Composition, form of production and packaging
Tablets are white or almost white, round, flat, with engraved "ZX 1" on one side.
1 tab.
Doxazosin mesylate 1.213 mg,
which corresponds to the content of doxazosin 1 mg
Excipients: lactose, microcrystalline granulated cellulose, microcrystalline cellulose, sodium carboxymethyl starch (type A), silicon dioxide colloidal anhydrous, sodium lauryl sulfate, magnesium stearate.
15 pcs. - blisters (1) - packs of cardboard.
15 pcs. - blisters (2) - packs of cardboard.
Tablets are white or almost white, oblong, biconcave, with engraved "ZX 2" and risk for division on one side.
1 tab.
doxazosin mesylate 2.425 mg,
which corresponds to the content of doxazosin 2 mg
Excipients: lactose, microcrystalline granulated cellulose, microcrystalline cellulose, sodium carboxymethyl starch (type A), silicon dioxide colloidal anhydrous, sodium lauryl sulfate, magnesium stearate.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
Tablets white or almost white, oblong, biconcave, with engraved "ZX 4" and risk for division on one side.
1 tab.
doxazosin mesylate 4.85 mg,
which corresponds to the content of doxazosin 4 mg
Excipients: lactose, microcrystalline granulated cellulose, microcrystalline cellulose, sodium carboxymethyl starch (type A), silicon dioxide colloidal anhydrous, sodium lauryl sulfate, magnesium stearate.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (9) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2012.
PHARMACHOLOGIC EFFECT
Selective blocker? 1- adrenoreceptors.
When benign prostatic hyperplasia blocks? 1- adrenoreceptors located in the stroma and capsule of the prostate gland, as well as in the neck of the bladder, which leads to improved urodynamics and a reduction in the symptoms of the disease.
The use of Zoxon in arterial hypertension leads to a decrease in blood pressure as a result of a decrease in OPSS. With the appointment of the drug 1 time / day achieved clinically significant hypotensive effect, which persists for 24 hours. There is a gradual decrease in blood pressure, while the maximum reduction in blood pressure is achieved 2-6 hours after taking the drug.
Zoxone has a positive effect on the lipid profile of blood, significantly reducing the level of triglycerides and cholesterol, which helps reduce the risk of developing coronary heart disease.
The use of the drug leads to a decrease in hypertrophy of the left ventricle of the heart, promotes inhibition of platelet aggregation and reduces the tendency to thrombosis.
Zoxon does not adversely affect the overall metabolism. The drug can be used in patients suffering from bronchial asthma, diabetes, gout, as well as in the elderly.
PHARMACOKINETICS
Suction
After oral administration, doxazosin is well absorbed into the digestive tract (80-90%). Simultaneous food intake slows the absorption of the drug for 1 hour.
C max in blood plasma is achieved in 1-2 hours after administration.
Distribution
Binding to plasma proteins - 98%.
Metabolism
Doxazosin undergoes significant biotransformation in the liver with the formation of pharmacologically inactive metabolites.
Bioavailability - 69-70% (presystemic metabolism).
In patients with impaired liver function, as well as when taking drugs that can alter hepatic metabolism, the biotransformation of the drug may be disrupted.
Excretion
The removal of the drug from the plasma is biphasic, with a finite T 1/2 of 22 hours. Most of the ingested doxazosin is excreted as inactive metabolites with feces, less than 5% of the dose taken is unchanged.
Studies of pharmacokinetics in elderly patients and patients with kidney disease have not revealed significant pharmacokinetic differences.
INDICATIONS
- Bovine hyperplasia of the prostate (Zoxon is intended for the treatment of urinary disorders caused by benign prostatic hyperplasia.) In patients with benign prostatic hyperplasia, Zoxon can be used in the presence of arterial hypertension or at a normal level of AD In patients with arterial hypertension and benign hyperplasia prostate Zoxon effectively affects both diseases);
- Arterial hypertension (Zoxon is used for the treatment of arterial hypertension.In the event that it is not possible to obtain the required blood pressure control using Zoxon as a monotherapy agent, the drug can be combined with other antihypertensive agents - thiazide diuretics, beta adrenoblockers, slow calcium channel blockers, ACE inhibitors).
DOSING MODE
Inside 1 time / day (morning or evening), regardless of food intake. Tablets should be swallowed whole, not liquid, squeezed with enough water.
In the treatment of urinary disorders due to benign prostatic hyperplasia , without hypertension, the recommended dose is 2-4 mg 1 time / day. The maximum dose is 8 mg / day.
In the treatment of hypertension, the dose of the drug, depending on the characteristics of the course of the disease and the severity of the condition, can vary from 1 mg / day to 16 mg / day. The maximum dose is 16 mg / day.
The initial dose of the drug is 1 mg 1 time / day before bedtime. After taking the first dose, the patient should lie in the prone position for 6-8 hours. This is required in connection with the possibility of developing a "first-dose phenomenon", especially pronounced against the background of the previous intake of diuretics.
