Дальфаз® WEDNESDAY

General characteristics. Structure:

One tablet contains 10 mg of an alfuzozin of a hydrochloride.

First layer   of Gipromelloz                      of 79,75 mg
Castor oil the hydrogenated                13,50 mg
                                         Mg ethyl cellulose 20 5,00
Dye ferrous oxide yellow (E172)       of 0,25 mg
Silicon dioxide of colloid water         0,50 mg
Magnesium stearate                                            of 1,00 mg
Second layer    of Alfuzozin hydrochloride   of 10,00 mg
Mannitolum                                                     of 10,00 mg
Gipromelloza                                              of 10,00 mg
Cellulose of microcrystallic               65,00 mg
Povidone                                                       of 3,20 mg
Silicon dioxide of colloid water         1,25 mg
Magnesium stearate                                            of 1,00 mg
Third layer    of Gipromelloz                       of 114,01 mg
Castor oil the hydrogenated                 27,90 mg
Povidone                                                       of 4,72 mg
Dye ferrous oxide yellow (E172)        of 0,15 mg
Silicon dioxide of colloid water           1,05 mg
Magnesium stearate                                             of 2,17 mg

Description. Round biconvex three-layered tablets: one white layer between two yellow layers with various intensity of coloring. Impregnations are allowed.

Pharmacological properties:

Pharmacodynamics. Alfuzozin is derivative quinazoline, active at oral administration.
This is the selective antagonist postsynaptic an alpha of 1 adrenoceptors. Pharmacological tests of in vitro showed selectivity of action of an alfuzozin on alpha 1 - the receptors located in a prostate at the bottom of a bladder and in a prostatic part of an urethra.
As a result of direct impact on smooth muscles of tissues of prostate gland, alpha 1 - adrenoblockers reduce resistance to urine outflow.
Alfuzozin improves urination parameters, reducing a tone of an urethra and resilience of outflow from a bladder, and facilitates emptying of a bubble.
In placebo - the controlled tests of an alfuzozin at patients with a benign hyperplasia of a prostate it was revealed:
- significant increase in the maximum speed of current (Qmax) on average for 30% at patients with Qmax <15 ml / page. Such improvement was observed, since the first dose;
- considerable decrease in resistance to current of urine and increase in volume of the emitted urine;
- considerable decrease in residual volume of urine.

Pharmacokinetics. The average of values of relative bioavailability makes 104,4% in comparison with a form of immediate release (2,5 mg twice a day) at healthy volunteers of middle age, and the maximum concentration in plasma is reached in 9 hours after administration of drug, in comparison with 1 hour for a form of not prolonged release. The elimination half-life of drug makes 9,1 hours.
Researches showed that consecutive pharmacokinetic curves receive at administration of drug after food.
In comparison with healthy volunteers of middle age at elderly patients pharmacokinetic parameters do not increase. In comparison with persons with normal function of kidneys average values of the maximum concentration and the area under a curve at patients with a renal failure are moderately increased, without change of an elimination half-life. This change of a pharmacokinetic profile of drug is not considered the possessing clinical value therefore it also does not demand correction of a dose.
Linkng of an alfuzozin of a hydrochloride with proteins of plasma makes about 90%. Alfuzozin is exposed to extensive metabolism in a liver, only 11% of drug in not changed look are found in urine. The majority of metabolites (which have no activity) is removed with a stake (75-90%). The pharmacokinetic profile of an alfuzozin does not change at chronic heart failure.

Indications to use:

Treatment of functional symptoms of a benign hyperplasia of a prostate.
As supportive application when using a catheter at the acute ischuria connected with a benign hyperplasia of a prostate.

Route of administration and doses:

Patients have to swallow a tablet entirely. It is forbidden to crush, crush, chew, grind a tablet in powder.
Doses
Treatment of functional symptoms of a benign hyperplasia of a prostate
The recommended dose makes: 1 tablet (10 mg) daily, after food.
Use as supportive application when using a catheter at the acute ischuria connected with a benign hyperplasia of a prostate
The recommended dose - 1 tablet (10 mg) a day, after food, since first day of catheterization.
Drug is used within 3 - 4 days, that is by 2-3 days during stay of a catheter in an urethra and 1 day after its removal.

Features of use:

