Tìm theo
Proguanil
Các tên gọi khác (6 ) :
  • N-(4-Chlorophenyl)-n'-(isopropyl)-imidodicarbonimidic diamide
  • 1-(P-Chlorophenyl)-5-isopropylbiguanide
  • Chlorguanide
  • Chloroguanide
  • N-(4-Chlorophenyl)-n'-(isopropyl)-imidodicarbonimidic diamide
  • Proguanilum
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 500-92-5
ATC: P01BB01
ĐG : A-S Medication Solutions LLC , http://orders.a-smeds.com
CTHH: C11H16ClN5
PTK: 253.731
Proguanil is a prophylactic antimalarial drug, which works by stopping the malaria parasite, Plasmodium falciparum and Plasmodium vivax, from reproducing once it is in the red blood cells. It does this by inhibiting the enzyme, dihydrofolate reductase, which is involved in the reproduction of the parasite.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C11H16ClN5
Phân tử khối
253.731
Monoisotopic mass
253.109423244
InChI
InChI=1S/C11H16ClN5/c1-7(2)15-10(13)17-11(14)16-9-5-3-8(12)4-6-9/h3-7H,1-2H3,(H5,13,14,15,16,17)
InChI Key
InChIKey=SSOLNOMRVKKSON-UHFFFAOYSA-N
IUPAC Name
(E)-1-({amino[(4-chlorophenyl)amino]methylidene}amino)-N'-(propan-2-yl)methenimidamide
Traditional IUPAC Name
proguanil
SMILES
CC(C)\N=C(/N)N=C(N)NC1=CC=C(Cl)C=C1
Độ tan chảy
129 °C
Độ hòa tan
156 mg/L
logP
2.53
logS
-3
pKa (strongest acidic)
19.77
pKa (Strongest Basic)
10.12
PSA
88.79 Å2
Refractivity
71.07 m3·mol-1
Polarizability
26.84 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Proguanil is a biguanide derivative that is converted to an active metabolite called cycloguanil. It exerts its antimalarial action by inhibiting parasitic dihydrofolate reductase enzyme. It has causal prophylactic and suppressive activity against P. falciparum and cures the acute infection. It is also effective in suppressing the clinical attacks of vivax malaria. However it is slower compared to 4-aminoquinolines.
Cơ Chế Tác Dụng : Proguanil is a prophylactic antimalarial drug, which works by stopping the malaria parasite, Plasmodium falciparum and Plasmodium vivax, from reproducing once it is in the red blood cells. It does this by inhibiting the enzyme, dihydrofolate reductase, which is involved in the reproduction of the parasite. Proguanil inhibits the dihydrofolate reductase of plasmodia and thereby blocks the biosynthesis of purines and pyrimidines, which are essential for DNA synthesis and cell multiplication. This leads to failure of nuclear division at the time of schizont formation in erythrocytes and liver.
Dược Động Học :
▧ Absorption :
Rapidly and well absorbed in humans following oral doses ranging from 50 to 500 mg.
▧ Protein binding :
Approximately 75%
▧ Metabolism :
Variably metabolized in the liver by cytochrome P450 isoenzymes to the active triazine metabolite, cycloguanil. This variable metabolism of proguanil may have profound clinical importance in poor metabolizers such as the Asian and African populations at risk for malaria infection. Prophylaxis with proguanil may not be effective in these persons because they may not achieve adequate therapeutic levels of the active compound, cycloguanil, even after multiple doses.
▧ Half Life :
Approximately 20 hours
Chỉ Định : For the causal prevention and suppression of malaria caused by susceptible strains of P. falciparum and other species of Plasmodium found in some geographical areas of the world.
Tương Tác Thuốc :
  • Artemether Proguanil may increase the adverse effects of artemether. Combination therapy is contraindicated unless there are no other treatment options.
  • Lumefantrine Proguanil may increase the adverse effects of lumefantrine. Combination therapy is contraindicated unless there are no other treatment options.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Chloroguanide
  • Công ty :
    Sản phẩm biệt dược : Paludrine
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01131
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6178111
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506228
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07631
ChemSpider
http://www.chemspider.com/Chemical-Structure.4754.html
PharmGKB
http://www.pharmgkb.org/drug/PA451124
Wikipedia
http://en.wikipedia.org/wiki/Proguanil
Drugs.com
http://www.drugs.com/cons/proguanil.html
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