Doxazosin

Chemical name

1-(4-Амино-6,7-диметокси-2 -хиназолинил)-4-[(2,3-диг��дро-1,4-бензодиоксин-2-��л)карбонил]пиперазин (and in the form of monometanculfonata)

Gross

C23-H25-N5-O5

Characteristics

Powder white. Easily soluble in demetilsulfoxide, soluble in dimethylformamide, it is difficult soluble in methanol, ethanol, water, acetone, metilenhloride.

Of drugs

The drugs-gipotenzivne, sossoudorasshiratee, gipolipidemicescoe, skin. Yes blocks postsinapticalkie альфа_1-адренорецепто��ы (ratio affinity to alfa_1 / alfa_2 less than 600). Impact round. Antigipertenzivny effect partly due ekranirovaniem альфа_1-адренорецепто��ов in the central nervous system. Adrainoliticescoe the more so receptacles kidney, skin, to a lesser, in crevnykh, cerebral and pulmonary vessels. During physical activity vazodilatiruty impact heavily expressed in the kidneys and skin and less - in muscles. Impact of pre - and postnagruzku, reduces the need for hospitalization of oxygen. Structured AD falls moderately without a reflex tachycardia. Reducyruet level of cholesterol, aterogennah lipoprotein fractions and adds LPVP. Suppress collagen synthesis in the vascular wall. Ingibiruet agregatia platelets, increases concentration woven plazminoguena activator. Provides tone gladkomyshechnykh stroma cells and capsules prostate, and the bladder neck Puzyr.pri introduction into rats quickly and adequately. The material is only 62-69%, which reflects the effect of a "through the liver. C_max achieved in 2-3 hours The evening reception for the C_max extended to 5 p.m. The plasma 98-99% drug linked to the protein. Biotransformiroetsa intensively in the liver, mainly by demethylation or gidrauxilirovania. A few active metabolites. T_1/2 - 19-22 h. Included in enterogepaticescuu circulation, and therefore, most of the (63%) excreted through the intestine with faeces, including 5-19% in unmodified form; the kidney is only 9%. The show starts at 1-2 h after administration of inwards and reaches its maximum at 5-6 hours Antigipertenzivny effect develops gradually and continues until 24 h, persisting for reversing the position of a body. Violation of the liver lengthens effect. With long-term use AD declining by an average of 22/15 mm Hg Down the isolationist left chamber. The effect of the first dose in the form of postural hypotonia expressed slightly. Ortostatical gipotenzia can develop only with a long reception of high doses. Effective in isolation sistolicescoy hypertension and its combination with metabolic disorders (obesity, giperlipidemia, reduced tolerance to glukoze). In heart failure reduces release predserdnyi natriyureticski peptide. Often used for the treatment of elderly patients with adenoma prostate gland. While operational when conservative therapy : effects estimate of 9 to 18 points IPSS (International system total of symptoms). The full extent reducing obstructive and inflammatory symptoms associated with giperplaziei prostate cancer (incomplete emptying of the bladder, nictoria, increases urination, FIRE), and the improvement of the urodynamics in 66-71% of patients. Improvement usually occurs within 1-2 weeks of treatment, reaching a peak at 14 weeks and remained for a long time. Admission to the drug normotonikov not accompanied by a decline in AD.

Indications

Arterial hypertension (monotherapy and combination with others antigipertenzivei drugs), including sistolical isolated hypertension in older men, hypertension in the face of the metabolic, chronic heart failure, feohromotsytoma, Good giperplazia prostate cancer (as of obstructive violations, and if there are signs of inflammation), the difficulty of urine outflow.

Contraindications

Hypersensitivity, stenoses aortalni and mitral valves, tromboembolia pulmonary artery severe violations of the liver, pregnancy, child.

Side-Effects

The "first dose" - hypotension, dizziness, sincopale state (rarely); Posturalnaya ortostatical hypotension (with the long-term care), edema, tachycardia, in rhythm, fatigue, shortness of breath, dizziness, headache, nervousness, irritability, pathological drowsiness, zatumanennosti view, rhinitis, xerostomia, discomfort in the abdomen, nausea, obstipation, pain in the chest, a violation of cerebral circulation, urinary (rarely).

Overdosing

Symptoms : gipotenzia, sincopale Sostojania.lechenie : it is necessary to give the patient a horizontal position on the back, head to torso, in the case of failure in / in infusions and the introduction vazopressornah drugs.

Precautions

It must be borne in mind that the effect of the first reception led to a dioreticescoy therapy, as well as diet restricted sodium. The elderly reduce the dosage. When driving vehicles and work in the workplace should take into account the possibility Orthostatic Hypotension, and the lowering of concentration and the reaction rate (normally at the beginning of treatment). To use caution if there is a violation of the functions of the liver. Before therapy sound hyperplasia of prostate cancer should be deleted its cancer transformation.

Dosing and Administration

Inside. Starting treatment with 1 mg / day, one with a steady increase (in 1-2 weeks) and 2 mg, then to 4-8 mg. The maximum daily intake for good hyperplasia prostate-8 mg, and hypertension - 16 mg in a single admission.

Directory → Organotropona funds → The governing bodies of the urinary and reproduction → Funds affecting the metabolism of the prostate gland and correctors urodynamics → Doxazosin