Antibacterial and anti-inflammatory apis Praziquantel Powder

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Praziquantel Usage and Synthesis.

Praziquantel has a significant killing effect on adult schistosomes. Its insecticidal mechanism, at the molecular level, is that praziquantel rapidly disrupts the Ca2+ balance in the body of the parasite.

On the one hand, it leads to the excitement of worm activity, muscle contracture, so that the schistosomes parasitised in the portal system can not be adsorbed in the blood vessel wall and carried by the blood flow into the liver (liver migration), and then damaged; Secondly, it leads to the syncytialisation of the schistosomes.

Secondly, it leads to the damage of the syncytiotrophoblast cortex of Schistosoma haematobium, which not only affects the absorptive, excretory and secretory functions of Schistosoma haematobium, leading to the disorders of glucose metabolism and enzyme system, but also exposes the antigenic determinant clusters of Schistosoma haematobium to be recognised by the immune system of the host, attracting a large number of inflammatory cells, such as neutrophils, eosinophils, macrophages, etc., which gather around the body of the Schistosoma haematobium and exert an attack.

Side-effects and functions of Praziquantel.

Common side effects of praziquantel are as follows:

1, dizziness, headache, nausea, abdominal pain, diarrhoea, fatigue, limb aches and pains, etc. may occur 1 hour after the first dose, which are usually mild and of short duration, do not affect the treatment and do not need to be treated.

2、A few cases have palpitation, chest tightness and other symptoms, ECG shows T-wave changes and extra-phase contraction, occasionally supraventricular tachycardia, atrial fibrillation.

3, a few cases may appear transient transaminase elevation, toxic hepatitis and so on.

4、Occasionally, it may induce mental disorder or gastrointestinal bleeding.

Brain hernia, allergic reactions (rash, asthma) are also seen.

Pharmacological Effect of Praziquantel.

Praziquantel is a commonly used drug for the treatment of schistosomiasis, with minimal toxicity to animals, and is rapidly absorbed in the digestive tract after oral administration. Peak blood time: 5 minutes in mice, l5-30 minutes in rats, 30-120 minutes in dogs and about 2h in sheep.

After absorption, the drug is widely distributed in all tissues and organs, and can even pass through the blood and brain barrier of rats, and can enter the bile of dogs, which can prompt the inward flow of Ca2+ outside the membrane of schistosome myocytes, cause muscle contracture, and lose the ability to suction the parasitic site.

At the same time cause sugar metabolism and energy metabolism disorders, "accompanying immune" state is destroyed, and then through the host immune system, and finally eliminate the worm, on the Schistosoma haematobium, cestode, Schistosoma lungworm, cysticercus and immature worms (tailed larvae, trichinella) are very good efficacy of the killing treatment!

Production Methods of  Bulk Praziquantel Powder.

Phenylethylamine as raw material, after acylation with chloroacetyl chloride, then amination reaction with potassium benzenedicarboxamide to introduce the amino group, cyclization under the action of phosphorus trichloride to obtain 3,4-dihydroisoquinoline derivatives, hydrogenation and hydrolysis to obtain 1-aminomethyltetrahydroquinoline, successively acylated with cyclohexanecarbonyl chloride and chloroacetyl chloride, and finally dehydrogenated to obtain the praziquantel by cyclization.

It can also be isoquinoline as raw material, through the Reissert reaction, the introduction of cyano in the l position and benzoylation on nitrogen, and then hydrogenation, at the same time, benzoyl transfer to the amino group of the side chain, and then the introduction of chloroacetyl chloride on the amino group on the ring, and then cyclization, hydrolysis, and cyclohexanecarbonyl chloride to get the praziquantel.

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