1. I. Basic Information on Piperazine Citrate Product​

Chinese Name:柠檬酸哌嗪 (Níngméngsuān Pàiqín); 枸橼酸哌嗪 (Jǔyuánsuān Pàiqín)

English Name: Piperazine Citrate

CAS Number: CAS 144-29-6 (Anhydrous), CAS No.: 41372-10-5 (Hydrate). Commercially available products are generally the hydrate form.

Molecular Formula:C₁₀H₁₆N₂O₇ (Note: Typically exists as a hydrate, commonly with the molecular formula C₁₀H₁₆N₂O₇ · 3H₂O)

Molecular Weight:642.66 (Hydrate)

Appearance:White crystalline powder or small translucent crystals.

Properties:Odorless, sour taste. Highly soluble in water, slightly soluble in ethanol, and practically insoluble in organic solvents such as ether

and chloroform. Its aqueous solution is acidic.Piperazine citrate is the salt formed from piperazine (a six-membered heterocyclic amine) and

citric acid. This salt form improves the stability and water solubility of piperazine, making it more suitable for pharmaceutical and veterinary applications.

II. Synthesis Methods of Piperazine Citrate​

The industrial synthesis of piperazine citrate typically follows this route:

Preparation of Piperazine:​

Common starting materials are ethanolamine (NH₂CH₂CH₂OH) or ethylenediamine (NH₂CH₂CH₂NH₂).

Ethanolamine Method:Ethanolamine reacts with ammonia under high temperature and pressure, cyclizing and dehydrating to

                                      form piperazine, often catalyzed by metals like nickel or cobalt.

Ethylenediamine Method:Ethylenediamine can react with ethylene oxide or undergo condensation under specific conditions

                                           to also produce piperazine.

Salt Formation Reaction:​​

The prepared piperazine (often piperazine hexahydrate) is dissolved in water or ethanol.

While stirring, citric acid is added slowly according to the stoichiometric ratio (approximately a 3:2 molar ratio of piperazine to citric acid).

The reaction equation can be simplified as:

3 C₄H₁₀N₂ + 2 C₆H₈O₇ → 2 (C₄H₁₀N₂)₃ · 2C₆H₈O₇ (or written as C₁₀H₁₆N₂O₇)

After the reaction is complete, high-purity piperazine citrate crystals are obtained through cooling crystallization, filtration, washing, and drying.

This process is technologically mature, offers high yield, and is suitable for industrial-scale production.

​III. Main Uses of Piperazine Citrate​

The primary use of piperazine citrate is as an anthelmintic (dewormer). Its mechanism of action involves anticholinergic effects that paralyze

the muscles of the parasites, causing them to detach from the host's intestinal wall and be expelled in the feces.

Human Medicine:

Mainly used to treat ascariasis (roundworm infection) and enterobiasis (pinworm infection). It is particularly effective against roundworms.

Common Dosage Forms: Tablets, syrups ("Pagoda Candy"), granules.

Due to its relatively high safety profile, it was widely used for deworming children. However, its use in human medicine has declined with the advent of newer, more efficient, broad-spectrum anthelmintics (such as albendazole and mebendazole).

Veterinary Field:​​

Widely used for deworming poultry (chickens, ducks), livestock (pigs, cattle, sheep), and pets.

Used to treat infections caused by nematodes like roundworms and pinworms in animals.

Often administered as a premix added to feed or dissolved in drinking water.

Chemical Intermediate:​

Serves as an important raw material and intermediate for synthesizing other piperazine derivatives (such as norfloxacin, quinolone antibiotics, psychotropic drugs, etc.).

Usage Precautions​

Safety:​​

Piperazine citrate has low toxicity and is relatively safe. However, adverse reactions can occur with overdose.

Common Adverse Reactions: Include gastrointestinal effects such as nausea, vomiting, abdominal pain, diarrhea, as well as headache, dizziness, drowsiness, and rash. Symptoms are usually mild and transient.

Serious Adverse Reactions: Rare neurological symptoms such as ataxia, tremor, visual disturbances, and seizures have been reported, typically associated with excessive doses.

Contraindications and Precautions:​​

Contraindications: Hypersensitivity to the product, patients with severe liver or kidney impairment, and individuals with a history of neurological disorders (e.g., epilepsy).

Special Populations: Should be used with caution in pregnant and breastfeeding women; use only under the guidance of a physician.

Interactions: Concurrent use with phenothiazine drugs (e.g., chlorpromazine) may increase the risk of seizures and should be avoided.

Usage and Dosage:

Strictly adhere to the dosage and course of treatment prescribed by a doctor or specified on the product label. Dosage varies significantly for different indications (roundworm vs. pinworm) and populations (adults vs. children); do not self-adjust the dose.

For pinworm treatment, due to the high risk of reinfection, a second course after 2-4 weeks is often necessary. Emphasis on personal hygiene (frequent handwashing, changing underwear) is crucial to prevent reinfection.

Storage and Handling:​​

Store in a sealed container in a cool, dry place to prevent moisture absorption.

When handling as a chemical, use appropriate protective equipment (e.g., gloves, mask) to avoid inhaling dust or direct contact with skin and eyes.

Summary:​​ Piperazine citrate is a classic and effective anthelmintic. Although its role in human medicine has diminished, it remains valuable in veterinary medicine and as a chemical intermediate. The key to its use is safety, rationality, and adherence to instructions.

Disclaimer:​​ The above information is for educational purposes only and does not substitute for professional medical or veterinary advice.

Always consult a doctor or qualified professional before using any medication.