Antimalarials: 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)Artemisinins: A group of SESQUITERPENES and their analogs that contain a peroxide group (PEROXIDES) within an oxepin ring (OXEPINS).Chloroquine: 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.Plasmodium falciparum: A species of protozoa that is the causal agent of falciparum malaria (MALARIA, FALCIPARUM). It is most prevalent in the tropics and subtropics.Parasitic Sensitivity Tests: Tests that demonstrate the relative effectiveness of chemotherapeutic agents against specific parasites.Mefloquine: A phospholipid-interacting antimalarial drug (ANTIMALARIALS). It is very effective against PLASMODIUM FALCIPARUM with very few side effects.Malaria: 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.Quinine: An alkaloid derived from the bark of the cinchona tree. It is used as an antimalarial drug, and is the active ingredient in extracts of the cinchona that have been used for that purpose since before 1633. Quinine is also a mild antipyretic and analgesic and has been used in common cold preparations for that purpose. It was used commonly and as a bitter and flavoring agent, and is still useful for the treatment of babesiosis. Quinine is also useful in some muscular disorders, especially nocturnal leg cramps and myotonia congenita, because of its direct effects on muscle membrane and sodium channels. The mechanisms of its antimalarial effects are not well understood.Malaria, Falciparum: 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.SesquiterpenesDrug Resistance: 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.Fluorenes: A family of diphenylenemethane derivatives.Sulfadoxine: A long acting sulfonamide that is used, usually in combination with other drugs, for respiratory, urinary tract, and malarial infections.Pyrimethamine: One of the FOLIC ACID ANTAGONISTS that is used as an antimalarial or with a sulfonamide to treat toxoplasmosis.Plasmodium cynomolgi: A protozoan parasite that occurs naturally in the macaque. It is similar to PLASMODIUM VIVAX and produces a type of malaria similar to vivax malaria (MALARIA, VIVAX). This species has been found to give rise to both natural and experimental human infections.PhenanthrenesPlasmodium: A genus of protozoa that comprise the malaria parasites of mammals. Four species infect humans (although occasional infections with primate malarias may occur). These are PLASMODIUM FALCIPARUM; PLASMODIUM MALARIAE; PLASMODIUM OVALE, and PLASMODIUM VIVAX. Species causing infection in vertebrates other than man include: PLASMODIUM BERGHEI; PLASMODIUM CHABAUDI; P. vinckei, and PLASMODIUM YOELII in rodents; P. brasilianum, PLASMODIUM CYNOMOLGI; and PLASMODIUM KNOWLESI in monkeys; and PLASMODIUM GALLINACEUM in chickens.Tetraoxanes: Compounds with two peroxide groups, that is, two pairs of adjacent OXYGEN atoms. They may have activity against PLASMODIUM similar to the ARTEMISININS.Drug Combinations: Single preparations containing two or more active agents, for the purpose of their concurrent administration as a fixed dose mixture.Proguanil: A biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.Amodiaquine: A 4-aminoquinoline compound with anti-inflammatory properties.Parasitemia: The presence of parasites (especially malarial parasites) in the blood. (Dorland, 27th ed)Self Medication: The self administration of medication not prescribed by a physician or in a manner not directed by a physician.Tanzania: A republic in eastern Africa, south of UGANDA and north of MOZAMBIQUE. Its capital is Dar es Salaam. It was formed in 1964 by a merger of the countries of TANGANYIKA and ZANZIBAR.Plasmodium berghei: A protozoan parasite of rodents transmitted by the mosquito Anopheles dureni.QuinolinesEthanolamines: AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.Trophozoites: Cells or feeding stage in the life cycle of sporozoan protozoa. In the malarial parasite, the trophozoite develops from the MEROZOITE and then splits into the SCHIZONT. Trophozoites that are left over from cell division can go on to form gametocytes.Blackwater