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Chemical Compound Review

alfuzosin     N-[3-[(4-amino-6,7-dimethoxy- quinazolin-2...

Synonyms: ALFLUZOSIN, Alfusosine, Alfuzosina, Alfuzosine, Alfuzosinum, ...
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Disease relevance of alfuzosin


Psychiatry related information on alfuzosin

  • Alfuzosin has been shown to improve patients' perception of quality of life, allowing patients to increase their physical activities and improve their ability to handle day-to-day activities [6].
  • Patients who agreed to be randomized were subsequently randomized to alfuzosin 5 mg twice daily or placebo and patients who agreed to participate but not be randomized were entered into a control or standard (except alpha-blockers) therapy group [7].
  • CONCLUSIONS: This study confirms the effectiveness of alfuzosin and the need to include HRQL measurement in the decision-making process when assessing patients with lower urinary tract symptoms [8].

High impact information on alfuzosin


Chemical compound and disease context of alfuzosin


Biological context of alfuzosin

  • The once-daily formulation of alfuzosin 10mg caused fewer vasodilatory adverse events than immediate-release alfuzosin 2.5mg three times daily and caused only slight decreases in systolic and diastolic blood pressure which were not clinically significant and did not differ significantly from those with placebo [19].
  • Of the 161 men 101 were reevaluated with a second clinical evaluation and urodynamics 1 to 5 years (mean 2) after watchful waiting in 20, medical treatment (alfuzosin 20 and finasteride 16) in 36 and surgery (transurethral incision of the prostate 13 and prostatectomy 32) in 45 [20].
  • The effect of renal impairment on the safety and pharmacokinetics of a once-daily formulation of alfuzosin, 10 mg, was evaluated [21].
  • This study confirms the long-term safety profile of alfuzosin in general practice and highlights the need to measure HRQL in the context of clinical uroselectivity [22].
  • The objective of this study was to evaluate the effect of 10mg alfuzosin on blood pressure (BP) and heart rate (HR) in young healthy volunteers [23].

Anatomical context of alfuzosin

  • Alfuzosin, a selective alpha 1-adrenoceptor antagonist in the lower urinary tract [24].
  • Evaluation of tamsulosin and alfuzosin activity in the rat vas deferens: relevance to ejaculation delays [25].
  • In contrast, alfuzosin, an alpha 1-adrenoceptor antagonist with poor brain penetration, did not significantly affect these levels even at the high dose of 0.4 mg/kg, i.v. When perfused into the hippocampus through the dialysis probe, prazosin (1-10 microM) induced a more limited (20-30%) and delayed decrease in 5-HT outflow [26].
  • This is the case for alfuzosin, which has been shown to enhance erectile function in experimental models, probably by reducing the sympathetic tone and thus relaxing corpus cavernosum smooth muscle cells [27].
  • Bladder-neck opening test in spinal cord injury patients using a new i.v. alpha-blocking agent, alfuzosin [28].

Associations of alfuzosin with other chemical compounds

  • With tamsulosin, the incidence of adverse events commonly associated with alpha 1 adrenoceptor antagonism is similar to that with placebo (except for ejaculation disorders) and alfuzosin [29].
  • Direct high-performance liquid chromatographic determination of the enantiomers of alfuzosin in plasma on a second-generation alpha 1-acid glycoprotein chiral stationary phase [30].
  • RESULTS: Alfuzosin showed a concentration-dependent relaxing effect on rabbit CC pre-contracted by 10 micro mol/L phenylephrine, with a mean (sd) pIC50 of 7.64 (0.06) [31].
  • OBJECTIVE To investigate the effects of acute intravenous (i.v.) delivery of tamsulosin and alfuzosin on the contractions of bulbospongiosus muscles (BS) induced by central delivery of a serotonin agonist, 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), in anaesthetized rats, as an experimental model of the expulsion phase of ejaculation [32].
  • In contrast to alfuzosin, sildenafil was equipotent in relaxing the rabbit CC against each contractile agent, with pIC50 values of 7.25 (0.09) and 7.23 (0.22) with 10 micro mol/L phenylephrine and 60 mmol/L KCl, respectively [31].
  • Improvement of IPSS was significant with the three treatments but greatest with the combination (-24.1%) compared with alfuzosin (-15.6%) and sildenafil (-11.8%) [corrected] alone (p<0.03) [33].

