Acetazolamide


Zydus Pharmaceuticals Usa Inc.
Human Prescription Drug
NDC 68382-076
Acetazolamide is a human prescription drug labeled by 'Zydus Pharmaceuticals Usa Inc.'. National Drug Code (NDC) number for Acetazolamide is 68382-076. This drug is available in dosage form of Injection, Powder, Lyophilized, For Solution. The names of the active, medicinal ingredients in Acetazolamide drug includes Acetazolamide Sodium - 500 mg/5mL . The currest status of Acetazolamide drug is Active.

Drug Information:

Drug NDC: 68382-076
The labeler code and product code segments of the National Drug Code number, separated by a hyphen. Asterisks are no longer used or included within the product code segment to indicate certain configurations of the NDC.
Proprietary Name: Acetazolamide
Also known as the trade name. It is the name of the product chosen by the labeler.
Product Type: Human Prescription Drug
Indicates the type of product, such as Human Prescription Drug or Human OTC Drug. This data element corresponds to the “Document Type” of the SPL submission for the listing.
Non Proprietary Name: Acetazolamide
Also known as the generic name, this is usually the active ingredient(s) of the product.
Labeler Name: Zydus Pharmaceuticals Usa Inc.
Name of Company corresponding to the labeler code segment of the ProductNDC.
Dosage Form: Injection, Powder, Lyophilized, For Solution
The translation of the DosageForm Code submitted by the firm. There is no standard, but values may include terms like `tablet` or `solution for injection`.The complete list of codes and translations can be found www.fda.gov/edrls under Structured Product Labeling Resources.
Status: Active
FDA does not review and approve unfinished products. Therefore, all products in this file are considered unapproved.
Substance Name:ACETAZOLAMIDE SODIUM - 500 mg/5mL
This is the active ingredient list. Each ingredient name is the preferred term of the UNII code submitted.
Route Details:INTRAVENOUS
The translation of the Route Code submitted by the firm, indicating route of administration. The complete list of codes and translations can be found at www.fda.gov/edrls under Structured Product Labeling Resources.

Marketing Information:

An openfda section: An annotation with additional product identifiers, such as NUII and UPC, of the drug product, if available.
Marketing Category: ANDA
Product types are broken down into several potential Marketing Categories, such as New Drug Application (NDA), Abbreviated New Drug Application (ANDA), BLA, OTC Monograph, or Unapproved Drug. One and only one Marketing Category may be chosen for a product, not all marketing categories are available to all product types. Currently, only final marketed product categories are included. The complete list of codes and translations can be found at www.fda.gov/edrls under Structured Product Labeling Resources.
Marketing Start Date: 09 Jan, 2020
This is the date that the labeler indicates was the start of its marketing of the drug product.
Marketing End Date: 21 Dec, 2025
This is the date the product will no longer be available on the market. If a product is no longer being manufactured, in most cases, the FDA recommends firms use the expiration date of the last lot produced as the EndMarketingDate, to reflect the potential for drug product to remain available after manufacturing has ceased. Products that are the subject of ongoing manufacturing will not ordinarily have any EndMarketingDate. Products with a value in the EndMarketingDate will be removed from the NDC Directory when the EndMarketingDate is reached.
Application Number: ANDA206533
This corresponds to the NDA, ANDA, or BLA number reported by the labeler for products which have the corresponding Marketing Category designated. If the designated Marketing Category is OTC Monograph Final or OTC Monograph Not Final, then the Application number will be the CFR citation corresponding to the appropriate Monograph (e.g. “part 341”). For unapproved drugs, this field will be null.
Listing Expiration Date: 31 Dec, 2023
This is the date when the listing record will expire if not updated or certified by the firm.

OpenFDA Information:

An openfda section: An annotation with additional product identifiers, such as NUII and UPC, of the drug product, if available.
Manufacturer Name:Zydus Pharmaceuticals USA Inc.
Name of manufacturer or company that makes this drug product, corresponding to the labeler code segment of the NDC.
RxCUI:307702
The RxNorm Concept Unique Identifier. RxCUI is a unique number that describes a semantic concept about the drug product, including its ingredients, strength, and dose forms.
Original Packager:Yes
Whether or not the drug has been repackaged for distribution.
UPC:0368382076106
UPC stands for Universal Product Code.
UNII:429ZT169UH
Unique Ingredient Identifier, which is a non-proprietary, free, unique, unambiguous, non-semantic, alphanumeric identifier based on a substance’s molecular structure and/or descriptive information.
Pharmacologic Class:Carbonic Anhydrase Inhibitor [EPC]
Carbonic Anhydrase Inhibitors [MoA]
Sulfonamides [CS]
These are the reported pharmacological class categories corresponding to the SubstanceNames listed above.

Packaging Information:

Package NDCDescriptionMarketing Start DateMarketing End DateSample Available
68382-076-101 VIAL in 1 CARTON (68382-076-10) / 5 mL in 1 VIAL09 Jan, 2020N/ANo
Package NDC number, known as the NDC, identifies the labeler, product, and trade package size. The first segment, the labeler code, is assigned by the FDA. Description tells the size and type of packaging in sentence form. Multilevel packages will have the descriptions concatenated together.

