Dalfuzin

General characteristics. Structure:

International and chemical names: alfuzocin, (RS) - N-[3-[(4-amino-6,7-dimetoksikhinazolin-2-silt) (methyl) of amine] spent on drink } tetrahydrofuran-2-karboksamida hydrochloride; Main physical and chemical properties: tablets of a round form with a biconvex surface, film coated, slight pink-brown color; Structure: one tablet contains an alfuzozin of a hydrochloride of 0,005 g; Excipients: cellulose microcrystallic 102, calcium hydrophosphate a dihydrate, колидон SR, povidone (30), the castor oil hydrogenated magnesium stearate, Sepifilm 752 Blanc or Spectrablend White, ferrous oxide yellow, ferrous oxide red;

Pharmacological properties:

Pharmacodynamics. Anti-dysuric means. Selectively blocking the postsynaptic _{alfa1-adrenoceptors} located in the field of a triangle of a bladder, an urethra and a prostate eliminates a spasm of sphincters of a bladder, urethra and prostate, reduces intra urethral pressure. Improves parameters of urodynamic: reducing a tone of an urethra and resistance to outflow from a bladder, considerably increases the maximum speed of current of urine, facilitates process of its emptying, considerably reduces the residual volume of urine; causes a strong desire to an urination owing to increase in volume of urine.

Pharmacokinetics. It is well soaked up from digestive tract. The maximum concentration in a blood plasma is reached in 3 h. Linkng with proteins of a blood plasma makes about 90 %. An elimination half-life of an alfuzozin — 8 h. Only 11 % of an alfuzozin are removed in not changed view with urine. It is metabolized in a liver, the most part of inactive metabolites (75-91 %) is removed with a stake.

At patients of advanced age higher plasma concentration and bioavailability (it is possible due to decrease in metabolism in a liver) is noted, the volume of distribution goes down, the elimination half-life remains invariable. Patients with a renal failure have a volume of distribution and the general clearance of an alfuzozin increase (perhaps due to reduction of extent of linkng with proteins of a blood plasma). Even in case of a heavy renal failure does not kumulirut owing to intensive biotransformation. At chronic heart failure pharmacokinetic parameters do not change.

Indications to use:

Symptomatic treatment of a benign hyperplasia of a prostate.

Route of administration and doses:

Appoint to adult men inside after food, without chewing, on 1 tablet (5 mg) in the morning and in the evening. To patients of advanced age, and also patients with a renal failure and/or to the patients receiving anti-hypertensive therapy appoint on 1 tablet in the evening, and if necessary increase a dose to 2 tablets (in the morning and in the evening).

The maximum daily dose — 2 tablets (10 mg).

Features of use:

At the patients with coronary heart disease, arterial hypertension, a renal failure receiving anti-hypertensive therapy dose adjustment is necessary. If against the background of therapy deterioration in a course of stenocardia is observed, drug should be cancelled. It is possible to appoint drug both in the presence of arterial hypertension, and at the normal level of arterial pressure, in the latter case the lowering of arterial pressure is insignificant.

As at administration of drug development of hypotension and dizziness is possible, it is not recommended to manage vehicles or to perform work which requires special attention.

Drug is not intended for use for women and children.

Side effects:

 From TsNS: headache, dizziness, sonitus, weakness; seldom — a syncope, an adynamy, drowsiness.  From cardiovascular system: seldom — orthostatic hypotension, palpitation, tachycardia, an aggravation of symptoms of stenocardia (at patients with coronary heart disease), pain in a breast, hypostases, inflows.  From the alimentary system: nausea, diarrhea, pain in epigastric area, it is rare — dryness in a mouth. Other: seldom — skin rashes, an itch.

Interaction with other medicines:

It is incompatible with other _{alfa1-adrenoblockers}. Drug exponentiates effects of anti-hypertensive means and the general anesthetics (instability of arterial pressure is possible).

Contraindications:

Hypersensitivity to drug components, orthostatic hypotension, a concomitant use of other _{alfa1-adrenoblockers}, a liver failure.

Overdose:

Symptoms: arterial hypotension. The patient has to is in a prone position. Treatment: symptomatic - introduction of vasoconstrictors, solutions of the high-molecular substances increasing the volume of whole blood. The hemodialysis is ineffective.

Storage conditions:

To store in protected from light and the place, unavailable to children, at a temperature not above 25 °C. Period of validity 2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging. On the 3rd blister strip packagings in a pack.