Active substanceDoxazosinDoxazosin
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  • Dosage form: & nbsppills
    Composition:

    One tablet contains:

    active substance: Doxazosin mesylate (in terms of doxazosin) - 2.00 mg.

    Excipients: potato starch - 21.00 mg, lactose monohydrate - 52.96 mg, microcrystalline cellulose - 18.00 mg, povidone - 2.80 mg, silicon dioxide colloid (aerosil) - 1.60 mg, sodium lauryl sulfate - 0.20 mg , magnesium stearate-1.00 mg.

    Description:Tablets are white or white with a creamy shade of color, flat-cylindrical.
    Pharmacotherapeutic group:Alfa1 - adrenoblocker
    ATX: & nbsp

    C.02.C.A.04   Doxazosin

    Pharmacodynamics:
    Doxazosin is a selective competitive blocker of postsynaptic alpha 1-adrenergic receptors. By reducing the tone of the muscles of blood vessels doxazosin reduces overall peripheral vascular resistance, which leads to lower blood pressure.
    After a single administration of the drug, a maximum of hypotensive action is observed in the period from 2 to 6 hours, and in general the hypotensive effect persists for 24 hours. During treatment with doxazosin in patients with arterial hypertension there are no differences in blood pressure values ​​in the standing and lying position.
    Effective in hypertension, including, accompanied by metabolic disorders (obesity, decreased tolerance to glucose).
    Reduces the risk of coronary heart disease.
    Reception of the drug in "normotonics" is not accompanied by a decrease in blood pressure.
    With prolonged use of doxazosin in patients, there is no decrease in antihypertensive effect
    During the treatment with doxazosin, the plasma concentration of triglycerides, total cholesterol is reduced. At the same time, there is a certain (by 4-13%) increase in the ratio of high-density lipoproteins / total cholesterol.
    With long-term treatment with the drug, regression of left ventricular hypertrophy, inhibition of platelet aggregation, and an increase in active plasminogen content in tissues are observed. Due to doxazosin blocks alpha-1 adrenergic receptors located in the stroma and capsule of the prostate gland and in the neck of the bladder, the resistance and pressure in the urethra decrease, the resistance of the internal sphincter decreases. Therefore, prescribing to patients with symptoms of benign prostatic hyperplasia leads to a significant improvement in urodynamics and decreased manifestations symptoms of the disease.
    The effect in 66-71% of patients, the onset of action - after 1-2 weeks of treatment, maximum - after 14 weeks, the effect persists for a long time.
    Pharmacokinetics:
    After oral administration at therapeutic doses doxazosin well absorbed in the gastrointestinal tract, absorption - 80-90% (simultaneous intake of food slows down intake for 1 hour), time to reach a maximum concentration of -3 hours, with evening intake - 5 hours. Bioavailability - 60-70% (presystemic metabolism).
    The connection with blood plasma proteins is about 98%. Excretion from the blood plasma occurs in 2 phases, with a finite half-life of -19-22 h, which allows you to prescribe the drug once a day. Rapidly metabolized in the liver by o-demethylation and hydroxylation.
    It is excreted through the intestine, mainly in the form of metabolites (up to 65%), only 5% is excreted by the kidneys unchanged.
    Studies of the pharmacokinetics of doxazosin in elderly patients and in patients with kidney disease have not revealed significant pharmacokinetic differences.
    Indications:
    Arterial hypertension:
    in combination with other antihypertensive agents (thiazide diuretics, beta-blockers, slow calcium channel blockers or angiotensin-converting enzyme (ACE) inhibitors).
    Benign prostatic hyperplasia:
    as in the presence of arterial hypertension, and at normal arterial pressure.
    Contraindications:Hypersensitivity to doxazosin, to any of the auxiliary components of the drug, to other quinazolone derivatives, age to 18 years (efficacy and safety not established).
    Carefully:Aortic and mitral stenosis, orthostatic hypotension, impaired liver function.
    Pregnancy and lactation:To date, the experience of using Artesin in patients with arterial hypertension during pregnancy and lactation is not enough. Therefore, despite the absence of teratogenic and embryotoxic effects from experimental studies, Artesin can be administered during pregnancy and during lactation only after careful weighing by the attending physician of the benefit / risk relationship.
    Dosing and Administration:
    Inside once a day (in the morning or in the evening) regardless of food intake, without chewing and washing down with enough water.
    To ensure the following dosing regimen, it is possible to use Artesin in the drugform: a tablet of 1 mg and 2 mg.
