Instruction for use: Doxazosin

Trade name of the drug – Doxazosin

Active substance: Doxazosinum

Chemical rational name: 1- (4-Amino-6,7-dimethoxy-2-quinazolinyl) -4 - [(2,3-dihydro-1,4-benzodioxin-2-yl) carbonyl] piperazine (in the form monomethanesulfonate)

Dosage Form: tablets

Composition (per tablet): 1 tablet comprises 2.43 mg of doxazosin mesylate (calculated as base - 2 mg), as well as auxiliary substances (milk sugar, sodium glycolate, starch, magnesium stearate, MCC, sodium lauryl sulfate); in blisters of 10 or 25 pc., in a cardboard unit 1, 2, 3, 4 or 5 packages or in banks or in polystyrene bottles of 30, 50 or 100 pcs., in a cardboard bundle one bank or 1 bottle.

Pharmacotherapeutic group: Alpha-blockers

Drugs affecting the metabolism of the prostate gland and correctors urodynamics

ATX C02CA04 Doxazosin

The nosological classification (ICD-10)

I10 Essential (primary) hypertension: hypertension; Arterial hypertension; Arterial hypertension crisis course; Essential Hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Primary hypertension; Arterial hypertension, complications of diabetes; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; arterial Hypertension; malignant Hypertension; Hypertonic disease; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; Isolated systolic hypertension

I15 Secondary hypertension: Arterial hypertension, complications of diabetes; hypertension; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; hypertension; arterial Hypertension; malignant Hypertension; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; hypertension; Arterial hypertension; Arterial hypertension crisis course; renovascular hypertension; Hypertension symptomatic; Renal hypertension; Renovascular hypertension; renovascular hypertension; Symptomatic hypertension

N40 Hyperplasia of prostate gland: Prostate adenoma; BPH; Prostatauxe; prostate Hypertrophy; Dysuric disorders caused by benign prostatic hyperplasia; Dizuricheskie disorder with benign prostatic hyperplasia; Dysuria with prostate cancer; Benign prostatic giperpalaziya; Benign prostatic hyperplasia; Benign prostatic hyperplasia stages 1 and 2; Benign prostatic hyperplasia I degree; Benign prostatic hyperplasia II degree; Benign prostatic hypertrophy; The disease of the prostate gland; Acute urinary retention related to benign prostatic hyperplasia; Benign prostatic hyperplasia stages 1 and 2 in combination with prostatitis; paradoxical ischuria

Pharmacological Properties of Doxazosin

Pharmachologic effect - Mode of action - vasodilator, antispasmodic, antihypertensive, lipid-lowering.

Selectively blocks postsynaptic alpha1-adrenergic receptors. By reducing vascular tone muscles reduces peripheral vascular resistance and lowers blood pressure. It reduces the concentration of triglycerides, total cholesterol and HDL cholesterol in the plasma. Simultaneously, there is a slight increase in HDL ratio with respect to total cholesterol (at 4-13%). Inhibits platelet aggregation and increases the content of active tissue plasminogen. It reduces the tonus of smooth muscle of the stroma and prostate cancer cells capsule and bladder neck. Resistance and lowers the pressure in the urethra, internal sphincter resistance decreases.

Pharmacodynamics

After a single dose of the hypotensive effect is achieved in 2-6 hours and lasts for 24 hours. In the period of treatment in hypertensive patients with no differences in blood pressure values in the standing and lying down. Long-term treatment is observed regression of left ventricular hypertrophy.

Pharmacokinetics

Well absorbed after oral administration. Absorption - 80-90% (together with food slows absorption by 1 h), Cmax is reached after 3 hours, while taking in the evening after 5 hours Bioavailability -. 60-70% (first pass metabolism). Binding to plasma proteins - about 98%. Rapidly metabolized in the liver by o-demethylation and hydroxylation. Elimination from the plasma takes place in 2 phases, T1 / 2 -. 19-22 hours Provided mainly through the intestine in the form of metabolites, 5% excreted in the urine in unchanged form.

Indications for Doxazosin

Arterial hypertension (monotherapy or in combination with other antihypertensive drugs: thiazide diuretics, beta-blockers, calcium channel blockers or ACE inhibitors), benign prostatic hyperplasia (in the presence of hypertension and normal blood pressure).

Contraindications for Doxazosin

Hypersensitivity, pregnancy, breast-feeding, age and 18 years of age.

Pregnancy and breast-feeding

Contraindicated. At the time of treatment should stop breastfeeding.

Doxazosin Dosage and Administration

Inside, regardless of meals, without chewing and drinking plenty of water, 1 time a day (morning or evening).

When hypertension: a dose range from 1 to 16 mg / day (maximum); the initial dose - 1 mg 1 time a day (at night), then the patient should be in bed for 6-8 hours (perhaps the phenomenon of "first dose", especially pronounced on the background of the previous diuretics). When insufficient therapeutic effect daily dose increased to only 2 mg 1-2 weeks of continuous treatment, then every 1-2 weeks the dose is increased by 2 mg to achieve optimum therapeutic effect. After reaching a stable therapeutic effect of the dose is usually reduced (the average therapeutic dose for maintenance therapy - 2-4 mg / day).

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

Side effect of Doxazosin

When applying doxazosin, especially at the beginning of treatment, the most frequently observed postural hypotension, which in rare cases can cause fainting. In order to prevent orthostatic hypotension, patients should avoid unexpected and sudden shifts in body position (transition from a lying position to a standing position).

May include the: headache, dizziness, general feeling of weakness, fatigue, drowsiness, rhinitis, nausea. In patients with hypertension rarely observed: tachycardia, arrhythmia, chest pain, angina pectoris, myocardial infarction, cerebrovascular disorders.

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

Overdose of Doxazosin

Symptoms: marked reduction of blood pressure, sometimes accompanied by fainting.

Treatment: it is necessary to transfer the patient to a horizontal position (lower her head down, lift the legs), symptomatic therapy.

Interaction

It enhances the hypotensive 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 may increase the effect of inhibitors - lowering. NSAIDs (especially indomethacin), estrogen and sympathomimetic agents reduce the hypotensive effect. It decreases the pressor effect of ephedrine. Eliminating alpha adrenostimuliruyuschee effects of epinephrine may lead to a distortion of its pressor effect and development of tachycardia.

SPECIAL INSTRUCTIONS for Doxazosin

With caution is prescribed for pulmonary edema, caused aortic or mitral stenosis; failure of the right ventricle of the heart caused by pulmonary embolism or pericardial effusion; left ventricular insufficiency of filling with low pressure; Cardiac insufficiency. With caution is prescribed for abnormal liver function, when both used drugs that can affect liver function. In case of deterioration of the functional state of the liver drug should be discontinued immediately.

At the beginning of treatment or during dosage increase is expedient to refrain from any potentially dangerous activities, in particular from road transport management and other vehicles and machinery.

Alcohol may increase adverse reactions.

Storage conditions of Doxazosin

In a dry, dark place at a temperature 5 - 25 ° C.

Keep out of the reach of children.

Shelf life

2 years.

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

Conditions of supply of pharmacies

On prescription.