Hormones
Evidence: strong_human
Levothyroxine (T4) is a prohormone converted to the active triiodothyronine (T3) by type 1 and type 2 deiodinase enzymes (DIO1/DIO2) in peripheral tissues. T3 binds nuclear thyroid hormone receptors (TRa and TRb), forming heterodimers with retinoid X receptors (RXR) that bind thyroid response elements (TREs) in DNA, directly modulating transcription of genes controlling basal metabolic rate, thermogenesis, mitochondrial biogenesis (via PGC-1a), cardiac output, and neuronal development. T3 also exerts rapid non-genomic effects on mitochondrial respiration, ion channels, and cell membrane transport.
Standard: Research indicates Levothyroxine (T4): 25-200 mcg daily based on TSH and free T4 levels. Liothyronine (T3): 5-25 mcg daily, often split into 2-3 doses. Combination T4/T3 ratio typically 4:1 to 3:1 when using both.
Maintenance: Research indicates titrate to TSH 0.5-2.0 mIU/L with free T4 in upper third and free T3 in mid-to-upper range. Start low (25-50 mcg T4) and increase by 12.5-25 mcg every 4-6 weeks.
Administration: oral
Timing: Levothyroxine: Take on empty stomach, 30-60 minutes before breakfast or at bedtime (3+ hours after last meal). Separate from calcium, iron, and antacids by 4 hours. Liothyronine: Split into 2-3 daily doses due to short half-life (2.5 hours for T3 vs. 6-7 days for T4).
Duration: Ongoing for diagnosed hypothyroidism. Optimization protocols may be shorter-term (3-6 months) with reassessment.
Thyroid optimization is foundational to metabolic health. CRITICAL: Always rule out adrenal insufficiency before initiating thyroid replacement — thyroid hormones increase cortisol clearance, which can precipitate adrenal crisis in undiagnosed adrenal insufficiency. Sustained-release T3 from compounding pharmacies avoids the peak/trough spikes of immediate-release liothyronine. Required bloodwork: TSH, free T4, free T3, reverse T3 (rT3), thyroid antibodies (TPO-Ab, TG-Ab) at baseline, then TSH + free T4/T3 every 6-8 weeks during titration, every 6-12 months once stable. Some optimization practitioners target TSH 0.5-2.0 with free T3 in the upper quartile of range. Medical supervision required.
FDA-approved pharmaceutical products: Levothyroxine (Synthroid, Levoxyl, Tirosint), Liothyronine (Cytomel). Brand-name preferred for levothyroxine due to narrow therapeutic index and variable generic bioequivalence. Compounding pharmacies can prepare sustained-release T3.
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