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  • Metopirone 250
    / CTS


    Active Ingredient
    Metyrapone 250 mg

    Status in Israel
    RX

    Presentation and Status in Health Basket

    Presentation Basket Yarpa Pharmasoft

    Capsules

    50 X 250 mg

    full basket chart 1324 13113

    Related information


    Dosage

    Single-dose short test to diagnose latent ACTH deficiency:
    This can be performed on an ambulatory basis. In this test, plasma 11-desoxycortisol and/or ACTH levels are determined after a single dose of Metopirone. The patient is given 30 mg/kg (maximum 3 g Metopirone) at midnight with yoghurt or milk to minimize nausea and vomiting. The same dose is recommended in children. The blood sample for the assay is taken early the following morning (7.30to 8.00 as described in [1,2]). The plasma should be frozen as soon as possible. The patient is then given a prophylactic dose of 50 mg cortisone acetate.
    Evaluation: Normal values will depend on the method used to determine ACTH and 11- desoxycortisol levels. An intact ACTH reserve is generally indicated by an increase in plasma ACTH to at least 44 pmol/L (200 ng/L) or by an increase in 11-desoxycortisol to over 0.2 micromol/L (70 micrograms/L). Patients with suspected adrenocortical insufficiency should be hospitalised overnight as a precautionary measure, although no cases of acute adrenocortical insufficiency have been reported to date in association with the single-dose short test.
    Multiple-dose test to diagnose latent ACTH deficiency:
    The patient must be hospitalised. In this test, urinary steroid levels are measured. First, baseline values are determined for the 24 hours preceding the test. Then 500 to 750 mg Metopirone is administered every 4 hours for 24 hours, giving a total dose of 3.0 to 4.5 g. In children the dosage should be 15 mg/kg body-weight, with a minimum dose of 250 mg every 4 hours for 6 doses. It is recommended that patients take the capsules with milk or after meals to minimize nausea and vomiting. The maximum effect of Metopirone on urinary steroid values should be reached within the next 24 hours.
    Evaluation: ACTH deficiency: If the anterior pituitary is functioning normally, Metopirone brings about a marked increase in 17-hydroxycorticosteroids (17-OHCS) or 17- ketogenic steroids (17-KGS) in the urine (to at least twice baseline levels). Lack of response indicates secondary adrenocortical insufficiency.
    For full details see prescribing information.


    Indications

    Diagnostic test of secondary adrenocortical insufficiency, treatment of resistant edema associated with increase of aldosterone secretion.


    Contra-Indications

    Hypersensitivity, manifest primary adrenocortical insufficiency.


    Special Precautions

    The ability of the adrenal cortex to respond to exogenous ACTH should be demonstrated before Metopirone is employed as a test, because Metopirone may induce acute adrenal insufficiency in patients with reduced adrenal secretory capacity as well as in patients with gross hypopituitarism. Hypertension may occur during treatment with Metopirone due to excessive secretion of desoxycorticosterone. Before the Metopirone test is carried out, drugs affecting pituitary or adrenocortical function should be discontinued. If adrenocortical or anterior pituitary function is more severely compromised than indicated by the results of the test, Metopirone may trigger transient adrenocortical insufficiency. This can be rapidly corrected by giving appropriate doses of corticosteroids. Since the plasma elimination half-life of cortisol is longer when hepatic function is impaired, patients with liver cirrhosis often respond to Metopirone more slowly. In patients with hypothyroidism, the Metopirone-induced increase in steroid values may be delayed or absent. When Metopirone is used as ACTH suppression test a diminished response was observed during pregnancy.


    Side Effects

    Nervous system disorders: Common: Dizziness, sedation, headache.
    Vascular disorders: Common: Hypotension.
    Gastrointestinal disorders: Common: Nausea, vomiting
    For full details see prescribing information.


    Drug interactions

    Observed interactions: Anticonvulsants (e.g. phenytoin, barbiturates), psychotropic drugs (e.g. amitriptyline, chlorpromazine, alprazolam), hormone preparations, corticosteroids, antithyroid agents and cyproheptadine may affect the results of the Metopirone test.
    Anticipated interactions: Metopirone may potentiate paracetamol (acetaminophen) toxicity in humans.


    Pregnancy and Lactation

    Pregnancy: Unless the potential benefit outweighs the risk to the foetus Metopirone should not be given to pregnant women, since the drug can impair the biosynthesis of foetal-placental steroids. Animal reproduction studies adequate to evaluate teratogenicity and postnatal development have not been conducted with Metopirone.
    Breast-feeding: Since it is not known whether metyrapone passes into the breast milk, Metopirone should not be given to breast-feeding women.
    Fertility: No data are available from animal reproduction studies.


    Overdose

    Signs and Symptoms: The clinical picture of poisoning with Metopirone is characterised by gastrointestinal symptoms and signs of acute adrenocortical insufficiency. Laboratory findings: hyponatraemia, hypochloraemia, hyperkalaemia. In patients under treatment with insulin or oral antidiabetics, the signs and symptoms of acute poisoning with Metopirone may be aggravated or modified.
    Treatment: There is no specific antidote. In addition to general measures to eliminate the drug and reduce absorption, a large dose of hydrocortisone should be administered at once, together with saline and glucose infusions. For a few days blood pressure and fluid and electrolyte balance should be monitored.


    Manufacturer
    Laboratoire HRA Pharma
    Licence holder
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