Product image of Metopirone Esteve Pharmaceuticals (Metyrapone) supplied by GNH India

Metopirone Esteve Pharmaceuticals

Active Ingredient:
Metyrapone
Origin:
EU

Metopirone Esteve Pharmaceuticals (Metyrapone)

Metyrapone, the active ingredient in Metopirone Esteve Pharmaceuticals, is an adrenal steroidogenesis inhibitor presented as an oral dosage form for oral use. It is employed in the diagnostic evaluation of adrenal insufficiency and in the medical management of Cushing's syndrome, particularly when rapid reduction of cortisol is required.

GNH India supplies Metopirone Esteve Pharmaceuticals 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

Metyrapone acts on adrenal cortisol synthesis and is used in conditions where modulation of cortisol production is required.

  • Diagnostic testing of adrenal insufficiency: helps assess residual adrenal function by blocking cortisol synthesis.
  • Evaluation of cortisol reserve: used in dynamic testing to determine adrenal responsiveness.
  • Treatment of Cushing's syndrome: reduces excessive cortisol levels in patients with endogenous hypercortisolism.

How It Works

  • Metyrapone inhibits the enzyme 11‑beta‑hydroxylase (CYP11B1) in the adrenal cortex, blocking the final step of cortisol biosynthesis. By preventing conversion of 11‑deoxycortisol to cortisol, it lowers circulating cortisol concentrations and allows clinicians to evaluate adrenal reserve or manage hypercortisolism.

Side Effects

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

Common Side Effects

  • Nausea: mild to moderate gastrointestinal upset.
  • Dizziness: transient light‑headedness, especially on standing.
  • Headache: pressure or throbbing sensation.
  • Fatigue: reduced energy levels.
  • Abdominal pain: discomfort in the upper abdomen.

Serious or Rare Side Effects

  • Adrenal insufficiency: signs of cortisol deficiency requiring urgent care.
  • Hypertension or hypotension: significant blood pressure changes.
  • Hypokalemia: low potassium levels leading to muscle weakness.
  • Severe allergic reactions: rash, swelling, or anaphylaxis.
  • Hepatic dysfunction: abnormal liver enzymes or jaundice.

Precautions & Warnings

When prescribing Metyrapone, clinicians should consider several safety measures.

  • Baseline adrenal assessment: evaluate cortisol status before initiation.
  • Blood pressure monitoring: watch for hypertension or hypotension.
  • Electrolyte surveillance: check potassium and sodium levels regularly.
  • Avoid abrupt discontinuation: taper to prevent adrenal crisis.
  • Hepatic impairment caution: adjust use in patients with liver disease.
  • Store at below 25°C: keep in the original packaging, protect from moisture.

Avoid Interactions

Metyrapone can alter the metabolism of several co‑administered drugs.

Major Interactions (Avoid)

  • Ketoconazole: potent CYP450 inhibition may increase Metyrapone levels.
  • Rifampin: strong enzyme induction can reduce Metyrapone efficacy.
  • Phenytoin: hepatic enzyme induction may diminish therapeutic effect.

Moderate Interactions (Monitor Closely)

  • Oral contraceptives: reduced steroid hormone efficacy may occur.
  • Antihypertensives: blood pressure response may be altered.
  • NSAIDs: may increase risk of renal impairment when combined.

Frequently Asked Questions

Metopirone, whose active ingredient is metyrapone, is used primarily for diagnostic testing of adrenal insufficiency and for medical management of Cushing's syndrome. By inhibiting cortisol synthesis, it helps clinicians assess adrenal function and reduce excess cortisol in patients with endogenous hypercortisolism.

Metyrapone blocks the enzyme 11‑beta‑hydroxylase (CYP11B1) in the adrenal cortex, preventing the final step of cortisol production. This reduction in cortisol allows for dynamic testing of adrenal reserve and provides therapeutic cortisol lowering in conditions such as Cushing's syndrome.

The dosage of Metopirone is individualized by the prescribing clinician based on the specific indication, patient age, weight, and clinical response. Physicians determine the appropriate amount and schedule, and patients should follow the prescribed regimen without deviation.

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

To request 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 differs from other agents such as ketoconazole or osilodrostat by specifically inhibiting 11‑beta‑hydroxylase, whereas ketoconazole has broader antifungal and steroidogenic effects. Metopirone is often chosen for rapid cortisol reduction in diagnostic settings or when alternative agents are contraindicated.

Metopirone should be stored at temperatures below 25 °C, in its original packaging, and protected from moisture. Keeping the product in a dry, cool environment helps maintain its stability and potency throughout its shelf life.

Metopirone is taken orally, usually as a tablet. The exact administration schedule—such as timing relative to meals—depends on the prescriber's instructions and the therapeutic goal, whether diagnostic or therapeutic.

The most serious risks include adrenal insufficiency, which can lead to life‑threatening cortisol deficiency, severe hypertension or hypotension, and rare hepatic dysfunction. Patients should be monitored closely for signs of these conditions, and any sudden symptoms should prompt immediate medical attention.

Metopirone is contraindicated in patients with known hypersensitivity to metyrapone or any of its excipients. Caution is also advised for individuals with uncontrolled hypertension, severe liver disease, or those who are pregnant or breastfeeding unless the benefits outweigh the risks.

Published by

GNH India Pharmaceuticals Limited

Licensed pharmaceutical supplier

Last updated:

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