Doxazosin-FPO, tablets 2 mg 30 pcs

Doxazosin is hypolypidemic, hypotensive, antispasmodic, vasodilator.

It selectively blocks postsynaptic alpha1-adrenoreceptors. By reducing the tone of the vascular muscles, it reduces the RAS and lowers BP. It decreases concentrations of triglycerides, total cholesterol and HDL in plasma. At the same time there is a slight increase in HDL to total cholesterol ratio (by 4-13%).

Inhibits platelet aggregation and increases the content of active plasminogen in tissues. Reduces the tone of the smooth muscle cells of the stroma and capsule of the prostate as well as the bladder neck. Lowers resistance and pressure in the urethra, reduces the resistance of the internal sphincter.

Pharmacodynamics

The hypotensive effect is achieved in 2-6 hours after single administration and persists for 24 hours. During treatment, there is no difference in BP values in standing and lying position in patients with arterial hypertension. With long-term treatment regression of left ventricular hypertrophy is observed.

Pharmacokinetics

It is well absorbed after oral administration. Absorption is 80-90% (simultaneous intake slows down absorption by 1 hour), Cmax is reached after 3 hours, when taken in the evening after 5 hours.

Bioavailability – 60-70% (presystemic metabolism). Binding to plasma proteins is about 98%. It is quickly metabolized in liver by o-demethylation and hydroxylation. Excretion from plasma occurs in two phases, T1/2 – 19-22 hours. It is excreted through the intestine mainly as metabolites, 5% is excreted unchanged in the urine.

Indications

Arterial hypertension (monotherapy and in combination with other antihypertensive agents: thiazide diuretics, beta-adrenoblockers, calcium channel blockers or ACE inhibitors), benign prostatic hyperplasia (if arterial hypertension and normal BP).

Active ingredient

Composition

Active ingredient:

doxazosin mesylate;

Supplements:

dairy sugar,

sodium glycolate,

starch,

magnesium stearate,

MCC,

sodium lauryl sulfate

How to take, the dosage

Overly, regardless of meals, without chewing and with plenty of water, once daily (morning or evening).

In arterial hypertension: doses range from 1 to 16 mg/day (maximum); the initial dose is 1 mg once daily (before bedtime), after which the patient should be in bed for 6-8 hours (development of “first-dose” phenomenon is possible, especially pronounced with prior diuretics).

If the therapeutic effect is insufficient, the daily dose is increased to 2 mg only after 1-2 weeks of continuous treatment, then at intervals of 1-2 weeks the dose is increased by 2 mg until optimal therapeutic effect is achieved.

After achieving a sustained therapeutic effect, the dose is usually reduced (the average therapeutic dose for maintenance therapy is 2-4 mg/day).

In benign prostatic hyperplasia without arterial hypertension: usually 2-4 mg/day, maximum dose is 8 mg/day.

Interaction

Enhances the hypotensive effect of antihypertensive drugs.

Compatible with thiazide diuretics, furosemide, beta-adrenoblockers, calcium channel blockers, ACE inhibitors, antibiotics, oral hypoglycemic agents, indirect anticoagulants and uricosuric agents.

When combined with inducers of microsomal oxidation in the liver may increase the effect, with inhibitors – a decrease. NSAIDs (especially indomethacin), estrogens and sympathomimetic agents decrease the hypotensive effect.

Decreases the pressor effect of ephedrine. By eliminating the alpha-adrenergic stimulating effects of epinephrine, may lead to perversion of its pressor effect and development of tachycardia.

Contraindications

Hypersensitivity, pregnancy, lactation, age under 18 years.

Side effects

When using doxazosin, especially at the beginning of treatment, orthostatic hypotension is the most common, which in rare cases may lead to fainting. In order to prevent orthostatic hypotension, patients should avoid sudden and abrupt changes in body position (from lying down to standing up).

Headache, dizziness, general weakness, fatigue, drowsiness, rhinitis, nausea may occur. Patients with arterial hypertension rarely report: tachycardia, arrhythmia, chest pain, angina attacks, myocardial infarction, and cerebrovascular disorders.

There have been single cases of allergic reactions (skin rash, jaundice, thrombocytopenic purpura, increased transaminases), dry mouth, nosebleeds, priapism, urinary incontinence, increased appetite, constipation, increased diuresis, myalgia, arthralgia.

Overdose

Symptoms: marked BP decrease, sometimes accompanied by fainting.

Treatment: the patient should be moved to a horizontal position (put the head down, raise the legs), symptomatic therapy.

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