Peringatan Keamanan

Data regarding overdoses of artesunate are rare.L14099 Patients experiencing an overdose may present with pancytopenia, melena, seizures, multiorgan failure, and death.L14099 Treat overdose with symptomatic and supportive measures.L14099

Artesunate

DB09274

small molecule approved investigational

Deskripsi

Artesunate is indicated for the initial treatment of severe malaria.L14099 The World Health Organization recommends artesunate as first line treatment for severe malaria.L890 Artesunate was developed out of a need for a more hydrophilic derivative of artemisinin.A203948

Artesunate was granted FDA approval on 26 May 2020.L14099

Struktur Molekul 2D

Berat 384.425
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half life of artesunate is 0.3h with a range of 0.1-1.8h.[L14099] The elimination half life of DHA is 1.3h with a range of 0.9-2.9h.[L14099] Half life after intramuscular administration is 48 min in children and 41 min in adults.[L891]
Volume Distribusi The volume of distribution of artesunate is 68.5L while the volume of distribution of DHA is 59.7L.[L14099]
Klirens (Clearance) The clearance of artesunate is 180L/h while the clearance of DHA is 32.3L/h.[L14099]

Absorpsi

The Cmax of artesunate is 3.3µg/mL while the Cmax of the active metabolite DHA is 3.1µg/mL.L14099 The AUC of artesunate is 0.7µg\*h/mL while the AUC of DHA is 3.5µg\*h/mL.L14099 After intravenous artesunate, DHA has a Tmax of 0.5-15 minutes in adult patients and 21-64 minutes in pediatric patients.L891 Intramuscular artesunate has a Tmax of 8-12 minutes.L891 Infants less than 6 months old will have a higher AUC due to an undeveloped UGT metabolic pathway.L14099

Metabolisme

Artesunate is rapidly metabolized to dihydroartemisinin (DHA) by plasma esterases.L14099 DHA is glucuronidated by UGT1A9 and UGT2B7 to DHA-glucuronide.A203894,L14099 DHA-glucuronide can undergo a minor metabolic pathway to for a furano acetate derivative of DHA-glucuronide.A203894 CYP2A6 may minorly contribute to the metabolism of artesunate.L891

Rute Eliminasi

The main route of elimination in humans is unknown.L14099 In rats, a dose of artesunate is 56.1% eliminated in the urine and 38.5% in the feces.A203906

Interaksi Obat

95 Data
Artemether The risk or severity of QTc prolongation can be increased when Artesunate is combined with Artemether.
Lumefantrine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Lumefantrine.
Thiethylperazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Thiethylperazine.
Promazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Promazine.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Prochlorperazine.
Triflupromazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Triflupromazine.
Fluphenazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Fluphenazine.
Thioridazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Thioridazine.
Moricizine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Moricizine.
Trifluoperazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Trifluoperazine.
Perphenazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Perphenazine.
Mesoridazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Mesoridazine.
Acetophenazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Acetophenazine.
Promethazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Promethazine.
Alimemazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Alimemazine.
Methotrimeprazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Methotrimeprazine.
Periciazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Periciazine.
Acepromazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Acepromazine.
Aceprometazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Aceprometazine.
Pipotiazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Pipotiazine.
Thioproperazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Thioproperazine.
BL-1020 The risk or severity of QTc prolongation can be increased when Artesunate is combined with BL-1020.
Cyamemazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Cyamemazine.
Propiopromazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Propiopromazine.
Perazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Perazine.
Butaperazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Butaperazine.
Chlorproethazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Chlorproethazine.
Thiazinam The risk or severity of QTc prolongation can be increased when Artesunate is combined with Thiazinam.
Dixyrazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Dixyrazine.
Perphenazine enanthate The risk or severity of QTc prolongation can be increased when Artesunate is combined with Perphenazine enanthate.
Chlorpromazine The risk or severity of QTc prolongation can be increased when Artesunate is combined with Chlorpromazine.
Methylene blue The risk or severity of QTc prolongation can be increased when Artesunate is combined with Methylene blue.
Dapsone The risk or severity of adverse effects can be increased when Artesunate is combined with Dapsone.
Vemurafenib The risk or severity of QTc prolongation can be increased when Vemurafenib is combined with Artesunate.
Phenytoin The metabolism of Artesunate can be decreased when combined with Phenytoin.
Sorafenib The metabolism of Artesunate can be decreased when combined with Sorafenib.
Mefenamic acid The metabolism of Artesunate can be decreased when combined with Mefenamic acid.
Diflunisal The metabolism of Artesunate can be decreased when combined with Diflunisal.
Rifampin The metabolism of Artesunate can be decreased when combined with Rifampicin.
Fosphenytoin The metabolism of Artesunate can be decreased when combined with Fosphenytoin.
Deferasirox The metabolism of Artesunate can be decreased when combined with Deferasirox.
Eltrombopag The metabolism of Artesunate can be decreased when combined with Eltrombopag.
Regorafenib The metabolism of Artesunate can be decreased when combined with Regorafenib.
Isavuconazole The metabolism of Artesunate can be decreased when combined with Isavuconazole.
Umifenovir The metabolism of Artesunate can be decreased when combined with Umifenovir.
Niflumic acid The metabolism of Artesunate can be decreased when combined with Niflumic acid.
Cannabidiol The metabolism of Artesunate can be decreased when combined with Cannabidiol.
Indomethacin The metabolism of Artesunate can be decreased when combined with Indomethacin.
Ketoconazole The metabolism of Artesunate can be decreased when combined with Ketoconazole.
Flunitrazepam The metabolism of Artesunate can be decreased when combined with Flunitrazepam.
Dovitinib The metabolism of Artesunate can be decreased when combined with Dovitinib.
Chenodeoxycholic acid The metabolism of Artesunate can be decreased when combined with Chenodeoxycholic acid.
Phenobarbital The metabolism of Artesunate can be increased when combined with Phenobarbital.
Ritonavir The serum concentration of Artesunate can be decreased when it is combined with Ritonavir.
Nevirapine The serum concentration of the active metabolites of Artesunate can be reduced when Artesunate is used in combination with Nevirapine resulting in a loss in efficacy.
Mefloquine Mefloquine may increase the QTc-prolonging activities of Artesunate.
Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Artesunate.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Artesunate.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Artesunate.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Artesunate.
Cannabinol The metabolism of Artesunate can be increased when combined with Cannabinol.
Lidocaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Quinisocaine.
Ambroxol The risk or severity of methemoglobinemia can be increased when Artesunate is combined with Ambroxol.
Etrasimod The risk or severity of immunosuppression can be increased when Artesunate is combined with Etrasimod.

