ACETAZOLAMIDE tablet

United States - English - NLM (National Library of Medicine)

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Active ingredient:
ACETAZOLAMIDE (UNII: O3FX965V0I) (ACETAZOLAMIDE - UNII:O3FX965V0I)
Available from:
Bryant Ranch Prepack
Administration route:
ORAL
Prescription type:
PRESCRIPTION DRUG
Therapeutic indications:
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. Acetazolamide Tablets are also indicated for the prevention or amelioration of symptoms associated with acute mountain sickness  in climbers  attempting  rapid  ascent and in those who are very susceptible to acute mountain sickness despite gradual ascent. 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
Product summary:
NDC: 63629-1195-1 100 Tablets in a BOTTLE
Authorization status:
Abbreviated New Drug Application
Authorization number:
63629-1195-1

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ACETAZOLAMIDE- acetazolamide tablet

Bryant Ranch Prepack

----------

Acetazolamide Tablets USP

Rx only

DESCRIPTION

Acetazolamide, USP an inhibitor of the enzyme carbonic anhydrase, is a white to faintly yellowish white

crystalline odorless powder, very slightly soluble in water, sparingly soluble in boiling water, 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:

Molecular Weight: 222.25

Molecular Formula: C H N O S

Acetazolamide, USP is available as oral tablets containing 125 mg and 250 mg of acetazolamide,

respectively, and the following inactive ingredients: lactose monohydrate, magnesium stearate, maize

starch, povidone, purified water, sodium starch glycolate-type A and talc.

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 nonbacteriostatic 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 nonglaucomatous conditions. Evidence seems to indicate that

acetazolamide has utility as an adjuvant in the 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 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.

Placebo-controlled clinical trials have shown that prophylactic administration of acetazolamide at a

dose of 250 mg every eight to 12 hours (or a 500 mg controlled-release capsule once daily) before and

during rapid ascent to altitude results in fewer and/or less severe symptoms (such as headache, nausea,

shortness of breath, dizziness, drowsiness, and fatigue) of acute mountain sickness (AMS). Pulmonary

function (e.g., minute ventilation, expired vital capacity and peak flow) is greater in the acetazolamide

treated group, both in subjects with AMS and asymptomatic subjects. The acetazolamide treated

climbers also had less difficulty in sleeping.

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. Acetazolamide Tablets are also indicated for the prevention or

amelioration of symptoms associated with acute mountain sickness in climbers attempting rapid ascent

and in those who are very susceptible to acute mountain sickness despite gradual ascent.

CONTRAINDICATIONS

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.

WARNINGS

Fatalities have occurred, although rarely, due to severe reactions to sulfonamides including Stevens-

Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, 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, coma and death have been reported.

PRECAUTIONS

General

Increasing the dose does not increase the diuresis and may increase the incidence of drowsiness and/or

paresthesia. Increasing the dose often results in a decrease in diuresis. Under certain circumstances,

however, very large doses have been given in conjunction with other diuretics in order to secure

diuresis in complete refractory failure.

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.

Gradual ascent is desirable to try to avoid acute mountain sickness. If rapid ascent is undertaken and

acetazolamide tablets are used, it should be noted that such use does not obviate the need for prompt

descent if severe forms of high altitude sickness occur, i.e., high altitude pulmonary edema (HAPE) or

high altitude cerebral edema.

Caution is advised for patients receiving concomitant high-dose aspirin and acetazolamide, as anorexia,

tachypnea, lethargy, coma and death have been reported (see WARNINGS).

Laboratory Tests

To monitor for hematologic reactions common to all sulfonamides, it is recommended that a baseline

CBC and platelet count be obtained on patients prior to initiating acetazolamide tablet therapy and at

regular intervals during therapy. If significant changes occur, early discontinuance and institution of

appropriate therapy are important. Periodic monitoring of serum electrolytes is recommended.

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.

