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Acetazolamide IV E (ah -set-ah -Z O E- la- my d) CLASSIFICATION(S): Anticonvulsant, carbonic anhydrase inhibitor PREGNANCY CATEGORY: C WRx: Apo-Acetazolamide. Acetazolamide sodium Rx: Acetazolamide sodium SEE ALSO ANTICONVULSANTS AND DIURETICS, CHAPTER 2. USES (1) Adjunct in the treatment of edema due to CHF or drug-induced edema. (2) Absence (petit mal), especially in children) and unlocalized seizures. (3) Open-angle, secondary, or acute-angle closure glaucoma when delay of surgery is desired to lower IOP. (4) Prophylaxis or treatment of acute mountain sickness in climbers attempting a rapid ascent or in those susceptible to mountain sickness even with gradual ascent. ACTION/KINETICS Action Sulfonamide derivative possessing carbonic anhydrase inhibitor activity. Anticonvulsant effects may be due to (1) inhibition of carbonic anhydrase in the CNS, which increases carbon dioxide tension resulting in a decrease in neuronal conduction, and (2) systemic acidosis. As a diuretic, the drug inhibits carbonic anhydrase in the kidney, which decreases formation of bicarbonate and hydrogen ions from carbon dioxide, thus reducing the availability of these ions for active transport. Use as a diuretic is limited because the drug promotes metabolic acidosis, which inhibits diuretic activity. This may be partially circumvented by giving acetazolamide on alternate days. Also reduces intraocular pressure. Pharmacokinetics Absorbed from the GI tract and widely distributed throughout the body, including the CNS. Tablets: Onset, 60–90 Bold Italic = life threatening side effect min; peak: 1–4 hr; duration: 8–12 hr. Sustained-release capsules: Onset, 2 hr; peak: 3–6 hr; duration: 18–24 hr. Injection (IV): Onset, 2 min; peak: 15 min; duration: 4–5 hr. Eliminated mainly unchanged through the kidneys. CONTRAINDICATIONS Low serum sodium and potassium levels. Renal and hepatic dysfunction. Hyperchloremic acidosis, adrenal insufficiency, suprarenal gland failure, hypersensitivity to thiazide diuretics, cirrhosis. Chronic use in noncongestive angleclosure glaucoma. SPECIAL CONCERNS • Use with caution in the presence of mild acidosis, advanced pulmonary disease, and during lactation. • Increasing the dose does not increase effectiveness but may increase the risk of drowsiness or paresthesia. • Safety and efficacy not established in children. SIDE EFFECTS Most Common Anorexia, dizziness, lightheadedness, blurred vision, pruritus, GI upset, headache, weakness. GI: Anorexia, GI upset, N&V, melena, constipation, alteration in taste, diarrhea. GU: Hematuria, glycosuria, urinary frequency, renal colic/calculi, crystalluria, polyuria, phosphaturia, decreased/ absent libido, impotence. CNS: Seizures, weakness, malaise, lightheadedness, fatigue, nervousness, drowsiness, depression, dizziness, disorientation, confusion, ataxia, tremor, headache, tinnitus, flaccid paralysis, lassitude, paresthesia of the extremities. Hematologic: Bone marrow depression, thrombocytopenic purpura, thrombocytopenia, hemolytic anemia, leukopenia, pancytopenia, agranulocytosis. Dermatologic: Pruritus, urticaria, skin rashes, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, photosensitivity. Miscellaneous: Weight loss, weakness, fever, acidosis, electrolyte imbalance, transient myopia, blurred vision, hepatic insufficiency. NOTE: Side effects similar to those produced by sulfonamides may also occur. ■ = black box warning W = Available in Canada OD OVERDOSE MANAGEMENT Symptoms: Drowsiness, anorexia, N&V, dizziness, ataxia, tremor, paresthesias, tinnitus. Treatment: Emesis or gastric lavage. Hyperchloremic acidosis may respond to bicarbonate. Administration of potassium may also be necessary. Observe carefully and give supportive treatment. DRUG INTERACTIONS SEE ALSO DIURETICS Amphetamine / 앖 Amphetamine effect by 앖 renal tubular reabsorption Cyclosporine / 앖 Cyclosporine levels 씮 possible nephrotoxicity and neurotoxicity Diflunisal / Significant 앗 in IOP with 앖 side effects Ephedrine / 앖 Ephedrine effect R/T 앖 renal tubular reabsorption Lithium carbonate / 앗 Lithium effect R/T 앖 renal excretion Methotrexate / 앗 Methotrexate effect R/T 앖 renal excretion Primidone / 앗 Primidone effect R/T 앗 GI absorption Pseudoephedrine / 앖 Pseudoephedrine effect by 앖 renal tubular reabsorption Quinidine / 앖 Quinidine effect by 앖 renal tubular reabsorption Salicylates / Accumulation and toxicity of acetazolamide (including CNS depression and metabolic acidosis). Also, acidosis due to 앖 CNS penetration of salicylates HOW SUPPLIED Acetazolamide: Capsules, Extended-Release: 500 mg; Tablets: 125 mg, 250 mg. Acetazolamide sodium: Powder for Injection: 500 mg. DOSAGE • CAPSULES, EXTENDED-RELEASE; IV; TABLETS