Alьfuzozin

When ATH:
G04CA01

Pharmacological action.

Alpha-blocker, acting mainly on the postsynaptic α₁-adrenoreceptory. Блокируя a₁-adrenoreceptory, arranged in a triangle and bladder sphincter, urethra, alfuzosin eliminates spasms of smooth muscle fibers, which reduces the resistance of outflow of urine. It reduces the tone of smooth muscles of arteries and veins. Decreases round and systemic blood pressure.

Pharmacokinetics

After oral administration, alfuzosin is absorbed from the gastrointestinal tract. C_max plasma levels achieved after 3 h and is 10.3 ng / ml. The difference of maximum and minimum plasma concentrations are insignificant. Food intake has no effect on absorption.

Binding to plasma proteins is approximately 90%. It is metabolized in the liver. T_1/2 – 8 no. 15-30% inactive metabolites excreted in the urine, 75-91% – with feces. 11% alfuzosin excreted in the urine as unchanged.

Patients older 75 years have higher plasma concentrations and bioavailability of alfuzosin (perhaps, by reducing hepatic metabolism). In patients with severe renal impairment is noted an increase in clearance of alfuzosin (perhaps, due to the smaller binding to plasma proteins).

Testimony

Treatment of the functional symptoms of benign prostatic hyperplasia in the absence of the possibility of surgery, and in cases of progressive growth, especially in elderly patients.

Dosage regimen

Inside – by 2.5 mg 3 times / day. For patients older 65 years – starting dose is 2.5 mg 2 times / day (in the morning and in the evening); further dose can be increased (but not more 10 mg / day).

Side effect

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

CNS: dizziness, headache; rarely – drowsiness.

Cardio-vascular system: rarely – tachycardia, orthostatic hypotension.

Allergic reactions: rarely – skin rash, itch.

Other: malaise; rarely – swelling, chest pain.

Contraindications

Notes a history of orthostatic hypotension, the simultaneous use of other alpha-blockers, Hypersensitivity to alfuzosin.

Cautions

To use caution in patients with coronary artery disease, stenokardiey. If you experience any worsening of angina, alfuzosin should be discontinued.

To use caution in patients over 75 years and in patients with severe renal impairment.

Drug Interactions

At simultaneous application with antihypertensive agents alfuzosin (especially calcium channel blockers) perhaps marked reduction of blood pressure, until the development of collapse.

With simultaneous use of alfuzosin with means for general anesthesia likely to develop blood pressure instability during anesthesia.

Incompatible with other alpha₁-adrenoblokatorami.