Peringatan Keamanan

Toxicity information regarding daptomycin is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as myopathy, rhabdomyolysis, muscular/neurological system symptoms, eosinophilic pneumonia, tubulointerstitial nephritis, vomiting/diarrhea, abdominal pain, headache, dizziness, pyrexia, sweating, and pruritus. Symptomatic and supportive measures are recommended, including maintenance of glomerular filtration. Due to its high serum protein binding, daptomycin is not easily removed by hemodialysis (~15% of a dose over four hours) or peritoneal dialysis (~11% of a dose over 48 hours). High-flux membranes in hemodialysis may improve the quantity of daptomycin removed using this approach.L32534

Daptomycin

DB00080

small molecule approved investigational

Deskripsi

Daptomycin is a cyclic lipopeptide antibacterial agent with a broad spectrum of activity against Gram-positive bacteria, including methicillin-susceptible and -resistant Staphylococcus aureus (MSSA/MRSA) and vancomycin-resistant Enterococci (VRE).A231379, A231384, L32534 Chemically, daptomycin comprises 13 amino acids, including several non-standard and D-amino acids, with the C-terminal 10 amino acids forming an ester-linked ring and the N-terminal tryptophan covalently bonded to decanoic acid.A231374, L32534 Daptomycin was first discovered in the early 1980s by researchers at Eli Lilly in soil samples from Mount Ararat in Turkey.A231384 Early work on developing daptomycin was abandoned due to observed myopathy but was resumed in 1997 when Cubist Pharmaceuticals Inc. licensed daptomycin; it was found that a once-daily dosing scheme reduced side effects while retaining efficacy.A231379

Daptomycin was approved by the FDA on September 12, 2003, and is marketed under the name CUBICIN® by Cubist Pharmaceuticals LLC (Merck & Co.).L32534

Struktur Molekul 2D

Berat 1620.693
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Daptomycin has a relatively long half-life, with ranges of 7.5-9 hours depending on dosing schemes and dose strength.[A231449, L32534] The half-life lengthens in patients with increasing renal impairment, being 27.83 ± 14.85 hours in patients with creatinine clearance <30 mL/min, 30.51 ± 6.51 hours in hemodialysis patients, and 27.56 ± 4.53 hours in continuous ambulatory peritoneal dialysis (CAPD) patients. Daptomycin half-life also tends to decrease with decreasing age.[L32534]
Volume Distribusi Daptomycin has a very small volume of distribution, averaging ~0.1 L/kg in healthy adult subjects independent of dose.[A231449, L32534] The volume of distribution tends to increase with decreasing renal function, being estimated at ~0.2 L/kg in patients with severe renal impairment.[L32534]
Klirens (Clearance) Daptomycin administered as a 30 minute IV infusion to healthy volunteers in doses of 4, 6, 8, 10, and 12 mg/kg once daily resulted in total plasma clearance values between 7.2 ± 1.1 and 9.6 ± 1.3 mL/h/kg, with no clear dose association.[A231449, L32534] As daptomycin is primarily renally excreted, patients with mild, moderate, and severe renal impairment had reduced total plasma clearance 9, 22, and 46 percent lower than healthy controls, respectively. Daptomycin clearance was also lower in obese (15-23%) and geriatric (aged 75 and older, by 35%) patients, whereas it tended to be higher in pediatric patients, even when normalized for body weight.[L32534]

Absorpsi

Daptomycin administered as a 30 minute IV infusion to healthy volunteers in doses of 4, 6, 8, 10, and 12 mg/kg once daily resulted in a Cmax between 57.8 ± 3.0 and 183.7 ± 25.0 ?g/mL and an AUC0-24 of between 494 ± 75 and 1277 ± 253 ?g\*h/mL.A231449, L32534 Daptomycin pharmacokinetics are generally linear, with some variation observed above 6 mg/kg, and the Cmax and AUC values are approximately 20% higher at steady-state, suggesting some accumulation.A231449 Steady-state trough concentrations between 5.9 ± 1.6 and 13.7 ± 5.2 ?g/mL are reached following the third once-daily dose.L32534 The data for a single daptomycin dose of 6 mg/kg administered IV over 30 minutes was used to estimate steady-state Cmax values for both 4 and 6 mg/kg doses administered over two minutes, which were estimated at 77.7 ± 8.1 and 116.6 ± 12.2 ?g/mL, respectively. Administration of IV daptomycin (4 or 6 mg/kg) over two minutes did not allow for measurement of the Cmax but resulted in steady-state AUC values of 475 ± 71 and 701 ± 82 ?g\*h/mL.L32534 Patients with severe renal impairment and those on dialysis had mean steady-state AUC values approximately 2-3 times higher than those with normal renal function. No clinically significant differences in daptomycin pharmacokinetics were observed in patients with mild to moderate hepatic impairment. The mean AUC0-? obtained in healthy elderly individuals (75 years of age and older) was approximately 58% higher than in healthy young adult controls, with no difference in Cmax. The AUC0-? is also increased in obese patients by approximately 30%. No significant differences in body weight- and age-adjusted Cmax or AUC was observed in pediatric patients.L32534

