acetazolamide

Class




  • Antiepileptic drug (AED), carbonic anhydrase inhibitor




Acetazolamide


Commonly Prescribed for


(FDA approved in bold)



  • Adjunctive treatment for centrencephalic epilepsies (petit mal, unlocalized)
  • Acute mountain sickness
  • Edema due to congestive heart failure or medication
  • Glaucoma
  • Idiopathic intracranial hypertension (IIH) (pseudotumor cerebrii)
  • Episodic ataxias type 1 and 2
  • Hemiplegic migraine
  • Marfan syndrome
  • Sleep apnea



Acetazolamide


How the Drug Works



  • Blocks the carbonic anhydrase enzyme, which is responsible for converting CO2 and H2O to bicarbonate. This increases excretion of sodium, potassium, bicarbonate and water, producing alkaline diuresis. In epilepsy, decreases excessive neuronal discharge in CNS due either to inhibition of carbonic anhydrase or slight degree of acidosis. It also reduces production of CSF and aqueous humor



Acetazolamide


How Long Until It Works



  • Seizures – by 2–3 weeks
  • IIH – maximum benefit in 4–6 weeks



Acetazolamide


If It Works



  • Seizures – goal is the remission of seizures. Continue as long as effective and well-tolerated. Consider tapering and slowly stopping after 2 years seizure-free, depending on the type of epilepsy
  • IIH – monitor visual fields and papilledema and symptoms such as visual obscurations and headache



Acetazolamide


If It Doesn’t Work


Increase to highest tolerated dose



  • Seizures – consider changing to another agent, adding a second agent or referral for epilepsy surgery evaluation. When adding a second agent keep in mind the drug interactions that can occur
  • IIH – eliminate symptomatic causes such as drugs or toxins, encourage weight loss if patient is obese, consider loop diuretics or topiramate. Lumbar puncture often provides short-term relief of symptoms. For visual loss, optic nerve defenestration or CSF shunting (lumboperitoneal or ventriculoperitoneal) may be needed



Acetazolamide


Best Augmenting Combos for Partial Response or Treatment-Resistance



  • Epilepsy – acetazolamide itself is usually an augmenting agent. Relatively few interactions with other AEDs. Topiramate and zonisamide have similar mechanisms of action, so acetazolamide is not usually combined with these agents
  • IIH – furosemide and topiramate may be helpful. Combine with caution due to risk of kidney stone formation



Acetazolamide


Tests



  • Obtain a CBC when starting drug and during therapy. Check bicarbonate, potassium, and sodium levels if symptoms of metabolic acidosis develop



Adverse Effects (AEs)




Acetazolamide


How Drug Causes AEs



  • Related to carbonic anhydrase inhibition, which can cause metabolic acidosis and electrolyte imbalances



Acetazolamide


Notable AEs



  • Paresthesias, tinnitus, anorexia, nausea/vomiting, diarrhea, taste alteration, myopia (transient), renal calculi, and photosensitivity



Acetazolamide


Life-Threatening or Dangerous AEs



  • Blood dyscrasias such as agranulocytosis, hemolytic anemia, leukopenia, thrombocytopenia. Hypokalemia. Rash including Stevens Johnson syndrome



Acetazolamide


Weight Gain



  • Unusual



Acetazolamide


Sedation



  • Not unusual

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Feb 16, 2017 | Posted by in PHARMACY | Comments Off on acetazolamide

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