    With arterial hypertension, the initial dose is 1 mg per day before bedtime.
    After taking the first dose, the patient should be in bed for 6-8 hours.
    This is required in connection with the possibility of developing a "first-dose phenomenon," especially pronounced against the background of previous intake of diuretics.
    If the therapeutic effect is insufficient, the daily dose can be increased to 2 mg in 1-2 weeks. In the following, every 1-2 weeks the dose can be increased by 2 mg. In the vast majority of patients, the optimal therapeutic effect is achieved at a dose of 8 mg per day. The maximum dose of -16 mg per day, can not be exceeded.
    After achieving a stable therapeutic effect, the dose is usually somewhat reduced (the average therapeutic dose with maintenance therapy is usually 2-4 mg Artesine per day).
    In the treatment of patients with benign prostatic hyperplasia, the initial dose is 1 mg / day in order to minimize the possibility of developing orthostatic hypotension and / or syncope. If necessary, depending on the parameters of urodynamics and the presence of symptoms, BPH increase the dose (with an interval of 1 -2 weeks) to 2-4 mg / day.
    The maximum permissible is a dose equal to 8 mg per day.The recommended maintenance dose is 2-4 mg / day.
    The drug is used for a long time. The duration of treatment is determined by the doctor.
    Side effects:
    Arterial hypertension
    In clinical trials, orthostatic hypotension was most often observed, especially at the beginning of treatment, which in rare cases can lead to fainting.
    Common reactions:
    asthenia, fatigue, malaise, allergic reactions, skin rash, urticaria.
    From the cardiovascular system:
    peripheral edema, fainting.
    From the central and peripheral nervous system: dizziness, headache, drowsiness.
    From the gastrointestinal tract:
    nausea
    From the respiratory system:
    rhinitis.
    As well as the following adverse reactions in patients with arterial hypertension (cause-and-effect relationship not established): bradycardia, tachycardia, palpitation, chest pain, angina pectoris, myocardial infarction, cerebral circulation disorder and arrhythmia.
    Benign prostatic hyperplasia (BPH)
    Patients with BPH have the same side effects as patients with hypertension, as well as:
    Common reactions:
    allergic reactions, skin rash, urticaria, back pain, sensation of heat ("hot flashes"), weight gain
    From the cardiovascular system:
    lowering of arterial pressure, orthostatic hypotension.
    From the central and peripheral nervous system:
    dry mouth, priapism, hypoesthesia, parasthesia, tremor, impotence, insomnia, increased excitability.
    From the endocrine system:
    gynecomastia.
    From the gastrointestinal tract:
    abdominal pain, constipation, diarrhea, indigestion, flatulence, nausea, loss of appetite
    From the hematopoiesis:
    leukopenia, purpura, thrombocytopenia.
    From the hepatobiliary system:
    increased activity of "hepatic", transaminases, cholestasis, hepatitis, jaundice
    From the musculoskeletal system:
    arthralgia, muscle cramps, weakness in the muscles, myalgia.
    From the respiratory system:
    bronchospasm, cough, shortness of breath, nosebleed.
    From the skin:
    alopecia.
    From the sense organs:
    blurred vision, tinnitus.
    From the urinary system:
    dysuria, hematuria, urination disorder, nocturia, polyuria, urinary incontinence.
    Overdose:
    Symptoms: marked reduction in blood pressure, sometimes accompanied by syncope.
    Treatment: the patient should be immediately placed in a horizontal position, raise his legs. Symptomatic therapy is performed. Dialysis is not effective.
    Interaction:
    Doxazosin enhances the antihypertensive effect of antihypergene agents.
    There was no adverse interaction with simultaneous use of doxazosin and thiazide diuretics, furosemide, beta-blockers, slow calcium channel blockers, angiotensin-converting enzyme inhibitors, antibiotics, oral hypoglycemic agents, indirect anticoagulants and uricosuric agents.
    Does not affect the degree of binding to plasma proteins digoxin, phenytoin.
    With simultaneous application with induction of microsomal oxidation in the liver, it is possible to increase the efficiency of doxazosin, with inhibitors - decrease.
    Non-steroidal anti-inflammatory drugs (especially indomethacin), estrogens and sympathomimetic drugs can reduce the hypotensive effect of doxazosin Eliminating alpha-adrenostimulating effects, can lead to the development of tachycardia and arterial hypotension.
    Cimetidine increases the bioavailability of doxazosin.Inhibitors of phosphodiesterase may increase the hypotensive effect (be careful).
    Special instructions:

