Country: United States
Language: English
Source: NLM (National Library of Medicine)
METHAZOLAMIDE (UNII: W733B0S9SD) (METHAZOLAMIDE - UNII:W733B0S9SD)
Sandoz Inc
METHAZOLAMIDE
METHAZOLAMIDE 25 mg
ORAL
PRESCRIPTION DRUG
Methazolamide is indicated in the treatment of ocular conditions where lowering intraocular pressure is likely to be of therapeutic benefit, such as chronic open-angle glaucoma, secondary glaucoma, and preoperatively in acute angle-closure glaucoma where lowering the intraocular pressure is desired before surgery. Methazolamide therapy is contraindicated in situations in which sodium and/or potassium serum levels are depressed, in cases of marked kidney or liver disease or dysfunction, in adrenal gland failure, and in hyperchloremic acidosis. In patients with cirrhosis, use may precipitate the development of hepatic encephalopathy. Long-term administration of methazolamide is contraindicated in patients with angle-closure glaucoma, since organic closure of the angle may occur in spite of lowered intraocular pressure.
Methazolamide tablets, USP for oral administration are available as: 25 mg: Round, white, unscored tablets debossed GG 78 on one side and plain on the reverse side, and supplied as: NDC 0781-1072-01 bottles of 100 NDC 0781-1072-10 bottles of 1000 50 mg: Round, white, scored tablets debossed GG 181 on one side and plain on the reverse side, and supplied as: NDC 0781-1071-01 bottles of 100 NDC 0781-1071-10 bottles of 1000 Store at 20°-25°C (68°-77°F) (see USP Controlled Room Temperature). Dispense in a tight, light-resistant container.
Abbreviated New Drug Application
METHAZOLAMIDE- METHAZOLAMIDE TABLET SANDOZ INC ---------- METHAZOLAMIDE TABLETS, USP DESCRIPTION Methazolamide, a sulfonamide derivative, is a white crystalline powder, weakly acidic, and slightly soluble in water, alcohol and acetone. It is available as 25 mg and 50 mg tablets. The chemical name for methazolamide is _N_ -[5-(aminosulfonyl)-3-methyl-1,3,4-thiadiazol-2(3_H_)-ylidene]-acetamide and it has the following structural formula: Methazolamide tablets, USP contain 25 mg or 50 mg of methazolamide. Inactive ingredients: croscarmellose sodium, hydroxypropyl methylcellulose, lactose (monohydrate), magnesium stearate, microcrystalline cellulose, and sodium lauryl sulfate. CLINICAL PHARMACOLOGY Methazolamide is a potent inhibitor of carbonic anhydrase. Methazolamide is well absorbed from the gastrointestinal tract. Peak plasma concentrations are observed 1 to 2 hours after dosing. In a multiple-dose, pharmacokinetic study, administration of methazolamide 25 mg b.i.d., 50 mg b.i.d. and 100 mg b.i.d. demonstrated a linear relationship between plasma methazolamide levels and methazolamide dose. Peak plasma concentrations (C ) for the 25 mg, 50 mg and 100 mg b.i.d. regimens were 2.5 mcg/mL, 5.1 mcg/mL and 10.7 mcg/mL, respectively. The area under the plasma concentration-time curves (AUC) were 1130 mcg. min/mL, 2571 mcg. min/mL and 5418 mcg. min/mL for the 25 mg, 50 mg and 100 mg dosage regimens, respectively. Methazolamide is distributed throughout the body including the plasma, cerebrospinal fluid, aqueous humor of the eye, red blood cells, bile and extracellular fluid. The mean apparent volume of distribution (V /F) ranges from 17 to 23 L. Approximately 55% is bound to plasma proteins. The steady-state methazolamide red blood cell: plasma ratio varies with dose and was found to be 27:1, 16:1 and 10:1 following the administration of methazolamide 25 mg b.i.d., 50 mg b.i.d. and 100 mg b.i.d., respectively. The mean steady-state plasma elimination half-life for methazolamide is approximately 14 hours. At steady-stat Read the complete document