Target Protein

Malaria protein EXP-1 EXP-1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25126794
    Lisewski AM, Quiros JP, Ng CL, Adikesavan AK, Miura K, Putluri N, Eastman RT, Scanfeld D, Regenbogen SJ, Altenhofen L, Llinas M, Sreekumar A, Long C, Fidock DA, Lichtarge O: Supergenomic network compression and the discovery of EXP1 as a glutathione transferase inhibited by artesunate. Cell. 2014 Aug 14;158(4):916-28. doi: 10.1016/j.cell.2014.07.011.
  • PMID: 12167566
    Ilett KF, Ethell BT, Maggs JL, Davis TM, Batty KT, Burchell B, Binh TQ, Thu le TA, Hung NC, Pirmohamed M, Park BK, Edwards G: Glucuronidation of dihydroartemisinin in vivo and by human liver microsomes and expressed UDP-glucuronosyltransferases. Drug Metab Dispos. 2002 Sep;30(9):1005-12. doi: 10.1124/dmd.30.9.1005.
  • PMID: 17123971
    Li Q, Xie LH, Haeberle A, Zhang J, Weina P: The evaluation of radiolabeled artesunate on tissue distribution in rats and protein binding in humans. Am J Trop Med Hyg. 2006 Nov;75(5):817-26.
  • PMID: 23684544
    Veerappan A, Eichhorn T, Zeino M, Efferth T, Schneider D: Differential interactions of the broad spectrum drugs artemisinin, dihydroartemisinin and artesunate with serum albumin. Phytomedicine. 2013 Aug 15;20(11):969-74. doi: 10.1016/j.phymed.2013.04.003. Epub 2013 May 16.
  • PMID: 26776328
    White NJ, Hien TT, Nosten FH: A Brief History of Qinghaosu. Trends Parasitol. 2015 Dec;31(12):607-610. doi: 10.1016/j.pt.2015.10.010.

Contoh Produk & Brand

Produk: 5 • International brands: 0
Produk
  • Artesunate
    Injection; Kit • - • Parenteral • US • Approved
  • Artesunate
    Injection; Kit • - • Parenteral • US • Approved
  • Artesunate
    Injection, powder, for solution; Kit • 110 mg/1 • Parenteral • US • Approved
  • Artesunate - Amivas
    Injection, powder, for solution • 110 mg • Intravenous • EU • Approved
  • Artesunate - Amivas
    Injection, powder, for solution • 110 mg • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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