Doxazosin tabs 4mg #30

Instruction for use of Doxazosin

To buy Doxazosin just add it to your shopping cart

Doxazosin is a drug with hypolipidemic, hypotensive, antispasmodic and vasodilating effects.

Release form and composition

Doxazosin is produced in the form of tablets: from white with a grayish-cream shade to white (7, 10, 14, 20, 25, 30, 50 pcs. In blisters, 1-5 packs in a cardboard box; 10, 14, 20, 28, 30, 50, 100 pcs. In cans or bottles, 1 can or bottle in a cardboard box).
The composition of 1 tablet includes:
    Active ingredient: doxazosin - 1, 2 or 4 mg (in the form of mesylate);
    Auxiliary components: milk sugar, sodium glycolate, starch, magnesium stearic acid, microcrystalline cellulose, sodium lauryl sulfate.

Pharmacodynamics

In benign prostatic hyperplasia (BPH), doxazosin significantly improves urodynamic parameters and reduces the manifestation of symptoms of the disease. This effect is due to the selective blockade of α-adrenergic receptors in the capsule and stroma of the prostate gland, as well as in the bladder neck.
The drug blocks α1-adrenergic receptors of subtype 1A, which make up about 70% of the total number of α1-adrenergic receptors of all subtypes located in the prostate gland. The action of the drug in BPH is based on this mechanism.
The safety and supportive effect of doxazosin treatment has been proven during long-term use of the drug (for example, up to 48 months).
With the use of doxazosin in patients with arterial hypertension, a decrease in the total peripheral vascular resistance is noted, which leads to a significant decrease in blood pressure. This effect is the result of a selective blockade of alpha1-adrenergic receptors in the vascular network.
When taken once a day, the drug provides a clinically significant antihypertensive effect for 24 hours. The decrease in blood pressure occurs gradually. After oral administration, the maximum effect is usually achieved after 2-6 hours. With arterial hypertension, the effect of doxazosin treatment was the same in the standing and lying positions.
It is noted that long-term treatment with doxazosin did not develop tolerance to the drug, in contrast to therapy with nonselective alpha1-blockers. In the course of maintenance therapy, tachycardia and an increase in plasma renin activity are uncommon.
Doxazosin therapy favorably affects the lipid profile of the blood, since in this case the ratio of high density lipoproteins to total cholesterol increases, and the concentration of total cholesterol and total triglycerides is significantly reduced. Treatment with the drug has an advantage over the use of beta-blockers and diuretics, which do not have a beneficial effect on these parameters.
Taking into account the established relationship between the lipid profile of blood, arterial hypertension and coronary heart disease, normalization of blood pressure and lipid concentration that occurs when taking doxazosin helps to reduce the likelihood of coronary heart disease.
It was found that, as a result of doxazosin therapy, regression of left ventricular hypertrophy was observed, platelet aggregation was suppressed, and the activity of tissue plasminogen activator increased. Research has also shown that in patients with impaired glucose tolerance, doxazosin increases insulin sensitivity.
The drug has no metabolic side effects and can be prescribed to patients with bronchial asthma, left ventricular failure, gout and diabetes mellitus.
In vitro, the antioxidant properties of 7 'and 6'-hydroxymetabolites of doxazosin are manifested at a concentration of 5 μmol.
When conducting controlled clinical trials with patients with arterial hypertension, doxazosin therapy was accompanied by an improvement in erectile function. Along with this, in patients who received doxazosin, subsequent erectile dysfunction occurred less frequently than in patients who received antihypertensive drugs.

Pharmacokinetics

After oral administration of therapeutic doses of Doxazosin, the active substance is well absorbed (from 80 to 90%). Its concentration in the blood reaches a maximum after about 2 hours.
The connection with blood plasma proteins is approximately 98%.
The drug is actively biotransformed in the liver. Its metabolites have no pharmacological activity. Bioavailability is about 69-70% (first pass effect). The primary pathways of doxazosin metabolism are hydroxylation and O-demethylation.
The drug is characterized by two-phase elimination from blood plasma. The half-life is 22 hours, which allows you to prescribe the drug once a day. When taken orally, most of doxazosin is excreted through the intestine in the form of inactive metabolites, and in unchanged form - up to 5% of the dose taken.
Data from pharmacokinetic studies of the effect of the drug in elderly patients and in patients with renal insufficiency show that the pharmacokinetics of doxazosin do not differ significantly from that in younger patients with normal renal function.
There are only limited data on the pharmacokinetics in patients with impaired liver function, as well as on the effect of drugs that can alter hepatic metabolism (for example, cimetidine). In a clinical study, a single dose of doxazosin in 12 patients with moderate hepatic dysfunction was accompanied by a 43% increase in AUC (area under the concentration-time curve) and a 40% decrease in true oral clearance.

Indications for use

    Arterial hypertension (as monotherapy or simultaneously with other antihypertensive drugs: beta-blockers, thiazide diuretics, angiotensin-converting enzyme inhibitors or calcium channel blockers);
    Benign prostatic hyperplasia (with normal blood pressure and in the presence of arterial hypertension).

