Artesul

Artesul Uses, Dosage, Side Effects, Food Interaction and all others data.

Artesunate is a potent and rapidly-acting blood schizontocide derived from the leaves of the chinese herb, Armesia annua. The exact mode of action is not clear but clinical studies have confirmed the effectiveness of artesunate in P. vivax and falciparum malaria.

Artesunate is an artemisinin derivative that is metabolized to DHA, which generates free radicals to inhibit normal function of Plasmodium parasites. It has a short duration of action due to its short half life, and a moderate therapeutic index. Patients should be counselled regarding the risk of post treatment hemolytic anemia and hypersenstivity.

A long acting sulfonamide that is used, usually in combination with other drugs, for respiratory, urinary tract, and malarial infections.

Sulfadoxine helps inhibit the enzyme dihydropteroate synthetase which is an enzyme necessary in the conversion of PABA to folic acid. As folic acid is vital to the synthesis, repair, and methylation of DNA which is vital to cell growth in Plasmodium falciparum. With this vital nutrient lacking, the parasite has difficulty in reproducing.

Artesul
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Artesul
Generic	Artesunate + Sulfadoxine
Type	Tablet
Therapeutic Class
Manufacturer	Zafa Pharmaceutical Laboratories (pvt) Ltd,
Available Country	Pakistan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Artesunate can quickly and reliably control the acute attack of malaria. It is suitable to salvage the patients with pernicious malaria and treat P. falciparum malaria and P. vivax malaria. It is effective against malaria caused by chloroquine resistant strain of plasmodium falciparum.

Sulfadoxine is a long acting sulfonamide used for the treatment or prevention of malaria.

Sulfadoxine is used in combination with pyrimethamine for the treatment or prevention of malaria. It can also be used to treat various infections in livestock as well. Sulfadoxine and pyrimethamine is indicated for the treatment of Plasmodium falciparum malaria in those patients in whom chloroquine resistance is suspected.

Artesul is also used to associated treatment for these conditions: Acute Uncomplicated Plasmodium Falciparum Malaria, Malaria, Cerebral, Severe MalariaPlasmodium Infections

How Artesul works

Artesunate is metabolized to the active DHA. the endoperoxide bridge of DHA reacts with heme, generating free radicals which inhibit protein and nucleic acid synthesis of the Plasmodium parasites during all erythrocytic stages. Reactions with these free radicals can also lead to alkylation of parasitic proteins such as a calcium adenosine triphosphatase and EXP1, a glutathione S-transferase.

Sulfadoxine is a sulfa drug, often used in combination with pyrimethamine to treat malaria. This medicine may also be used to prevent malaria in people who are living in, or will be traveling to, an area where there is a chance of getting malaria. Sulfadoxine targets Plasmodium dihydropteroate synthase and dihydrofolate reductase. Sulfa drugs or Sulfonamides are antimetabolites. They compete with para-aminobenzoic acid (PABA) for incorporation into folic acid. The action of sulfonamides exploits the difference between mammal cells and other kinds of cells in their folic acid metabolism. All cells require folic acid for growth. Folic acid (as a vitamin) diffuses or is transported into human cells. However, folic acid cannot cross bacterial (and certain protozoan) cell walls by diffusion or active transport. For this reason bacteria must synthesize folic acid from p-aminobenzoic acid.

Dosage

Artesul dosage

Adult: 5 days treatment: on the 1st day 2 tablets twice and 2nd day onward 1 tablet twice daily for remaining 4 days

Children:

1-3 years: 5 days treatment: on the 1st day ½ tablet twice and 2nd day onward ¼ tablet twice daily for remaining 4 days
4-5 years: 5 days treatment: on the 1st day 1 tablet twice and 2nd day onward ½ tablet twice daily for remaining 4 days
6-12 years: 5 days treatment: on the 1st day ½ tablet twice, 2nd day 1 tablet twice and 3rd day onward ½ tablet twice daily for remaining 3 days

Prophylmcis: 100 mg tablet once a week, from 1 week before entering malarial areas, to 4 weeks after leaving the area.

Side Effects

Transient and reversible reticulocytopaenia, drug fever, rash, bradycardia, transient 1st-degree heart block and reversible elevation of serum transaminases.

Toxicity

Data regarding overdoses of artesunate are rare. Patients experiencing an overdose may present with pancytopenia, melena, seizures, multiorgan failure, and death. Treat overdose with symptomatic and supportive measures.

Precaution

Hepatic or renal insufficiency; Pregnancy and lactation.

Interaction

Antimalarial potentiating action seen with mefloquine, primaquine and tetracycline. Additive effect with chloroquine. Antagonistic effect with pyrimethamine and sulphonamides.

Volume of Distribution

The volume of distribution of artesunate is 68.5L while the volume of distribution of DHA is 59.7L.

Elimination Route

The C_max of artesunate is 3.3µg/mL while the C_max of the active metabolite DHA is 3.1µg/mL. The AUC of artesunate is 0.7µg*h/mL while the AUC of DHA is 3.5µg*h/mL. After intravenous artesunate, DHA has a T_max of 0.5-15 minutes in adult patients and 21-64 minutes in pediatric patients. Intramuscular artesunate has a T_max of 8-12 minutes. Infants less than 6 months old will have a higher AUC due to an undeveloped UGT metabolic pathway.

Half Life

The elimination half life of artesunate is 0.3h with a range of 0.1-1.8h. The elimination half life of DHA is 1.3h with a range of 0.9-2.9h. Half life after intramuscular administration is 48 min in children and 41 min in adults.