Active substanceDoxazosinDoxazosin
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  • Dosage form: & nbspPills.
    Composition:
    1 tablet contains
    active substance
    doxazosin 1, 2 or 4 mg of doxazosin mesylate.
    Excipients:
    microcrystalline cellulose, sodium starch glycolate, magnesium stearate, sodium lauryl sulfate, lactose monohydrate.
    Description:
    Tablets 1 mg - round, slightly biconvex tablets of white color with bevelled edges.
    Tablets 2 mg and 4 mg round, flat tablets of white color with bevelled edges and notching on one side.
    Pharmacotherapeutic group:Alpha 1 - adrenoblocker
    ATX: & nbsp

    C.02.C.A.04   Doxazosin

    Pharmacodynamics:
    Doxazosin is a selective competitive blocker of postsynaptic alpha1- adrenergic receptors. By reducing the tone of the muscles of blood vessels doxazosin reduces the overall peripheral vascular resistance, which leads to a decrease in blood pressure (BP). 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 the values ​​of blood pressure 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.
    Admission of the drug in "normotonics" is not accompanied by a decrease in blood pressure. With prolonged use of doxazosin in patients, there is no change in tolerance to the therapeutic antihypertensive effect.
    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 HDL / total cholesterol ratio.
    With prolonged treatment with doxazosin, regression of left ventricular hypertrophy, suppression of platelet aggregation and an increase in active plasminogen in tissues are observed.
    Due to doxazosin blocks alpha1 - 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, the appointment of doxazosin to patients with symptoms of benign prostatic hyperplasia leads to a significant improvement in urodynamics and a decrease in 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 absorbed - 80-90% (simultaneous intake of food slows down absorption by 1 hour), time to reach a maximum concentration of -3 hours, with evening reception - the time for reaching the maximum concentration is extended to 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 - 19-22 hours, which allows you to prescribe the drug once a day.
    Intensively metabolized in the liver by o-demethylation and hydroxylation. 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. The main excretion through the intestine, mainly in the form of metabolites, only 5% is excreted in the urine unchanged. The kidneys show 10%. A study of the pharmacokinetics of doxazosin in elderly patients and patients with kidney disease did not reveal significant pharmacokinetic differences.
    Indications:The drug is recommended for the treatment of mild to moderate arterial hypertension (in combination with other antihypertensive agents - thiazide diuretics, beta adrenoblockers, slow calcium channel blockers, angiotensin converting enzyme (ACE) inhibitors) and for symptomatic treatment of benign prostatic hyperplasia .
    Contraindications:Camirin should not be administered to patients with hypersensitivity to doxazosin and other quinazoline derivatives (prazozin, terazosin) or to other components of the drug, under the age of 18 years (efficacy and safety not established).
    Carefully:Aortic or mitral stenosis, impaired liver function, orthostatic hypotension.
    Pregnancy and lactation:Pregnant women can prescribe the drug only for vital signs, when the benefit to the mother exceeds the potential risk for the fetus / child. Safety of the drug in infants is not established, therefore, it is recommended that nursing mothers stop feeding during doxazosin treatment.
    Dosing and Administration:
    Inside, 1 time per day (morning or evening), regardless of food intake, without chewing and drinking with sufficient water.
    The dose of the drug to adjust depending on the effectiveness of the drug or possible side effects of specific patients. Patients with hepatic insufficiency require lower doses due to a slowed metabolism of the drug. If the patient forgot to take the drug at the usual time, he should take the appropriate dose of the drug 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). It is important to take the drug regularly. If the patient did not take the drug for several days, the new therapeutic course should begin with the lowest dose.
    Arterial hypertension: the initial dose of Camirena® is 1 mg per day. The first dose should be taken 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 developing a "first-dose phenomenon", especially pronounced against the background of previous intake of diuretics.
    Depending on the therapeutic effect of the drug, the dose can be gradually increased at intervals of 1-2 weeks to 2 mg, 4 mg and 8 mg 1 time per day. Typically, the usual daily dosage is from 2 mg to 8 mg. The maximum daily dose is 16 mg.
    If the therapeutic effect is not enough, patients can simultaneously receive other antihypertensive agents: beta-blockers, diuretics, slow calcium channel blockers, and ACE inhibitors.
    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).
