Tìm theo
Valganciclovir
Các tên gọi khác (4 ) :
  • Cymeval
  • L-valine, ester with ganciclovir
  • Valcyte
  • Valganciclovir
antiviral agents
Thuốc Gốc
Small Molecule
CAS: 175865-60-8
ĐG : F Hoffmann-La Roche Ltd. , http://www.roche.com
CTHH: C14H22N6O5
PTK: 354.3617
Valganciclovir hydrochloride (Valcyte, manufactured by Roche) is an antiviral medication used to treat cytomegalovirus infections. As the L-valyl ester of ganciclovir, it is actually a prodrug for ganciclovir. After oral administration, it is rapidly converted to ganciclovir by intestinal and hepatic esterases.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H22N6O5
Phân tử khối
354.3617
Monoisotopic mass
354.165167844
InChI
InChI=1S/C14H22N6O5/c1-7(2)9(15)13(23)24-4-8(3-21)25-6-20-5-17-10-11(20)18-14(16)19-12(10)22/h5,7-9,21H,3-4,6,15H2,1-2H3,(H3,16,18,19,22)/t8?,9-/m0/s1
InChI Key
InChIKey=WPVFJKSGQUFQAP-GKAPJAKFSA-N
IUPAC Name
2-[(2-amino-6-oxo-6,9-dihydro-3H-purin-9-yl)methoxy]-3-hydroxypropyl (2S)-2-amino-3-methylbutanoate
Traditional IUPAC Name
valganciclovir
SMILES
CC(C)[C@H](N)C(=O)OCC(CO)OCN1C=NC2=C1NC(N)=NC2=O
Độ hòa tan
4.79e+00 g/l
logP
-1.1
logS
-1.9
pKa (strongest acidic)
8.1
pKa (Strongest Basic)
7.36
PSA
167.08 Å2
Refractivity
86.6 m3·mol-1
Polarizability
34.88 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
9
H Bond Donor Count
4
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Dược Lực Học : Valganciclovir is an antiviral medication used to treat cytomegalovirus infections. As the L-valyl ester of ganciclovir, it is actually a prodrug for ganciclovir. After oral administration, it is rapidly converted to ganciclovir by intestinal and hepatic esterases. After this, it (being an analogue of guanosine) gets incorporated into DNA and thus cannot be properly read by DNA polymerase. This results in the termination of the elongation of viral DNA.
Cơ Chế Tác Dụng : Valganciclovir hydrochloride (Valcyte, manufactured by Roche) is an antiviral medication used to treat cytomegalovirus infections. As the L-valyl ester of ganciclovir, it is actually a prodrug for ganciclovir. After oral administration, it is rapidly converted to ganciclovir by intestinal and hepatic esterases. Valganciclovir is a prodrug of ganciclovir that exists as a mixture of two diastereomers. After administration, these diastereomers are rapidly converted to ganciclovir by hepatic and intestinal esterases. In cytomegalovirus (CMV)-infected cells, ganciclovir is initially phosphorylated to the monophosphate form by viral protein kinase, then it is further phosphorylated via cellular kinases to produce the triphosphate form. This triphosphate form is slowly metabolized intracellularly. The phosphorylation is dependent upon the viral kinase and occurs preferentially in virus-infected cells. The virustatic activity of ganciclovir is due to the inhibition of viral DNA synthesis by ganciclovir triphosphate. Ganciclovir triphosphate is incorporated into the DNA strand replacing many of the adenosine bases. This results in the prevention of DNA synthesis, as phosphodiester bridges can longer to be built, destabilizing the strand. Ganciclovir inhibits viral DNA polymerases more effectively than it does cellular polymerase, and chain elongation resumes when ganciclovir is removed.
Dược Động Học :
▧ Absorption :
Valganciclovir is well absorbed from the gastrointestinal tract and the absolute bioavailability from valganciclovir tablets (following administration with food) is approximately 60%.
▧ Volume of Distribution :
* 0.703 ± 0.134 L/kg
▧ Protein binding :
Plasma protein binding of ganciclovir is 1% to 2% over concentrations of 0.5 and 51 mg/mL.
