WordNet

vasodilator that is used to treat spasms of peripheral blood vessels (as in acrocyanosis)
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）』「2015/12/02 07:47:31」(JST)

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Tolazoline is a non-selective competitive α-adrenergic receptor antagonist. It is a vasodilator that is used to treat spasms of peripheral blood vessels (as in acrocyanosis). It has also been used (in conjunction with Sodium nitroprusside) successfully as an antidote to reverse the severe peripheral vasoconstriction which can occur as a result of overdose with certain 5-HT_2A agonist drugs such as 25I-NBOMe,^{[citation needed]} DOB and Bromodragonfly (prolonged severe vasoconstriction can lead to gangrene if untreated).^[1]^[2]

It is however most commonly used in veterinary medicine, to reverse xylazine-induced sedation.^[3]^[4]

References

^ Bowen JS, Davis GB, Kearney TE, Bardin J. Diffuse vascular spasm associated with 4-bromo-2,5-dimethoxyamphetamine ingestion. Journal of the American Medical Association 1983 Mar 18;249(11):1477-9. PMID 6827726
^ Thorlacius K, Borna C, Personne M. Bromo-dragon fly--life-threatening drug. Can cause tissue necrosis as demonstrated by the first described case. (Swedish) Lakartidningen. 2008 Apr 16-22;105(16):1199-200. PMID 18522262
^ Boothe DM (2001). "Anticonvulsant drugs and analeptic agents". In Adams HR (ed.). Veterinary pharmacology and therapeutics. Ames: Iowa State University Press. pp. 378–9. ISBN 0-8138-1743-9. Retrieved September 8, 2008 through Google Book Search.
^ Hall LW, Clarke KW, Trim CM (2001). "Principles of sedation, analgesia and premedication". Veterinary anaesthesia. Philadelphia: W.B. Saunders. pp. 90–1. ISBN 0-7020-2035-4. Retrieved September 8, 2008 through Google Book Search.

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English Journal

Effects of three antagonists on selected pharmacodynamic effects of sublingually administered detomidine in the horse.

Knych HK1, Stanley SD.Author information 1K. L. Maddy Equine Analytical Chemistry Laboratory, School of Veterinary Medicine, University of California, Davis, CA, USA; Department of Veterinary Molecular Biosciences, School of Veterinary Medicine, University of California, Davis, CA, USA.AbstractOBJECTIVE: To describe the effects of alpha2 -adrenergic receptor antagonists on the pharmacodynamics of sublingual (SL) detomidine in the horse.
Veterinary anaesthesia and analgesia.Vet Anaesth Analg.2014 Jan;41(1):36-47. doi: 10.1111/vaa.12081. Epub 2013 Oct 17.
OBJECTIVE: To describe the effects of alpha2 -adrenergic receptor antagonists on the pharmacodynamics of sublingual (SL) detomidine in the horse.STUDY DESIGN: Randomized crossover design.ANIMALS: Nine healthy adult horses with an average age of 7.6 ± 6.5 years.METHODS: Four treatment groups were
PMID 24134603

Activity of the adrenergic nerve system in the airways permeability of healthy persons.

Gashi N1, Islami P2, Mustafa L3, Maloku H4, Veseli A5, Islami H6.Author information 1Department of Pediatric, Faculty of Medicine. University of Prishtina. Clinical Centre, Prishtina, Kosova.2Smartmed, St.Rexhep Krasniqi, EXDC, Prishtina, Kosova.3Liri-Med, St. Agim Ramadani, SHPK, Prishtina, Kosova.4Department of Surgery, Faculty of Medicine. University of Prishtina, Clinical Centre, Prishtina, Kosova.5Department of Pharmacy, Faculty of Medicine. University of Prishtina. Clinical Centre, Prishtina, Kosova.6Department of Clinical Pharmacology, Faculty of Medicine. University of Prishtina. Clinical Centre, Prishtina, Kosova.AbstractOBJECTIVE: In this work, role of the adrenergic nerve system (alpha1 and beta2) in adjustment of the bronchomotor tonus in healthy people was researched.
Acta informatica medica : AIM : journal of the Society for Medical Informatics of Bosnia & Herzegovina : časopis Društva za medicinsku informatiku BiH.Acta Inform Med.2013 Dec;21(4):266-9. doi: 10.5455/aim.2013.21.266-269. Epub 2013 Dec 4.
OBJECTIVE: In this work, role of the adrenergic nerve system (alpha1 and beta2) in adjustment of the bronchomotor tonus in healthy people was researched.METHODS: Parameters of the lung function are determined by Body plethysmography. Raw and ITGV were registered and SRaw was calculated as well. Aero
PMID 24554803

Vasomodulation influences on the transdermal delivery of Ibuprofen.

