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Praziquantel

Praziquantel 구조식 이미지
카스 번호:
55268-74-1
상품명:
Praziquantel
동의어(영문):
Cesol;Azinox;droncit;WarMnil;pyquiton;Prazinon;embay8440;Distocide;Cysticide;biltricide
CBNumber:
CB8178956
분자식:
C19H24N2O2
포뮬러 무게:
312.41
MOL 파일:
55268-74-1.mol

Praziquantel 속성

녹는점
136-138 C
끓는 점
1377℃
밀도
1.1209 (rough estimate)
굴절률
1.5600 (estimate)
인화점
>110°(230°F)
저장 조건
−20°C
용해도
ethanol: soluble5mg/mL
산도 계수 (pKa)
-0.98±0.20(Predicted)
물리적 상태
powder or crystals
색상
Crystals from EtOAc/hexane
수용성
Freely soluble in ethanol or dichloromethane. Slightly soluble in water
Merck
13,7802
BRN
761557
EPA
Praziquantel (55268-74-1)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 F,C
위험 카페고리 넘버 11-34
안전지침서 16-26-36/37/39-45-24/25
WGK 독일 1
RTECS 번호 UQ4150000
HS 번호 29339900
독성 LD50 in mice, rats (mg/kg): 2000-3000 orally; >3000 s.c. (Muermann)
그림문자(GHS):
신호 어:
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H303 삼키면 유해할 수 있음 급성 독성 물질 - 경구 구분 5 P312
예방조치문구:

Praziquantel MSDS


2-Cyclohexyl-carbonyl-1,3,4,6,7,11b-hexahydro-2H-pyrazine(2,1-a)isoquinoline-4-one

Praziquantel C화학적 특성, 용도, 생산

화학적 성질

White Solid

용도

anthelmintic; EMBAY-8440

용도

Anthelmintic, effective against flatworms.

Indications

The neuromuscular effects of praziquantel (Biltricide) appear to increase parasite motility leading to spastic paralysis. The drug increases calcium permeability through parasite-specific ion channels, so that the tegmental and muscle cells of the parasite accumulate calcium.This action is followed by vacuolization and the exposure of hitherto masked tegmental antigens, lipidanchored protein, and actin. Insertion of the drug into the fluke’s lipid bilayer causes conformational changes, rendering the fluke susceptible to antibody- and complement-mediated assault.

상표명

Biltricide (Bayer).

원료

There is evidence that resistance to praziquantel is emerging in schistosomes, although there is debate as to whether treatment failures are due to resistance or innate tolerance.

Pharmaceutical Applications

A synthetic pyrazinoquinoline formulated for oral administration. It is stable in the dry state, but hygroscopic.

Mechanism of action

Praziquantel is readily absorbed (80% in 24 hours) after oral administration, with serum concentrations being maximal in 1 to 3 hours; the drug has a half-life of 0.8 to 1.5 hours. Its bioavailability is reduced by phenytoin or carbamazepine and increased by cimetidine. Dexamethasone decreases plasma praziquantel levels by 50%. Praziquantel is excreted by the kidneys.

Pharmacokinetics

Oral absorption: >80%
Cmax 50 mg/kg oral: 1 mg/L after 1–2 h
Plasma half-life: parent drug: 1–1.5 h
metabolites: 4–6h
Plasma protein binding: 80%
Praziquantel is rapidly absorbed when given orally, but it undergoes extensive first-pass biotransformation and the concentration of unchanged drug in plasma is low. The major metabolite, a 4-hydroxy derivative, retains little to no antiparasitic activity. About 80% of the oral dose, as parent drug and its metabolites, is excreted in the urine by the fourth day post-treatment, 90% of this in 24 h. A higher peak plasma concentration is achieved in infected people, but other pharmacokinetic values are unchanged.

