Artequick

Indications

• Malaria caused by Plasmodium falciparum
• Multidrug-resistant malaria
• Severe malaria

Dosage

Children: Refer to the BNF for Children for specific dosing guidelines in paediatric patients. Dosage is typically weight-based and may differ depending on the formulation used and the severity of the disease.

Adults: Refer to the BNF for specific dosing guidance. Generally, artemisinin is given as part of combination therapy, and the dosage may vary based on the specific formulation and clinical guidelines.

Mechanism of action

Artemisinin decreases lipid accumulation in hepatocytes by inhibiting CD36 expression and reducing TAG content. This mechanism is associated with its ability to disrupt the metabolism of malaria parasites and increase reactive oxygen species production, ultimately leading to parasite death.

Pharmacodynamics

The pharmacodynamics of artemisinin involves its rapid action against the malaria parasite. The drug is known to have a quick onset of action and effectively reduces parasitemia. Its efficacy is attributed to the production of free radicals that damage the parasite's membranes and essential cellular components, leading to cell lysis and death.

Pharmacokinetics

Artemisinin is well absorbed when administered orally, with peak plasma concentrations typically reached within 1 to 2 hours. It is extensively metabolized in the liver, primarily by cytochrome P450 enzymes, and has a half-life of about 1 to 3 hours, necessitating multiple doses for sustained antimalarial activity. The drug is excreted mainly in the urine, and its pharmacokinetics can be affected by factors such as food intake and the presence of other medications.

Pregnancy

Artemisinin use during pregnancy should be avoided, particularly in the first trimester, due to potential risks to the fetus. Alternative treatments for malaria should be considered.

Breast-feeding

Limited data are available on the excretion of artemisinin in human milk. Caution is advised when administering artemisinin to breastfeeding mothers.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Indications

• Plasmodium falciparum malaria
• Uncomplicated malaria
• Treatment of malaria in combination with other antimalarials

Dosage

Children: Refer to the BNF for Children for specific paediatric dosing information.

Adults: Refer to the BNF for specific dosing information based on the treatment regimen and patient condition.

Mechanism of action

The mechanism of piperaquine inhibition of the haem detoxification pathway is unknown but is expected to be similar to that of other antimalarial agents. It is thought to interfere with the parasite's ability to detoxify haem, leading to toxic accumulation within the parasite, thereby inhibiting its growth and replication.

Pharmacodynamics

Piperaquine exhibits a mechanism of action that inhibits the Plasmodium falciparum parasite's haem detoxification pathway. This action is crucial in preventing the survival of the parasite within the host, leading to a reduction in parasitemia and clinical symptoms associated with malaria.

Pharmacokinetics

Piperaquine displays a relatively long half-life, allowing for once-daily dosing in treatment regimens. It is well absorbed following oral administration, with peak plasma concentrations achieved within several hours. The drug is extensively distributed in body tissues, and its elimination involves hepatic metabolism and renal excretion. The pharmacokinetics may be influenced by various drug interactions.

Interactions

• grapefruit juice: Severe (increases concentration)
• mitotane: Severe (decreases concentration)
• St John's Wort: Severe (decreases concentration)
• rifampicin: Severe (decreases concentration)
• dronedarone: Unknown (increases concentration)
• cobicistat: Unknown (increases concentration)
• crizotinib: Unknown (increases concentration)
• idelalisib: Unknown (increases concentration)
• imatinib: Unknown (increases concentration)
• letermovir: Unknown (increases concentration)

Pregnancy

Data on the use of piperaquine in pregnancy are limited. Consult local guidelines for the management of malaria in pregnant women.

Breast-feeding

Piperaquine is excreted in breast milk; caution should be exercised when administering to breastfeeding women.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Formulations

• Piperaquine phosphate tablet

Mechanism of action

A 2025 systematic review notes that Artemisinin decreases lipid accumulation in hepatocytes by inhibiting CD36 expression and reducing TAG content.

Mechanism of action

The mechanism of piperaquine inhibition of the haem detoxification pathway is unknown but is expected to be similar to that of [DB00608].

Pharmacodynamics

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