Active substanceDoxazosinDoxazosin
Similar drugsTo uncover
  • Artesin®
    pills inwards 
    VALENTA PHARM, PAO     Russia
  • Artesin®
    pills inwards 
    VALENTA PHARM, PAO     Russia
  • Artesin® retard
    pills inwards 
    VALENTA PHARM, PAO     Russia
  • Doxazosin
    pills inwards 
    ZIO-HEALTH, JSC     Russia
  • Doxazosin
    pills inwards 
    ATOLL, LLC     Russia
  • Doxazosin
    pills inwards 
  • Doxazosin Belupo
    pills inwards 
  • Doxazosin Zentiva
    pills inwards 
    Zentiva c.s.     Czech Republic
  • Doxazosin Sandoz
    pills inwards 
    Sandoz d.     Slovenia
  • Doxazosin-Teva
    pills inwards 
  • Doxazosin-FPO®
    pills inwards 
  • Camiren®
    pills inwards 
  • Camirin® HL
    pills inwards 
  • Cardura®
    pills inwards 
    Pfizer Inc.     USA
  • Cardura® Neo
    pills inwards 
    Pfizer Inc.     USA
  • Tonocardin®
    pills inwards 
  • Urokard
    pills inwards 
  • Dosage form: & nbsptabscesses
    Composition:

    One tablet contains:

    active substance: Doxazosin mesylate - 1.22 mg (in terms of doxazosin - 1.00 mg);

    Excipients: pregelatinized starch - 10.00 mg, lactose monohydrate - 65.78 mg, microcrystalline cellulose - 20.00 mg, sodium carboxymethyl starch - 1.00 mg, silicon dioxide colloid (aerosil) - 1.00 mg, magnesium stearate - 1.00 mg

    Description:

    Round, flat-cylindrical tablets of white or almost white color, with a bevel.

    Pharmacotherapeutic group:Alpha-blocker
    ATX: & nbsp

    C.02.C.A.04   Doxazosin

    Pharmacodynamics:

    Pharmacological properties

    Doxazosin is a selective competitive blocker of postsynaptic alpha 1 -adrenoceptors.

    Pharmacodynamics

    In patients with benign prostatic hypertrophy doxazosin leads to a significant improvement in urodynamic parameters and a reduction in the symptoms of the disease. The effect is associated with a selective blockade of doxazosin alpha1-adrenergic receptors located in the muscular stroma and prostatic capsule in the neck of the bladder and in the proximal part of the urethra, which reduces resistance and pressure in the urethra, reduces the resistance of the internal sphincter and facilitates urination.Effective in 66-71% of patients, the onset of action - after 1-2 weeks of treatment, the maximum effect - after 14 weeks, the effect persists for a long time.

    The use of doxazosin in patients with arterial hypertension leads to a significant reduction in blood pressure (BP) due to blockade of alpha 1-adrenergic receptors located in the vascular network, reducing the tone of vascular muscles and reducing the overall peripheral vascular resistance. Doxazosin, including, it is effective at an arterial hypertensia, accompanied by metabolic disturbances (adiposity, depression of tolerance to glucose). After a single dose of doxazosin, the maximum hypotensive effect / effect is observed in the period from 2 to 6 hours, and in general the hypotensive effect / effect persists for 24 hours. With prolonged use of doxazosin in patients, there is no decrease in antihypertensive effect / effect. When carrying out maintenance therapy, increased blood renin activity and tachycardia are rare.

    Reduces the risk of coronary heart disease. With prolonged treatment with doxazosin, regression of left ventricular hypertrophy, suppression of platelet aggregation, and an increase in active plasminogen content in tissues are observed.In addition, it is established that doxazosin increases insulin sensitivity in patients with impaired glucose tolerance.

    During the treatment with doxazosin, a decrease in the plasma concentration of triglycerides, total cholesterol, is observed. At the same time, there is a certain (by 4-13%) increase in the ratio of high-density lipoproteins / total cholesterol.

    The administration of doxazosin in patients with normal arterial pressure is not accompanied by a decrease in blood pressure. The development of orthostatic hypotension during treatment is uncharacteristic (it can only develop with prolonged use of high doses).

    Doxazosin does not have side metabolic effects and can be used in patients with bronchial asthma, diabetes, left ventricular failure and gout.

