What are the contraindications of Methimazole (MMI)?

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Contraindications of Methimazole (MMI)

Methimazole is absolutely contraindicated in patients with hypersensitivity to the drug or any of its components. 1

Primary Contraindications

  • Hypersensitivity reactions: Any previous allergic reaction to methimazole or its components represents an absolute contraindication 1
  • First trimester of pregnancy: Methimazole is contraindicated during the first trimester due to potential teratogenicity 2
  • Breastfeeding mothers: While limited amounts are excreted in breast milk, caution is advised 3
  • Severe hepatic impairment: Patients with significant liver disease should avoid methimazole due to risk of hepatotoxicity 4

Relative Contraindications/Use with Caution

Pregnancy Considerations

  • First trimester: Propylthiouracil (PTU) is preferred during the first trimester due to methimazole's association with rare congenital anomalies 2, 5
  • Second and third trimesters: Methimazole is preferred after the first trimester due to lower risk of hepatotoxicity compared to PTU 2, 5
  • Specific birth defects associated with first-trimester use:
    • Aplasia cutis (scalp defects)
    • Choanal atresia
    • Esophageal atresia
    • Facial abnormalities 6

Other Precautions

  • Agranulocytosis: Although rare, this serious adverse effect requires immediate discontinuation if suspected 7
  • Hepatotoxicity: While less common than with PTU, liver function should be monitored 4
  • Renal impairment: Dose adjustment may be needed in patients with significant kidney disease

Clinical Decision Algorithm

  1. For non-pregnant patients with hyperthyroidism:

    • Methimazole is first-line therapy unless contraindicated by hypersensitivity
    • Monitor for side effects including rash, hepatotoxicity, and agranulocytosis
  2. For pregnant patients with hyperthyroidism:

    • First trimester: Use PTU (avoid methimazole)
    • Second and third trimesters: Switch to methimazole due to lower hepatotoxicity risk 2
    • Monitor thyroid function closely throughout pregnancy
  3. For patients with hypersensitivity to methimazole:

    • Switch to PTU as alternative therapy
    • Consider desensitization to methimazole under allergist supervision if PTU is not tolerated 7
    • Plan for definitive therapy (radioactive iodine after pregnancy or surgery) if appropriate

Important Clinical Considerations

  • Patients should be educated about signs of agranulocytosis (fever, sore throat) and hepatotoxicity (jaundice, abdominal pain)
  • Regular monitoring of complete blood count and liver function tests is recommended
  • For patients with hypersensitivity reactions that are not severe (e.g., mild rash), desensitization protocols under allergist supervision may be considered 7
  • Uncontrolled hyperthyroidism during pregnancy poses greater risks than controlled medication use, including increased risk of preterm labor and low birth weight 6

Remember that the benefits of treating hyperthyroidism generally outweigh the risks of medication, but proper selection of therapy based on individual patient factors is essential for optimal outcomes.

References

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Research

Excretion of methimazole in human milk.

European journal of clinical pharmacology, 1982

Research

The safety of methimazole and propylthiouracil in pregnancy: a systematic review.

Journal of obstetrics and gynaecology Canada : JOGC = Journal d'obstetrique et gynecologie du Canada : JOGC, 2012

Research

Hyperthyroidism during pregnancy.

Canadian family physician Medecin de famille canadien, 2009

Research

Desensitization to Methimazole.

Endocrine practice : official journal of the American College of Endocrinology and the American Association of Clinical Endocrinologists, 2021

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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