Definition
Praziquantel is a systemic anthelmintic dewormer, used to treat several parasitic worm infections in mammals, amphibians, reptiles, birds, and fishes. It is to be taken orally and cannot be administered for eye worms. In humans, it especially acts against schistosomiasis and liver fluke infections, caused by worms found in Africa, Middle Eastern countries, South America, the Caribbean, and some parts of Asia. In animals, praziquantel is effective against the intestinal parasite and tapeworm. (1)(2)(3)(4)
Chemical and Physical Features
CAS number: 55268-74-1 (5)
Molecular Structure: (6)
Molecular Formula: C19H24N2O2 (6)
Weight: 312.4 g/mol. (6)
Appearance:
Praziquantel comes in powder or crystal form, which is then made into tablets, syrups, and injection forms.
Praziquantel in powder form- It is a white or almost white crystalline powder. (8)
Praziquantel as tablets- Praziquantel tablets are small and white, without any waxy coating.
Praziquantel as injections-It is a clear thick liquid.
Praziquantel tablets, when taken in combination can have other colors too (Drontal, containing praziquantel is yellow). (4)
Other Physical Features:
Praziquantel is a hygroscopic, white crystalline powder. It is slightly bitter and is odorless.
It is freely soluble in ethanol and dichloromethane. Slightly soluble in water and insoluble in ether.
Praziquantel produces toxic fumes and nitrogen oxides, upon combustion.
Praziquantel’s extinguishing agents’ are dry powder, foam, water spray, carbon dioxide, and sand. (7)
The tablets are recommended to be stored under 30℃ (or 86℉). (8)
Brand Names
For human use- Biltricide, Distocide, Milbemycin Oxime (oral oil suspension form)
For veterinarian use- Cestoved (tablet and injection form), Drontal, D-worm, Fish tapes, PraziPro, Milbemax, Praz-Tastic, Pure Prazi, Profender, Tapeworm tabs. (3)
Praziquantel forms and specifications
Praziquantel API Powder 99%
In powder form, praziquantel is a white crystalline with a bitter taste. It can be taken orally to treat schistosomiasis with a single dose of 40mg/kg body weight. Currently, the most available tablet form poses a bit of dosage and consumption issues. The 600mg tablet is not easily consumable for pediatric use. When it is crushed to be given to the children, it is difficult to consume due to its bitter taste and inaccurate dosage to the prescription. (8)
Praziquantel Tablets
The most common praziquantel tablet is the Biltricide. It is to be swallowed with water or crushed into powder and consumed by mixing with soft foods or liquids and not to be chewed or sucked, as the bitter taste might cause gagging or vomiting. It is not to be consumed along with any grapefruit preparations, as it results in side effects. Praziquantel Tablets are to be stored in an air-tight container at room temperature, away from moisture, direct light, and heat, and not to be frozen either. (9)
Praziquantel liquid
Praziquantel in liquid form is found in oil suspensions. It is to be consumed along with small amounts of food. It comes in a wide variety of flavors such as apple, banana, marshmallow, bacon/fish/beef/cheddar cheese, chicken, liver, chili pepper, strawberry, etc. The oral oil suspension is prescribed especially for dogs, cats, pocket pets, reptiles, and ferrets. It treats infection-parasitic, worms, and infection-cestodes. (10)
Praziquantel Injection
Dogs and cats are administered with injectable cestodes of praziquantel. It is a clear solution used for treating tapeworms and is given intramuscularly or subcutaneously. (11)
Milbemycin oxime and praziquantel
Interceptor Plus is a combination of milbemycin oxime and praziquantel and is used to treat heartworm disease, adult roundworm, adult hookworm, adult whipworm, and adult tapeworm in dogs and cats. (12)
Mechanism of action of Praziquantel
