Peringatan Keamanan

Rhein DB13174 has an oral LD50 of >5000mg/kg in mice. This is equivalent to a diacerein dose of >6476mg/kg.

Diacerein

DB11994

small molecule approved investigational

Deskripsi

Diacerein is a prodrug which is metabolized to rhein. It is currently approved in France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including severe diarrhea L780. Diacerein is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications.

Struktur Molekul 2D

Berat 368.297
Wujud -

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 4-10h [A19300].
Volume Distribusi 15-60L [A19300].
Klirens (Clearance) Total CL is 1.5L/h and renal CL is 0.1L/h [A19300].

Absorpsi

Bioavailability of 50-60% A19300. Entirely converted to the active metabolite rhein DB13174 before reaching systemic circulation.

Metabolisme

Entirely converted to rhien DB13174 through double deacetylation before reaching systemic circulation A19300. Rhein DB13174 is further metabolized to rhein glucuronide and rhein sulfate.

Rute Eliminasi

37% excreted in urine and 53% in feces as estimated in rats A19250.

Interaksi Obat

504 Data
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Diacerein.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Diacerein.
Aripiprazole The metabolism of Aripiprazole can be decreased when combined with Diacerein.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be decreased when combined with Diacerein.
Enflurane The metabolism of Enflurane can be decreased when combined with Diacerein.
Trimethadione The metabolism of Trimethadione can be decreased when combined with Diacerein.
Chlorzoxazone The metabolism of Chlorzoxazone can be decreased when combined with Diacerein.
Isoflurane The metabolism of Isoflurane can be decreased when combined with Diacerein.
Ethanol The metabolism of Ethanol can be decreased when combined with Diacerein.
Methoxyflurane The metabolism of Methoxyflurane can be decreased when combined with Diacerein.
Halothane The metabolism of Halothane can be decreased when combined with Diacerein.
Sevoflurane The metabolism of Sevoflurane can be decreased when combined with Diacerein.
Nilvadipine The metabolism of Nilvadipine can be decreased when combined with Diacerein.
Aniline The metabolism of Aniline can be decreased when combined with Diacerein.
Benzyl alcohol The metabolism of Benzyl alcohol can be decreased when combined with Diacerein.
Felbamate The metabolism of Felbamate can be decreased when combined with Diacerein.
Cenobamate The metabolism of Cenobamate can be decreased when combined with Diacerein.
Fingolimod The metabolism of Fingolimod can be decreased when combined with Diacerein.
Ethosuximide The metabolism of Ethosuximide can be decreased when combined with Diacerein.
Selumetinib The metabolism of Selumetinib can be decreased when combined with Diacerein.
Benzocaine The metabolism of Benzocaine can be decreased when combined with Diacerein.
Aminophylline The metabolism of Aminophylline can be decreased when combined with Diacerein.
Tamoxifen The metabolism of Tamoxifen can be decreased when combined with Diacerein.
Phenobarbital The metabolism of Phenobarbital can be decreased when combined with Diacerein.
Dolasetron The metabolism of Dolasetron can be decreased when combined with Diacerein.
Amphetamine The metabolism of Amphetamine can be decreased when combined with Diacerein.
Cevimeline The metabolism of Cevimeline can be decreased when combined with Diacerein.
Esmolol The metabolism of Esmolol can be decreased when combined with Diacerein.
Ticlopidine The metabolism of Ticlopidine can be decreased when combined with Diacerein.
Citalopram The metabolism of Citalopram can be decreased when combined with Diacerein.
Ranolazine The metabolism of Ranolazine can be decreased when combined with Diacerein.
Benzatropine The metabolism of Benzatropine can be decreased when combined with Diacerein.
Metoprolol The metabolism of Metoprolol can be decreased when combined with Diacerein.
Bupivacaine The metabolism of Bupivacaine can be decreased when combined with Diacerein.
Gefitinib The metabolism of Gefitinib can be decreased when combined with Diacerein.
Codeine The metabolism of Codeine can be decreased when combined with Diacerein.
Atenolol The metabolism of Atenolol can be decreased when combined with Diacerein.
Terfenadine The metabolism of Terfenadine can be decreased when combined with Diacerein.
Palonosetron The metabolism of Palonosetron can be decreased when combined with Diacerein.
Remoxipride The metabolism of Remoxipride can be decreased when combined with Diacerein.
Prochlorperazine The metabolism of Prochlorperazine can be decreased when combined with Diacerein.
Buspirone The metabolism of Buspirone can be decreased when combined with Diacerein.
Darifenacin The metabolism of Darifenacin can be decreased when combined with Diacerein.
Oxycodone The metabolism of Oxycodone can be decreased when combined with Diacerein.
Ritonavir The metabolism of Ritonavir can be decreased when combined with Diacerein.
