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 a tablet for oral use. It is employed in the management of Cushing's syndrome, in diagnostic testing of adrenal function, and as adjunct therapy for adrenal insufficiency.
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 steroid synthesis pathways and is indicated for several endocrine conditions.
  • Cushing's syndrome: reduces excess cortisol production to improve clinical symptoms.
  • Diagnostic testing of adrenal function: blocks cortisol synthesis to assess adrenal reserve and ACTH response.
  • Adrenal insufficiency (adjunct therapy): used alongside glucocorticoid replacement to aid evaluation and management of adrenal disorders.

How It Works

  • Metyrapone selectively inhibits the enzyme 11‑beta‑hydroxylase (CYP11B1) in the adrenal cortex, preventing the conversion of 11‑deoxycortisol to cortisol. This blockade lowers cortisol output, leading to a compensatory rise in ACTH, which can be harnessed diagnostically or to control hypercortisolism in disease states.

Side Effects

Adverse reactions to Metopirone may vary in frequency and severity.

Common Side Effects

  • Nausea or vomiting
  • Dizziness or headache
  • Fatigue or weakness
  • Abdominal discomfort
  • Mild hypertension

Serious or Rare Side Effects

  • Adrenal insufficiency with severe cortisol deficiency
  • Significant hypertension or hypertensive crisis
  • Electrolyte disturbances such as hypokalemia
  • Allergic reactions including rash or angioedema
  • Hepatic dysfunction or elevated liver enzymes

Precautions & Warnings

  • Metopirone requires careful monitoring and specific safety considerations.
  • Pregnancy: safety not established; use only if benefits outweigh risks.
  • Breastfeeding: unknown excretion; consider potential infant exposure.
  • Renal impairment: monitor renal function and electrolytes closely.
  • Cardiovascular disease: observe blood pressure as drug may increase hypertension.
  • Drug interactions: review concomitant medications that affect steroid metabolism.
  • Store at ambient temperature below 25°C: keep in the original pack, protect from moisture.

Avoid Interactions

Metyrapone can interact with several drug classes, necessitating vigilance.

Major Interactions (Avoid)

  • Potent CYP3A4 inducers (e.g., rifampicin): may markedly reduce efficacy.
  • Concurrent high‑dose glucocorticoids: can mask signs of adrenal insufficiency.

Moderate Interactions (Monitor Closely)

  • Antihypertensive agents: metyrapone may elevate blood pressure.
  • Diuretics: risk of worsening electrolyte imbalances.
  • Oral contraceptives: possible alteration of steroid metabolism.

Frequently Asked Questions

Metopirone (generic name Metyrapone) is prescribed primarily for the medical management of Cushing's syndrome, for diagnostic testing of adrenal gland function, and as an adjunct in the treatment of adrenal insufficiency. It works by inhibiting cortisol synthesis, allowing clinicians to control excess cortisol or evaluate adrenal responsiveness.

Metyrapone blocks the enzyme 11‑beta‑hydroxylase (CYP11B1) in the adrenal cortex, preventing the conversion of 11‑deoxycortisol to cortisol. This reduction in cortisol production leads to a rise in ACTH, which can be used diagnostically, and helps lower cortisol levels in conditions such as Cushing's syndrome.

The dosage of Metopirone is individualized and must be determined by a qualified healthcare professional based on the specific indication, severity of disease, and patient characteristics. Prescribers typically start with a low dose and adjust according to clinical response and laboratory monitoring.

Safety data for Metyrapone in pregnancy and lactation are limited. The drug is classified as pregnancy category unknown, and it should only be used if the potential benefit justifies the potential risk to the fetus. Breastfeeding mothers should consult their physician, as the drug may be excreted in milk.

To place an order, submit an enquiry on the product page at gnhindia.com, specifying the required quantity of Metopirone. 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.

Compared with alternative agents such as ketoconazole or osilodrostat, Metyrapone offers a more selective inhibition of 11‑beta‑hydroxylase, which can result in fewer hepatic side effects but may cause more pronounced ACTH‑driven mineralocorticoid excess. Choice of therapy depends on patient tolerance, comorbidities, and physician experience.

Metopirone tablets should be stored at ambient temperature below 25 °C, protected from moisture and direct sunlight. Keep the medication in its original container with the lid tightly closed, and store out of reach of children. Do not refrigerate or freeze the tablets.

Metopirone is taken orally, usually with food or a glass of water to reduce gastrointestinal discomfort. The tablets are swallowed whole and should not be chewed, crushed, or split unless specifically instructed by a healthcare provider. Administration timing may be adjusted based on the prescribed dosing schedule.

The most serious adverse reactions include adrenal insufficiency, severe hypertension, electrolyte disturbances such as hypokalemia, and rare cases of hepatic dysfunction or allergic reactions. Patients should be monitored regularly for signs of cortisol deficiency, blood pressure changes, and laboratory abnormalities.

Metopirone is contraindicated in patients with known hypersensitivity to Metyrapone or any tablet excipients. Caution is advised for individuals with uncontrolled hypertension, severe cardiac disease, or active infections, as the drug may exacerbate these conditions. Pregnant or breastfeeding women should only use it when clearly indicated by a physician.

Published by

GNH India Pharmaceuticals Limited

Licensed pharmaceutical supplier

Last updated:

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