Tìm theo
Retapamulin
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 224452-66-8
ĐG : GlaxoSmithKline Inc. , http://www.gsk.com
CTHH: C30H47NO4S
PTK: 517.763
Retapamulin is a topical antibiotic developed by GlaxoSmithKline. It was approved by the United States Food and Drug Administration in April 2007 for the treatment of bacterial skin infections such as impetigo. It is marketed as an ointment under the name brand Altabax.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C30H47NO4S
Phân tử khối
517.763
Monoisotopic mass
517.322579687
InChI
InChI=1S/C30H47NO4S/c1-7-28(4)16-24(35-25(33)17-36-22-14-20-8-9-21(15-22)31(20)6)29(5)18(2)10-12-30(19(3)27(28)34)13-11-23(32)26(29)30/h7,18-22,24,26-27,34H,1,8-17H2,2-6H3/t18-,19+,20-,21+,22?,24-,26+,27+,28-,29+,30+/m1/s1
InChI Key
InChIKey=STZYTFJPGGDRJD-FJJJPKKESA-N
IUPAC Name
(1S,2R,3S,4S,6R,7R,8R,14R)-4-ethenyl-3-hydroxy-2,4,7,14-tetramethyl-9-oxotricyclo[5.4.3.0^{1,8}]tetradecan-6-yl 2-{[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]sulfanyl}acetate
Traditional IUPAC Name
retapamulin
SMILES
C[C@@H]1CC[C@@]23CCC(=O)[C@H]2[C@]1(C)[C@@H](C[C@@](C)(C=C)[C@@H](O)[C@@H]3C)OC(=O)CSC1C[C@@H]2CC[C@H](C1)N2C
Độ hòa tan
3.94e-04 g/l
logP
5
logS
-6.1
pKa (strongest acidic)
14.43
pKa (Strongest Basic)
9.69
PSA
66.84 Å2
Refractivity
145.45 m3·mol-1
Polarizability
59.49 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
5
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Retapamulin is a semisynthetic pleuromutilin antibiotic. This drug is usually bacteriostatic in action, but may become bactericidal at highed concentrations (when MBC is 1000 times higher than MIC). Retapamulin acts by selectively inhibiting the initiation of protein synthesis in bacteria at the level of bacterial 50S ribosome.
Cơ Chế Tác Dụng : Retapamulin is a topical antibiotic developed by GlaxoSmithKline. It was approved by the United States Food and Drug Administration in April 2007 for the treatment of bacterial skin infections such as impetigo. It is marketed as an ointment under the name brand Altabax. Retapamulin is a bacterial protein synthesis inhibitor belonging to a class of compounds called pleuromutilins. These compounds inhibit the initiation of protein synthesis by binding to a specific site on the 50S subunit of bacterial ribosome (domain V of 23S rRNA). This binding site involves ribosomal protein L3 and is in the region of the ribosomal P site and peptidyl transferase center. By virtue of binding to this site, pleuromutilins inhibit peptidyl transfer, block P-site interactions, and prevent the normal formation of active 50S ribosomal subunits.
Dược Động Học :

▧ Protein binding :
Retapamulin is approximately 94% bound to human plasma proteins, and the protein binding is independent of concentration.
▧ Metabolism :
In vitro studies with human liver microsomes demonstrated that retapamulin is extensively metabolized to numerous metabolites, of which the predominant routes of metabolism were mono-oxygenation and N-demethylation. The major enzyme responsible for metabolism of retapamulin in human liver microsomes was cytochrome P450 3A4 (CYP3A4).
Chỉ Định : For use in adults and pediatric patients aged 9 months and older for the topical treatment of impetigo (up to 100 cm2 in total area in adults or 2% total body surface area in pediatric patients aged 9 months or older) due to Staphylococcus aureus (methicillin-susceptible isolates only) or Streptococcus pyogenes.
Liều Lượng & Cách Dùng : Ointment - Topical - 10 mg/g
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Altabax 1% ointment
    Giá bán buôn : USD >8.64
    Đơn vị tính : g
Nhà Sản Xuất
  • Công ty : Glaxo
    Sản phẩm biệt dược : Altabax
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01256
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0007-5180-05
PharmGKB
http://www.pharmgkb.org/drug/PA164749341
Wikipedia
http://en.wikipedia.org/wiki/Retapamulin
RxList
http://www.rxlist.com/cgi/generic/altabax.htm
Drugs.com
http://www.drugs.com/cdi/retapamulin-ointment.html
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