• At some persons, in particular, at the patients receiving hypotensive drugs within several hours after reception of an alfuzozin (as well as after reception of any other alfa1-adrenoblockers) orthostatic hypotension with clinical symptomatology (dizziness, sharp weakness, cold sweat) or without it can develop. Orthostatic hypotension usually happens passing and is observed, as a rule, at the beginning of administration of drug and usually does not demand treatment cancellation. At emergence of these phenomena of the patient has to be before their total disappearance in horizontal position. Before an initiation of treatment of the patient it has to be warned about possibility of such phenomena.
• It is necessary to be careful at purpose of an alfuzozin to patients with orthostatic hypotonia with clinical symptomatology, to patients with indications of the anamnesis on the expressed hypotensive reaction in response to reception of other blockers of alfa1-adrenoceptors: more careful control of arterial pressure is necessary, including, upon transition from horizontal position in vertical, especially in an initiation of treatment.
• Patients with coronary insufficiency at reception of an alfuzozin need to continue anti-anginal therapy. When resuming or weighting stenocardia treatment alfuzoziny should be stopped.
• It is necessary to be careful at purpose of an alfuzozin to patsitseta with the inborn or acquired lengthening of an interval of QT or receiving medicines capable to extend QT interval.
• During ophthalmologic operations for a cataract at some patients accepting at this time or accepting earlier some alfa1-adrenoblockers development of an intraoperative syndrome of a sluggish iris (option of a syndrome of a narrow pupil) was observed. Though the risk of development of such complication at a prema of the drug Dalfaz® WEDNESDAY is represented very low, before carrying out operation for a cataract the surgeon-ophthalmologist has to be informed that the patient accepts alfa1-adrenoblockers or accepted them earlier as development of an intraoperative syndrome of a sluggish iris can increase quantity of complications at this operational vmeshatelst. Ophthalmologists have to be ready to possible change of a technique of an operative measure. • Patients should be warned that it is forbidden to crush, crush, chew, grind a tablet in powder. Such actions can lead to excessive release and absorption of drug owing to what perhaps bystry development of side effects that is especially dangerous at patients with the cerebrovascular frustration proceeding with the corresponding symptoms and also at those patients at whom cerebrovascular frustration proceed asymptomatically as at such patients at a sharp lowering of arterial pressure strengthening of ischemia of a brain is possible.

Influence on ability to manage vehicles and to be engaged in other potentially dangerous types of activity.
There are no data on influence of drug on control of vehicles.
It is necessary to take into account a possibility of development вертиго, dizziness and an adynamy, especially in an initiation of treatment that can affect ability to manage vehicles and to be engaged in other potentially dangerous types of activity, in particular to work with mechanisms.

Side effects:

The undesirable effects provided below are given in a soovetstviye with the following gradation of frequency of their emergence:
Very often: (> 10%);
Often: (> 1% - <10%);
Infrequently: (> 0,1% - <1%);
Seldom: (0,01% - 0,1%);
Very seldom: (<0,01%) (including separate cases).
Unknown frequency: according to the available data it is not possible to establish the frequency of emergence of side effect.

Disturbances from heart Infrequently: tachycardia.
Very seldom: stenocardia at patients with earlier existing coronary insufficiency (see the section "With Care", "Special Instructions"). Unknown frequency: fibrillation of auricles. Disturbances from an organ of sight Infrequently: vision disorders.
Unknown frequency: an intraoperative syndrome of a sluggish iris (see the section "Special Instructions").
The general frustration and disturbances in an injection site it is frequent: adynamy.
Infrequently: hypostases, stethalgias.
Disturbances from digestive tract
Often: nausea, abdominal pains. Infrequently: diarrhea.
Disturbances from a liver and biliary tract
Unknown frequency: hepatocellular jaundice, a cholestasia and connected with
them liver diseases.
Disturbances from a nervous system
Often: feeling faintness/dizziness, headache.
Infrequently: syncope, вертиго.
Disturbances from generative organs and a mammary gland Unknown frequency: priapism.
Disturbances from respiratory system, bodies of a thorax and
mediastinums
Infrequently: rhinitis.
Disturbances from skin and hypodermic fabrics Infrequently: rash, itch.
Very seldom: small tortoiseshell, Quincke's disease. Disturbances from vessels
Infrequently: orthostatic hypotension, hyperemia of integuments.

Interaction with other medicines:

Unrecommended combinations
With blockers of alfa1-receptors (Prazozinum, urapidit, minoksidit): strengthening of hypotensive effect, risk of heavy postural hypotension.

Combinations which should be taken into account
With hypotensive drugs: strengthening of hypotensive effect and risk of postural hypotension (additive action).
With SUR3A4 system inhibitors (кетоконазол, итраконазол, ритонавир): increase in concentration of an alfuzozin in blood.

Contraindications:

Hypersensitivity to an alfuzozin and/or other components of drug.
Orthostatic hypotension. Heavy abnormal liver functions.
Heavy renal failure (clearance of creatinine <30 ml/min.). Intestinal impassability (in connection with the content in drug of castor oil).

With care
• At the patients receiving hypotensive drugs (development of the orthostatic hypotonia which is followed by symptoms, such as dizziness, weakness, cold sweat or proceeding asymptomatically is possible).
• At patients of advanced age (75 years are more senior).
• At patients with indications of the anamnesis on the expressed hypotonic reaction to other alfagadrenoblokator.
• At patients with orthostatic hypotonia with clinical manifestations.
• At patients with coronary heart disease, stenocardia (a possibility of increase and weighting of attacks of stenocardia).
• Patients with the inborn or acquired lengthening of an interval have QT or at the patients accepting the medicines extending QT interval.

Overdose:

Arterial hypotension, reflex tachycardia. Treatment
In case of overdose of the patient is subject to hospitalization. At overdose of the patient has to is in situation "lying" and it needs continuous monitoring of arterial pressure. At a lowering of arterial pressure introduction of vasoconstrictors and plasma substitutes is recommended (for increase in volume of the circulating blood). After recovery of arterial pressure (elimination of hypotonia) it is necessary to continue control of arterial pressure still approximately within a day.
Alfuzozin is badly brought by means of a hemodialysis because of high extent of linkng with proteins of plasma.

Storage conditions:

To store at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. After a period of validity drug cannot be used.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister PVC Is scarlet/. 1 or 3 blisters together with the application instruction in a cardboard pack.