WordNet

a complex consisting of an organic base in association with hydrogen chloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/02/22 12:35:35」(JST)

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Oxprenolol (Trasacor, Trasicor, Coretal, Laracor, Slow-Pren, Captol, Corbeton, Slow-Trasicor, Tevacor, Trasitensin, Trasidex) is a non-selective beta blocker with some intrinsic sympathomimetic activity. It is used for the treatment of angina pectoris, abnormal heart rhythms and high blood pressure.

Oxprenolol is a lipophilic beta blocker which passes the blood–brain barrier more easily than water-soluble beta blockers. As such, it is associated with a higher incidence of CNS-related side effects than hydrophilic ligands such as atenolol, sotalol and nadolol.^[1]

Oxprenolol is a potent beta blocker and should not be administered to asthmatics under any circumstances due to their low beta levels as a result of depletion due to other asthma medication, and because it can cause irreversible, often fatal, airway failure and inflammation.^[2]

Stereochemistry

Oxprenolol is a chiral compound, the beta blocker is used as a racemate, e. g. a 1:1 mixture of (R)-(+)-oxprenolol and (S)-(–)-oxprenolol. Analytical methods (HPLC) for the separation and quantification of (R)-(+)-oxprenolol and (S)-(–)-oxprenolol in urine and in pharmaceutical formulations have been described in the literature.^[3]

(R)-(+)-Oxprenolol (top) and (S)-(–)-oxprenolol

References

^ McDevitt DG (1987). "Comparison of pharmacokinetic properties of beta-adrenoceptor blocking drugs". Eur. Heart J. 8. Suppl M: 9–14. doi:10.1093/eurheartj/8.suppl_M.9. PMID 2897304.
^ I P Williams and F J Millard (1980). "Severe asthma after inadvertent ingestion of oxprenolol". Thorax 35 (2): 160. doi:10.1136/thx.35.2.160. PMC 471246. PMID 7376124.
^ Abounassif, Mohammed A.; Hefnawy, Mohammed M.; Mostafa, Gamal A. E. (2011). "Separation and quantitation of oxprenolol in urine and pharmaceutical formulations by HPLC using a Chiralpak IC and UV detection". Monatshefte für Chemie - Chemical Monthly 143 (3): 365. doi:10.1007/s00706-011-0605-4.

UpToDate Contents

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1. β遮断剤中毒 beta blocker poisoning

English Journal

Interactions of beta-blockers with model lipid membranes: molecular view of the interaction of acebutolol, oxprenolol, and propranolol with phosphatidylcholine vesicles by time-dependent fluorescence shift and molecular dynamics simulations.

Först G1, Cwiklik L2, Jurkiewicz P3, Schubert R4, Hof M5.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V.Eur J Pharm Biopharm.2014 Aug;87(3):559-69. doi: 10.1016/j.ejpb.2014.03.013. Epub 2014 Mar 28.
Since pharmacokinetic and pharmacodynamic activities of drugs are often related to their interactions with biomembranes, it is of high interest to establish an approach for the characterization of these interactions at the molecular level. For the present study, beta-blockers (oxprenolol, propranolo
PMID 24681296

New trends in the treatment of nicotine addiction.

Sliwińska-Mossoń M, Zieleń I, Milnerowicz H.
Acta poloniae pharmaceutica.Acta Pol Pharm.2014 Jul-Aug;71(4):525-30.
The aim of this study was to discuss the therapeutic substances used to treat nicotine addiction, not registered in Poland. This paper presents the results of the latest clinical trials and the possibility of their use in the treatment of nicotine addiction. The first two discussed drugs clonidine a
PMID 25272878

A comparative ex vivo drug permeation study of beta-blockers through porcine buccal mucosa.

Amores S1, Lauroba J2, Calpena A1, Colom H1, Gimeno A3, Domenech J1.
International journal of pharmaceutics.Int J Pharm.2014 Jul 1;468(1-2):50-4. doi: 10.1016/j.ijpharm.2014.03.050. Epub 2014 Apr 13.
Apparent permeability coefficients (kp) of a series of beta-blockers: acebutolol, atenolol, labetalol, metoprolol, oxprenolol and propranolol, through porcine buccal mucosa were determined. The aim of the study was to determine the permeation parameters (apparent permeability coefficient, kp; flux,
PMID 24727142

Japanese Journal

Studies on Production of Higher Functional Pharmaceutical Preparations by Using Various Additives. III. Application of Hollow Glass Beads for Intragastric Floating Granules

Chemical & pharmaceutical bulletin 46(7), 1173-1176, 1998-07-15
NAID 110003617000

Studies on Production of Higher Functional Pharmaceutical Preparations by Using Various Additives. III. Application of Hollow Glass Beads for Intragastric Floating Granules.

Chemical and Pharmaceutical Bulletin 46(7), 1173-1176, 1998
NAID 130003773843

Application of the Solid Dispersion Method to the Controlled Release of Medicine. VIII. Medicine Release and Viscosity of the Hydrogel of a Water-Soluble Polymer in a Three-Component Solid Dispersion System

Chemical & pharmaceutical bulletin 43(9), 1574-1579, 1995-09-15
NAID 110003631705

Related Pictures

★リンクテーブル★

リンク元	「オクスプレノロール」
関連記事	「oxprenolol」「hydrochloride」

「オクスプレノロール」

Oxprenolol
Systematic (IUPAC) name
	(RS)-1-[2-(Allyloxy)phenoxy]-3-(isopropylamino)propan-2-ol
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Pregnancy; category	AU: C; ;
Legal status	℞ (Prescription only);
Routes of; administration	oral
Pharmacokinetic data
Bioavailability	20-70%
Metabolism	Hepatic
Biological half-life	1-2hours
Excretion	Renal; Lactic (In lactiferous females)
Identifiers
CAS Number	6452-71-7
ATC code	C07AA02
PubChem	CID 4631
IUPHAR/BPS	7255
DrugBank	DB01580
ChemSpider	4470
UNII	519MXN9YZR
KEGG	D08318
ChEMBL	CHEMBL546
Chemical data
Formula	C15H23NO3
Molar mass	265.348
Chirality	1 : 1 mixture (racemate)
	SMILES O(c1ccccc1OC\C=C)CC(O)CNC(C)C ;
	InChI InChI=1S/C15H23NO3/c1-4-9-18-14-7-5-6-8-15(14)19-11-13(17)10-16-12(2)3/h4-8,12-13,16-17H,1,9-11H2,2-3H3 ; Key:CEMAWMOMDPGJMB-UHFFFAOYSA-N ;
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