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Artemether
Botanical source: artemisia annua
CAS: 71963-77-4
Molecular formula: C16H26O5
Molecular weight: 298.38
Formulation: White crystalline powder
Purity: 99%
Synonyms: Riamet, Coartem, dihydroartemisinin methyl ether，Artemether Injection, Artem, Haojiami(Chinese Pin Yin)
What is Artemether?
Artemether is a methyl ether derivative of artemisinin, which is a peroxide lactone isolated from the Chinese anti-malarial plant, Artemisia annua. Artemether, from the definition of Wikipedia,is an anti-malarial for the treatment of multi-drug resistant strains of falciparum malaria. Its combination (co-formulation) with Lumefantrine has first been marketed by Novartis under the brand names Riamet and Coartem. Today, this combination therapy is available as generic from several manufacturers, and Hunan keyuan Bio-products co., Ltd is one of the largest real manufacturers within China, with plant growing base and factory in Shaoyang, Hunan province, and Shanghai Natural Bio-engineering as the sales office and R&D center in Shanghai. Artemether is synthesized from Artemisinin using methanol and a catalyst in hydrochloric acid medium. This results in the production of predominantly βα-artemether. The alpha-epimer is also present and causes a difficult purification of the product. The pure alpha product behaves differently and has a melting point of 100 ℃ whereas the βα-epimer has a melting point of 84-86℃. Both the alpha and the βα-epimers are active antimalarials. It is the purification and separation of alpha fromβαthat leads to low yields and hence this increases the cost price of Artemether significantly.
Working principle of artemether (mechanism of action)
How does artemether work? As Artemether becomes popular in anti-malarial sector, how it works makes experts interested. Artemether treats malaria by killing the Plasmodium parasite. Although it is not entirely known how it does this, it is thought that the medication prevents Plasmodium from using blood glucose for energy and from making proteins and nucleic acid, which are essential for the parasite to live.
Artemether interacts with ferriprotoporphyrin IX (“heme”), or ferrous ions, in the acidic parasite food vacuole, which results in the generation of cytotoxic radical species. The generally accepted mechanism of action of peroxide anti-malarias involves interaction of the peroxide-containing drug with heme, a hemoglobin degradation byproduct, derived from proteolysis of hemoglobin. This interaction is believed to result in the formation of a range of potentially toxic oxygen and carbon-centered radicals. Numerous studies have investigated the type of damage oxygen radicals may induce. For example, Pandey et al. have observed inhibition of digestive vacuole cysteine protease activity of malarial parasites by artemether. These observations were supported by ex vivo experiments showing accumulation of hemoglobin in the parasites treated with artemether in and inhibition of hemozoin formation by malaria parasites. Electron microscopic evidence linking artemisinin action to the parasite's digestive vacuole has been obtained showing that the digestive vacuole membrane suffers damage soon after parasites are exposed to artemether. This would also be consistent with data showing that the digestive vacuole is already established by the mid-ring stage of the parasite's blood cycle, a stage that is sensitive to artemether but not other antimalarials.
Benefits of taking artemether-containing medicine drug
Artemether is famous as the anti-malarial drug,and as well as Anthelmintic, Anticancer and other uses. The detailed key benefits of artemether are as below:
Artemether and Antimalarial benefits
Artemether is highly effective against the blood schizonts of both malarial parasites P. falciparum and P. vivax. It is available as mono-therapy but usually applied in combination with lumefantrine in clinical treatments of malaria. World Health Organization guidelines for the treatment of uncomplicated falciparum malaria recommend the use of this artemisinin-based combination therapy, and approved by Swissmedic in December 2008 and recently approved by the United States Food and Drug Administration (FDA). Zambia was the first African country to adopt artemether/lumefantrine (commonly called Coartem) as first-line therapy in national malaria treatment guidelines in 2002. Clinical records show that by 2008, the rates of in-patient malaria cases and deaths decreased by 61% and 66%, respectively, compared with the 2001-2002 reference period. In South Africa also the number of malaria-related outpatient cases and hospital admissions to each fall by 99% from 2001 to 2003, and malaria-related deaths decreased by 97% over the same period. The efficacy of the six-dose regimen of Coartem has been confirmed in many different patient populations around the world, consistently achieving 28-day polymerase chain reaction-corrected cure rates of >95% in the evaluable population, rapidly clearing parasitaemia and fever, and demonstrating a significant gametocidal effect, even in areas of widespread parasite resistance to other antimalarials.Coartem is much more effective than quinine, the classical antimalarial. Randomised clinical trial in Uganda shows cure rate of malaria as high as 96% in the Coartem-treated group compared with 64% for the quinine group.[4] For Plasmodium vivax infection, combination with piperaquine is more effective than Coartem.