The exact mode of action is not completely known in certainty. However, there is evidence that praziquantel paralysis the muscles of the worm and also causes severe spasms, by influxing a sudden high dose of calcium ions. The morphological alterations caused due to this are then accompanied by antigens at the parasite surface. This destroys the worms completely, removing them from the stool.(3)
Praziquantel manufacturing process
Types of production process-
Synthesis through Isoquinoline route:
Praziquantel can be manufactured by various synthesis methods. The best and most common method is using the isoquinoline route. In this process, first, there is an adduct reaction between benzoyl chloride and isoquinoline, along with potassium cyanide. This is then carried forward through catalytic hydrogenation and chlorine acetylation. The final product is then produced post cyclization and hydrolysis through high pressure. (7)
Synthesis through phenethylamine route:
In this method phenethylamine is the raw material used. Chloroacetyl chloride is first used for acylation and then taken through an amination reaction with terephthalamide potassium. Further process of cyclization reaction results in dihydro isoquinoline derivative. Hydrogenation and hydrolysis are further conducted. Post this, acylation is performed using chloroacetyl chloride and cyclohexane carboxylic acid chloride. Praziquantel is finally obtained after dehydrochlorination and cyclization. (7)
Types of process involved- Direct compress, Wet and dry granulation:
WHO has ruled out the direct compression method due to the poor flow properties of the API. The most commonly used and convenient form of production is through wet granulation. The process involves multiple steps including raw material weighing, dry mixing, lubrication, and compression. (8)
Praziquantel uses
Praziquantel for cats- Praziquantel is effective against tapeworms and cestodes in cats. The Dipylidium caninum tapeworm in cats can be treated by administering small doses of 23mg-34mg tablets. (13)
Praziquantel for dogs- The most common tapeworm in dogs is Dipylidium caninum. Praziquantel is effective against these tapeworms.(4)
Praziquantel for humans- Praziquantel is used to treat schistosomiasis, clonorchiasis, opisthorchiasis, cysticercosis, and liver flukes in humans. (3)
Praziquantel for fish- Praziquantel is used to kill monogenetic and digenetic trematodes in fishes. It is available in bath form for treating fishes. (14)
Praziquantel dosage
Praziquantel under the name Biltricide is available in 600mg as tablets.
For humans- (1)
For schistosomiasis- Adults and children above 4 years of age- 20mg/kg 3 times per day for 1 day, every 4 to 6 hrs.
For clonorchiasis and opisthorchiasis- Adults and children above 4 years of age- 75mg/kg 3 times per day for 1 day, every 4 to 6 hrs.
For cysticercosis- Adults – 50-100 mg/kg 3 times per day every 8 hours for 14 days, Children above 4 years of age- 50-100 mg/kg 3 times per day every 8 hours for 30 days.
For Flukes- Adults and children above 4 years of age- 75mg/kg per day divided 3 times per day for 1-2 days
For tapeworms- Adults and children above 4 years of age- 5-10 mg/kg as a single dose.
For animals- (2)
For animal tapeworms- Cats and kittens 6 weeks of age – 4lbs and under- ½ tablet, 5-11lbs- 1 tablet, over 11lbs- 1.5 tablets.
For dogs and puppies of 4 weeks and above- 5lbs and under- ½ tablet, 6-10lbs- 1 tablet, 11-15lbs- 1.5 tablets, 16-30lbs- 2 tablets, 31-45lbs- 3 tablets, 46-60lbs- 4 tablets, over 60lbs- 5 tablets max.
Praziquantel side effects
The most common side effects include abdominal pain, allergic reaction, cerebrospinal reaction syndrome, dizziness, diarrhea, fever, drowsiness, itching, headache, malaise, mild rash, hives, sweating, feeling tired, upset stomach, and vomiting. (1)
Praziquantel API Price
The API price of Praziquantel powder is somewhere around $ 145/kg. (7)
Praziquantel API manufacturers in China
Below are some professional active pharmaceutical ingredients manufacturers in China.
