| 药品名称 |
Methazolamide
|
| 分子靶点 |
Carbonic anhydrase 1;Carbonic anhydrase 2;Carbonic anhydrase 4;Carbonic anhydrase 7;Carbonic anhydrase 3
|
| 酶 |
Cytochrome P450 2C19;Cytochrome P450 2D6;Cytochrome P450 2E1;Cytochrome P450 3A4
|
| 药物类型 |
Small Molecule
|
| 研发阶段 |
Approved
|
| 药物描述 |
A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. [PubChem]
|
| 结构式 |
 |
| 药物别名 |
Metazolamida;Methazolamid;Méthazolamide;Methazolamide;Methazolamidum;Methenamide;Neptazaneat
|
| 治疗类别 |
Antiglaucoma Preparations and Miotics;Carbonic Anhydrase Inhibitors;Cardiovascular Agents;Cytochrome P-450 CYP2C19 Inhibitors;Cytochrome P-450 CYP2D6 Inhibitors;Cytochrome P-450 CYP2E1 Inhibitors;Cytochrome P-450 CYP3A Inhibitors;Cytochrome P-450 CYP3A4 Inhibitors;Cytochrome P-450 Enzyme Inhibitors;Diuretics;Enzyme Inhibitors;Hypotensive Agents;Natriuretic Agents;Ophthalmologicals;Sensory Organs;Sulfur Compounds;Thiadiazoles;Thiazoles
|
| UNII号 |
W733B0S9SD
|
| CAS号 |
554-57-4
|
| 分子量 |
236.26
|
| 分子式 |
C5H8N4O3S2
|
| 适应症 |
For treatment of chronic open-angle glaucoma and acute angle-closure glaucoma
|
| 药效学 |
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.
|
| 作用机制 |
Methazolamide is a potent inhibitor of carbonic anhydrase. Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport.
|
| 吸收 |
Methazolamide is well absorbed from the gastrointestinal tract.
|
| 分布量 |
17 to 23 L
|
| 蛋白结合 |
55%
|
| 半衰期 |
14 hours
|
| 毒理 |
Electrolyte imbalance, development of an acidotic state, and central nervous system effects might be expected to occur in the case of an overdose.
|
| ATC代码 |
S01EC05
|
