药品详细

Tolazamide(妥拉磺脲)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

妥拉磺脲

英文名

Tolazamide

分子式

C₁₄H₂₁N₃O₃S

化学名

1-(azepan-1-yl)-3-[(4-methylbenzene)sulfonyl]urea

分子量

Average: 311.4
Monoisotopic: 311.130362243

CAS号

1156-19-0

ATC分类

A10B Oral Blood Glucose Lowering Drugs, Excl. Insulins

药物类型

small molecule

阶段

approved

商品名

Norglycin;Tolanase;Tolinase;

同义名

基本介绍

A sulphonylurea hypoglycemic agent with actions and uses similar to those of chlorpropamide. [PubChem]

生产厂家

Barr laboratories inc
Duramed pharmaceuticals inc sub barr laboratories inc
Interpharm inc
Ivax pharmaceuticals inc sub teva pharmaceuticals usa
Mutual pharmaceutical co inc
Mylan pharmaceuticals inc
Par pharmaceutical inc
Pharmacia and upjohn co
Sandoz inc
Superpharm corp
Usl pharma inc
Watson laboratories inc

封装厂家

Apotheca Inc.
Central Texas Community Health Centers
Dispensing Solutions
Ivax Pharmaceuticals
Kaiser Foundation Hospital
Major Pharmaceuticals
Murfreesboro Pharmaceutical Nursing Supply
Mutual Pharmaceutical Co.
Mylan
PCA LLC
PD-Rx Pharmaceuticals Inc.
Pharmaceutical Utilization Management Program VA Inc.
Pharmedix
Physicians Total Care Inc.

参考

Synthesis Reference	Not Available
General Reference	Not Available

剂型

规格

化合物类型

Type	small molecule

Classes

Sulfonylureas

Substructures

Sulfonylureas
Sulfonyls
Benzene and Derivatives
Benzenesulfonamides
Heterocyclic compounds
Aromatic compounds
Sulfonamides
Semicarbazides
Hydrazine Derivatives

适应症

药理

Indication	For use as an adjunct to diet to lower the blood glucose in patients with non-insulin dependent diabetes mellitus (Type II) whose hyperglycemia cannot be satisfactorily controlled by diet alone.
Pharmacodynamics	Tolazamide is an oral blood glucose lowering drug of the sulfonylurea class. Tolazamide appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. The mechanism by which tolazamide lowers blood glucose during long-term administration has not been clearly established. With chronic administration in Type II diabetic patients, the blood glucose lowering effect persists despite a gradual decline in the insulin secretory response to the drug. Extrapancreatic effects may be involved in the mechanism of action of oral sulfonylurea hypoglycemic drugs. Some patients who are initially responsive to oral hypoglycemic drugs, including tolazamide, may become unresponsive or poorly responsive over time. Alternatively, tolazamide may be effective in some patients who have become unresponsive to one or more other sulfonylurea drugs. In addition to its blood glucose lowering actions, tolazamide produces a mild diuresis by enhancement of renal free water clearance.
Mechanism of action	Sulfonylureas likely bind to ATP-sensitive potassium-channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin.
Absorption	Rapidly and well absorbed from the gastrointestinal tract.
Volume of distribution	Not Available
Protein binding	Not Available
Metabolism	Tolazamide is metabolized to five major metabolites ranging in hypoglycemic activity from 0 to 70%.
Route of elimination	Tolazamide is metabolized to five major metabolites ranging in hypoglycemic activity from 0% to 70%. They are excreted principally in the urine.
Half life	The average biological half-life of the drug is 7 hours.
Clearance	Not Available
Toxicity	Overdosage of sulfonylureas can produce hypoglycemia. Severe hypoglycemic reactions with coma, seizure, or other neurological impairment occur infrequently, but constitute medical emergencies requiring immediate hospitalization.
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
melting point	170-173 °C	PhysProp
water solubility	65.4 mg/L (at 30 °C)	YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP	2.69	SANGSTER (1993)
logS	-3.68	ADME Research, USCD

Predicted Properties

Property	Value	Source
water solubility	3.08e-01 g/l	ALOGPS
logP	1.4	ALOGPS
logP	1.91	ChemAxon
logS	-3	ALOGPS
pKa (strongest acidic)	4.07	ChemAxon
pKa (strongest basic)	1.61	ChemAxon
physiological charge	-1	ChemAxon
hydrogen acceptor count	4	ChemAxon
hydrogen donor count	2	ChemAxon
polar surface area	78.51	ChemAxon
rotatable bond count	2	ChemAxon
refractivity	81.34	ChemAxon
polarizability	32.82	ChemAxon

药物相互作用

Drug	Interaction
Acebutolol	Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
Acetylsalicylic acid	Acetylsalicylic acid increases the effect of the sulfonylurea, tolazamide.
Amifostine	Additive hypotensive effects may occur. At chemotherapeutic doses of Amifostine, Tolazamide should be withheld for 24 hours prior to Amifostine administration. Use caution at lower doses of Amifostine.
Atenolol	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Bisoprolol	The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
Carvedilol	The beta-blocker, carvedilol, may decrease symptoms of hypoglycemia.
Chloramphenicol	Chloramphenicol may increase the effect of sulfonylurea, tolazamide.
Clofibrate	Clofibrate may increase the effect of sulfonylurea, tolazamide.
Esmolol	The beta-blocker, esmolol, may decrease symptoms of hypoglycemia.
Labetalol	The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
Metoprolol	The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia.
Nadolol	The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
Oxprenolol	The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
Phenylbutazone	Phenylbutazone increases the effect of the hypoglycemic agent
Pindolol	The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
Propranolol	The beta-blocker, propranolol, may decrease symptoms of hypoglycemia.
Rifampin	Rifampin may decrease the effect of sulfonylurea, tolazamide.
Rituximab	Additive hypotensive effects may occur. Consider withholding Tolazamide for 12 hours prior to administration of Rituximab.
Somatropin recombinant	Somatropin may antagonize the hypoglycemic effect of Tolazamide. Dose adjustments of Tolazamide may be required.
Timolol	The beta-blocker, timolol, may decrease symptoms of hypoglycemia.

食物相互作用

Not Available

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