Product Elements:

Acetazolamide acetazolamide acetazolamide sodium acetazolamide sodium hydroxide hydrochloric acid

Indications and Usage:

Indications and usage for adjunctive treatment of: edema due to congestive heart failure; drug-induced edema; centrencephalic epilepsies (petit mal, unlocalized seizures); 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.

Warnings:

Warnings fatalities have occurred, although rarely, due to severe reactions to sulfonamides including stevens-johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, anaphylaxis, agranulocytosis, aplastic anemia, and other blood dyscrasias. sensitizations may recur when a sulfonamide is readministered irrespective of the route of administration. if signs of hypersensitivity or other serious reactions occur, discontinue use of this drug. caution is advised for patients receiving concomitant high-dose aspirin and acetazolamide, as anorexia, tachypnea, lethargy, metabolic acidosis, coma, and death have been reported.

Dosage and Administration:

Dosage and administration preparation and storage of parenteral solutions each 500 mg vial containing sterile acetazolamide sodium should be reconstituted with at least 5 ml of sterile water for injection prior to use. reconstituted solutions retain their physical and chemical properties for 3 days under refrigeration at 2° to 8°c (36° to 46°f), or 12 hours at room temperature 20° to 25°c (68° to 77°f). contains no preservative. the direct intravenous route of administration is preferred. intramuscular administration is not recommended. glaucoma acetazolamide should be used as an adjunct to the usual therapy. the dosage employed in the treatment of chronic simple (open-angle) glaucoma ranges from 250 mg to 1 g of acetazolamide per 24 hours, usually in divided doses for amounts over 250 mg. it has usually been found that a dosage in excess of 1 g per 24 hours does not produce an increased effect. in all cases, the dosage should be adjusted with careful individual
attention both to symptomatology and ocular tension. continuous supervision by a physician is advisable. in treatment of secondary glaucoma and in the preoperative treatment of some cases of acute congestive (closed-angle) glaucoma, the preferred dosage is 250 mg every four hours, although some cases have responded to 250 mg twice daily on short-term therapy. in some acute cases, it may be more satisfactory to administer an initial dose of 500 mg followed by 125 or 250 mg every four hours depending on the individual case. intravenous therapy may be used for rapid relief of ocular tension in acute cases. a complementary effect has been noted when acetazolamide has been used in conjunction with miotics or mydriatics as the case demanded. epilepsy it is not clearly known whether the beneficial effects observed in epilepsy are due to direct inhibition of carbonic anhydrase in the central nervous system or whether they are due to the slight degree of acidosis produced by the divided dosage. the best results to date have been seen in petit mal in children. good results, however, have been seen in patients, both children and adult, in other types of seizures such as grand mal, mixed seizure patterns, myoclonic jerk patterns, etc. the suggested total daily dose is 8 to 30 mg per kg in divided doses. although some patients respond to a low dose, the optimum range appears to be from 375 to 1000 mg daily. however, some investigators feel that daily doses in excess of 1 g do not produce any better results than a 1 g dose. when acetazolamide is given in combination with other anticonvulsants, it is suggested that the starting dose should be 250 mg once daily in addition to the existing medications. this can be increased to levels as indicated above. the change from other medications to acetazolamide should be gradual and in accordance with usual practice in epilepsy therapy. congestive heart failure for diuresis in congestive heart failure, the starting dose is usually 250 to 375 mg once daily in the morning (5 mg/kg). if, after an initial response, the patient fails to continue to lose edema fluid, do not increase the dose but allow for kidney recovery by skipping medication for a day. acetazolamide yields best diuretic results when given on alternate days, or for two days alternating with a day of rest. failures in therapy may be due to overdosage or too frequent dosage. the use of acetazolamide does not eliminate the need for other therapy such as digitalis, bed rest, and salt restriction. drug induced edema recommended dosage is 250 to 375 mg of acetazolamide once a day for one or two days, alternating with a day of rest. note the dosage recommendations for glaucoma and epilepsy differ considerably from those for congestive heart failure, since the first two conditions are not dependent upon carbonic anhydrase inhibition in the kidney which requires intermittent dosage if it is to recover from inhibitory effect of the therapeutic agent. parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

Contraindications:

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 is 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:

Adverse reactions adverse reactions, occurring most often early in therapy, include paresthesias, particularly a "tingling" feeling in the extremities, hearing dysfunction or tinnitus, loss of appetite, taste alteration and gastrointestinal disturbances such as nausea, vomiting and diarrhea; polyuria, and occasional instances of drowsiness and confusion. metabolic acidosis and electrolyte imbalance may occur. transient myopia has been reported. this condition invariably subsides upon diminution or discontinuance of the medication. other occasional adverse reactions include urticaria, melena, hematuria, glycosuria, hepatic insufficiency, flaccid paralysis, photosensitivity and convulsions. also see precautions: information for patients for possible reactions common to sulfonamide derivatives. fatalities have occurred although rarely, due to severe reactions to sulfonamides including stevens-johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplast
ic anemia and other blood dyscrasias (see warnings ).

