Acetazolamide (extended-release capsule)

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Acetazolamide (extended-release capsule)
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1];

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Overview

Acetazolamide (extended-release capsule) is a carbonic anhydrase inhibitor that is FDA approved for the treatment of chronic primary open-angle glaucoma and secondary glaucoma. Acetazolamide is also indicated for the prevention or amelioration of symptoms associated with acute mountain sickness despite gradual ascent. Common adverse reactions include dizziness and lightheadedness.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Glaucoma
  • Dosing Information
  • 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.
  • In those unusual instances where adequate control is not obtained by the twice-a-day administration of acetazolamide, 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
  • Dosing Information
  • The recommended dosage is 500 mg to 1000 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 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.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of acetazolamide in adult patients.

Non–Guideline-Supported Use

Glaucoma Following Surgery
  • Dosing Information
  • 500 mg PO 1 hour postoperatively[1]
Macular Retinal Edema
  • Dosing Information
  • 500 mg PO qd for 4 weeks[2]
Periodic Ataxia
  • Dosing Information

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

The safety and effectiveness of acetazolamide in pediatric patients below the age of 12 years have not been established. Growth retardation has been reported in children receiving long-term therapy, believed secondary to chronic acidosis.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of acetazolamide in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of acetazolamide in pediatric patients.

Contraindications

  • Chronic non-congestive angle-closure glaucoma
  • 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

  • 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.
  • 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.
  • 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 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.

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of acetazolamide in the drug label.

Postmarketing Experience

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.

Special senses

Hearing disturbances, tinnitus, transient myopia.

Drug Interactions

  • Because of possible additive effects with other carbonic anhydrase inhibitors, concomitant use is not advisable.
  • Drug/laboratory test interactions

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C

Teratogenic effects

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.
Pregnancy Category (AUS): B3 There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Acetazolamide (extended-release capsule) in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Acetazolamide (extended-release capsule) during labor and delivery.

Nursing Mothers

Because of the potential for serious adverse reactions 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. Acetazolamide should only be used by nursing women if the potential benefit justifies the potential risk to the child.

Pediatric Use

The safety and effectiveness of acetazolamide in pediatric patients below the age of 12 years have not been established. Growth retardation has been reported in children receiving long-term therapy, believed secondary to chronic acidosis.

Geriatic Use

Metabolic acidosis, which can be severe, may occur in the elderly with reduced renal function. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant disease or other drug therapy.

Gender

There is no FDA guidance on the use of Acetazolamide (extended-release capsule) with respect to specific gender populations.

Race

There is no FDA guidance on the use of Acetazolamide (extended-release capsule) with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Acetazolamide (extended-release capsule) in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Acetazolamide (extended-release capsule) in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Acetazolamide (extended-release capsule) in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Acetazolamide (extended-release capsule) in patients who are immunocompromised.

Administration and Monitoring

Administration

Oral

Monitoring

Electrolyte Imbalances

Acetazolamide treatment may cause electrolyte imbalances, including hyponatremia and hypokalemia, as well as metabolic acidosis. Therefore, periodic monitoring of serum electrolytes is recommended.

Hematologic Distrubances

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 therapy and at regular intervals during therapy. If significant changes occur, early discontinuance and institution of appropriate therapy are important.

IV Compatibility

There is limited information regarding IV Compatibility of acetazolamide in the drug label.

Overdosage

Acute Overdose

Management

  • 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 may be dialyzable. This may be particularly important in the management of acetazolamide overdosage when complicated by the presence of renal failure.

Pharmacology

Template:Px
Template:Px
Acetazolamide (extended-release capsule)
Systematic (IUPAC) name
N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide
Identifiers
CAS number 59-66-5
ATC code S01EC01
PubChem 1986
DrugBank DB00819
Chemical data
Formula Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox 
Mol. mass 222.245 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability ?
Metabolism None
Half life 2-4 hours
Excretion Urine (90%)
Therapeutic considerations
Pregnancy cat.