Artemether has been assigned to category C by the FDA on the basis of animal data which shows an association with fetal-loss and deformity. However, clinical data appears to show that artemether is safe in pregnancy. A meta-analysis of 14 clinical trials that looked at artemether use in a total of 945 pregnant women did not find evidence of harm and a clinical trial of artemether-lumefantrine designed to look at this question found fewer adverse events in the 138 pregnant women treated with artemther-lumefantrine than women treated with quinine.
Artemether and Anthelmintic benefits
During early 1980s Chinese scientists, by serendipity, discovered that artemether was not only an antimalarial agent, but also effective against the blood flukes. Eventually, laboratory experiments have confirmed the broad spectrum of activity against different trematodes, including all human schistosomes, Clonorchis sinensis, Fasciola hepatica and Opisthorchis viverrini.These studies revealed that artemether exhibits the highest activity against juvenile stages of the trematodes, while adult worms are significantly less susceptible. In addition, there are no indications of neurotoxicity following repeated high doses. Randomized controlled clinical trials confirmed that artemether, orally administered at a dose of 6 mg/kg once every 2–3 weeks, results in no drug-related adverse effects, and significantly reduces the incidence and intensity of schistosome infections, including those of Scistosoma mansoni, S. japonicum and S. haematobium
Artemether and Anticancer benefits
Artemether has been shown to have significant anticancer and antitumor activities. It is demonstrated that artemether caused strong inhibitory effects on brain glioma growth and angiogenesis in rats. It exhibits a dose- and time-dependent cytotoxicity, and induced apoptosis and G2 cell cycle arrest in ovarian cancer cell lines, human leukemia HL60 cells,and human pancreatic cancer BxPC-3 and AsPC-1 cells
Other uses
Some medications have more than one effect on the body. In addition to anti malarial action Artemether has analgesic–antipyretic effects on the body by relieving pain and reducing fever.
Dosage of artemether
For both uncomplicated and severe falciparum malaria, the recommended dose schedule is 3.2 mg/kg on day 1, followed by 1.6 mg/kg daily for up to 7 days. An oral dose of approximately 2 mg/kg daily, for up to 7 days has also been suggested for the treatment of uncomplicated malaria.
For the combined artemether (20 mg)/ lumefantrine (120mg) tablet preparation, a dose of artemether (80 mg)/ lumefantrine (500 mg) given to adult patients (travellers returning to Europe after visiting tropical countries) at the time of diagnosis, and repeated at 6-8, 24 and 48 h is recommended.
For the treatment of patients who have no natural immunity, an adult dose of artemether 80 mg/ lumefantrine 500 mg given at the time of initial diagnosis, and repeated after 8, 24, 36, 48 and 60 h is suggested.
Children’s doses should be scaled appropriately as recommended in the manufacturer’s international product information.
Disease state based dosing:
Renal failure: Although clearance decreases in patients with acute renal failure, overall the data suggest no dosage adjustment is necessary.
Side effect of taking artemether medications
Some side effects of artemether may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
If any of the following side effects, such as Abdominal or stomach pain, chills, cough, fever, headache, muscle aches occur while taking artemether, please check with your doctor immediately.