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 11-beta-hydroxylase inhibitor presented as an oral tablet for oral use. It is employed in diagnostic testing for Cushing’s syndrome, treatment of adrenal insufficiency, and management of congenital adrenal hyperplasia in selected patients.

GNH India supplies Metopirone as a licensed, GDP-compliant international pharmaceutical supplier serving hospitals, pharmacies and clinics worldwide, providing reliable sourcing, regulatory support and consistent quality for endocrine therapeutics. The company’s distribution network spans Europe, Asia, Africa and the Americas, ensuring timely delivery under appropriate storage conditions.

Manufacturer / TM Owner

Hra Pharma Rare Diseases

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Indications & Clinical Uses

Metopirone (metyrapone) acts as a cortisol synthesis inhibitor, targeting the adrenal steroidogenesis pathway, and is employed in several endocrine conditions where modulation of cortisol production is required.

  • Cushing's syndrome: assists in diagnostic testing by evaluating adrenal cortisol production and confirming hypercortisolism.
  • Adrenal insufficiency: helps restore cortisol levels when endogenous synthesis is inadequate, supporting stress response and metabolic balance.
  • Congenital adrenal hyperplasia: used to control excess androgen production by reducing cortisol synthesis, aiding hormonal regulation.

How It Works

  • Metopirone (metyrapone) inhibits the enzyme 11‑beta‑hydroxylase, which catalyzes the final step of cortisol synthesis in the adrenal cortex. By blocking this conversion of 11‑deoxycortisol to cortisol, the drug reduces cortisol output and leads to accumulation of upstream precursors, thereby altering the hypothalamic‑pituitary‑adrenal feedback loop. The resulting decrease in cortisol feedback stimulates ACTH release, which can be measured during diagnostic testing, and the shift in steroid intermediates can be therapeutically useful in conditions requiring cortisol suppression.

Side Effects

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

Common Side Effects

  • Nausea: mild gastrointestinal upset.
  • Headache: transient cranial discomfort.
  • Dizziness: sensation of lightheadedness.
  • Fatigue: general tiredness.

Serious or Rare Side Effects

  • Adrenal crisis: severe cortisol deficiency causing hypotension and shock.
  • Acute liver injury: marked elevation of hepatic enzymes.
  • Severe hypertension: rapid and dangerous rise in blood pressure.

Precautions & Warnings

When prescribing Metopirone, clinicians should consider several precautionary measures to ensure safe use.

  • Monitor cortisol levels: assess adrenal function before and during therapy.
  • Adjust dose in hepatic impairment: reduce dosage if liver function is compromised.
  • Caution in cardiovascular disease: watch for hypertension or fluid retention.
  • Evaluate electrolyte status: check potassium and sodium concentrations regularly.
  • Avoid abrupt discontinuation: taper gradually to prevent adrenal insufficiency.
  • Store at ambient temperature: keep below 25 °C in original packaging, protect from moisture.

Avoid Interactions

Metopirone can interact with other medicines, influencing its efficacy or safety.

Major Interactions (Avoid)

  • Ketoconazole: combined inhibition of steroidogenesis may cause severe cortisol deficiency.
  • Rifampicin: strong enzyme induction can markedly reduce metyrapone plasma levels.

Moderate Interactions (Monitor Closely)

  • Antihypertensives: metyrapone‑induced hypertension may diminish blood pressure control.
  • Oral contraceptives: altered steroid metabolism can affect hormonal balance.
  • Antidiabetic agents: hyperglycemia risk may be enhanced, requiring glucose monitoring.

Frequently Asked Questions

Metopirone (metyrapone) is used primarily for diagnostic testing of Cushing’s syndrome, to assess adrenal cortisol production, and as a therapeutic option in adrenal insufficiency and congenital adrenal hyperplasia where reduction of cortisol synthesis is required.

Metyrapone blocks the enzyme 11‑beta‑hydroxylase in the adrenal cortex, preventing the final conversion of 11‑deoxycortisol to cortisol. This inhibition lowers cortisol output, raises upstream steroid precursors, and alters the feedback loop that regulates ACTH secretion.

The dose of Metopirone is individualized by the prescribing clinician based on the specific indication, patient age, weight, renal and hepatic function, and response to therapy. No fixed regimen is provided here.

Safety data for metyrapone during pregnancy and lactation are limited. It should only be used when the potential benefit to the mother outweighs any possible risk to the fetus or infant, and under close medical supervision.

To order Metopirone, submit an enquiry on the product page at gnhindia.com with 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.

The most common alternative to metyrapone is ketoconazole, another cortisol synthesis inhibitor. Ketoconazole inhibits multiple enzymes in steroidogenesis, whereas metyrapone selectively blocks 11‑beta‑hydroxylase, offering a more targeted reduction of cortisol with a different side‑effect profile.

Metopirone tablets should be stored at ambient temperature, below 25 °C, in the original packaging to protect them from moisture and light. Keep the container tightly closed and out of reach of children.

Metopirone is taken orally, usually with a glass of water. The exact timing relative to meals or other medications is determined by the prescribing clinician based on the therapeutic goal and patient tolerance.

Serious risks include adrenal crisis, which can cause severe hypotension and shock, acute liver injury indicated by marked enzyme elevations, and severe hypertension that may lead to cardiovascular complications. Prompt medical attention is required if any of these occur.

Metopirone should be avoided in patients with known hypersensitivity to metyrapone, severe hepatic impairment, uncontrolled hypertension, or in those where rapid cortisol withdrawal could be dangerous. Clinicians must evaluate each patient’s medical history before initiating therapy.

Published by

GNH India Pharmaceuticals Limited

Licensed pharmaceutical supplier

Last updated:

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