Acetazolamide

INDICATIONS AND USAGE: For adjunctive treatment of: chronic simple (open-angle) glaucoma, secondary glaucoma, and preoperatively in acute angle-closure glaucoma where delay of surgery is desired in order to lower intraocular pressure. Acetazolamide extended-release capsules are also indicated for the prevention or amelioration of symptoms associated with acute mountain sickness despite gradual ascent.

DOSAGE AND ADMINISTRATION: Glaucoma The recommended dosage is 1 capsule (500 mg) two times a day. Usually 1 capsule is administered in the morning and 1 capsule in the evening. It may be necessary to adjust the dose, but it has usually been found that dosage in excess of 2 capsules (1 g) does not produce an increased effect. The dosage should be adjusted with careful individual attention both to symptomatology and intraocular tension. In all cases, continuous supervision by a physician is advisable. In those unusual instances where adequate control is not obtained by the twice-a-day administration of acetazolamide extended-release capsules, the desired control may be established by means of acetazolamide (tablets or parenteral). Use tablets or parenteral in accordance with the more frequent dosage schedules recommended for these dosage forms, such as 250 mg every four hours, or an initial dose of 500 mg followed by 250 mg or 125 mg every four hours, depending on the case in question. Acute Mountain Sickness Dosage is 500 mg to 1,000 mg daily, in divided doses using tablets or extended-release capsules as appropriate. In circumstances of rapid ascent, such as in rescue or military operations, the higher dose level of 1,000 mg is recommended. It is preferable to initiate dosing 24 to 48 hours before ascent and to continue for 48 hours while at high altitude, or longer as necessary to control symptoms.

CONTRAINDICATIONS: Hypersensitivity to acetazolamide or any excipients in the formulation. Since acetazolamide is a sulfonamide derivative, cross sensitivity between acetazolamide, sulfonamides and other sulfonamide derivatives is possible. Acetazolamide therapy is contraindicated in situations in which sodium and/or potassium blood serum levels are depressed, in cases of marked kidney and liver disease or dysfunction, in suprarenal gland failure, and in hyperchloremic acidosis. It is contraindicated in patients with cirrhosis because of the risk of development of hepatic encephalopathy. Long-term administration of acetazolamide extended-release capsules are contraindicated in patients with chronic non-congestive angle-closure glaucoma since it may permit organic closure of the angle to occur while the worsening glaucoma is masked by lowered intraocular pressure.

ADVERSE REACTIONS: Body as a whole: Headache, malaise, fatigue, fever, pain at injection site, flushing, growth retardation in children, flaccid paralysis, anaphylaxis. Digestive: Gastrointestinal disturbances such as nausea, vomiting, diarrhea. Hematological/Lymphatic: Blood dyscrasias such as aplastic anemia, agranulocytosis, leukopenia, thrombocytopenic purpura, melena. Hepato-biliary disorders: Abnormal liver function, cholestatic jaundice, hepatic insufficiency, fulminant hepatic necrosis. Metabolic/Nutritional: Metabolic acidosis, electrolyte imbalance, including hypokalemia, hyponatremia, osteomalacia with long-term phenytoin therapy, loss of appetite, taste alteration, hyper/hypoglycemia. Nervous: Drowsiness, paresthesia (including numbness and tingling of extremities and face), depression, excitement, ataxia, confusion, convulsions, dizziness. ​Skin: Allergic skin reactions including urticaria, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis. Otologic: Hearing disturbances, tinnitus. Eye Disorders: Choroidal effusion, choroidal detachment, transient myopia. Transient myopia is the result of forward movement of the ciliary body leading to a narrowing of the angle. Urogenital: Crystalluria, increased risk of nephrolithiasis with long-term therapy, hematuria, glycosuria, renal failure, polyuria. To report SUSPECTED ADVERSE REACTIONS, contact Avet Pharmaceuticals Inc. at 1-866-901-DRUG (3784) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Drug Interactions Aspirin - See WARNINGS Acetazolamide extended-release capsules modifies phenytoin metabolism with increased serum levels of phenytoin. This may increase or enhance the occurrence of osteomalacia in some patients receiving chronic phenytoin therapy. Caution is advised in patients receiving chronic concomitant therapy. By decreasing the gastrointestinal absorption of primidone, acetazolamide extended-release capsules may decrease serum concentrations of primidone and its metabolites, with a consequent possible decrease in anticonvulsant effect. Caution is advised when beginning, discontinuing, or changing the dose of acetazolamide extended-release capsules in patients receiving primidone. Because of possible additive effects with other carbonic anhydrase inhibitors, concomitant use is not advisable. Acetazolamide may increase the effects of other folic acid antagonists. Acetazolamide decreases urinary excretion of amphetamine and may enhance the magnitude and duration of their effect. Acetazolamide reduces urinary excretion of quinidine and may enhance its effect. Acetazolamide may prevent the urinary antiseptic effect of methenamine. Acetazolamide increases lithium excretion and the lithium may be decreased. Acetazolamide and sodium bicarbonate used concurrently increase the risk of renal calculus formation. Acetazolamide may elevate cyclosporine levels.

DESCRIPTION: Acetazolamide extended-release capsules are an inhibitor of the enzyme carbonic anhydrase. Acetazolamide is a white to faintly yellowish white crystalline, odorless powder, weakly acidic, very slightly soluble in water, and slightly soluble in alcohol. The chemical name for acetazolamide is N-(5-Sulfamoyl-1,3, 4-thiadiazol-2-yl)acetamide and has the following chemical structure: MW 222.24C 4 H 6 N 4 O 3 S 2 Acetazolamide extended-release capsules are extended-release capsules, for oral administration, each containing 500 mg of acetazolamide and the following inactive ingredients: Ethyl acrylate and methacrylate copolymer, microcrystalline cellulose, purified talc and sodium lauryl sulfate. The ingredients in the capsule shell are FD &C Blue 1, FD&C Yellow 6, gelatin, iron oxide yellow and titanium dioxide. The ingredients in the imprinting ink are shellac, iron oxide black and potassium hydroxide. acetazolamide-structure

OVERDOSAGE: No specific antidote is known. Treatment should be symptomatic and supportive. Electrolyte imbalance, development of an acidotic state, and central nervous system effects might be expected to occur. Serum electrolyte levels (particularly potassium) and blood pH levels should be monitored. Supportive measures are required to restore electrolyte and pH balance. The acidotic state can usually be corrected by the administration of bicarbonate. Despite its high intraerythrocytic distribution and plasma protein binding properties, acetazolamide extended-release capsules may be dialyzable. This may be particularly important in the management of acetazolamide extended-release capsules overdosage when complicated by the presence of renal failure.

HOW SUPPLIED: Acetazolamide extended-release capsules are available as: 500 mg: Orange opaque cap and orange opaque body, size ‘00’ capsule having imprinting ‘A’ on cap and ‘247’ on body with black ink, filled with white to off-white pellets. NDC 62332-349-31 Bottle of 100 capsules NDC 62332-349-91 Bottle of 1000 capsules Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. You may also report side effects to Alembic Pharmaceuticals Limited at 1-866-210-9797. Manufactured by: Alembic Pharmaceuticals Limited (Formulation Division), Panelav 389350, Gujarat, India Manufactured for: Alembic Pharmaceuticals, Inc. Bedminster, NJ 07921, USA Revised: 09/2024