Hypothyroidism: Replacement or supplemental therapy in congenital or acquired hypothyroidism of any etiology.
Pituitary thyrotropin-stimulating hormone suppression: An adjunct to surgery and radioiodine therapy in the management of thyrotropin-dependent well-differentiated thyroid cancer.
Should not be used for the treatment of obesity or for weight loss: Thyroid supplements are ineffective and potentially toxic when used for the treatment of obesity or for weight reduction, especially in euthyroid patients. High doses may produce serious or even life-threatening toxic effects, particularly when used with some anorectic drugs (eg, sympathomimetic amines).<2021/6/11>
#仿單變更2021
藥理
Thyroid Product
藥動學
Onset of action: 3-5 days; peak therapeutic effect may require 4-6 weeks
Absorption: Erratic (40%-80% [per manufacturer]); reported bioavailability in fasting state is 79%-81%. Absorption may be decreased by age and specific foods and drugs.
Protein binding: >99% bound to plasma proteins including thyroxine-binding globulin, thyroxine-binding prealbumin, and albumin.
Metabolism: Hepatic to triiodothyronine (T3; active); ~80% thyroxine (T4) deiodinated in kidney and periphery; glucuronidation/conjugation also occurs; undergoes enterohepatic recirculation
Excretion: Urine (major route, decreases with age), feces
禁忌症
Uncorrected adrenal insufficiency; hypersensitivity to glycerol; acute myocardial infarction, acute myocarditis, or acute pancarditis <2021/6/11>
懷孕分類
Levothyroxine is the preferred treatment of maternal hypothyroidism; other agents should not be used in pregnant females. Close monitoring of pregnant patients is recommended.
哺乳分類
Levothyroxine is present in breast milk. Should consider risk and benefit.
副作用
Hyperthyroidism due to therapeutic overdosage: Cardiac arrhythmia, Flushing, Tachycardia, Anxiety, Skin rash, Goiter, Weight loss, Abdominal cramps, Diarrhea, Vomiting, Reduced fertility, Dyspnea, Fever, Decrease bone mineral density
劑量和給藥方法
Hypothyroidism: Dose is individualized according to clinical response and serum thyroid stimulating hormone (TSH) and/or free T4 concentrations. Average dose is ~1.6 mcg/kg/day; range of required doses is wide and varies from 50 to >200 mcg/day.
TSH suppression: Initial 1.6-2 mcg/kg/day immediately postsurgery; adjust dose as needed in 6 weeks based on TSH suppression goals.
Elderly: Use with caution, start with lower initial dose and increase dose slowly; suppressed TSH levels may increase risk of atrial fibrillation and mortality secondary to cardiovascular disease. Monitor for signs/symptoms of angina.<2021/6/11>
小兒調整劑量
Doses should be adjusted based on clinical response and laboratory parameters; on a weight basis, dosing is higher in infants and children than adults due to the higher metabolic clearance.
Hypothyroidism: 1 to 3 months: 10-15 mcg/kg/dose QD; in severe cases (serum T4 <5 mcg/dL), initiating at higher doses (12-17 mcg/kg/dose) may be necessary >3 to 6 months: 8-10 mcg/kg/dose QD >6 to 12 months: 6-8 mcg/kg/dose QD 1 to 5 years: 5-6 mcg/kg/dose QD 6 to 12 years: 4-5 mcg/kg/dose QD >12 years: 2-3 mcg/kg/dose QD
TSH suppresion: Highly individualized; doses >2 mcg/kg/day may be needed to suppress TSH to <0.1 mU/L in high-risk tumors; for intermediate-risk tumors, initial TSH suppression to 0.1-0.5 mU/L is recommended; for low-risk tumors, TSH may be maintained at 0.5-1 mU/L
腎功能調整劑量
No dosage adjustment necessary (expert opinion).
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling