Product image of Metopiron (Metyrapone) supplied by GNH India

Metopiron

Active Ingredient:
Metyrapone
Origin:
EU

Metopiron (Metyrapone)

Metyrapone, the active ingredient in Metopiron, is a 11β-hydroxylase inhibitor presented as an oral formulation for oral use. It is employed in diagnostic testing for Cushing's syndrome and may be used off‑label for treatment of the condition.

GNH India supplies Metopiron as a licensed, GDP‑compliant international pharmaceutical supplier serving hospitals, pharmacies and clinics worldwide.

Manufacturer / TM Owner

Hra Pharma Rare Diseases

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Indications & Clinical Uses

Metyrapone acts on adrenal steroid synthesis, making it useful in disorders of cortisol excess.

  • Diagnostic testing for Cushing's syndrome: helps assess endogenous cortisol production during suppression tests.
  • Treatment of Cushing's syndrome (off‑label): reduces cortisol synthesis when conventional therapy is unsuitable.
  • Evaluation of adrenal function in research settings: provides a pharmacologic tool to study 11β‑hydroxylase activity.

How It Works

  • Metyrapone selectively inhibits the enzyme 11β‑hydroxylase in the adrenal cortex, blocking the final step of cortisol biosynthesis. By preventing conversion of 11‑deoxycortisol to cortisol, it lowers circulating cortisol levels and allows clinicians to evaluate adrenal reserve or manage hypercortisolism under controlled conditions.

Side Effects

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

Common Side Effects

  • Nausea
  • Dizziness
  • Headache
  • Fatigue
  • Abdominal discomfort
  • Mild hypotension

Serious or Rare Side Effects

  • Acute adrenal insufficiency
  • Severe hypotension or shock
  • Allergic reactions (rash, angioedema)
  • Hepatic dysfunction
  • Cardiac arrhythmias
  • Adrenal crisis in abrupt withdrawal

Precautions & Warnings

Use of Metyrapone requires careful clinical monitoring to avoid hormonal imbalance and related complications.

  • Monitor cortisol levels: assess endocrine response before and during therapy.
  • Assess adrenal function: ensure baseline adrenal reserve is adequate.
  • Use with caution in hepatic impairment: adjust dose if liver function is compromised.
  • Avoid abrupt discontinuation: taper to prevent adrenal crisis.
  • Administer under specialist supervision: endocrinology input is recommended.
  • Store at ambient temperature: keep in the original container, protect from moisture and direct sunlight.

Avoid Interactions

Metyrapone can alter the activity of several drugs that share metabolic pathways or hormonal targets.

Major Interactions (Avoid)

  • Ketoconazole: strong CYP inhibition may increase Metyrapone plasma levels.
  • Rifampin: enzyme induction can markedly reduce Metyrapone effectiveness.
  • Phenytoin, carbamazepine: hepatic enzyme inducers that lower drug exposure.
  • High‑dose glucocorticoids: may counteract the intended cortisol‑lowering effect.

Moderate Interactions (Monitor Closely)

  • Oral contraceptives: hormonal changes may affect efficacy.
  • Antidepressants (e.g., SSRIs): potential additive effects on cortisol regulation.
  • NSAIDs: increased risk of gastrointestinal irritation when combined with Metyrapone.

Frequently Asked Questions

Metopiron contains Metyrapone, which is used primarily for diagnostic testing of Cushing's syndrome to evaluate cortisol production, and it may be prescribed off‑label to lower cortisol levels in patients with confirmed Cushing's syndrome when other therapies are unsuitable.

Metyrapone blocks the enzyme 11β‑hydroxylase in the adrenal cortex, preventing the final step of cortisol synthesis. This inhibition reduces cortisol output, allowing clinicians to assess adrenal function or manage hypercortisolism under controlled conditions.

The specific dose of Metopiron is determined by the prescribing clinician based on the indication, patient characteristics, and laboratory monitoring. Dosage regimens are individualized and should follow the healthcare provider's instructions.

Safety data for Metyrapone in pregnancy and lactation are limited. It should only be used if the potential benefit justifies any potential risk to the fetus or infant, and the decision must be made by a qualified healthcare professional.

To request Metopiron, 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.

Metyrapone is a selective 11β‑hydroxylase inhibitor, whereas other agents such as ketoconazole or osilodrostat target multiple steps in steroidogenesis. Metyrapone’s specificity can offer a clearer diagnostic profile, but its off‑label therapeutic use may be limited compared with broader‑acting inhibitors.

Metopiron should be stored at ambient temperature, below 25 °C, in its original packaging. Protect the product from moisture, excessive heat and direct sunlight to maintain stability.

Metopiron is taken orally, usually as a tablet or capsule, with or without food as directed by the prescriber. The exact administration schedule is individualized based on the clinical scenario and monitoring results.

The most serious risks include acute adrenal insufficiency, severe hypotension, allergic reactions such as angioedema, hepatic dysfunction, and cardiac arrhythmias. Prompt medical attention is required if any of these symptoms develop.

Metopiron should be avoided in patients with known hypersensitivity to Metyrapone, uncontrolled adrenal insufficiency, severe hepatic impairment, or in individuals where rapid cortisol reduction could be dangerous without close monitoring.

Published by

GNH India Pharmaceuticals Limited

Licensed pharmaceutical supplier

Last updated:

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