Dalfaz® SR (Dalfaz® SR)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceAlfuzosinAlfuzosin
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    • Dosage form: & nbspsustained-release tablets
    Composition:

    One tablet contains:

    The first layer (external inactive)

    Excipients: hypromellose - 79.75 mg; castor oil hydrogenated - 13.50 mg; ethylcellulose - 20-5.00 mg; ferric iron oxide yellow (E172) 0.25 mg; silicon dioxide colloidal water - 0.50 mg; magnesium stearate - 1.00 mg.

    The second layer (internal active)

    Active substance: alfuzosin hydrochloride 10.00 mg.

    Excipients: mannitol - 10.00 mg; hypromellose-10,00 mg; cellulose microcrystalline - 65.00 mg; povidone - 3.20 mg; silicon dioxide colloidal water - 1.25 mg; magnesium stearate - 1.00 mg.

    The third layer (external inactive)

    Excipients: hypromellose - 114.01 mg; castor oil hydrogenated - 27.90 mg; povidone - 4.72 mg; ferric iron oxide yellow (E172) - 0.15 mg; silicon dioxide colloidal water - 1.05 mg; magnesium stearate - 2.17 mg.

    Description:Round, biconvex three-layer tablets: one white layer between two yellow layers with differentintensity of color. Inclusions are allowed.
    Pharmacotherapeutic group:Alpha-blocker
    ATX: & nbsp

    G.04.C   Drugs for the treatment of benign prostatic hyperplasia

    Pharmacodynamics:

    Alfuzosin is a quinazoline derivative that is active in oral use. He is a selective antagonist of postsynaptic alfaa1adrenoreceptors located in the prostate gland, the triangle of the bladder and the urethra.

    Clinical manifestations of benign prostatic hypertrophy are expressed in the infravesical obstruction of the urinary tract, due to both anatomical (static) and functional (dynamic) factors.

    The functional component of obstruction is due to the excitation of the alphaa1-adrenoreceptors leading to a reduction in the smooth muscles of the prostate gland, its membrane, the triangle of the bladder and the prostatic part of the urethra, which leads to an increase in resistance to urine outflow from the bladder and, apparently, to secondary instability of the bladder.

    Due to a direct effect on the smooth muscle tissue of the prostate gland associated with the blockade of alphaa1β-adrenoreceptors, alfuzosin reduces infravesical obstruction, pressure in the urethra and resistance to urine outflow during urination. Thereby alfuzosin improves the flow of urine and facilitates the emptying of the bladder. These beneficial effects on urodynamics lead to a reduction in urinary tract irritation symptoms and symptoms due to impairment of urinary outflow in patients with benign prostatic hyperplasia. In patients with a maximum rate of outflow of urine (Qmax) ≤15 ml / s alfuzosin, already starting with the first dose, significantly increases Qmax (an average of 30%). In addition, in patients with benign prostatic hypertrophy alfuzosin significantly reduces the pressure in the detrusor of the bladder and increases the amount of urine causing a urge to urinate, and also significantly reduces the amount of residual urine. These effects lead to a decrease in obstructive and irritative symptoms of benign prostatic hypertrophy.The drug has no adverse effect on sexual function.

    In connection with the selectivity of the action of alfuzosin, its effect on alphaa1-adrenoceptors of blood vessels and, accordingly, on arterial pressure (BP), in case of its use in therapeutic doses, is practically absent.

    Pharmacokinetics:

    The average relative bioavailability is 104.4%, compared with the use of alfuzosin 7.5 mg in immediate-release dosage form (2.5 mg 3 times daily) in healthy middle-aged volunteers. The maximum concentration of alfuzosin in plasma is achieved 9 hours after taking the drug, compared to 1 hour for an immediate-release form.

    The half-life of alfuzosin is 9.1 hours.

    Studies have shown that the bioavailability of alfuzosin increases with the administration of the drug after a meal (see section "Method of administration and dose").

    Binding to plasma proteins is about 90%.

    Alfuzosin undergoes significant metabolism in the liver, mainly with the help of isoenzyme CYP3A4.

    In urine, only 11% of unchanged alfuzosin is found.

    Metabolites of alfuzosin do not have pharmacological activity.Most metabolites are excreted through the intestine (75-90%).

    Pharmacokinetics in specific patient groups

    Compared with healthy middle-aged volunteers, the pharmacokinetic parameters of alfuzosin do not increase in elderly patients (over 75 years). In comparison with persons with normal renal function, the mean values ​​of the maximum concentration in the blood plasma (CmOh) and the area under the curve "concentration-time" (AUC) Alfuzosin in patients with renal insufficiency moderately increased, without changing the half-life (T1/2). This change in the pharmacokinetic profile of alfuzosin is not clinically significant, so dose adjustment is not required in patients with mild to moderate renal impairment (creatinine clearance> 30 mL / min).