Metabolisme

Radiolabeled daptomycin administered to five healthy adults revealed the presence of inactive metabolites in the urine. A separate study using 6 mg/kg daptomycin in healthy adults revealed small amounts of three oxidative and one unidentified metabolite(s) in urine but not in plasma.L32534 The site of metabolism is unclear, as studies using human hepatocytes suggest that daptomycin effectively does not interact at all with the various CYP450 enzymes present in the liver.A231474, L32534

Rute Eliminasi

Daptomycin is excreted primarily by the kidneys, approximately 78% of an administered dose recovered in urine and only 5.7% recovered in feces.A231449, L32534 Approximately 52% of the dose, recovered in urine, retains microbiological activity.L32534

Interaksi Obat

1034 Data
Ranolazine The serum concentration of Daptomycin can be increased when it is combined with Ranolazine.
Pravastatin The risk or severity of myopathy can be increased when Pravastatin is combined with Daptomycin.
Lovastatin The risk or severity of myopathy can be increased when Lovastatin is combined with Daptomycin.
Cerivastatin The risk or severity of myopathy can be increased when Cerivastatin is combined with Daptomycin.
Simvastatin The risk or severity of myopathy can be increased when Simvastatin is combined with Daptomycin.
Atorvastatin The risk or severity of myopathy can be increased when Atorvastatin is combined with Daptomycin.
Fluvastatin The risk or severity of myopathy can be increased when Fluvastatin is combined with Daptomycin.
Rosuvastatin The risk or severity of myopathy can be increased when Rosuvastatin is combined with Daptomycin.
Mevastatin The risk or severity of myopathy can be increased when Mevastatin is combined with Daptomycin.
Pitavastatin The risk or severity of myopathy can be increased when Pitavastatin is combined with Daptomycin.
Lumacaftor The serum concentration of Daptomycin can be decreased when it is combined with Lumacaftor.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Daptomycin.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Daptomycin.
Vemurafenib The serum concentration of Daptomycin can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Daptomycin can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Daptomycin can be increased when it is combined with Pitolisant.
Isavuconazonium The serum concentration of Daptomycin can be increased when it is combined with Isavuconazonium.
Isavuconazole The serum concentration of Daptomycin can be increased when it is combined with Isavuconazole.
Cyclosporine The serum concentration of Daptomycin can be increased when it is combined with Cyclosporine.
Tacrolimus The serum concentration of Daptomycin can be increased when it is combined with Tacrolimus.
Lopinavir The serum concentration of Daptomycin can be increased when it is combined with Lopinavir.
Fluconazole The serum concentration of Daptomycin can be increased when it is combined with Fluconazole.
Reserpine The serum concentration of Daptomycin can be increased when it is combined with Reserpine.
Sorafenib The serum concentration of Daptomycin can be increased when it is combined with Sorafenib.
Verapamil The serum concentration of Daptomycin can be increased when it is combined with Verapamil.
Arsenic trioxide The serum concentration of Daptomycin can be increased when it is combined with Arsenic trioxide.
Paliperidone The serum concentration of Daptomycin can be increased when it is combined with Paliperidone.
Mirabegron The serum concentration of Daptomycin can be increased when it is combined with Mirabegron.
Enzalutamide Daptomycin may decrease the excretion rate of Enzalutamide which could result in a higher serum level.
Ledipasvir The serum concentration of Daptomycin can be increased when it is combined with Ledipasvir.
Methylene blue The serum concentration of Daptomycin can be increased when it is combined with Methylene blue.
Erythromycin The serum concentration of Daptomycin can be increased when it is combined with Erythromycin.
Sapropterin The serum concentration of Daptomycin can be increased when it is combined with Sapropterin.
Loxapine The serum concentration of Daptomycin can be increased when it is combined with Loxapine.
Quinine The serum concentration of Daptomycin can be increased when it is combined with Quinine.
Toremifene The serum concentration of Daptomycin can be increased when it is combined with Toremifene.
Tamoxifen The serum concentration of Daptomycin can be increased when it is combined with Tamoxifen.
Mifepristone The serum concentration of Daptomycin can be increased when it is combined with Mifepristone.
Clofazimine The serum concentration of Daptomycin can be increased when it is combined with Clofazimine.
Vardenafil The serum concentration of Daptomycin can be increased when it is combined with Vardenafil.
Tipranavir The serum concentration of Daptomycin can be increased when it is combined with Tipranavir.
Norgestimate The serum concentration of Daptomycin can be increased when it is combined with Norgestimate.
Ketoconazole The serum concentration of Daptomycin can be increased when it is combined with Ketoconazole.
Carvedilol The serum concentration of Daptomycin can be increased when it is combined with Carvedilol.
Itraconazole The serum concentration of Daptomycin can be increased when it is combined with Itraconazole.
Propafenone The serum concentration of Daptomycin can be increased when it is combined with Propafenone.
