Tìm theo
Oseltamivir
Các tên gọi khác (10 ) :
  • (-)-Oseltamivir
  • (−)-oseltamivir
  • 1-Cyclohexene-1-carboxylic acid, 4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-, ethyl ester, (3R-(3alpha,4beta,5alpha))-
  • Agucort
  • Ethyl (3R,4R,5S)-4-acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate
  • GS-4104
  • HSDB 7433
  • Oseltamivir
  • Oseltamivirum
  • Tamiflu
antiviral agents, enzyme inhibitors
Thuốc Gốc
Small Molecule
CAS: 204255-11-8
ATC: J05AH02
ĐG : A-S Medication Solutions LLC , http://orders.a-smeds.com
CTHH: C16H28N2O4
PTK: 312.4045
An acetamido cyclohexene that is a structural homolog of sialic acid and inhibits neuraminidase. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
312.4045
Monoisotopic mass
312.204907394
InChI
InChI=1S/C16H28N2O4/c1-5-12(6-2)22-14-9-11(16(20)21-7-3)8-13(17)15(14)18-10(4)19/h9,12-15H,5-8,17H2,1-4H3,(H,18,19)/t13-,14+,15+/m0/s1
InChI Key
InChIKey=VSZGPKBBMSAYNT-RRFJBIMHSA-N
IUPAC Name
ethyl (3R,4R,5S)-5-amino-4-acetamido-3-(pentan-3-yloxy)cyclohex-1-ene-1-carboxylate
Traditional IUPAC Name
oseltamivir
SMILES
CCOC(=O)C1=C[[email protected]@H](OC(CC)CC)[[email protected]](NC(C)=O)[[email protected]@H](N)C1
Độ hòa tan
Soluble
logP
1
logS
-2.7
pKa (strongest acidic)
14.03
pKa (Strongest Basic)
9.31
PSA
90.65 Å2
Refractivity
84.2 m3·mol-1
Polarizability
34.65 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Oseltamivir is an antiviral drug, a neuraminidase inhibitor used in the treatment and prophylaxis of both influenza A and influenza B. Oseltamivir is a prodrug (usually administered as phosphate), it is hydrolysed hepatically to the active metabolite, the free carboxylate of oseltamivir (GS4071). Like zanamivir, oseltamivir acts as a transition-state analogue inhibitor of influenza neuraminidase.
Cơ Chế Tác Dụng : An acetamido cyclohexene that is a structural homolog of sialic acid and inhibits neuraminidase. [PubChem] Oseltamivir is an ethyl ester prodrug requiring ester hydrolysis for conversion to the active form, oseltamivir carboxylate. The proposed mechanism of action of oseltamivir is inhibition of influenza virus neuraminidase with the possibility of alteration of virus particle aggregation and release.
Dược Động Học :
▧ Absorption :
Readily absorbed from the gastrointestinal tract after oral administration with a bioavailability of 75%.
▧ Volume of Distribution :
* 23 to 26 L
▧ Protein binding :
Oseltamivir carboxylate: low (3%), Oseltamivir free base: 42%.
▧ Metabolism :
Extensively converted to oseltamivir carboxylate by esterases located predominantly in the liver. Neither oseltamivir nor oseltamivir carboxylate is a substrate for, or inhibitor of, cytochrome P450 isoforms. At least 75% of an oral dose reaches the systemic circulation as oseltamivir carboxylate.
▧ Route of Elimination :
Absorbed oseltamivir is primarily (>90%) eliminated by conversion to oseltamivir carboxylate. Oseltamivir carboxylate is not further metabolized and is eliminated in the urine. Oseltamivir carboxylate is eliminated entirely (>99%) by renal excretion.
▧ Half Life :
1 to 3 hours in most subjects after oral administration.
Độc Tính : At present, there has been no experience with overdose. Single doses of up to 1000 mg of oseltamivir have been associated with nausea and/or vomiting. Mean LD (intravenous, mouse) = 100 mg/kg.
Chỉ Định : Oseltamivir (Tamiflu) is for the treatment of uncomplicated acute illness due to influenza infection in patients 1 year and older who have been symptomatic for no more than 2 days. It is also used for the prophylaxis of influenza in adult patients and adolescents 13 years and older.
Liều Lượng & Cách Dùng : Capsule - Oral
Capsule - Oral - 75 mg
Powder, for suspension - Oral
Powder, for suspension - Oral - 12 mg/mL
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Tamiflu
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