Piperazine
Mechanism :
Piperazine acts by paralysing parasites, which allows the host body to easily remove or expel the invading organism. This action is mediated by its agonist effects upon the inhibitory GABA receptor. Its selectivity for helminths is because vertebrates only use GABA in the CNS and the helminths GABA receptor is a different isoform to the vertebrate.
Indication :
Contraindications :
Liver disease, impaired renal function and epilepsy are contraindications to its use.
Dosing :
Oral: >2 years:
50-75 mg/kg PO. Repeat after 2 weeks for enterobiasis and monthly for 3 months if risk of ascariasis persists.
Adverse Effect :
In patients with neurological or renal abnormalities, nausea, vomiting, colic, diarrhoea, allergic reactions, dizziness, muscular incoordination, drowsiness has been reported.
Interaction :
Pyrantel: Antagonizes the mode of action of piperazine and therefore should not be administered concurrently.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Dose as in normal renal function |
| 10-20 | Dose as in normal renal function |
| <10 | Dose as in normal renal function but avoid repeated administration |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unknown dialysability. Dose as in GFR<10 mL/min |
| HD | Unknown dialysability. Dose as in GFR<10 mL/min |
| HDF/High flux | Unknown dialysability. Dose as in GFR<10 mL/min |
| CAV/VVHD | Unknown dialysability. Dose as in normal renal function |
Hepatic Dose :
Because piperazine is partially metabolized in the liver, accumulation of piperazine may occur in patients with hepatic function impairment, with an increased incidence of side effects