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Metopirone (Metyrapone) - Summary



Metopirone, metyrapone USP, is an inhibitor of endogenous adrenal corticosteriod synthesis, available as 250-mg capsules for oral administration.

METOPIRONE (METYRAPONE) is indicated for the following:

Metopirone is a diagnostic drug for testing hypothalamic?pituitary ACTH function.

See all Metopirone indications & dosage >>


Published Studies Related to Metopirone (Metyrapone)

Metyrapone administration reduces the strength of an emotional memory trace in a long-lasting manner. [2011.08]
CONTEXT: It has recently been demonstrated that the process of memory retrieval serves as a reactivation mechanism whereby the memory trace that is reactivated during retrieval is once again sensitive to modifications by environmental or pharmacological manipulations. Recent studies have shown that glucocorticoids (GCs) have the capacity to modulate the process of memory retrieval. This suggests that GCs could be an interesting avenue to investigate with regard to reduction of emotional memory. OBJECTIVE: The current study assessed whether a pharmacological decrease in GC levels, induced by metyrapone, a potent inhibitor of GC secretion, would affect retrieval of emotional and neutral information in an acute and/or long-lasting manner... CONCLUSIONS: These results show that decreasing GC levels via metyrapone administration is an efficient way to reduce the strength of an emotional memory in a long-lasting manner.

Mineralocorticoid receptor function in posttraumatic stress disorder after pretreatment with metyrapone. [2006.10.01]
BACKGROUND: Alterations of mineralocorticoid receptor (MR) mediated negative feedback inhibition of cortisol might contribute to abnormalities of hypothalamic-pituitary adrenal (HPA) activity in posttraumatic stress disorder (PTSD)... CONCLUSIONS: While HPA responses after metyrapone seem to be stronger in PTSD compared to controls, no alterations of mineralocorticoid receptor function in PTSD were found in this study.

Metyrapone improves endothelial dysfunction in patients with treated depression. [2006.07.04]
OBJECTIVES: This study sought to examine the effect of metyrapone on endothelial dysfunction in patients with treated recurrent major depression. BACKGROUND: Depression is an independent risk factor for the development of coronary heart disease, and patients with depression have endothelial dysfunction, an atherogenic abnormality. This abnormality may be attributable to abnormal hypothalamic-pituitary-adrenal (HPA) axis function, a feature of depression, resulting in increased exposure to cortisol. Cortisol administration produces endothelial dysfunction in healthy subjects... CONCLUSIONS: Inhibition of cortisol production by metyrapone ameliorates the endothelial dysfunction seen in depression, suggesting that the mechanism of the endothelial dysfunction may involve cortisol.

Inhibition of cortisol production with metyrapone prevents mental stress-induced endothelial dysfunction and baroreflex impairment. [2005.07.19]
OBJECTIVES: This study was designed to investigate the role of cortisol in stress-induced endothelial dysfunction and impaired baroreflex sensitivity (BRS) by blocking cortisol production with metyrapone before subjecting healthy volunteers to mental stress. BACKGROUND: Mental stress raises cortisol levels and is associated with increased coronary heart disease (CHD) morbidity and mortality, especially from sudden cardiac death. It also causes endothelial dysfunction and impaired BRS... CONCLUSIONS: Stress-related endothelial dysfunction and BRS impairment can be prevented by blocking cortisol production with metyrapone, demonstrating a direct or facilitative role for cortisol in these phenomena and suggesting mechanisms by which stress contributes to CHD and sudden cardiac death.

Metyrapone and cocaine: a double-blind, placebo-controlled drug interaction study. [2005.04]
Pre-clinical research suggests that suppression of adrenocorticosteroid synthesis might decrease susceptibility to stress-induced relapse... The results of the present study suggest that metyrapone at the dose studied can likely be used safely in an outpatient study with active cocaine users.

more studies >>

Clinical Trials Related to Metopirone (Metyrapone)

Effects of Metyrapone in Patients With Endogenous Cushing's Syndrome [Not yet recruiting]
The purpose of this prospective, international phase III/IV study is to assess the efficacy and safety of metyrapone in patients with endogenous Cushing's syndrome during up to 36 weeks of treatment. The ability of metyrapone (250 mg capsules) to normalize urinary free cortisol (UFC) levels will be assessed during up to 36 weeks (9 months) of treatment.