Clarithromycin The serum concentration of Daptomycin can be increased when it is combined with Clarithromycin.
Lapatinib The serum concentration of Daptomycin can be increased when it is combined with Lapatinib.
Mibefradil The serum concentration of Daptomycin can be increased when it is combined with Mibefradil.
Everolimus The serum concentration of Daptomycin can be increased when it is combined with Everolimus.
Ixabepilone The serum concentration of Daptomycin can be increased when it is combined with Ixabepilone.
Biricodar The serum concentration of Daptomycin can be increased when it is combined with Biricodar.
Dronedarone The serum concentration of Daptomycin can be increased when it is combined with Dronedarone.
Nilotinib The serum concentration of Daptomycin can be increased when it is combined with Nilotinib.
Elacridar The serum concentration of Daptomycin can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Daptomycin can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Daptomycin can be increased when it is combined with Vandetanib.
Telaprevir The serum concentration of Daptomycin can be increased when it is combined with Telaprevir.
Zosuquidar The serum concentration of Daptomycin can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Daptomycin can be increased when it is combined with Tariquidar.
Temsirolimus The serum concentration of Daptomycin can be increased when it is combined with Temsirolimus.
Simeprevir The serum concentration of Daptomycin can be increased when it is combined with Simeprevir.
Cethromycin The serum concentration of Daptomycin can be increased when it is combined with Cethromycin.
Lonafarnib The serum concentration of Daptomycin can be increased when it is combined with Lonafarnib.
Brefeldin A The serum concentration of Daptomycin can be increased when it is combined with Brefeldin A.
Ticagrelor The serum concentration of Daptomycin can be increased when it is combined with Ticagrelor.
Ivacaftor The serum concentration of Daptomycin can be increased when it is combined with Ivacaftor.
Lomitapide The serum concentration of Daptomycin can be increased when it is combined with Lomitapide.
Crizotinib The serum concentration of Daptomycin can be increased when it is combined with Crizotinib.
Linagliptin The serum concentration of Daptomycin can be increased when it is combined with Linagliptin.
Carfilzomib The serum concentration of Daptomycin can be increased when it is combined with Carfilzomib.
Regorafenib The serum concentration of Daptomycin can be increased when it is combined with Regorafenib.
Ponatinib The serum concentration of Daptomycin can be increased when it is combined with Ponatinib.
Afatinib The serum concentration of Daptomycin can be increased when it is combined with Afatinib.
Diosmin The serum concentration of Daptomycin can be increased when it is combined with Diosmin.
Vorapaxar The serum concentration of Daptomycin can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Daptomycin can be increased when it is combined with Suvorexant.
Eliglustat The serum concentration of Daptomycin can be increased when it is combined with Eliglustat.
Netupitant The serum concentration of Daptomycin can be increased when it is combined with Netupitant.
Cobicistat The serum concentration of Daptomycin can be increased when it is combined with Cobicistat.
Palbociclib The serum concentration of Daptomycin can be increased when it is combined with Palbociclib.
Daclatasvir The serum concentration of Daptomycin can be increased when it is combined with Daclatasvir.
Niguldipine The serum concentration of Daptomycin can be increased when it is combined with Niguldipine.
Rolapitant The serum concentration of Daptomycin can be increased when it is combined with Rolapitant.
Venetoclax The serum concentration of Daptomycin can be increased when it is combined with Venetoclax.
Asunaprevir The serum concentration of Daptomycin can be increased when it is combined with Asunaprevir.
Velpatasvir The serum concentration of Daptomycin can be increased when it is combined with Velpatasvir.
Voclosporin The serum concentration of Daptomycin can be increased when it is combined with Voclosporin.
Istradefylline The serum concentration of Daptomycin can be increased when it is combined with Istradefylline.
Neratinib The serum concentration of Daptomycin can be increased when it is combined with Neratinib.
Valspodar The serum concentration of Daptomycin can be increased when it is combined with Valspodar.
Dacomitinib The serum concentration of Daptomycin can be increased when it is combined with Dacomitinib.
Glasdegib The serum concentration of Daptomycin can be increased when it is combined with Glasdegib.
Elagolix The serum concentration of Daptomycin can be increased when it is combined with Elagolix.
Entrectinib The serum concentration of Daptomycin can be increased when it is combined with Entrectinib.
Voxilaprevir The serum concentration of Daptomycin can be increased when it is combined with Voxilaprevir.
Sarecycline The serum concentration of Daptomycin can be increased when it is combined with Sarecycline.
Favipiravir The serum concentration of Daptomycin can be increased when it is combined with Favipiravir.
Fedratinib The serum concentration of Daptomycin can be increased when it is combined with Fedratinib.
Laniquidar The serum concentration of Daptomycin can be increased when it is combined with Laniquidar.