Fever: A complication of MALARIA, FALCIPARUM characterized by the passage of dark red to black urine.Spiro Compounds: A group of compounds consisting in part of two rings sharing one atom (usually a carbon) in common.Dosage Forms: Completed forms of the pharmaceutical preparation in which prescribed doses of medication are included. They are designed to resist action by gastric fluids, prevent vomiting and nausea, reduce or alleviate the undesirable taste and smells associated with oral administration, achieve a high concentration of drug at target site, or produce a delayed or long-acting drug effect.Peroxides: A group of compounds that contain a bivalent O-O group, i.e., the oxygen atoms are univalent. They can either be inorganic or organic in nature. Such compounds release atomic (nascent) oxygen readily. Thus they are strong oxidizing agents and fire hazards when in contact with combustible materials, especially under high-temperature conditions. The chief industrial uses of peroxides are as oxidizing agents, bleaching agents, and initiators of polymerization. (From Hawley's Condensed Chemical Dictionary, 11th ed)Primaquine: An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404)Inhibitory Concentration 50: 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.Protozoan Proteins: Proteins found in any species of protozoan.Hydroxychloroquine: A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970)Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.Dapsone: A sulfone active against a wide range of bacteria but mainly employed for its actions against MYCOBACTERIUM LEPRAE. Its mechanism of action is probably similar to that of the SULFONAMIDES which involves inhibition of folic acid synthesis in susceptible organisms. It is also used with PYRIMETHAMINE in the treatment of malaria. (From Martindale, The Extra Pharmacopoeia, 30th ed, p157-8)Erythrocytes: Red blood cells. Mature erythrocytes are non-nucleated, biconcave disks containing HEMOGLOBIN whose function is to transport OXYGEN.Hemeproteins: Proteins that contain an iron-porphyrin, or heme, prosthetic group resembling that of hemoglobin. (From Lehninger, Principles of Biochemistry, 1982, p480)Drug Discovery: The process of finding chemicals for potential therapeutic use.Asia, Southeastern: The geographical area of Asia comprising BORNEO; BRUNEI; CAMBODIA; INDONESIA; LAOS; MALAYSIA; the MEKONG VALLEY; MYANMAR (formerly Burma), the PHILIPPINES; SINGAPORE; THAILAND; and VIETNAM.Folic Acid Antagonists: Inhibitors of the enzyme, dihydrofolate reductase (TETRAHYDROFOLATE DEHYDROGENASE), which converts dihydrofolate (FH2) to tetrahydrofolate (FH4). They are frequently used in cancer chemotherapy. (From AMA, Drug Evaluations Annual, 1994, p2033)Fever: An abnormal elevation of body temperature, usually as a result of a pathologic process.Drug Evaluation, Preclinical: Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.CambodiaParasites: 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.Case Management: A traditional term for all the activities which a physician or other health care professional normally performs to insure the coordination of the medical services required by a patient. It also, when used in connection with managed care, covers all the activities of evaluating the patient, planning treatment, referral, and follow-up so that care is continuous and comprehensive and payment for the care is obtained. (From Slee & Slee, Health Care Terms, 2nd ed)Drug Therapy, Combination: Therapy with two or more separate preparations given for a combined effect.Nigeria: A republic in western Africa, south of NIGER between BENIN and CAMEROON. Its capital is Abuja.Sudan: A country in northeastern Africa. The capital is Khartoum.Kenya: A republic in eastern Africa, south of ETHIOPIA, west of SOMALIA with TANZANIA to its south, and coastline on the Indian Ocean. Its capital is Nairobi.Uganda: A republic in eastern Africa, south of SUDAN and west of KENYA. Its capital is Kampala.Aminoquinolines: Quinolines substituted in any position by one or more amino groups.Malaria, Vivax: