Tìm theo
Daptomycin
Thuốc Gốc
Biotech
CAS: 103060-53-3
ATC: J01XX09
ĐG : Cardinal Health , http://www.cardinal.com
CTHH: C72H101N17O26
PTK: 1620.6706
Daptomycin is a lipopeptide antibiotic that kills susceptible gram positive bacteria by disrupting their membrane potential. It is a naturally-occurring compound found in the soil bacterium Streptomyces roseosporus. Antibiotics are used in the treatment of infections caused by bacteria. They work by killing bacteria or preventing their growth. Daptomycin will not work for colds, flu, or other virus infections. It was approved in September 2003 for the treatment of complicated skin and soft tissue infections. It has a safety profile similar to other agents commonly administered to treat gram-positive infections.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C72H101N17O26
Phân tử khối
1620.6706
Dược Lực Học : Daptomycin is a 13 member amino acid cyclic lipopeptide antibiotic active against Gram-positive bacteria only. It has proven in vitro activity against enterococci (including glycopeptide-resistant Enterococci (GRE)), staphylococci (including methicillin-resistant Staphylococcus aureus), streptococci and corynebacteria. Daptomycin is derived from the fermentation product of Streptomyces roseosporus.
Cơ Chế Tác Dụng : Daptomycin is a lipopeptide antibiotic that kills susceptible gram positive bacteria by disrupting their membrane potential. It is a naturally-occurring compound found in the soil bacterium Streptomyces roseosporus. Antibiotics are used in the treatment of infections caused by bacteria. They work by killing bacteria or preventing their growth. Daptomycin will not work for colds, flu, or other virus infections. It was approved in September 2003 for the treatment of complicated skin and soft tissue infections. It has a safety profile similar to other agents commonly administered to treat gram-positive infections. Daptomycin appears to bind or insert into the outer membrane of gram positive bacteria. The binding and integration of daptomycin into the cell membrane is calcium dependent. Calcium ions cause a conformational change in daptomycin, augmenting its amphipathicity (hydrophilic head group and hydrophobic tail group), leading to incorporation into the cell membrane. This binding causes rapid depolarisation, resulting in a loss of membrane potential leading to inhibition of protein, DNA and RNA synthesis, which results in bacterial cell death. The bactericidal activity of daptomycin is concentration-dependent. There is in vitro evidence of synergy with β-lactam antibiotics.
Dược Động Học :
▧ Absorption :
Generally exhibits linear and time-independent pharmacokinetics at a dosage of 4–12 mg/kg IV once every 24 hours. Steady-state trough serum concentrations are achieved by the third daily dose.
▧ Volume of Distribution :
* 0.1 L/Kg [healthy adult subjects]
▧ Protein binding :
Daptomycin is reversibly bound to human plasma proteins, primarily to serum albumin, in a concentration-independent manner. The overall mean binding ranged from 90 to 93%.
▧ Metabolism :
Minor amounts of three oxidative metabolites and one unidentified compound have been detected in urine. The site of metabolism has not been identified.
▧ Route of Elimination :
Daptomycin is excreted primarily by the kidney. In a mass balance study of 5 healthy subjects using radiolabeled daptomycin, approximately 78% of the administered dose was recovered from urine based on total radioactivity (approximately 52% of the dose based on microbiologically active concentrations) and 5.7% of the dose was recovered from feces (collected for up to 9 days) based on total radioactivity. Because renal excretion is the primary route of elimination, dosage adjustment is necessary in patients with severe renal insufficiency (CLCR <30 mL/min)
▧ Half Life :
Half-life elimination: 8-9 hours (up to 28 hours in renal impairment)
▧ Clearance :
Excreted primarily in the urine as unchanged drug (78%) and in the feces (6%)
Chỉ Định : For the treatment of complicated skin and skin structure infections caused by susceptible strains of Gram-positive microorganisms.
Liều Lượng & Cách Dùng : Injection, powder, lyophilized, for solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Cubicin 500 mg vial
    Giá bán buôn : USD >272.7
    Đơn vị tính : vial
Nhà Sản Xuất
  • Công ty : Novartis
    Sản phẩm biệt dược : Cubicin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00080
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C12013
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01080
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/67919-011-01
PharmGKB
http://www.pharmgkb.org/drug/PA164768820
Wikipedia
http://en.wikipedia.org/wiki/Daptomycin
RxList
http://www.rxlist.com/cgi/generic3/cubicin.htm
Drugs.com
http://www.drugs.com/cdi/daptomycin.html
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