Doksazozin

General characteristics. Structure:

Active agent: a doksazozina мезилат 2.43 mg (in terms of доксазозин - 2 mg)

Pharmacological properties:

Pharmacodynamics. The selection competitive blocker of postsynaptic alfa1-adrenergic receptors (affinity to alfa1-receptors is 600 times higher, than to alfa2), reduces OPSS, warns the vasoconstriction caused by catecholamines that finally leads to decrease in the ABP without development of reflex tachycardia. Reduces before - and an afterload. After a single dose decrease in the ABP develops gradually, the maximum decrease is observed in 2-6 h; the hypotensive effect remains during 24 h. Increase in coefficient of LPVP is promoted / by the general cholesterol, reduces the summary contents of TG and cholesterol. It is effective at arterial hypertension, including followed by metabolic disturbances (obesity, a lipidemia, decrease in tolerance to glucose). At prolonged treatment regression of a hypertrophy of LZh, suppression of aggregation of thrombocytes, increase in activity in fabrics of the activator of plasminogen (plasminogen) and decrease in formation of collagen in walls of arteries is noted. Reduces risk of development of an ischemic heart disease. Increases the maintenance of APF, development of orthostatic hypotension in response to reception of the first dose is uncharacteristic (can develop only at long reception of high doses). Administration of drug at normotonik is not followed by decrease in the ABP. At patients with a high-quality prostatauxe leads to considerable improvement of urodynamic indicators and reduction of symptoms of a disease. The effect is connected with the selection blockade of alfa1-adrenoceptors of the Ia subtype (70% of all subtypes presented in a prostate) which are localized in a muscular stroma, the prostate capsule, in a neck of a bladder and in proximal department of an urethra that reduces a muscle tone of a prostate and facilitates an urination). Renders effect at 66-71% of patients, the beginning of action - in 1-2 weeks of treatment, at most - after 14 weeks, remains for a long time.

Pharmacokinetics. Absorption - 80-90% (the concomitant use of food slows down absorption on 1 h), TCmax - 2-3 h, at evening reception - 5 h. Bioavailability - 60-70% (presistemny metabolism). Communication with proteins of plasma - about 98%. It is quickly metabolized in a liver by au demethylation and a hydroxylation. Removal from plasma happens in 2 phases. Final T1/2 - 19-22 h. It is removed through intestines, 5% - in not changed look are preferential in the form of metabolites (to 65%); through kidneys about 10% are removed.

Indications to use:

Benign hyperplasia of a prostate (both at obstructive disturbances, and in the presence of inflammation signs), the complicated urine outflow. Arterial hypertension (including symptomatic), HSN.

Route of administration and doses:

Pill should be taken in the morning or for the night (it is better on an empty stomach), without chewing, washing down with enough water. At arterial hypertension and SN an initial dose - 1 mg/days. Depending on reaction of the patient the dose can gradually (from 1-2 weeks an interval) to raise to 2 mg, then to 4-8 mg. The recommended maintenance dose - 2-4 mg/days. At insufficient expressiveness of hypotensive effect perhaps further gradual increase in a dose up to maximum - 16 mg/days or addition of other hypotensive HP (thiazide diuretics, beta adrenoblockers, BMKK, APF inhibitors). At a prostate hyperplasia an initial dose - 1 mg/days. If necessary the dose is increased (with an interval of 1-2 weeks) to 2-4 mg/days. The maximum dose - 8 mg/days. The recommended maintenance dose - 2-4 mg/days. Dosing in special situations. Elderly patients have no need for correction of the mode of dosing, and also at HPN. At patients with a liver failure the dose decline of a doksazozin can be required.

Features of use:

The effect of "the first reception" is especially expressed against the background of the previous diuretic therapy and a diet with restriction of Na+. Against the background of reception of a doksazozin in order to avoid development of orthostatic hypotonia it is necessary to abstain from bystry postural changes of a body. Before symptomatic therapy of a hyperplasia of a prostate it is necessary to exclude its cancer regeneration. During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions. With care. Pregnancy, the lactation period, a liver failure, a mitral and aortal stenosis, orthostatic hypotension, children's age (data on efficiency and safety are absent).

Side effects:

Orthostatic hypotension, dizziness, unconscious states - a phenomenon of "the first dose"; headache, sleeplessness, hypostases, tachycardia, disturbances of a heart rhythm, weakness, asthma, adynamy; dryness in a mouth, a polyuria, a hamaturia, dyspepsia, pathological drowsiness, vision disorders (blurring of the image), a cholestasia, hepatitis, jaundice, increase in activity of "hepatic" transaminases, locks, skin rash, a small tortoiseshell, an itch, thrombocytopenia, a Werlhof's disease, a leukopenia; nasal bleedings, rhinitis, decrease in a libido, thorax pain and/or in a back, disturbance of cerebral circulation. Seldom - an urine incontience, a priapism.

Interaction with other medicines:

Increases expressiveness of action of hypotensive HP (when using a combination with them dose adjustment is required). Not otmechyno adverse interaction at simultaneous use of a doksazozin and antibiotics, peroral hypoglycemic HP, indirect anticoagulants and uricosuric HP. Does not influence extent of linkng with proteins of plasma of digoxin, Phenytoinum, indometacin. At simultaneous use with inductors of a microsomal oxidation in a liver increase in efficiency of a doksazozin, with inhibitors - decrease is possible. Cimetidinum raises AUC of a doksazozin. NPVP (especially indometacin), estrogen (a liquid delay) and sympathomimetic HP can reduce hypotensive action of a doksazozin. Eliminating alpha адреностимулирующие effects of Epinephrinum, can lead to development of tachycardia and hypotension.

Contraindications:

Hypersensitivity (including to other quinazolines).

Overdose:

Symptoms: the expressed decrease in the ABP which sometimes is followed by an unconscious state. Treatment: to lay the patient on a back, having raised legs; symptomatic therapy. Dialysis is inefficient.

Storage conditions:

List B. In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

tablets of 2 mg (planimetric strip packagings)