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Artemether

$52

  • Brand : BIOFRON

  • Catalogue Number : BD-D0979

  • Specification : HPLC≥98%

  • CAS number : 71963-77-4

  • Formula : C16H26O5

  • Molecular Weight : 298.38

  • PUBCHEM ID : 68911

  • Volume : 20mg

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Catalogue Number

BD-D0979

Analysis Method

Specification

HPLC≥98%

Storage

-20℃

Molecular Weight

298.38

Appearance

White powder

Botanical Source

This product is isolated and purified from the herb of Artemisia annua L.

Structure Type

Category

SMILES

CC1CCC2C(C(OC3C24C1CCC(O3)(OO4)C)OC)C

Synonyms

ArteMos/Artesaph/3,12-Epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin, decahydro-10-methoxy-3,6,9-trimethyl-, (5aS,6R,8aS,9R,10S,12R,12aR)-/Dihydroqinghaosu Methyl Ether/Gvither/Artesian/Larither/(4S,5R,8S,9R,10S,12R,13R)-10-Methoxy-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0.0]hexadecane/3,12-Epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin, decahydro-10-methoxy-3,6,9-trimethyl-, (3R,5aS,6R,8aS,9R,10S,12R,12aR)-/Falcidol/SM-224/Paluther/ArtenaM/(1R,4S,5R,8S,9R,10S,12R,13R)-10-Methoxy-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0.0]hexadecane/Artemether/MalarteM/(3R,5aS,6R,8aS,9R,10S,12R,12aR)-10-methoxy-3,6,9-trimethyldecahydro-3,12-epoxy[1,2]dioxepino[4,3-i]isochromene

IUPAC Name

Applications

Fatal neurotoxicity of arteether and artemether.[Pubmed: 7943542]Enhanced antimalarial activity by a novel artemether-lumefantrine lipid emulsion for parenteral administration.[Pubmed: 24982079]Antimicrob Agents Chemother. 2014 Oct;58(10):5658-65. Artemether and lumefantrine (also known as benflumetol) are difficult to formulate for parenteral administration because of their low aqueous solubility. Cremophor EL as an emulsion excipient has been shown to cause serious side effects. METHODS AND RESULTS: This study reports a method of preparation and the therapeutic efficacies of novel lipid emulsion (LE) delivery systems with Artemether, lumefantrine, or Artemether in combination with lumefantrine, for parenteral administration. Their physical and chemical stabilities were also evaluated. Furthermore, the in vivo antimalarial activities of the lipid emulsions developed were tested in Plasmodium berghei-infected mice. Artemether, lumefantrine, or Artemether in combination with lumefantrine was encapsulated in an oil phase, and the in vivo performance was assessed by comparison with artesunate for injection. It was found that the lumefantrine lipid emulsion (LUM-LE) and Artemether-lumefantrine lipid emulsion (ARM-LUM-LE-3) (1:6) began to decrease the parasitemia levels after only 3 days, and the parasitemia inhibition was 90% at doses of 0.32 and 0.27 mg/kg, respectively, with immediate antimalarial effects greater than those of the positive-control group and constant antimalarial effects over 30 days. CONCLUSIONS: LUM-LE and ARM-LUM-LE-3 demonstrated the best performance in terms of chemical and physical stabilities and antiplasmodial efficacy, with a mean particle size of 150 nm, and they have many favorable properties for parenteral administration, such as biocompatibility, physical stability, and ease of preparation.Am J Trop Med Hyg. 1994 Sep;51(3):251-9. Artemisinin (qinghaosu) and several derivatives have been developed and are in use as antimalarial drugs but scant information is available regarding animal or human toxicity. Following a eight-day, multiple-dose, pharmacokinetic study of arteether (AE) (10 mg/kg/day [n = 6] and 20 mg/kg/day [n = 6]) in dogs, all high-dose animals displayed a progressive syndrome of clinical neurologic defects with progressive cardiorespiratory collapse and death in five of six animals. Neurologic findings included gait disturbances, loss of spinal and pain response reflexes, and prominent loss of brain stem and eye reflexes. Animals had prolongation of QT interval corrected for rate (QTc) on electrocardiograms (ECGs) with bizarre ST-T segment changes. Prominent neuropathic lesions were noted to be primarily limited to the pons and medulla. Similar lesions with dose-related severity were noted in eight other dogs studied in a second study with intramuscular (IM) administration of AE in sesame oil during a 28-day, dose-ranging study using 5, 10, 15, and 20 mg/kg/day. Injury, graded by a pathologist blinded to the dose group, showed a dose-related, region-specific injury in all animals that was most pronounced in the pons. Further studies in Sprague-Dawley rats using IM administration of AE and Artemether (AM) at a dose of 12.5-50 mg/kg/day for 28 days confirmed the onset of a clinical neurologic syndrome with dose-related changes in body weight, activity, and seizure-like activity, stereotypic movement disorders, and ECG changes

