A group of SESQUITERPENES and their analogs that contain a peroxide group (PEROXIDES) within an oxepin ring (OXEPINS).
Agents used in the treatment of malaria. They are usually classified on the basis of their action against plasmodia at different stages in their life cycle in the human. (From AMA, Drug Evaluations Annual, 1992, p1585)
Tests that demonstrate the relative effectiveness of chemotherapeutic agents against specific parasites.
Diminished or failed response of an organism, disease or tissue to the intended effectiveness of a chemical or drug. It should be differentiated from DRUG TOLERANCE which is the progressive diminution of the susceptibility of a human or animal to the effects of a drug, as a result of continued administration.
A species of protozoa that is the causal agent of falciparum malaria (MALARIA, FALCIPARUM). It is most prevalent in the tropics and subtropics.
Malaria caused by PLASMODIUM FALCIPARUM. This is the severest form of malaria and is associated with the highest levels of parasites in the blood. This disease is characterized by irregularly recurring febrile paroxysms that in extreme cases occur with acute cerebral, renal, or gastrointestinal manifestations.
A protozoan disease caused in humans by four species of the PLASMODIUM genus: PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PLASMODIUM OVALE; and PLASMODIUM MALARIAE; and transmitted by the bite of an infected female mosquito of the genus ANOPHELES. Malaria is endemic in parts of Asia, Africa, Central and South America, Oceania, and certain Caribbean islands. It is characterized by extreme exhaustion associated with paroxysms of high FEVER; SWEATING; shaking CHILLS; and ANEMIA. Malaria in ANIMALS is caused by other species of plasmodia.
The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.
The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.
Therapy with two or more separate preparations given for a combined effect.
A plant species of the genus ARTEMISIA, family ASTERACEAE. It is the source of the antimalarial artemisinin (ANTIMALARIALS).
A plant genus of the family ASTERACEAE with strong-smelling foliage. It is a source of SANTONIN and other cytotoxic TERPENES.
A plant species of the genus ARTEMISIA, family ASTERACEAE that has been used in ABSINTHE. The oil contains neurotoxic 1-thujone and d-isothujone.
Infection with flukes (trematodes) of the genus SCHISTOSOMA. Three species produce the most frequent clinical diseases: SCHISTOSOMA HAEMATOBIUM (endemic in Africa and the Middle East), SCHISTOSOMA MANSONI (in Egypt, northern and southern Africa, some West Indies islands, northern 2/3 of South America), and SCHISTOSOMA JAPONICUM (in Japan, China, the Philippines, Celebes, Thailand, Laos). S. mansoni is often seen in Puerto Ricans living in the United States.
Invertebrate organisms that live on or in another organism (the host), and benefit at the expense of the other. Traditionally excluded from definition of parasites are pathogenic BACTERIA; FUNGI; VIRUSES; and PLANTS; though they may live parasitically.
Disciplines concerned with the interrelationships of individuals in a social environment including social organizations and institutions. Includes Sociology and Anthropology.
Diseases that are underfunded and have low name recognition but are major burdens in less developed countries. The World Health Organization has designated six tropical infectious diseases as being neglected in industrialized countries that are endemic in many developing countries (HELMINTHIASIS; LEPROSY; LYMPHATIC FILARIASIS; ONCHOCERCIASIS; SCHISTOSOMIASIS; and TRACHOMA).
The branch of medicine concerned with diseases, mainly of parasitic origin, common in tropical and subtropical regions.
A loose confederation of computer communication networks around the world. The networks that make up the Internet are connected through several backbone networks. The Internet grew out of the US Government ARPAnet project and was designed to facilitate information exchange.
A species of the genus SACCHAROMYCES, family Saccharomycetaceae, order Saccharomycetales, known as "baker's" or "brewer's" yeast. The dried form is used as a dietary supplement.
Unanticipated information discovered in the course of testing or medical care. Used in discussions of information that may have social or psychological consequences, such as when it is learned that a child's biological father is someone other than the putative father, or that a person tested for one disease or disorder has, or is at risk for, something else.
Proteins obtained from the species SACCHAROMYCES CEREVISIAE. The function of specific proteins from this organism are the subject of intense scientific interest and have been used to derive basic understanding of the functioning similar proteins in higher eukaryotes.
A general term for single-celled rounded fungi that reproduce by budding. Brewers' and bakers' yeasts are SACCHAROMYCES CEREVISIAE; therapeutic dried yeast is YEAST, DRIED.
Experiments designed to determine the potential toxic effects of a long-term exposure to a chemical or chemicals.
An array of tests used to determine the toxicity of a substance to living systems. These include tests on clinical drugs, foods, and environmental pollutants.
A family of diphenylenemethane derivatives.
A republic in central Africa lying east of CHAD and the CENTRAL AFRICAN REPUBLIC and west of NIGERIA. The capital is Yaounde.
Single preparations containing two or more active agents, for the purpose of their concurrent administration as a fixed dose mixture.
A 4-aminoquinoline compound with anti-inflammatory properties.
AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.
Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS.
Drug regimens, for patients with HIV INFECTIONS, that aggressively suppress HIV replication. The regimens usually involve administration of three or more different drugs including a protease inhibitor.
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).

Declining concentrations of dihydroartemisinin in plasma during 5-day oral treatment with artesunate for Falciparum malaria. (1/1442)

Six patients with uncomplicated falciparum malaria received artesunate for 5 days. Plasma concentrations of artesunate and dihydroartemisinin were determined by high-performance liquid chromatography with electrochemical detection. The concentrations of dihydroartemisinin in plasma 2 h after a dose showed a time-dependent decline. Concentrations of artesunate in plasma especially after the last dose, were very low. Despite this, all patients responded with a fast recovery.  (+info)

A randomized, double-blind, comparative trial of a new oral combination of artemether and benflumetol (CGP 56697) with mefloquine in the treatment of acute Plasmodium falciparum malaria in Thailand. (2/1442)

CGP 56697, a new oral fixed combination of artemether and benflumetol, was tested in a double-blinded, randomized trial in 252 adult patients treated either with CGP 56697 (4 x 4 tablets each containing 20 mg of artemether and 120 mg of benflumetol, given at 0, 8, 24, and 48 hr), or with mefloquine (three tablets of 250 mg at initial diagnosis, followed by two tablets of 250 mg at 8 hr). Baseline data of the two groups were comparable. The 28-day cure rate with CGP 56697 was lower than with mefloquine (69.3% versus 82.4%; P = 0.002). However, CGP 56697 was more effective than mefloquine in parasite clearance time (43 hr versus 66 hr; P < 0.001) fever clearance time (32 hr versus 54 hr; P < 0.005), and gametocyte clearance time (152 hr versus 331 hr; P < 0.001). This study revealed that CGP 56697 is effective against multidrug-resistant Plasmodium falciparum malaria in Thailand, but higher doses will probably be needed to improve the cure rate.  (+info)

The pharmacokinetics of artemisinin after administration of two different suppositories to healthy Vietnamese subjects. (3/1442)

Eight healthy Vietnamese male subjects received 400 mg artemisinin formulated into fatty suppositories (FS), and six different subjects received 500 mg of artemisinin formulated in polyethylene glycol suppositories (PEGS). Plasma concentrations were measured by high-performance liquid chromatography with electrochemical detection; concentration versus time curves were analyzed with nonparametric methods. No statistically significant differences were found between the two formulations. The maximum concentration (Cmax) was 100 +/- 102 microg/L (mean +/- SD, range = 24-330) microg/L (FS), the pharmacokinetic lag time (Tlag) was 1.3 +/- 1.0 hr (range = 0-3) (FS), and the time of the maximum concentration (Tmax) was 7.1 +/- 2.1 hr (range = 3-10) hr (FS). Because artemisinin is not available for intravenous dosage, absolute bioavailability cannot be assessed. However, compared with a previous study on oral artemisinin in healthy Vietnamese subjects, bioavailability relative to oral administration was estimated to be approximately 30%. We conclude that therapeutic blood concentrations of artemisinin can be reached after rectal dosage. The dose after rectal administration should probably be higher than after oral administration; doubling or tripling the oral dose might be necessary, which would imply a rectal dose of at least 20 mg/kg of body weight given twice a day.  (+info)

Effect of artemether on glucose uptake and glycogen content in Schistosoma japonicum. (4/1442)

AIM: To study the effect of artemether (Art) on glucose uptake and glycogen content in schistosomes. METHODS: Schistosomes recovered from mice treated intragastrically with Art 300 mg.kg-1 for 24-48 h, were incubated in the drug-free medium containing [U-14C]glucose 11.1 MBq.L-1. The glycogen content, [U-14C]glucose uptake, and incorporation of [U-14C]glucose into worm glycogen in both male and female worms were determined. RESULTS: When above-mentioned schistosomes were exposed to drug-free medium containing [U-14C]glucose for 1-24 h, the glycogen contents of male and female worms decreased 27%-61% and 39%-78%, respectively. Only 3 out of 6 male worm groups showed 23%-35% decrease in glucose uptake, while much less glucose uptake was found in female worms in all groups with reduction rates of 18%-38%. Apart from 2 male groups no apparent change in the incorporation of [U-14C]glucose into the worm glycogen was seen. CONCLUSIONS: Art-induced glycogen reduction in schistosomes was related to an inhibition of glycolysis rather than an interference with glucose uptake.  (+info)

Inhibitory effect of artemether on proteinase of Schistosoma japonicum. (5/1442)

AIM: To study the effect of artemether (Art) on the thio proteinase ("hemoglobinase", Hem) of Schistosoma japonicum. METHODS: Hem was extracted from S japonicum adults. The inhibitory effect of Art on the activity of Hem to degrade human hemoglobin (Hgb) was examined with UV-photometer at 280 nm, SDS-PAGE and scanning at 600 nm on a chromoscanner. RESULTS: Human Hgb was degraded at pH 4.0 by the Hem. The activities of Hem preincubated at 37 degrees C with Art 0.14, 1.4, and 14 mmol.L-1, were inhibited by 30.2%, 39.8%, and 45.0%, respectively. CONCLUSION: Art possesses an inhibitory effect to Hem of S japonicum.  (+info)

Metabolism of the antimalarial endoperoxide Ro 42-1611 (arteflene) in the rat: evidence for endoperoxide bioactivation. (6/1442)

