Pharmacokinetics of arteether in dog

Benakis, A.; Schopfer, C.; Paris, Maria; Plessas, Ch. T.; Karayannakos, P; Dondas, I.; D, Kotsarelis; Plessas, S. T.; Skalkeas, G

doi:10.1007/bf03189978

Cited by 13 publications

(6 citation statements)

References 2 publications

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“…After oral administration, artemisinin is completely absorbed, but due to a high first-pass effect, a relatively low bioavailability is seen. It has been suggested that the finding that these drugs are rapidly eliminated from the circulation could be explained by an interaction with proteins [127]. Intramuscular injection of a suspension in oil results in a rapid absorption and relatively high plasma peak concentrations.…”

Section: [I I 0 124]mentioning

confidence: 99%

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Progress in the research of artemisinin-related antimalarials: An update

et al. 1994

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Artemisinin, a sesquiterpene lactone endoperoxide isolated from Artemisia annua L., and a number of its semisynthetic derivatives have shown to possess antimalarial properties. They are all effective against Plasmodium parasites that are resistant to the newest and commonly used antimalarial drugs. This article gives a survey of the literature dealing with artemisinin-related antimalarial issues that have appeared from the end of 1989 up to the beginning of 1994. A broad range of medical and pharmaceutical disciplines is covered, including phytochemical aspects like the selection of high-producing plants, analytical procedures, and plant biotechnology. Furthermore, the organic synthesis of artemisinin derivatives is discussed, as well as their mechanism of action and antimalarial activity, metabolism and pharmacokinetics, clinical studies, side-effects and toxicology, and biological activities other than antimalarial activity.

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Section: [I I 0 124]mentioning

confidence: 99%

“…After rectal administration, in the form of suppositories or an aqueous suspension, the absorption is incomplete. Artemisinin is rapidly distributed over the tissues, passes the erythrocyte wall, the bloodbrain barrier, the salivary glands and the placenta [127].…”

Section: [I I 0 124]mentioning

confidence: 99%

Progress in the research of artemisinin-related antimalarials: An update

et al. 1994

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“…Furthermore, AE has a relatively long elimination half -life compared to other artemisinins, especially AS (e.g., Refs. [1,6,13]). AL is similar to AS in that it is also water-soluble.…”

Section: Introductionmentioning

confidence: 99%

Behavioral and neural toxicity of the artemisinin antimalarial, arteether, but not artesunate and artelinate, in rats

Genovese

Newman

Brewer

2000

Pharmacology Biochemistry and Behavior

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Three artemisinin antimalarials, arteether (AE), artesunate (AS), and artelinate (AL) were evaluated in rats using an auditory discrimination task (ADT) and neurohistology. After rats were trained on the ADT, equimolar doses of AE (25 mg/kg, in sesame oil, n=6), AS (31 mg/kg, in sodium carbonate, n=6), and AL (36 mg/kg, in saline, n=6), or vehicle (sodium carbonate, n=6) were administered (IM) for 7 consecutive days. Behavioral performance was evaluated, during daily sessions, before, during, and after administration. Histological evaluation of the brains was performed using thionine staining, and damaged cells were counted in specific brainstem nuclei of all rats. Behavioral performance was not significantly affected in any rats treated with AS, AL, or vehicle. Furthermore, histological examination of the brains of rats treated with AS, AL, and vehicle did not show damage. In stark contrast, all rats treated with AE showed a progressive and severe decline in performance on the ADT. The deficit was characterized by decreases in accuracy, increases in response time and, eventually, response suppression. When performance on the ADT was suppressed, rats also showed gross behavioral signs of toxicity that included tremor, gait disturbances, and lethargy. Subsequent histological assessment of AE-treated rats revealed marked damage in the brainstem nuclei, ruber, superior olive, trapezoideus, and inferior vestibular. The damage included chromatolysis, necrosis, and gliosis. These results demonstrate distinct differences in the ability of artemisinins to produce neurotoxicity. Further research is needed to uncover pharmacokinetic and metabolic differences in artemisinins that may predict neurotoxic potential.

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“…A large number of comparative studies have been done to determine the kinetic parameters of artenimol, artesunate, artemether, arteether and artelinate in the plasma of rats and those of arteether also in dogs [4,5] . A comparison of human data is presented in table 1 [6] .…”

Section: Artemisinin Pharmacokineticsmentioning

confidence: 99%

Pharmacokinetic and Toxicological Profile of Artemisinin Compounds: An Update

et al. 2009

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Artemisinin has been used effectively in malaria treatment. With the emerging resistance to malaria, the optimum and judicial use of the drug has become important. The drug metabolism and toxicology can have an impact on the therapeutic profile and clinical use of this antimalarial agent. In this review, we discuss the pharmacokinetics and toxicological aspects of artemisinin and its therapeutic implications. Artemisinins have several dosing routes including oral, intramuscular, intravenous and rectal. With repeated dosing, artemisinin has propensity for autoinduction, leading to decreased plasma levels on repeated dosing. Combination with other antimalarials in most cases did not influence the pharmacokinetics of artemisinins. Interactions with cytochrome P₄₅₀ inhibitors are known but these neither affect the efficacy nor the toxicity of the respective derivative. Artemisinins are generally regarded to be of low toxicity. Two major problems associated with them are neurotoxicity and reproductive toxicity. But the extent of this neurotoxicity is dependent on the nature of the compound, on the route of administration, and on the nature of the formulation. Moreover, it occurs in humans at very high doses. However, as a matter of precaution, the use of artemisinins in the first trimester of pregnancy has been contraindicated.

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Pharmacokinetics of arteether in dog

Cited by 13 publications

References 2 publications

Progress in the research of artemisinin-related antimalarials: An update

Progress in the research of artemisinin-related antimalarials: An update

Behavioral and neural toxicity of the artemisinin antimalarial, arteether, but not artesunate and artelinate, in rats

Pharmacokinetic and Toxicological Profile of Artemisinin Compounds: An Update

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