PIPERAZINE
Chemistry - Piperazine occurs as a white, crystalline powder that may have a slight odor. It issoluble in water and alcohol. Piperazine is available commercially in a variety of salts, includingcitrate, adipate, phosphate, hexahydrate and dihydrochloride. Each salt contains a variable amount ofpiperazine (base): adipate (37%), chloride (48%), citrate (35%), dihydrochloride (50-53%), hexahydrate (44%), phosphate (42%) and sulfate (46%).
Uses, Indications - Piperazine is used for the treatment of ascarids in dogs, cats, horses, swine andpoultry. Piperazine is considered to be safe to use in animals with concurrent gastroenteritis andduring pregnancy.
Contraindications/Precautions - Piperazine should be considered contraindicated in patientswith chronic liver or kidney disease, and in patients with gastrointestinal hypomotility. There issome evidence in man, that piperazine may provoke seizures in patients with a seizure history orwith renal disease when given in high dosages.
If used in horses with heavy infestations of P. equorum, rupture or blockage of intestines ispossible due to the rapid death and detachment of the worm.
Overdosage - Acute massive overdosage can lead to paralysis and death, but the drug is generallyconsidered to have a wide margin of safety. The oral LD50 of piperazine adipate in mice is 11.4g/kg.
In cats, adverse effects occur within 24 hours after a toxic dose is ingested. Emesis, weakness, dyspnea, muscular fasiculations of ears, whiskers, tail and eyes, rear limb ataxia, hypersalivation, depression, dehydration, head-pressing, positional nystagmus and slowed pupillary responses haveall been described after a toxic ingestion. Many of these effects may also be seen in dogs after toxicpiperazine ingestions.
Treatment is symptomatic and supportive. If ingestion was recent, use of activated charcoal and acathartic has been suggested. Intravenous fluid therapy and keeping the animal in a quiet, dark placeis also recommended. Recovery generally takes place within 3-4 days.
Piperazine and pyrantel/morantel have antagonistic modes of action and should generally not beused together.
The use of purgatives (laxatives) with piperazine is not recommended as the drug may beeliminated before its full efficacy is established.
Drug/Laboratory Interactions - Piperazine can have an effect on uric acid blood levels, butreferences conflict with regard to the effect. Both falsely high and low values have been reported.
Use results cautiously.
Storage, Stability, Compatibility
Unless otherwise specified by the manufacturer, piperazineproducts should be stored at room temperature (15-30°C).Pharmacology - PIPERAZINE
Piperazine is thought to exert "curare-like" effects on susceptible nematodes, thereby paralyzing or narcotizing the worm and allowing it to be passed out with the feces. Theneuromuscular blocking effect is believed to be caused by blocking acetylcholine at the myoneuraljunction. In ascarids, succinic acid production is also inhibited.Uses, Indications - Piperazine is used for the treatment of ascarids in dogs, cats, horses, swine andpoultry. Piperazine is considered to be safe to use in animals with concurrent gastroenteritis andduring pregnancy.
Pharmacokinetics - PIPERAZINE
Piperazine and its salts are reportedly readily absorbed from the proximalsections of the GI tract and the drug is metabolized and excreted by the kidneys. Absorptive, distribution and elimination kinetics on individual species were not located.Contraindications/Precautions - Piperazine should be considered contraindicated in patientswith chronic liver or kidney disease, and in patients with gastrointestinal hypomotility. There issome evidence in man, that piperazine may provoke seizures in patients with a seizure history orwith renal disease when given in high dosages.
If used in horses with heavy infestations of P. equorum, rupture or blockage of intestines ispossible due to the rapid death and detachment of the worm.
Adverse Effects, Warnings
Adverse effects are uncommon at recommended doses, but diarrhea, emesis and ataxia may be noted in dogs or cats. Horses and foals generally tolerate the drug quitewell, even at high dosage rates, but a transient softening of the feces may be seen. Other adverseeffects have been seen at toxic dosages, refer to the Overdosage section below for moreinformation.Overdosage - Acute massive overdosage can lead to paralysis and death, but the drug is generallyconsidered to have a wide margin of safety. The oral LD50 of piperazine adipate in mice is 11.4g/kg.
In cats, adverse effects occur within 24 hours after a toxic dose is ingested. Emesis, weakness, dyspnea, muscular fasiculations of ears, whiskers, tail and eyes, rear limb ataxia, hypersalivation, depression, dehydration, head-pressing, positional nystagmus and slowed pupillary responses haveall been described after a toxic ingestion. Many of these effects may also be seen in dogs after toxicpiperazine ingestions.
Treatment is symptomatic and supportive. If ingestion was recent, use of activated charcoal and acathartic has been suggested. Intravenous fluid therapy and keeping the animal in a quiet, dark placeis also recommended. Recovery generally takes place within 3-4 days.
Drug Interactions
Although data conflicts, piperazine and chlorpromazine may precipitateseizures if used concomitantly.Piperazine and pyrantel/morantel have antagonistic modes of action and should generally not beused together.
The use of purgatives (laxatives) with piperazine is not recommended as the drug may beeliminated before its full efficacy is established.
Drug/Laboratory Interactions - Piperazine can have an effect on uric acid blood levels, butreferences conflict with regard to the effect. Both falsely high and low values have been reported.
Use results cautiously.