Description

Simple

A medication used to treat seizures, glaucoma, swelling from water retention, and heart failure.

Clinical

A carbonic anhydrase inhibitor used to treat edema from heart failure or medications, certain types of epilepsy, and glaucoma.

Overview

One of the carbonic anhydrase inhibitors that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)

Pharmacology

Indication

For adjunctive treatment of: edema due to congestive heart failure; drug-induced edema; centrencephalic epilepsies; chronic simple (open-angle) glaucoma

Pharmacodynamic

Acetazolamide is a potent carbonic anhydrase inhibitor, effective in the control of fluid secretion, in the treatment of certain convulsive disorders and in the promotion of diuresis in instances of abnormal fluid retention. Acetazolamide is not a mercurial diuretic. Rather, it is a nonbacteriostati... Read more

Mechanism of action

The anticonvulsant activity of Acetazolamide may depend on a direct inhibition of carbonic anhydrase in the CNS, which decreases carbon dioxide tension in the pulmonary alveoli, thus increasing arterial oxygen tension. The diuretic effect depends on the inhibition of carbonic anhydrase, causing a re... Read more

Absorption

Information currently not available.

Protein binding

98%

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

3 to 9 hours

Route of elimination

Information currently not available.

Toxicity

Information currently not available.

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Marked kidney and liver disease or dysfunction
      • Drugbank Id: DBCOND0108029
  • Regions: US
  • Patient Conditions:
      • Name: Suprarenal gland failure
      • Drugbank Id: DBCOND0108030
  • Regions: US
  • Patient Conditions:
      • Name: Hyperchloremia acidosis
      • Drugbank Id: DBCOND0108031
  • Regions: US
  • Patient Conditions:
      • Name: Cirrhosis
      • Drugbank Id: DBCOND0028910
  • Regions: US
  • Patient Conditions:
      • Name: Chronic non-congestive angle-closure glaucoma
      • Drugbank Id: DBCOND0108032
  • Regions: US
  • Patient Conditions:
      • Name: Depressed sodium and/or potassium blood serum levels
      • Drugbank Id: DBCOND0108028

Food Interactions

  • Drink plenty of fluids.
  • Take with food. Take at least 6 hours before bedtime.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The serum concentration of (R)-warfarin can be increased when it is combined with Acetazolamide.
(S)-Warfarin
The serum concentration of (S)-Warfarin can be increased when it is combined with Acetazolamide.
2,4-thiazolidinedione
The therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Acetazolamide.
2,5-Dimethoxy-4-ethylamphetamine
Acetazolamide may decrease the excretion rate of 2,5-Dimethoxy-4-ethylamphetamine which could result in a higher serum level.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when Acetazolamide is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthine
Acetazolamide may increase the excretion rate of 3-isobutyl-1-methyl-7H-xanthine which could result in a lower serum level and potentially a reduction in efficacy.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when Acetazolamide is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarin
The metabolism of 4-hydroxycoumarin can be decreased when combined with Acetazolamide.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Acetazolamide is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Acetazolamide is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanine
Acetazolamide may increase the excretion rate of 6-O-benzylguanine which could result in a lower serum level and potentially a reduction in efficacy.
7-Deazaguanine
Acetazolamide may increase the excretion rate of 7-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Acetazolamide is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Acetazolamide is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
7,9-Dimethylguanine
Acetazolamide may increase the excretion rate of 7,9-Dimethylguanine which could result in a lower serum level and potentially a reduction in efficacy.
8-azaguanine
Acetazolamide may increase the excretion rate of 8-azaguanine which could result in a lower serum level and potentially a reduction in efficacy.
8-chlorotheophylline
Acetazolamide may increase the excretion rate of 8-chlorotheophylline which could result in a lower serum level and potentially a reduction in efficacy.
9-aminocamptothecin
The metabolism of 9-aminocamptothecin can be decreased when combined with Acetazolamide.
9-Deazaguanine
Acetazolamide may increase the excretion rate of 9-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
9-Methylguanine
Acetazolamide may increase the excretion rate of 9-Methylguanine which could result in a lower serum level and potentially a reduction in efficacy.