Piperaquine is an anti malarial drug, which was the first quinolone synthesized in the 1960s, and was used extensively for the treatment of malaria in China.

The usage became obsolete as Plasmodium falciparum became resistant to Piperaquine, and that brought about its combination with artemisinin-based antimalarials.

It’s believed that Chinese scientists discovered that piperaquine became a suitable combination with artemisinin combination therapies (Acts).

Characteristics of Piperaquine

• Piperaquine has a slow absorption rate and a long biological half-life which makes it a good partner drug with artemisinin derivatives and is fast acting, although have a short biological half-life.
• Piperaquine has been used to replace Chloroquine and has played a huge role in the treatment of malaria.
• Piperaquine has a slow onset of action, but a long half-life which makes it unique and lasts as long as 36 days.
• When Piperaquine is taken orally, 80-90% of it is absorbed within 24 hours.
• Piperaquine is distributed in the body where it fights the parasite, especially in the liver, kidney, lungs, etc.
• Piperaquine cannot be easily gotten rid of because its half-life is always 9.4 days or more.
• Piperaquine goes out of the body through the bile.

Mode of action of Piperaquine

• Piperaquine always binds with hematin to form a toxic complex for the parasite inside its food vacuole
• Piperaquine, as a weak base, tends to have high lipophilic
• The properties of Piperaquine help to distribute drugs in a high volume when inside the parasite lipid membrane.

Characteristics of Dihydroartemisinin

• When administered orally, it facilitates its rapid absorption, and the maximum blood concentration is attained within 1 hour with a half-life of about 4 hours.
• It’s also distributed in the liver, kidneys, and bile.
• Dihydroartemisinin is excreted from the body through urine, and faeces within 24 hours.

Mode of action of Dihydroartemisinin

• Dihydroartemisinin is activated by heme which is present in the blood.
• Once they are activated, they form free radicals. which are made of carbon.
• These free radicals formed by carbon kill parasites in various ways.
• The free radicals formed by carbon damage the lipids and vacuole membrane of the parasite.
• They inactivate the parasite’s protein
• They also obstruct the conversion of hamatin to hemozoin.

This combination of Piperaquine and Dihydroartemisinin has shown highest cure rates as compared to other ACTs, and they clear the parasites about 99.8% witchin 24 hours. Although, some people react to this combination when administered.

Contraindications of Dihydroartemisinin and Piperaquine

• It’s not safe for pregnant women during the first 3 months of pregnancy.
• Patients who are hypersensitivity to any of the components should not take it.