Prazicon

Uses

Praziquantel is an anthelmintic medication used to treat a number of parasitic worm infections such as schistosomiasis.

For the treatment of infections due to all species of schistosoma.

Pyrantel is an anthelmintic used to treat helminth infections.

For the treatment of enterobiasis including roundworm (ascariasis), pinworm (enterobius) and hookworm (strongyloides) and hookworm (ancylostoma) in the pyrantel pamoate form .

Pyrantel is available in various formulations for humans, dogs, and cats as the pamoate (US Pharmacopeia nomenclature) or embonate (European Pharmacopoeia nomenclature) salt, which contains 34.7% pyrantel base combined with pamoic acid . , .

Pyrantel pamoate (embonate) ingested orally is effective for removal and control of ascarid and hookworm infections in puppies and dogs (adult Toxocara canis, Toxascaris leonina, Ancylostoma tubaeforme, An. braziliense, Uncinaria stenocephala), cats (adult Toxocara cati, Toxa. leonina, An. caninum, An. braziliense, U. stenocephala), horses and ponies (adult and immature Parascaris equorum, adult Strongylus vulgaris, S. edentatus, S. equinus, Cyathostomes (Triodontophorus spp., Cyathostomum spp., Cylicodontophorus spp., Cylicocyclus spp., Cylicostephanus spp., Poteriostomum spp.), Oxyuris equi, Anoplocephala perfoliata), swine (adult Ascaris suum, Oesophagostomum dentatum), and humans (adult A. lumbricoides, Enterobius vermicularis, An. duodenale, Necator americanus) .

Prazicon is also used to associated treatment for these conditions: Cestode infections, Cysticercosis, Liver fluke infection, Trematode infections, Schistosoma infectionEnterobiasis, Helminthic infection

How Prazicon works

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.

By promoting the release of acetylcholine, inhibiting cholinesterase, and stimulating ganglionic neurons, pyrantel serves as a depolarizing neuromuscular blocking agent in helminths. This causes extensive depolarization of the helminth muscle membrane, resulting in tension to the helminth's muscles, leading to paralysis and release of their attachment to the host organism intestinal walls .

This action is unlike piperazine, which is a hyperpolarizing neuromuscular blocking agent that causes relaxation of the helminth muscles, leading to a subsequent detachment from the intestinal wall. Excretion of the parasites in the feces occurs by normal peristalsis .

Toxicity

Mild adverse effects include nausea, vomiting, diarrhea, headache, and dizziness .

LD50 in rats is 535 mg/kg .

Reported effects in humans in case of overdose include gastrointestinal disturbance, central nervous system effects, and superficial skin reactions. In one study, serum aspartate aminotransferase (AST) and serum alanine-aminotransferase (ALT) values were increased in approximately 2% of patients .

Pyrantel should be used with caution in patients with severe malnutrition or anemia. Supportive therapy is recommended for anemic, dehydrated, or malnourished patients before administration of the drug .

Pyrantel pamoate has been placed in pregnancy category C. This refers to the fact that animal studies have revealed adverse effects on the fetus (teratogenic/embryocidal, or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus .Data on the use of pyrantel pamoate in pregnant women are quite limited. In mass treatment programs for which the World Health Organization (WHO) has observed that the benefits of treatment outweigh the risks, WHO allows the use of pyrantel pamoate in the 2nd and 3rd trimesters of pregnancy, due to the fact that the effects of pyrantel on birth outcome are uncertain. The risk of treatment in pregnant women already known to have an infection needs to be balanced with the risk of disease progression if treatment were to be omitted . Individuals with liver disease are more susceptible to the toxicity in cases of pyrantel overexposure , .

There are no data regarding the presence of pyrantel in breast milk. Pyrantel is poorly absorbed from the GI tract; therefore, excretion into breast milk may be minimal. Some experts recommend that a single dose of pyrantel therapy may be given to breastfeeding women .

Elimination Route

Rapidly absorbed (80%)

Pyrantel is poorly absorbed from the GI tract of humans , .

Peak serum concentrations occur 1–3 hours after a single dose .

Half Life

0.8-1.5 hours (in serum)

In pigs, following intravenous administration, pyrantel exhibited a half-life of 1.75 +/- 0.19 h .

Elimination Route

Approximately 50% of an oral dose is excreted unchanged in feces; 7% excreted in urine as unchanged drug and metabolites .

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