Ro 42-1611 (arteflene) is a synthetic endoperoxide antimalarial. The antimalarial activity of endoperoxides is attributed to iron(II)-mediated generation of carbon-centered radicals. An alpha, beta-unsaturated ketone (enone; 4-[2',4' bis(trifluoromethyl)phenyl]-3-buten-2-one), obtained from arteflene by reaction with iron(II), was identified previously as the stable product of a reaction that, by inference, also yields a cyclohexyl radical. The activation of arteflene in vivo has been characterized with particular reference to enone formation. [14C]Arteflene (35 micromol/kg) was given i.v. to anesthetized and cannulated male rats: 42.2 +/- 7.0% (mean +/- S.D., n = 7) of the radiolabel was recovered in bile over 5 h. In the majority of rats, the principal biliary metabolites were 8-hydroxyarteflene glucuronide (14.2 +/- 3. 9% dose, 0-3 h) and the cis and trans isomers of the enone (13.5 +/- 4.6% dose, 0-3 h). In conscious rats, 15.3 +/- 1.6% (mean +/- S.D., n = 8) of the radiolabel was recovered in urine over 24 h. The principal urinary metabolite appeared to be a glycine conjugate of a derivative of the enone. Biliary excretion of the glucuronide, but not of the enones, was inhibited by ketoconazole. 8-Hydroxyarteflene was formed extensively by rat and human liver microsomes but no enone was found. Bioactivation is a major pathway of arteflene's metabolism in the rat. Although the mechanism of in vivo bioactivation is unclear, the reaction is not catalyzed by microsomal cytochrome P-450 enzymes.  (+info)

Artemether for severe malaria: a meta-analysis of randomized clinical trials. (7/1442)

The treatment of choice for severe malaria is quinine. However, a gradual progression of resistance to quinine has become a concern in parts of the world. Artemisinin-related compounds are a relatively new class of drugs. This meta-analysis assesses the evidence regarding the clinical effectiveness of artemether for severe malaria. Computerized literature searches identified all randomized clinical trials of artemether in comparison with quinine. Standardized data extraction was independently performed by both authors. Results of nine trials, entered in the meta-analysis, demonstrate the absence of a significant difference between artemether and quinine in terms of mortality rate (odds ratio [OR], 0.76; 95% confidence interval [CI], 0.50-1.14). Statistical pooling of data from trials in Southeast Asia showed a trend toward enhanced reduction of mortality (OR, 0.38; 95% CI, 0.14-1.02). These data demonstrate the equality of artemether and quinine for severe malaria and indicate a trend toward greater effectiveness of artemether in regions where there is recognized quinine resistance.  (+info)

Cost-effectiveness analysis of artesunate and quinine + tetracycline for the treatment of uncomplicated falciparum malaria in Chanthaburi, Thailand. (8/1442)

A randomized, controlled, malaria-clinic-based field trial was carried out to compare the cost-effectiveness of a 5-day 700-mg oral artesunate and a 7-day quinine + tetracycline regimen for the treatment of uncomplicated falciparum malaria in Thailand. Cost-effectiveness was determined from the providers' perspective and based on curative effectiveness. A total of 137 patients, aged 15-60 years, attending a malaria clinic were followed for 28 days, 60 of them received quinine + tetracycline and 77 received artesunate. Cure rates were assessed on day 5 (artesunate) and day 7 (quinine + tetracycline), using the intention-to-treat approach. Cost-effectiveness and sensitivity analyses were performed by varying the day 5/day 7 curative effectiveness and cost of artesunate. The cure rate with artesunate (100%) was significantly higher than with quinine + tetracycline (77.4%) (relative risk adjusted for sex (aRR) = 1.32, 95% confidence interval (CI) = 1.12-1.55; referent quinine + tetracycline). Artesunate was more cost-effective than quinine + tetracycline at the following costs: artesunate, < or = US$0.36 per 50-mg tablet; quinine, US$0.06 per 300-mg tablet; tetracycline, US$0.02 per 250-mg capsule; and services per case found, < or = US$11.49. Because of the higher cure rate and higher cost-effectiveness of the artesunate regimen compared with quinine + tetracycline, we recommend its use for the treatment of uncomplicated falciparum malaria in malaria clinics in Thailand.  (+info)

