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 11β‑hydroxylase inhibitor presented as a tablet for oral use. It reduces cortisol synthesis and is employed for diagnostic testing of adrenal function and for treatment of Cushing's syndrome.
GNH India supplies Metopirone as a licensed, GDP‑compliant international pharmaceutical supplier serving hospitals, pharmacies and clinics worldwide.

Manufacturer / TM Owner

Esteve Pharmaceuticals, S.A.

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Indications & Clinical Uses

  • Metopirone acts on adrenal steroidogenesis and is used in specific endocrine indications.
  • Diagnostic testing of adrenal function: helps assess cortisol production capacity during endocrine evaluation.
  • Cushing's syndrome: lowers excess cortisol in patients with endogenous hypercortisolism.
  • ACTH stimulation test: employed to evaluate adrenal responsiveness in specialized diagnostic protocols.

How It Works

  • Metyrapone selectively inhibits adrenal 11β‑hydroxylase (CYP11B1), blocking the conversion of 11‑deoxycortisol to cortisol. This reduction in cortisol synthesis diminishes negative feedback on the hypothalamic‑pituitary axis, leading to increased ACTH secretion and accumulation of upstream steroid precursors, which can be measured for diagnostic purposes or used therapeutically to control hypercortisolism.

Side Effects

Metyrapone may cause a range of adverse reactions, most of which are dose‑related and reversible.

Common Side Effects

  • Nausea or vomiting
  • Fatigue or dizziness
  • Headache
  • Abdominal discomfort
  • Mild hypotension
  • Transient electrolyte changes

Serious or Rare Side Effects

  • Acute adrenal insufficiency
  • Severe hypotension or shock
  • Allergic reactions including rash or angioedema
  • Hepatic dysfunction
  • Hyponatremia or hypokalemia
  • Persistent hypertension or cardiovascular instability

Precautions & Warnings

Use of Metopirone requires careful clinical monitoring and patient education.

  • Monitor cortisol levels: assess endocrine response before and during therapy.
  • Assess adrenal function before discontinuation: avoid abrupt withdrawal.
  • Use with caution in hepatic impairment: dose adjustment may be needed.
  • Avoid in patients with known hypersensitivity to metyrapone or excipients.
  • Adjust dose in elderly patients: start low and titrate slowly.
  • Store at below 25°C: keep in the original pack, protect from moisture.

Avoid Interactions

Metyrapone can alter the activity of several co‑administered drugs, necessitating vigilance.

Major Interactions (Avoid)

  • Ketoconazole: potent CYP450 inhibition may raise metyrapone concentrations.
  • Rifampin: strong enzyme induction reduces metyrapone efficacy.
  • Phenytoin or carbamazepine: induce metabolism, potentially lowering therapeutic effect.

Moderate Interactions (Monitor Closely)

  • Glucocorticoids: may mask cortisol reduction and complicate assessment.
  • Antidepressants affecting serotonin: possible additive effects on blood pressure.
  • Oral contraceptives: hormonal changes may interfere with endocrine testing.
  • Antihypertensives: monitor blood pressure as metyrapone can cause hypotension.

Frequently Asked Questions

Metopirone (metyrapone) is used primarily for diagnostic testing of adrenal function and for the medical management of Cushing's syndrome, a condition characterized by excess cortisol production.

Metyrapone inhibits the adrenal enzyme 11β‑hydroxylase, which blocks the final step of cortisol synthesis. This reduces cortisol levels and leads to an increase in upstream steroid precursors that can be measured for diagnostic purposes.

The dose of Metopirone is individualized by the prescribing clinician based on the specific indication, patient characteristics, and response to therapy. Patients should follow the prescriber’s instructions and not adjust the dose on their own.

The safety of metyrapone in pregnancy and lactation has not been fully established. It should only be used if the potential benefit justifies the potential risk to the fetus or infant, and this decision must be made by a qualified healthcare professional.

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 required import documentation.

Metyrapone is a selective 11β‑hydroxylase inhibitor, whereas other agents such as ketoconazole or osilodrostat inhibit multiple steps in steroidogenesis. Metyrapone’s targeted mechanism can offer a different side‑effect profile and may be preferred in certain diagnostic or therapeutic scenarios.

Metopirone tablets should be stored at temperatures below 25 °C, in the original packaging, and protected from moisture and direct sunlight to maintain stability and potency.

Metopirone is taken orally as a tablet, usually with water. The exact timing and frequency are determined by the prescribing clinician based on the therapeutic goal and patient response.

Serious risks include acute adrenal insufficiency, severe hypotension, allergic reactions such as rash or angioedema, and hepatic dysfunction. Patients should be monitored closely for these events, especially during dose adjustments.

Metopirone should be avoided in individuals with known hypersensitivity to metyrapone or its excipients, and it should be used with caution in patients with severe hepatic impairment or uncontrolled cardiovascular disease.

Published by

GNH India Pharmaceuticals Limited

Licensed pharmaceutical supplier

Last updated:

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