FALCI CARE
SWISS PARENTERALS PVT
Identification
- Active ingredient (INN)
- ARTESUNATE
- Internal code
- 19 C 032
- Country of Origin
- India
- Pharmaceutical form
- Powder + Solvent for IV/IM Injectable Sol.
- Prescription List
- Highly Regulated (List I)
- Packaging
- b/01fl pdr de 5ml + 01 ampoule de 01ml de bicarbonate de sdium bp 5% (im) + 01 ampoule de 5ml de chloride de sodium bp 0.9% (iv)
DAWA Clinical Workbench v2.0
Information may not be accurate. Always consult a physician, pharmacist, or specialist before acting on any data shown here.
Description
Artesunate is indicated for the initial treatment of severe malaria.
Organization recommends artesunate as first line treatment for severe malaria.
Artesunate was developed out of a need for a more hydrophilic derivative of artemisinin.
Artesunate was granted
FDA approval on 26 May 2020.
Indications
Artesunate is indicated for the initial treatment of severe malaria in adult and pediatric patients.
Pharmacodynamics
Artesunate is an artemisinin derivative that is metabolized to DHA, which generates free radicals to inhibit normal function of Plasmodium parasites. 1, 7, 8 It has a short duration of action due to its short half life, and a moderate therapeutic index. 7, 8 Patients should be counselled regarding the risk of post treatment hemolytic anemia and hypersenstivity.
Absorption
C max of artesunate is 3.3 µg/mL while the C max of the active metabolite DHA is 3.1 µg/mL.
AUC of artesunate is 0.7 µgh/mL while the AUC of DHA is 3.5 µgh/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.
Volume of Distribution
The volume of distribution of artesunate is 68.5 L while the volume of distribution of DHA is 59.7 L.
Metabolism
Artesunate is rapidly metabolized to dihydroartemisinin (DHA) by plasma esterases.
DHA is glucuronidated by
UGT1A9 and UGT2B7 to DHA-glucuronide. 2, 8 DHA-glucuronide can undergo a minor metabolic pathway to for a furano acetate derivative of DHA-glucuronide.
CYP2A6 may minorly contribute to the metabolism of artesunate.
Hover over products below to view reaction partners Artesunate Dihydroartemisinin (DHA) Dihydroartemisinin Glucuronide Furano Acetate of Dihydroartemisinin Glucuronide.
Route of Elimination
The main route of elimination in humans is unknown.
In rats, a dose of artesunate is 56.1% eliminated in the urine and 38.5% in the feces.
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.
Clearance
The clearance of artesunate is 180 L/h while the clearance of DHA is 32.3 L/h.
Adverse Effects
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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.