BACKGROUND: Gametocytes are responsible for transmission of malaria from human to mosquito. Artemisinin combination therapy (ACT) reduces post-treatment gametocyte carriage, dependent upon host, parasite and pharmacodynamic factors. The gametocytocidal properties of antimalarial drugs are important for malaria elimination efforts. An individual patient clinical data meta-analysis was undertaken to identify the determinants of gametocyte carriage and the comparative effects of four ACTs: artemether-lumefantrine (AL), artesunate/amodiaquine (AS-AQ), artesunate/mefloquine (AS-MQ), and dihydroartemisinin-piperaquine (DP). METHODS: Factors associated with gametocytaemia prior to, and following, ACT treatment were identified in multivariable logistic or Cox regression analysis with random effects. All relevant studies were identified through a systematic review of PubMed. Risk of bias was evaluated based on study design, methodology, and missing data. RESULTS: The systematic review identified 169 published
The World Health Organization recommends the use of artemisinin-based combination therapy (ACT) to treat uncomplicated malaria for the control of malaria across the world. There are several types of ACT used across malaria-endemic countries, yet there is little information about preferences and adherence practices regarding different types of ACT. The objective of this study was to evaluate levels of adherence to two types of ACT, artemether-lumefantrine (AL) and artesunate + amodiaquine (ASAQ), for the treatment of uncomplicated malaria among prescribers and patients in Guinea in 2016. The study included a review of records of malaria patients and three health-facility, cross-sectional surveys. Patients diagnosed with uncomplicated malaria and prescribed ACT (n = 1830) were recruited and visited in their home after receiving the medication and administered a questionnaire regarding ACT adherence. Prescribers (n = 115) and drug dispensers (n = 43) were recruited at the same public health facilities and
TY - JOUR. T1 - Imported malaria and artemisinin-based combination therapy failure in travellers returning to Belgium: a retrospective study. AU - Rovira-Vallbona, Eduard. AU - Bottieau, Emmanuel. AU - Guetens, Pieter. AU - Verschueren, Jacob. AU - Rebolledo, Javiera. AU - Nulens, Eric. AU - Van der Hilst, Jeroen. AU - Clerinx, Jan. AU - Van Esbroeck, Marjan. AU - Rosanas-Urgell, Anna. N1 - CPDF. PY - 2019. Y1 - 2019. N2 - BACKGROUND: Malaria (Plasmodium spp) remains a top cause of travel-associated morbidity among European residents. Here, we describe recent trends of imported malaria to Belgium and characterize the first cases of P.falciparum failure to artemisinin-based combination therapy (ACT).METHODS: National surveillance data and registers from national reference laboratory were used to investigate malaria cases and ACT failures in the past 20 years. Recurrent infections were confirmed by pfmsp genotyping and polymorphisms in drug resistance-associated genes pfk13, pfcrt, pfmdr1, pfpm2, ...
Hemolytic anemia after treatment of severe malaria with intravenous artesunate has been described in malaria-endemic and non-malaria-endemic countries. However, evidence of hemolytic anemia after treatment of malaria with oral ACTs is limited to 2 case reports. Data from the current prospective study confirm our hypothesis that delayed posttreatment hemolysis also occurs after oral artemisinin treatment and provide insight into its frequency and clinical course. In 40% of the patients in our study with uncomplicated malaria and oral ACT treatment, laboratory signs of hemolysis were detected 2 weeks after therapy. In 5 patients, hemolysis persisted 1 month after treatment. Patients with posttreatment hemolysis showed a larger decrease in Hb levels after treatment than did patients without hemolysis. The intensity of hemolysis was mild compared with that after intravenous artesunate. In many reported cases of PADH after intravenous artesunate, patients received blood transfusions (2,9). In other ...
Artemisinin-based combination therapies (ACTs) are the treatment of choice for uncomplicated Plasmodium falciparum malaria in malaria endemic countries. ACT resistance has already been documented in the main, but not solely in Asia,1 therefore therapeutic alternatives should be investigated. As there are no new drugs at advance stages in the pipeline, current focus should be on novel combinations of existing drugs. This prospective randomised study compares the effectiveness of three antimalaria combination drugs-two well-established combination drugs (artesunate-amodiaquine (AA) and atovaquone-proguanil (AP)) and one … ...
The World Health Organization (WHO) recommends combinations of an artemisinin derivative plus an anti-malarial drug of longer half-life as treatment options for uncomplicated Plasmodium falciparum infections. In Africa, artesunate-mefloquine (ASMQ) is an infrequently used artemisinin-based combination therapy (ACT) because of perceived poor tolerance to mefloquine. However, the WHO has recommended reconsideration of the use of ASMQ in Africa. In this large clinical study, the pharmacokinetics (PK) of a fixed dose combination of ASMQ was investigated in an African paediatric population to support dosing recommendations used in Southeast Asia and South America. Among the 472 paediatric patients aged 6-59 months from six African centres included in the large clinical trial, a subset of 50 Kenyan children underwent intensive sampling to develop AS, its metabolite dihydroartemisinin (DHA) and MQ PK models. The final MQ PK model was validated using sparse data collected in the remaining participants (NONMEM®
Artesunate-amodiaquine (AS-AQ) is one of the most widely used artemisinin-based combination therapies (ACTs) to treat uncomplicated Plasmodium falciparum malaria in Africa. We investigated the impact of different dosing strategies on the efficacy of this combination for the treatment of falciparum malaria. Individual patient data from AS-AQ clinical trials were pooled using the WorldWide Antimalarial Resistance Network (WWARN) standardised methodology. Risk factors for treatment failure were identified using a Cox regression model with shared frailty across study sites. Forty-three studies representing 9,106 treatments from 1999-2012 were included in the analysis; 4,138 (45.4%) treatments were with a fixed dose combination with an AQ target dose of 30 mg/kg (FDC), 1,293 (14.2%) with a non-fixed dose combination with an AQ target dose of 25 mg/kg (loose NFDC-25), 2,418 (26.6%) with a non-fixed dose combination with an AQ target dose of 30 mg/kg (loose NFDC-30), and the remaining 1,257 (13.8%) with a co
Background: In Tanzania, many people seek malaria treatment from retail drug sellers. The National Malaria Control Program identified the accredited drug dispensing outlet (ADDO) program as a private sector mechanism to supplement the distribution of subsidized artemisinin-based combination therapies (ACTs) from public facilities and increase access to the first-line antimalarial in rural and underserved areas. The ADDO program strengthens private sector pharmaceutical services by improving regulatory and supervisory support, dispenser training, and record keeping practices.. Methods: The governments pilot program made subsidized ACTs available through ADDOs in 10 districts in the Morogoro and Ruvuma regions, covering about 2.9 million people. The program established a supply of subsidized ACTs, created a price system with a cost recovery plan, developed a plan to distribute the subsidized products to the ADDOs, trained dispensers, and strengthened the adverse drug reactions reporting system. ...
This multi-agency report, led by MSH, with input from CHAI, FIND, MMV, JSI/Deliver, PMI, RBM, WDI and WHO provides guidance for the specific interaction between artemisinin-based combination therapies (ACTs) and rapid diagnostic tests (RDTs). It shows users how to develop a stepwise approach to quantifying ACT and RDT demand at the program level and to understand the data and the assumptions that are needed for quantification, especially when the data are imperfect.. Specifically, the manual illustrates how to plan, forecast, and ensure supplies of ACTs and RDTs through the following steps: ...
THE KELCH PROPELLER HYPOTHESIS. Over the last century all monotherapies (quinine, chloroquine, mefloquine, pyrimethamine, halofantrine,methylene blue, lumefantrine) have lead to rapid resistances of Plasmodium falciparum. Combination therapy betweeen artemisinin and molecules with long lasting action had raised optimism. But already in 2003 first signs of resistance developed in South-East Asia. It has been established meanwhile that they were mostly related to mutations in the kelch13 propeller region of the parasite. Mutations have meanwhile raised to 90%. (Timothy J.C. Anderson, Shalini Nair, Marina McDew-White, Ian H. Cheeseman, Standwell Nkhoma, Fatma Bilgic, Rose McGready, Elizabeth Ashley, Aung Pyae Phyo, Nicholas J. White, François Nosten. Why are there so many independent origins of artemisinin resistance in malaria parasites? bioRxiv preprint first posted online May. 31, 2016; doi: http://dx.doi.org/10.1101/056291).. Artemisinin resistance in Plasmodium falciparum has emerged in ...
It is generally agreed that artemisinin-based combination therapy (ACT) is the malaria therapy of choice but there is much less agreement about the best ACT-deployment strategies. Countries are now beginning to adopt policies to enhance ACT deployment that aim to address 2 key goals: (i) making ACTs more readily and speedily accessible to patients: or (ii) targeting ACTs to patients shown to have malaria parasitaemia.. The Tanzanian Government has secured funding to address both ACT access and targeting on a national scale. Access is to be improved through the distribution of subsidised ACTs through private facilities and retail drug shops under the Affordable Medicines Facility-malaria (AMFm). Targeting is to be addressed through enhancing microscopy and introducing rapid diagnostic tests (RDTs) in health facilities at every level of the system.. This study will evaluate these two interventions in 3 rural regions of Tanzania which are all expected to receive both interventions during the study ...
Over the years, reports implicate improper anti-malarial use as a major contributor of morbidity and mortality amongst millions of residents in malaria endemic areas, Kenya included. However, there are limited reports on improper use of Artemisinin-based Combination Therapy (ACT) which is a first-line drug in the treatment of malaria in Kenya. Knowing this is important for ensured sustainable cure rates and also protection against the emergence of resistant malarial parasites. We therefore investigated ACT adherence level, factors associated with non-adherence and accessibility in households (n = 297) in rural location of Southeast Alego location in Siaya County in western Kenya. ACT Adherence level was assessed with reference to the duration of treatment and number of tablets taken. Using systematic random sampling technique, a questionnaire was administered to a particular household member who had the most recent malaria episode (|2 weeks) and used ACT for cure. Parents/caretakers provided information
The costs of delivering specific products are poorly understood and ballpark estimates are often used to inadequately plan for the budgetary implications of supply chain expenses. The purpose of this research was to estimate the country level costs of the public sector supply chain for artemisinin-based combination therapy (ACT) and rapid diagnostic tests (RDTs) from the central to the peripheral levels in Benin and Kenya. A micro-costing approach was used and primary data on the various cost components of the supply chain was collected at the central, intermediate, and facility levels between September and November 2013. Information sources included central warehouse databases, health facility records, transport schedules, and expenditure reports. In Benin, supply chain costs added US$0.20 to the initial acquisition cost of ACT and US$0.34 to RDTs; in Kenya, they added US$0.24 to the acquisition cost of ACT and US$0.19 to RDTs (normalized to US$1). Total supply chain costs accounted for more ...
From chloroquine to artemisinin-based combination therapy: the Sudanese experience. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
Artemisinin-based combination therapy (ACT) is used extensively as first-line treatment for uncomplicated falciparum malaria. There has been no rigorous assessment of the potential for racial/ethnic differences in the pharmacokinetic properties of ACTs that might influence their efficacy. Areas covered: A comprehensive literature search was performed that identified 72 publications in which the geographical origin of the patients could be ascertained and the key pharmacokinetic parameters maximum drug concentration (Cmax), area under the plasma concentration-time curve (AUC) and elimination half-life (t½β) were available for one or more of the five WHO-recommended ACTs (artemether-lumefantrine, artesunate-amodiaquine, artesunate-mefloquine, dihydroartemisinin-piperaquine and artesunate-sulfadoxine-pyrimethamine ...
