Indication |
Used as alternative treatment for ascariasis caused by Ascaris lumbricoides (roundworm) and enterobiasis (oxyuriasis) caused by Enterobius vermicularis
(pinworm). It is also used to treat partial intestinal obstruction by
the common roundworm, a condition primarily occurring in children. |
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. |
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. |
Absorption |
Rapidly absorbed from the gastrointestinal tract |
Volume of distribution |
Not Available |
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). |
Route of elimination |
Not Available |
Half life |
Not Available |
Clearance |
Not Available |
Toxicity |
LD50 = 5 g/kg (Human, oral). Symptoms of overdose include muscle fatigue, seizures, and difficulty breathing. |
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