Piperaquine Specifications

Product Name	Piperaquinoline
CAS Registry Number	4085-31-8
Molecular Formula	C29H32Cl2N6
Molecular Weight	535.51 g/mol
Purity	>99.0 %
Appearance	White powder
Shelf life	2 years
Functions	highly active against chloroquine-resistant Plasmodium falciparum and Plasmodium vivax

Piperaquine Description

Piperaquine is an antiparasitic drug used in combination with dihydroartemisinin to treat malaria. It is a bis-quinoline compound that inhibits the vitro growth of P. falciparum isolates from malaria-infected patients with IC50s ranging from 11.8-217.3 nM. Piperaquine was developed under the Chinese National Malaria Elimination Programme in the 1960s and was adopted throughout China as a replacement for the structurally similar antimalarial drug chloroquine.

Piperazine phosphate has also recently become a potential drug against COVID-19.

[caption id="attachment_7486" align="alignnone" width="640"] Piperaquine[/caption]

Piperaquine Applications

• Used in combination with artemisinin to treat malaria
• Potential drug against SARS-COV-2

Piperaquine Mechanism of Action

The mechanism by which piperaquine inhibits the heme detoxification pathway is unknown but is expected to be similar to that of chloroquine. It acts by accumulating in the parasite's digestive vacuole and interfering with the detoxification of heme to hemozoin.

Piperaquine Mechanism Side Effects

While piperaquine is generally well-tolerated, it can cause some side effects. Common and serious side effects include:
Common Side Effects:
Gastrointestinal Issues: Nausea, vomiting, abdominal pain, and diarrhea.
Headache: Mild to moderate headaches can occur.
Dizziness: Some patients may experience dizziness or light-headedness.

Although clinical trials have found no evidence of cardiotoxicity, the World Health Organization recommends against the use of piperaquine in patients with congenital QT prolongation or who are taking other drugs that prolong the QT interval.
Additionally, studies of piperaquine in monkeys and dogs have shown some hepatotoxicity and reversible suppression of leukocytes and neutrophils.

Reference:

1. Akoachere, M., Buchholz, K., Fischer, E., et al. In vitro assessment of methylene blue on chloroquine-sensitive and -resistant Plasmodium falciparum strains reveals synergistic action with artemisinins. Antimicrob. Agents Chemother. 49(11), 4592-4597 (2005).
2. Davis TM, Hung TY, Sim IK, Karunajeewa HA, Ilett KF (2005). "Piperaquine: a resurgent antimalarial drug". Drugs. 65 (1): 75–87.
3. Haldar K, Bhattacharjee S, Safeukui I (2018). "Drug resistance in Plasmodium". Nature Reviews Microbiology. 16: 156–170.