Density

1.2±0.1 g/cm3

Solubility

Methanol; Chloroform

Flash Point

140.5±27.8 °C

Boiling Point

357.5±42.0 °C at 760 mmHg

Melting Point

86-89ºC

InChl

InChl Key

SXYIRMFQILZOAM-HVNFFKDJSA-N

WGK Germany

RID/ADR

HS Code Reference

Personal Projective Equipment

Correct Usage

For Reference Standard and R&D, Not for Human Use Directly.

Meta Tag

provides coniferyl ferulate(CAS#:71963-77-4) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate

No Technical Documents Available For This Product.

PMID

31481806

Abstract

BACKGROUND:
Malaria is a public health problem compounded with a widespread emergence of drug-resistant Plasmodium falciparum which necessitated the formulation of a new antimalarial drug policy (AMP).

OBJECTIVE:
This study was designed to assess adherence to the policy among physicians in health facilities in Delta state, Nigeria.

DESIGN:
Cross-sectional, analytic study. Data were collected with a semi-structured questionnaire.

SETTING:
Two secondary and one tertiary health facilities in Delta State, Nigeria.

PARTICIPANTS:
Physicians selected with a simple random technique from the facilities.

MAIN OUTCOME MEASURES:
Prescribing pattern of antimalarial drugs and adherence to WHO treatment guideline among doctors.

RESULTS:
Majority (90.8%) of respondents believed the antimalarial policy (AMP) should be strictly adhered to, although three-fifth (61.0%) of them rated its performance as poor. The level of adherence to the national antimalarial drug policy was high (78.5%) as most doctors prescribed Arthemeter-Lumefantrine, AL for uncomplicated malaria however barely two-fifth (35.4%) adhered to prescribing injectable Artesunate for complicated malaria. AL, (71.9%) was the most prescribed antimalarial drug for uncomplicated malaria The most prescribed antimalarial drugs for complicated malaria was artesunate (40.0%) followed by quinine (27.6%) and artemether (26.7%); although, chloroquine was also prescribed.

CONCLUSION:
The level of adherence to AMP among doctors was sub-optimal. Continuous education of doctors on the new AMP is needed to achieve malarial control.

FUNDING:
No funding was received for this study.

KEYWORDS

Adherence; antimalarial; drug policy; guidelines; resistance

Title

Adherence to antimalarial drug policy among doctors in Delta State, Nigeria: implications for malaria control.

Author

Obiebi IP1.

Publish date

2019 Jun

PMID

31378747

Abstract

Lung cancer is the most common cause of cancer death, approximately 85% of which are non-small cell lung cancer (NSCLC). Here we found that artemether (ART), a natural derivative of artemisinin, significantly inhibits the proliferation of NSCLC cells in a dose- and time-dependent manner. We also demonstrated that high concentration of ART induces apoptosis in NSCLC cells through down-regulating the level of anti-apoptotic protein B-cell lymphoma-2 (Bcl-2), cellular inhibitor of apoptosis protein 1 (cIAP1) and cellular inhibitor of apoptosis protein 2 (cIAP2). While low concentration of ART inhibits the mRNA level of cell cycle related genes including cyclin-dependent kinase 1 (CDK1), cyclin-dependent kinase 2 (CDK2), cyclin-dependent kinase 6 (CDK6), cyclin A2, cyclin B1 and cyclin D1, leading to cell cycle arrest in NSCLC cells. Moreover, we confirmed that low concentration of ART induces DNA double-stranded breaks (DSBs), as well as promoting cellular senescence in NSCLC cells by up-regulating the mRNA and protein level of p16. Taken together, ART represents a promising new anti-NSCLC drug candidate that could attenuate progression of NSCLC cells in a p53-independent manner through inducing apoptosis, cell cycle arrest and promoting cellular senescence.

