Levothyroxine

Synthroid | Levoxyl | Euthyrox | Tirosint

FDA ApprovedEndocrine AgentsThyroid Agents
FDA: 2002Half-life: 6-7 daysPregnancy: Category A

Overview

Synthetic form of endogenous thyroid hormone T4. Converted to T3 (active form) in peripheral tissues. Binds to thyroid hormone receptors, regulating gene expression for metabolism, growth, and develop

Indications

  • Hypothyroidism
  • Thyroid-stimulating hormone (TSH) suppression in thyroid cancer
  • Myxedema coma (IV)
  • Diagnostic use in thyroid suppression tests

Contraindications

  • Uncorrected adrenal insufficiency
  • Acute myocardial infarction
  • Thyrotoxicosis

Classification

Mechanism of Action

Synthetic form of endogenous thyroid hormone T4. Converted to T3 (active form) in peripheral tissues. Binds to thyroid hormone receptors, regulating gene expression for metabolism, growth, and development.

Pharmacodynamics

Increases basal metabolic rate, oxygen consumption, and heat production. Affects protein, carbohydrate, and lipid metabolism.

Pharmacokinetics

Absorption
Incomplete and variable (40-80%); affected by food, calcium, iron, antacids. Take on empty stomach.
Distribution
Highly protein bound (>99%) to TBG, TBPA, and albumin.
Metabolism
Deiodination in liver, kidneys, and other tissues to T3 (active) and reverse T3 (inactive).
Excretion
Renal and fecal elimination of metabolites.
Half-life
6-7 days
Bioavailability
40-80%
Protein Binding
>99%

Dosage

Typical dosage: 25-200 mcg once daily (individualized by TSH levels)

Available Forms

  • Tablet
  • Capsule (gel)
  • Oral solution
  • IV injection

Side Effects

Common

  • Usually well-tolerated at correct dose
  • Hair loss (transient, first few months)

Serious

  • Cardiac arrhythmias (overdose)
  • Osteoporosis (chronic excessive doses)
  • Angina pectoris

Rare

  • Seizures
  • Pseudotumor cerebri (pediatric)

Drug Interactions

moderate

Calcium reduces levothyroxine absorption. Separate administration by at least 4 hours.

moderate

Levothyroxine increases warfarin effect by increasing catabolism of vitamin K-dependent clotting factors. Monitor INR.

Warnings

⚠️BLACK BOX WARNING

Thyroid hormones should not be used for the treatment of obesity or weight loss. Doses within the range of daily hormonal requirements are ineffective for weight reduction.

Pregnancy

Category A

Toxicity

Not established (wide therapeutic index when monitored)

Overdose

Symptoms: thyrotoxicosis - tachycardia, tremor, weight loss, diarrhea, fever. Treatment: reduce dose or temporarily discontinue; beta-blockers for sympathetic symptoms.

References

Looking for patient-friendly information? Visit RemedyDoor for easy-to-read guides about this medication.