Artemisinin-based combination therapies (ACTs) are now the treatment of choice for malaria in non-pregnant individuals living in areas with established chloroquine resistance; they have been shown to be both safe and highly efficacious. There is rapidly increasing experience with artemisinin derivatives in the 2nd and 3rd trimesters of pregnancy, with over 1,000 well documented cases with no reported serious adverse effects to mother or fetus (WHO Malaria Treatment Guidelines, 2006). Many countries in Latin America have abandoned the previous 1st line regimen of Quinine-Clindamycin for treatment of malaria in pregnancy, a complex and poorly tolerated regimen with low adherence, in favor of ACTs, despite limited safety and pharmacokinetic data on the use of these compounds in pregnant women. Lack of pharmacokinetic data may lead to underdosing of pregnant women, with subsequent reduced efficacy and increased potential for development of resistance.. One ACT regimen, Artesunate-Mefloquine, has ...
The molecular and cellular action properties of artemisinins: what has yeast told us? - Artemisinin (ART) or Qinghaosu is a natural compound possessing superior anti-malarial activity. Although intensive studies have been done in the medicinal chemistry field to understand the structure-effect relationship, the biological actions of artemisinin are poorly understood and controversial. Due to the current lack of a genetic amiable model to address this question, and an accidental finding made more than a decade ago during our initial exploratory efforts that yeast Saccharomyces cerevisiae can be inhibited by artemisinin, we have since been using the bakers yeast as a model to probe the molecular and cellular properties of artemisinin and its derivatives (ARTs) in living cells. ARTs were found to possess potent and specific anti-mitochondrial properties and, to a lesser extent, the ability to generate a relatively general oxidative damage...
Artesunate is an anti-malarial drug with promising anti-inflammatory effects in allergic asthma. We investigated the protective effects of artesunate in experimental allergic asthma, in comparison to corticosteroids, dexamethasone. We demonstrate that artesunate possess favourable pharmacological effects against oxidative lung damage markers, 8-isoprostane, 3-nitrotyrosine and 8-hydroxy-2-deoxyguanosine. These effects include modulation of pulmonary antioxidants (catalase and SOD) and broad suppression of pulmonary pro-oxidants (NADPH oxidases and iNOS), via promotion of nuclear Nrf2 levels. Correspondingly, metabolomics was employed understand altered pulmonary metabolism and the protective effects of artesunate in allergic asthma. Liquid and gas chromatography mass spectrometry (LC/MS & GC/MS) were employed to investigate bronchoalveolar lavage fluid and serum of experimental allergic asthma with artesunate treatment. Our results reveal that artesunate can reverse disease-associated metabolite ...
Without an effective vaccine for the prevention of malaria, a fundamental component of the strategy for the control of this disease is based on prompt and effective treatment. Due to the high resistance level of Plasmodium falciparum to the most affordable drugs such as chloroquine and sulfadoxine-pyrimethamine, artemisinin-based combination therapies are presently used in many countries or are being developed for registration. One artemisinin combination therapy that is drawing a certain degree of interest is the combination of artesunate (a short half-life drug) plus amodiaquine (a long half-life drug that is presently used in loose combination in many countries). The short half-life drug achieves substantial and rapid parasite killing, while a high concentration of the long half-life drug kills off the remaining malaria parasites. In addition to the effectiveness of 3 days of treatment (rapid clearance of fever and malaria parasites) in western and central Africa, where resistance to ...
The National Institute of Malariology, Parasitology, and Entomology conducted this study as part of routine surveillance on drug efficacy following the 2009 World Health Organization protocol (2). After obtaining written consent, patients (age of inclusion, 2-60 years) were enrolled and given dihydroartemisinin/piperaquine (Pharbaco, Hanoi, Vietnam) at a target dosage of 2.4 mg/kg for dihydroartemisinin and 18 mg/kg for piperaquine once a day for 3 days. Patients with treatment failures were subsequently given quinine hydrochlorate (30 mg/kg/d) and doxycycline (3 mg/kg/d) for 7 days. Primary endpoint was adequate clinical and parasitologic response (ACPR) on day 42; PCR genotyping, comparing day 0 and day of failure samples, was used to distinguish recrudescence from reinfection with another strain (2). Dried blood spots were collected on day 0 and analyzed for mutations in the K13 propeller domain (3), Pfmdr1 copy number (4), and Pfplasmepsin2 (PfPM2) copy number (5), which are markers ...
Significant interest has been placed on the utility of PK parameters in predicting the treatment response. Most attention has been placed on the correlates of the AUC, as AUC represents both the duration and the degree of exposure. The accurate measurement of AUC in field studies is difficult, so recent efforts for studying the PKs of artemisinin partner drugs have focused on single day 7 drug levels (34). The rationale for this approach is that by day 7 the remaining parasites will be exposed only to the partner drug, as the rapidly eliminated artemisinin derivatives are no longer present. The level of partner drug in the days following dosing may be critical for determining both the clearance of the infection and the potential selection of drug-resistant parasites. Importantly, for the longer-acting partner drugs, the day 7 levels appear to correlate with the AUC (5), as seen for both DEAQ and LR in our study. Several studies from Thailand have examined the relationship between the day 7 ...
A constant struggle between the search for new drug formulations and evolving drug-resistant parasites has marked the history of antimalarial medicine. Resistance to chloroquine has rendered the drug ineffective for instance in many parts of the world. Therapies that combine artemisinin derivatives with other companion drugs are currently being focused on by anti-malaria experts. Artemisinin-based combination therapy (ACT) is what these combinations are called. Acting quickly in the bloodstream, artemisinins help the patient feel better faster and clear away the parasites rapidly. By reducing the number of gametocytes - the infective version of the parasite - in the bloodstream, they may also help reduce transmission of the disease. ACT has few known side effects. Theres little documented resistance to artemisinins, and their combination with other drugs may slow resistance to these companion drugs as well. The bad thing about these combination drugs is that they are more expensive than the ...
ABSTRACT: BACKGROUND: Artemisinin-based combination therapies (ACT) are widely used in African countries, including Cameroon. Between 2005 and 2007, five randomized studies comparing different treatment arms among artesunate-amodiaquine and other ACT were conducted in Cameroonian children aged two to 60 months who had uncomplicated Plasmodium falciparum malaria. In these studies, the categorical criterion proposed by the World Health Organization (WHO) to assess the relative effectiveness of anti- malarial drugs, was repeatedly evaluated on Days 14, 21 and 28 after treatment initiation. The aim of the present study was to compare the effects of different treatments on this repeated ordinal outcome, hence using the fully available information. METHODS: The quantitative synthesis was based on individual patient data. Due to the incomplete block design concerning treatment arms between different trials, a mixed treatment comparison (MTC) meta-analysis approach was adopted. The repeated ordinal outcome was
The purpose of this thesis is to investigate the therapeutic potential of artesunate, an anti-malaria drug, on allergy and allergic asthma. Firstly, we studied the anti-inflammatory effects of artesunate on allergic asthma by employing a murine asthma model. In this study, female Balb/c mice were actively sensitized and challenged by ovalbumin to induce airway inflammation, mucus hypersecretion and airway hyperresponsiveness. Artesunate (3, 10, 30 mg/kg, given intraperitoneally) markly inhibited OVA-induced increases in total cell counts and eosinophil counts and IL-4, IL-5, IL-13 and eotaxin levels in bronchoalveolar lavage fluid in a dose dependent manner. Artesunate also substantially (P,0.05) reduced serum levels of OVA-IgE and IgG1; whereas the levels of OVA-specific IgG2a were not significantly affected. In addition, artesunate was shown to restore the levels of Th1 related cytokines such as IFN-gamma and IL-12 back to basal level in a dose dependent manner. Histological analysis further ...
Background: Malaria is a mosquito-borne infectious disease, with the most severe form caused by the parasite Plasmodium falciparum. The first-line defence against uncomplicated falciparum malaria is artemisinin-based combination therapy (ACT), involving multiple administrations of two or more antimalarial drugs. ACTs are highly effective worldwide, however, recently decreased efficacy of the ACT artesunate-mefloquine has been reported […]. ...
|jats:sec||jats:title|Summary|/jats:title||jats:p|Multiple alleles at the |jats:italic|kelch13|/jats:italic| locus conferring artemisinin resistance (ART-R) are currently spreading through malaria parasite populations in Southeast Asia, providing a unique opportunity to directly observe an ongoing soft selective sweep, to investigate why resistance alleles have evolved multiple times and to determine fundamental population genetic parameters for Plasmodium. We sequenced the |jats:italic|kelch13|/jats:italic| gene (n=1,876), genotyped 75 flanking SNPs, and measured clearance rate (n=3,552) in parasite infections from Western Thailand (2001-2014). We describe 32 independent coding mutations: these included common mutations outside the |jats:italic|kelch13|/jats:italic| propeller region associated with significant reductions in clearance rate. Mutations were first observed in 2003 and rose to 90% by 2014, consistent with a selection coefficient of ~0.079. There was no change in diversity in flanking
<p>An outline of the opportunities and challenges in large-scale use of artemisinin combination therapies to treat malaria.</p>
The population pharmacokinetics of artesunate (AS) and its active metabolite dihydroartemisinin (DHA) were studied in healthy subjects receiving single- or multiple-dosing of AS orally either in combination with pyronaridine (PYR) or as a monotherapy with or without food.. ...
BACKGROUND: Use of different methods for assessing the efficacy of artemisinin-based combination antimalarial treatments (ACTs) will result in different estimates being reported, with implications for changes in treatment policy. METHODS: Data from different in vivo studies of ACT treatment of uncomplicated falciparum malaria were combined in a single database. Efficacy at day 28 corrected by PCR genotyping was estimated using four methods. In the first two methods, failure rates were calculated as proportions with either (1a) reinfections excluded from the analysis (standard WHO per-protocol analysis) or (1b) reinfections considered as treatment successes. In the second two methods, failure rates were estimated using the Kaplan-Meier product limit formula using either (2a) WHO (2001) definitions of failure, or (2b) failure defined using parasitological criteria only. RESULTS: Data analysed represented 2926 patients from 17 studies in nine African countries. Three ACTs were studied: ...
Best practices, policy and innovations in the administration of healthcare in developing communities and countries. For administrators, academics, researchers and policy leaders. Includes peer reviewed research papers. Edited by Dr. Judith Shamian, President of the International Council of Nurses, Geneva CH
The emergence of resistance to the artemisinin drug, a potent anti-malarial medicine, now threatens to affect the big gains achieved in recent years in reducing the global burden of malaria - an estimated 1.2 billion fewer malaria cases and 6.2 million fewer malaria deaths globally between 2001 and 2015. This resistance, to artemisinin, becomes all…
