| Artemether Pharmacology |
| Artemether |
| About Artemether |
| It is a derivative of artemesinin. Methylether of dihydroartemisinin, a novel sesquiterpene lactone very rapid schizontocidal, used to treat fever and malaria. |
| Mechanism of Action of Artemether |
| It is a schizonticidal drug. The endoperoxide bridges in Artemether are cleaved by the binding of haeme and liberate highly active free radicals. These radicals bind to membrane proteins and cause lipid peroxidation and damages endoplasmic reticulum. It also inhibits protein synthesis and lysis of the parasite. |
| Pharmacokinets of Artemether |
| Absorption: Artemether is orally well absorbed. Distribution: It is distributed in plasma protein bound form. Metabolism: It is metabolised in the liver to active dihydro artemisnin |
| Onset of Action for Artemether |
| N/A |
| Duration of Action for Artemether |
| N/A |
| Half Life of Artemether |
| 45 minutes |
| Side Effects of Artemether |
| 1.Nausea 2.Vomiting 3.Diarrhoea 4.Abdominal pain 5.Tinnitus 6.Reduction in reticulocyte and leucocytes count 7.Dizziness 8.Bradycardia 9.Pain at the site of injection |
| Contra-indications of Artemether |
| 1.Hypersensitivity to Artemether and other Artemisnin derivatives |
| Special Precautions while taking Artemether |
| 1.Renal impairment 2.Hepatic impairment 3.Cardiac failure 4.Monitor patients on concomitant use of drugs which cause prolongation of QT intervals |
| Pregnancy Related Information |
| Use with caution First trimester: contraindicated |
| Old Age Related Information |
| Use with caution |
| Breast Feeding Related Information |
| Contraindicated |
| Children Related Information |
| N/A |
| Indications for Artemether |
| 1.Multi drug resistant Malaria 2.Ceribral Malaria 3.Chloroquine resistant Malaria |
| Interactions for Artemether |
| Erythromycin, terfenadine, astemizole, quinidine, amiodarone, disopyramide, bretylium, bearidil, sotalol, TCAs should be avoided. |
| Typical Dosage for Artemether |
| Adult(IM)80 mg twice daily for 1 day followed by 80 mg once daily for 4 days Maximum dose: 480 mg for 5 days Children (IM): 3.2 mg/kg body weight /day in 2 divided dose followed by 1.6 mg / kg body weight / day once daily for 4 days Maximum dose: 9.6 mg / kg for 5 days |
| Schedule of Artemether |
| H |
| Storage Requirements for Artemether |
| Store at 15-30 degree C in a tightly closed container. Protect from heat and moisture. |
| Effects of Missed Dosage of Artemether |
| Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose. |
| Effects of Overdose of Artemether |
| Give supportive measures and symptomatic treatment. Drug can be removed from the body by gastric lavage or by inducing emesis. Absorption of the drug can be reduced by administration of activated charcoal. Excretion of the drug can be enhanced by administration of sodium bicarbonate. Haemodialysis can be done in emergency conditions. |