Clinical Use

2-(Cyclohexylcarbonyl)-1,2,3,6,7, 11b-hexahydro-4Hpyrazino[2,1-a]isoquinolin-4-one (Biltricide) is a broadspectrumagent that is effective against various trematodes (flukes). It has become the agent of choice for the treatmentof infections caused by schistosomes (blood flukes).
The drug also provides effective treatment for fasciolopsiasis(intestinal fluke), clonorchiasis (Chinese liver fluke),fascioliasis (sheep liver fluke), opisthorchosis (liver fluke),and paragonimiasis (lung fluke). Praziquantel increases cellmembrane permeability of susceptible worms, resulting inthe loss of extracellular calcium. Massive contractions andultimate paralysis of the fluke musculature occurs, followedby phagocytosis of the parasite.
Following oral administration, about 80% of the doseis absorbed. Maximal plasma concentrations are achievedin 1 to 3 hours. The drug is rapidly metabolized in theliver in the first-pass. It is likely that some of the metabolitesare also active. Praziquantel occurs as a white crystallinesolid that is insoluble in water. It is available as600-mg film-coated tablets. The drug is generally welltolerated.

Clinical Use

Praziquantel is an extremely active broad-spectrum anthelmintic that is well tolerated. It is the most effective of the drugs used in the treatment of schistosomiasis, possessing activity against male and female adults and immature stages. Unlike other agents, it is active against all three major species (S. haematobium, S. mansoni, and S. japonicum). In addition, it has activity against other flukes, such as C. sinensis, Paragonimus westermani, O. viverrini, and the tapeworms (D. latum, H. nana, T. saginata, and T. solium). It is not as effective against F. hepatica. It is used effectively in the treatment of clonorchiasis and paragonimiasis and is an effective alternative agent to niclosamide in the treatment of tapeworm infestations.

Clinical Use

Schistosomiasis
Other trematode infections (except F. hepatica)
Tapeworm infection, including cerebral cysticercosis
Treatment may need to be prolonged in cerebral cysticercosis.

부작용

Very few side effects have been reported. In the treatment of cerebral cysticercosis the death of cysts in the brain may cause local inflammation and edema, but this usually subsides quickly. Ocular cysticercosis should not be treated with this drug, because parasite destruction in the eye can lead to irreparable lesions. Adverse events seen in the treatment of schistosomiasis, including abdominal pain, nausea, anorexia, diarrhea and mild neurological effects, are almost certainly due to the death and disintegration of the large adult worms.

부작용

Adverse reactions tend to occur within a few hours of administration. They include gastrointestinal intolerance with nausea, vomiting, and abdominal discomfort. This may be due to the liberation of helminth proteins from dead worms rather than any direct effect of the drug.

Safety Profile

Poison by intraperitoneal route.Moderately toxic by ingestion and other routes. Humanmutation data reported. When heated to decomposition itemits toxic fumes of NOx.

Veterinary Drugs and Treatments

Praziquantel is indicated for (approved labeling) for the treatment of Dipylidium caninum, Taenia pisiformis, and Echinococcus granulosis in dogs, and Dipylidium caninum and Taenia taeniaeformis in cats. Fasting is not required nor recommended before dosing. A single dose is usually effective, but measures should be taken to prevent reinfection, particularly against D. caninum. Praziquantel can also be used for treating Alaria spp. in dogs and cats and Spirometra mansonoides infections in cats.
Praziquantel has been used in birds and other animals, but it is usually not economically feasible to use in large animals. In humans, praziquantel is used for schistosomiasis, other trematodes (lung, liver, intestinal flukes) and tapeworms. It is not routinely effective in treating F. hepatica infections in humans.
Combination products can give a wide spectrum of internal parasite control in a variety of species.

Praziquantel 준비 용품 및 원자재

원자재

준비 용품


Praziquantel 공급 업체

글로벌( 395)공급 업체
공급자 전화 팩스 이메일 국가 제품 수 이점
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
+86 (576) 8169-6105 sales@frappschem.com China 886 50
Capot Chemical Co.,Ltd.
+86-571-85586718
+86-571-85864795 sales@capotchem.com China 19921 60
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22631 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070
product@chemlin.com.cn CHINA 3015 60
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
Hubei XinRunde Chemical Co., Ltd.
+8615102730682
02783214688 bruce@xrdchem.cn CHINA 569 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24686 60
Hefei TNJ Chemical Industry Co.,Ltd.
86-0551-65418684 18949823763
86-0551-65418684 info@tnjchem.com China 2368 55
Hebei Chisure Biotechnology Co., Ltd.
+8613292890173
0311 66567340 luna@speedgainpharma.com CHINA 1010 58

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