Name: | alfuzosin |
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PubChem Compound ID: | 2092 |
Molecular formula: | C19H27N5O4 |
Molecular weight: | 389.449 g/mol |
Synonyms: |
Alfuzosin; Prestwick1_000322; KBioGR_001616; Spectrum2_000505; N-(3-((4-Amino-6,7-dimethoxy-2-quinazolinyl)methylamino)propyl)tetrahydro-2-furancarboxamide; HSDB 7290; KBio3_001866; 2-Furancarboxamide, N-(3-((4-amino-6,7-dimethoxy-2-quinazolinyl)methylamino)propyl)tetrahydro-; Spectrum4_001208; Spectrum3_001063.
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Name: | alfuzosin |
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Name (isomeric): | DB00346 |
Drug Type: | small molecule |
Synonyms: |
Alfusosine
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Brand: | Xatral, Uroxatral |
Category: | Adrenergic alpha-Antagonists, Antihypertensive Agents |
CAS number: | 81403-80-7 |
Indication: | For the reduction of urinary obstruction and relief of associated manifestations (eg. sensation of incomplete bladder emptying or straining, urgency, interrupted or weak stream) in patients with symptomatic beningn prostatic hyperplasia. |
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Pharmacology: |
Alfuzosin is a quinazoline-derivative alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. Accordingly, alfuzosin is a selective inhibitor of the alpha(1) subtype of alpha adrenergic receptors. In the human prostate, alfuzosin antagonizes phenylephrine (alpha(1) agonist)-induced contractions, in vitro,...
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Mechanism of Action: |
Alfuzosin is a non-subtype specific alpha(1)-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...
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Absorption: | Absorption is 50% lower under fasting conditions |
Protein binding: | 82%-90% |
Biotransformation: | Hepatic. Alfuzosin undergoes extensive metabolism by the liver, with only 11% of the administered dose excreted unchanged in the urine. Alfuzosin is metabolized by three metabolic pathways: oxidation, O-demethylations, and N-dealkylation. The metabolites are not pharmacologically active. CYP3A4 is the principal hepatic enzyme isoform involved in its metabolism. |
Route of elimination: | Following oral administration of 14C-labeled alfuzosin solution, the recovery of radioactivity after 7 days (expressed as a percentage of the administered dose) was 69% in feces and 24% in urine. |
Half Life: | 10 hours |
Toxicity: | Side effects are dizziness (due to postural hypotension), upper respiratory tract infection, headache, and fatigue. |
Affected organisms: | Humans and other mammals |
Food interaction: |
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Drug interaction: |
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