Peringatan Keamanan

Doses titrated up to 300 mg once daily have been safely administered to patients on dialysis. Overdosage of cinacalcet may lead to hypocalcemia.

Cinacalcet

DB01012

small molecule approved

Deskripsi

Cinacalcet is a calcimimetic sold by Amgen under the trade name Sensipar® in North America and Australia and as Mimpara® in Europe. It is used to treat hyperparathyroidism due to parathyroid tumours or renal failure.

Struktur Molekul 2D

Berat 357.412
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Terminal half-life is 30 to 40 hours. The mean half-life of cinacalcet is prolonged by 33% and 70% in patients with moderate and severe hepatic impairment, respectively.
Volume Distribusi * 1000 L
Klirens (Clearance) -

Absorpsi

Rapidly absorbed following oral administration.

Metabolisme

Metabolism is hepatic by multiple enzymes, primarily CYP3A4, CYP2D6, and CYP1A2. After administration of a 75 mg radiolabeled dose to healthy volunteers, cinacalcet was rapidly and extensively metabolized via: 1) oxidative N-dealkylation to hydrocinnamic acid and hydroxy-hydrocinnamic acid, which are further metabolized via ß-oxidation and glycine conjugation; the oxidative N-dealkylation process also generates metabolites that contain the naphthalene ring; and 2) oxidation of the naphthalene ring on the parent drug to form dihydrodiols, which are further conjugated with glucuronic acid.

Rute Eliminasi

Cinacalcet is metabolized by multiple enzymes, primarily CYP3A4, CYP2D6 and CYP1A2. Renal excretion of metabolites was the primary route of elimination of radioactivity.

