Peringatan Keamanan

Treatment with antibacterial agents can alter the normal flora of the colon leading to growth of C. difficile and commonly occurs in the development of C. difficile-associated diarrhea FDA Label, F2356. Other common side effects include nausea, vomiting, diarrhea, headache, rash, and pruritis FDA Label, F2356. Side effects that occurred in less than 2% of patients during clinical trials include blood and lymphatic system disorders, gastrointestinal disorders, hepatotoxicity, anaphylactoid reactions, hepatic enzyme elevation, hypoglycaemia, dizziness, bronchospasm, urticaria, and vascular disorders FDA Label, F2356. There have been no adequate or well-controlled studies to conclude that use of dalbavancin is safe during pregnancy or breastfeeding FDA Label, F2356.

Dalbavancin

DB06219

small molecule approved investigational

Deskripsi

Dalbavancin is a second-generation lipoglycopeptide antibiotic that was designed to improve on the natural glycopeptides currently available, such as vancomycin and teicoplanin A4072, A4073. Modifications from these older glycoprotein classes facilitated a similar mechanism of action for dalbavancin but with increased activity and once-weekly dosing FDA Label, F2356, A4072, A4073. Its use is indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by the following gram-positive microorganisms: Staphylococcus aureus (including methicillin-susceptible and methicillin-resistant strains), S. pyogenes, S. agalactiae, S. dysgalactiae, the S. anginosus group (including S. anginosus, S. intermedius, and S. constellatus), and Enterococcus faecalis (vancomycin susceptible strains) FDA Label, F2356. Dalbavancin acts by interfering with bacterial cell wall synthesis by binding to the D-alanyl-D-alanine terminus of nascent cell wall peptidoglycan and preventing cross-linking FDA Label, F2356, A4072, A4073.

Struktur Molekul 2D

Struktur tidak tersedia

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 346 hours [FDA Label, F2356].
Volume Distribusi Clearance and volume of distribution at steady state are comparable between healthy subjects and patients with infections [F2380]. The volume of distribution at steady state was similar to the volume of extracellular fluid [F2380].
Klirens (Clearance) 0.0513 L/h [FDA Label, F2356].

Absorpsi

In healthy subjects, dalbavancin AUC0-24h and Cmax both increased proportionally to dose following single intravenous (IV) dalbavancin doses ranging from 140 mg to 1500 mg, indicating linear pharmacokinetics FDA Label, F2356. No apparent accumulation of dalbavancin was observed following multiple IV infusions administered once weekly for up to eight weeks, with 1000 mg on Day 1 followed by up to seven weekly 500 mg doses, in healthy adults with normal renal function FDA Label, F2356.

Metabolisme

Dalbavancin is not a substrate, inhibitor, or inducer of CYP450 isoenzymes FDA Label, F2356. Subsequently, metabolites have not been observed in significant amounts in human plasma FDA Label, F2356. The metabolites hydroxy-dalbavancin and mannosyl aglycone have been detected in urine (< 25% of administered dose) FDA Label, F2356. The metabolic pathways responsible for producing these metabolites have not been identified; however, due to the relatively minor contribution of metabolism to the overall elimination of dalbavancin, drug-drug interactions via inhibition or induction of metabolism of dalbavancin are not anticipated FDA Label, F2356. Hydroxy-dalbavancin and mannosyl aglycone show significantly less antibacterial activity compared to dalbavancin FDA Label, F2356.

Rute Eliminasi

Following administration of a single 1000 mg dose in healthy subjects, an average of 33% of the administered dalbavancin dose was excreted in urine as unchanged dalbavancin and approximately 12% of the administered dose was excreted in urine as the metabolite hydroxy-dalbavancin through 42 days post-dose. Approximately 20% of the administered dose was excreted in feces through 70 days post-dose FDA Label, F2356.

Interaksi Obat

53 Data
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Dalbavancin.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Dalbavancin.
Dicoumarol The risk or severity of bleeding can be increased when Dalbavancin is combined with Dicoumarol.
Phenindione The risk or severity of bleeding can be increased when Dalbavancin is combined with Phenindione.
Warfarin The risk or severity of bleeding can be increased when Dalbavancin is combined with Warfarin.
Phenprocoumon The risk or severity of bleeding can be increased when Dalbavancin is combined with Phenprocoumon.
Acenocoumarol The risk or severity of bleeding can be increased when Dalbavancin is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Dalbavancin is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of bleeding can be increased when Dalbavancin is combined with Coumarin.
(R)-warfarin The risk or severity of bleeding can be increased when Dalbavancin is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Dalbavancin is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of bleeding can be increased when Dalbavancin is combined with Fluindione.
Clorindione The risk or severity of bleeding can be increased when Dalbavancin is combined with Clorindione.
Diphenadione The risk or severity of bleeding can be increased when Dalbavancin is combined with Diphenadione.
Tioclomarol The risk or severity of bleeding can be increased when Dalbavancin is combined with Tioclomarol.
(S)-Warfarin The risk or severity of bleeding can be increased when Dalbavancin is combined with (S)-Warfarin.
Vibrio cholerae CVD 103-HgR strain live antigen The therapeutic efficacy of Vibrio cholerae CVD 103-HgR strain live antigen can be decreased when used in combination with Dalbavancin.
Estetrol The therapeutic efficacy of Estetrol can be decreased when used in combination with Dalbavancin.
Lidocaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Quinisocaine.
Cisatracurium Dalbavancin may increase the neuromuscular blocking activities of Cisatracurium.
Ambroxol The risk or severity of methemoglobinemia can be increased when Dalbavancin is combined with Ambroxol.
Fecal microbiota The therapeutic efficacy of Fecal microbiota can be decreased when used in combination with Dalbavancin.

Target Protein

D-Ala-D-Ala moiety of NAM/NAG peptide subunits of peptidoglycan
Pancreatic triacylglycerol lipase PNLIP

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18359966
    Bailey J, Summers KM: Dalbavancin: a new lipoglycopeptide antibiotic. Am J Health Syst Pharm. 2008 Apr 1;65(7):599-610. doi: 10.2146/ajhp070255.
  • PMID: 18728718
    Bennett JW, Lewis JS, Ellis MW: Dalbavancin in the treatment of complicated skin and soft-tissue infections: a review. Ther Clin Risk Manag. 2008 Feb;4(1):31-40.
  • PMID: 25578881
    Leuthner KD, Yuen A, Mao Y, Rahbar A: Dalbavancin (BI-387) for the treatment of complicated skin and skin structure infection. Expert Rev Anti Infect Ther. 2015 Feb;13(2):149-59. doi: 10.1586/14787210.2015.995633.

Contoh Produk & Brand

Produk: 3 • International brands: 1
Produk
  • Dalvance
    Injection, powder, for solution • 500 mg/25mL • Intravenous • US • Approved
  • Xydalba
    Powder, for solution • 500 mg / vial • Intravenous • Canada • Approved
  • Xydalba
    Injection, powder, for solution • 500 mg • Intravenous • EU • Approved
International Brands
  • Zeven — Pfizer

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul