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Alfuzosin

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Alfuzosin

Alfuzosin, sold under the brand name Uroxatral among others, is a medication of the α1 blocker class. It is used to treat benign prostatic hyperplasia (BPH).

As an antagonist of the α1-adrenergic receptor, it works by relaxing the muscles in the prostate and bladder neck, making urination easier.

The most common side effects are dizziness (due to postural hypotension), upper respiratory tract infection, headache, fatigue, and abdominal disturbances. Side effects include stomach pain, heartburn, and congested nose. Adverse effects of alfuzosin are similar to that of tamsulosin, but with 70% lower rate of retrograde ejaculation.

The drug is indicated for the treatment of symptoms associated with benign prostatic hyperplasia. It has no effect on prostate size.

Administration is contraindicated in patients with severe hepatic impairment or arterial hypotension (low blood pressure), as well as in those undergoing treatment with other alpha blockers.

As an antagonist, alfuzosin selectively binds to postsynaptic Α1-adrenoceptors, leading to relaxation of the smooth muscle in the prostate and urethra. This increases uroflowmetry and facilitates micturition. The bioavailability is 64%, and the plasma half-life is 4 to 6 hours. The maximum plasma concentration is reached after approximately 90 minutes.

Alfuzosin contains a stereocenter, so is chiral, with two enantiomeric forms, (R)- and (S)-alfuzosin. The drug is used as a racemate, (RS)-alfuzosin, a 1:1 mixture of the (R)- and (S)- forms.

It is provided as the hydrochloride salt.

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