    The pharmacokinetic profile of alfuzosin does not change with chronic heart failure.

    Indications:

    Treatment of functional symptoms of benign prostatic hyperplasia glands.

    As an aid in the use of a catheter for acute urinary retention associated with benign prostatic hyperplasia.

    Contraindications:

    - Hypersensitivity to alfuzosin and / or excipients of the drug.

    - Orthostatic hypotension.

    - Liver failure.

    - Severe renal insufficiency (creatinine clearance <30 mL / min).

    - Intestinal obstruction (in connection with the content of castor oil in the preparation).

    - Simultaneous reception of other alphasa1adrenoblockers.

    - Children under 18 years.

    Carefully:

    - In patients taking antihypertensive drugs or nitrates (possibly the development of orthostatic hypotension, both asymptomatic and symptomatic, accompanied by dizziness, weakness, cold sweat).

    - In elderly patients (over 75 years).

    - In patients with severe hypotensive reaction to other alphaa1-adrenoconjunctors in the anamnesis.

    - In patients with orthostatic hypotension with clinical manifestations.

    - In patients with coronary heart disease, angina (there may be an increase and augmentation of angina attacks).

    - In patients with congenital or acquired lengthening of the interval QT or in patients taking medications that increase the duration of the interval QT.

    - In patients with cerebral ischemia.

    - With inhibitors of isoenzyme CYP3A4 (ketoconazole, itraconazole, ritonavir) (possibly increasing the concentration of alfuzosin in blood plasma).

    Pregnancy and lactation:The drug Dalfaz® SR is not intended for use in women.
    Dosing and Administration:

    The drug is intended for oral administration. Patients should swallow the whole tablet. It is forbidden to grind, crush, chew, grind the tablet into powder. These actions can lead to improper release of alfuzosin from tablet and its rapid absorption, which increases the risk of unwanted reactions (see section "Special instructions").

    Treatment of functional symptoms of benign prostatic hyperplasia

    The recommended dose is: 1 tablet (10 mg) daily, after a meal.

    Use as an aid in the use of a catheter for acute urinary retention associated with benign prostatic hyperplasia

    The recommended dose is 1 tablet (10 mg) per day, after meals, starting from the first day of catheterization.

    The drug is used for 3-4 days, that is, 2-3 days while the catheter is in the urethra and 1 day after its removal.

    Side effects:

    The undesirable reactions listed below (HP) are given in accordance with the following gradations of the frequency of their occurrence: very often: (≥ 10%); often (≥ 1% - <10%); infrequently (≥ 0,1% - <1%); rarely (0.01% - 0.1%); very rarely (<0.01%) (including individual cases); unknown frequency (according to available data, establish the frequency of occurrence HP does not seem possible).

    Violations of the blood and lymphatic system

    Unknown frequency: thrombocytopenia.

    Heart Disease

    Infrequently: tachycardia, palpitation.

    Rarely: possible increased frequency or weighting of angina attacks (see sections "With caution", "Special instructions").

    Unknown frequency: atrial fibrillation.

    Disturbances on the part of the organ of sight

    Infrequently: visual impairment.

    Unknown frequency: intraoperative syndrome of a flaccid iris (see section "Special instructions").

    General disorders and disorders at the site of administration

    Often: asthenia, malaise.

    Infrequently: swelling, chest pain.

    Disorders from the gastrointestinal tract

    Often: nausea, pain in the abdomen.

    Infrequently: diarrhea.

    Unknown frequency: vomiting.

    Disturbances from the liver and bile ducts

    Unknown frequency: hepatocellular jaundice, cholestasis and associated liver disease.

    Disturbances from the nervous system

    Often: feeling faint / dizzy, headache.

    Infrequently: syncope, vertigo, drowsiness.

    Unknown frequency: ischemic impairment of cerebral circulation in patients with already existing cerebrovascular pathology.

    Violations of the genitals and mammary gland

    Unknown frequency: priapism.

    Disturbances from the respiratory system, chest and mediastinal organs

    Infrequently: rhinitis.

    Disturbances from the skin and subcutaneous tissues

    Infrequently: rash, itching.

    Rarely: urticaria, angioedema.

    Vascular disorders

    Infrequently: a decrease in blood pressure, including orthostatic hypotension, flushing of the skin.

    Overdose:

    Symptoms

    Excessive decrease in blood pressure, reflex tachycardia.

    Treatment

    In case of an overdose, the patient is hospitalized. In case of an overdose, the patient should be in the "lying" position and he needs constant monitoring of blood pressure. When blood pressure is lowered, the introduction of vasoconstrictors and plasma substitutes (to increase the volume of circulating blood) is recommended.After restoration of blood pressure (elimination of hypotension), it is necessary to continue blood pressure control for approximately 24 hours.

    Alfuzosin is poorly excreted by hemodialysis because of the high degree of binding to plasma proteins.