    Pharmacokinetics:

    After oral administration at therapeutic doses doxazosin well absorbed in the gastrointestinal tract, absorption - 80-90% (simultaneous intake of food slows down absorption for 1 hour), time to reach a maximum concentration of 2-3 hours, with evening intake - 5 hours Bioavailability - 60-70% (pre-systemic metabolism ).

    The connection with blood plasma proteins is about 98%.Excretion from the blood plasma occurs in 2 phases, with a finite half-life - 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 patients with kidney disease have not revealed significant pharmacokinetic differences.

    Indications:

    - Benign prostatic hyperplasia (both in the presence of arterial hypertension and at normal arterial pressure);

    - arterial hypertension - in combination with other antihypertensive agents (thiazide diuretics, beta-blockers, slow calcium channel blockers or angiotensin-converting enzyme (ACE) inhibitors).

    Contraindications:

    - Hypersensitivity to quinazolines, doxazosin, or any of the auxiliary components of the drug;

    - lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

    - severe hepatic impairment;

    - benign prostatic hyperplasia in combination with arterial hypotension or orthostatic hypotension in anamnesis;

    - benign prostatic hyperplasia in combination with impaired patency of the upper sections of the urinary tract;

    - chronic urinary tract infectious disease, urolithiasis, urinary incontinence due to overfilling of the bladder, anuria, progressive renal failure;

    - age under 18 years (no data on effectiveness and safety);

    - the period of breastfeeding.

    Carefully:

    The mitral and aortic stenosis, cardiac failure with an increase in minute ejection, right ventricular failure due to pulmonary embolism or exudative pericarditis, left ventricular failure with low filling pressure, cerebrovascular disease, advanced age, the simultaneous application of phosphodiesterase inhibitors of type 5 (PDE-5 ), hepatic insufficiency, pregnancy.

    Pregnancy and lactation:

    Although in animal experiments doxazosin does not have a teratogenic effect, but when used in extremely high doses, a decrease in fetal survival is observed. These doses are about 300 times greater than the maximum recommended dose for a person. To date, the experience with doxazosin in pregnant or lactating women is not enough. In this regard, the use of the drug during pregnancy is recommended only if the intended benefit to the mother exceeds the potential risk to the fetus and the baby.

    If you need to use the drug during lactation at the time of treatment should stop breastfeeding.

    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.

    If the drug is missed at the usual time, you should take this dose as soon as possible. If the time is right for taking the next dose, you should only take it without doubling the dose of the drug. If the therapy with Artesin® was interrupted for several days, the drug should be resumed from the initial dose.

    Dose adjustments Artesin® in elderly patients not required.

    Pharmacokinetics of doxazosin in patients with renal insufficiency does not change, but itself doxazosin does not worsen the existing renal dysfunction, so in such patients Artesin® is used in usual doses.

    In patients with hepatic insufficiency Artesin® is used in smaller doses (due to delayed metabolism of doxazosin).

    When benign prostatic hyperplasia the recommended initial dose in patients with normal blood pressure is 1 mg / day in order to minimize the possibility of postural hypotension and / or syncope (fainting). If necessary, depending on the parameters of urodynamics and the presence of symptoms of the disease, the dose is increased (with an interval of 1-2 weeks) to 2-4 mg / day. The maximum daily dose is 8 mg. 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.

    With benign prostatic hyperplasia in patients with hypertension, the drug is prescribed in the same doses,as well as patients with only arterial hypertension.

    When arterial hypertension the recommended initial dose is 1 mg / day in the evening 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 development after the first dose of orthostatic hypotension (the phenomenon of "first dose"). If the therapeutic effect is insufficient, the daily dose can be increased to 2 mg / day after 1-2 weeks. In the future, to achieve the desired reduction in blood pressure every 1-2 weeks, you can increase the dose by 2 mg. In most patients, the optimal therapeutic effect is achieved with a daily dose of 8 mg. The maximum daily dose is 16 mg. After achieving a stable therapeutic effect, the dose is usually somewhat reduced (the average therapeutic dose with maintenance therapy is usually 2-4 mg per day).

    If a diuretic or other antihypertensive agent is added to the therapy, it is necessary to adjust the dose of Artesin®. In this case, the dose of Artesin® is reduced depending on the patient's condition, and then again gradually increased, selecting the necessary dosage regimen.

    Side effects:

    The frequency of side effects is presented in the following classification: very frequent (≥10%), frequent (≥1% and <10%), infrequent (≥0,1% and <1%), rare (≥0,01% and <0 , 1%), very rare (<0.01%).

