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Piperazine | CAS No: 110-85-0 | GMP-certified suppliers
A medication that provides targeted treatment for ascariasis, enterobiasis, and roundworm‑related intestinal obstruction, supporting reliable management of common helminth infections in pediatric and general populations.
Therapeutic categories
Primary indications
- Used as alternative treatment for ascariasis caused by <i>Ascaris lumbricoides</i> (roundworm) and enterobiasis (oxyuriasis) caused by <i>Enterobius vermicularis</i> (pinworm)
- It is also used to treat partial intestinal obstruction by the common roundworm, a condition primarily occurring in children
Product Snapshot
- Oral small‑molecule anthelmintic supplied in multiple liquid and powder formulations for reconstitution
- Used for management of ascariasis, enterobiasis, and related roundworm‑associated intestinal obstruction
- Approved for human and veterinary use in Canada
Clinical Overview
Piperazine exerts its pharmacological effect by acting as a gamma‑aminobutyric acid receptor agonist at parasite neuromuscular sites. Direct binding to GABA receptors on helminth muscle membranes induces hyperpolarization of nerve endings, producing flaccid paralysis. The immobilized worm is then expelled intact through normal intestinal peristalsis. Piperazine hydrate and piperazine citrate are the forms most commonly employed in clinical practice, with similar functional properties.
After entry into systemic circulation, piperazine undergoes partial oxidative metabolism, while a proportion is eliminated unchanged. Available data indicate mixed renal and metabolic clearance mechanisms, although detailed pharmacokinetic parameters are not well defined in standard references.
Safety considerations include the need to avoid use in individuals with documented hypersensitivity to piperazine derivatives. Neurological reactions have been reported with excessive dosing or in patients with pre‑existing seizure disorders, consistent with the compound’s GABAergic activity. Use should be guided by local treatment guidelines, especially where alternative anthelmintics with broader spectra are available.
Piperazine has long-standing human and veterinary approval in multiple regions. It is not associated with specific brand names in the supplied data but is widely formulated as its hydrate or citrate salt.
For API procurement, sourcing should prioritize suppliers able to provide consistent control of residual solvents, impurities related to ring synthesis, and verified identity and purity of the piperazine base or its approved salts, supported by appropriate regulatory documentation.
Identification & chemistry
| Generic name | Piperazine |
|---|---|
| Molecule type | Small molecule |
| CAS | 110-85-0 |
| UNII | 1RTM4PAL0V |
| DrugBank ID | DB00592 |
Pharmacology
| Summary | Piperazine acts as a GABA receptor agonist on helminth muscle cells, producing membrane hyperpolarization and flaccid paralysis. This pharmacologic effect disrupts worm motility, enabling expulsion through normal intestinal transit. Its activity is primarily directed at GABA receptor subunit beta‑3, supporting use in infections caused by Ascaris and Enterobius species. |
|---|---|
| Mechanism of action | Piperazine is a GABA receptor agonist. Piperzine binds directly and selectively to muscle membrane GABA receptors, presumably causing hyperpolarization of nerve endings, resulting in flaccid paralysis of the worm. While the worm is paralyzed, it is dislodged from the intestinal lumen and expelled live from the body by normal intestinal peristalsis. |
| Pharmacodynamics | Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Gamma-aminobutyric acid receptor subunit beta-3 | Humans | agonist |
ADME / PK
| Absorption | Rapidly absorbed from the gastrointestinal tract |
|---|---|
| Protein binding | 60-70% |
| Metabolism | About 25% is metabolized in the liver. Piperazine is nitrosated to form N -mononitrosopiperazine (MNPz) in gastric juice, which is then metabolized to N-nitroso-3-hydroxypyrrolidine (NHPYR). |
Formulation & handling
- High aqueous solubility and small‑molecule character support simple oral liquid and solution formulations with minimal solubilization aids.
- Chemical stability is generally good, but hygroscopic solid handling may require controlled humidity during blending and packaging.
- Absorption is not affected by food, allowing flexible administration without specific fed‑state considerations in formulation design.
