Description of Artemisinin and Piperaquine
Artemisinin and Piperaquine is an antimalarial combination drug. This drug is a fixed dose Artemisinin based Combination Therapy (ACT), and each tablet contains artemisinin 62.5 mg and piperaquine 375 mg.
Pharmacology and Toxicology of Artemisinin and Piperaquine
Thia drug is used for the treatment of malaria, particularly drug-resistant falciparum malaria. It Is well tolerated and has rapid action, high efficacy, low toxicity and offers a short course treatment. Using artequick to treat falciparum malaria with 56-day follow-up, the results showed that the cure rate was >95%, the fever and parasite clearance time were 16-30 and 36-60 hours respectively. Artemisinin and Piperaquine also has parasiticidal effect on plasmodium vivax in intraerythrocyte stage.
Artemisinin in these tablets has powerful and quick parasiticidal effect on those parasites in intraerythrocyte stage. Moreover, its efficacy is much quicker than that of quinine, chloroquine and all other nonartemisinin antimalarial drugs. It therefore relieves clinical symptoms much faster. This product has significant gametocidal effects on falciparum malaria thus interrupts the generation of gametocytes in bone marrow and reduces the transmission.
The resistance culture showed that the drug resistance to this product is hard to occur. Piperaquine is a 4-aminoquinolone compound. Studies of the pharmacodynamic and toxicological properties in rodent malaria showed that the efficacy and curative index of piperaquine were 2.6 and 6.6 times higher than those of chloroquine. Since 1978, piperaquine has been used widely to replace chloroquine to treat malaria in China and proven its higher therapeutic efficacy and fewer side effects than those of chloroquine.
The results of acute toxicity tests in mice given the drug by intra-gastric administration showed that LDs of the product was 1053.5 mg/kg, and the toxicity of the combination of the two components was not potentiated but additive.
Genetic toxicology tests showed that the product has no mutagenic effects. It was showed that artemisinin, one component of the product has fetus toxicity in the 9-14 day pregnant mice, mainly represented as absorptive fetus.
Taking this product consecutively with high dose would induce slight injury of the liver function and decrease of reticulocyte count, but this change is reversible, and it can recover quickly after quitting the drug
Pharmacokinetics of Artemisinin and Piperaquine
After taking orally, Artemisinin shows wide distribution, quick and complete absorption, rapid metabolism and excretion. The half-life of artemisinin is 1.6-2.6 hrs.
Some metabolites which have lost their antimalarial activity can be detected in urine and feces 48 hours later after orally taking artemisinin. Piperaquine has a long half-life with 9.5 days in mice and not less than 14 days in the blood.
Indications and Uses of Artemisinin and Piperaquine
It is intended for the treatment of malaria attacks, especially for falciparum and vivax malaria.
Dosage and Administration of Artemisinin and Piperaquine
For adults, give 2 tablets at 0 hr and 2 tablets at 24 hrs with 4 tablets as total dosage or directed by the physician.
For children, a two-dose regimen is recommended with 1 to 2 tablets dose, grouped as follows. The tablet may be broken and crushed before giving.
Children dosage schedule by age groups as follows:
- Age 16 and above: Give 2 tablets at 0 hr and 2 tablets at 24 hrs.
- Age 11 to 15 years: Give 1½ (one and half) tablets at 0 hr and 1½ (one and half) tablets at 24 hrs.
- Age 7 to 10 years: Give 1 tablets at 0 hr and 1 tablets at 24 hrs
Adverse Effects of Artemisinin and Piperaquine
The adverse or Side effects are mainly gastrointestinal tract symptoms. The occurrence rate of nausea is 0%-5% and vomiting in 0%-2% Abdominal pain, diarrhea, dizziness, etc. are observed occasionally.
Since long half-life antimalarial is contained in this combination, patients with serious hepatic or renal dysfunction are not advised to take this drug repeatedly within 15 days.
Artemisinin and Piperaquine and PREGNANCY
The product should not be used in the first trimester of pregnancy. It is safe for use during lactation.
Artemisinin and Piperaquine Use in Children
Please follow doctor’s advice
Artemisinin and Piperaquine Use in Elderly Patients
The product can be used in geriatric patients.
Artemisinin and Piperaquine Drug Interactions
No related report.
Artemisinin and Piperaquine Overdose and Treatment
The main symptoms of Artemisinin and Piperaquine overdose include nausea, vomiting, dizziness, fatigue or numb feeling of the face. If it is the case, emetic and purgative agent can be used to accelerate the discharge of the drug
Storage of Artemisinin and Piperaquine
The product should be protected from light and humidity, and kept in dry and cool place
Shelf Life of Artemisinin and Piperaquine