Methazolamide Tablets

The chemical structure of this product is similar to acetazolamide (with an extra methyl group on the nitrogen atom). Therefore, the pharmacological effects and mechanism of action are the same as those of acetazolamide. Because the structural design of methazolamide reduces ionization, the intraocular permeability is enhanced compared with acetazolamide. The function of this product to penetrate the blood-aqueous humor and blood-brain barriers is also stronger than that of acetazolamide (the concentration of human cerebrospinal fluid is 50 times higher than that of acetazolamide). The inhibition of carbonic anhydrase is 60% stronger than that of acetazolamide. In the body, only 55% of methazolamide is bound to plasma proteins (while 90% to 95% of acetazolamide is bound to plasma proteins). Because only the unbound part of the drug dose exerts pharmacological effects, a lower dose can significantly reduce intraocular pressure. Methazolamide can inhibit the production of aqueous humor, and the production of aqueous humor can be reduced by 40% in most patients after taking the drug. The intraocular pressure-lowering effect occurs 1 to 2 hours after oral administration and lasts for 16 to 18 hours. The intraocular pressure-lowering effect of this product is dose-dependent. Taking 25, 50 and 100 mg orally once every 8 hours can reduce intraocular pressure by 3.3, 4.3 and 5.6 mmHg respectively.

The main ingredients of this product and their chemical names: Main ingredient: methazolamide, chemical name: 5-acetamido-4-methyl-1-thio-3,4-diazolylsulfonamide. Its molecular formula and molecular weight: C5H8N4O3S2, 236.26

This product is white tablets.

It is used as an adjuvant treatment for patients with primary open-angle glaucoma, angle-closure glaucoma and some secondary glaucoma whose intraocular pressure is not well controlled by topical anti-glaucoma drugs. Because this product has less effect on acid-base balance while lowering intraocular pressure, it is better than acetazolamide for patients with severe obstructive pulmonary disease. Methazolamide has less effect on urinary citrate secretion than acetazolamide, so it is recommended for patients who need oral carbonic anhydrase inhibitor treatment but are prone to kidney stone formation.

For adults, the initial oral administration is 25 mg twice a day. This dose can usually reduce intraocular pressure by 4 to 5 mmHg with minimal side effects. If the intraocular pressure-lowering effect is not satisfactory after medication, the dose can be increased to 50 mg twice a day.

1. There are reports that methazolamide can cause serious hematological adverse reactions, including aplastic anemia and agranulocytosis. 2. There are reports that taking methazolamide can cause kidney stones, but this is very rare. 3. Other adverse reactions include nausea, anorexia, paresthesia, discomfort, fatigue and skin erosion.

1. It is contraindicated for patients with liver and kidney dysfunction causing hyponatremia, hypokalemia, hyperchloremic acidosis, adrenal failure and adrenal cortex insufficiency (Addison's disease) and those with a tendency to hepatic coma. 2. It is contraindicated for patients with a history of allergy to sulfonamides.

Precautions for children: The safety and efficacy of this product for children are still unclear. Precautions for pregnancy and lactation: 1. This product can cause malformations in rodents, so pregnant women should avoid taking it. 2. It is not clear whether this product is secreted into the milk. If lactating women use this product for treatment, they should stop breastfeeding. Precautions for the elderly: The elderly and adults have good tolerance to this product, so this product is suitable for elderly patients.

1. Carbonic anhydrase inhibitors combined with high-dose aspirin can cause serious metabolic disorders. Therefore, this product should be used with caution in combination with salicylic acid preparations. 2. Low-dose methazolamide itself does not cause hypokalemia, but carbonic anhydrase inhibitors can increase the potassium excretion effect of other drugs. 3. Combined use with adrenocorticotropic hormone and glucocorticoids can lead to severe hypokalemia. When combined with other drugs, attention should be paid to monitoring serum potassium concentration and cardiac function. It should also be estimated that long-term simultaneous use increases the risk of hypocalcemia and can cause osteoporosis because these drugs increase calcium excretion.

Keep away from light and store in airtight container.

25 mg x 10 tablets

Tentative 24 months

Hangzhou Qianyuan Baoling Pharmaceutical Co., Ltd.

• Founded in:

  1994-12-30

• Address:

  No. 668, No. 23 Street, Qiantang New District, Hangzhou, Zhejiang

• Tax NO.:

  91330101609132986R

• Registered Funds:

  360 million yuan

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