Tìm theo
Praziquantel
Các tên gọi khác (1) :
  • Biltricide
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 55268-74-1
ATC: P02BA01
ĐG : Bayer Healthcare , http://www.bayerhealthcare.com
CTHH: C19H24N2O2
PTK: 312.4061
An anthelmintic used in most schistosome and many cestode infestations. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H24N2O2
Phân tử khối
312.4061
Monoisotopic mass
312.183778022
InChI
InChI=1S/C19H24N2O2/c22-18-13-20(19(23)15-7-2-1-3-8-15)12-17-16-9-5-4-6-14(16)10-11-21(17)18/h4-6,9,15,17H,1-3,7-8,10-13H2
InChI Key
InChIKey=FSVJFNAIGNNGKK-UHFFFAOYSA-N
IUPAC Name
2-cyclohexanecarbonyl-1H,2H,3H,4H,6H,7H,11bH-piperazino[2,1-a]isoquinolin-4-one
Traditional IUPAC Name
praziquantel
SMILES
O=C(C1CCCCC1)N1CC2N(CCC3=CC=CC=C23)C(=O)C1
Độ tan chảy
136 °C
Độ hòa tan
400 mg/L
logP
2.5
logS
-2.9
pKa (strongest acidic)
19.38
pKa (Strongest Basic)
-0.22
PSA
40.62 Å2
Refractivity
88.79 m3·mol-1
Polarizability
34.84 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Praziquantel is an anthelmintic used in most schistosome and many cestode infestations. Praziquantel effects the permeability of the cell membrane resulting in the contraction of schistosomes. The drug further causes vacuolization and disintegration of the schistosome tegument. The effect is more marked on adult worms compared to young worms. An increased calcium influx may play an important role. Secondary effects are inhibition of glucose uptake, lowering of glycogen levels and stimulation of lactate release. The action of praziquantel is limited very specifically to trematodes and cestodes; nematodes (including filariae) are not affected.
Cơ Chế Tác Dụng : An anthelmintic used in most schistosome and many cestode infestations. [PubChem] Praziquantel works by causing severe spasms and paralysis of the worms' muscles. This paralysis is accompanied - and probably caused - by a rapid Ca 2+ influx inside the schistosome. Morphological alterations are another early effect of praziquantel. These morphological alterations are accompanied by an increased exposure of schistosome antigens at the parasite surface. The worms are then either completely destroyed in the intestine or passed in the stool. An interesting quirk of praziquantel is that it is relatively ineffective against juvenile schistosomes. While initially effective, effectiveness against schistosomes decreases until it reaches a minimum at 3-4 weeks. Effectiveness then increases again until it is once again fully effective at 6-7 weeks. Glutathione S-transferase (GST), an essential detoxification enzyme in parasitic helminths, is a major vaccine target and a drug target against schistosomiasis. Schistosome calcium ion channels are currently the only known target of praziquantel.
Dược Động Học :
▧ Absorption :
Rapidly absorbed (80%)
▧ Protein binding :
80 to 85%
▧ Metabolism :
renal
▧ Half Life :
0.8-1.5 hours (in serum)
Chỉ Định : For the treatment of infections due to all species of schistosoma.
Tương Tác Thuốc :
  • Carbamazepine Markedly lower praziquantel levels
  • Chloroquine Markedly lower praziquantel levels
  • Etravirine Praziquantel, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
  • Etravirine Praziquantel, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
  • Phenytoin Markedly lower praziquantel levels
  • Rifampicin Significant decrease in praziquantel level
  • Telithromycin Telithromycin may reduce clearance of Praziquantel. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Praziquantel if Telithromycin is initiated, discontinued or dose changed.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of praziquantel by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of praziquantel if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Biltricide
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01058
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4891
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507082
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07367
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00471
ChemSpider
http://www.chemspider.com/Chemical-Structure.4722.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0085-1747-01
PharmGKB
http://www.pharmgkb.org/drug/PA164764583
Wikipedia
http://en.wikipedia.org/wiki/Praziquantel
RxList
http://www.rxlist.com/cgi/generic2/praziquantel.htm
Drugs.com
http://www.drugs.com/cdi/praziquantel.html
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