Overview

Arteether is an effective anti-malarial medicine. It is used to treat severe malaria caused by Plasmodium falciparum strains when other medicines are not effective.  The injectable form is specifically used for severe malaria rather than quinine. I t may not be as effective as artesunate. It is given by injection in a muscle. It is also available by mouth in combination with lumefantrine, known as artemether/lumefantrine.

Therapeutic Indication

Arteether can treat both children and adults suffering from uncomplicated multi-drug resistant falciparum malaria or severe falciparum malaria.

PHARMACOLOGY

Mechanism of action:

Arteether is an artemisinin derivative and the mechanism of action for artemisinins is unknown. proposed mechanisms is that through inhibiting anti-oxidant and metabolic enzymes, artemisinin derivatives inflict oxidative and metabolic stress on the cell. Some pathways affected may concern glutathione and glucose metabolism. As a consequence, lesions and reduced growth of the parasite may result. Another possible mechanism of action suggests that arteristinin drugs exert their cidal action through inhibiting PfATP6. Since PfATP6 is an enzyme regulating cellular calcium concentration, its malfunctioning will lead to intracellular calcium accumulation, which causes cell death.

Pharmacodynamics:

Inside the body, Arteether is metabolized into the active metabolite metabolite dihydroartemisinin. The drug works against the erythrocytic stages of P. falciparum by inhibiting nucleic acid and protein synthesis. Artemether is administered in combination with lumefantrine for improved efficacy. It has a rapid onset of action and is rapidly cleared from the body. It is thought that artemether provides rapid symptomatic relief by reducing the number of malarial parasites. Lumefantrine has a much longer half life and is believed to clear residual parasites.

Pharmacokinetics:

Absorption of artemether is improved 2- to 3-fold with food. It is highly bound to protein (95.4%). Peak concentrations are seen 2 hours after administration. It is metabolized in the human body to the active metabolite, dihydroartemisinin, primarily by hepatic enzymes CYP3A4/5. Both the parent drug and active metabolite are eliminated with a half-life of about 2 hours .

Contraindications

This is contraindicated in :

Known hypersensitivity to artemotil and sesame oil

Treatment of uncomplicated falciparum malaria

Treatment of vivax malaria

Pregnancy and Lactation: Contact your doctor or pharmacist before using this.

Side Effects

Headache

Nausea or Vomiting

Dizziness

Body pain

Pain at the injection site

Chills and rigor

Watery diarrhea

Swelling of the liver