Malaria caused by PLASMODIUM VIVAX. This form of malaria is less severe than MALARIA, FALCIPARUM, but there is a higher probability for relapses to occur. Febrile paroxysms often occur every other day.Pregnancy Complications, Parasitic: The co-occurrence of pregnancy and parasitic diseases. The parasitic infection may precede or follow FERTILIZATION.Plasmodium vivax: A protozoan parasite that causes vivax malaria (MALARIA, VIVAX). This species is found almost everywhere malaria is endemic and is the only one that has a range extending into the temperate regions.NaphthyridinesTablets: Solid dosage forms, of varying weight, size, and shape, which may be molded or compressed, and which contain a medicinal substance in pure or diluted form. (Dorland, 28th ed)Life Cycle Stages: The continuous sequence of changes undergone by living organisms during the post-embryonic developmental process, such as metamorphosis in insects and amphibians. This includes the developmental stages of apicomplexans such as the malarial parasite, PLASMODIUM FALCIPARUM.Thailand: Formerly known as Siam, this is a Southeast Asian nation at the center of the Indochina peninsula. Bangkok is the capital city.Drug Resistance, Multiple: Simultaneous resistance to several structurally and functionally distinct drugs.Tetrahydrofolate Dehydrogenase: An enzyme of the oxidoreductase class that catalyzes the reaction 7,8-dihyrofolate and NADPH to yield 5,6,7,8-tetrahydrofolate and NADPH+, producing reduced folate for amino acid metabolism, purine ring synthesis, and the formation of deoxythymidine monophosphate. Methotrexate and other folic acid antagonists used as chemotherapeutic drugs act by inhibiting this enzyme. (Dorland, 27th ed) EC 1.5.1.3.Lupus Erythematosus, Systemic: A chronic, relapsing, inflammatory, and often febrile multisystemic disorder of connective tissue, characterized principally by involvement of the skin, joints, kidneys, and serosal membranes. It is of unknown etiology, but is thought to represent a failure of the regulatory mechanisms of the autoimmune system. The disease is marked by a wide range of system dysfunctions, an elevated erythrocyte sedimentation rate, and the formation of LE cells in the blood or bone marrow.Heme: The color-furnishing portion of hemoglobin. It is found free in tissues and as the prosthetic group in many hemeproteins.Molecular Structure: The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.Membrane Transport Proteins: Membrane proteins whose primary function is to facilitate the transport of molecules across a biological membrane. Included in this broad category are proteins involved in active transport (BIOLOGICAL TRANSPORT, ACTIVE), facilitated transport and ION CHANNELS.Health Policy: Decisions, usually developed by government policymakers, for determining present and future objectives pertaining to the health care system.AfricaStructure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Hemoglobins: The oxygen-carrying proteins of ERYTHROCYTES. They are found in all vertebrates and some invertebrates. The number of globin subunits in the hemoglobin quaternary structure differs between species. Structures range from monomeric to a variety of multimeric arrangements.Drug Design: The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.DNA, Protozoan: Deoxyribonucleic acid that makes up the genetic material of protozoa.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Cross-Sectional Studies: Studies in which the presence or absence of disease or other health-related variables are determined in each member of the study population or in a representative sample at one particular time. This contrasts with LONGITUDINAL STUDIES which are followed over a period of time.Anti-Bacterial Agents: Substances that reduce the growth or reproduction of BACTERIA.Treatment Outcome: Evaluation undertaken to assess the results or consequences of management and procedures used in combating disease in order to determine the efficacy, effectiveness, safety, and practicability of these interventions in individual cases or series.
