Praziquantel

Praziquantel 속성

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

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 Solid

용도

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%
C_max 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

준비 용품

Praziquantel 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Hebei ZB Gamay Biological Technology Co.,Ltd	+86-031189171450 +86-15632359451	chem@zbvet.net	China	222	58
ENBRIDGE PHARMTECH CO., LTD.	+8613812269233	tinayang@enbridgepharm.com	China	303	58
Hebei Guanlang Biotechnology Co., Ltd.	+86-19930503282	alice@crovellbio.com	China	8829	58
Honest Joy Holdings Limited	0755-36694831 +8613717124449	sale@feiyang.com.cn	China	300	58
Hebei Guanlang Biotechnology Co,.LTD	+86-19930503253; +8619930503252	daisy@crovellbio.com	China	5956	58
Guangzhou Tengyue Chemical Co., Ltd.	+86-86-18148706580 +8618826483838	evan@tyvovo.com	China	153	58
Henan Bao Enluo International TradeCo.，LTD	+86-17331933971 +86-17331933971	deasea125996@gmail.com	China	2503	58
Anhui Ruihan Technology Co., Ltd	+8617756083858	daisy@anhuiruihan.com	China	994	58
Hebei Jingbo New Material Technology Co., Ltd	+8619931165850	hbjbtech@163.com	China	1000	58
Sigma Audley	+86-18336680971 +86-18126314766	nova@sh-teruiop.com	China	525	58

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