Usage
Piperazine is an anthelmintic medication primarily prescribed for treating intestinal roundworm (ascariasis) and pinworm (enterobiasis or oxyuriasis) infections. It belongs to the pharmacological classification of anthelmintics, specifically, it’s a GABA receptor agonist. Piperazine works by paralyzing the worms, which are then expelled from the body through the digestive tract.
Alternate Names
Piperazine is also known as piperazine hexahydrate, piperazine citrate, piperazine adipate, and piperazine phosphate, depending on the specific salt form. Brand names vary regionally; some examples include Pripsen, Antepar, Vermizine, and Ascalix.
How It Works
Pharmacodynamics: Piperazine acts as a GABA receptor agonist at the neuromuscular junction of susceptible helminths (worms). By mimicking the action of GABA, it causes an influx of chloride ions into the worm’s muscle cells, leading to hyperpolarization and flaccid paralysis of the worm’s musculature. This paralysis prevents the worms from maintaining their position in the intestine, and they are subsequently expelled in the feces.
Pharmacokinetics: Piperazine is readily absorbed from the gastrointestinal tract. It is metabolized in the liver and excreted primarily by the kidneys. The elimination half-life is relatively short, generally within 24 hours.
Mode of Action: Piperazine’s anthelmintic activity results from its agonist action on GABA receptors in the worm’s neuromuscular system. This leads to paralysis of the worm.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: Piperazine primarily acts through GABA receptor agonism. No significant enzyme inhibition or other neurotransmitter modulation has been reported.
Elimination Pathways: Piperazine is predominantly eliminated through renal excretion, with some hepatic metabolism.
Dosage
Dosage guidelines for piperazine vary depending on the infection being treated, the patient’s age and weight, and the specific piperazine salt used. It is crucial to consult specific product information and consider renal function before prescribing.
Standard Dosage
Adults:
- Roundworm: 3.5 g of piperazine hexahydrate orally per day for two consecutive days. Treatment may be repeated after one week.
- Pinworm: 65 mg/kg of body weight orally per day for seven consecutive days. Treatment may be repeated after one week.
Children:
- Dosing is typically weight-based, and accurate dosing must be determined by the physician. General guidelines are available based on age, but weight-based calculations are preferred, especially in young children.
Special Cases:
- Elderly Patients: Dose adjustments may be necessary based on kidney function.
- Patients with Renal Impairment: Dosage should be reduced in patients with impaired kidney function. Contraindicated in severe renal impairment.
- Patients with Hepatic Dysfunction: Use with caution; dosage adjustments may be necessary. Contraindicated in severe hepatic dysfunction.
- Patients with Comorbid Conditions: Use with caution in patients with epilepsy or neurological disorders.
Clinical Use Cases
Piperazine is not typically used in settings like intubation, surgical procedures, mechanical ventilation, ICU, or emergency situations. Its use is primarily limited to outpatient treatment of intestinal helminth infections.
Dosage Adjustments
Dose adjustments are required for patients with renal or hepatic impairment. Dosage should be reduced in patients with mild to moderate renal impairment.
Side Effects
Common Side Effects:
Nausea, vomiting, abdominal pain, diarrhea, headache, dizziness, drowsiness, muscle weakness, and tremors.
Rare but Serious Side Effects:
Allergic reactions (rash, itching, hives, swelling), visual disturbances (blurred vision, nystagmus), ataxia, seizures (especially in patients with pre-existing seizure disorders), and extrapyramidal symptoms.
Long-Term Effects:
Long-term effects are generally not observed with the typical short-term use of piperazine.
Adverse Drug Reactions (ADR):
Serious ADRs include severe allergic reactions, seizures, and severe neurological effects.
Contraindications
- Hypersensitivity to piperazine.
- Severe renal or hepatic impairment.
- Epilepsy or history of seizures.
Drug Interactions
- Pyrantel pamoate: Antagonistic effect; avoid concurrent use.
- Phenothiazines (e.g., chlorpromazine): May potentiate adverse effects.
- CNS depressants: Additive effects; use with caution.
Pregnancy and Breastfeeding
Pregnancy Safety: Piperazine should be avoided during pregnancy, particularly in the first trimester, unless absolutely necessary. Consult with a physician to assess the risks and benefits.
Breastfeeding: Piperazine is excreted in breast milk. Mothers may need to interrupt breastfeeding or express and discard milk for a period after taking piperazine, as advised by their physician.
Drug Profile Summary
- Mechanism of Action: GABA receptor agonist, leading to flaccid paralysis of worms.
- Side Effects: Nausea, vomiting, diarrhea, dizziness, headache, allergic reactions, neurological effects.
- Contraindications: Hypersensitivity, severe renal/hepatic impairment, epilepsy.
- Drug Interactions: Pyrantel, phenothiazines, CNS depressants.
- Pregnancy & Breastfeeding: Use with caution; consult a physician.
- Dosage: Varies depending on infection and patient factors; consult product information.
- Monitoring Parameters: Observe for neurological symptoms and allergic reactions.
Popular Combinations
Piperazine is not typically used in combination with other anthelmintics.
Precautions
- General Precautions: Assess for allergies, renal/hepatic function, and neurological history before prescribing.
- Specific Populations: Use with caution in pregnant/breastfeeding women, children, and the elderly.
- Lifestyle Considerations: May cause drowsiness or dizziness; advise patients to avoid operating machinery or driving.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Piperazine?
A: Dosage varies; see the “Dosage” section for details based on age, weight, and infection type. Consult specific product information.
Q2: How does Piperazine work?
A: Piperazine paralyzes worms by acting as a GABA receptor agonist in their neuromuscular system.
Q3: What are the common side effects of Piperazine?
A: Nausea, vomiting, diarrhea, headache, dizziness, and drowsiness.
Q4: Is Piperazine safe during pregnancy?
A: It’s generally avoided unless absolutely necessary. Consult a physician.
Q5: Can Piperazine be used during breastfeeding?
A: It is excreted in breast milk. Consult a physician for guidance.
Q6: What are the contraindications for Piperazine?
A: Hypersensitivity, severe renal/hepatic impairment, and epilepsy.
Q7: Does Piperazine interact with other medications?
A: Yes, it can interact with pyrantel pamoate, phenothiazines, and CNS depressants.
Q8: What should I monitor in patients taking Piperazine?
A: Observe for neurological symptoms and allergic reactions.
Q9: What type of infection does Piperazine treat?
A: Roundworm (ascariasis) and pinworm (enterobiasis) infections.
