| Artesunate Pharmacology |
| Artesunate |
| About Artesunate |
| A semi-synthetic derivative of artemisinin, a sesquiterpene lactone potent blood schizonticide, Anti malarial. |
| Mechanism of Action of Artesunate |
| This antimalarial drug binds tightly to parasitized erythrocyte membranes. Its endoperoxide bond is responsible for antimalarial activity. Release of an active oxygen species (free radicals) from this bond kills the parasite if accumulated in the erythrocytic cells. It also suppresses the production or activity of antioxidant enzymes in the erythrocytes, causing lysis of the parasitic cell due to the highly reactive free oxygen radicals. |
| Pharmacokinets of Artesunate |
| Absorption- Rapidly absorbed after administration Distribution- Widely distributed in the body. High concentration is seen in liver, kidney and intestine Metabolism- Metabolized in the liver to its metabolites Excretion- Excreted through urine and feces |
| Onset of Action for Artesunate |
| N/A |
| Duration of Action for Artesunate |
| N/A |
| Half Life of Artesunate |
| N/A |
| Side Effects of Artesunate |
| 1. Dizziness 2. Itching 3. Vomiting 4. Abdominal pain 5. Flatulence 6. Headache 7. Bodyache 8. Diarrhoea 9. Tinnitus 10. Alopecia 11. Macular rash 12. Neutropenia 13. Convulsions 14. Skin rash 15. Pruritis |
| Contra-indications of Artesunate |
| 1. Hypersensitivity to the drug or any ingredients of it 2. G6PD deficiency 3. Immunocompromised patients. |
| Special Precautions while taking Artesunate |
| Parenteral artesunate should be used for the treatment of severe falciparum malaria only where there is evidence that the antimalarial efficacy of quinine is declining. |
| Pregnancy Related Information |
| Contraindicated (1st trimester) |
| Old Age Related Information |
| May be used. |
| Breast Feeding Related Information |
| Use with caution |
| Children Related Information |
| May be used |
| Indications for Artesunate |
| 1.Uncomplicated falciparum malaria (in areas where there is evidence of chloroquine, pyrimethamine/sulfadoxine, mefloquine and quinine resistance). 2. Severe falciparum malaria (in areas where there is evidence of quinine resistance) |
| Interactions for Artesunate |
| NULL |
| Typical Dosage for Artesunate |
| Adults- Oral- Monotherapy: 4mg/Kg loading dose on the first day followed by 2mg/Kg once a day for 6 days Combination therapy: 4mg/Kg once a day for 3 days plus mefloqine (15mg or 25mg of base per Kg) as a single dose or split dose on the second and/or third day. Intramuscular- 2.4mg/Kg followed by 1.2mg/Kg at 12 and 24 hours then 1.2mg/Kg daily for 6 days. Intravenous- 2.4mg/Kg on the first day followed by 1.2mg/Kg daily Note: The speed for intravenous injection is 3-4 ml per minute |
| Schedule of Artesunate |
| H |
| Storage Requirements for Artesunate |
| Store in a cool dry dark place. |
| Effects of Missed Dosage of Artesunate |
| 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 Artesunate |
| Give symptomatic and supportive treatment |