Contraindications

    Age under 18;
    Pregnancy and lactation period;
    Hypersensitivity to the components of the drug.
According to the instructions, Doxazosin should be taken with caution in the following diseases / conditions:
    Pulmonary edema due to mitral or aortic stenosis;
    Left ventricular insufficiency with low filling pressure;
    Insufficiency of the right ventricle of the heart, due to effusion into the pericardial cavity or pulmonary embolism;
    Insufficiency of cardiac output.
Particular care is required to prescribe the drug for functional disorders of the liver, when drugs that can have a negative effect on liver function are simultaneously used. If the indicators of the functional state of the liver deteriorate, Doxazosin should be immediately canceled.

Instructions for use: method and dosage

The drug is taken orally, regardless of food intake. The tablets should be taken with plenty of water without chewing.
The drug is taken once a day (in the morning or evening). The daily dose is determined by the indications:
    Arterial hypertension: the dose can vary from 1 (initial) to 16 mg (maximum). The initial dose is recommended to be taken at bedtime. After taking the drug, the patient must be in bed for 6-8 hours (due to the possible development of the "first dose" phenomenon, especially pronounced after the previous intake of diuretics). After 7-14 days of continuous treatment, in case of insufficient therapeutic effect, it is possible to increase the daily dose by 2 times. If necessary, after the same time interval, you can increase the dose by another 2 mg, and so on until the optimal therapeutic effect is achieved. In the future, after achieving a stable therapeutic effect, the daily dose is usually reduced (with maintenance therapy, the average therapeutic daily dose is 2-4 mg);
    Benign prostatic hyperplasia without arterial hypertension: from 2-4 (usually) to 8 mg (maximum) per day.

Side effects

During therapy, especially at the beginning, orthostatic hypotension most often develops, which in some cases can lead to fainting. To prevent the occurrence of this disorder, it is recommended to avoid abrupt and unexpected changes in body position (transition to a standing position from a prone position).
In addition, when taking Doxazosin, you may experience: nausea, dizziness, headache, a general feeling of weakness, drowsiness, fatigue, and rhinitis. Patients with arterial hypertension can sometimes experience: arrhythmia, tachycardia, chest pain, myocardial infarction, angina attacks, cerebrovascular disorders.
There were also isolated cases of allergic reactions (jaundice, skin rash, increased transaminase levels, thrombocytopenic purpura), nosebleeds, dry mouth, priapism, urinary incontinence, constipation, increased appetite, increased urine output, arthralgia and myalgia.

Overdose

Symptoms: dizziness, headache, shortness of breath, nausea, vomiting, loss of consciousness, a marked decrease in blood pressure, sometimes with concomitant fainting, tachycardia, palpitations, arrhythmia, hypokalemia, hypoglycemia.
Treatment: symptomatic therapy. Blood pressure monitoring is shown. Dialysis is ineffective, since the binding of the active substance to blood plasma proteins is high.

Special instructions

Alcohol increases unwanted reactions.
At the beginning of therapy or during an increase in the daily dose, it is advisable to refrain from performing all potentially hazardous types of work, in particular, from driving a car and other vehicles and mechanisms.

Application during pregnancy and lactation

In the course of experiments on animals, it was proved that doxazosin does not have a teratogenic effect. At the same time, the use of extremely high doses of the substance led to a decrease in fetal survival. As a result, despite the absence of embryotoxic and teratogenic effects in the results of experimental studies, the drug can be prescribed to pregnant women only in cases where the potential benefit to the mother is higher than the potential risk to the fetus.
Studies in rats have shown that doxazosin accumulates in the milk of females.
It is not known whether this substance is excreted in human breast milk. If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Childhood use

It is forbidden to use Doxazosin for the treatment of patients under the age of 18.

With impaired renal function

It is forbidden to use the drug in case of progressive renal failure.

For violations of liver function

It is forbidden to use Doxazosin for severe hepatic impairment. The drug should be used with caution in case of mild to moderate hepatic impairment.

Use in the elderly

When treating elderly patients, the drug should be used with caution.

Drug interactions

With the simultaneous use of Doxazosin with certain drugs, undesirable effects may occur:
    Antihypertensive drugs: increased hypotensive effect;
    Inducers of microsomal oxidation in the liver: an increase in the effect of doxazosin is possible;
    Inhibitors of microsomal oxidation in the liver: may reduce the effect of doxazosin;
    Non-steroidal anti-inflammatory drugs (especially indomethacin), sympathomimetic agents and estrogens: lowering the hypotensive effect;
    Ephedrine: lowering the pressor effect;
    Epinephrine: simultaneously with the elimination of alpha-adrenostimulating effects, it is possible to develop a perversion of its pressor action and tachycardia.
The drug is compatible with furosemide, thiazide diuretics, calcium channel blockers, beta-blockers, angiotensin-converting enzyme inhibitors, oral hypoglycemic agents, antibiotics, uricosuric agents, and indirect anticoagulants.

Terms and conditions of storage

Store in a dark, dry place out of reach of children at a temperature of 5-25 ° C.
Shelf life is 2 years.

Reviews

Reviews of Doxazosin from users with BPH indicate that when taking this drug, there is often an improvement in the condition, but complete recovery does not occur. Many men note that while taking pills and carrying out physiotherapy procedures, they feel better, but after stopping therapy, the manifestations of the disease return.
The effectiveness of the use of Doxazosin in the treatment of arterial hypertension is assessed by users in different ways. In such cases, the drug is often used as part of complex therapy.
In any case, users note that Doxazosin can only be used as directed by a specialist and under medical supervision.

Terms of sell

You can buy Doxazosin without a prescription from a doctor.