Regulatory status
| Lifecycle | In Canada, the API is now marketed in a post‑patent environment, indicating a mature phase with established generic availability. Market activity is stable, reflecting limited remaining lifecycle expansion opportunities. |
|---|
| Markets | Canada |
|---|
Supply Chain
| Supply chain summary | Piperazine has multiple historical originator and legacy pharmaceutical manufacturers, with current supply supported largely by generic producers and repackagers. Branded products appear mainly in the Canadian market, with no recent evidence of active US or EU brand promotion. Patent protection for piperazine expired long ago, so the ingredient is fully open to generic competition. |
|---|
Safety
| Toxicity | LD<sub>50</sub> = 5 g/kg (Human, oral). Symptoms of overdose include muscle fatigue, seizures, and difficulty breathing. |
|---|
- High oral LD50 (~5 g/kg in humans) indicates relatively low acute toxicity, but concentrated API should be handled to prevent accidental ingestion or dust exposure
- Overdose is associated with neuromuscular effects such as muscle fatigue, seizures, and respiratory compromise
- Processes should minimize risk of high-level exposure
Piperazine is a type of Anthelmintics
Anthelmintics belong to the pharmaceutical API subcategory used in the treatment of parasitic infections caused by helminths, commonly known as worms. These parasitic infections can affect various parts of the body, including the intestines, liver, and lungs. Anthelmintics act by either paralyzing or killing the helminths, thereby eliminating the infection.
There are different classes of anthelmintics, each targeting specific types of helminths. The benzimidazoles class includes compounds like albendazole and mebendazole, which disrupt the energy metabolism of the worms, leading to their paralysis and eventual death. Another class is the avermectins, which includes ivermectin and moxidectin. These compounds work by affecting the neurotransmitter functions in the worms, resulting in paralysis and death.
Anthelmintics are available in various formulations, including tablets, suspensions, and injectables, allowing for convenient administration to patients. Depending on the type and severity of the infection, the duration of treatment may vary.
When using anthelmintics, it is crucial to follow the prescribed dosage and duration to ensure the effective elimination of the parasitic infection. However, as with any medication, there may be potential side effects, such as gastrointestinal disturbances or allergic reactions, which should be monitored.
In conclusion, anthelmintics are a vital class of pharmaceutical APIs used to combat parasitic infections caused by helminths. Their targeted action and diverse range of formulations make them an essential tool in the fight against these debilitating conditions.
Piperazine (Anthelmintics), classified under Antiparasitics
Antiparasitics are a category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that are used to combat parasitic infections in humans and animals. These APIs play a crucial role in the field of medicine and veterinary care by targeting and eliminating various parasites, such as protozoa, helminths, and ectoparasites.
The use of antiparasitics is essential in preventing and treating parasitic diseases, which can cause significant health issues and even be life-threatening. These APIs work by interfering with the parasite's vital biological processes, such as reproduction, metabolism, and survival mechanisms.
Pharmaceutical companies develop and manufacture a wide range of antiparasitic APIs to cater to different parasitic infections. Some common examples of antiparasitics include anthelmintics (used against intestinal worms), antimalarials (used to treat malaria), and ectoparasiticides (used to control external parasites like ticks and fleas).
The development of antiparasitic APIs requires rigorous research, including the identification of suitable targets within the parasite's biology and the formulation of effective chemical compounds. Safety and efficacy are paramount in the manufacturing of antiparasitics, ensuring that they effectively combat the targeted parasites while minimizing adverse effects on the host.
Overall, antiparasitics are vital tools in the fight against parasitic infections, benefiting both human and animal health. Through ongoing research and development, the pharmaceutical industry continues to innovate and improve antiparasitic APIs, contributing to the advancement of healthcare and the well-being of individuals and their animal companions.
Piperazine API manufacturers & distributors
Compare qualified Piperazine API suppliers worldwide. We currently have 3 companies offering Piperazine API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| BAJAJ HEALTHCARE LTD | Producer | India | India | CoA, GMP, WC | 8 products |
| MOLTUS RESEARCH LABORATOR... | Producer | India | India | CoA | 1 products |
| Vital Laboratories Pvt. L... | Producer | India | India | CoA, WC | 22 products |
When sending a request, specify which Piperazine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Piperazine API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Piperazine API
Sourcing
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Technical
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Regulatory
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Pharmaoffer
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