Malaria prophylaxis using azithromycin: a double-blind, placebo-controlled trial in Irian Jaya, Indonesia. (1/4748)
New drugs are needed for preventing drug-resistant Plasmodium falciparum malaria. The prophylactic efficacy of azithromycin against P. falciparum in malaria-immune Kenyans was 83%. We conducted a double-blind, placebo-controlled trial to determine the prophylactic efficacy of azithromycin against multidrug-resistant P. falciparum malaria and chloroquine-resistant Plasmodium vivax malaria in Indonesian adults with limited immunity. After radical cure therapy, 300 randomized subjects received azithromycin (148 subjects, 750-mg loading dose followed by 250 mg/d), placebo (77), or doxycycline (75, 100 mg/d). The end point was slide-proven parasitemia. There were 58 P. falciparum and 29 P. vivax prophylaxis failures over 20 weeks. Using incidence rates, the protective efficacy of azithromycin relative to placebo was 71.6% (95% confidence interval [CI], 50.3-83.8) against P. falciparum malaria and 98.9% (95% CI, 93.1-99.9) against P. vivax malaria. Corresponding figures for doxycycline were 96.3% (95% CI, 85.4-99.6) and 98% (95% CI, 88.0-99.9), respectively. Daily azithromycin offered excellent protection against P. vivax malaria but modest protection against P. falciparum malaria. (+info)8-Aminoquinolines active against blood stage Plasmodium falciparum in vitro inhibit hematin polymerization. (2/4748)
From the Walter Reed Army Institute of Research (WRAIR) inventory, thirteen 8-aminoquinoline analogs of primaquine were selected for screening against a panel of seven Plasmodium falciparum clones and isolates. Six of the 13 8-aminoquinolines had average 50% inhibitory concentrations between 50 and 100 nM against these P. falciparum clones and were thus an order of magnitude more potent than primaquine. However, excluding chloroquine-resistant clones and isolates, these 8-aminoquinolines were all an order of magnitude less potent than chloroquine. None of the 8-aminoquinolines was cross resistant with either chloroquine or mefloquine. In contrast to the inactive primaquine prototype, 8 of the 13 8-aminoquinolines inhibited hematin polymerization more efficiently than did chloroquine. Although alkoxy or aryloxy substituents at position 5 uniquely endowed these 13 8-aminoquinolines with impressive schizontocidal activity, the structural specificity of inhibition of both parasite growth and hematin polymerization was low. (+info)Alternative oxidase inhibitors potentiate the activity of atovaquone against Plasmodium falciparum. (3/4748)
Recent evidence suggests that the malaria parasite Plasmodium falciparum utilizes a branched respiratory pathway including both a cytochrome chain and an alternative oxidase. This branched respiratory pathway model has been used as a basis for examining the mechanism of action of two antimalarial agents, atovaquone and proguanil. In polarographic assays, atovaquone immediately reduced the parasite oxygen consumption rate in a concentration-dependent manner. This is consistent with its previously described role as an inhibitor of the cytochrome bc1 complex. Atovaquone maximally inhibited the rate of P. falciparum oxygen consumption by 73% +/- 10%. At all atovaquone concentrations tested, the addition of the alternative oxidase inhibitor, salicylhydroxamic acid, resulted in a further decrease in the rate of parasite oxygen consumption. At the highest concentrations of atovaquone tested, the activities of salicylhydroxamic acid and atovaquone appear to overlap, suggesting that at these concentrations, atovaquone partially inhibits the alternative oxidase as well as the cytochrome chain. Drug interaction studies with atovaquone and salicylhydroxamic acid indicate atovaquone's activity against P. falciparum in vitro is potentiated by this alternative oxidase inhibitor, with a sum fractional inhibitory concentration of 0.6. Propyl gallate, another alternative oxidase inhibitor, also potentiated atovaquone's activity, with a sum fractional inhibitory concentration of 0.7. Proguanil, which potentiates atovaquone activity in vitro and in vivo, had a small effect on parasite oxygen consumption in polarographic assays when used alone or in the presence of atovaquone or salicylhydroxamic acid. This suggests that proguanil does not potentiate atovaquone by direct inhibition of either branch of the parasite respiratory chain. (+info)Declining concentrations of dihydroartemisinin in plasma during 5-day oral treatment with artesunate for Falciparum malaria. (4/4748)
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)Comparison of in vivo and in vitro tests of resistance in patients treated with chloroquine in Yaounde, Cameroon. (5/4748)