    Interaction:

    Contraindicated combinations

    - With alpha blockersa1-receptors (prazozin, urapidil): increased hypotensive effect, the risk of severe orthostatic hypotension (see section "Contraindications").

    Interactions that should be taken into account

    - With antihypertensive drugs: increased hypotensive effect and the risk of developing orthostatic hypotension (additive effect) (see section "Special instructions").

    - With nitrates: increased risk of developing reflex tachycardia and lowering blood pressure.

    - With funds for inhalation and non-inhaling general anesthesia: possible instability of BP during general anesthesia.

    - With inhibitors of isoenzyme CYP3A4 (ketoconazole, itraconazole, ritonavir): it is possible to increase the concentration of alfuzosin in the blood plasma. When a combination of alfuzosin at a dose of 10 mg per day with a course application of ketoconazole at a dose of 200 mg per day for 7 days Cmax and AUC of alfuzosin increased 2.1 times and 2.46 times, respectively, and when combined with a course application of ketoconazole at a dose of 400 mg per day for 8 days Cmax and AUC of alfuzosin increase 2.3 times and 3.0 times, respectively (see the section "With caution").

    Special instructions:

    - Within hours after taking alfuzosin (as well as after taking any other alfaa1-adrenoconvertors) in some individuals, especially in patients taking antihypertensive drugs, may develop orthostatic hypotension with clinical symptoms (dizziness, severe weakness, cold perspiration) or without it. At occurrence of these phenomena the patient should be in horizontal position before their full disappearance.

    Orthostatic hypotension is usually transient and is observed, as a rule, at the beginning of the drug and usually does not require the withdrawal of treatment.

    In post-marketing use of the drug in patients with risk factors for reducing blood pressure (such as heart disease or concomitant therapy with antihypertensive drugs), a pronounced decrease in blood pressure was reported. The risk of excessive blood pressure lowering and associated adverse reactions may be higher in elderly patients.

    Before starting treatment, the patient should be warned about the possibility of occurrence of the reactions described above.

    - Caution should be exercised when using alfuzosin in patients with orthostatic hypotension with clinical symptoms or in patients taking antihypertensive drugs or nitrates: more careful monitoring of blood pressure is necessary, including when moving from horizontal to vertical position, especially at the beginning of treatment.

    - Caution should be exercised when using alfuzosin in patients with severe hypotensive reaction in response to the use of other alpha blockersa1-adrenoceptors in the anamnesis.

    - Patients with coronary insufficiency with alfuzosin should continue antianginal therapy. With the resumption or weighting of angina, treatment with alfuzosin should be discontinued.

    - Caution should be exercised when using alfuzosin in patients with congenital or acquired lengthening of the interval QT or in patients taking medications that can lengthen the interval QT.

    - During ophthalmic operations for cataracts in some patients who have taken or previously taken some alphaa1-adrenoconvertors, development of intraoperative syndrome of flaccid iris was observed (variant of narrow pupil syndrome). Although the risk of developing such a complication when taking Dalfaz® SR is very low, before the operation for cataracts, the ophthalmic surgeon should be informed that the patient is taking the alphaa1- adrenoblockers or took them earlier, since the development of intraoperative syndrome of a flaccid iris can increase the number of complications in this surgical intervention. Ophthalmologists should be prepared for a possible change in the methods of surgical intervention.

    - Patients should be warned that it is forbidden to grind, crush, chew, grind the tablet into powder. Such actions can lead to excessive release and absorption of the drug, which can lead to the rapid development of side effects, which is especially dangerous in patients with cerebrovascular disorders that occur with the corresponding symptoms, as well as in those patients whose cerebrovascular disorders are asymptomatic, because such patients with a sharp decrease in blood pressure may increase cerebral ischemia.

    - There are reports of cases of development in the background of therapy with alpha g adrenoblokatorami priapizma (prolonged painful erection of the penis, not related to sexual activity). If priapism therapy has not been carried out immediately, it can lead to damage to the tissues of the penis and an irreversible loss of potency. Patients should Inform about the severity of this condition (see the "Side effect" section) and the need to seek immediate medical help if the erection persists for more than 4 hours.

    Effect on the ability to drive transp. cf. and fur:

    Care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions, as the drug may cause dizziness and other side effects that may affect these abilities.

    Form release / dosage:

    Tablets of prolonged action, 10 mg.

    Packaging:

    For 10 or 30 tablets per blister PVC / Al.

    For 1 or 3 blisters for 10 tablets or 1 blister for 30 tablets together with instructions for use in a cardboard pack.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    After the expiration date, the drug can not be used.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013178 / 01
    Date of registration:17.04.2007 / 16.06.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:Sanofi Winthrop IndustrySanofi Winthrop Industry France
    Manufacturer: & nbsp
    Representation: & nbspSanofi Russia, JSCSanofi Russia, JSCRussia
    Information update date: & nbsp21.04.2017
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