Praziquantel
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Praziquantel 속성
- 녹는점
- 136-138 C
- 끓는 점
- 1377℃
- 밀도
- 1.1209 (rough estimate)
- 굴절률
- 1.5600 (estimate)
- 인화점
- >110°(230°F)
- 저장 조건
- Sealed in dry,Store in freezer, under -20°C
- 용해도
- 에탄올: 용해성5mg/mL
- 물리적 상태
- 분말 또는 결정
- 산도 계수 (pKa)
- -0.98±0.20(Predicted)
- 색상
- 초산 에틸렌/헥산으로부터 얻은 결정입니다
- 수용성
- 에탄올이나 디클로로메탄에 잘 녹습니다. 물에 약간 용해됨
- Merck
- 13,7802
- BRN
- 761557
- BCS Class
- 2
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) |
Praziquantel C화학적 특성, 용도, 생산
개요
Praziquantel (PZQ) is an isoquinoline derivative with most of the biological activity found in the levo enantiomer. The compound has no activity against nematodes, but it is highly effective against cestodes and trematodes.화학적 성질
White Solid용도
Praziquantel is a potent anthelmintic used against schistosome and many cestode infestations. It is used to study voltage-gated Ca2+ channels and is a potential small molecule neurogenic.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.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.
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.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.신진 대사
Praziquantel is rapidly absorbed and undergoes hepatic first-pass metabolism. The metabolites are either less active or inactive and consist of hydroxylated compounds. In the serum, the major metabolite appears to be the monohydroxylated 4-hydroxycyclohexylcarboxylate, whereas in the urine, 50 to 60% of the initial PZQ exists as dihydroxylated products.These hydroxylation reactions are catalyzed by CYP2B6 and CYP3A4. The metabolites would be expected to exist in the conjugated form in the urine.Praziquantel 준비 용품 및 원자재
원자재
Formyl chloride
Pyrazine
이소퀴놀린
oxazine
Tetrahydroquinoline
Cyclohexanecarboxylic acid chloride
아세틸 염화물
피페라진
클로로아세틸 클로라이드
3,4-DIHYDROISOQUINOLINE
염화벤조일
사이안화 칼륨
수소
준비 용품
Praziquantel 공급 업체
글로벌( 686)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Hebei ZB Gamay Biological Technology Co.,Ltd | +8617330018573 |
info@zbvet.net | China | 245 | 58 |
ENBRIDGE PHARMTECH CO., LTD. | +8613812269233 |
tinayang@enbridgepharm.com | China | 302 | 58 |
Hebei Guanlang Biotechnology Co., Ltd. | +86-19930503282 |
alice@crovellbio.com | China | 8820 | 58 |
Honest Joy Holdings Limited | 0755-36694831 +8613717124449 |
sale@feiyang.com.cn | China | 300 | 58 |
Hebei Chuanghai Biotechnology Co,.LTD | +86-13131129325 |
sales1@chuanghaibio.com | China | 5882 | 58 |
Guangzhou Tengyue Chemical Co., Ltd. | +86-86-18148706580 +8618826483838 |
evan@tyvovo.com | China | 153 | 58 |
Hebei Weibang Biotechnology Co., Ltd | +8615350571055 |
Sibel@weibangbio.com | China | 5848 | 58 |
Watson Biotechnology Co.,Ltd | +86-18186686046 +86-18186686046 |
sales01@watsonbiotech.cn | China | 5851 | 58 |
HebeiShuoshengImportandExportco.,Ltd | +86-18532138899 +86-18532138899 |
L18532138899@163.com | China | 931 | 58 |
Shaanxi Dideu Medichem Co. Ltd | +86-29-81148696 +86-15536356810 |
1022@dideu.com | China | 3878 | 58 |
Praziquantel 관련 검색:
나트륨-N-라로일사코신산 이소퀴놀린 피라조포스 카보닐 황화합물
Sodium lauroylglutamate
Pyrazine
Pyrazole
1-(CYCLOHEXYLMETHYL)PIPERAZINE
1-(2-PHENYLETHYL)PIPERAZINE
1-ACETYL-4-METHYLPIPERAZINE HYDROCHLORIDE
N,N,2-TRIMETHYLPROPIONAMIDE
Pexantel
(2-AMINO-1-PHENYLETHYL)DIMETHYLAMINE
1-Butylpiperazine
2-Phenylpiperazine
1-Piperazinecarbaldehyde
1-Methylpiperazin-2-one
1-FORMYL-4-METHYLPIPERAZINE