    In patients with benign prostatic hyperplasia there are the same side effects as in patients with hypertension, as well as:

    From the side of the cardiovascular system: infrequent - marked reduction in blood pressure, orthostatic arterial hypotension, "hot flashes" of blood to the skin of the face.

    From the central and peripheral nervous system: frequent - paresthesia, dry mouth, insomnia, increased excitability; infrequent - hypoesthesia, tremor, depression; very rare - priapism, impotence.

    From the endocrine system: very rare - gynecomastia.

    From the gastrointestinal tract: frequent - abdominal pain, diarrhea, dyspepsia, nausea; infrequent - flatulence, constipation, vomiting, loss of appetite.

    On the part of the organs of hematopoiesis: very rare - leukopenia, thrombocytopenia.

    From the hepatobiliary system: very rare - increased activity of "liver" transaminases, cholestasis, hepatitis, jaundice.

    From the musculoskeletal system: infrequent - arthralgia, muscle cramps, weakness in the muscles, myalgia.

    From the respiratory system: frequent - shortness of breath, rhinitis; infrequent - cough, nosebleeds; very rare - bronchospasm.

    From the skin: infrequent - alopecia, skin rash, skin itch, purpura; very rare - hives.

    From the sense organs: frequent - blurred vision; infrequent - noise in the ears, a syndrome of an atonic iris.

    Co the side of the urinary system: infrequent - urination disorder, polyuria, urinary incontinence; very rare - dysuria, hematuria, nocturia.

    From the side of the reproductive system: very rare - retrograde ejaculation.

    From the immune system: very rare - anaphylactic reactions.

    Other: infrequent - an increase in body weight, pain of varying localization.

    Arterial hypertension

    In clinical studies, orthostatic arterial hypotension was most often observed, especially at the beginning of treatment, which in rare cases can lead to fainting.

    From the side of the cardiovascular system: frequent - peripheral edema.

    From the central and peripheral nervous system: very frequent - dizziness, headache; frequent - drowsiness.

    From the gastrointestinal tract: frequent - nausea.

    From the respiratory system: frequent - rhinitis.

    Other: frequent - asthenia, fatigue, malaise.

    Patients with hypertension also had the following adverse reactions (cause-and-effect relationship not established): frequent - tachycardia, palpitation, chest pain; infrequent - angina pectoris, myocardial infarction, arrhythmia; very rare - bradycardia, impaired cerebral circulation.

    Overdose:

    Symptoms: marked decrease in blood pressure, sometimes accompanied by syncope.

    Treatment: the patient is transferred to a horizontal position with a low head and raised legs. Symptomatic therapy (measures aimed at maintaining blood pressure) is performed. Hemodialysis is ineffective.

    Interaction:

    Doxazosin enhances the hypotensive effect / effect of antihypertensive drugs (when used in combination, dose adjustment is required). It is not recommended to take doxazosin simultaneously with other alpha-adrenoreceptor blockers.

    There were no adverse interaction with the simultaneous application of doxazosin and thiazide diuretics, furosemide, beta-blockers, blockers "slow" calcium channels, angiotensin converting enzyme inhibitors, antibiotics, hypoglycemic agents for oral administration, anticoagulants and uricosuric agents.

    Doxazosin has no effect on protein binding of plasma digoxin, phenytoin.

    With simultaneous use of doxazosin with inducers of microsomal oxidation in the liver may increase the efficiency of doxazosin, inhibitors - lowering.

    Non-steroidal anti-inflammatory drugs (especially indomethacin), Estrogens and sympathomimetic drugs can reduce the hypotensive action / effect of doxazosin.

    Cimetidine increases the bioavailability of doxazosin.

    The combined use of doxazosin with PDE5 inhibitors (udenafil, sildenafil, tadalafil, vardenafil) can lead to symptomatic hypotension.

    Doxazosin, eliminating the effects of alpha-adrenostimuliruyuschee epinephrine may lead to the development of hypotension and tachycardia.

    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 during cataract operation, which 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, 1 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 the instructions for use are placed in a pack of cardboard for consumer containers.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-003659/07
    Date of registration:07.11.2007 / 28.06.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Manufacturer: & nbsp
    Representation: & nbspVALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Information update date: & nbsp25.09.2017
    Illustrated instructions
      Instructions
      Up