Gene context of alfuzosin

  • Effects of short-term treatment with the alpha 1-blocker alfuzosin on urodynamic pressure/flow parameters in patients with benign prostatic hyperplasia [34].
  • Supine systolic blood (SBP) pressure was not reduced by alfuzosin although significant increases occurred in supine heart rate (HR) after 2.5 and 5 mg [35].
  • PATIENTS AND METHODS: Videocystometry was used to measure the detrusor LPP and several other variables before and 3 weeks after the oral administration of alfuzosin (2.5-7.5 mg/day) in 17 children (mean age 6.3 years) with an upper motor neurone lesion [36].
  • Results from the Medical Therapy of Prostatic Symptoms study and the Alfuzosin Long-Term Efficacy and Safety Study also suggest that using the PVR in clinical practice needs to be reconsidered as a predictor of BPH progression [37].
  • OBJECTIVES: To examine the hemodynamic interactions of the phosphodiesterase type 5 (PDE-5) inhibitor tadalafil with the uroselective alpha1-blocker alfuzosin (10 mg daily), commonly prescribed for benign prostatic hyperplasia-related lower urinary tract symptoms [38].

Analytical, diagnostic and therapeutic context of alfuzosin

  • In addition, alfuzosin offers an alternative to prostatectomy (the current 'gold standard') in patients who require surgery but are unfit for this treatment, and in patients requiring symptomatic relief while awaiting surgery [14].
  • Data from short- (3 months) and long-term (up to 12 months) clinical trials show that the prolonged-release formulation of alfuzosin controls the symptoms associated with BPH as effectively as immediate-release alfuzosin 2.5mg three times daily and clinical improvement is maintained for up to 1 year [19].
  • MATERIALS AND METHODS: Using a randomized, 3-way crossover design, the effects of 5 days of treatment with 0.8 mg tamsulosin daily, 10 mg alfuzosin daily and placebo on ejaculation in healthy adult men were compared [39].
  • MATERIALS AND METHODS: A total of 360 patients presenting with a first episode of spontaneous AUR related to BPH underwent emergency catheterization and were then randomly and blindly assigned to receive 10 mg alfuzosin once daily or placebo at a ratio of 2:1 for 3 days [4].
  • METHODS: This is a 9-month open-label extension of a 3-month double-blind, placebo-controlled evaluation of alfuzosin 10 mg o.d. and standard alfuzosin 2.5 mg, three times daily (t.i.d.), administered without dose titration in both cases [40].


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  16. A meta-analysis on the efficacy and tolerability of alpha1-adrenoceptor antagonists in patients with lower urinary tract symptoms suggestive of benign prostatic obstruction. Djavan, B., Marberger, M. Eur. Urol. (1999) [Pubmed]
  17. In vivo studies on the effects of alpha1-adrenoceptor antagonists on pupil diameter and urethral tone in rabbits. Michel, M.C., Okutsu, H., Noguchi, Y., Suzuki, M., Ohtake, A., Yuyama, H., Yanai-Inamura, H., Ukai, M., Watanabe, M., Someya, A., Sasamata, M. Naunyn Schmiedebergs Arch. Pharmacol. (2006) [Pubmed]
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  19. Alfuzosin: a review of the therapeutic use of the prolonged-release formulation given once daily in the management of benign prostatic hyperplasia. McKeage, K., Plosker, G.L. Drugs (2002) [Pubmed]
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  21. Pharmacokinetics and safety of a single oral dose of once-daily alfuzosin, 10 mg, in male subjects with mild to severe renal impairment. Marbury, T.C., Blum, R.A., Rauch, C., Pinquier, J.L. Journal of clinical pharmacology. (2002) [Pubmed]
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  25. Evaluation of tamsulosin and alfuzosin activity in the rat vas deferens: relevance to ejaculation delays. Tambaro, S., Ruiu, S., Dessi, C., Mongeau, R., Marchese, G., Pani, L. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
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