Description
Release form
Tablets
Packing
30 pcs.
Pharmacological action
Doxazosin – hypolipidemic, hypotensive, antispasmodic, vasodilator.
Selectively blocks postsynaptic alpha1-adrenergic receptors. By reducing the tone of the muscles of the vessels reduces OPSS and lowers blood pressure. It reduces the concentration of triglycerides, total cholesterol and HDL in plasma. At the same time, there is a slight increase in the HDL ratio relative to total cholesterol (by 4 13%).
Suppresses platelet aggregation and increases the content of active plasminogen in tissues. Reduces the tone of the smooth muscle cells of the stroma and capsules of the prostate gland, as well as the neck of the bladder. Reduces resistance and pressure in the urethra, reduces the resistance of the internal sphincter.
Pharmacodynamics
After a single dose, the hypotensive effect is achieved after 2-6 hours and persists for 24 hours. During treatment, patients with arterial hypertension do not have differences in the values of blood pressure in standing and lying down. With prolonged treatment, regression of left ventricular hypertrophy is observed.
Pharmacokinetics
Well absorbed after oral administration. Absorption – 80 90% (simultaneous food intake slows down absorption by 1 hour), Cmax is reached after 3 hours, when taken in the evening after 5 hours. Bioavailability is 60 70% (presystem metabolism). Plasma protein binding is about 98%. It is rapidly metabolized in the liver by o-demethylation and hydroxylation.
Excretion from plasma occurs in 2 phases, T1 / 2 – 19-22 hours. It is excreted through the intestine mainly in the form of metabolites, 5% is excreted unchanged in the urine.
Contraindications
Hypersensitivity, pregnancy, lactation, age up to 18 years.
Use during pregnancy and lactation
Contraindicated.
Composition
Active ingredient:
doxazosin mesylate 2 mg
Dosage and administration
Inside, regardless of food intake, without chewing and drinking with enough water, 1 time per day (morning or evening).
In arterial hypertension: doses vary from 1 to 16 mg / day (maximum), the initial dose is 1 mg 1 time per day (at bedtime), after this, the patient should be in bed for 6-8 hours (the development of the phenomenon of “first dose”, especially pronounced against the background of the previous intake of diuretics, is possible).
If the therapeutic effect is insufficient, the daily dose is increased to 2 mg only after 12 weeks of continuous treatment, then with an interval of 12 sub-doses is increased by 2 mg until the optimal therapeutic effect is achieved.
After achieving a stable therapeutic effect, the dose is usually reduced (the average therapeutic dose with maintenance therapy is 24 mg / day).
In benign prostatic hyperplasia without arterial hypertension: usually 24 mg / day, maximum dose 8 mg / day.
Side effects of
When using doxazosin, especially at the beginning of treatment, orthostatic hypotension is most often observed, which in rare cases can lead to fainting. In order to prevent orthostatic hypotension, patients should avoid sudden and abrupt changes in body position (transition from a lying position to a standing position).
May occur: headache, dizziness, general feeling of weakness, fatigue, drowsiness, rhinitis, nausea. In patients with arterial hypertension rarely noted: tachycardia, arrhythmia, chest pain, angina attacks, myocardial infarction, cerebrovascular disorders.
There have been isolated cases of allergic reactions (skin rash, jaundice, thrombocytopenic purpura, increased transaminases), dry mouth, nosebleeds, priapism, urinary incontinence, increased appetite, constipation, increased urine output, myalgia, arthralgia.
Drug Interactions
Enhances the antihypertensive effect of antihypertensive drugs. Compatible with thiazide diuretics, furosemide, beta-blockers, calcium channel blockers, ACE inhibitors, antibiotics, oral hypoglycemic agents, indirect anticoagulants and uricosuric agents.
When combined with inducers of microsomal oxidation in the liver, an increase in the effect is possible, with inhibitors, a decrease. NSAIDs (especially indomethacin), estrogens, and sympathomimetic drugs lower the hypotensive effect.
Reduces the pressor effect of ephedrine. Eliminating the alpha-adrenostimulating effects of epinephrine, can lead to a distortion of its pressor action and the development of tachycardia.
Overdose
Symptoms: marked decrease in blood pressure, sometimes accompanied by fainting.
Treatment: it is necessary to transfer the patient to a horizontal position (lower your head down, raise your legs), symptomatic therapy.
Storage conditions
In a dark place, at a temperature of 5-25 ° C.
Term hodnosty
2 years
active substance
Doxazosin
Terms leave through pharmacies
In retseptu
lekarstvennaja form
tablets
Obolensky AF Russian
