Antispermatogenic effects of artemether: An animal model

Various antimalarial drugs have been shown to exert different adverse effects; however, scanty information is available for artemether-induced potential side effects. The present study assessed effects of artemether on lipid profile, sperm count, and histological features of testes in an animal model. The mean total cholesterol, high-density lipoproteins, low-density lipoproteins, triglyceride, and total proteins in mice-administered artemether were higher compared with controls. The mean sperm counts in mice treated with artemether were reduced when compared with controls. In addition, it was observed that artemether affected the histopathology of seminiferous epithelia and Leydig cells. Evidence indicates that artemether exerts adverse effects in mice testes.     

Biochemical evaluation of hepatotoxicity in mice due to administration of artemether

Effects of artemether administration on liver and selected biochemical parameters were evaluated. Eighty albino mice were divided into four equal groups. Group 1 was given water which served as control, while groups 2, 3, and 4 were given 1.2, 2.4, or 4.8 mg kg^?1 body weight artemether intramuscularly for five consecutive days. On day 6 all mice were sacrificed by cervical dislocation and blood was collected for analysis of alanine and aspartate transaminases, alkaline phosphatase, copper, and total proteins. Liver tissues were prepared for histological studies. It was found that the serum alanine and aspartate transaminase and alkaline phosphatase activities were higher in groups treated with artemether compared to control. The serum concentrations of copper and total proteins were lower than control. The histological features of liver tissues after administration of artemether showed histopathological alterations. These findings showed that artemether administration may have reversible adverse effects on mouse hepatocytes.     

Assessment of the neurotoxicity of intramuscular artemether in mice

Artemether has been shown to be a very reliable antimalarial drug particularly because of its potency against multidrug resistant strain of malaria parasite; however, there is concern about its potential toxic effects. This study was designed to evaluate the neurotoxic effect of artemether using a mouse model. The photomicrographs of brains of the mice in the different artemether treated groups showed neurodegeneration. This observation is an indication that artemether may be neurotoxic in mice.     

Histopathological effects of artemether on selected organs in rat

Dose and treatment-duration neurotoxic effects are reported for artemisinin drugs of mostly the liposoluble derivatives; and yet artemether, the only parenteral formulation of the artemisinin series available in Nigeria is fat-soluble and also has a treatment-duration of 5–7 days (in an attempt to delay recrudescence). Since parenteral drugs are usually resorted to in severe/complicated or multidrug-resistant malaria against the oral artemisinin co-formulated therapies (ACT), this study is aimed to investigate the pathological changes on selected tissues (if any), in rats, of the normal 7-days artemether-injections when used both in the normal and higher doses. Artemether was administered i.p., at three dose levels, equivalent to therapeutic dose (1.5 mg kg^?1) as well as 5 and 10 times higher (7.5 and 15 mg kg^?1). A three percentage v/v Tween 80 vehicle was used for the control experiment. The pathological changes in the kidney, heart, liver, and lungs evaluated using percentage mean organ:body-weight ratio showed no changes in the organs. No histopathological effect was observed in the organs of rats treated with 1.5 mg kg^?1. However, rats treated with 7.5 and 15 mg kg^?1 revealed necrositic lesions with mononuclear cellular-infiltration in the liver and brain. The liver had focal area necrosis, while the brain had liquefactive necrosis, neuronal degeneration, congested blood vessels, hemorrhage, and vacuolations. The interstitial spaces of the glomerulus and renal tubules of one kidney from rats that received 15 mg kg^?1 had focal area fibrositic-necrosis.