Lisuride The metabolism of Lisuride can be decreased when combined with Diacerein.
Piperazine The metabolism of Piperazine can be decreased when combined with Diacerein.
Chloroquine The metabolism of Chloroquine can be decreased when combined with Diacerein.
Simvastatin The metabolism of Simvastatin can be decreased when combined with Diacerein.
Dextropropoxyphene The metabolism of Dextropropoxyphene can be decreased when combined with Diacerein.
Trazodone The metabolism of Trazodone can be decreased when combined with Diacerein.
Galantamine The metabolism of Galantamine can be decreased when combined with Diacerein.
Thioridazine The metabolism of Thioridazine can be decreased when combined with Diacerein.
Nicergoline The metabolism of Nicergoline can be decreased when combined with Diacerein.
Delavirdine The metabolism of Delavirdine can be decreased when combined with Diacerein.
Tamsulosin The metabolism of Tamsulosin can be decreased when combined with Diacerein.
Risperidone The metabolism of Risperidone can be decreased when combined with Diacerein.
Meclizine The metabolism of Meclizine can be decreased when combined with Diacerein.
Pentamidine The metabolism of Pentamidine can be decreased when combined with Diacerein.
Minaprine The metabolism of Minaprine can be decreased when combined with Diacerein.
Alprenolol The metabolism of Alprenolol can be decreased when combined with Diacerein.
Phenformin The metabolism of Phenformin can be decreased when combined with Diacerein.
Almotriptan The metabolism of Almotriptan can be decreased when combined with Diacerein.
Tipranavir The metabolism of Tipranavir can be decreased when combined with Diacerein.
Mesoridazine The metabolism of Mesoridazine can be decreased when combined with Diacerein.
Hydrocodone The metabolism of Hydrocodone can be decreased when combined with Diacerein.
Pindolol The metabolism of Pindolol can be decreased when combined with Diacerein.
Promethazine The metabolism of Promethazine can be decreased when combined with Diacerein.
Mequitazine The metabolism of Mequitazine can be decreased when combined with Diacerein.
Perhexiline The metabolism of Perhexiline can be decreased when combined with Diacerein.
Tegaserod The metabolism of Tegaserod can be decreased when combined with Diacerein.
Chlorpheniramine The metabolism of Chlorpheniramine can be decreased when combined with Diacerein.
Nefazodone The metabolism of Nefazodone can be decreased when combined with Diacerein.
Escitalopram The metabolism of Escitalopram can be decreased when combined with Diacerein.
Oxymorphone The metabolism of Oxymorphone can be decreased when combined with Diacerein.
Acebutolol The metabolism of Acebutolol can be decreased when combined with Diacerein.
Nadolol The metabolism of Nadolol can be decreased when combined with Diacerein.
Quetiapine The metabolism of Quetiapine can be decreased when combined with Diacerein.
Encainide The metabolism of Encainide can be decreased when combined with Diacerein.
Metoclopramide The metabolism of Metoclopramide can be decreased when combined with Diacerein.
Bepridil The metabolism of Bepridil can be decreased when combined with Diacerein.
Lisdexamfetamine The serum concentration of dextroamphetamine, an active metabolite of Lisdexamfetamine, can be increased when used in combination with Diacerein.
Paliperidone The metabolism of Paliperidone can be decreased when combined with Diacerein.
Bevantolol The metabolism of Bevantolol can be decreased when combined with Diacerein.
Practolol The metabolism of Practolol can be decreased when combined with Diacerein.
Penbutolol The metabolism of Penbutolol can be decreased when combined with Diacerein.
Yohimbine The metabolism of Yohimbine can be decreased when combined with Diacerein.
Methotrimeprazine The metabolism of Methotrimeprazine can be decreased when combined with Diacerein.
Tiotropium The metabolism of Tiotropium can be decreased when combined with Diacerein.
Aprindine The metabolism of Aprindine can be decreased when combined with Diacerein.
Midomafetamine The metabolism of Midomafetamine can be decreased when combined with Diacerein.
Ethylmorphine The metabolism of Ethylmorphine can be decreased when combined with Diacerein.
4-Methoxyamphetamine The metabolism of 4-Methoxyamphetamine can be decreased when combined with Diacerein.
Dihydrocodeine The metabolism of Dihydrocodeine can be decreased when combined with Diacerein.
Dextroamphetamine The metabolism of Dextroamphetamine can be decreased when combined with Diacerein.
Metamfetamine The metabolism of Metamfetamine can be decreased when combined with Diacerein.
Oxprenolol The metabolism of Oxprenolol can be decreased when combined with Diacerein.
Solifenacin The metabolism of Solifenacin can be decreased when combined with Diacerein.
Pipotiazine The metabolism of Pipotiazine can be decreased when combined with Diacerein.
Zuclopenthixol The metabolism of Zuclopenthixol can be decreased when combined with Diacerein.