Carter SG1, Zhu Z, Varadi G, Veves A, Riviere JE.Author information 1BioChemics, Inc, Danvers, Massachusetts, 01923.AbstractThe purpose of the study was to evaluate the effect of adding peripheral vasodilators, tolazoline, or papaverine, to transdermal drug delivery vehicles with the goal of improving the tissue bioavailability of transdermally delivered ibuprofen. Ibuprofen (150 mg) formulations with several concentrations of two different vasodilators and/or a penetration enhancer (PE) complex were topically applied to rabbits. Plasma levels of ibuprofen were determined by a validated high-performance liquid chromatography method and evaluated at 0, 0.5, 1, 2, and 3 h. The PE complex enhanced the plasma ibuprofen level approximately sevenfold versus control, and tolazoline (0.005%) added to the PE complex increased the plasma levels of ibuprofen approximately another twofold compared with the PE. Higher concentrations of tolazoline paradoxically did not exhibit vasodilator enhancement to ibuprofen delivery. Papaverine was tested in the same manner. In this set of experiments, PE increased the plasma ibuprofen 3.7-fold versus control, and addition of papaverine (0.0005%) increased plasma ibuprofen an additional 3.3-fold compared with the PE formulation. Transdermal formulations of ibuprofen containing low concentrations of tolazoline or papaverine increased plasma ibuprofen levels in the presence of passive PE components.
Journal of pharmaceutical sciences.J Pharm Sci.2013 Nov;102(11):4072-8. doi: 10.1002/jps.23719. Epub 2013 Aug 29.
The purpose of the study was to evaluate the effect of adding peripheral vasodilators, tolazoline, or papaverine, to transdermal drug delivery vehicles with the goal of improving the tissue bioavailability of transdermally delivered ibuprofen. Ibuprofen (150 mg) formulations with several concentrati
PMID 23996466

Japanese Journal

A Case of Ventricular Septal Defect and Atrial Septal Defect in an Infant with Right Lung Aplasia.

石川和徳,星野俊一,岩谷文夫,小野隆志,佐藤晃一,三沢幸辰
日本心臓血管外科学会雑誌 28(3), 163-166, 1999
… Tolazoline hydrochloride decreased pulmonary vascular resistance (Rp) from 6.92 units·m2 to 3.11 units·m2. …
NAID 130003438529

A case of general anaesthsia in ophthalmectomy on a steller sea lion (Eumetopias jubatus).

山下和人,水野信哉,井上久美子,奥村正裕,成清美智代,浅野和之,小林俊明,平知子,野村卓司,藤永徹
獣医麻酔外科学雑誌 21(4), 85-91, 1990
… After preanesthesia using atropine sulfate (0.01 mg/kg, IM) and diazepam (0.2 mg/kg, IM), and induction of anesthesia using xylazine hydrochloride (1 mg/kg, IM) and ketamine hydrochloride (7 mg/kg, IM), a young steller sea lion was maintained with inhalation anesthesia using oxygen-halothane mixture to ophthalmectomize. …
NAID 130004184840

Actions of desoxynupharidine hydrochloride in the central nervous system of experimental animals (I).

Suzuki Yukiko [他],HAGIWARA Yukihiko,TAGUCHI Kyoji,KAJIYAMA Kazuyo,IKEDA Takato
The Japanese Journal of Pharmacology 31(3), 391-400, 1981
… The effects of desoxynupharidine hydrochloride (DN) as the extractive component of the Nuphar japonicum DC on the central nervous system were studied. … These spontaneous EEG activities were significantly inhibited by epinephrine hydrochloride and were potentiated by tolazoline hydrochloride and dibenamine hydrochloride etc. …
NAID 130000835620

「塩酸トラゾリン」

Tolazoline
Systematic (IUPAC) name
	2-benzyl-4,5-dihydro-1H-imidazole
Clinical data
AHFS/Drugs.com	International Drug Names
Routes of; administration	IV
Identifiers
CAS Number	59-98-3
ATC code	C04AB02 M02AX02 QV03AB94
PubChem	CID: 5504
IUPHAR/BPS	7310
DrugBank	DB00797
ChemSpider	5303
UNII	CHH9H12AQ3
KEGG	D08614
ChEBI	CHEBI:28502
ChEMBL	CHEMBL770
Chemical data
Formula	C10H12N2
Molecular mass	160.216 g/mol
	SMILES N\1=C(\NCC/1)Cc2ccccc2 ;
	InChI InChI=1S/C10H12N2/c1-2-4-9(5-3-1)8-10-11-6-7-12-10/h1-5H,6-8H2,(H,11,12) ; Key:JIVZKJJQOZQXQB-UHFFFAOYSA-N ;
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