▧ Metabolism :
Rapidly hydrolyzed in the intestinal wall and liver to ganciclovir. No other metabolites have been detected.
▧ Route of Elimination :
The major route of elimination of valganciclovir is by renal excretion as ganciclovir through glomerular filtration and active tubular secretion.
▧ Half Life :
Approximately 4.08 hours. Increased in patients with renal function impairment.
▧ Clearance :
* 3.07+/- 0.64 mL/min/kg [IV administration] * 5.3 L/hr [Patient with creatinine clearance of 70.4 mL/min]
Độc Tính : It is expected that an overdose of valganciclovir could also possibly result in increased renal toxicity.
Chỉ Định : Valganciclovir is an antiviral medication used for the treatment of cytomegalovirus infections.
Tương Tác Thuốc :
  • Abacavir The adverse/toxic effects of reverse transcriptase inhibitors (nucleoside), such as Abacavir, may be enhanced by Valganciclovir. There is a risk of hematologic toxicity. Diligent monitoring during concomitant therapy is recommended.
  • Adefovir Dipivoxil The adverse/toxic effects of reverse transcriptase inhibitors (nucleoside), such as Adefovir Dipivoxil, may be enhanced by Valganciclovir. There is a risk of hematologic toxicity. Diligent monitoring during concomitant therapy is recommended.
  • Cilastatin Generalized convulsions have been reported in patients taking Ganciclovir and Imipenem-cilastatin. Concomitant therapy should be avoided. (Note: Valganciclovir is converted to Ganciclovir in vivo)
  • Didanosine The adverse/toxic effects of Didanosine, a reverse transcriptase inhibitor (nucleoside), may be enhanced by Valganciclovir. There is a significant risk of hematologic toxicity. Concomitant therapy should be avoided.
  • Emtricitabine The adverse/toxic effects of reverse transcriptase inhibitors (nucleoside), such as Emtricitabine, may be enhanced by Valganciclovir. There is a risk of hematologic toxicity. Diligent monitoring during concomitant therapy is recommended.
  • Imipenem Generalized convulsions have been reported in patients taking Ganciclovir and Imipenem-cilastatin. Concomitant therapy should be avoided. (Note: Valganciclovir is converted to Ganciclovir in vivo)
  • Lamivudine The adverse/toxic effects of reverse transcriptase inhibitors (nucleoside), such as Lamivudine, may be enhanced by Valganciclovir. There is a risk of hematologic toxicity. Diligent monitoring during concomitant therapy is recommended.
  • Mycophenolate mofetil The excretion rates of Valganciclovir and/or Mycophenolate mofetil may decrease. Monitor for increased serum concentrations and toxicity of both agents.
  • Mycophenolic acid The excretion rates of Valganciclovir and/or Mycophenolic acid may decrease. Monitor for increased serum concentrations and toxicity of both agents.
  • Probenecid Probenecid may decrease excretion of Valganciclovir. Monitor for increased serum concentration and toxicity of Valganciclovir.
  • Tenofovir The excretion rates of Valganciclovir and/or Tenofovir may decrease as both drugs are eliminated by active tubular secretion. Monitor for increased serum concentrations and toxicity of both agents.
  • Zidovudine The adverse/toxic effects of Zidovudine, a reverse transcriptase inhibitor (nucleoside), may be enhanced by Valganciclovir. There is a significant risk of hematologic toxicity. Concomitant therapy should be avoided.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Valcyte 450 mg tablet
    Giá bán buôn : USD >46.99
    Đơn vị tính : tablet
  • Biệt dược thương mại : Valcyte
    Giá bán buôn : USD >48.87
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Cymeval
  • Công ty :
    Sản phẩm biệt dược : Valcyt
  • Công ty :
    Sản phẩm biệt dược : Valcyte
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01610
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=64147
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505524
ChemSpider
http://www.chemspider.com/Chemical-Structure.57721.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0004-0038-22
PharmGKB
http://www.pharmgkb.org/drug/PA10227
Wikipedia
http://en.wikipedia.org/wiki/Valganciclovir
RxList
http://www.rxlist.com/cgi/generic/valganciclovir.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/val1584.shtml
Drugs.com
http://www.drugs.com/cdi/valganciclovir.html
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