Faldp

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

Faldp 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.

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

Trade Name Faldp
Generic Piperaquine
Type Capsule
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 Zuventus Health Care Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Faldp
Faldp

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.

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

How Faldp 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

Faldp 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

Faldp 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 . Faldp 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.

Half Life

The terminal elimination half-life was observed to be 576h or 24 days . This is thought to be due to the extensive distribution of piperaquine.

Clearance

The mean apparent total clearance has been observed to be 1.12 L/h/kg in adult malaria patients .

Elimination Route

Faldp is mainly excreted in the feces with a negligible amount in the urine .

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