The usefulness of an isotopic in vitro assay in the field was evaluated by comparing its results with the therapeutic response determined by the simplified WHO in vivo test in symptomatic Cameroonian patients treated with chloroquine. Of the 117 enrolled patients, 102 (87%) completed the 14-day follow-up, and 95 isolates obtained from these patients (46 children, 49 adults) yielded an interpretable in vitro test. A total of 57 of 95 patients (60%; 28 children and 29 adults) had an adequate clinical response with negative smears (n = 46) or with an asymptomatic parasitaemia (n = 11) on day 7 and/or day 14. The geometric mean 50% inhibitory concentration of the isolates obtained from these patients was 63.3 nmol/l. Late and early treatment failure was observed in 29 (30.5%) and 9 (9.5%) patients, respectively. The geometric mean 50% inhibitory concentrations of the corresponding isolates were 173 nmol/l and 302 nmol/l. Among the patients responding with late and early treatment failure, five isolates and one isolate, respectively, yielded a discordant result (in vivo resistance and in vitro sensitivity). The sensitivity, specificity, and predictive value of the in vitro test to detect chloroquine-sensitive cases was 67%, 84% and 86%, respectively. There was moderate concordance between the in vitro and in vivo tests (kappa value = 0.48). The in vitro assay agrees relatively well with the therapeutic response and excludes several host factors that influence the results of the in vivo test. However, in view of some discordant results, the in vitro test cannot substitute for in vivo data on therapeutic efficacy. The only reliable definition of "resistance" in malaria parasites is based on clinical and parasitological response in symptomatic patients, and the in vivo test provides the standard method to determine drug sensitivity or resistance as well as to guide national drug policies. (+info)Intrinsic efficacy of proguanil against falciparum and vivax malaria independent of the metabolite cycloguanil. (6/4748)
Mutations in human CYP2C19 and parasite dihydrofolate reductase (dhfr) genes, related to poor metabolism of proguanil and resistance to cycloguanil, respectively, have both been assumed to be associated with poor antimalarial effect by proguanil. To study this, 95 subjects with uncomplicated Plasmodium falciparum or Plasmodium vivax infections in Vanuatu received proguanil treatment for 3 days (adult relative dose of 300-500 mg/day) and were followed up for 28 days. A similarly high antimalarial efficacy against both infections was observed in 62 patients with CYP2C19-related poor metabolizer genotype and in 33 with extensive metabolizer genotype, even though blood cycloguanil was significantly more often detected in those with extensive metabolizer genotype than in those with poor metabolizer genotype. All 28 P. falciparum isolates had two dhfr mutations (residues 59 and 108), suggesting moderate resistance to cycloguanil. The results suggest that the parent compound proguanil has significant intrinsic efficacy against falciparum and vivax malaria independent of the metabolite cycloguanil. (+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. (7/4748)
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. (8/4748)
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)DrugsArtemisininCompoundsDrugEfficacyRevealed antimalarial activityAssociated with the antimalarial drugVivoTypes of antimalarialsAtovaquoneCompoundMedicationsMalaria controlPotentSystemic Lupus ErythemDerivativesAnaloguesAnticancer PropertiesRheumatoid arthritisSearchVivaxCentersPiperaquineAnti-inflammatoryAmodiaquineCounterfeitTreatmentQuinacrinePotentialPyrimethamineEffectiveTherapeuticLupusInjectableResearchDevelopmentChemicalPatientsInhibitorsStructuresAntineoplastic
- Antimalarial drugs are used for the treatment and prevention of malaria infection. (uptodate.com)
- Most antimalarial drugs target the erythrocytic stage of malaria infection, which is the phase of infection that causes symptomatic illness ( figure 1 ). (uptodate.com)
- The extent of preerythrocytic (hepatic stage) activity for most antimalarial drugs is not well characterized. (uptodate.com)
- The mechanisms of action, resistance, and toxicities of antimalarial drugs will be reviewed here. (uptodate.com)
- Antimalarial Drugs are used for treating and curing the malarial disease by fighting with plasmodium tissues. (lexicarepharma.com)
- All these Antimalarial Drugs are made under strict norms and actions by our skilled workers and team member. (lexicarepharma.com)
- Therefore, there is an urgent need to develop new antimalarial clinical candidate drugs. (edu.au)
- She wanted to determine whether antimalarial drugs, particularly quinoline antimalarials, caused cardiovascular side effects such as prolongation of the QT interval on the electrocardiogram. (ox.ac.uk)
