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Rimantadine
Các tên gọi khác (3) :
  • Rimantadin
  • Rimantadine
  • SID29215455
Thuốc Gốc
Small Molecule
CAS: 13392-28-4
ATC: J05AC02
ĐG : Caraco Pharmaceutical Labs , http://www.caraco.com
CTHH: C12H21N
PTK: 179.3018
An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
179.3018
Monoisotopic mass
179.167399677
InChI
InChI=1S/C12H21N/c1-8(13)12-5-9-2-10(6-12)4-11(3-9)7-12/h8-11H,2-7,13H2,1H3
InChI Key
InChIKey=UBCHPRBFMUDMNC-UHFFFAOYSA-N
IUPAC Name
1-(adamantan-1-yl)ethan-1-amine
Traditional IUPAC Name
rimantadine
SMILES
CC(N)C12CC3CC(CC(C3)C1)C2
Độ tan chảy
>300 °C
Độ hòa tan
Hydrochloride salt freely soluble (50 mg/ml at 20 °C)
logP
3.6
logS
-4.3
pKa (Strongest Basic)
10.14
PSA
26.02 Å2
Refractivity
54.52 m3·mol-1
Polarizability
21.79 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
1
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Rimantadine, a cyclic amine, is a synthetic antiviral drug and a derivate of adamantane, like a similar drug amantadine. Rimantadine is inhibitory to the in vitro replication of influenza A virus isolates from each of the three antigenic subtypes (H1N1, H2H2 and H3N2) that have been isolated from man. Rimantadine has little or no activity against influenza B virus. Rimantadine does not appear to interfere with the immunogenicity of inactivated influenza A vaccine.
Cơ Chế Tác Dụng : An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. [PubChem] The mechanism of action of rimantadine is not fully understood. Rimantadine appears to exert its inhibitory effect early in the viral replicative cycle, possibly inhibiting the uncoating of the virus. Genetic studies suggest that a virus protein specified by the virion M2 gene plays an important role in the susceptibility of influenza A virus to inhibition by rimantadine.
Dược Động Học :
▧ Absorption :
Well absorbed, with the tablet and syrup formulations being equally absorbed after oral administration.
▧ Protein binding :
Approximately 40% over typical plasma concentrations.
▧ Metabolism :
Following oral administration, rimantadine is extensively metabolized in the liver with less than 25% of the dose excreted in the urine as unchanged drug. Glucuronidation and hydroxylation are the major metabolic pathways.
▧ Route of Elimination :
Following oral administration, rimantadine is extensively metabolized in the liver with less than 25% of the dose excreted in the urine as unchanged drug.
▧ Half Life :
25 to 30 hours in young adults (22 to 44 years old). Approximately 32 hours in elderly (71 to 79 years old) and in patients with chronic liver disease. Approximately 13 to 38 hours in children (4 to 8 years old).
Độc Tính : Oral LD50 in rats is 640 mg/kg. Overdoses of a related rug, amantadine, have been reported with adverse reactions consisting of agitation, hallucinations, cardiac arrhythmia and death.
Chỉ Định : For the prophylaxis and treatment of illness caused by various strains of influenza A virus in adults.
Liều Lượng & Cách Dùng : Syrup - Oral
Tablet, film coated - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Flumadine
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