We describe an analysis of genome variation in 825 P. falciparum samples from Asia and Africa that identifies an unusual pattern of parasite population structure at the epicenter of artemisinin resistance in western Cambodia. Within this relatively small geographic area, we have discovered several distinct but apparently sympatric parasite subpopulations with extremely high levels of genetic differentiation. Of particular interest are three subpopulations, all associated with clinical resistance to artemisinin, which have skewed allele frequency spectra and high levels of haplotype homozygosity, indicative of founder effects and recent population expansion. We provide a catalog of SNPs that show high levels of differentiation in the artemisinin-resistant subpopulations, including codon variants in transporter proteins and DNA mismatch repair proteins. These data provide a population-level genetic framework for investigating the biological origins of artemisinin resistance and for defining ...
Artemisinin combinations hold great promise for tackling malaria, but they must be used prudently to ensure they are sustainable for decades to come, says <EM>Ramanan Laxminarayan.</EM>
Articles that is. The spread of resistance to artemisinin drugs, the main-stay of modern Plasmodium falciparum (and even P. vivax in some places) malaria therapy, would endanger control programs globally (previously discussed here, here, here, and here). Last week saw a series of high-profile publications which received an impressive amount of coverage in the general…
Dihydroartemisinin (DHA), the main active metabolite of artemisinin derivatives strongly inhibits human papillomavirus-induced tumor formation.
Artemisinin resistance in falciparum malaria has emerged in western Cambodia exactly where chloroquine resistance arose 50 years ago. Similarly to the resistance to chloroquine that spread to Africa, the experts are wondering whether artemisinin resistance will spread as widely. In such a case the consequences would be disastrous.. ...
1. Cytochrome P450 enzyme system is the most important contributor to oxidative metabolism of drugs. Modification, and more specifically inhibition, of this system is an important determinant of several drug-drug interactions (DDIs). 2. Effects of the antimalarial agent artemisinin and its structural analogues, artemether, artesunate and dihydroartemisinin, on seven of the major human liver CYP isoforms (CYP1A2, 2A6, 2B6, 2C9, 2C19, 2D6 and 3A4) were evaluated using recombinant enzymes (fluorometric assay) and human liver microsomes (LC-MS/MS analysis). Inhibitory potency (IC50) and mechanisms of inhibition were evaluated using nonlinear regression analysis. In vitro-in vivo extrapolation using the [I]/Ki ratio was applied to predict the risk of DDI in vivo. 3. All compounds tested inhibited the enzymatic activity of CYPs, mostly through a mixed type of inhibition, with CYP1A2, 2B6, 2C19 and 3A4 being affected. A high risk of interaction in vivo was predicted if artemisinin is coadministrated ...
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Artemisinin and its derivatives, artesunate, artemether, and dihydroartemisinin, are the most rapidly acting of all antimalarials
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WANG PHA, Thailand-Dr. Aung Pyae Phyo hasnt seen a malaria case in five days. Thats not so unusual anymore at the clinic he runs in this small town j ...
those artemisinins again... Hi, Lisa; I dont know exactly how these things work, and the best source of info I have found to date is the review...
The efficacy and safety of artemether-lumefantrine for the treatment of malaria in nonimmune populations are not well defined. In this study, 165 nonimmune patients from Europe and non-malarious areas of Colombia with acute, uncomplicated falciparum malaria or mixed infection including P. falciparum were treated with the six-dose regimen of artemether-lumefantrine. The parasitologic cure rate at 28 days was 96.0% for the per protocol population (119/124 patients). Median times to parasite clearance and fever clearance were 41.5 and 36.8 hours, respectively. No patient had gametocytes after Day 7. Treatment was well tolerated; most adverse events were mild to moderate and seemed to be related to malaria. There were few serious adverse events, none of which were considered to be drug-related. No significant effects on ECG or laboratory parameters were observed. In conclusion, the six-dose regimen of artemether-lumefantrine was effective and well tolerated in the treatment of acute uncomplicated falciparum
This study evaluated and compared the efficacy of five brands of Artemisinin Combination Therapies (ACTs); Dihydroartemisinin plus Piperaquine, Artesunate plus Amodiaquine, Artesunate plus Sulphadoxine/Pyrimethamine, Artemether plus lumefantrine and Artesunate plus mefloquine combinations in vivo in P.berghei infected swiss albino mice. The experimental animals were pre-screened to rule out infection. All drugs were administered as clinical doses for the curative test and the Mean Percentage Parasitemia level assessed daily for seven days and on day 60. The results showed that all the drugs were effective with artesunate plus amodiaquine combination being the most efficacious followed by dihydroartemisinin plus piperaquine and artesunate plus sulphadoxine plus pyrimethamine combinations followed by artesunate plus mefloquine combination and artemether plus lumefantrine combination which was the least efficacious. Results on day 60 showed increasing parasitemia levels in mice which received Artemether
Since 2012, a single low dose of primaquine (SLDPQ; 0.25 mg/kg of body weight) with artemisinin-based combination therapies has been recommended as the first-line treatment of acute uncomplicated Plasmodium falciparum malaria to interrupt its transmission, especially in low-transmission settings of multidrug resistance, including artemisinin resistance. Policy makers in Cambodia have been reluctant to implement this recommendation due to primaquine safety concerns and a lack of data on its efficacy. In this randomized controlled trial, 109 Cambodians with acute uncomplicated P. falciparum malaria received dihydroartemisinin-piperaquine (DP) alone or combined with SLDPQ on the first treatment day. The transmission-blocking efficacy of SLDPQ was evaluated on days 0, 1, 2, 3, 7, 14, 21, and 28, and recrudescence by reverse transcriptase PCR (RT-PCR) (gametocyte prevalence) and membrane feeding assays with Anopheles minimus mosquitoes (gametocyte infectivity). Without the influence of recrudescent
Abstract. The emergence of artemisinin-resistant Plasmodium falciparum in the Greater Mekong Subregion threatens both the efficacy of artemisinin-based combination therapy (ACT), the first-line treatment for malaria, and prospects for malaria elimination. Monitoring of ACT efficacy is essential for ensuring timely updates to elimination policies and treatment recommendations. In 2014-2015, we assessed the therapeutic efficacies of artemether-lumefantrine (AL) and dihydroartemisinin-piperaquine (DP) for the treatment of uncomplicated P. falciparum at three study sites in Rakhine, Shan, and Kachin states in Myanmar. Patients presenting with uncomplicated P. falciparum malaria were enrolled, treated, and followed up for 28 days for AL or 42 days for DP. Both AL and DP demonstrated good therapeutic efficacy at all three study sites. The 28-day cure rate for AL was > 96% across all study sites, and the 42-day cure rate for DP was 100%. Parasitemia on day 3 was detected in 0%, 3.3%, and 3.6% of
Malnutrition and malaria frequently coexist in sub-Saharan African countries. Studies on efficacy of antimalarial treatments usually follow the WHO standardized protocol in which severely malnourished children are systematically excluded. Few studies have assessed the efficacy of chloroquine, sulfadoxine-pyrimethamine and quinine in severe acute malnourished children. Overall, efficacy of these treatments appeared to be reduced, attributed to lower immunity and for some antimalarials altered pharmacokinetic profiles and lower drug concentrations. However, similar research on the efficacy and pharmacokinetic profiles of artemisinin-combination therapies (ACTs) and especially artemether-lumefantrine in malnourished children is currently lacking. The main objective of this study is to assess whether artemether-lumefantrine is less efficacious in children suffering from severe acute malnutrition (SAM) compared to non-SAM children, and if so, to what extent this can be attributed to a sub-optimal ...
Artemisinins are derived from extracts of sweet wormwood (Artemisia annua) and are well established for the treatment of malaria, including highly drug-resistant strains. Their efficacy also extends to phylogenetically unrelated parasitic infections such as schistosomiasis. More recently, they have …
BACKGROUND: The emergence of resistance against artemisinin combination treatment is a major concern for malaria control. ACTs are recommended as the rescue treatment, however, there is limited evidence as to whether treatment and re-treatment with ACTs select for drug-resistant P. falciparum parasites. Thus, the purpose of the present study is to investigate the impact of (re-)treatment using artesunate-amodiaquine (ASAQ) and artemether-lumefantrine (AL) on the selection of P. falciparum multidrug resistance-1 (Pfmdr1) alleles in clinical settings.. METHODS: P. falciparum positive samples were collected from children aged 12-59 months in a clinical trial in DR Congo and Uganda. Pfmdr1 single nucleotide polymorphisms (SNPs) analysis at codons N86Y, Y184F, and D1246Y were performed at baseline and post-treatment with either AL or ASAQ as a rescue treatment using nested PCR followed by restriction fragment length polymorphism (RFLP) assays.. RESULTS: The pre-treatment prevalence of Pfmdr1 N86 and ...
A study recently published in Nature Medicine1 reports of the emergence of de novo laboratory markers for artemisinin resistance in Rwanda. While concerning, the study has also shown that the artemisinin-based combination therapies (ACTs), which are the first-line treatment for acute uncomplicated P. falciparum malaria, nevertheless continue to cure the disease in Africa.
Introduction: Artesunate is a semi-synthetic derivative of artemisinin, a natural compound from the herb sweet wormwood (Artemisia annua L). Artemisinin has been used for centuries in traditional Chinese medicine while artesunate has recently been used as an anti-malarial drug. Artesunate is also cytotoxic to human cancer cells. Since the use of artesunate as an anti-malarial agent is associated with few adverse effects, artesunate may represent a less toxic alternative to conventional chemotherapy. This study investigates the effects of artesunate on ovarian cancer cell lines and the mechanism(s) underlying its activity. Methods and Results: Artesunate had a time- and dose-dependent growth inhibitory effect on all ovarian carcinoma cell lines examined (SKOV3, OVCAR3, IG-OV-1, HEY) using an MTT assay. Further examination of artesunate-treated SKOV3 and HEY cells using Oregon Green-488 and Annexin-V-FLUOS/propidium iodide staining indicated that artesunate had a strong anti-proliferative effect ...
We report a large multicenter genome-wide association study of Plasmodium falciparum resistance to artemisinin, the frontline antimalarial drug. Across 15 locations in Southeast Asia, we identified at least 20 mutations in kelch13 (PF3D7_1343700) affecting the encoded propeller and BTB/POZ domains, which were associated with a slow parasite clearance rate after treatment with artemisinin derivatives. Nonsynonymous polymorphisms in fd (ferredoxin), arps10 (apicoplast ribosomal protein S10), mdr2 (multidrug resistance protein 2) and crt (chloroquine resistance transporter) also showed strong associations with artemisinin resistance. Analysis of the fine structure of the parasite population showed that the fd, arps10, mdr2 and crt polymorphisms are markers of a genetic background on which kelch13 mutations are particularly likely to arise and that they correlate with the contemporary geographical boundaries and population frequencies of artemisinin resistance. These findings indicate that the risk of new
Artemisinin and its derivatives provide faster clearance of parasitemia than any other antimalarial drugs and these drugs are part of frontline combination therapies in areas where drug-resistant Plasmodium falciparum exists. Clinical resistance to artemisinins is emerging on the Thailand-Cambodia border, making it imperative to investigate mechanisms of artemisinin resistance. Previous work in our laboratory showed ring-stage parasites enter a dormant state after exposure to artemisinin. We hypothesize that this period of dormancy is directly related to recrudescence and prolonged parasite clearance times in patients, and possibly resistance. The target of artemisinin is currently unknown, and potential resistance mechanisms are not well described. Our laboratory previously selected artemisinin resistance in P. falciparum clones D6 (Africa), W2 (southeast Asia), and a patient isolate from Thailand, TM91c235. Studies were attempted in order to characterize artemisinin resistant phenotypes and ...
