单词 | acetazolamide |
释义 | acetazolamideacetazolamide(əˌsɛtəˈzɒləˌmaɪd; əˌsiːtə-; -ˈzəʊlə-)acetazolamideacetazolamide[‚as·ə·tə′zäl·ə‚mīd]acetazolamideinhibitor[in-hib´ĭ-tor]acetazolamidePharmacologic class: Carbonic anhydrase inhibitor Therapeutic class: Diuretic, antiglaucoma drug, anticonvulsant, altitude agent, urinary alkalinizer Pregnancy risk category C ActionInhibits carbonic anhydrase in kidney, decreasing water reabsorption and increasing excretion of sodium, potassium, and bicarbonate. Lowers intraocular pressure by decreasing aqueous humor production. May raise seizure threshold by reducing carbonic anhydrase in CNS, thereby decreasing neuronal conduction. AvailabilityCapsules (sustained-release): 500 mg Injection: 500 mg/vial Tablets: 125 mg, 250 mg Indications and dosages➣ Open-angle (chronic simple) glaucoma (given with miotics) Adults: 250 mg P.O. one to four times daily, or 500-mg sustained-release capsule P.O. once or twice daily. Don't exceed total daily dosage of 1 g. ➣ Preoperative treatment of closed-angle (secondary) glaucoma Adults: 250 mg P.O. q 4 hours or 250 mg P.O. b.i.d.; in acute cases only, 500 mg P.O. followed by 125 to 250 mg P.O. q 4 hours. For rapid relief of increased intraocular pressure, 500 mg I.V., repeated in 2 to 4 hours; then 125 to 250 mg P.O. q 4 to 6 hours. Children: 10 to 15 mg/kg/day P.O. in divided doses q 6 to 8 hours, or 5 to 10 mg/kg I.V. q 6 hours ➣ Seizure disorder (given with other anticonvulsants) Adults and children: 250 mg P.O. daily when given with another anticonvulsant, or 8 to 30 mg/kg daily P.O. in one to four divided doses. Usual dosage range is 375 mg to 1 g daily. ➣ Drug-induced edema or edema secondary to heart failure Adults: Initially, 250 to 375 mg P.O. daily. If diuresis fails, give dose on alternate days, or give for 2 days alternating with day of rest. Children: 5 mg/kg P.O. daily, or 150 mg/m2 P.O. or I.V. once daily in morning ➣ Acute high-altitude (mountain) sickness Adults: 500 mg to 1 g P.O. daily in divided doses, or sustained-release capsule q 12 to 24 hours. Dosing should begin 24 to 48 hours before ascent and continue during ascent and for 48 hours after reaching desired altitude. For rapid ascent, 1-g P.O. dose is recommended. Dosage adjustment• Mild renal failure Off-label uses• Acute pancreatitis • Alkalosis after open-heart surgery • Hereditary ataxia • Peptic ulcer • Periodic paralysis • Renal calculi • Phenobarbital or lithium overdose • Hydrocephalus in infants Contraindications• Hypersensitivity to drug or sulfonamides • Adrenocortical insufficiency • Closed-angle glaucoma • Severe pulmonary obstruction • Severe renal disease, hypokalemia, hyponatremia • Hepatic disease PrecautionsUse cautiously in: • respiratory, renal, or hepatic disease; diabetes mellitus, hypercalcemia, gout, adrenocortical insufficiency • pregnant or breastfeeding patients. AdministrationSee Before giving, ask if patient is pregnant. Drug may cause fetal toxicity. • Direct I.V. administration is preferred. When giving by direct I.V. route, reconstitute 500-mg vial with more than 5 ml of sterile water for injection; administer over 1 minute. • When giving drug intermittently by I.V. infusion, further dilute with normal saline solution or dextrose solution and infuse over 4 to 8 hours. • Be aware that I.M. administration is painful because solution is alkaline. • If necessary, crush tablets and mix in nonsweet, nonalcoholic syrup or non-glycerin solution. ![]() Adverse reactionsCNS: weakness, nervousness, irritability, drowsiness, confusion, dizziness, depression, tremor, headache, paresthesia, flaccid paralysis, seizures EENT: transient myopia, tinnitus, hearing dysfunction, sensation of lump in throat GI: nausea, vomiting, diarrhea, constipation, melena, abdominal distention, dry mouth, anorexia GU: dysuria, hematuria, glycosuria, polyuria, crystalluria, renal colic, renal calculi, uremia, sulfonamide-like