Zokson

General characteristics. Structure:

Active agent: 
Zokson (tablets on 1 mg): 1 tablet contains active agent of a doksazozin 1 mg (a doksazozin of a mezilat of 1,213 mg).
Zokson (tablets ло 2 mg): 1 tablet contains active agent of a doksazozin 2 mg (a doksazozin of a mezilat of 2,425 mg).
Zokson (tablets on 4 mg): 1 tablet contains active agent of a doksazozin 4 mg (a doksazozin of a mezilat of 4,850 mg).
Excipients: the lactose, cellulose microcrystallic granulated cellulose microcrystallic, sodium carboxymethylstarch (type A), silicon dioxide colloid anhydrous, sodium lauryl sulfate, magnesium stearate.

DESCRIPTION
ZOKSON (tablets no of 1 mg)
Round flat tablets of white or almost white color with an engraving of "ZX 1" on one of the parties. ZOKSON (tablets on 2 mg)
Oblong shape, biconvex tablets white or mail of white color, with an engraving of "ZX 2" and risky for division on one of the parties. ZOKSON (tablets on 4 mg)
Oblong shape, biconvex tablets of white or almost white color, with an engraving of "ZX 4" and risky for division on one of the parties.

Pharmacological properties:

Pharmacodynamics. Active ingredient of drug ZOKSON is доксазозин - the selection blocker of alfa1-adrenoceptors. Purpose of drug to patients with a benign hyperplasia of a prostate leads to considerable improvement of indicators of urodynamic and reduction of manifestations of symptoms of a disease. The effect of positive action is explained by blockade of the alfa1-adrenoceptors located in a stroma and the capsule of a prostate and also in a bladder neck.
Use of drug ZOKSON leads to essential decrease in level of arterial pressure as a result of reduction of the general peripheric vascular resistance. At purpose of drug of 1 times a day clinically significant hypotensive effect which remains for 24 hours is reached. Gradual decrease in level of arterial pressure is noted, at the same time the level of the maximum lowering of arterial pressure is reached in 2-6 hours after administration of drug.
Exerts positive impact on a blood lipid profile, substantially reduces the level of concentration of triglycerides and cholesterol that promotes decrease in risk of development of coronary heart disease, use of drug leads to reduction of a hypertrophy of a left ventricle of heart, promotes oppression of aggregation of thrombocytes and reduces tendency to a thrombogenesis.
ZOKSON does not exert negative impact on the general metabolism, can be applied at the patients having bronchial asthma, a diabetes mellitus, gout and also at elderly people.

Pharmacokinetics. After intake доксазозин it is well soaked up in digestive tract (80-90%), the concomitant use of food slows down absorption for 1 hour. The maximum concentration in a blood plasma is reached in 1 - 2 hour after reception. To 98% contacts proteins of a blood plasma. Doksazozin is exposed to considerable biotransformation in a liver, metabolites have no pharmacological activity. Bioavailability - 69-70% (presistemny metabolism). At patients with the broken function of a liver, and also at administration of drugs, capable to change hepatic metabolism, process of biotransformation of drug can be broken. Removal of drug from a blood plasma is two-phase, with a final elimination half-life 22 hours. The most part of the doksazozin accepted inside is removed in the form of inactive metabolites with a stake, less than 5% of the accepted dose are allocated in not changed look. A pharmacokinetics research at elderly patients and at patients with diseases of kidneys did not reveal essential pharmacokinetic distinctions.

Indications to use:

Benign hyperplasia of a prostate
ZOKSON is intended for treatment of the disturbances of an urination caused by a benign hyperplasia of a prostate. At patients with a benign hyperplasia of a prostate of ZOKSON it is possible to apply both in the presence of arterial hypertension, and at the normal level of arterial pressure. At the patients who at the same time have arterial hypertension and a benign hyperplasia of a prostate, ZOKSON effectively influences both diseases.
Arterial hypertension
ZOKSON is applied to treatment of arterial hypertension. If it is not possible to receive required control of arterial pressure, using ZOKSON as means of monotherapy, drug can be combined with other anti-hypertensive means (thiazide diuretics, β-adrenoblockers, blockers of "slow" calcium channels, inhibitors of an angiotensin-converting enzyme).

Route of administration and doses:

Inside, once a day (in the morning or in the evening) irrespective of meal, without chewing and washing down with enough water.
At treatment of patients with a benign hyperplasia of a prostate without arterial hypertension usually use the doses equal to 2-4 mg a day. The most admissible is the dose equal of 8 mg a day.
At treatment of patients with arterial hypertension of a dose of drug depending on features of a course of a disease and weight of a state can vary from 1 mg a day to 16 mg a day (the most admissible daily dose).
The initial dose of drug makes 1 mg a day once a day before going to bed. After reception of the first dose of the patient has to be in a bed within 6-8 hours. It is required in connection with a possibility of development of "a phenomenon of the first dose" which is especially expressed against the background of the previous reception of diuretics.
At insufficiency of therapeutic effect the daily dose can be increased to 2 mg only in 1-2 weeks of continuous treatment by drug. In the subsequent in 1-2 weeks the dose can be increased by 2 mg before achievement of optimum therapeutic effect.
At the vast majority of patients the optimum therapeutic effect is reached at a dose of 8 mg a day. A dose of equal 16 mg a day, it is impossible to exceed (the maximum daily dose). After achievement of lasting therapeutic effect the dose is usually a little reduced (the average therapeutic dose at a maintenance therapy is usually equal to 2 - 4 mg a day).
Drug ZOKSON is used it is long. Duration of treatment is determined by the attending physician.

