2-furancarboxamide, N-[3-[(5-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro-
Alfuzosin
CAS: 81403-80-7
Molecular Formula: C19H27N5O4
2-furancarboxamide, N-[3-[(5-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro- - Names and Identifiers
2-furancarboxamide, N-[3-[(5-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro- - Physico-chemical Properties
| Molecular Formula | C19H27N5O4 |
| Molar Mass | 389.45 |
| Density | 1.272±0.06 g/cm3(Predicted) |
| Melting Point | 178-180 °C |
| Solubility | DMSO (Sparingly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 14.80±0.20(Predicted) |
| Storage Condition | -20°C Freezer |
| Refractive Index | 1.62 |
2-furancarboxamide, N-[3-[(5-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.568 ml | 12.839 ml | 25.677 ml |
| 5 mM | 0.514 ml | 2.568 ml | 5.135 ml |
| 10 mM | 0.257 ml | 1.284 ml | 2.568 ml |
| 5 mM | 0.051 ml | 0.257 ml | 0.514 ml |
Last Update：2024-01-02 23:10:35
2-furancarboxamide, N-[3-[(5-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro- - Reference Information
| drugs for benign prostatic hyperplasia and hypertension | benign prostatic hyperplasia (BPH) is a common disease in middle-aged and elderly men. Prostatic Hyperplasia hinders urine discharge, can cause irritation and obstructive urethral symptoms, the most common symptoms are: nocturia, daytime urgency, urinary frequency, urinary flow thinning and so on. Many men over the age of 70 will have moderate or severe urinary symptoms due to BPH. Although BPH itself is rarely life-threatening, it can lead to irreversible damage to the bladder or kidneys if left untreated. Acute urinary retention is the most serious complication of BPH. Its clinical manifestation is characterized by sudden inability to urinate and pain. alfuzosin is a selective alpha 1 receptor blocker, belonging to the quinazoline derivatives, which can reduce the resistance of urine flow by relaxing the tension of smooth muscles around the prostate, bladder neck and prostatic urethra, thus, the symptoms of urethral tension, resistance and pressure increase, bladder outlet obstruction and the like related to prostatic hypertrophy can be alleviated. It has a rapid onset of action, little effect on the cardiovascular system, and no annoying adverse effects on sexual function of some other BPH treatment drugs. The oral absorption of alfuzosin was good, and the peak blood concentration reached 0.5-3 hours after oral administration, and the bioavailability was 64%. In the therapeutic dose range, the Pharmacokinetics is linear. About 87% of the absorbed drug binds to plasma proteins. This product is mainly eliminated by the liver metabolism, inactive metabolites 75%-91% by the bile from the feces, 15%-30% by the urine. About 11% of them were excreted through urine as the same form. The elimination half-life was 4-8 hours. Its pharmacokinetic properties are not affected by meals. In the elderly over 75 years old, the absorption of the product is faster, the peak concentration of the blood drug is higher, the AUC is higher than that of the younger, and the volume of distribution can be reduced, The elimination half-life was unchanged. There was no significant change in the pharmacokinetics of alfuzosin in patients with renal insufficiency. In patients with hepatic insufficiency, the peak plasma concentration, elimination half-life and AUC value increased, and the free fraction also increased. In addition, alfuzosin has similar effects to both prazosin and papaverine, which not only block α1 receptor, but also directly dilate vascular smooth muscle, so it has good antihypertensive effect. For high blood pressure, 1 oral 7.5~10mg, divided into 3 times. Note that alfuzosin hydrochloride should not be combined with calcium antagonists, alpha blockers. |
| biological activity | Alfuzosin is a selective, competitive α1-adrenergic receptor (α1-adrenoptor) antagonist. |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-10 22:29:15
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