If the therapeutic effect is insufficient, the daily dose can be increased to 2 mg only after 1-2 weeks of continuous treatment with the drug. In a subsequent 1-2 weeks the dose can be increased by 2 mg until the optimal therapeutic effect is achieved.
In the vast majority of patients, the optimal therapeutic effect is achieved at a dose of 8 mg / day. After achieving a stable therapeutic effect, the dose is usually somewhat reduced, the average therapeutic dose with maintenance therapy is usually 2-4 mg / day.
The drug is used for a long time. The doctor determines the duration of treatment individually.
SIDE EFFECT
Arterial hypertension
From the side of the cardiovascular system: in clinical studies, the most frequently observed, especially at the beginning of treatment, orthostatic hypotension, which in rare cases can lead to fainting; edema. Causal relationship is not established - bradycardia, tachycardia, palpitations, chest pain, angina pectoris, myocardial infarction, arrhythmia, cerebrovascular accident.
From the side of the central nervous system: dizziness, headache, drowsiness.
From the respiratory system: rhinitis.
From the side of the digestive system: nausea.
Common reactions: asthenia, fatigue, malaise.
Benign prostatic hyperplasia
In addition to the following side effects, patients with benign prostatic hyperplasia have the same side effects as patients with hypertension.
From the cardiovascular system: a decrease in blood pressure, orthostatic hypotension.
From the nervous system: insomnia, increased excitability, dry mouth, hypoesthesia, paresthesia, tremor, priapism, impotence.
On the part of the respiratory system: nosebleeds, dyspnea, cough, bronchospasm.
On the part of the digestive system: nausea, loss of appetite, indigestion, flatulence, abdominal pain, constipation, diarrhea, increased activity of hepatic transaminases, hepatitis, cholestasis, jaundice.
From the urinary system: dysuria, urinary incontinence, hematuria, nocturia, polyuria.
On the part of the endocrine system: gynecomastia.
From the musculoskeletal system: weakness in the muscles, muscle cramps, myalgia, arthralgia.
From the senses: blurred vision, tinnitus.
From the hematopoiesis: leukopenia, thrombocytopenia, purpura.
From the skin: alopecia.
Common reactions: allergic reactions, skin rash, urticaria, back pain, sensation of heat (hot flashes).
CONTRAINDICATIONS
- age under 18 years (effectiveness and safety not established);
- hypersensitivity to doxazosin, quinazoline derivatives or other components of the drug.
Use with caution in patients with impaired liver function, aortic and mitral stenosis, orthostatic hypotension.
PREGNANCY AND LACTATION
To date, the experience of doxazosin in patients with hypertension during pregnancy and during breastfeeding is not enough. Therefore, despite the absence of teratogenic and embryogenic effects from experimental studies, doxazosin may be prescribed during pregnancy and during lactation only after an assessment of the benefit / risk ratio.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Caution should be given to Saxon patients with impaired liver function.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years.
SPECIAL INSTRUCTIONS
Caution should be given to Saxon patients with impaired liver function, especially in cases where concurrent use of drugs that can adversely affect liver function. In case of deterioration of the functional state of the liver, the drug should be immediately withdrawn.
To prevent orthostatic reactions, patients should avoid sudden and abrupt transitions from lying to standing.
Taking alcohol can increase unwanted reactions.
The effect of the "first reception" of the drug is particularly pronounced against the background of previous diuretic therapy and a diet with sodium restriction.
Before starting therapy with Zoxon, malignancy of the prostate gland should be avoided.
Impact on the ability to drive vehicles and manage mechanisms
Due to the fact that doxazosin is able to cause orthostatic reactions at the beginning of treatment or during the period of increasing the dose, it is advisable for patients to refrain from any potentially dangerous activities, in particular from the management of motor vehicles and other vehicles and mechanisms.
OVERDOSE
Symptoms: severe arterial hypotension, sometimes with fainting.
Treatment: stop taking the drug, put the patient on his back, with his head down and raised his legs. When signs of an overdose appear, it is necessary to wash the stomach, assign activated charcoal. Conduct symptomatic therapy. Dialysis is ineffective.
DRUG INTERACTION
With the simultaneous use of Zoxon and other medications intended for the treatment of hypertension, a mutual strengthening of the hypotensive effect is possible.
There was no negative manifestation of the interaction of doxazosin with thiazide diuretics, beta adrenoblockers, furosemide, slow calcium channel blockers, ACE inhibitors, antibiotics, oral hypoglycemic agents, uricosuric agents and indirect anticoagulants.
With simultaneous use with induction of microsomal oxidation in the liver, it is possible to increase the effectiveness of doxazosin, with inhibitors - decrease.
NSAIDs (especially indomethacin), estrogens (fluid retention), and sympathomimetic drugs can reduce the hypotensive effect of doxazosin.
Eliminating the alpha-adrenostimulating effects of epinephrine, the use of doxazosin can lead to tachycardia and arterial hypotension.
Cimetidine increases the AUC of doxazosin.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, protected from light at a temperature of 10 В° to 25 В° C. Shelf life - 3 years.
