DHQHS 2

Absorption

The reported oral bioavailability of Artenimol was reported to be 45% in healthy adults . The observed Tmax was 1-2 h This is known to increase in malaria infected patients which could be attributed to reduced metabolism by the liver or the drug's collection in infected erythrocytes. Artenimol was obeserved to have flip-flop kinetics with an overall absorption half-life of 1.04 h. When administered with food the AUC for Artenimol increases by 144%. Cmax was observed to increase by 129% but was not found to be statistically significant. Food was observed to delay Tmax by 1 h.

Toxicity

In single dose studies in CD-1 male mice, Artenimol did not show signs of toxicity up to 1200 mg/kg .
In repeated dose studies in CD-1 mice, the NOAEL for Artenimol was determined to be 200 mg/kg/day . This value was determined to be 90 mg/kg/day in beagle dogs. The maximum tolerable dose in rats was observed to be 270 mg/kg/day. Doses of 540 mg/kg/day resulted in acute toxicity progressing to lethal effects. Toxicity was characterized by infiltration of macrophages and intracytoplasmic deposition of basophilic granular materials in macrophages consistent with phospholipidosis. Toxicity at high doses were accompanied by decreases in reticulocytes, and increases in AST and ALT.

Chemical properties

White Solid

The Uses of DHQHS 2

The main metabolite of Artemisinin, Arteether, Artemether, Artesunate. An active antimalarial metabolite

Indications

For the treatment of uncomplicated Plasmodium falciparum infection in adults, children, and infants aged 6 months and up weighing over 5 kg . Used in combination with Piperaquine.

Background

Artenimol is an artemisinin derivative and antimalarial agent used in the treatment of uncomplicated Plasmodium falciparum infections . It was first authorized for market by the European Medicines Agency in October 2011 in combination with Piperaquine as the product Eurartesim. Artemisinin combination therapy is highly effective against malaria and stongly recommended by the World Health Organization .

What are the applications of Application

Dihydro Artemisinin is An active antimalarial metabolite

Definition

ChEBI: Artenimol is an artemisinin derivative.

Pharmacokinetics

Artenimol is thought to form a reactive carbon radical intermediate which kills P. falciparum through alkylation of a wide array of proteins.

Metabolism

The primary metabolite of Artenimol is the glucuronide conjugate, α-artenimol-β-glucuronide . It is largely metabolized by UGT1A9 with some contribution by UGT2B7 .