KEYWORDS

apoptosis; artemether; cell cycle arrest; cellular senescence; non-small cell lung cancer

Title

Artemether Attenuates the Progression of Non-small Cell Lung Cancer by Inducing Apoptosis, Cell Cycle Arrest and Promoting Cellular Senescence.

Author

Chen J1,2,3, Huang X4, Tao C1,2,3,5, Xiao T6, Li X3, Zeng Q1,2,3, Ma M7,8, Wu Z1,2,3,9.

Publish date

2019 Oct 1

PMID

31210357

Abstract

BACKGROUND:
In 2011 the World Health Organization (WHO) recommended parenteral artesunate in preference to quinine as first-line treatment for people with severe malaria. Prior to this recommendation many countries, particularly in Africa, had begun to use artemether, an alternative artemisinin derivative. This Cochrane Review evaluates intramuscular artemether compared with both quinine and artesunate.

OBJECTIVES:
To assess the efficacy and safety of intramuscular artemether versus any other parenteral medication in the treatment of severe malaria in adults and children.

SEARCH METHODS:
We searched the Cochrane Infectious Diseases Group Specialized Register, CENTRAL (the Cochrane Library), MEDLINE, Embase, and LILACS, ISI Web of Science, conference proceedings, and reference lists of articles. We also searched the WHO International Clinical Trial Registry Platform, ClinicalTrials.gov, and the metaRegister of Controlled Trials (mRCT) for ongoing trials up to 7 September 2018. We checked the reference lists of all studies identified by the search. We examined references listed in review articles and previously compiled bibliographies to look for eligible studies.

SELECTION CRITERIA:
Randomized controlled trials (RCTs) comparing intramuscular artemether with intravenous/intramuscular quinine or artesunate for treating severe malaria.

DATA COLLECTION AND ANALYSIS:
The primary outcome was all-cause death. Two review authors independently screened each article by title and abstract, and examined potentially relevant studies for inclusion using an eligibility form. Two review authors independently extracted data and assessed risk of bias of included studies. We summarized dichotomous outcomes using risk ratios (RRs) and continuous outcomes using mean differences (MDs), and have presented both measures with 95% confidence intervals (CIs). Where appropriate, we combined data in meta-analyses and used the GRADE approach to summarize the certainty of the evidence.

MAIN RESULTS:
We included 19 RCTs, enrolling 2874 adults and children with severe malaria, carried out in Africa (12 trials) and in Asia (7 trials).Artemether versus quinineFor children, there is probably little or no difference in the risk of death between intramuscular artemether and quinine (RR 0.97, 95% CI 0.77 to 1.21; 13 trials, 1659 participants, moderate-certainty evidence). Coma resolution time may be about five hours shorter with artemether (MD -5.45, 95% CI -7.90 to -3.00; six trials, 358 participants, low-certainty evidence). Artemether may make little difference to neurological sequelae (RR 0.84, 95% CI 0.66 to 1.07; seven trials, 968 participants, low-certainty evidence). Compared to quinine, artemether probably shortens the parasite clearance time by about nine hours (MD -9.03, 95% CI -11.43 to -6.63; seven trials, 420 participants, moderate-certainty evidence), and may shorten the fever clearance time by about three hours (MD -3.73, 95% CI -6.55 to -0.92; eight trials, 457 participants, low-certainty evidence).For adults, treatment with intramuscular artemether probably results in fewer deaths than treatment with quinine (RR 0.59, 95% CI 0.42 to 0.83; four trials, 716 participants, moderate-certainty evidence).Artemether versus artesunateArtemether and artesunate have not been directly compared in randomized trials in children.For adults, mortality is probably higher with intramuscular artemether (RR 1.80, 95% CI 1.09 to 2.97; two trials, 494 participants, moderate-certainty evidence).

AUTHORS’ CONCLUSIONS:
Artemether appears to be more effective than quinine in children and adults. Artemether compared to artesunate has not been extensively studied, but in adults it appears inferior. These findings are consistent with the WHO recommendations that artesunate is the drug of choice, but artemether is acceptable when artesunate is not available.

Title

Artemether for severe malaria.

Author

Esu EB1, Effa EE, Opie ON, Meremikwu MM.

Publish date

2019 Jun 18