Diuresis in CHF. Adults, initial: 250–375 mg (5 mg/kg) once daily in the morning. If the client stops losing edema fluid after an initial response, do not increase doses; rather, skip medication for a day to allow the kidney to recover. The best diuretic effect occurs when the drug is given on alternate days or for 2 days alternating with a day of rest. Drug-induced edema. Adults: 250–375 mg once daily for 1 or 2 days. Most effective if given every C = see color insert H = Herbal other day or for 2 days followed by a day of rest. Children: 5 mg/kg/dose PO or IV once daily in the morning. Absence and unlocalized seizures. Adults/children: 8–30 mg/kg/day in divided doses. Optimum daily dosage: 375–1,000 mg (doses higher than 1,000 mg do not increase therapeutic effect). Adjunct to other anticonvulsants. Initial: 250 mg/day; dose can be increased up to 1,000 mg/day in divided doses if necessary. Glaucoma, simple open-angle. Adults: 250–1,000 mg/day in divided doses. Doses greater than 1,000 mg/day do not increase the effect. Glaucoma, secondary or acute congestive (closed-angle). Adults, short-term therapy: 250 mg q 4 hr or 250 mg twice a day. Adults, acute therapy: 500 mg followed by 125–250 mg q 4 hr using tablets. For extended-release capsules, give 500 mg twice a day in the morning and evening. IV therapy may be used for rapid decrease in intraocular pressure. Pediatric: 5–10 mg/kg/dose IM or IV q 6 hr or 10–15 mg/kg/day in divided doses q 6–8 hr using tablets. Acute mountain sickness. Adults: 500 mg 1–2 times per day of tablets or extended-release capsules. During rapid ascent, 1,000 mg/day is recommended. NURSING CONSIDERATIONS E Do not confuse acetazolamide with acetohexamide (oral antidiabetic). ADMINISTRATION/STORAGE 1. Changeover from other anticonvulsant therapy should be gradual. 2. Acetazolamide tablets may be crushed and suspended in a cherry, chocolate, raspberry, or other sweet syrup. Do not use vehicles containing glycerin or alcohol. 3. Tolerance after prolonged use may necessitate dosage increase. 4. Do not administer the extended-release dosage form as an anticonvulsant; used only for glaucoma and acute mountain sickness. 5. With mountain sickness prophylaxis, initiate dosage 1–2 days before ascent and continue for at least 2 days while at high altitudes. IV = Intravenous E = sound alike drug 6. Due to possible differences in bioavailability, do not interchange brands. IV 7. IV administration is preferred; IM administration is painful due to alkalinity of solution. 8. For direct IV use, administer over at least 1 min. For intermittent IV use, further dilute in dextrose or saline solution and infuse over 4–8 hr. Reconstitute each 500-mg vial with at least 5 mL of sterile water for injection. 9. Refrigerate reconstituted solution at 28° C (36–46° F). Use within 12 hr; contains no preservative. ASSESSMENT 1. Note reasons for therapy, onset/ characteristics of symptoms. 2. Review I&O, CBC, electrolytes, uric acid, and glucose. Assess for liver/renal dysfunction. Metabolic acidosis and electrolyte imbalance may occur. 3. List drugs prescribed to ensure no interactions. 4. With glaucoma, note baseline ophthalmic exam and intraocular pressures; assess for visual effects. 5. Perform CV/pulmonary assessment with CHF history. Obtain VS and weight. CLIENT/FAMILY TEACHING 1. Taking drug with food may decrease GI upset/irritation. 2. Assess drug effects before undertaking tasks that require mental alertness; may cause drowsiness. Bold Italic = life threatening side effect 3. Increases voiding frequency; take early to avoid interrupting sleep. 4. Use only as directed. If prescribed every other day, record to ensure adherence. 5. Increase fluids (2–3 L/day) to prevent urine crystals/stone formation. 6. May increase blood glucose levels. Monitor FS and report increases; diabetes agent may need adjustment. Avoid high-sodium foods. 7. Report if nausea, dizziness, rapid weight gain, muscle weakness, cramps, or any changes in the color/consistency of stools occur. 8. Practice reliable contraception; may cause fetal defects. 9. To avoid mountain sickness, gradual ascent should occur. If rapid ascent is undertaken and acetazolamide tablets are used, such use does not obviate the need for prompt descent if severe forms of high altitude sickness occur, i.e., high altitude pulmonary edema or high altitude cerebral edema. 10. Avoid excess exposure to sunlight to prevent photosensitivity reaction. 11. Keep all F/U to assess response, labs (may need potassium replacement), and for adverse SE. OUTCOMES/EVALUATE • 앗 Seizure activity • 앗 Intraocular pressure • 앗 CHF-associated edema • Prevention of mountain sickness ■ = black box warning W = Available in Canada