TRIOSTAT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TRIOSTAT (TRIOSTAT).
TRIOSTAT (liothyronine sodium) is a synthetic form of the thyroid hormone triiodothyronine (T3). It binds to thyroid hormone receptors in the nucleus, altering gene expression and increasing cellular metabolism, oxygen consumption, and heat production.
| Metabolism | Metabolized primarily in the liver via deiodination (type I and II deiodinases) and conjugation (glucuronidation and sulfation). Minor metabolism via deamination and decarboxylation. CYP450 enzymes not significantly involved. |
| Excretion | Renal (40% unchanged, 20% as liothyronine conjugates); fecal (35%) |
| Half-life | 2.5 days (terminal); shortened in hyperthyroidism, prolonged in hypothyroidism |
| Protein binding | >99.7% bound to thyroxine-binding globulin, transthyretin, and albumin |
| Volume of Distribution | 0.2-0.4 L/kg (primarily distributes to liver and kidneys) |
| Bioavailability | Oral: 90-95% (well absorbed); IV: 100% |
| Onset of Action | IV: 2-4 hours (thyroid hormone replacement); Oral: 6-12 hours |
| Duration of Action | IV: 2-3 days; Oral: 1-2 weeks (clinical effects persist beyond serum half-life) |
Adult: 5 mcg/kg IV every 8 hours. Adjust based on clinical response.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No specific guidelines; use with caution in severe hepatic impairment. |
| Pediatric use | Weight-based: 0.5-1 mcg/kg IV every 8-12 hours. |
| Geriatric use | Start at lower end of dosing range, monitor thyroid function closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TRIOSTAT (TRIOSTAT).
| Breastfeeding | Liothyronine is excreted in breast milk in very low amounts. M/P ratio: 0.5-1.0. Considered compatible with breastfeeding; monitor infant thyroid function if mother on high doses. |
| Teratogenic Risk | Pregnancy Category A. No evidence of fetal harm in first trimester; animal studies show no risk. Second and third trimesters: risk of maternal hypothyroidism may affect fetal neurodevelopment; monitor thyroid function. |
| Fetal Monitoring |
■ FDA Black Box Warning
WARNING: In patients with cardiac disease, particularly angina pectoris or myocardial infarction, administration of TRIOSTAT may precipitate cardiac arrhythmias, myocardial ischemia, or infarction. Use with extreme caution.
| Serious Effects |
["Untreated thyrotoxicosis (hyperthyroidism)","Untreated adrenal insufficiency","Hypersensitivity to liothyronine or any component of the formulation","Recent myocardial infarction (relative contraindication unless myxedema coma is life-threatening)"]
| Precautions | ["Cardiac toxicity: Risk of arrhythmias, myocardial infarction, and cardiac arrest, especially in elderly or patients with underlying heart disease.","Thyrotoxic crisis: Overdose may cause symptoms of hyperthyroidism including tachycardia, palpitations, chest pain, diaphoresis, and tremors.","Exacerbation of diabetes mellitus: May increase insulin or oral hypoglycemic requirements.","Adrenal insufficiency: May precipitate acute adrenal crisis in patients with borderline adrenal function; treat with corticosteroids before initiating thyroid hormone.","Osteoporosis: Long-term therapy with supraphysiologic doses may decrease bone mineral density."] |
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| Monitor maternal thyroid function tests (TSH, FT4) every 4-6 weeks during pregnancy. Assess fetal growth and development; consider umbilical blood sampling if signs of thyroid dysfunction. |
| Fertility Effects | No direct effects on fertility. Thyroid hormone replacement in hypothyroid women improves ovulation and pregnancy outcomes. Overtreatment or undertreatment may disrupt menstrual cycles. |