Alfuzosin HCl - CAS 81403-68-1
Catalog number: 81403-68-1
Category: Inhibitor
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Molecular Formula:
C19H28ClN5O4
Molecular Weight:
425.91
COA:
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Targets:
Adrenergic Receptor
Description:
Alfuzosin HCl is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Purity:
>98%
MSDS:
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InChIKey:
YTNKWDJILNVLGX-UHFFFAOYSA-N
InChI:
InChI=1S/C19H27N5O4.ClH/c1-24(8-5-7-21-18(25)14-6-4-9-28-14)19-22-13-11-16(27-3)15(26-2)10-12(13)17(20)23-19;/h10-11,14H,4-9H2,1-3H3,(H,21,25)(H2,20,22,23);1H
Canonical SMILES:
CN(CCCNC(=O)C1CCCO1)C2=NC3=CC(=C(C=C3C(=N2)N)OC)OC.Cl
1.Kinetic Spectrophotometric Methods for the Determination of Alfuzosin Hydrochloride in Bulk and Pharmaceutical Formulations1
Salma A. AlTamimi, Fatma A. Aly, and Adibah M. Almutairi. Journal of Analytical Chemistry, 2013, Vol. 68, No. 4, pp. 313–320
The aim of the present work was to develop simple and sensitive kinetic spectrophotometric methods for the determination of alfuzosin HCl in bulk and in its pharmaceutical preparations using alkaline potassium permanganate as an oxidizing agent. The methods involve determination of alfuzosin HCl by kinetic studies of its oxidation at room temperature for a fixed time of 15 min. The absorbance of the colored manganate ions was measured at 610 nm. Alternatively, the decrease in the absorbance of permanganate upon addition of the studied drug was also measured at 525 nm. The methods were successfully applied to the determination of this drug in its dosage forms.
2.Alfuzosin: a clinically uroselective a1-blocker
Klaus Hofner, Udo Jonas. World J Urol (2002) 19: 405–412
Recently, a once-daily (o.d.) formulation of alfuzosin has been developed to improve the treatment compliance and optimise the pharmacokinetic coverage over a 24-h period. To achieve these goals, an innovative extended-release formulation, based on the Geomatrix technology(Geomatrix is a registered trademark of Jagotec AG, a member of SkyePharma Group of Companies), was used. It consists of a white hydrophilic active matrix core containing alfuzosin and two yellow inert layers, one swellable and one erodible, whose functions are to control the hydration and swelling rate of the core, leading to a controlled release of alfuzosin over the dosing interval (Fig. 3). As aqueous fluids progressively penetrate the matrix core, alfuzosin is released through a process of diffusion. Simultaneously, the swellable layer swells at a predetermined rate, increasing the surface area and the volume of the tablet to permit a slow and constant release of alfuzosin in the upper part of the digestive tract. Finally, the erodible layer dissolves with time in the lower part of the digestive tract, which allows a constant dissolution rate of alfuzosin to be maintained as the concentration decreases in the active matrix core.
3.The efficacy of Alfuzosin treatment in patients with prostatism
M. Murad Basar, Ali Atan, Osmanzergin & Mslm Yldz. International Urology and Nephrology 33: 493–497, 2001
The tone of the smooth muscle of the prostate, bladder neck and prostatic urethra is regulated by sympathetic innervation via alpha-1 adrenoceptors. Alpha-1 adrenoceptor blockers decrease the tone of the smooth muscle in the prostatic stroma, prostatic capsule, bladder neck and prostatic urethra, resulting in improving irritative and obstructive symptoms of BPH and increasing urine flow rate. Caine et al. first reported the therapeutic application of the alpha blockage for the treatment of BPH. Although Kirby et al. claimed that symptomatic improvement is generally evident in 60 to 80% of patients receiving alpha adrenocpetor blocker treatment and improvement in symptoms and urodynamic parameters are observed within 2 to 4 weeks after the treatment, Jardin et al. reported that clinical improvement with alfuzosin treatment was apparent after 6 weeks whereas peak flow rate increased and postvoiding residual urine volume decreased by 6 months. Buzelin et al. found that improvement in symptoms was significant after 1 month of the treatment and continued to improve further between weeks 4 and 12 of alfuzosin treatment. In the present study, symptomatic improvement initiated in the 2nd week of the treatment, reaching its maximum level in the 6th week whereas improvement in urodynamic parameters was obtained later than symptomatic improvement.
4.Effects of alfuzosin with methylprednisolone for spontaneous expulsion and pain control of lower ureteral stone
Eu Chang Hwang • In Sang Hwang • Ho Song Yu • Sun-Ouck Kim. Urol Res (2012) 40:605–609
Compared to tamsulosin, alfuzosin exhibits no pharmacological uroselectivity for any of the a1 subtypes (a1A, a1B, and a1D), however, alfuzosin has the lack of adverse effect and blood pressure changes, it has been claimed to be uroselective drug. Thus, it is expected to have the same effect in promoting the spontaneous stone passage. However, this is unclear, given the paucity of studies to date. Also, studies concerning the influence of corticosteroids on stone passage have mainly involved combinations with tamsulosin. Therefore, we investigated the effect of combination therapy with alfuzosin and methylprednisolone on spontaneous passage of lower ureteral stones.
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CAS 81403-68-1 Alfuzosin HCl

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