81403-80-7 Usage
Description
Alfuzosin is a quinazoline α1-blocker that selectively targets the α1A-receptor subtype in the prostate gland, making it a first-line drug for treating benign prostatic hypertrophy (BPH) with fewer cardiovascular side effects compared to other α1-blockers.
Uses
Used in Pharmaceutical Industry:
Alfuzosin is used as a therapeutic agent for the symptomatic treatment of benign prostatic hypertrophy (BPH) and acute adenoma. It works by lowering urethral contractions induced by alpha1 stimulation, providing relief from BPH symptoms.
Alfuzosin is also being developed as an antihypertensive agent, with its efficacy in this indication being comparable to prazosin without causing significant changes in heart rate.
Therapeutic drugs for benign prostatic hyperplasia and hypertension
Benign prostatic hyperplasia (BPH) is a common disease in medium-elderly men. Prostatic hyperplasias obstruct urine excretion, which can cause irritant and obstructive urethral symptoms. The most common symptoms are nocturia, increased urgency during the day, frequent micturition, and urinary rheology. Many men over 70 years old have moderate or severe urethral symptoms due to BPH. Although BPH itself rarely endangers life, it can cause irreversible damage to the bladder or kidney if not treated. Acute urinary retention is the most serious complication of BPH. Its clinical features are sudden inability to urinate and pain. If not treated in time, it can endanger life. Alfuzosin is a selective alpha 1 receptor blocker, which belongs to the quinazoline derivative. By relaxing the tension of the urethra smooth muscle around the prostate, bladder neck and prostate, it can reduce the resistance of the urine flow, so that the symptoms such as urethral tension, resistance and pressure increase, bladder outlet obstruction and other symptoms related to prostatic hypertrophy can be alleviated. It has a quick effect and has little effect on the cardiovascular system, and there are no other adverse effects on sexual function like other annoying BPH drugs. The absorption of alfuzosin is good. The concentration of blood drug reaches peak 0.5-3 hours after taking, and the bioavailability is 64%. In the range of treatment dose, the pharmacokinetics is linear. About 87% of the drugs absorbed are combined with plasma protein. This product is mainly eliminated by liver metabolism.75%-91% of the inactive metabolite is excreted by the feces through the bile, and 15%-30% is excreted in the urine. Another 11% is excreted in the original form in the urine. The half-life of the elimination is 4-8 hours. Its pharmacokinetic characteristics are not affected by the meal.
In the elderly over 75 years of age, this product is absorbed faster and the concentration of the blood drug peak is higher. In addition, AUC is also higher than the young, but the volume of distribution can be reduced and the half-life will be eliminated. In renal insufficiency, it pharmacokinetic characteristics have no obvious change. In the patients with liver dysfunction, the concentration of blood drug peak, the elimination half life and the AUC value are all increased, and the free fraction is also increased. In addition, alfuzosin is similar to proposing and palavering in function. It not only blocks the alpha 1 receptor, but also smooths diastolic blood vessel muscle, so it has good antihypertensive effect. For high blood pressure, 7.5 to 10mg should be taken for 1 day 3 times daily.
It should be noticed that alfuzosin hydrochloride cannot be used with calcium antagonist and alpha blocker.
Originator
Synthelabo (France)
Check Digit Verification of cas no
The CAS Registry Mumber 81403-80-7 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 8,1,4,0 and 3 respectively; the second part has 2 digits, 8 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 81403-80:
(7*8)+(6*1)+(5*4)+(4*0)+(3*3)+(2*8)+(1*0)=107
107 % 10 = 7
So 81403-80-7 is a valid CAS Registry Number.
InChI:InChI=1/C19H27N5O4/c1-24(8-5-7-21-18(25)14-6-4-9-28-14)19-22-11-12-13(23-19)10-15(26-2)17(27-3)16(12)20/h10-11,14H,4-9,20H2,1-3H3,(H,21,25)
81403-80-7Relevant articles and documents
Chemoselective calcium-catalysed direct amidation of carboxylic esters
Nguyen, D. Thao,Lenstra, Danny C.,Mecinovi?, Jasmin
, p. 77658 - 77661 (2015/09/28)
Unactivated carboxylic esters and primary amines undergo calcium-catalysed direct amide bond formation in excellent yields under homogeneous conditions in toluene. This green and mild reaction proceeds chemoselectively with esters, whereas related carboxylic acids and amides remain unreactive.
METHOD OF PREPARING ANHYDROUS ALFUSOZIN HYDROCHLORIDE
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Page/Page column 14, (2010/04/03)
There is described a method of preparing anhydrous alfuzosin hydrochloride by means of a condensation reaction between N1-methyl-N2-(tetrahydrodrofuroyl-2)-propylenediamine and 4-amino-2-chloro-6,7-dimethoxyquinazoline. The obtained crude product is subsequently purified by further stages that include steps of preparing novel intermediates. The described alfuzosin synthesis and purification process allow to obtain this active ingredient with a high yield and purity, and therefore suitable to be employed as an active ingredient in medicaments.
PROCESS FOR PREPARING ALFUZOSIN
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Page/Page column 9-10, (2008/12/07)
Processes for preparing alfuzosin and pharmaceutically acceptable salts, solvates, hydrates thereof are disclosed. The present invention also discloses processes for preparation of anhydrous alfuzosin hydrochloride having substantially free from other pseudopolymorphic crystalline forms particularly dihydrate form of alfuzosin hydrochloride.
