mg or 8 mg a day. Efficiency of a dose of 2 - 4 mg a day is finished. The maximum daily dose should not exceed 8 mg.
Benign hyperplasia of a prostate at hypertensia. A dosage it, as well as at hypertensia.
Side effect. In an initiation of treatment at increase of a dose in some patients orthostatic reactions are possible that they are shown in a look lowering of arterial pressure, dizziness and even unconsciousness when changing position of a body. These effects are temporary, but at emergence of long-term or strong side effects it is recommended to reduce a dose or to stop treatment. To side effects of a doksazozin also general weakness, drowsiness, a headache, weakness of muscles, hypostasis of the lower extremities, nausea and rhinitis belong. In isolated cases - tachycardia, heartbeat and an incontience of urine.
Contraindications. Hypersensitivity to a doksazozin, its derivatives (Prazozinum, terazozin) and any other components of drug.
Kamiren's overdose. Overdose of a doksazozin can cause, first of all, hypotension, dizziness and a faint. For most of patients it is enough to reduce a dose of drug or to quickly stop treatment.
After reception of too high dose hypotension can be observed.
The patient it is necessary to put with a little lifted head over heels and the head hung down. Vomiting it is not necessary to cause. For removal of not absorbed drug in a digestive tract it is necessary to carry out a gastric lavage, to use absorbent carbon, laxative drug. Overdose treatment symptomatic by means of agonists of a-adrenoceptors (for example, noradrenaline).
For drug removal the hemodialysis is inefficient as doksazozin almost completely contacts proteins of plasma.
Features of use. Tickling the dose of a doksazozin can cause considerable lowered arterial pressure. Dizziness and even a faint can be observed. To avoid to these phenomena, it is necessary to begin treatment with a dose of 1 mg before going to bed. The dose needs to be increased gradually within 1 – 2 weeks. The patient should be warned about possibility orthostatic hypotensions and to recommend to rise carefully after a sitting position or lying. Especially it concerns patients of advanced age and those which at the same time accept other anti-hypertensive drugs and diuretics.
It is not recommended to patients to accept drug with low arterial pressure.
At patients with the broken function of a liver the metabolism of a doksazozin is slowed down and the dose should be titrated carefully.
Safety and efficiency of use of a doksazozin at children are not revealed therefore for treatment of children the drug which is not recommended.
Pregnancy and lactation
Risk of influence of drug on a fruit it is not established. Therefore pregnant women should accept drug only in cases when the possible advantage for mother exceeds potential risk for a fruit.
Feeding by a breast during treatment is not recommended because safety of drug for the newborn of the child was not established.
Influence on ability to manage motor transport and to work with other mechanisms
In an initiation of treatment and at increase of a dose of Kamiren arterial pressure can strongly decrease and the patient can have a dizziness. For this period it is necessary to refrain from driving by transport and works with mechanisms.
Interaction with other medicines. Doksazozin it is possible to accept together with other anti-hypertensive drugs (antagonists of beta receptors, diuretics, blockers of calcium channels, APF inhibitors), however, it is recommended to adhere to care in an initiation of treatment as the anti-hypertensive effect can amplify considerably. Sharing of drugs, such as nitrates, anesthetics, tricyclic antidepressants and alcohol mostly can promote lowering of arterial pressure.
It is also necessary to adhere to care at simultaneous use of drugs which influence metabolism speed in a liver as there is opportunity delay or increase of a metabolism of a doksazozin.
Laboratory tests: doksazozin does not influence concentration of prostatspetsifichesky antigen (PSA).
Conditions and periods of storage. To store at a temperature not above 30 °C.