    Before the beginning of the treatment of prostatic hyperplasia, the cancer degeneration of the prostate gland should be excluded.

    The effect of the "first" administration of the drug is particularly pronounced against the background of previous diuretic therapy and a diet with sodium restriction. It should be borne in mind that the risk of orthostatic reactions is also increased when drinking alcohol, in hot weather, prolonged standing or performing physical exercises. In order to prevent orthostatic reactions, unexpected and abrupt changes in body position (the transition from lying to standing position) should be avoided.

    Doxazosin should be used with caution in elderly patients due to the possibility of developing orthostatic hypotension. With age, the risk of dizziness, visual impairment and fainting increases.

    The patient should be informed of the increased risk of developing orthostatic hypotension with alcohol, prolonged standing or exercise, and in hot weather.

    As any vasodilator hypotensive agent doxazosin should be used with caution in patients with heart conditions requiring urgent care: pulmonary edema due to aortic or mitral stenosis, right ventricular failure due to pulmonary embolism or exudative pericarditis, left ventricular failure with low ventricular filling pressure; as well as in patients with severe myocardial ischemia, in whom a too rapid or pronounced decrease in blood pressure can lead to an increase in the symptoms of angina pectoris.

    As with the use of other drugs completely exposed to biotransformation in the liver, caution should be exercised in prescribing doxazosin to patients with impaired hepatic function, especially when drugs that can adversely affect liver function are used simultaneously. In the event of a deterioration in the functional status of the liver, the drug is immediately withdrawn.

    Caution should be exercised in the combined use of doxazosin with PDE-5 inhibitors, as this may lead to symptomatic hypotension in some patients.It is necessary to observe a 6-hour interval between the use of PDE-5 inhibitors and the use of doxazosin (to reduce the risk of lowering blood pressure, treatment is begun with the use of PDE-5 inhibitors).

    There are reports of cases of development of prolonged erection and priapism against the background of therapy with alpha1-adrenergic blockers. If the erection persists for more than 4 hours, you should immediately seek medical help. If priapism therapy has not been carried out immediately, it can lead to damage to the tissues of the penis and an irreversible loss of potency.

    Doxazosin does not affect the concentration of prostate-specific antigen (PSA) in the blood plasma.

    In some patients, intraoperative atonic iris syndrome (a variant of the narrow pupil syndrome) was observed when performing a cataract operation that received or received treatment with alpha 1-adrenoblockers. Since intraoperative atonic iris syndrome can lead to more complications during surgical interventions, it is necessary to alert the operating surgeon that doxazosin is currently being accepted or taken before surgery.

    Effect on the ability to drive transp. cf. and fur:Due to doxazosin can cause orthostatic reactions at the beginning of treatment or during the period of increasing dosages, when taking the drug, care must be taken when driving vehicles and engaging in other potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Tablets 2 mg and 4 mg.
    Packaging:

    For 10 or 15 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    3 contour packs of 10 tablets or 2 contour packs of 15 tablets together with instructions for use are placed in a pack of cardboard.

    Storage conditions:
    List B. In dry the dark place at a temperature of no higher than 25 ° C.
    Keep out of the reach of children.
    Shelf life:4 years.
    Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:P N001615 / 01
    Date of registration:08.08.2008 / 03.08.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp27.01.2016
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