Product image of Metopirone (Metyrapone) supplied by GNH India

Metopirone

Active Ingredient:
Metyrapone
Origin:
EU

Metopirone (Metyrapone)

Metyrapone, the active ingredient in Metopirone, is a steroidogenesis inhibitor presented as an oral tablet for systemic use. It works by blocking cortisol synthesis, making it useful in the medical management of Cushing's syndrome and as a diagnostic agent for evaluating adrenal gland function in patients with suspected endocrine disorders.

GNH India supplies Metopirone as a licensed, GDP‑compliant international pharmaceutical supplier serving hospitals, pharmacies and clinics worldwide, ensuring quality and regulatory compliance across global markets.

Manufacturer / TM Owner

Esteve Pharmaceuticals, S.A.

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Indications & Clinical Uses

  • Metyrapone is employed in conditions related to excess cortisol production and adrenal function testing.
  • Cushing's syndrome: reduces cortisol levels in patients with endogenous hypercortisolism.
  • Diagnostic testing of adrenal function: helps evaluate ACTH reserve and adrenal responsiveness during endocrine assessment.

How It Works

  • Metyrapone inhibits the enzyme 11‑beta‑hydroxylase (CYP11B1) in the adrenal cortex, preventing the final step of cortisol synthesis. This blockade reduces circulating cortisol, leading to a compensatory rise in ACTH and increased production of adrenal androgens, which can be exploited diagnostically to assess adrenal reserve and therapeutically to lower cortisol excess.

Side Effects

Metyrapone may cause a range of adverse reactions, from mild to serious.

Common Side Effects

  • Nausea
  • Dizziness
  • Headache
  • Fatigue

Serious or Rare Side Effects

  • Adrenal insufficiency
  • Severe hypertension
  • Allergic reaction, including rash or anaphylaxis

Precautions & Warnings

  • When prescribing Metopirone, clinicians should consider several safety measures.
  • Monitor electrolyte levels: watch for hypokalemia and sodium imbalance.
  • Assess cortisol before discontinuation: avoid abrupt withdrawal in dependent patients.
  • Use caution in cardiovascular disease: hypertension may worsen.
  • Avoid in known hypersensitivity: discontinue if allergic signs appear.
  • Adjust dose in hepatic impairment: liver function may affect metabolism.
  • Store at room temperature: keep in the original pack, protect from moisture.

Avoid Interactions

Metyrapone can interact with other medicines, requiring attention to avoid reduced efficacy or increased toxicity.

Major Interactions (Avoid)

  • Ketoconazole: potent CYP3A4 inhibition may increase metyrapone levels.
  • Rifampin: strong enzyme induction can markedly lower drug exposure.
  • Phenytoin and other anticonvulsants: accelerate metabolism, reducing effectiveness.

Moderate Interactions (Monitor Closely)

  • Oral contraceptives: cortisol reduction may affect hormone balance.
  • Antihypertensives: blood pressure changes may require dose adjustment.
  • NSAIDs: may increase risk of gastrointestinal irritation.

Frequently Asked Questions

Metopirone contains metyrapone, which is used primarily to treat Cushing's syndrome by lowering cortisol production and to aid in diagnostic testing of adrenal gland function, helping clinicians assess ACTH reserve and adrenal responsiveness.

Metyrapone blocks the enzyme 11‑beta‑hydroxylase (CYP11B1) in the adrenal cortex, preventing the final step of cortisol synthesis. This reduces cortisol levels, triggers a rise in ACTH, and increases adrenal androgen output, which can be measured for diagnostic purposes.

The specific dose of Metopirone is determined by the prescribing physician based on the individual patient's condition, severity, and response to therapy. Dosage regimens are not standardized and should follow the prescriber's instructions.

The safety of Metopirone in pregnancy and lactation has not been established. It is classified as pregnancy category unknown, and the drug should only be used if the potential benefit justifies any potential risk to the fetus or infant.

To order Metopirone, submit an enquiry on the product page at gnhindia.com, specifying the required quantity. GNH India works with hospitals, pharmacies and procurement teams worldwide, verifies trade or institutional credentials, and then provides pricing, availability, shipping details and any necessary import documentation.

Metopirone (metyrapone) differs from other inhibitors such as ketoconazole or osilodrostat in its specific target of 11‑beta‑hydroxylase. It is often preferred for diagnostic testing because its effect is reversible and it provides a clear biochemical profile, whereas other agents may have broader enzyme inhibition and distinct side‑effect profiles.

Metopirone tablets should be stored at room temperature, below 25 °C, in their original packaging. Protect them from moisture and direct sunlight to maintain stability and potency throughout the shelf life.

Metopirone is taken orally as a tablet. The exact timing and frequency are prescribed by the treating physician, often with meals or as directed to optimize absorption and minimize gastrointestinal discomfort.

The most serious risks include adrenal insufficiency, which can cause severe fatigue, hypotension, and electrolyte disturbances, and severe hypertension. Prompt medical attention is required if these symptoms develop while on therapy.

Metopirone should be avoided in individuals with known hypersensitivity to metyrapone or any tablet excipients, and in patients where cortisol reduction could be dangerous, such as those with uncontrolled cardiovascular disease or active adrenal insufficiency.

Published by

GNH India Pharmaceuticals Limited

Licensed pharmaceutical supplier

Last updated:

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