Target Protein

Dihydropteroate synthase folP
Cytoplasmic membrane

Referensi & Sumber

Synthesis reference: Dennis Keith, "Methods for preparing purified daptomycin." U.S. Patent US20030045484, issued March 06, 2003.
Artikel (PubMed)
  • PMID: 1318678
    Woodworth JR, Nyhart EH Jr, Brier GL, Wolny JD, Black HR: Single-dose pharmacokinetics and antibacterial activity of daptomycin, a new lipopeptide antibiotic, in healthy volunteers. Antimicrob Agents Chemother. 1992 Feb;36(2):318-25.
  • PMID: 11020247
    Tally FP, DeBruin MF: Development of daptomycin for gram-positive infections. J Antimicrob Chemother. 2000 Oct;46(4):523-6.
  • PMID: 15540967
    Charles PG, Grayson ML: The dearth of new antibiotic development: why we should be worried and what we can do about it. Med J Aust. 2004 Nov 15;181(10):549-53.
  • PMID: 16914701
    Fowler VG Jr, Boucher HW, Corey GR, Abrutyn E, Karchmer AW, Rupp ME, Levine DP, Chambers HF, Tally FP, Vigliani GA, Cabell CH, Link AS, DeMeyer I, Filler SG, Zervos M, Cook P, Parsonnet J, Bernstein JM, Price CS, Forrest GN, Fatkenheuer G, Gareca M, Rehm SJ, Brodt HR, Tice A, Cosgrove SE: Daptomycin versus standard therapy for bacteremia and endocarditis caused by Staphylococcus aureus. N Engl J Med. 2006 Aug 17;355(7):653-65.
  • PMID: 16805723
    Lee SY, Fan HW, Kuti JL, Nicolau DP: Update on daptomycin: the first approved lipopeptide antibiotic. Expert Opin Pharmacother. 2006 Jul;7(10):1381-97.
  • PMID: 29059358
    Heidary M, Khosravi AD, Khoshnood S, Nasiri MJ, Soleimani S, Goudarzi M: Daptomycin. J Antimicrob Chemother. 2018 Jan 1;73(1):1-11. doi: 10.1093/jac/dkx349.
  • PMID: 27288182
    Taylor SD, Palmer M: The action mechanism of daptomycin. Bioorg Med Chem. 2016 Dec 15;24(24):6253-6268. doi: 10.1016/j.bmc.2016.05.052. Epub 2016 May 28.
  • PMID: 32687352
    Karas JA, Carter GP, Howden BP, Turner AM, Paulin OKA, Swarbrick JD, Baker MA, Li J, Velkov T: Structure-Activity Relationships of Daptomycin Lipopeptides. J Med Chem. 2020 Nov 25;63(22):13266-13290. doi: 10.1021/acs.jmedchem.0c00780. Epub 2020 Aug 6.
Menampilkan 8 dari 20 artikel.

Contoh Produk & Brand

Produk: 80 • International brands: 2
Produk
  • Cubicin
    Injection, powder, lyophilized, for solution • 500 mg/10mL • Intravenous • US • Approved
  • Cubicin
    Injection • 350 mg/350mg • Intravenous • US
  • Cubicin
    Powder, for solution • 500 mg / vial • Intravenous • Canada • Approved
  • Cubicin
    - • 350 mg • Intravenous • EU • Approved
  • Cubicin
    Solution • 500 mg • Intravenous • EU • Approved
  • Cubicin
    - • 350 mg • Intravenous • EU • Approved
  • Cubicin
    Solution • 500 mg • Intravenous • EU • Approved
  • Cubicin RF
    Injection, powder, lyophilized, for solution • 500 mg/10mL • Intravenous • US • Approved
Menampilkan 8 dari 80 produk.
International Brands
  • Cidecin
  • Cubicin

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