    Benign hyperplasia prostate gland in patients with normal blood pressure: the initial dose is 1 mg of Camiren® per day. The patient should take the first dose in the evening before bedtime. Depending on the effect of the drug, the dose can be gradually increased at intervals of 1-2 weeks to 2 mg, 4 mg and 8 mg once a day. Typically, the average daily dose is from 2 mg to 4 mg. The maximum daily dose is 8 mg.
    Benign hyperplasia prostate gland in patients with arterial hypertension: the dose of the drug is the same,as in the case of hypertension without benign prostatic hyperplasia (see doses for arterial hypertension).
    The drug is used for a long time. The duration of treatment is determined by the attending physician.
    Side effects:
    Doxazosin enhances the antihypertensive effect of antihypertensive agents.
    There was no adverse interaction with simultaneous use of doxazosin with thiazide diuretics, furosemide, beta-blockers, slow calcium blockers: channels, ACE inhibitors, antibiotics, oral hypoglycemic agents, indirect: anticoagulants and uricosuric agents.
    With simultaneous use with induction of microsomal oxidation in the liver, it is possible to increase the effectiveness of doxazosin, with inhibitors - decrease. Non-steroidal anti-inflammatory drugs (especially indomethacin), estrogens (fluid retention) sympathomimetic agents can reduce the hypotensive effect of doxazosin. In countries, alpha-adrenostimulating effects of epinephrine, can lead to tachycardia of arterial hypotension.
    Overdose:
    Overdose
    Symptoms: marked decrease in blood pressure, sometimes accompanied by fainting.
    Treatment: the patient must immediately put in a horizontal position, lower his head down, raise his legs. Symptomatic therapy is performed. Dialysis is ineffective.
    Interaction:
    Doxazosin enhances the antihypertensive effect of antihypertensive agents.
    There was no adverse interaction with concomitant use of doxazosin with thiazide diuretics, furosemide, (β-adrenoblockers, slow calcium blockers: channels, ACE inhibitors, antibiotics, oral hypoglycemic agents, indirect: anticoagulants and uricosuric agents.
    With simultaneous use with induction of microsomal oxidation in the liver, an increase in the efficacy of doxazosin, with inhibitors, a decrease. Non-steroidal anti-inflammatory drugs (especially indomethacin), estrogens (fluid retention) sympathomimetic agents can reduce the hypotensive effect of doxazosin. In countries, alpha-adrenostimulating effects of epinephrine, can lead to tachycardia of arterial hypotension.
    Special instructions:
    During the application of the drug Camyrin®, patients should be warned about the possibility of developing orthostatic hypotension.
    Postural effects, including fainting, are particularly likely after the first dose of Kamiren® . Therefore, the first dose of the drug (1 mg) is taken in the evening, before bedtime. The dose of Kamiren® should be increased gradually, at intervals of 1 or 2 weeks. Against the backdrop of using the drug Camiren®, in order to avoid the development of orthostatic hypotension, you should refrain from rapid changes in body position.
    The drug Camiren® is not recommended for people with lowered blood pressure. Caution should be exercised when using phosphodiesterase-5 inhibitors and Camiren®, since blood pressure can be reduced. A 6-hour interval between applications must be observed inhibitors of phosphodiesterase-5 and the use of the drug Camiren® (to reduce the risk of lowering blood pressure treatment start with the use of phosphodiesterase-5 inhibitors).
    When surgical interventions for cataracts against the backdrop of the use of the drug Camiren®, the development of the syndrome of intraoperative iris of the iris can be considered, which must be taken into account in the preoperative preparation of the patient and the surgical intervention.
    There are reports of cases of development of prolonged erection and priapism in the background of therapy alpha 1-adrenoblockers. 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.
    If liver function is impaired (especially with the simultaneous use of drugs with hepatotoxic action), a minimal dose of Camiren® should be used. In case of worsening of the parameters of the functional state of the liver, the drug Camiren® must be canceled.
    Before the onset of symptomatic therapy of prostatic hyperplasia it is necessary to undergo an examination with an oncologist.
    Special information on auxiliary substances The drug Camiren® contains lactose, in connection with which the use of the drug is not recommended for patients with intolerance lactose, a deficiency of lactase or a syndrome of glucose galactose malabsorption.
    Form release / dosage:
    Tablets of 1, 2 and 4 mg.
    Packaging:
    For 10 tablets in a blister of PVC / PVDH-aluminum foil.
    2 or 3 blisters in a cardboard pack together with instructions for use.
    Storage conditions:

    Store at a temperature not exceeding 30 ° C.

    Keep out of the reach of children.

    Shelf life:
    5 years.
    Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N012827 / 01
    Date of registration:14.12.2011 / 17.11.2015
    The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
    Manufacturer: & nbsp
    Information update date: & nbsp21.01.2016
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