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QuickView for Alfuzosin (compound)

Name: alfuzosin
PubChem Compound ID: 2092
Molecular formula: C19H27N5O4
Molecular weight: 389.449 g/mol
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
Name (isomeric): DB00346
Drug Type: small molecule
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.
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:
Take after a meal (always the same meal), product bioavailability is reduced when taken on an empty stomach.
Drug interaction:
TamsulosinConcomitant use of alpha1-adrenergic antagonists, Tamsulosin and Alfuzosin, may result in additive antihypertensive effects. Combination therapy is not recommended.
RitonavirRitonavir increases the effect/toxicity of alfuzosin
ItraconazoleThe antifungal increases the effect of alfuzosin
ConivaptanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Alfuzosin. Concomitant use of alfuzosin with a strong CYP3A4 inhibitor is a listed contraindication according to alfuzosin prescribing information.
TerazosinAdditive antihypertensive effects may occur. Increase risk of orthostatic hypotension and syncope. Concomitant therapy should be avoided.
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