B3(AU) C(US)

Legal status

Prescription Only (S4)(AU) ?(CA) POM(UK) [[Prescription drug|Template:Unicode-only]](US)

Routes oral or intravenous

Mechanism of Action

Structure

The chemical name for acetazolamide is N-(5-Sulfamoyl-1,3, 4-thiadiazol-2-yl) acetamide and has the following chemical structure:

This image is provided by the National Library of Medicine.

Pharmacodynamics

  • Acetazolamide provide prolonged action to inhibit aqueous humor secretion for 18 to 24 hours after each dose, whereas tablets act for only eight to 12 hours. The prolonged continuous effect of acetazolamide permits a reduction in dosage frequency.

Pharmacokinetics

  • Plasma concentrations of acetazolamide peak from three to six hours after administration of acetazolamide, compared to one to four hours with tablets. Food does not affect bioavailability of acetazolamide.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of acetazolamide in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of acetazolamide in the drug label.

How Supplied

  • Diamox Sequels (Acetazolamide Extended-Release Capsules) are available as 500 mg:
Orange opaque cap and orange opaque body filled with white to off-white pellets. Imprinted in black ink, DIAMOX 754.
  • Available in bottles of:
100 NDC 51285-754-02
DURAMED PHARMACEUTICALS, INC.
Subsidiary of Barr Pharmaceuticals, Inc.
Pomona, New York 10970
Revised JULY 2008
BR-754

Storage

Store at 20° to 25°C (68° to 77°F).

Images

Drug Images

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Package and Label Display Panel

This image is provided by the National Library of Medicine.
This image is provided by the National Library of Medicine.

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Patient Counseling Information

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

Precautions with Alcohol

Alcohol-acetazolamide interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Diamox Sequels®

Look-Alike Drug Names

  • acetaZOLAMIDE — acetoHEXAMIDE[8]
  • Diamox® — Diabinese®[8]

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. Byrd, S.; Singh, K. (1998). "Medical control of intraocular pressure after cataract surgery". J Cataract Refract Surg. 24 (11): 1493–7. PMID 9818340. Unknown parameter |month= ignored (help)
  2. Whitcup, SM.; Csaky, KG.; Podgor, MJ.; Chew, EY.; Perry, CH.; Nussenblatt, RB. (1996). "A randomized, masked, cross-over trial of acetazolamide for cystoid macular edema in patients with uveitis". Ophthalmology. 103 (7): 1054–62, discussion 1062-3. PMID 8684794. Unknown parameter |month= ignored (help)
  3. Baloh, RW.; Winder, A. (1991). "acetazolamide-responsive vestibulocerebellar syndrome: clinical and oculographic features". Neurology. 41 (3): 429–33. PMID 2006014. Unknown parameter |month= ignored (help)
  4. Friedman, JH.; Hollmann, PA. (1987). "acetazolamide responsive hereditary paroxysmal ataxia". Mov Disord. 2 (1): 67–72. doi:10.1002/mds.870020110. PMID 3332806.
  5. Bouchard, JP.; Roberge, C.; van Gelder, NM.; Barbeau, A. (1984). "Familial periodic ataxia responsive to acetazolamide". Can J Neurol Sci. 11 (4 Suppl): 550–3. PMID 6439406. Unknown parameter |month= ignored (help)
  6. Griggs, RC.; Moxley, RT.; Lafrance, RA.; McQuillen, J. (1978). "Hereditary paroxysmal ataxia: response to acetazolamide". Neurology. 28 (12): 1259–64. PMID 366453. Unknown parameter |month= ignored (help)
  7. "DIAMOX SEQUELS (ACETAZOLAMIDE) CAPSULE, EXTENDED RELEASE [DURAMED PHARMACEUTICALS, INC.]".
  8. 8.0 8.1 "http://www.ismp.org". External link in |title= (help)

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