Artemether
Mechanism :
There are three common forms of artemisinin. The water-soluble form is called artesunate. It is the most active and the least toxic within the body. Artemether is the lipid soluble form. It has the longest life but also the most toxic in high dosage which is seldom needed. The biggest advantage of artemether is that it can cross the blood brain barrier. Artemisinin is the active parent compound of the plant. Its half-life is intermediate. It is also very safe and can cross the blood-brain barrier. Artemisinin has been shown to work through oxygen and carbon based free radical mechanisms. Artemether has been combined with lumefantrine for use as combination therapy orally.
Indication :
Contraindications :
First trimester of pregnancy.
Dosing :
3.2 mg/kg/IM loading dose followed by 1.6 mg/kg/IM after 24 hours & then 1.6 mg/kg/M 12 hourly till the child can eat orally. Then shift to oral therapy.
Artemether + Lumefantrine (Available as 20 mg of artemether + 120 mg
lumefantrine FDC or 40 mg of artemether + 240 mg
lumefantrine): oral therapy for 3 days.
Adverse Effect :
Gastrointestinal disturbances, dizziness, tinnitus and prolongation of QT interval.
Interaction :
Quinidine and halofantrine: Caution in concurrent usage with drugs that prolong QT interval.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Dose as in normal renal function |
| 10-20 | Dose as in normal renal function |
| <10 | Dose as in normal renal function |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unknown dialysability. Dose as in GFR<10 mL/min |
| HD | Unknown dialysability. Dose as in GFR<10 mL/min |
| HDF/High flux | Unknown dialysability. Dose as in GFR<10 mL/min |
| CAV/VVHD | Unknown dialysability. Dose as in normal renal function |
Hepatic Dose :
Mild to moderate hepatic impairment: Dosage adjustments are not recommended.
Severe hepatic impairment: Use with caution.