- The question of cardiotoxic effects of antimalarial drugs is very relevant to clinical practice on a global scale, so Ilsa found this project very stimulating. (ox.ac.uk)
- Managing the largest portfolio of antimalarial R&D projects ever assembled, of over 65 projects, we have nine new drugs in clinical development addressing unmet medical needs in malaria, including medicines for children, pregnant women and relapsing malaria, and drugs that could support the elimination and eradication of malaria. (devfinance.net)
- The largest genome-wide association study to date of the malaria parasite Plasmodium falciparum unveils a complex genetic architecture that enables the parasite to develop resistance to our most effective antimalarial drug, artemisinin. (science20.com)
- The scientists, who analyzed blood samples from 1,241 malaria patients in 10 countries across Asia and Africa, found resistance to the world's most effective antimalarial drug, artemisinin, is now widespread in Southeast Asia. (irrawaddy.com)
- It may still be possible to prevent the spread of artemisinin-resistant malaria parasites across Asia and then to Africa by eliminating them, but that window of opportunity is closing fast," said Nicholas White, a professor of tropical medicine at Oxford University who led the research and is chair of the Worldwide Antimalarial Resistance Network. (irrawaddy.com)
- Today, we are also reaping the benefits of extensive screening efforts, with many novel antimalarial compounds progressing through the portfolio. (devfinance.net)
- No new class of antimalarial drug has entered the market in the last 15 years resulting in the emergence of resistance against all clinically used drug classes. (edu.au)
- This project will utilise medicinal chemistry to optimise the antimalarial activity of recently identified classes of drug-like small molecules to achieve efficacy in laboratory models of malaria. (edu.au)
- MMV, a leading product development partnership (PDP) in the field of antimalarial drug research, is committed to playing its part in the fight against malaria. (devfinance.net)
- if used, monitor closely for antimalarial efficacy and lumefantrine toxicity. (medscape.com)
- To assess the short-term efficacy and toxicity of antimalarials for the treatment of rheumatoid arthritis (RA). (cochrane.org)
- Antimalarial agents can treat certain photosensitive eruptions, including those of solar urticaria, but their efficacy is unpredictable. (medscape.com)
- Antimalarials are used to treat certain photosensitive eruptions, including solar urticaria, but their efficacy is unpredictable. (medscape.com)
- Global database on antimalarial drug efficacy and https://www.who.int/malaria/areas/drug_resistance/drug_efficacy_database/en THERAPEUTIC EFFICACY STUDY DATA MOLECULAR MARKERS OF ANTIMALARIAL DRUG RESISTANCE DATA MALARIA THREATS MAP GLOBAL REPORT ON ANTIMALARIAL DRUG EFFICACY AND DRUG RESISTANCE UPDATES ON DRUG EFFICACY AND RESISTANCE KEY DOCUMENTS The database includes data on TES conducted in accordance with the WHO standard protocol for monitoring antimalarial drug efficacy. (schule.de)
- Scientists specialized in natural substances, investigating the chemical structure and properties of the phloeodictines as part of the French malaria control research programme Pal +, have revealed antimalarial activity among phloeodictines extracted from the reef sponge Oceanapia fistulosa. (innovations-report.com)
- According to the New York Times FDA is advising the public about neurologic and psychiatric side effects associated with the antimalarial drug mefloquine hydrochloride. (digitaljournal.com)
- B. orellona seed extracts showed moderate in vitro and in vivo antimalarial activity. (greenmedinfo.com)
- Other investigations are planned to seek confirmation of these results and find out accurate information on this antimalarial activity in vivo, using infected rodent models, and to attempt to unravel phloeodictines' action mechanism. (innovations-report.com)
- 2016) " Metabolite identification of the antimalarial piperaquine in vivo using liquid chromatography-high resolution mass spectrometry in combination with multiple data-mining tools in tandem ," doi: 10.1002/bmc.3689. (thermofisher.com)
- The antenatal clinics cards were checked in order to record the types of antimalarials prescribed during pregnancy according to gestational age. (hindawi.com)
- With the new breakthrough the scientists have utilized nanotechnology in order to improve the delivery of an existing antimalarial drug called atovaquone. (digitaljournal.com)
- The authors found that the antimalarial drug atovaquone, which inhibits the mitochondrial protein cytochrome b - as well as other types of cytochrome b inhibitor drug - could kill parasites in a mosquito host. (bioedonline.org)