Interaksi Makanan

1 Data
  • 1. Take with food. Food markedly increases product bioavailability.

Interaksi Obat

559 Data
Deferasirox The serum concentration of Cinacalcet can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Cinacalcet can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Cinacalcet can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Cinacalcet can be decreased when it is combined with Teriflunomide.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Cinacalcet.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Cinacalcet.
Vortioxetine The metabolism of Vortioxetine can be decreased when combined with Cinacalcet.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Cinacalcet.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Cinacalcet.
Tetrabenazine The metabolism of Tetrabenazine can be decreased when combined with Cinacalcet.
Tacrolimus The serum concentration of Tacrolimus can be decreased when it is combined with Cinacalcet.
Abiraterone The serum concentration of Cinacalcet can be increased when it is combined with Abiraterone.
Cyproterone acetate The metabolism of Cinacalcet can be increased when combined with Cyproterone acetate.
Albendazole The metabolism of Cinacalcet can be increased when combined with Albendazole.
Carbamazepine The metabolism of Cinacalcet can be increased when combined with Carbamazepine.
Primidone The metabolism of Cinacalcet can be increased when combined with Primidone.
Rifampin The metabolism of Cinacalcet can be increased when combined with Rifampicin.
Moxifloxacin The metabolism of Cinacalcet can be decreased when combined with Moxifloxacin.
Alosetron The metabolism of Cinacalcet can be decreased when combined with Alosetron.
Gatifloxacin The metabolism of Cinacalcet can be decreased when combined with Gatifloxacin.
Simeprevir The metabolism of Cinacalcet can be decreased when combined with Simeprevir.
Lobeglitazone The metabolism of Cinacalcet can be decreased when combined with Lobeglitazone.
Pazufloxacin The metabolism of Cinacalcet can be decreased when combined with Pazufloxacin.
Osilodrostat The metabolism of Cinacalcet can be decreased when combined with Osilodrostat.
Amphetamine The metabolism of Amphetamine can be decreased when combined with Cinacalcet.
Cevimeline The metabolism of Cevimeline can be decreased when combined with Cinacalcet.
Esmolol The metabolism of Esmolol can be decreased when combined with Cinacalcet.
Bortezomib The metabolism of Bortezomib can be decreased when combined with Cinacalcet.
Betaxolol The metabolism of Betaxolol can be decreased when combined with Cinacalcet.
Ticlopidine The metabolism of Ticlopidine can be decreased when combined with Cinacalcet.
Citalopram The metabolism of Citalopram can be decreased when combined with Cinacalcet.
Ranolazine The metabolism of Ranolazine can be decreased when combined with Cinacalcet.
Benzatropine The metabolism of Benzatropine can be decreased when combined with Cinacalcet.
Metoprolol The metabolism of Metoprolol can be decreased when combined with Cinacalcet.
Lidocaine The metabolism of Lidocaine can be decreased when combined with Cinacalcet.
Venlafaxine The metabolism of Venlafaxine can be decreased when combined with Cinacalcet.
Bupivacaine The metabolism of Bupivacaine can be decreased when combined with Cinacalcet.
Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Cinacalcet.
Gefitinib The metabolism of Gefitinib can be decreased when combined with Cinacalcet.
Codeine The metabolism of Codeine can be decreased when combined with Cinacalcet.
Methadone The metabolism of Methadone can be decreased when combined with Cinacalcet.
Olanzapine The metabolism of Olanzapine can be decreased when combined with Cinacalcet.
Atenolol The metabolism of Atenolol can be decreased when combined with Cinacalcet.
Diltiazem The metabolism of Diltiazem can be decreased when combined with Cinacalcet.
Chlorzoxazone The metabolism of Chlorzoxazone can be decreased when combined with Cinacalcet.
Clozapine The serum concentration of Clozapine can be increased when it is combined with Cinacalcet.
Mirtazapine The metabolism of Mirtazapine can be decreased when combined with Cinacalcet.
Palonosetron The metabolism of Palonosetron can be decreased when combined with Cinacalcet.
Mexiletine The metabolism of Mexiletine can be decreased when combined with Cinacalcet.
Progesterone The metabolism of Progesterone can be decreased when combined with Cinacalcet.
Remoxipride The metabolism of Remoxipride can be decreased when combined with Cinacalcet.
Promazine The metabolism of Promazine can be decreased when combined with Cinacalcet.
Prochlorperazine The metabolism of Prochlorperazine can be decreased when combined with Cinacalcet.
Quinine The metabolism of Quinine can be decreased when combined with Cinacalcet.
Fluoxetine The metabolism of Fluoxetine can be decreased when combined with Cinacalcet.
Duloxetine The metabolism of Duloxetine can be decreased when combined with Cinacalcet.
Chlorpromazine The metabolism of Chlorpromazine can be decreased when combined with Cinacalcet.
Celecoxib The metabolism of Celecoxib can be decreased when combined with Cinacalcet.
Oxycodone The metabolism of Oxycodone can be decreased when combined with Cinacalcet.
Dextromethorphan The metabolism of Dextromethorphan can be decreased when combined with Cinacalcet.
Cinnarizine The metabolism of Cinnarizine can be decreased when combined with Cinacalcet.
Propranolol The metabolism of Propranolol can be decreased when combined with Cinacalcet.
Lisuride The metabolism of Lisuride can be decreased when combined with Cinacalcet.
Doxazosin The metabolism of Doxazosin can be decreased when combined with Cinacalcet.
Piperazine The metabolism of Piperazine can be decreased when combined with Cinacalcet.
Chloroquine The metabolism of Chloroquine can be decreased when combined with Cinacalcet.
Imatinib The metabolism of Imatinib can be decreased when combined with Cinacalcet.
Dextropropoxyphene The metabolism of Dextropropoxyphene can be decreased when combined with Cinacalcet.
Trazodone The metabolism of Trazodone can be decreased when combined with Cinacalcet.
Galantamine The metabolism of Galantamine can be decreased when combined with Cinacalcet.
Thioridazine The metabolism of Thioridazine can be decreased when combined with Cinacalcet.
Nicergoline The metabolism of Nicergoline can be decreased when combined with Cinacalcet.
Tamsulosin The metabolism of Tamsulosin can be decreased when combined with Cinacalcet.
Paroxetine The metabolism of Paroxetine can be decreased when combined with Cinacalcet.
Nateglinide The metabolism of Nateglinide can be decreased when combined with Cinacalcet.
Risperidone The metabolism of Risperidone can be decreased when combined with Cinacalcet.
Meclizine The metabolism of Meclizine can be decreased when combined with Cinacalcet.
Pentamidine The metabolism of Pentamidine can be decreased when combined with Cinacalcet.
Dolasetron The metabolism of Dolasetron can be decreased when combined with Cinacalcet.
Minaprine The metabolism of Minaprine can be decreased when combined with Cinacalcet.
Donepezil The metabolism of Donepezil can be decreased when combined with Cinacalcet.
Perphenazine The metabolism of Perphenazine can be decreased when combined with Cinacalcet.
Alprenolol The metabolism of Alprenolol can be decreased when combined with Cinacalcet.
Ondansetron The metabolism of Ondansetron can be decreased when combined with Cinacalcet.
Phenformin The metabolism of Phenformin can be decreased when combined with Cinacalcet.
Almotriptan The metabolism of Almotriptan can be decreased when combined with Cinacalcet.
Buprenorphine The metabolism of Buprenorphine can be decreased when combined with Cinacalcet.
Mesoridazine The metabolism of Mesoridazine can be decreased when combined with Cinacalcet.
Maprotiline The metabolism of Maprotiline can be decreased when combined with Cinacalcet.
Pindolol The metabolism of Pindolol can be decreased when combined with Cinacalcet.
Azelastine The metabolism of Azelastine can be decreased when combined with Cinacalcet.
Formoterol The metabolism of Formoterol can be decreased when combined with Cinacalcet.
Methoxyflurane The metabolism of Methoxyflurane can be decreased when combined with Cinacalcet.
Tolterodine The metabolism of Tolterodine can be decreased when combined with Cinacalcet.
Promethazine The metabolism of Promethazine can be decreased when combined with Cinacalcet.
Mequitazine The metabolism of Mequitazine can be decreased when combined with Cinacalcet.
Perhexiline The metabolism of Perhexiline can be decreased when combined with Cinacalcet.
Diphenhydramine The metabolism of Diphenhydramine can be decreased when combined with Cinacalcet.
Tegaserod The metabolism of Tegaserod can be decreased when combined with Cinacalcet.
Fluvastatin The metabolism of Fluvastatin can be decreased when combined with Cinacalcet.

