Artequick is a fixed dose Artemisinin-based combination therapy (ACT) which contains artemisinin and piperaquine. In their combination the drug artemisinin kills the malaria parasites and potentiates the effects of piperaquine, which has a long elimination half-life. The combination therapy permits a shorter duration of treatment, which improves compliance. The risk for drug resistance emerging of both artemisinin and piperaquine could be reduced by using the combination therapy.
Artemisinin is a sesquiterpene lactone isolated from the plant Artemisia annua L.Piperaquine is a member of the 4-aminoquinolone group of anti-malarial drugs.
Indications
Artequick® is indicated for the treatment of all forms of malaria, especially multiple drug-sesistant strains of P.falciparum
Pharmacological action
Artemisinin and piperaquine combination is of rapid action and low toxicity. The antimalarial activity of the combination is greater than that of either ingredient substances alone. In P.falciparum patients, 56-days cure rate of Artequick was above 95% and the time to fever clearance and the time to parasite clearance were 16 to 30 hours and 36 to 60 hours respectively.
The combination has significant gametocidal effect on falciparum malaria and thus interrupts the generation of gametocytes in bone marrow and reduces the risk of transmission. On plasmodium vivax, Artequick also has parasiticidal effects in intraerythrocyte stage.
Artemisinin and its semi-synthetic derivatives such as dihydroartemisinin and artesunate are typical schizonticides. Piperaquine is a 4-aminoquinolone compound. Studies in rodent malaria showed that the efficacy and cure rates of piperaquine were 2.6 and 6.6 times to those of chloroquine. Since 1978, piperaquine has been used widely to replace chloroquine as the first line treatment for malaria in China and it has been proven that its therapeutic efficacy is hingher than that of chloroquine while adverse effects are fewer
The results of acute toxicity tests in mice given the drug by intragastric administration showed that LD50 of Artequick was 1053.5mg/kg and the toxicity of the two components of the combination was not potentiated. Genetic toxicology tests showed that artemisinin and piperaquine combination has no mutagenic effects
Pharmacokinetics
Following oral administration, Artemisinin shows wide distribution, quick and complete absorption, rapid metabolism and excretion. The half-life of artemisinin is 1.6 to 2.6 hours. Some metabolites which have lost their antimalarial activity can be detected in urine and feces 48 hours later after oral artemisinin administration. The half-life of piperaquine is approximately 9.5 days in mice and not less than 14 days in blood.
Dosage and administration
Tablets for oral administration. In the event of vomiting within 1 hour of administration a repeat dose should be taken.
Adults: 2 tablets as a single dose at the time of initial diagnosis and then 2 tablets after 24 hours and 48 hours (total course comprises 6 tablets)
Children, 16 years and above: : 2 tablets as a single dose at the time of initial diagnosis and then 2 tablets after 24 hours and 48 hours (total course comprises 6 tablets)
Children, 11 to 15 years: 1 ½ tablets as a single dose at the time of initial diagnosis and then 1 ½ tablets after 24 hours and 48 hours
Children, 7 to 10 years: : 1 tablet as a single dose at the time of initial diagnosis and then 1 tablet after 24 hours and 48 hours
Adverse drug reactions
Artemisinin and piperaquine combination is well tolerated by children and adults, with most adverse events self-limited and being of mild to moderate severity and duration. Many of the reported adverse events are likely to be related to the underlying malaria rather than to the combination. Adverse effects caused by artemisinin and piperaquine combination are uncommon and rare cases of nausea, diarrhea, dizziness, abdominal pain, vomiting and anorexia have been reported.
Contraindications
Artequick is contraindicated
In the first trimester of pregnancy
In those with hypersensitivity to the active substances or any of the excipients
In case of severe malaria
Precautions
Artemisinin are known to be embryotoxicin in animal. Artequick is contraindicated during the first trimester of pregnancy.
Use with caution in patients with severe hepatic or renal dysfunctions.
Effects on ability to drive and use machines-Driving and use of machinery are not recommended due to risk of dizziness and fatigue
Drug interactions
There has been no report of drug interactions to date. As to the interaction with other antimalarials, data on safety and efficacy are limited so that Artequick should not be given concurrently with other antimalarials unless there is no other treatment option.
