Alphuzosin (Tablets) Instructions for Use

ATC Code

G04CA01 (Alphuzosin)

Active Substance

Alfuzosin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Drug used for urination disorders associated with benign prostatic hyperplasia. Alpha₁-adrenergic blocker

Pharmacotherapeutic Group

Alpha- and beta-adrenergic blocker

Pharmacological Action

An alpha-adrenergic blocker acting primarily on postsynaptic α₁-adrenergic receptors.

By blocking the α₁-adrenergic receptors located in the trigone and sphincter of the urinary bladder, and in the urethra, Alfuzosin relieves spasm of smooth muscle fibers, which leads to a reduction in the resistance to urine outflow.

It reduces the tone of the smooth muscles of arteries and veins. It decreases total peripheral vascular resistance (TPVR) and systemic blood pressure.

Pharmacokinetics

After oral administration, Alfuzosin is absorbed from the gastrointestinal tract.

The maximum plasma concentration (C_max) is reached after 3 hours and is 10.3 ng/ml. The differences between maximum and minimum plasma concentrations are insignificant. Food intake does not affect absorption.

Plasma protein binding is about 90%. It is metabolized in the liver. The elimination half-life (T_1/2) is 8 hours.

15-30% of inactive metabolites are excreted in the urine, 75-91% – in the feces. 11% of alfuzosin is excreted unchanged in the urine.

In patients over 75 years of age, higher plasma concentrations and bioavailability of alfuzosin are observed (possibly due to reduced liver metabolism).

In patients with severe renal impairment, an increase in the clearance of alfuzosin is noted (possibly due to lower plasma protein binding).

Indications

Treatment of functional manifestations of benign prostatic hyperplasia when surgical intervention is not possible, as well as in cases of progressive growth, especially in elderly patients.

ICD codes

Dosage Regimen

Administer tablets orally.

The standard adult dosage is 2.5 mg three times daily.

For patients over 65 years of age, initiate therapy at a reduced dose of 2.5 mg twice daily, taken in the morning and evening.

Subsequently, the dose may be carefully titrated upward based on individual therapeutic response and tolerability.

Do not exceed the maximum total daily dose of 10 mg under any circumstances.

Swallow the tablet whole with a sufficient amount of water.

Take during or immediately after a meal to improve gastrointestinal tolerability.

Adhere strictly to the prescribed dosing schedule to maintain stable plasma concentrations.

Monitor for signs of orthostatic hypotension, especially during the initial dose titration phase and in elderly patients.

If a dose is missed, take it as soon as remembered unless it is almost time for the next scheduled dose.

Do not double the dose to make up for a missed one.

Discontinuation of therapy should be supervised by a physician.

Adverse Reactions

From the digestive system epigastric pain, nausea, diarrhea; rarely – dry mouth.

From the central nervous system dizziness, headache; rarely – drowsiness.

From the cardiovascular system rarely – tachycardia, orthostatic hypotension.

Allergic reactions rarely – skin rash, itching.

Other malaise; rarely – edema, chest pain.

Contraindications

History of orthostatic hypotension, concurrent use of other alpha-adrenergic blockers, hypersensitivity to alfuzosin.

Use in Pregnancy and Lactation

The drug is not intended for use in women.

Use in Renal Impairment

Use with caution in patients with severe renal impairment.

Pediatric Use

The drug is not intended for use in children.

Geriatric Use

For patients over 65 years of age – the initial dose is 2.5 mg twice a day (morning and evening); subsequently, the dose may be increased (but not more than 10 mg per day).

Use with caution in patients over 75 years of age.

Special Precautions

Use with caution in patients with coronary artery disease (CAD), angina pectoris. If worsening of angina is observed, Alfuzosin should be discontinued.

Use with caution in patients over 75 years of age and in patients with severe renal impairment.

Drug Interactions

With the simultaneous use of alfuzosin with antihypertensive agents (especially calcium channel blockers), a pronounced decrease in blood pressure is possible, up to the development of collapse.

With the simultaneous use of alfuzosin with agents for general anesthesia, instability of blood pressure during anesthesia is likely.

Incompatible with other alpha₁-adrenergic blockers.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.