Peringatan Keamanan

Oral LD50 in rats is 521 mg/kg. One case has been recorded in which a 6-year-old girl died after two doses of Metopirone, 2 g. Symptoms of overdose include cardiac arrhythmias, hypotension, dehydration, anxiety, confusion, weakness, impairment of consciousness, nausea, vomiting, epigastric pain, and diarrhea.

Metyrapone

DB01011

small molecule approved investigational

Deskripsi

An inhibitor of the enzyme steroid 11-beta-monooxygenase. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of cushing syndrome.

Struktur Molekul 2D

Berat 226.2738
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 1.9 ±0.7 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Absorbed rapidly and well when administered orally. Peak plasma concentrations are usually reached 1 hour after administration.

Metabolisme

Hepatic. The major biotransformation is reduction of the ketone to metyrapol, an active alcohol metabolite. Metyrapone and metyrapol are both conjugated with glucuronide.

Rute Eliminasi

After administration of 4.5 g metyrapone (750 mg every 4 hours), an average of 5.3% of the dose was excreted in the urine in the form of metyrapone (9.2% free and 90.8% as glucuronide) and 38.5% in the form of metyrapol (8.1% free and 91.9% as glucuronide) within 72 hours after the first dose was given.

Interaksi Makanan

1 Data
  • 1. Take with food. Take metyrapone with milk or a snack according to the specific instructions for a single or multi-dose test.

Interaksi Obat

945 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Metyrapone.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Metyrapone.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Metyrapone.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Metyrapone.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Metyrapone.
Colchicine The metabolism of Colchicine can be decreased when combined with Metyrapone.
Fentanyl Fentanyl may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Metyrapone.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Metyrapone.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Metyrapone.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Metyrapone.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Metyrapone.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Metyrapone.
Phenytoin The serum concentration of Metyrapone can be decreased when it is combined with Phenytoin.
Mephenytoin The serum concentration of Metyrapone can be decreased when it is combined with Mephenytoin.
Carbamazepine The serum concentration of Metyrapone can be decreased when it is combined with Carbamazepine.
Primidone The serum concentration of Metyrapone can be decreased when it is combined with Primidone.
Methylphenobarbital The serum concentration of Metyrapone can be decreased when it is combined with Methylphenobarbital.
Phenobarbital The serum concentration of Metyrapone can be decreased when it is combined with Phenobarbital.
Fosphenytoin The serum concentration of Metyrapone can be decreased when it is combined with Fosphenytoin.
Acetaminophen Metyrapone may increase the hepatotoxic activities of Acetaminophen.
Propacetamol Metyrapone may increase the hepatotoxic activities of Propacetamol.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Metyrapone.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Metyrapone.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Metyrapone.
Perampanel The metabolism of Perampanel can be increased when combined with Metyrapone.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Metyrapone.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Metyrapone.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Metyrapone.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Metyrapone.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Metyrapone.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Metyrapone.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Metyrapone.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Metyrapone.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Metyrapone.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Metyrapone.
Segesterone acetate The metabolism of Segesterone acetate can be increased when combined with Metyrapone.
Icosapent Icosapent may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Metyrapone which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Metyrapone which could result in a higher serum level.

Target Protein

Cytochrome P450 11B1, mitochondrial CYP11B1
Camphor 5-monooxygenase camC

Referensi & Sumber

Belum ada data referensi/link/attachment untuk obat ini pada database. Jalankan import DrugBank untuk mengisi field referensi.

Contoh Produk & Brand

Produk: 3 • International brands: 1
Produk
  • Metopirone
    Capsule, gelatin coated • 250 mg/1 • Oral • US • Approved
  • Metopirone
    Capsule, gelatin coated • 250 mg/1 • Oral • US • Approved
  • Metopirone
    Capsule, gelatin coated • 250 mg/1 • Oral • US • Approved
International Brands
  • Metopiron

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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