Artemisinin and its derivatives provide faster clearance of parasitemia than any other antimalarial drugs and these drugs are part of frontline combination therapies in areas where drug-resistant Plasmodium falciparum exists. Clinical resistance to artemisinins is emerging on the Thailand-Cambodia border, making it imperative to investigate mechanisms of artemisinin resistance. Previous work in our laboratory showed ring-stage parasites enter a dormant state after exposure to artemisinin. We hypothesize that this period of dormancy is directly related to recrudescence and prolonged parasite clearance times in patients, and possibly resistance. The target of artemisinin is currently unknown, and potential resistance mechanisms are not well described. Our laboratory previously selected artemisinin resistance in P. falciparum clones D6 (Africa), W2 (southeast Asia), and a patient isolate from Thailand, TM91c235. Studies were attempted in order to characterize artemisinin resistant phenotypes and molecular
BACKGROUND: The World Health Organization (WHO) in 2015 stated atovaquone-proguanil can be used in travellers, and is an option in malaria-endemic areas in combination with artesunate, as an alternative treatment where first-line artemisinin-based combination therapy (ACT) is not available or effective. This review is an update of a Cochrane Review undertaken in 2005. OBJECTIVES: To assess the efficacy and safety of atovaquone-proguanil (alone and in combination with artemisinin drugs) versus other antimalarial drugs for treating uncomplicated Plasmodium falciparum malaria in adults and children. SEARCH METHODS: The date of the last trial search was 30 January 2020. Search locations for published trials included the Cochrane Infectious Diseases Group Specialized Register, CENTRAL, MEDLINE, Embase, and LILACS. To include recently published and unpublished trials, we also searched ClinicalTrials.gov, the metaRegister of Controlled Trials and the WHO International Clinical Trials Registry Platform ...
Artemisinin-based combination therapy (ACT) is recommended as a means of prolonging the effectiveness of first-line malaria treatment regimens. Different brands of mefloquine (MQ) have been reported to be non-bioequivalent; this could result in sub-therapeutic levels of mefloquine with decreased efficacy. In 2002, mefloquine-artesunate (MQ-AS) combination therapy was adopted as the first-line treatment for uncomplicated Plasmodium falciparum malaria in the Amazon region of Peru. Although MQ resistance has yet to be reported from the Peruvian Amazon, it has been reported from other countries in the Amazon Region. Therefore, continuous monitoring is warranted to ensure that the first-line therapy remains efficacious. This study examines the in vivo efficacy and pharmacokinetic parameters through Day 56 of three commercial formulations of MQ (Lariam®, Mephaquin®, and Mefloquina-AC® Farma) given in combination with artesunate ...
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The combined gametocidal effect of primaquine plus artemisinin-combination therapy (ACT) to reduce post-treatment transmission of P. falciparum malaria is a key operational research question for malaria treatment (previously discussed here). And the evidence of adding primaquine, particularly in areas of low to medium transmission, keeps piling up. Smithius et al. report results from a massive…
Resistance to malaria drugs can be found at varying levels and low levels of resistance may not impact on control. Artemisinin and its derivatives, are not used alone for the treatment of uncomplicated malaria, but are combined with a partner drug; this is known as artemisinin-based combination therapy (ACT). Currently the level of artemisinin resistance means that ACT treatment can still be effective in these areas provided the partner drug is efficacious. However, there is a real and serious risk that drug resistance will worsen and spread further. ACT resistance has already been identified on the Thai-Cambodia border. Intense efforts by the global malaria control community are underway to attempt to halt the spread of these resistant parasites and to delay emergence of resistance elsewhere ...
Background.The spread of Plasmodium falciparum resistance to artemisinin derivatives in Southeast Asia is a major source of concern and the emergence of resistance in Africa would have dramatic consequences, by increasing malaria mortality and morbidity. It is therefore urgent to implement regular monitoring in sentinel sites in sub-Saharan Africa using robust and easy-to-implement tools. The prevalence of k13-propeller mutations and the phenotypic profiles are poorly known in sub-Saharan Africa. Here, the k13-propeller polymorphism was compared to both ex vivo susceptibility to DHA and early parasitological and clinical responses to artemisinin combination therapy (ACT). Methods. Plasmodium falciparum isolates were collected in 2015 in Yaoundé (Cameroon) from patients treated with dihydroartemisinin-piperaquine combination. Samples were analysed for their susceptibility to artemisinin using the k13-propeller sequencing, the ex vivo ring-stage survival assay, the in vivo parasite positive rate and the
The study was conducted in southern Zambia, with colleagues from the Johns Hopkins Malaria Research Institute in Macha. Researchers analyzed data from surveys conducted in 2007 and between 2008 and 2009. In both surveys, households were screened for malaria using rapid diagnostic tests and treated with artemisinin combination therapy when malaria was detected.. According to the new study, a proactive test-and-treat case-detection strategy resulted in a sixfold reduction in prevalence in 2008 and 2009, with the initial parasite prevalence at 4 percent. Test and treat showed a twofold reduction in 2007, when community prevalence was higher at 24 percent.. Proactive case detection with treatment using artemisinin-combination therapy can reduce transmission and provide indirect protection to household members. If resources permit, this strategy could be targeted to hot spots to achieve further reductions in malaria transmission, said William J. Moss, MD, senior author of the study and associate ...
The SEAQUAMAT trial was a multicentre, open-label, randomised comparison of parenteral artesunate (Inj AS) and parenteral quinine (Inj Q) in patients with severe P. falciparum over the age of two. The study was carried out between June 2003 and May 2005 in Bangladesh, Myanmar (Burma), India, and Indonesia. Based on previous studies that suggested Inj AS as more beneficial over artemether and positive results from an initial pilot comparing quinine with artesunate, the aim of the study was to establish conclusively which, of parenteral artesunate or parenteral quinine, is the more effective drug for the treatment of severe malaria.. The study was stopped by DSMC after 1461 patients were enrolled and had received either Inj AS (730 assigned) or Inj Q (731 assigned). There were 202 children (younger than age 15 years) in the study of whom 89 were aged younger than 6 years.. Conclusions of the study. ...
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This is probably the first publication on efficacy of AS+SMP in the treatment of uncomplicated falciparum malaria. The high cure rate demonstrated for AS+-SMP (,90%) in this study was expected because of the synergistic effect of artesunate and SMP and potentially because of the non-wide use of SMP as an antimalarial in this country. Previously high efficacy of SMP for the treatment of uncomplicated P. falciparum malaria was reported in other African countries [8-10].. Although the loose combinations of AS+SMP was slightly (not significantly) more efficacious than the fixed one, the fixed regimen of AS+SMP is most promising since it permits reduction of the treatment duration to a maximum of 24 h. The mechanism of action of SM drug is the same as of sulfadoxine(S), but its protein binding and elimination half-life permit the new regimen to be developed in SM rather than in SP [6, 7, 16]. The repeated loading dose of AS is responsible for a drastic destruction of parasites whereas the SMP ...
Abstract Artemisinin resistance in Plasmodium falciparum threatens the remarkable efficacy of artemisinin-based combination therapies worldwide. Thus, greater insight into the resistance mechanism using monitoring tools is essential. The ring-stage survival assay is used for phenotyping artemisinin-resistance or decreased artemisinin sensitivity. Here, we review the progress of this measurement assay and explore its limitations and potential applications ...
Artemisinin derivative drugs are central to the management of malaria.6 Parenteral artesunate should be first line treatment in all patients diagnosed with severe malaria including children and all trimesters of pregnancy. Artesunate has been shown to reduce mortality compared to quinine in two large trials (SEAQUAMAT in south east Asia and AQUAMAT in Africa).7,8 Artesunate does not hold a UK license, but is available in many UK infectious diseases units and can be urgently supplied from specialist tropical medicine centres in London and Liverpool (contact details below). Malaria is life-threatening, and can progress rapidly, so if artesunate is not immediately available, treatment of severe malaria with intravenous (IV) quinine should not be delayed whilst artesunate is being obtained. If you are not experienced in managing severe malaria we recommend getting advice from a specialist centre for the complications including cerebral malaria, acute lung injury and renal failure, but in all ...
A growing public health risk originating in Asia, drug resistance, is threatening to undermine gains in malaria control. Significant progress has been made in recent years in the fight against malaria. Since 2000, mortality from malaria has decreased by over 25 percent globally. Scale-up of effective malaria interventions, including the use of artemisinin-based combination therapies - the most effective drug for treating the disease - have been instrumental to this success. However, growing resistance to artemisinins by the malaria parasite has been emerging in Southeast Asia and is threatening to reverse the gains that have been made to date. In this interview, Senior Technical Officer at Malaria Consortium, Dr Prudence Hamade, explains how dangerous a spread the spread of parasite resistance to anti-malarial drugs could be in Asia and beyond.. Q: Can you explain what drug-resistant malaria is and what the state of resistance is now in Southeast Asia?. A: Drug-resistant malaria refers to the ...
We included 27 trials, enrolling 16,382 adults and children, and conducted between 2002 and 2010. Most trials excluded infants aged less than six months and pregnant women.. DHA-P versus artemether-lumefantrine In Africa, over 28 days follow-up, DHA-P is superior to artemether-lumefantrine at preventing further parasitaemia (PCR-unadjusted treatment failure: RR 0.34, 95% CI 0.30 to 0.39, nine trials, 6200 participants, high quality evidence), and although PCR-adjusted treatment failure was below 5% for both ACTs, it was consistently lower with DHA-P (PCR-adjusted treatment failure: RR 0.42, 95% CI 0.29 to 0.62, nine trials, 5417 participants, high quality evidence). DHA-P has a longer prophylactic effect on new infections which may last for up to 63 days (PCR-unadjusted treatment failure: RR 0.71, 95% CI 0.65 to 0.78, two trials, 3200 participants, high quality evidence).. In Asia and Oceania, no differences have been shown at day 28 (four trials, 1143 participants, moderate quality evidence), ...
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This study showed that AL and AS-AQ remain efficacious, well-tolerated, and are safe to treat uncomplicated malaria in children from Lambaréné. However, a regular monitoring of efficacy and a study of molecular markers of drug resistance to artemisinin in field isolates is essential. Trial registrat …
The artemisinin compounds, which are well-known for their potent therapeutic antimalarial activity, possess in vivo and in vitro antitumor effects. Although the anticancer effect of artemisinin compounds has been extensively reported, the precise mechanisms underlying its cytotoxicity remain under intensive study. In the present study, a high-throughput quantitative proteomics approach was applied to identify differentially expressed proteins of HCT116 colorectal cancer cell line with artesunate (ART) treatment. Through Ingenuity Pathway Analysis, we discovered that the top-ranked ART-regulated biological pathways are abrogation of fatty acid biosynthetic pathway and mitochondrial dysfunction. Subsequent assays showed that ART inhibits HCT116 cell proliferation through suppressing the fatty acid biosynthetic pathway and activating the mitochondrial apoptosis pathway. In addition, ART also regulates several proteins that are involved in NF-κB pathway, and our subsequent assays showed that ART suppresses
