ACETAZOLAMIDE Uses, Mechanism of Action, Dosing, and Adverse Effects
ACETAZOLAMIDE is a medication used for the prevention or treatment of hyperkalemic periodic paralysis (HYPP) in horses, caused by a genetic mutation. It works as a noncompetitive, reversible inhibitor of carbonic anhydrase, affecting ion levels and insulin secretion. The dosing, available dosage forms, and potential adverse effects like GI upset, CNS effects, hematologic issues, renal effects, and hypersensitivity reactions are discussed in detail.
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Presentation Transcript
ACETAZOLAMIDE Erin Panizza, PharmD Candidate Rood and Riddle Veterinary Pharmacy May 2024
USES Prevention or treatment of HYPP (extra-label) HYPP: hyperkalemic periodic paralysis Muscular disease caused by inherited (dominant) genetic mutation Only one copy of the mutation is needed to affect the horse Affects both males and females DNA test for diagnosis: hair sample with the root attached
HYPP Unpredictable episodesof muscle tremors, twitching, and weakness caused by closed sodium ion channels and high potassium levels in the blood Homozygous horses are usually more severely affected than heterozygous horses Typically affects quarter horses AQHA will no longer register a foal that tests H/H for the gene Wood JS. HYPP and the Impressive line of American Quarter Horses.
MECHANISM OF ACTION Noncompetitive, reversible inhibitor of the enzyme carbonic anhydrase Reduces formation of hydrogen and bicarbonate ions Causes decreased resorption of bicarb and sodium Increases renal tubular secretion of sodium, potassium, and bicarbonate within the kidney Reduces availability of ions for active transport into body secretions Stabilizes blood sugar and potassium levels by stimulating the excretion of insulin in the body
DOSING Plumb s: 2.2 4.4 mg/kg PO twice daily R&R: 2-4 mg/kg PO q 8-12 hours
AVAILABLE DOSAGE FORMS Tablets 125, 250 mg Capsules (Extended-Release) 500 mg Injection 500 mg Powder jar 30, 60, or 100 scoop 1, 2, or 2.5 g per scoop Suspension 120, 240, or 480 mL 250 mg/mL
ADVERSE EFFECTS GI upset: nausea, vomiting, diarrhea, anorexia CNS effects: sedation, depression, weakness, excitement, paresthesia Hematologic effects: bone marrow depression Renal effects: crystalluria, dysuria, renal colic, polyuria, hypokalemia, hyperchloremia, hyperglycemia, hyponatremia, hyperuricemia, hepatic insufficiency Dermatologic effects: rash Hypersensitivity reactions: Stevens-Johnson syndrome and toxic epidermal necrolysis Other: acidosis and mild tremors
OTHER CONSIDERATIONS The ARCI (Association of Racing Commissioners International) has designated this drug as a class 4 substance Class 4: Drugs in this category comprise primarily therapeutic medications routinely used in racehorses. These may influence performance, but generally have a more limited ability to do so. Penalty Class C: Antihistamines that do not have a significant CNS depressant effect.
REFERENCES ASSOCIATION OF RACING COMMISSIONERS INTERNATIONAL. Uniform- classification-guidelines-version-17.0.pdf. 2023. Accessed May 26, 2024. https://www.arci.com/docs/Uniform-Classification-Guidelines-Version-17.0.pdf Plumb s Veterinary Drug Handbook Rood & Riddle 2023-2024 Drug Formulary UpToDate Lexidrug Wood JS. Hypp and the impressive line of American Quarter Horses: The facts. TSLN.com. May 22, 2012. Accessed May 26, 2024. https://www.tsln.com/news/hypp-and-the-impressive-line-of-american-quarter- horses-the-facts/ Young A. Hyperkalemic periodic paralysis (HYPP). School of Veterinary Medicine. August 1, 2023. Accessed May 26, 2024. https://ceh.vetmed.ucdavis.edu/health- topics/hyperkalemic-periodic-paralysis-hypp