Target Protein

Interleukin-1 beta IL1B
Oxysterols receptor LXR-alpha NR1H3
Oxysterols receptor LXR-beta NR1H2
Arylamine N-acetyltransferase
Polyunsaturated fatty acid 5-lipoxygenase ALOX5
Cytochrome P450 1A2 CYP1A2
Cytochrome P450 3A Subfamily CYP3A4
Cytochrome P450 2E1 CYP2E1
Cytochrome P450 2C9 CYP2C9
Cytochrome P450 2D6 CYP2D6

Referensi & Sumber

Artikel (PubMed)
  • PMID: 9839088
    Nicolas P, Tod M, Padoin C, Petitjean O: Clinical pharmacokinetics of diacerein. Clin Pharmacokinet. 1998 Nov;35(5):347-59.
  • PMID: 2907037
    De Witte P, Lemli J: Excretion and distribution of 14Crhein and 14Crhein anthrone in rat. J Pharm Pharmacol. 1988 Sep;40(9):652-5.
  • PMID: 11327257
    Pelletier JP, Lajeunesse D, Reboul P, Mineau F, Fernandes JC, Sabouret P, Martel-Pelletier J: Diacerein reduces the excess synthesis of bone remodeling factors by human osteoblast cells from osteoarthritic subchondral bone. J Rheumatol. 2001 Apr;28(4):814-24.
  • PMID: 10806046
    Moldovan F, Pelletier JP, Jolicoeur FC, Cloutier JM, Martel-Pelletier J: Diacerhein and rhein reduce the ICE-induced IL-1beta and IL-18 activation in human osteoarthritic cartilage. Osteoarthritis Cartilage. 2000 May;8(3):186-96.
  • PMID: 11300749
    Tamura T, Kosaka N, Ishiwa J, Sato T, Nagase H, Ito A: Rhein, an active metabolite of diacerein, down-regulates the production of pro-matrix metalloproteinases-1, -3, -9 and -13 and up-regulates the production of tissue inhibitor of metalloproteinase-1 in cultured rabbit articular chondrocytes. Osteoarthritis Cartilage. 2001 Apr;9(3):257-63.

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Sekuens Gen/Protein (FASTA)

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