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Praziquantel (Biltricide) syrup, a broad-spectrum anthelmintic agent, has revolutionized the treatment of parasitic infections caused by trematodes (flukes) and cestodes (tapeworms). Since its discovery in the 1970s, it has become the cornerstone of global schistosomiasis control programs and is widely used in veterinary medicine. This article provides an in-depth analysis of praziquantel syrup's chemical properties, pharmacodynamics, pharmacokinetics, clinical efficacy, safety profile, and emerging applications in pediatric and neglected tropical disease settings. Recent advancements in formulation development, including orally dispersible tablets (ODTs) for children, are also discussed to address gaps in current treatment strategies.
1.General Specification
(1)Injection
Customizable
(2)Paste
Customizable
(3)Sirop
Customizable
2.Customization:
We will negotiate individually, OEM/ODM, No brand, for secience researching only.
Internal Code: BM-3-045
Praziquantel CAS 55268-74-1
Analysis: HPLC, LC-MS, HNMR
Technology support: R&D Dept.-4
Additional information of chemical compound:
praziquantel +. COA
Mechanism of Action
Praziquantel (Biltricide) exerts its therapeutic effect by disrupting calcium ion homeostasis in parasitic worms. The drug induces a rapid influx of calcium ions into the parasite's musculature, causing severe spasms and paralysis. This disruption impairs the worm's ability to maintain its grip on host tissues, facilitating expulsion from the body. While the exact molecular targets remain under investigation, current evidence suggests that antagonizes voltage-gated calcium channels, leading to uncontrolled muscle contraction. Notably, it is less effective against juvenile schistosomes, with efficacy peaking around 6-7 weeks post-infection. This age-dependent susceptibility underscores the importance of timing in treatment protocols.
Clinical application
I. Core indications: covering the whole life cycle of parasitic infections
As a broad-spectrum antiparasitic drug, the clinical application of praziquantel syrup covers the three major types of parasitic infections, namely trematode, cestode, and cysticercus, and it is effective against worms at different developmental stages.
Schistosomiasis: a core drug for global control
It has a potent killing effect on both adult and child worms of Schistosoma japonicum, Schistosoma mansoni, and Schistosoma aegypti. Its mechanism of action includes:
Muscle spasmodic paralysis: the drug activates the slow calcium channels of the worm cells, which increases the inward flow of calcium ions, leading to the continuous contraction of the worm muscles, losing the ability to adsorb the host vascular wall, and being cleared by phagocytosis after entering the liver with the blood flow.
Cortical damage and immune clearance: destroy the epidermal structure of the worm, expose the body surface antigens, activate the host immune system (e.g., eosinophilic infiltration), and accelerate the death of the worm.
Hepatic schistosomiasis
Hepatic schistosomiasis (Chinese testicular schistosomiasis): the first choice of targeted treatment
Chinese testicular schistosomiasis parasitizes the liver and bile ducts, causing cholestasis, cirrhosis and even bile duct cancer. It blocks the energy metabolism of the worms by inhibiting their mitochondrial respiratory chain and protein synthesis.
Schistosomiasis
Schistosomiasis: rapid relief of respiratory symptoms
Schistosoma (Schistosoma weihei, Schistosoma sichuanensis) parasitizes the lungs, triggering symptoms such as coughing, coughing up sputum, chest pain, shortness of breath and so on. It works by destroying the cortex and muscular structure of the worms, leading to their death and elimination from the body:
Tapeworm
Tapeworm: broad-spectrum killing of intestinal parasites
It is highly effective in killing beef tapeworms, pork tapeworms, short membranous shell tapeworms and so on, and its mechanism includes:
Destroying the structure of the worm body: it acts on the head, neck and body segments of the tapeworms to make them dislodge from the intestinal wall and be discharged with the feces.
Inhibiting the development of eggs: blocking the life history of tapeworms and preventing recurrence.
Cysticercosis and encapsulation: key drugs to assist surgical treatment
Cysticercosis: It kills cysticerci in the brain and muscle, and reduces headache and epilepsy. The total dose is 120-180 mg/kg over 3-5 days, with the daily amount divided into 2-3 doses. Note that patients with cerebral cysticercosis need to be hospitalized and supplemented with dexamethasone and mannitol to prevent cerebral edema.
Cysticercosis: As an adjunct to surgery, it inhibits the growth of the worm (Echinococcus granulosus) and reduces postoperative recurrence. The total dose of 50mg/kg is given in 2 doses for 30 days.
What are the contraindications
Contraindications to the use of syrup include allergy to drug ingredients, patients with specific diseases, patients with specific infections, and behavioral contraindications during administration, as follows:
Allergy Contraindication:
Contraindicated in persons who are allergic to praziquantel or any of the excipients; allergic reactions may include severe symptoms such as rash, dyspnea, and anaphylaxis.
Disease Contraindications
Patients with severe cardiac, hepatic, or renal disease: It may aggravate cardiac burden and induce cardiac arrhythmias; metabolized in the liver, it may aggravate hepatic injury; excreted in the kidneys, it may aggravate renal burden. Therefore, it should be used with caution in patients with severe cardiac, hepatic and renal diseases, and under close monitoring when necessary.
