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Doxazosin
UK 33274 · UK 33,274 · DOXAZOSIN · Doxazosin base · DOXAZOSINMESYTL · DOXAZOSIN(CARDULAR) · Doxazosin USP/EP/BP · Doxazosin (UK 33274)
Identifikatoren & physikalische Daten
| CAS No. | 74191-85-8 |
|---|---|
| Summenformel | C23H25N5O5 |
| Durchschnittliche Molmasse | 451,5 g/mol |
| Monoisotopische Masse | 451,1855689 g/mol |
| SMILES | COc1cc2nc(N3CCN(C(=O)C4COc5ccccc5O4)CC3)nc(N)c2cc1OC |
| InChIKey | RUZYUOTYCVRMRZ-UHFFFAOYSA-N |
| PubChem CID | 3157 |
| ChEMBL | CHEMBL707 |
| ChEBI | CHEBI:4708 |
| EC No. | 616-059-6 |
| DTXSID | DTXSID7022964 |
Chemische & physikalische Eigenschaften
| XLogP | 2,5 |
|---|---|
| Polarare Oberfläche (TPSA) | 112 |
| H-Brücken-Donoren | 1 |
| H-Brücken-Akzeptoren | 9 |
| Frei drehbare Bindungen | 4 |
| Schwere Atome | 33 |
| Formalladung | 0 |
| Komplexität | 678 |
| Arzneimittel | Pharmaceuticals -> Antihypertensives |
| LogP (Verteilungskoeffizient) | 2.13.38 |
| Löslichkeit | 0.8%7.90e-01 g/LSoluble in DMSO |
| Human Drugs | Breast FeedingLactationMilk, HumanAdrenergic alpha-AntagonistsAntihypertensive Agents |
| Schmelzpunkt | 275-277289 - 290 °C289-290°C |
| Physical Description | Solid |
| Dissociation Constants | 6.52 |
| Collision Cross Section | 202.9 Ų [M+H]+ [CCS Type: TWMethod: Major Mix IMS/Tof Calibration Kit (Waters)]196.92 Ų [M+Na]+ [CCS Type: TWMethod: calibrated with polyalanine and drug standards] |
| Siedepunkt | 718.0±70.0 °C(Predicted) |
| Dichte | 1.371±0.06 g/cm3(Predicted) |
| Lagerbedingungen | Store at -20°C |
| Aggregatzustand | Powder |
| pKa (Säurekonstante) | 6.52±0.50(Predicted) |
| Farbe | White to off-white |
| CAS Datenbank | 74191-85-8(CAS DataBase Reference) |
Sicherheit & Vorschriften
| GHS-Einstufung | DangerH302 (20%): Harmful if swallowed [Warning Acute toxicity, oral]P260, P264, P270, P273, P280, P301+P317, P301+P330+P331, P302+P361+P354, P304+P340, P305+P354+P338, P316, P319, P321, P330, P363, P391, P405, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 5 reports by companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies. |
|---|---|
| Regulatorische Informationen | Status: Active Update: 01-07-2020 https://echa.europa.eu/registration-dossier/-/registered-dossier/31210 |
| Hazard Classes and Categories | Skin Corr. 1B (80%) |
| Hepatotoxicity | Doxazosin has been associated with a low rate of serum aminotransferase elevations that in controlled trials was no higher than with placebo therapy. These elevations were transient and did not require dose modification. No instances of clinically apparent acute liver injury due to doxazosin have been published in the literature, but reports of cholestatic hepatitis have been received by the sponsor. Among the alpha adrenergic receptor antagonists, the most frequently implicated agent in causing liver injury has been alfuzosin with only single, and not well documented cases linked to other alpha blockers. Thus, acute symptomatic liver injury due to doxazosin is quite rare, and severe hepatotoxicity must be exceeding rare, if it occurs at all. |
| Unerwünschte Wirkungen | Dose-related Adverse Effects |
| Toxizitätsübersicht | Reports with overdosage and toxicity with the alpha-1 antagonists, including doxazosin, remain very limited in the literature. There is a report of one case of acute doxazosin overdose in 2005. The study found that the patient presented to the emergency department (ED) with drowsiness, decreased blood pressure, and reflex tachycardia but did not have orthostatic hypotension or any other abnormalities. This patient was able to fully awaken with supportive therapy in 8 hours and was discharged 48 hours after admission to the ED. Although there are limited works of literature for the toxicity of doxazosin, it appears to have low acute toxicity. |
| Drug Induced Liver Injury | Drug-Induced Liver Injury Severity and Toxicity (DILIst)doxazosinDILI NegativeOralDOI:10.1016/j.drudis.2019.09.022 |
| Effects During Pregnancy and Lactation | ◉ Summary of Use during Lactation |
| Alarmwort | Achtung |
| Gefahrenhinweise | Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code H302 |
Anwendungen & Verwendung
Beschreibung
Doxazosin mesylate is a selective alpha, blocker indicated for the treatment of hypertension, reportedly of special benefit as a first-line agent in the most hypertonic patient population. Another advantage of doxazosin is its favorable effect on blood lipids; it significantly increases the HDL/total cholesterol ratio and decreases the total cholesterol as well as triglycerides levels.
Verwenden
ACIPHEX therapeutic Erosive or Ulcerative Gastroesophageal Reflux Disease