Features of use:

Extra care should be shown at purpose of this drug the patient with an abnormal liver function, especially when at the same time use the drugs capable negatively to influence functions of a liver. In cases of deterioration in indicators of a functional condition of a liver drug is immediately cancelled.
For the purpose of prevention of orthostatic reactions patients have to avoid unexpected and sharp changes of provision of a tep (transition from a prone position to a standing position).
Because доксазозин it is capable to cause orthostatic reactions in an initiation of treatment or during increase in dosages, it is reasonable to patient to abstain from all potentially dangerous types of activity, in particular from control of motor transport and other vehicles and mechanisms.
Alcohol intake is capable to strengthen undesirable reactions.
The effect of the "first" administration of drug is especially expressed against the background of the previous diuretic therapy and a diet with sodium restriction.
Before therapy it is necessary to exclude cancer regeneration of a prostate.

Side effects:

Arterial hypertension
In clinical trials were most often observed, especially in an initiation of treatment, orthostatic hypotension which in rare instances can lead to a faint.
General reactions: adynamy, fatigue, indisposition.
From cardiovascular system: hypostases, faint.
From the central and peripheral nervous system: dizziness, headache, drowsiness.
From digestive tract: nausea.
From respiratory system: rhinitis.

Benign Hyperplasia of a Prostate (BHP) 
At sick DGPZh the same side effects, as occur at patients with arterial hypertension, and also:
General reactions: allergic reactions, skin rash, small tortoiseshell, dorsodynia, feeling of heat ("inflows").
From cardiovascular system: decrease in the ABP, orthostatic hypotension.
From the central and peripheral nervous system: dryness in a mouth, a priapism, a giposteziya, parasthesias, a tremor, impotence, sleeplessness, a hyperexcitability.
From endocrine system: gynecomastia.
From digestive tract: abdominal pain, lock, diarrhea, dyspepsia, meteorism, nausea, appetite loss,
From bodies of a hemopoiesis: leukopenia, purpura, thrombocytopenia.
From gepatobiliarny system: increase in activity of "hepatic" transaminases, cholestasia, hepatitis, jaundice.
From skeletal and muscular system: an arthralgia, muscular spasms, weakness in muscles, a mialgiya.
From respiratory system: bronchospasm, cough, short wind, nasal bleeding.
From integuments: allopecia.
From sense bodys: illegibility of visual perception, sonitus.
From outside urinary systems: dysuria, hamaturia, disturbance of an urination, nocturia, polyuria, urine incontience.
And also the following side reactions at patients with arterial hypertension were noted (relationship of cause and effect is not established): bradycardia, tachycardia, heartbeat, stethalgia, stenocardia, myocardial infarction, Disturbance of a brain krovobrashcheniye and arrhythmia.

Interaction with other medicines:

Doksazozin strengthens hypotensive effect of anti-hypertensive means. Adverse interaction at simultaneous use of a doksazozin and thiazide diuretics, furosemide, β-adrenoblockers, blockers of "slow" calcium channels, APF inhibitors, antibiotics, peroral hypoglycemic means, indirect anticoagulants and uricosuric means is noted. At simultaneous use with inductors of a microsomal oxidation in a liver increase in efficiency of a doksazozin, with inhibitors - decrease is possible. Non-steroidal anti-inflammatory drugs (especially indometacin), estrogen (a liquid delay) and sympathomimetic means can reduce hypotensive action of a doksazozin. Eliminating an alpha - adrenostimuliruyushchy effects of Epinephrinum, can lead to tachycardia and arterial hypotension. Cimetidinum raises AUC of a doksazozin.

Contraindications:

Hypersensitivity to a doksazozin, derivatives of quinazoline or other components of drug. Drug is not intended for use for children aged up to 18 years (efficiency and safety are not established).
With care to apply: to patients with abnormal liver functions, an aortal and mitral stenosis, orthostatic hypotension.

Use of drug at pregnancy and during feeding by a breast
 So far experience of use of a doksazozin for patients with arterial hypertension during pregnancy and during feeding by a breast is insufficient. Therefore, despite the lack of teratogenic and embriogenny effects according to pilot studies, доксазозин it can be appointed at pregnancy and during feeding a breast only after careful weighing by the doctor of a ratio advantage/risk.

Overdose:

Symptoms: the expressed decrease in the ABP which sometimes is followed by a faint.
Treatment: the patient it is necessary to put immediately in horizontal position, having hung the head down, to raise legs. At emergence of signs of overdose it is necessary to wash out a stomach, to appoint absorbent carbon, patients need to see a doctor urgently. Symptomatic therapy is carried out. Dialysis is inefficient.

Storage conditions:

To store at a temperature of 10 - 25 °C, in the place protected from light. To store in the place unavailable to children. PERIOD OF VALIDITY 3 years. Drug cannot be used after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 1,2 and 4 mg.
Tablets of 1 mg: On 15 tablets in the blister from A1/PVH/PVDH. On 1 or 2 blisters in a cardboard pack together with the application instruction.
Tablets of 2 mg: On 10 tablets in the blister from A1/PVH/PVDH. On 1 or 3 blisters in a cardboard pack together with the application instruction.
Tablets of 4 mg: On 10 tablets in the blister from AI/PVH/PVDH. On 3,9 or 10 blisters in a cardboard pack together with the application instruction.