People with a history of mental illness: it may cause dizziness, drowsiness and other neurological reactions, the use of people with a history of mental illness may aggravate the condition.
Contraindications for specific infections
Patients with ocular cysticercosis: praziquantel treatment of ocular cysticercosis may lead to destruction of the intraocular parasites, triggering irreversible lesions such as retinal detachment and loss of vision. Therefore, patients with ocular cysticercosis must have the worms surgically removed before drug treatment.
Patients with cerebral cysticercosis: praziquantel treatment for cerebral cysticercosis may cause serious complications such as cerebral edema, high cranial pressure, and even life-threatening. Therefore, patients with cerebral cysticercosis need to be hospitalized and supplemented with measures to prevent cerebral edema and reduce high cranial pressure.
Behavioral contraindications during medication
Prohibition: alcohol may irritate the gastrointestinal tract and aggravate the gastrointestinal adverse reactions caused by praziquantel, such as nausea, vomiting, abdominal pain. Therefore, alcohol should be abstained from during the medication and for 1 week after stopping the medication.
Abstaining from spicy and stimulating food: spicy and stimulating food may aggravate gastrointestinal adverse reactions, and may also induce allergic reactions. Therefore, spicy and irritating foods such as chili pepper, mustard, onion, garlic, etc. should be prohibited while taking the drug.
Avoid strenuous exercise: It may cause dizziness, headache, fever and other adverse reactions, and strenuous exercise may aggravate these symptoms and even cause accidents. Therefore, you should rest for a period of time after taking the medicine and avoid strenuous exercise.
Avoid driving or mechanical operation: Praziquentel may cause dizziness, drowsiness and other nervous system reactions, affecting the safety of driving or mechanical operation. Therefore, people with obvious dizziness, drowsiness and other neurological reactions, during the treatment period and within 24 hours after stopping the drug, do not carry out driving, mechanical operation and other work.
Drug interactions are contraindicated
Avoid taking with other anthelmintics: other anthelmintics may have bactericidal and insecticidal effects, and taking with praziquantel may lead to a decrease in the efficacy of the drug, or even aggravate the condition.
Avoid taking with strong cytochrome P450 (CYP450) inducers: such as rifampicin, may reduce the plasma concentration of praziquantel and affect the efficacy. If treatment with praziquantel must be used, rifampicin should be discontinued 4 weeks prior to the administration of praziquantel, and rifampicin therapy should be restarted one day after completion of praziquantel therapy.
Medication for special populations
Medication for children: two-dimensional adjustment for age and body weight
Note: Children need to adjust the dosage according to their body weight to avoid overdose leading to neurological reactions (e.g. dizziness, drowsiness).
Elderly: Liver function compensation ability assessment
Elderly people have decreased liver function compensation ability, drug metabolism slows down, it is recommended to use a low dose (such as 30mg/kg) and prolong the course of treatment, and monitor liver function indicators (ALT, AST).
Pregnant women and lactating women: caution in weighing the advantages and disadvantages
Pregnant women: It may affect the fetus through the placental barrier, and is contraindicated in the early stages of pregnancy; in the middle and late stages of pregnancy, it is necessary to weigh the severity of the infection against the risk of the drug, and use it under close monitoring if necessary.
Nursing women: the drug can be secreted into breast milk, need to suspend breastfeeding for 72 hours after taking the drug to avoid infant ingestion.
It remains indispensable in global health, offering a safe, effective, and affordable solution for parasitic infections. Its role in MDA programs, coupled with ongoing innovations in formulation and delivery, underscores its enduring relevance. However, challenges such as pediatric dosing, hepatic metabolism variability, and emerging resistance necessitate continued research and vigilance. As a cornerstone of neglected tropical disease control, praziquantel syrup exemplifies the synergy between pharmacological advancement and public health strategy, promising a future where parasitic infections are no longer a global scourge.
Frequently Asked Questions
What is praziquantel used for?
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Praziquantel is used to treat schistosoma (infection with a type of worm that lives in the bloodstream) and liver fluke (infection with a type of worm that lives in or near the liver). Praziquantel is in a class of medications called anthelmintics.
How quickly does It work?
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The time it takes for Praziquantel to start working depends on several factors, including the type of parasite, the dosage administered, and the individual's metabolism. However, in most cases, Praziquantel begins to take effect within 1 to 3 hours after ingestion.
Is ivermectin better than praziquantel?
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Highlights. Ivermectin and fenbendazole individually administered were effective against nematodes. Praziquantel was effective against cestodes, but not against nematodes. I+F+P were more effective than individual administration against nematodes and cestodes.
Who should not take praziquantel?
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Patients who have previously shown hypersensitivity to the drug. Since parasite destruction within the eye may cause irreparable lesions, ocular cysticercosis should not be treated with praziquantel.
How safe is praziquantel?
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Praziquantel is a well tolerated and safe drug. However, it may produce some side effects, the most common of which are abdominal pain, nausea, anorexia, diarrhea or loose stools, dizziness, headache, pruritis, skin eruption and fever, which appear shortly after the drug administration.
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