Piperaquine

Piperaquine Uses, Dosage, Side Effects, Food Interaction and all others data.

Piperaquine is an antimalarial agent first synthesized in the 1960's and used throughout China . Its use declined in the 1980's as piperaquine resistant strains of Plasmodium falciparum appeared and artemisinin derivatives became available. It has come back into use in combination with the artemisinin derivative Artenimol as part of the combination product Eurartesim . Eurartesim was first authorized for market by the European Medicines Agency in October 2011.

Piperaquine inhibits the P. Falciparum parasite's haem detoxification pathway .

Piperaquine
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Piperaquine
Generic	Piperaquine
Type
Formula	C₂₉H₃₂Cl₂N₆
Weight	Average: 535.52 Monoisotopic: 534.2065505
Protein binding	Piperaquine's binding to plasma proteins is considered to be virtually complete . It has been measured to be >99% in humans, rats, and dogs.
Groups	Approved, Experimental, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

For the treatment of uncomplicated Plasmodium falciparum infection in adults, children, and infants aged 6 months and up weighing over 5 kg . Used in combination with Artenimol.

Piperaquine is also used to associated treatment for these conditions: Malaria caused by Plasmodium falciparum

How Piperaquine works

The mechanism of piperaquine inhibition of the haem detoxification pathway is unknown but is expected to be similar to that of Chloroquine.

Toxicity

Studies of piperaquine in monkeys and dogs have shown some hepatotoxicity and reversible depression in white blood cells and neutrophils . Additional observations include infiltration of macrophages with intracytoplasmic basophilic granular material consistent with phospholipidosis and degenerative lesions in numerous organs and tissues. These effects were seen at exposure levels similar to clinical dosing in humans. At high doses, piperaquine can interfere with cardiac conduction and produce effects on blood pressure. Mild phototoxicity has been observed with piperaquine in rats exposed to UV light.

Volume of Distribution

Piperaquine is thought to distribute into a central compartment with an apparent volume of 26.7 L/kg, and two peripheral compartments with apparent volumes of 76.8 L/kg and 617 L/kg . These combine for a total volume of distribution of 720.5 L/kg.

Elimination Route

Piperaquine is slowly absorbed and exhibits multiple peaks in its plasma concentration curve suggestive of enterohepatic recycling occurring alongside the absorption process . Due to this complication there is no discreet value for bioavailability but piperaquine is highly absorbed into systemic circulation. When taken with food, Cmax increases by 217% and mean exposure increases by 177%. Tmax is not affected by food and remains around 5 h . Piperaquine has been observed to accumulate more in females to a degree of 30-50% more than males . It also collects in red blood cells similar to Artenimol.