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Methazolamide

产品号 DB00703 公司名称 DrugBank
CAS号 554-57-4 公司网站 http://www.ualberta.ca/
分子式 C5H8N4O3S2 电 话 (780) 492-3111
分子量 236.27202 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 584

产品价格信息

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产品别名

标题
Methazolamide
IUPAC标准名
N-[(2Z)-3-methyl-5-sulfamoyl-2,3-dihydro-1,3,4-thiadiazol-2-ylidene]acetamide
IUPAC传统名
methazolamide
商标名
Neptazaneat
Neptazane
Naptazane
MZM
Methenamide

产品登记号

CAS号 554-57-4
PubChem CID 4100
PubChem SID 46506393

产品性质

疏水性(logP) -1.6
溶解度 3500 mg/L

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. [PubChem]
Indication For treatment of chronic open-angle glaucoma and acute angle-closure glaucoma
Pharmacology Methazolamide is topical carbonic anhydrase inhibitor. Methazolamide is indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension who are insufficiently responsive to beta-blockers. Methazolamide is a sulfonamide derivative; however, it does not have any clinically significant antimicrobial properties. Although methazolamide achieves a high concentration in the cerebrospinal fluid, it is not-considered an effective anticonvulsant. Methazolamide has a weak and transient diuretic effect, therefore use results in an increase in urinary volume, with excretion of sodium, potassium and chloride.
Toxicity Electrolyte imbalance, development of an acidotic state, and central nervous system effects might be expected to occur in the case of an overdose.
Affected Organisms
Humans and other mammals
Absorption Methazolamide is well absorbed from the gastrointestinal tract.
Half Life 14 hours
Protein Binding 55%
Distribution * 17 to 23 L
References
Iyer GR, Bellantone RA, Taft DR: In vitro characterization of the erythrocyte distribution of methazolamide: a model of erythrocyte transport and binding kinetics. J Pharmacokinet Biopharm. 1999 Feb;27(1):45-66. [Pubmed]
Shirato S, Kagaya F, Suzuki Y, Joukou S: Stevens-Johnson syndrome induced by methazolamide treatment. Arch Ophthalmol. 1997 Apr;115(4):550-3. [Pubmed]
Skorobohach BJ, Ward DA, Hendrix DV: Effects of oral administration of methazolamide on intraocular pressure and aqueous humor flow rate in clinically normal dogs. Am J Vet Res. 2003 Feb;64(2):183-7. [Pubmed]
External Links
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参考文献

  • Iyer GR, Bellantone RA, Taft DR: In vitro characterization of the erythrocyte distribution of methazolamide: a model of erythrocyte transport and binding kinetics. J Pharmacokinet Biopharm. 1999 Feb;27(1):45-66. Pubmed
  • Shirato S, Kagaya F, Suzuki Y, Joukou S: Stevens-Johnson syndrome induced by methazolamide treatment. Arch Ophthalmol. 1997 Apr;115(4):550-3. Pubmed
  • Skorobohach BJ, Ward DA, Hendrix DV: Effects of oral administration of methazolamide on intraocular pressure and aqueous humor flow rate in clinically normal dogs. Am J Vet Res. 2003 Feb;64(2):183-7. Pubmed