Pregnancy

Teratogenic Effect

Acetazolamide, administered orally or parenterally, has been shown to be teratogenic (defects of the

limbs) in mice, rats, hamsters and rabbits. There are no adequate and well-controlled studies in pregnant

women. Acetazolamide should be used in pregnancy only if the potential benefit justifies the potential

risk to the fetus.

Nursing Mothers

Because of the potential for serious adverse reaction in nursing infants from acetazolamide, a decision

should be made whether to discontinue nursing or to discontinue the drug taking into account the

importance of the drug to the mother.

Pediatric Use

The safety and effectiveness of acetazolamide in pediatric patients has not been established.

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, aplastic anemia and

other blood dyscrasias (see WARNINGS).

To report SUSPECTED ADVERSE REACTIONS, contact Lifestar Pharma LLC at 1-888-995-

4337 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

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.

DOSAGE AND ADMINISTRATION

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 mg or 250 mg every four hours depending on

the individual case. A complementary effect has been noted when acetazolamide has been used in

conjunction with miotics or mydriatics as the case demanded.

Epileps y

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 tablets are

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 tablets yield 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.

Acute Mountain Sickness

Dosage is 500 mg to 1000 mg daily, in divided doses. In circumstances of rapid ascent, such as in

rescue or military operations, the higher dose level of 1000 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.

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 the inhibitory effect

of the therapeutic agent.

HOW SUPPLIED

NDC: 63629-1195-1 100 Tablets in a BOTTLE

Manufactured for:

Lifestar Pharma LLC

1200 MacArthur Blvd.

Mahwah, NJ 07430 USA

Made in India

Revised: March 2020, V-02

Manufactured in India for:

Lifestar Pharma LLC

1200 MacArthur Blvd.

Mahwah, NJ 07430 USA

Product of Poland

Revised: August 2020, P-01

Acetazolamide 250 mg # 100

ACETAZOLAMIDE

acetazolamide tablet

Product Information

Product T ype

HUMAN PRESCRIPTION DRUG

Ite m Code (Source )

NDC:6 36 29 -119 5(NDC:70 756 -721)

Route of Administration

ORAL

Active Ingredient/Active Moiety

Ingredient Name

Basis of Strength

Stre ng th

ACETAZO LAMIDE (UNII: O3FX9 6 5V0 I) (ACETAZOLAMIDE - UNII:O3FX9 6 5V0 I)

ACETAZOLAMIDE

250 mg

Inactive Ingredients

Ingredient Name

Stre ng th

LACTO SE MO NO HYDRATE (UNII: EWQ57Q8 I5X)

MAGNESIUM STEARATE (UNII: 70 0 9 7M6 I30 )

PO VIDO NE K3 0 (UNII: U725QWY32X)

SO DIUM STARCH GLYCO LATE TYPE A PO TATO (UNII: 58 56 J3G2A2)

STARCH, CO RN (UNII: O8 232NY3SJ)

TALC (UNII: 7SEV7J4R1U)

WATER (UNII: 0 59 QF0 KO0 R)

Product Characteristics

Color

WHITE

S core

4 pieces

S hap e

ROUND

S iz e

11mm

Flavor

Imprint Code

LS;721

Contains

Packag ing

Bryant Ranch Prepack

#

Item Code

Package Description

Marketing Start Date

Marketing End Date

1

NDC:6 36 29 -119 5-1

10 0 in 1 BOTTLE; Type 0 : No t a Co mbinatio n Pro duct

12/0 9 /20 20

Marketing Information

Marke ting Cate gory

Application Numbe r or Monograph Citation

Marke ting Start Date

Marke ting End Date

ANDA

ANDA21428 2

11/13/20 20

Labeler -

Bryant Ranch Prepack (171714327)

Registrant -

Bryant Ranch Prepack (171714327)

Establishment

Name

Ad d re s s

ID/FEI

Busine ss Ope rations

Bryant Ranch Prepack

171714327

REPACK(6 36 29 -119 5) , RELABEL(6 36 29 -119 5)

Revised: 12/2020

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