Single and Multiple Rising Dose Study of Safety and PK of Metyrapone/Oxazepam Combination (EMB-001) [Recruiting]
This is a study of EMB-001 (a combination of two FDA-approved drugs, metyrapone and oxazepam) in otherwise healthy adults who are regular cigarette smokers. There will be 3 groups of 8 subjects; in each group, 6 subjects will get the drug combination and 2 will get placebo. Neither the subjects nor the study personnel will know who got drug and who got placebo (double-blind). In the first group the drug doses will be low, and they will be increased in the second and third groups. Subjects will receive a single dose on Day 1, followed 24 hours later by the start of doses twice daily for 7 days, and then a final morning dose on the last day. The levels of the drugs in the blood will be assessed by repeated blood draws after the first day and after the end of dosing. Safety will be assessed after the single dose and repeated dosing. Effects of study drug on smoking and craving cigarettes will be assessed at the end of repeated dosing. The hypothesis is that this drug combination will be safe, with relatively few side effects.

A Placebo-Controlled Study of a Combination of Metyrapone and Oxazepam in Cocaine Addiction [Completed]
Subjects will be randomly assigned to receive either one of the two potential dose combinations of the study medications or placebo over 6 weeks. The study will include twice weekly visits to the research clinic for laboratory studies, safety assessments and urine drug screens. Subjects will also be questioned regarding drug craving and mood symptoms.

Cortisol and Nutritional Sympathetic Responsiveness [Recruiting]
This project will examine whether short-term (over a 12-hour period) pharmacological lowering of the stress hormone 'cortisol' improves the nervous system response to food intake in overweight or obese individuals who have metabolic syndrome. The investigators know from our previous research that overweight/obese persons who are insulin resistant, have a blunted sympathetic nervous response to carbohydrate ingestion. This means that they are less able to dissipate energy from caloric intake, which would favour the maintenance of the obese state. Cortisol adversely impacts on insulin action and transport into the brain and cortisol levels are often elevated in persons with central (abdominal) obesity. A randomized, double-blind, placebo controlled, cross-over design will be used to compare the effects of overnight treatment with metyrapone (15 mg/kg at midnight and 15 mg/kg at 6 am) versus placebo on sympathetic nervous system activity in response to a standard 75-g oral sugar (glucose) tolerance test. A 2 week washout will separate treatments. Metyrapone is a drug that reversibly inhibits the enzyme 11beta-hydroxylase, and therefore the production of cortisol. It is used clinically to test the activity of the adrenal gland (the key site of cortisol production) and the pituitary gland. The investigators anticipate that at the dosage used, it will lower blood cortisol concentration by 44 to 64% during the experimental morning. The study protocol comprises two screening visits and two experimental mornings. Key procedures will include:

- Assessment of insulin action (sensitivity) using the gold standard 'clamp' method.

- Measurement of sympathetic nervous system activity by both biochemical methods (isotope

dilution which provides a measure of the apparent rate of release of 'noradrenaline'-the key neurotransmitter in the sympathetic nervous system) and direct intra-neuronal nerve recordings from the peroneal nerve in the lower leg.

- Indirect calorimetry to assess resting metabolic rate and the response to sugar


- DEXA scan to quantify fat and lean mass.

- Assessment of arterial elasticity and calf blood flow by non-invasive methods.

- A standard 75g oral sugar tolerance test.

The results will provide important new information regarding the role of cortisol on nervous system function in overweight/obese individuals.

Metyrapone as Additive Treatment in Major Depression [Completed]
The purpose of this study is to test whether metyrapone is an effective and safe augmenting agent in the treatment of major depression.

more trials >>

Reports of Suspected Metopirone (Metyrapone) Side Effects

Asthenia (4)Myoclonus (3)OFF Label USE (2)Gamma-Glutamyltransferase Increased (2)Liver Function Test Abnormal (2)Adrenal Insufficiency (2)Hyponatraemia (2)Diarrhoea (2)Pain (1)Tachycardia (1)more >>

Page last updated: 2011-12-09

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