Metyrapone
Also known as: Metyrapone Tartrate, Metopirone, Methopyraphone
Metyrapone is inhibitor of 11b-hydroxylase, an important cytochrome P450 enzyme involved in the biosynthesis of cortisol and alsosterone. Metyrapone is administered orally. Metyrapone is used in the treatment of cushing's syndrome. Metyrapone is also used in tests of pituitary gland function..
Primary Characteristics
Metyrapone is also known as Metyrapone Tartrate, Metopirone, Methopyraphone.
It is of Natural origin and belongs to Pyridylalkane.
It belongs to Setroid 11-B-hydroxylase inhibitor pharmacological group on the basis of mechanism of action. It is also classified under Diagnostic Aids .
Molecular Weight: 226.3 · Solubility in Water: 1 in 100 · Solubility in Alcohol: 1 in 3 · Non-proprietary name: Metyrapone.
Pharmacokinetics
Absorption: Metyrapone has an oral bioavailability is 103%.
Elimination: it is metabolised via extensive by Liver, plasma half-life is 30 min, renal excretion is 50 %.
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Indications
Metyrapone is primarily indicated in conditions like Adrenal failure, Cushing's syndrome, Differential diagnosis of acth-dependent cushing`s syndrome, Edema, Management of cushing`s syndrome, Oedema, Resistant oedema.
Metyrapone is also indicated for secondary conditions like Hypersensitivity, Lactation, Porphyria, Pregnancy.
Contraindications
Metyrapone is contraindicated in conditions like Adrenal insufficiency.
Dosage
Metyrapone's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 750 mg | 750 mg | Every 4h | PO | For 6 doses |
| Paediatric Dosage (20kg) | ||||
| 15 mg/kg | 15 mg/kg | Every 4h | Oral | 6 divided doses |
| Neonatal Dosage (3kg) | ||||
| 15 mg/kg | 15 mg/kg | Every 4h | Oral | For One Day |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Metyrapone in overdosage may give rise to further complications which include Alopecia , Bone marrow depression .
The signs and symptoms that are produced after acute overdosage of Metyrapone are Convulsions , Unconsciousness, Cardiac arrest, Extensor spasm of fingers, Glucocorticoid insufficiency.
Metyrapone is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Allergic, Dizziness, Headache, Hypertension , Hypoadrenalism, Hypotension , Nausea and vomiting, Sedation .
Warnings / Precautions
Interference in Pathology
Metyrapone may interfere in the diagnosis of ACTH test.
Available Brands
None recorded.
Storage Conditions
Drug Classification
- 1.18.9 — ACTH