Target Protein

Extracellular calcium-sensing receptor CASR

Referensi & Sumber

Synthesis reference: Revital Lifshitz-Liron, "Process for the preparation of cinacalcet base." U.S. Patent US20070259964, issued November 08, 2007.
Artikel (PubMed)
  • PMID: 16825031
    Torres PU: Cinacalcet HCl: a novel treatment for secondary hyperparathyroidism caused by chronic kidney disease. J Ren Nutr. 2006 Jul;16(3):253-8.
  • PMID: 19566113
    Padhi D, Harris R: Clinical pharmacokinetic and pharmacodynamic profile of cinacalcet hydrochloride. Clin Pharmacokinet. 2009;48(5):303-11. doi: 10.2165/00003088-200948050-00002.
  • PMID: 16368445
    Dong BJ: Cinacalcet: An oral calcimimetic agent for the management of hyperparathyroidism. Clin Ther. 2005 Nov;27(11):1725-51.

Contoh Produk & Brand

Produk: 188 • International brands: 1
Produk
  • Apo-cinacalcet
    Tablet • 30 mg • Oral • Canada • Generic • Approved
  • Apo-cinacalcet
    Tablet • 60 mg • Oral • Canada • Generic • Approved
  • Apo-cinacalcet
    Tablet • 90 mg • Oral • Canada • Generic • Approved
  • Auro-cinacalcet
    Tablet • 30 mg • Oral • Canada • Generic • Approved
  • Auro-cinacalcet
    Tablet • 60 mg • Oral • Canada • Generic • Approved
  • Auro-cinacalcet
    Tablet • 90 mg • Oral • Canada • Generic • Approved
  • Cinacalcet
    Tablet, film coated • 30 mg/1 • Oral • US • Generic • Approved
  • Cinacalcet
    Tablet, film coated • 60 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 188 produk.
International Brands
  • Mimpara

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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