This study is evaluating the safety of Dihydroartemisinin-Piperaquine for the use in mass treatment campaigns to block malaria transmission.
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The parasite that causes malaria is showing signs of resistance to the most potent drugs currently used against it. Scientists report that top-line drugs called
COARTEM (Artemether,Lumefantrine) drug information & product resources from MPR including dosage information, educational materials, & patient assistance.
COARTEM (Artemether,Lumefantrine) drug information & product resources from MPR including dosage information, educational materials, & patient assistance.
Eurartesim(R) - dihydroartemisinin piperaquine (DHA-PQP) - the first artemisinin combination therapy (ACT) has been approved by the European Medicines Agency (EMA) for the treatment of uncomplicated malaria.
Artemisinins can be used alone, but this leads to a high rate of return of parasites and other drugs are required to clear the ... Artemisinins are not used for malaria prevention because of the extremely short activity (half-life) of the drug. To be ... Artemisinins are generally well tolerated at the doses used to treat malaria. The side effects from the artemisinin class of ... Artemisinins were later found to possess a broad spectrum of activity against a wide range of trematodes, including Schistosoma ...
"Rectal artemisinins rapidly eliminate malarial parasites". EurekAlert!. 2008-03-27. Archived from the original on 3 April 2008 ...
August 2003). "Artemisinins target the SERCA of Plasmodium falciparum". Nature. 424 (6951): 957-61. doi:10.1038/nature01813. ... The main evidence came from a Xenopus oocyte system describing specific interactions between artemisinins and PfATP6 as well as ... A single amino acid residue can determine the sensitivity of SERCAs to artemisinins". Nature Structural & Molecular Biology. 19 ... "A single amino acid residue can determine the sensitivity of SERCAs to artemisinins". Nature Structural & Molecular Biology. 19 ...
Dellicour S, Hall S, Chandramohan D, Greenwood B (2007). "The safety of artemisinins during pregnancy: a pressing question". ... Artemether is an artemisinin derivative and the mechanism of action for artemisinins is.[medical citation needed] Artemether ...
Keiser, J.; Utzinger, J. R. (2007). "Artemisinins and synthetic trioxolanes in the treatment of helminth infections". Current ...
Keiser J, Utzinger J (December 2007). "Artemisinins and synthetic trioxolanes in the treatment of helminth infections". Current ...
The cost of artemisinins limits their use in the developing world. Malaria strains found on the Cambodia-Thailand border are ... Resistance is now common against all classes of antimalarial drugs apart from artemisinins. Treatment of resistant strains ... Artemisinins, discovered by Chinese scientist Tu Youyou and colleagues in the 1970s from the plant Artemisia annua, became the ... to artemisinin monotherapies in subtherapeutic doses for over 30 years and the availability of substandard artemisinins likely ...
They recommend that it be used only when artemisinins are not available. Quinine is also used to treat lupus and arthritis. ...
Artemisinins are sesquiterpene lactones isolated from Artemisia annua, a Chinese traditional medicine. These suppositories are ...
Artesunate is in the class of medications known as artemisinins, which are derivatives from sweet wormwood (Artemisia annua). ... His team, however, demonstrated resistance of Plasmodium falciparum to artemisinins in Western Cambodia. New treatments would ...
The best recognised adverse effect of the artemisinins is that they lower reticulocyte counts. This is not usually of clinical ... It is in the class of medications known as artemisinins, which are derivatives from "qinghao," or sweet wormwood plant ( ... Clark RL (2012). "Effects of artemisinins on reticulocyte count and relationship to possible embryotoxicity in confirmed and ...
The artemisinins became the most potent as well as the safest and most rapidly acting antimalarial drugs, recommended by the ... Weina, PJ (2008). "Artemisinins from folklore to modern medicine--transforming an herbal extract to life-saving drugs". ... For their high efficacy, safety and stability, artemisinins such as artemether and artesunate became the drugs of choice in ... All clinical trials by this time confirmed that artemisinins are more effective than the conventional antimalarial drugs, such ...
Artemisinins and derivatives are proving to be candidates as drugs of choice for trematodiasis. In regions where helminthiasis ...
... evaluation to determine and predict the neurotoxicity of artemisinins". Toxicology. 279 (1-3): 1-9. doi:10.1016/j.tox.2010.09. ...
The project resulted in the discovery of artemisinins, a class of antimalarial drugs, from the medicinal plant Artemisia annua ...
4-trioxane ring are important potential improvements over the naturally derived artemisinins. The peroxide group in the 1,2,4- ...
Eckstein-Ludwig U, Webb R, Van Goethem I, East J, Lee A, Kimura M, O'Neill P, Bray P, Ward S, Krishna S (2003). "Artemisinins ... CAs to artemisinins". Nat Struct Mol Biol 12 (7): 628-9. doi:10.1038/nsmb947. பப்மெட் 15937493. ...
... including chloroquine and artemisinins, were used to resist the scourge. Today, artemisinin is present in every remedy applied ...
"Toxicokinetic and toxicodynamic (TK/TD) evaluation to determine and predict the neurotoxicity of artemisinins". Toxicology ...
... except for the artemisinins. Malaria was once common in most of Europe and North America, where it is now for all purposes non- ...
Eckstein-Ludwig U, Webb R, Van Goethem I, East J, Lee A, Kimura M, O'Neill P, Bray P, Ward S, Krishna S (2003). "Artemisinins ... CAs to artemisinins". Nat Struct Mol Biol. 12 (7): 628-9. doi:10.1038/nsmb947. PMID 15937493.. CS1 maint: multiple names: ...
... artemisinins MeSH D02.455.849.765.424 - farnesol MeSH D02.455.849.765.444 - gossypol MeSH D02.455.849.765.750 - santonin MeSH ... artemisinins MeSH D02.389.338.450 - lipid peroxides MeSH D02.389.338.825 - tert-butylhydroperoxide MeSH D02.389.338.912 - ...
... ngaphandle kwe-artemisinins [20] Umalaleveva wake wayisifo esivamile e-Yurophu naseNyakatho neMelika, lapho ongasabonwa khona.[ ...
Prudent use can make artemisinins sustainable. By Ramanan Laxminarayan. Since its introduction in the 1950s, chloroquine has ... But, despite their promise, artemisinins need to be used prudently to ensure that they can be used to treat malaria for decades ... But, despite their promise, artemisinins need to be used prudently to ensure that they can be used to treat malaria for decades ...
Artemisinins are derived from extracts of sweet wormwood (Artemisia annua) and are well established for the treatment of ... Artemisinins: their growing importance in medicine Trends Pharmacol Sci. 2008 Oct;29(10):520-7. doi: 10.1016/j.tips.2008.07.004 ... Artemisinins are derived from extracts of sweet wormwood (Artemisia annua) and are well established for the treatment of ... In this review, we discuss recent advances in defining the role of artemisinins in medicine, with particular focus on their ...
Review: Plasmodium sensitivity to artemisinins: magic bullets hit elusive targets February 2, 2011 - 13:53 -- Patrick Sampao. ... Lack of Association of the S769N Mutation in Plasmodium falciparum SERCA (PfATP6) with Resistance to Artemisinins. April 13, ... Artemisinins are proposed to act in the malaria parasite cytosol by oxidizing dihydroflavin cofactors of redox-active ... Artemisinins rapidly oxidize leucomethylene blue (LMB) to methylene blue (MB); they also oxidize dihydroflavins such as the ...
... and artemisinins (ART) with long UTLs. Unfortunately, almost all new targets currently being explored for development of novel ... rational drug design lessons from pleiotropic action of quinolines and artemisinins.. Muregi FW1. ...
Inducing Effect of Dihydroartemisinic Acid in the Biosynthesis of Artemisinins with Cultured Cells of Artemisia annua by ... Jianhua Zhu, Jiazeng Yang, Zihan Zeng, et al., "Inducing Effect of Dihydroartemisinic Acid in the Biosynthesis of Artemisinins ...
Malaria Parasite Showing Signs of Resistance to Top-Line Drugs (Artemisinins). October 29, 2008. By MedNews Leave a Comment ... Scientists report that top-line drugs called artemisinins take nearly twice as long to knock out the parasite in people who ...
In this study, the antiplasmodial activity of SC83288 against artemisinins was profiled in order to assess its potential to ... The results obtained in this study are consistent with artemisinins and SC83288 having distinct modes of action and different ... Based on growth inhibition and ring survival assays, no cross-resistance was observed between artemisinins and SC83288, using ... supports efforts to continue the clinical development of SC83288 against severe malaria as an alternative to artemisinins in ...
西太平洋区域委员会, 060 (马尼拉:世卫组织西太平
Quick test can predict anaemia in malaria patients treated with artemisinins Share ... Quick test can predict anaemia in malaria patients treated with artemisinins * Microbiology laboratory reopened after ... Artemisinins should replace quinine for first-trimester malaria treatment, says new study ...
Artemisinins-based combination therapies (ACTs) are being recommended against uncomplicated malaria in endemic areas of Africa ... Molecular screening for Plasmodium falciparum resistance markers for artemisinins in Mbita, Kenya. ...
Fingerprint Dive into the research topics of Artemisinins. Together they form a unique fingerprint. * Sort by ...
Mechanism of Resistance in Artemisinins. The resistance of plasmodium parasites to artemisinin is attributed to young ring ...
Fully Synthetic Artemisinins. It is important to recall that some limitations of artemisinins such as short half-life (between ... 6. Future Development of Artemisinins as Anticancer Drugs. Artemisinins have been recommended and widely used as antimalarials ... Artemisinins seems to regulate key players participating in multiple pathways such as NF-κB, survivin, NOXA, HIF-1α, and BMI-1 ... The first generation of semisynthetic artemisinins includes arteeter and artemether, the lipophilic artemisinins, whereas ...
Book; Format: print Publisher: Geneva : World Health Organization, 2007Other title: Use of rectal artemisinin-based suppositories in the management of severe malaria.Title translated: Suppositoires à base dαartemisinine : utilisation des suppositoires à base dartémisinine dans la prise en charge du paludisme grave : rapport dune consultation informelle de lOMS..Online access: Full text now in IRIS Availability: Items available for loan: WHO HQ [Call number: WC 770 2007AR] (1). ...
Antimalarial Drugs: Age of the Artemisinins. $105.00. - $330.00. Select options. Sort by popularity. Sort by latest. Sort by ...
Artemisinins: A class of drugs used for the treatment (not prevention) of malaria usually as a part of a combination therapy, ...
The molecular and cellular action properties of artemisinins: what has yeast told us? - Artemisinin (ART) or Qinghaosu is a ... Please cite this article as: Chen Sun and Bing Zhou (2016). The molecular and cellular action properties of artemisinins: what ... C.M. Moore, E.M. Hoey, A. Trudgett, and D.J. Timson, "Artemisinins act through at least two targets in a yeast model", FEMS ... Q. Huang, and B. Zhou, " Exploring artemisinins protein targets in yeast.", JOURNAL-TSINGHUA UNIVERSITY 48(3): 408-411., 2008. ...
Results of search for su:{Artemisinins} and su-to:Drug resistance. Refine your search. *Availability * Limit to currently ...
Recent researches of antitumor activity of artemisinins on breast cancer mainly focus on the nanoliposomal artemisinins [11, 39 ... indicating that the anticancer activity of artemisinins have selectivity. Artemisinins might cause antitumor activity in cancer ... Deeper investigations showed us that artemisinins also cause immune response to the cancer cells [7, 10, 40]. Five kinds of ... Since then, increasing number of literatures proved the anti-leukemia potentials of artemisinins, detailed in Table 1.. Table 1 ...
Artemisinins can be used alone, but this leads to a high rate of return of parasites and other drugs are required to clear the ... Artemisinins are not used for malaria prevention because of the extremely short activity (half-life) of the drug. To be ... Artemisinins are generally well tolerated at the doses used to treat malaria. The side effects from the artemisinin class of ... Artemisinins were later found to possess a broad spectrum of activity against a wide range of trematodes, including Schistosoma ...
