DALFAZ CP

Active material: Alьfuzozin
When ATH: G04CA01
CCF: Preparation, used in violation of urination, associated with benign prostatic hyperplasia. Alpha₁-adrenoblokator
Codes ICD-10 (testimony): N40
When CSF: 28.01.02.01
Manufacturer: SANOFI WINTHROP INDUSTRY (France)

Pharmaceutical form, composition and packaging

Sustained-release tablets round, lenticular, sandwich (one white layer between two yellow layers with different color intensity); allowed blotches.

The composition of the first layer tablet: gipromelloza, Hydrogenated castor oil, ethyl cellulose 20, dye iron oxide yellow (E172), aqueous colloidal silica, magnesium stearate.

The composition of the second layer tablets: alfuzosin hydrochloride, mannitol, gipromelloza, microcrystalline cellulose, povidone, aqueous colloidal silica, magnesium stearate.

The composition of the third layer tablets: gipromelloza, Hydrogenated castor oil, povidone, dye iron oxide yellow (E172), aqueous colloidal silica, magnesium stearate.

10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.

Pharmacological action

Alpha₁-adrenoblokator, quinazoline derivative. Selectively acts on the postsynaptic α₁-adrenoreceptory. In in vitro studies show selectivity of action on α alfuzosin₁-adrenoreceptory, located in the prostate gland, in the bottom of the bladder and prostatic urethra.

As a result, the direct impact on the smooth muscles of the prostate reduces the resistance to the flow of urine.

Alfuzosin improves voiding parameters, reducing urethral tone and resistance to outflow from the bladder, and facilitates emptying of the bladder.

In placebo-controlled trials of alfuzosin in patients with benign prostatic hyperplasia showed a significant increase in the maximum flow rate (Q_max) urine average 30% patients with Q_max ≤15 mL / s. This improvement was noted after the first dose. Also, there was a significant reduction in current urine resistance and an increase in urine output; a significant decrease in residual urine volume.

Pharmacokinetics

Absorption and distribution

Before the drug Dalfaz^® CP due to the nature of the dosage form, provides sustained release of alfuzosin hydrochloride, In healthy volunteers, the mean age of the average bioavailability of 104.4% compared with an immediate release form (upon receipt of 2.5 mg 2 times / day).

C_max achieved through 9 hours after dosing as compared with 1 h to form an immediate release. Plasma protein binding is about 90%.

Metabolism and excretion

Alfuzosin undergoes considerable metabolism in the liver, only 11% the dose is excreted in the urine as unchanged; most of the inactive metabolites (75-90%) – with feces.

T_1/2 is 9.1 no.

Pharmacokinetics in special clinical situations

In elderly patients, the pharmacokinetic parameters (C_max и AUC) do not increase.

In patients with renal impairment C_max and AUC moderately increased (that has no clinical significance and requires no changes to the dosing regimen), T_1/2 It is not changed.

The pharmacokinetic profile of the drug is not changed in patients with chronic heart failure.

Testimony

- Treatment of the functional symptoms of benign prostatic hyperplasia;

- As an aid when using a catheter in acute urinary retention, associated with benign prostatic hyperplasia.

Dosage regimen

The drug is taken orally, after meal.

At treatment of functional symptoms of benign prostatic hyperplasia The recommended dose is 1 tab. (10 mg) 1 time / day.

IN as an adjunct to the use of a catheter in acute urinary retention, associated with benign prostatic hyperplasia, the recommended dose – 1 tab. (10 mg) 1 time / day, from the first day of catheterization. The drug is used for 3-4 d, ie. 2-3 day on the background of the catheter and 1 day after its removal.

Tablets should be taken as a whole.

Side effect

From the digestive system: nausea, epigastric pain, diarrhea, dry mouth.

CNS: headache, dizziness, weakness, drowsiness, asthenic syndrome, insensibility, syncope.

Cardio-vascular system: tachycardia, orthostatic hypotension, in patients with coronary artery disease – exacerbation of angina.

Allergic reactions: rarely – skin rash, itch.

Other: swelling, dermahemia.

Contraindications

- Orthostatic hypotension;

- Severe liver;

- Severe renal insufficiency (CC < 30 ml / min);

- Bowel obstruction (in connection with the contents of the preparation of castor oil);

- Hypersensitivity to alfuzosin, and / or other ingredients.

Cautions

In some cases, especially in patients, receiving antihypertensive therapy, for several hours after ingestion (as well as other α blockers₁-adrenoreceptorov) may develop postural hypotension with or without symptoms (dizziness, fatigue, increased perspiration). In such situations the patient must lie until complete disappearance of symptoms. These reactions are usually temporary, occur early in treatment and usually does not affect the continuation of therapy. Patients should be warned of the possibility of such reactions.

Patients with coronary insufficiency should not be given Dalfaz^® CP as monotherapy. It is necessary to continue the treatment of coronary insufficiency. If angina persists or worsens during their, the drug should be discontinued.

Patients should be warned about, that the tablets should be swallowed whole. Violating the integrity of the tablets may lead to inappropriate release and absorption of the active substance and, respectively, to the adverse reactions, which can quickly develop.

Effects on ability to drive vehicles and management mechanisms

Side effects, such as dizziness, blurred vision and fatigue may occur mainly at the beginning of treatment. This should be taken into account when driving transport and work on the machines.

Overdose

Symptoms: hypotension.

Treatment: hospitalization, the patient should be supine. Is the treatment of arterial hypotension (the introduction of a vasoconstrictor, solutions and high-molecular substances; measures, to increase bcc). Dialysis is ineffective because of the high degree of binding to plasma proteins alfuzosin.

Drug Interactions

When using α blockers₁-adrenoreceptorov (prazosin, urapidil, minoksidil) there is a strengthening of the hypotensive effect, It increases the risk of severe postural hypotension (mixture, which should be taken into account).

In an application Dalfaza^® SL with antihypertensive drugs increases the risk of postural hypotension due to additive effect (combination should be taken into account).

In an application with inhibitors of CYP3A4 (ketoconazole, itraconazole, ritonavir) observed increased concentration in plasma alfuzosin (combination should be taken into account).

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.