Terazosin

TERAZOSIN HCL · terazosine · Urodie · HYTRIN · erazosin · arbonyl)- · Terazosin · CID 663211

식별자 및 물리적 특성

CAS No.	63590-64-7
분자식	C19H25N5O4
평균 분자량	387.4 g/mol
단동위원소 질량	387.19065428 g/mol
SMILES	COc1cc2nc(N3CCN(C(=O)C4CCCO4)CC3)nc(N)c2cc1OC
InChIKey	VCKUSRYTPJJLNI-UHFFFAOYSA-N
PubChem CID	5401
ChEMBL	CHEMBL611
ChEBI	CHEBI:9445
EC No.	613-265-8
DTXSID	DTXSID3023639

화학 및 물리적 성질

XLogP	1.4
극성 표면적	103
수소 결합 공여자 수	1
수소 결합 수용자 수	8
회전 가능 결합 수	4
무거운 원자 수	28
형식 전하	0
복잡도	544
의약품	Pharmaceuticals -> Antihypertensives
LogP(분배 계수)	11.14
용해도	1.50e+00 g/LH2O: 25 mg/mL
Human Drugs	Breast FeedingLactationMilk, HumanAdrenergic alpha-AntagonistsAntihypertensive AgentsPharmaceuticals
녹는점	271-274273 °C281-283°C
Physical Description	Solid
Collision Cross Section	189.79 Å² [M+Na]+ [CCS Type: TWMethod: calibrated with polyalanine and drug standards]
끓는 점	664.5±65.0 °C(Predicted)
밀도	1.332±0.06 g/cm3(Predicted)
저장 조건	-20°C Freezer
물리적 상태	가루
pKa(산도 계수)	pKa (0.1N NaOH): 7.1(at 25℃)
색상	흰색에서 황백색까지
용해도	30.6mg/L(22.5℃)
BCS Class	1/3
InChIKey	VCKUSRYTPJJLNI-UHFFFAOYSA-N

화학적 성질

White to Off-White Crystalline Powder

안전 및 규제

GHS 분류	This chemical does not meet GHS hazard criteria for 2.3% (1 of 44) of reports.WarningH302 (97.7%): Harmful if swallowed [Warning Acute toxicity, oral]P264, P270, P301+P317, P330, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 44 reports by companies from 3 notifications to the ECHA C&L Inventory.
규제 정보	Status: Active Update: 25-07-2018 https://echa.europa.eu/registration-dossier/-/registered-dossier/25502
Hazard Classes and Categories	Acute Tox. 4 (97.7%)
Treatment	Should overdosage of Terazosin lead to hypotension, support of the cardiovascular system is of first importance. Restoration of blood pressure and normalization of heart rate may be accomplished by keeping the patient in the supine position. If this measure is inadequate, shock should first be treated with volume expanders. If necessary, vasopressors should then be used and renal function should be monitored and supported as needed. Laboratory data indicate that Terazosin is highly protein boundtherefore, dialysis may not be of benefit. (L1712)
건강 영향	Hypotension, palpitations, postural hypotension, syncope, peripheral edema, weight gain, dyspnea, nasal congestion/rhinitis, impotence.
Hepatotoxicity	Terazosin 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. Instances of serum enzyme elevations, but no instances of clinically apparent acute liver injury with jaundice due to terazosin, have been published. Furthermore, product labels do not include discussion of hepatic toxicity. Cholestatic hepatitis and jaundice have been reported with other alpha-adrenergic blockers. Thus, acute symptomatic liver injury due to terazosin must be exceedingly rare if it occurs at all.
유해 작용	Terazosin is generally well-tolerated. Many adverse effects of terazosin are explainable due to its blockade of alpha-1 adrenergic receptors.
노출 경로	Oral. Essentially completely absorbed in man (90% bioavailability).
독성 요약	Overdose of terazosin may lead to hypotension, and standard life-support protocols should be in place for instances of hemodynamic instability. There are no specific antidotes for terazosin toxicity. Vasopressors may be used to support physiologic blood pressure parameters in the event of terazosin overdose. Terazosin is long-acting, with an elimination half-life of approximately 12 hours, and is highly protein-bound. Elimination is via renal excretion (40%) and excretion of feces (60%).Terazosin selectively and competitively inhibits vascular postsynaptic alpha(1)-adrenergic receptors, resulting in peripheral vasodilation and a reduction of vascular resistance and blood pressure. Unlike the nonselective alph-adrenergic blockers phenoxybenzamine and phentolamine, terazosin does not block presynaptic alpha(2)-receptors and, hence, does not cause reflex activation of norepinephrine release to produce reflex tachycardia.
Signs and Symptoms	Asthenia, postural hypotension, dizziness, somnolence, nasal congestion/rhinitis.
Carcinogen Classification	No indication of carcinogenicity to humans (not listed by IARC).
Drug Induced Liver Injury	Drug-Induced Liver Injury Severity and Toxicity (DILIst)terazosinDILI NegativeOralDOI:10.1016/j.drudis.2019.09.022
Effects During Pregnancy and Lactation	◉ Summary of Use during Lactation
Toxicity Data	LD50: 259.3mg/kg (parental-intravenous, Mouse) (A308)
수질 위해 등급(WGK)	3
RTECS 번호	TK8044925
위험 문구(R)	22-36/37/38
위험 표시	Xn,Xi
안전 문구(S)	26-36

용도

Terazosin is used for the same indications as is prazosin; however, it has the advantage of being able to be used once a day.