Dalfaz SR, retard pills 10mg, 30pcs

Composition

1 tablet contains:

first layer:

hypromellose 79.75 mg,

hydrogenated castor oil 13.5 mg,

ethylcellulose 20.5 mg,

iron oxide yellow dye (E172) 0.25 mg,

colloidal water silicon dioxide 0.5 mg,

magnesium stearate 1 mg,

second layer:

alfuzosin hydrochloride 10 mg,

mannitol 10 mg,

hypromellose 10 mg,

MCC 65 mg,

povidone 3.2 mg,

colloidal water silicon dioxide 1.25 mg,

magnesium stearate 1 mg,

third layer:

Hypromellose 114.01 mg,

hydrogenated castor oil 27.9 mg,

Povidone 4.72 mg,

iron oxide yellow (E172) dye 0.15 mg,

colloidal water silicon dioxide 1.05 mg,

magnesium stearate 2.17 mg

Pharmacological action

Pharmacodynamics

Alfuzosin is an oral quinazoline derivative active as a selective antagonist of postsynaptic alpha-1 adrenergic receptors with a peripheral site of action Pharmacological tests in vitro showed the selectivity of alfuzosin action on alpha-1-adrenergic receptors located in the prostate gland, in the triangle of the bladder and in the prostatic part of the urethra. As a result of direct action on the smooth muscles of prostate tissues, alpha-1-adrenoblockers reduce the resistance to urine flow. Alfuzosin improves discharge parameters, reducing urethral tone and resistance to outflow from the bladder, and facilitates emptying the bladder. In placebo-controlled trials of alfuzosin in patients with benign prostatic hypertrophy, it was found that: :

• A significant increase in the maximum flow rate (Qmax) by an average of 30% in patients with Qmax < 15 ml / sec. This improvement was observed starting with the first dose.
• A significant decrease in resistance to the flow of urine and an increase in the volume of urine released, causing the urge to urinate.
• Significant reduction in residual urine volume.

Pharmacokinetics:

The maximum concentration in the blood plasma is reached approximately 3 hours after ingestion of the drug. The binding of alfuzosin hydrochloride to plasma proteins is about 90%.

The half-life of the drug is 8 hours.

The bioavailability of retard tablets is approximately 15% lower compared to 2.5 mg of alfuzosin. Food intake does not affect the absorption of the Active ingredient.

Alfuzosin is mainly metabolized in the liver, only 11% is excreted unchanged in the urine. Most of the metabolites (which have no activity) are excreted in the faeces (75-91%).

In individuals over 75 years of age, absorption is faster, and maximum concentrations and bioavailability are higher. The volume of distribution is reduced. The

pharmacokinetic profile of alfuzosin does not change when the drug is taken with food.

The volume of distribution and clearance of alfuzosin are increased in patients with renal insufficiency, both with and without dialysis. There is no need to modify the dosage in patients with impaired renal function and creatinine clearance > 30 ml/min. In patients with severe hepatic insufficiency, the elimination half-life is prolonged. Bioavailability, compared with healthy volunteers, is increased.

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

Indications

Treatment of functional symptoms of benign prostatic hyperplasia.

As an auxiliary agent when using a catheter for acute urinary retention associated with benign prostatic hyperplasia.

Contraindications

• hypersensitivity to alfuzosin and/or other components of the drug;
• orthostatic hypotension;
• severe liver function disorders (Child-Pugh class C);
• severe renal function disorders (Cl creatinine
• intestinal obstruction (due to the presence of castor oil in the drug);
• simultaneous use of other alpha_-1-blockers.

Side effects

From the central nervous system and the psyche: often-weakness, general discomfort, headache; infrequently-drowsiness, dizziness, brain ischemia (in patients with ischemic brain disease).

From the cardiovascular system: infrequently-tachycardia, palpitation, syncope, orthostatic hypotension; very rarely-angina pectoris in patients suffering from coronary heart disease, atrial fibrillation.

From the gastrointestinal tract: often — nausea, abdominal pain, dry mouth; infrequently-diarrhea; very rarely-damage to hepatocytes, liver diseases with cholestasis.

Skin and allergic reactions: infrequently-rash, pruritus; very rarely-urticaria, angioedema.

From the whole body: often-asthenia; infrequently-hyperemia of the skin, swelling, chest pain; very rarely-priapism.

Interaction

When used with blockers ? 1-adrenergic receptors (prazosin, urapidil, minoxidil) increase the hypotensive effect, the risk of severe postural hypotension increases (the combination is not recommended).

Concomitant use of Dalfaz SR with antihypertensive drugs increases the risk of postural hypotension due to its additive effect (the combination should be used with caution).

When used concomitantly with CYP3A4 inhibitors ( ketoconazole, itraconazole, ritonavir), an increase in the concentration of alfuzosin in blood plasma is observed (the combination should be used with caution).

How to take, course of use and dosage

Inside, after eating, swallowing whole,10 mg daily.

Application as an auxiliary agent when using a catheter for acute urinary retention associated with benign prostatic hyperplasia: the recommended dose is 1 tablet of 10 mg per day, after meals, starting from the first day of catheterization. The drug is used for 3-4 days, i. e. 2-3 days during the catheter application and 1 day after its removal.

Overdose

e recommended combinations:

• With alpha-1 receptor blockers (prazosin, urapidil and minoxidil): increased antihypertensive effect. Risk of severe postural hypotension.
• Combinations to take into account:
• With antihypertensive drugs: increased hypotensive effect and risk of postural hypotension (additive effect) (see “Special instructions”)
• With nitrates: increased hypotensive effect.
• With inhibitors of the CYP3A4 system-ketoconazole, itraconazole and ritonavir: increased concentration of alfuzosin in the blood

Special instructions

Some individuals, especially those receiving antihypertensive medications, may develop orthostatic hypotension within a few hours after taking alfuzosin (as well as after taking other alpha_-1blockers), with or without clinical symptoms (dizziness, sudden weakness, cold sweat). Orthostatic hypotension is usually transient and usually occurs at the beginning of taking the drug and usually does not require discontinuation of treatment. When these phenomena occur, the patient should be in a horizontal position until they completely disappear. Before starting treatment, the patient should be warned about the possibility of such phenomena.

Caution should be exercised when prescribing alfuzosin to patients with orthostatic hypotension with clinical symptoms, patients with a history of severe hypotensive reaction in response to the use of other alpha_-1— blockers-more careful monitoring of blood pressure is necessary, including when moving from a horizontal position to a vertical one, especially at the beginning of treatment.

Antianginal therapy should be continued in patients with CHD. Treatment with alfuzosin should be discontinued if angina persists or becomes more severe.

Influence on the ability to drive vehicles and work with mechanisms. Especially at the beginning of treatment, you should take into account the possibility of developing dizziness and asthenic state, which may affect the ability to drive vehicles and work with mechanisms.

Form of production

Long-acting tablets

Storage conditions

In a dry place, at a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Alfuzosin

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets

Purpose

For adults

Indications

Prostatic Hyperplasia