Metyrapone


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Diagnostic test in differentiating pituitary and ectopic production of ACTH in patients with ACTH-dependent Cushing's syndrome
Adult: For single-dose test: 30 mg/kg at midnight. Max: 3 g. For multiple-dose test: 750 mg every 4 hours for 6 doses.
Child: For single-dose test: Same as adult dose. For multiple-dose test: 15 mg/kg (Min 250 mg and Max 750 mg) every 4 hours for 6 doses.

Oral
Resistant oedema
Adult: In combination with glucocorticoid: 3,000 mg daily in divided doses.

Oral
Cushing's syndrome
Adult: 250 mg to 6,000 mg daily in divided doses, adjusted according to patient’s requirement.
Cách dùng
Should be taken with food. Take w/ milk or yoghurt or after a meal.
Chống chỉ định
Adrenal cortical insufficiency.
Thận trọng
Patient with hypo-or hyperthyroidism, reduced adrenal secretory capacity, gross hypopituitarism, ectopic Cushing’s syndrome. Hepatic impairment. Children. Pregnancy and lactation.
Phản ứng phụ
Significant: Acute adrenal insufficiency, hypertension (long-term use), opportunistic infections (e.g. P. Jirovecii pneumonia).
Endocrine disorders: Hirsutism.
Gastrointestinal disorders: Abdominal pain/discomfort, nausea, vomiting.
Nervous system disorders: CNS depression (e.g. dizziness, sedation), headache.
Skin and subcutaneous tissue disorders: Rash.
Vascular disorders: Hypotension.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness and sedation, if affected, do no drive or operate machinery.
MonitoringParameters
Monitor for signs and symptoms of acute adrenal insufficiency.
Quá liều
Symptoms: Gastrointestinal symptoms (e.g. vomiting, nausea, epigastric pain, diarrhoea), acute adrenocortical insufficiency, cardiac arrhythmias, hypotension, dehydration, anxiety, confusion, weakness, impairment of consciousness, hyponatremia, hypochloraemia, hyperkalaemia. Management: Perform gastric lavage, forced emesis and administration of large dose hydrocortisone, together with IV saline and glucose infusion to reduce drug absorption. Repeat if necessary according to patient’s condition. Monitor blood pressure, fluid and electrolyte imbalance.
Tương tác
Decreased serum concentration with phenytoin. May increase serum concentration and potentiate acetaminophen toxicity. Amitriptyline, chlorpromazine, barbiturates, corticosteroids, cyproheptadine may affect the result of metyrapone test.
Tác dụng
Description: Metyrapone is a diagnostic agent that inhibits 11β-hydroxylase enzyme in the adrenal cortex hence, blocking the synthesis of cortisol and corticosterone production resulting to increase adrenocorticotropic hormone (ACTH) production thereby, increasing cortisol precursors in the urine (17-hyroxycorticosteroids [17-OHCS] and 17-ketogenic steroids [17-KGS]).
Onset: Peak steroid secretion: Within 24 hours.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Time to peak plasma concentration: 1 hour.
Distribution: Enters breast milk.
Metabolism: Metabolised in the liver via rapid reduction of the ketone to active metabolite, metyrapol. Both parent drug and metabolite also undergoes glucuronide conjugation.
Excretion: Mainly via urine (approx 5%, as metyrapone; approx 38%, as metyrapol). Elimination half-life: Approx 1.9 hours.
Đặc tính

Chemical Structure Image
Metyrapone

Source: National Center for Biotechnology Information. PubChem Database. Metyrapone, CID=4174, https://pubchem.ncbi.nlm.nih.gov/compound/Metyrapone (accessed on Jan. 22, 2020)

Bảo quản
Store below 30°C. Protect from moisture and heat.
Phân loại ATC
V04CD01 - metyrapone ; Belongs to the class of diagnostic agents used to test for pituitary function.
References
Anon. Metyrapone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/12/2017.

Buckingham R (ed). Metyrapone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/12/2017.

Joint Formulary Committee. Metyrapone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/12/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Metyrapone. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 04/12/2017.

Metopirone Capsule, Gelatin Coated (Laboratoire HRA Pharma). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/12/2017.

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