toxicity of artemisinins. Submitted by David Warhurst on March 20, 2015 - 12:54. Way back, there was so much convincing ... Rapid elimination of artemisinins after oral intake represents a relatively safe route of administration compared to delayed ... There is now good evidence to support the use of artemisinins in the current dosing regimens (Efferth & Kaina 2010) but the ... However, in rats and monkeys, the embryonic erythroblasts are much more sensitive to artemisinins than are erythroblasts in the ...
Artemisinins. Lumefantrine. Artemether. Piperaquine. Amodiaquine. Artemether-lumefantrine combination. Dihydroartemisinin. ...
Artemisinins. Antimalarials. HIV Protease Inhibitors. Protease Inhibitors. Enzyme Inhibitors. Molecular Mechanisms of ...
Artemisinins. Ivermectin. Antimalarials. Antiprotozoal Agents. Antiparasitic Agents. Anti-Infective Agents. To Top ...
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the contacts provided below. For general information, Learn About Clinical Studies. ...
... multifaceted resistance to artemisinins. Malar J 15:149. https://doi.org/10.1186/s12936-016-1206-9 CrossRefPubMedPubMedCentral ...
Artemisinins target the SERCA of Plasmodium falciparum. Nature 424, 957-961 (2003). ... Krishna, S., Woodrow, C.J., Staines, H.M., Haynes, R.K. & Mercereau-Puijalon, O. Re-evaluation of how artemisinins work in ...
  • Nowadays, artemisinins are the mainstay of malaria treatment, but initial indications of resistance against clinically used derivatives are present. (malariaworld.org)
  • Based on growth inhibition and ring survival assays, no cross-resistance was observed between artemisinins and SC83288, using parasite lines that were resistant to either one of these drugs. (biomedcentral.com)
  • The results obtained in this study are consistent with artemisinins and SC83288 having distinct modes of action and different mechanisms of resistance. (biomedcentral.com)
  • This study further supports efforts to continue the clinical development of SC83288 against severe malaria as an alternative to artemisinins in areas critically affected by artemisinin-resistance. (biomedcentral.com)
  • WHO HQ Library catalog › Results of search for 'su:{Artemisinins} and su-to:Drug resistance. (who.int)
  • More importantly, artemisinins demonstrated minor side effects to normal cells and manifested the ability to overcome multidrug-resistance which is widely observed in cancer patients. (springer.com)
  • multifaceted resistance to artemisinins. (springer.com)
  • A concern was raised about the resistance to artemisinins of falciparum malaria in the country. (nih.gov)
  • The potential emergence and spread of resistance to artemisinins in the Plasmodium falciparum malaria parasite constitutes a major global health threat. (biomedcentral.com)
  • Because no other drugs as potent as artemisinins are available, the potential emergence of artemisinin resistance at Thai/Cambodia border and its spread to other areas has caused significant concerns [ 7 - 11 ], including the failure of front line ACT due to secondary partner drug resistance. (biomedcentral.com)
  • The powerful medicines known as artemisinins have plenty of mileage in them in the global fight against malaria, and concern about partial resistance has been overstated. (medicalxpress.com)
  • However, it is feasible that a drastic increase in resistance could occur, rendering artemisinins, and thus some combination therapies, ineffective. (healthmap.org)
  • This understanding may eventually help us to stem the rise of drug-resistant malaria, such as the emerging resistance to artemisinins," said Lisewski. (eurekalert.org)
  • As we are witnessing a rise of resistance to artemisinins, these results may help finding new pathways to successor drugs," said Lichtarge. (eurekalert.org)
  • It is no exaggeration to say that the consequences of widespread resistance to artemisinins would be catastrophic. (ibtimes.com)
  • Use of oral artemisinin-based monotherapy (oAMT) is considered a contributing factor to the development and spread of resistance to artemisinins. (who.int)
  • Countries where resistance to artemisinins or to ACT partner drugs is reported need to intensify malaria control in order to reduce the burden of the disease, and delay or prevent the spread of resistance. (who.int)
  • Especially important is that the combination makes it more difficult for resistance to artemisinins to develop. (uni-heidelberg.de)
  • In vitro tests showed that the susceptibility of Plasmodium falciparum to artemisinins was declining in China. (nih.gov)
  • Artemisinins are a family of drugs that currently form the frontline treatment against Plasmodium falciparum malaria. (eurekalert.org)
  • In this way, the profiles of methylene blue and artemisinins, which quickly and effectively eliminate the parasites in the red blood cells, complement each other. (uni-heidelberg.de)
  • Hence, improving the efficacy of artemisinins and of artemisinin-based combination therapy (ACT) represents a major short-term goal in the global fight against malaria. (biomedcentral.com)
  • The molecular and cellular action properties of artemisinins: what has yeast told us? (microbialcell.com)
  • In light of the vast preclinical literature on anticancer properties of artemisinins and their excellent, well-established safety profile it is surprising that there are not more reports, or more widespread off-label use of artemisinins for cancer. (plos.org)
  • Antimalarial drugs and their useful therapeutic lives: rational drug design lessons from pleiotropic action of quinolines and artemisinins. (nih.gov)
  • Drugs that target single and specific targets such as antimalarial antifolates and atovaquone (ATQ) are rendered ineffective within a short time of their clinical use, unlike drugs with pleiotropic action such as chloroquine (CQ) and artemisinins (ART) with long UTLs. (nih.gov)
  • University of Notre Dame researchers led an international team to identify a molecular mechanism responsible for making malaria parasites resistant to artemisinins, the leading class of antimalarial drugs. (medicalxpress.com)
  • Artemisinins are extremely important antimalarial drugs. (healthmap.org)
  • Derivatives of this extract, known collectively as artemisinins, are today very potent and effective antimalarial drugs, especially in combination with other medicines. (archive.org)
  • Along with artemisinins, quinine is one of the most effective antimalarial drugs available today. (archive.org)
  • In this study, the antiplasmodial activity of SC83288 against artemisinins was profiled in order to assess its potential to replace, or be combined with, artemisinin derivatives. (biomedcentral.com)
  • With the further development of artemisinin and its derivatives, studies have found that artemisinins also have desirable antitumor activity in human cancer treatment. (springer.com)
  • Il a été aussi noté que la chloroquine a été le médicament antipaludéen le plus prescrit et que les médicaments spécialisés à base de l'Artémisinine ont été, en tout et pour tout, prescrits en première et en deuxième positions de traitement couvrant ainsi 18,2 pour cent seulement des cas. (who.int)
  • Les prescriptions étaient en majorité la chloroquine au lieu des médicaments spécialisés a base Artémisinine. (who.int)
  • Inducing Effect of Dihydroartemisinic Acid in the Biosynthesis of Artemisinins with Cultured Cells of Artemisia annua by Enhancing the Expression of Genes," The Scientific World Journal , vol. 2014, Article ID 293190, 7 pages, 2014. (hindawi.com)
  • Artemisinins: pharmacological actions beyond anti-malarial. (springer.com)
  • But, despite their promise, artemisinins need to be used prudently to ensure that they can be used to treat malaria for decades to come. (scidev.net)
  • Artemisinins are generally well tolerated at the doses used to treat malaria. (wikipedia.org)
  • Discover new partner drugs for combination with artemisinins to treat malaria. (nih.gov)
  • In close collaboration with research groups at CeMM lead by Christoph Bock and Giulio Superti-Furga as well as the group of Tibor Harkany at the Medical University of Vienna they managed to elucidate the molecular mode of action by which artemisinins reshape alpha cells: The compound binds to a protein called gephyrin, that activates GABA receptors, central switches of the cellular signaling. (eurekalert.org)
  • As the molecular targets for artemisinins in fish, rodents and humans are very similar, chances are high that the effect on alpha cells will also occur in humans. (eurekalert.org)
  • However, the rationale for the use of artemisinins in anticancer therapy must be addressed by a greater understanding of the underlying mechanisms involved in their cytotoxic effects. (hindawi.com)
  • Scientists report that top-line drugs called artemisinins take nearly twice as long to knock out the parasite in people who contract malaria in western Cambodia as the drugs take in other areas-suggesting the parasite is finding ways to thwart the drugs' effects. (mednews.com)
  • Malaria is thwarting frontline drugs called artemisinins in Cambodia. (sciencenews.org)
  • Three classes of drugs: artemisinins, synthetic peroxides and DHFR (dihydrofolate reductase) inhibitors effected potent inhibition of proliferation with IC 50 s in the nM- low µM range, whereas a DHODH (dihydroorotate dehydrogenase) and a putative kinase inhibitor displayed no activity. (plos.org)
  • Common malaria drugs known as artemisinins block reproduction of the parasites in the human body and reduce the number of gametocytes in blood by half. (uni-heidelberg.de)
  • Then a team coordinated by Stefan Kubicek, Group Leader at CeMM, eventually got a lead: In their latest study, published in Cell (DOI: 10.1016/j.cell.2016.11.010), they showed that artemisinins hit the bulls eye. (eurekalert.org)
  • With our study, we could show that artemisinins change the epigenetic program of glucagon-producing alpha cells and induce profound alterations of their biochemical function", Stefan Kubicek explains. (eurekalert.org)
  • Obviously, the long term effect of artemisinins needs to be tested," says Stefan Kubicek. (eurekalert.org)
  • His infection did not respond to two kinds of artemisinins but was eventually cleared by quinine, an older drug. (newscientist.com)
  • Globally, artemisinins are the mainstay of treatment. (mdedge.com)
  • In xenograft models, exposure to artemisinins substantially reduces tumor volume and progression. (hindawi.com)
  • A considerable motivation for the interest in artemisinins in additional indications is their excellent, well-established safety profile. (plos.org)
  • By considering the benefits, limitations, and current and future development of artemisinins, we can then identify emerging questions and address future research needs in this promising field of cancer drug discovery. (hindawi.com)
  • Artemisinins are not used for malaria prevention because of the extremely short activity (half-life) of the drug. (wikipedia.org)
  • Artemisinins induce drug metabolism through the activation of the pregnane X receptor (PXR) in vitro. (gu.se)
  • Artemisinins-based combination therapies (ACTs) are being recommended against uncomplicated malaria in endemic areas of Africa. (ac.ke)
  • In the current study in Burkina Faso with 160 malaria patients between the ages of six and ten the Heidelberg scientists tested the effect of combination therapies with artemisinins and methylene blue on gametocytes in the blood. (uni-heidelberg.de)
  • Because of artemisinins' rapid elimination, they are used in combination with an agent that also kills blood parasites but has a slower elimination rate and a different mechanism of action. (mdedge.com)
  • In addition, potentiation occurs at sub-optimal concentrations of artemisinins and Cys that on their own have little or no effect on parasite growth. (biomedcentral.com)
  • Cys also dramatically enhances the efficacy and protective effect of artemisinins against cerebral malaria induced by infection with the P. berghei ANKA parasite. (biomedcentral.com)
  • With those cell lines, the researchers at CeMM where now able to test their compound library and found artemisinins to have the same effect as an Arx loss. (eurekalert.org)
  • 1 Groupe de recherche action en santé, Ouagadougou, Burkina Faso. (nih.gov)
  • The ability of Cys to improve the anti-plasmodial activity of different clinically used artemisinins was tested. (biomedcentral.com)
  • Ex vivo experiments, indicate that potentiation of the anti-plasmodial activity of artemisinins by Cys is direct and does not require the presence of host factors. (biomedcentral.com)
  • Artemisinins: their growing importance in medicine. (bewell.com)
  • The expectation among researchers is that this will also happen eventually with artemisinins. (kuow.org)
  • So the big fear is that the same could happen with artemisinins. (wuky.org)
  • Artemisinins are proposed to act in the malaria parasite cytosol by oxidizing dihydroflavin cofactors of redox-active flavoenzymes, and under aerobic conditions by inducing their autoxidation. (malariaworld.org)