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Alfuzosin

It is an antagonist of Alpha 1 adrenoreceptor, it relaxes the muscles of bladder and prostate. More

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Description

It is an antagonist of Alpha 1 adrenoreceptor, it relaxes the muscles of bladder and prostate.

Generic Name

Alfuzosin

Chemical names

Alfuzosin, Alfuzosina, Alfuzosine, Alfuzosinum

Brand names

Afdura, Alfanage, Alfoo, Alfupro, Alfusin, Alfusin-D, Dutalfa, Efzu, Flotral, Flotral-D, Fual, Fuzocin, Profuzo, Solitral, Urizosin-ER, Xelflo, Zofu-ER.

IUPAC name

N-{3-[(4-amino-6,7-dimethoxyquinazolin-2 yl)(methyl)amino]propyl}oxolane-2-carboxamide

Pharmacokinetics

  • Absorption: Oral
  • Distribution: 82%-90% protein binding
  • Metabolism: Hepatic
  • Excretion: Faeces via bile and 11% through urine

Actions

Alfuzosin is an adrenergic blocking agent that exhibits selectivity for alpha (1)-adrenergic receptors in the lower urinary tract. Inhibition of these adrenoreceptors leads to the relaxation of smooth muscle in the bladder neck and prostate, resulting in the improvement in urine flow and a reduction in symptoms in benign prostate hyperplasia. Alfuzosin also inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation.

Dosage/Dosage form

The recommended dose is 10 mg/day PO

Therapeutic uses

Used to treat signs and symptoms of benign enlargement of the prostate (BPH)

Adverse effects/Side effects

Drowsiness, GI disturbances, postural hypotension, syncope, depression, headache, edema, dry mouth, rhinitis, blurred vision, erectile disorders, palpitation, tachycardia, flushes, hypersensitivity reactions, dizziness, chest pain, lack of energy.

Interaction

  • Reduced serum levels when used with CYP3A4 inducers e.g. nafcillin, aminoglutethimide, carbamazepine, phenobarbital, nevirapine, phenytoin and rifamycins.
  • Concurrent use with potent CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, or ritonavir) is contraindicated.
  • CYP3A4 inhibitors e.g. clarithromycin, azole antifungals, doxycycline, diclofenac, erythromycin, imatinib, nefazodone, nicardipine, propofol, telithromycin, protease inhibitors, quinidine, and verapamil may increase the levels of alfuzosin.

Contraindications

Contraindicated in patients with the history of liver or kidney problems, and in patients with hypersensitivity reactions.

Storage

  • Store between 15-30°C.
  • Protect from heat, moisture and light.

Information

Molecular weight

389.4488

Molecular formula

C19H27N5O4

CAS number

81403-80-7

Precautions

  • May affect ability to drive or operate machinery.
  • Caution should be exercised in patients with irregular heartbeat, chest pain, prostate cancer, who are taking other medications.