Jiayi Pharmaceutical Co., Ltd: Jiayi Pharmaceutical Co., Ltd is involved in research and development, and sales and production of the APIs. The products have been registered and certified in countries like Japan, Brazil, India, Turkey, Australia, Iran, Russia, etc. Some of the products manufactured include Praziquantel, Doxycycline Hyclate, Colistin sulphate, Neomycin sulphate, Albendazole, Streptomycin sulphate, Avermectin B1, Ivermectin, Amoxicillin, etc. (15)
Zhejiang Hisun Pharma. Co., Ltd.: Zhejiang Hisun Pharmaceutical Co. Ltd., established in 1956, deals with the development, manufacturing, and commercialization of Generics, APIs, specialty, and animal health products. They produce tablets, capsules, and parenterals for cardiovascular, anti-infective, oncology, animal health, CNS, and other therapeutic areas of drugs. (16)
Valiant CO. , Ltd: Valiant CO., Ltd deals with pharmaceutical intermediates, environmentally friendly OLED materials, and life science and diagnostic reagents. (17)
Taizhou Yongfeng Chemical Industry Co., Ltd.: Taizhou Yongfeng Chemical Industry Co., Ltd. was built in 2011 in the province of Shandong. They are specialized in manufacturing pharmaceutical and pesticide intermediates. (18)
Yixing City Xingyu Pharmaceutical Co., Ltd.: Yixing City Xingyu Pharmaceutical Co., Ltd. was founded in 1993. They deal with APIs and intermediates. Their main products include 4-dimethoxy-2-butanone, N-(4-chlorobenzoyl)-tyramine, allopurinol, Aspirin, Praziquantel, 4-benzyly-2-oxazolidinone, and 4-phenyl-2-oxazolidinone. (19)
HEBEI MEIHE PHARMACEUTICALCO., LTD: HEBEI MEIHE PHARMACEUTICALCO., LTD was founded in 2006. They engage in focused production and sales of raw materials of Ivermectin. (20)
You can also find details around more suppliers for Praziquantel API in bulk at PharmaSources.com. PharmaSources.com is one of the leading and trustworthy vertical e-commerce online pharmaceutical marketplaces. It gives information on quality pharmaceutical products and suppliers for its esteemed customers and delivers services to 90,000+ active members. The services are provided to about 211 countries and regions. PharmaSources.com has been successfully selling over 1,600,000 products in 30 major pharmaceutical categories across the supply chain. (21)
FAQs:
Will praziquantel kill roundworms?
Praziquantel is used to treat several varieties of tapeworm, however, it does not protect dogs and cats against roundworms. (4)
What is the market size of praziquantel?
The global market for praziquantel is expanding and is expected to grow at a CAGR of 3.8% for the period 2020-2027. (23)
How often do I give praziquantel to my dog?
In most cases, it is a one-time treatment. However, it depends on the health of the animal and the exposure it has to the tapeworm disease and the infection. Animals with a higher risk of infection may require regular doses repeatedly. (4)
Sources:
1) https://www.rxlist.com/consumer_praziquantel_biltricide/drugs-condition.htm
2) https://web.stanford.edu/group/parasites/ParaSites2005/Praziquantel/Praziquantel.htm
3) https://en.wikipedia.org/wiki/Praziquantel
4) https://www.greatpetcare.com/pet-medication/praziquantel-for-dogs/
5)https://www.caymanchem.com/product/20508/praziquantel#:~:text=Praziquantel%20(Embay%208440%2C%20(%C2%B1,74%2D1)%20%7C%20Cayman%20Chemical
6) https://pubchem.ncbi.nlm.nih.gov/compound/4891
7) https://www.chemicalbook.com/ChemicalProductProperty_EN_CB8178956.htm
8) https://www.usp-pqm.org/sites/default/files/pqms/article/product-information-report-praziquantel-091319.pdf
9) https://www.webmd.com/drugs/2/drug-8873/praziquantel-oral/details
10) https://www.wedgewoodpharmacy.com/items/praziquantel-oral-oil-suspension.html
11) https://www.drugs.com/vet/praziquantel-injection.html
12) https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=86b367e3-64e5-4c44-9961-6caea5d12e75
13) https://www.msdvetmanual.com/pharmacology/anthelmintics/praziquantel-and-epsiprantel
14) https://www.vin.com/apputil/content/defaultadv1.aspx?id=3980162&pid=11107&print=1
15) http://chjyyy.com/info/About-Us-1-1.htm
16) http://www.hisunusa.com/about-us/company-profile/
17) http://www.valiant-cn.com/enOverview/
18) http://www.yongfengchemical.com/index.html
19) http://www.xingyu-chem.com/pages/eindex.html
20) http://en.meihe-pharm.com/
21) www.Pharmasources.com
22) https://www.go4worldbusiness.com/find?searchText=praziquantel&BuyersOrSuppliers=suppliers#Suppliers
23) https://www.datamintelligence.com/research-report/schistosomiasis-drugs-market
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