METHAZOLAMIDE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

METHAZOLAMIDE (UNII: W733B0S9SD) (METHAZOLAMIDE - UNII:W733B0S9SD)

Available from:

ANI Pharmaceuticals, Inc.

INN (International Name):

METHAZOLAMIDE

Composition:

METHAZOLAMIDE 25 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Methazolamide Tablets are 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.

Product summary:

Methazolamide Tablets USP, 25 mg, are white, square, un-scored tablets, debossed “ANI” on one side and “240” on the other side; supplied in bottles of 100 (NDC 62559-240-01). Methazolamide Tablets USP, 50 mg, are white, round tablets, scored on one side and debossed “ANI” and “241” on the other side; supplied in bottles of 100 (NDC 62559-241-01). Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Dispense in a tight container as defined in the USP, with a child-resistant closure (as required). Rx only Manufactured by: ANI Pharmaceuticals, Inc. Baudette, MN 56623 9656 Rev 07/23

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

METHAZOLAMIDE- METHAZOLAMIDE TABLET
ANI PHARMACEUTICALS, INC.
----------
METHAZOLAMIDE TABLETS USP
RX ONLY
DESCRIPTION
Methazolamide, a sulfonamide derivative, is a white crystalline
powder, weakly acidic,
slightly soluble in water, alcohol and acetone. The chemical name for
methazolamide is:
N-[5-(aminosulfonyl)-3-methyl-1,3,4-thiadiazo1-2(3H)-ylidene]-acetamide
and it has the
following structural formula:
Molecular Formula: C H N O S Molecular
Weight: 236.26
Each tablet, for oral administration, contains 25 mg or 50 mg of
methazolamide USP. In
addition, each tablet contains the following inactive ingredients:
dibasic calcium
phosphate dihydrate, glyceryl behenate, povidone, pregelatinized
starch, and sodium
starch glycolate.
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 bid, 50
mg bid, and 100
mg bid demonstrated a linear relationship between plasma methazolamide
levels and
methazolamide dose. Peak plasma concentrations (C
) for the 25 mg, 50 mg and 100
mg bid 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) was 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
extra-cellular fluid. The mean
apparent volume of distribution (V
/F) ranges from 17 L 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 bid, 50 mg bid, and 100 mg bid, respectively.
5
8
4
3 2
max
area
The mean steady-state plasma elimination half-life for