renal lesions, renal failure Hematologic: thrombocytopenia, leukopenia, agranulocytosis, hemolytic anemia, thrombocytopenic purpura, pancytopenia, bone marrow depression with aplastic anemia Hepatic: hepatic insufficiency Metabolic: hypokalemia, hyperglycemia and glycosuria, hyperuricemia and gout, metabolic acidosis, hyperchloremic acidosis Respiratory: hyperpnea Skin: rash, pruritus, urticaria, photosensitivity, hirsutism, cyanosis Other: altered taste and smell, weight loss, fever, excessive thirst, pain at I.M. injection site, hypersensitivity reaction, Stevens-Johnson syndrome InteractionsDrug-drug. Amphetamines, procainamide, quinidine, tricyclic antidepressants: decreased excretion and enhanced or prolonged effect of these drugs, leading to toxicity Amphotericin B, corticosteroids, corticotrophin, other diuretics: increased risk of hypokalemia Lithium, phenobarbital, salicylates: increased excretion of these drugs, possibly reducing their efficacy Methenamine compounds: inactivation of these drugs Phenytoin, primidone: severe osteomalacia Salicylates: increased risk of salicylate toxicity Drug-diagnostic tests. Ammonia, bilirubin, calcium, chloride, glucose, uric acid: increased levels Thyroid iodine uptake: decreased in patients with hyperthyroidism or normal thyroid function Urinary protein (with some reagents): false-positive result Drug-behaviors. Sun exposure: increased risk of photosensitivity Patient monitoringSee Evaluate for signs and symptoms of sulfonamide sensitivity; drug can cause fatal hypersensitivity. See Monitor laboratory test results for hematologic changes; blood glucose, potassium, bicarbonate, and chloride levels; and liver and kidney function changes. • Observe for signs and symptoms of bleeding tendency. • Monitor fluid intake and output. Patient teaching• Advise patient to take drug with food if GI upset occurs. • Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness. • Tell patient to eat potassium-rich foods (such as seafood, bananas, and oranges) if taking drug long term or receiving other potassium-depleting drugs. • Advise patient to avoid activities that can cause injury. Advise him to use soft toothbrush and electric razor to avoid gum and skin injury. • Tell patient to report significant numbness or tingling. • Inform patient that he'll undergo regular blood testing during therapy. • As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above. a·cet·a·zol·a·mide(as'ĕ-tă-zol'ă-mīd),acetazolamide(ăs′ĭ-tə-zō′lə-mīd′)AcetazolamideA heterocyclic sulphonamide used to manage respiratory acidosis by inhibiting renal carbonic anhydrase, which increases renal excretion of Na+, K+, and bicarbonate, and reduces ammonia excretion. Acetazolamide is also used to reduce fluid retention in congestive heart failure, control secondary glaucoma and preoperatively in acute angle-closure glaucoma, and may be of use in seizures, especially absence seizures.Effect Reduced serum pH; increased urine pH acetazolamideDazamide®, Diamox® Therapeutics A heterocyclic sulfonamide used to manage respiratory acidosis by inhibiting renal carbonic anhydrase, which ↑ renal excretion of Na+, K+, and bicarbonate, and ↓ ammonia excretion; acetazolamide is also used to ↓ fluid retention in CHF, control 2º glaucoma and preoperatively in acute angle-closure glaucoma, epilepsy Effect ↓ Serum pH; ↑ urine pH Therapeutic range 10–15 µg/mL Toxic range ≥ 20 µg/mLacetazolamideA drug that inhibits the enzyme carbonic anhydrase in the kidney tubules, thus acting as a diuretic. In the eye it acts similarly to reduce the rate of secretion of aqueous humour and is useful in the treatment of GLAUCOMA when the intraocular pressure rise cannot be controlled with eye drops alone. The drug is also used in the treatment of EPILEPSY. A brand name is Diamox.carbonic anhydrase inhibitorsa·cet·a·zol·a·mide(as'ĕ-tă-zol'ă-mīd) |
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