Pediatric Use:

Pediatric use the safety and effectiveness of acetazolamide in children have not been established.

Overdosage:

Overdosage no data are available regarding acetazolamide overdosage in humans as no cases of acute poisoning with this drug have been reported. animal data suggest that acetazolamide is remarkably nontoxic. no specific antidote is known. treatment should be symptomatic and supportive. electrolyte imbalance, development of an acidotic state, and central nervous 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 may be dialyzable. this may be particularly important in the management of acetazolamide overdosage when complicated by the presence of renal failure.

Description:

Description acetazolamide, an inhibitor of the enzyme carbonic anhydrase, 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-2yl)-acetamide and has the following structural formula: acetazolamide is available for intravenous use, and is supplied as a sterile powder requiring reconstitution. each vial contains acetazolamide sodium equivalent to 500 mg of acetazolamide. the bulk solution is adjusted to ph 9.6 using sodium hydroxide and, if necessary, hydrochloric acid prior to lyophilization. figure01

Clinical Pharmacology:

Clinical pharmacology acetazolamide is a potent carbonic anhydrase inhibitor, effective in the control of fluid secretion (e.g., some types of glaucoma), in the treatment of certain convulsive disorders (e.g., epilepsy) and in the promotion of diuresis in instances of abnormal fluid retention (e.g., cardiac edema). acetazolamide is not a mercurial diuretic. rather, it is a non-bacteriostatic sulfonamide possessing a chemical structure and pharmacological activity distinctly different from the bacteriostatic sulfonamides. acetazolamide is an enzyme inhibitor that acts specifically on carbonic anhydrase, the enzyme that catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. in the eye, this inhibitory action of acetazolamide decreases the secretion of aqueous humor and results in a drop in intraocular pressure, a reaction considered desirable in cases of glaucoma and even in certain non-glaucomatous conditions. evidence seems to
indicate that acetazolamide has utility as an adjuvant in treatment of certain dysfunctions of the central nervous system (e.g., epilepsy). inhibition of carbonic anhydrase in this area appears to retard abnormal, paroxysmal, excessive discharge from central nervous system neurons. the diuretic effect of acetazolamide is due to its action in the kidney on the reversible reaction involving hydration of carbon dioxide and dehydration of carbonic acid. the result is renal loss of hco 3 ion, which carries out sodium, water, and potassium. alkalinization of the urine and promotion of diuresis are thus affected. alteration in ammonia metabolism occurs due to increased reabsorption of ammonia by the renal tubules as a result of urinary alkalinization.

Carcinogenesis and Mutagenesis and Impairment of Fertility:

Carcinogenesis, mutagenesis, impairment of fertility long-term studies in animals to evaluate the carcinogenic potential of acetazolamide have not been conducted. in a bacterial mutagenicity assay, acetazolamide was not mutagenic when evaluated with and without metabolic activation. the drug had no effect on fertility when administered in the diet to male and female rats at a daily intake of up to 4 times the recommended human dose of 1000 mg in a 50 kg individual.

How Supplied:

How supplied ndc acetazolamide for injection, usp (lyophilized) powder packaging 68382-076-10 500 mg per vial 1 single-dose vial individually packed in a carton storage: store drug product at 20° to 25°c (68° to 77°f) [see usp controlled room temperature]. reconstituted solution should be stored in refrigerator at 2° to 8°c (36° to 46°f). use within 12 hours of reconstitution. contains no preservative. discard unused portion. call your doctor for medical advice about side effects. you may report side effects to fda at 1-800-fda-1088. this product's label may have been updated. for current full prescribing information, please visit www.zydususa.com

Information for Patients:

Information for patients adverse reactions common to all sulfonamide derivatives may occur: anaphylaxis, fever, rash (including erythema multiforme, stevens-johnson syndrome, toxic epidermal necrolysis), crystalluria, renal calculus, bone marrow depression, thrombocytopenic purpura, hemolytic anemia, leukopenia, pancytopenia and agranulocytosis. precaution is advised for early detection of such reactions and the drug should be discontinued and appropriate therapy instituted. in patients with pulmonary obstruction or emphysema where alveolar ventilation may be impaired, acetazolamide which may precipitate or aggravate acidosis, should be used with caution. caution is advised for patients receiving concomitant high-dose aspirin and acetazolamide, as anorexia, tachypnea, lethargy, coma and death have been reported (see warnings ).

Package Label Principal Display Panel:

Package label.principal display panel container label ndc 68382-076-10 acetazolamide for injection usp 500 mg* per vial for intravenous use 1 single-dose vial zydus pharmaceuticals rx only carton label ndc 68382-076-10 acetazolamide for injection usp 500 mg* per vial for intravenous use 1 single-dose vial zydus pharmaceuticals rx only figure02 figure03


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