- Recently, by using a bioassay-guided fractionation, an antimalarial compound, Gancidin-W, has been discovered from these bacteria. (hindawi.com)
- Earlier this month, Indian regulatory authorities granted conditional approval to the country's first homegrown drug, a malaria-fighting pill that combines a new synthetic form of artemisinin with an older antimalarial compound called piperaquine. (nature.com)
- Of these, four (M1-M4) are major metabolites resulting from N-oxidation and/or carboxylation of the antimalarial compound. (thermofisher.com)
- Antimalarial medications, also known as antimalarials, are designed to prevent or cure malaria. (wikipedia.org)
- Packaging materials for counterfeit antimalarial medications have been confiscated in Nigeria. (medicalnewstoday.com)
- Treatment includes antimalarial , antiseizure and anti inflammatory medications. (reportbuyer.com)
- Under the terms of the agreement, MMV will provide funding in order to advance the development of azithromycin-based treatments that may address resistance and side effects associated with existing antimalarial medications. (webwire.com)
- What are antimalarial medications? (dermnetnz.org)
- How do antimalarial medications work? (dermnetnz.org)
- Antimalarial medications prevent platelet aggregation and act as prostaglandin antagonists due to inhibition of phospholipase A2 . (dermnetnz.org)
- By deploying different antimalarial therapies simultaneously - including non-artemisinin-based therapies - national malaria control programs in Africa should be able to slow down the spread of artemisinin-resistant parasites when they are imported into the continent. (eurekalert.org)
- NUS scientists discovered that a combination of artemisinin, which is a potent antimalarial drug, and aminolaevulinic acid, which is a photosensitizer, could kill colorectal cancer cells and suppress tumor growth more effectively than administering artemisinin alone. (photonics.com)
- A never-ending search for more potent and less toxic antimalarials has continued and will undoubtedly do so until this scourge is no longer of importance. (ku.edu)
- To investigate whether antimalarials decrease the risk of cancer in systemic lupus erythematosus (SLE). (bmj.com)
- Artemisinin derivatives are the best antimalarials, experts say. (medicalnewstoday.com)
- China Cooperative Research Group on Qinghaosu and Its Derivatives as Antimalarials. (springer.com)
- Ferroquine and its derivatives: new generation of antimalarial agents. (sigmaaldrich.com)
- Not only ferroquine, but also its derivatives have shown promising potential as antimalarials of clinical interest. (sigmaaldrich.com)
- Presently, much research is dedicated to the development of ferroquine derivatives as safe alternatives to antimalarial chemotherapy. (sigmaaldrich.com)
- The researchers measured certain properties of several antimalarial chemical structures called 4-aminoquinoline analogues, including their so-called log P and pKa values. (westminster.ac.uk)
- Scientists have shown that the anticancer properties of artemisinin, an antimalarial drug that is also a promising alternative cancer treatment, could be enhanced potentially tenfold when used with the photosensitizer aminolaevulinic acid (ALA). When exposed to light, ALA leads to the generation of free radicals that can kill cells. (photonics.com)
- Antimalarials have been used for the treatment of rheumatoid arthritis (RA) for several decades. (cochrane.org)
- Thus, the search for new promising antimalarials continues, however, the battle against malaria is far from over. (sigmaaldrich.com)
- Structures of clinical antimalarials for vivax radical cure. (nih.gov)
- Request for injectable antimalarial was significantly more among educated patients and those attending private clinics and health centers. (who.int)
- 2006) " Characterization of human urinary metabolites of the antimalarial piperaquine ," Drug Metabolism and Disposition 34(12) (pp. 2011-2019). (thermofisher.com)
- Antimalarials, which have a broad array of anti-inflammatory, immunomodulatory, and antithrombotic effects, now are recommended for all patients with lupus and have demonstrated benefits in reducing disease flares and improving survival, the authors wrote. (medpagetoday.com)
- Results: Of the 300 households visited 25 (8.3) were found to store antimalarials.The most commonly stored antimalarials were amodiaquine (30.8) and quinine (34.6). (who.int)
- The researchers set out to determine how prevalent counterfeit and substandard antimalarials were in Africa. (medicalnewstoday.com)
- substandard and counterfeit antimalarials and the availability of artemisinin monotherapies threaten to lead to the spread of drug resistance in Africa. (medicalnewstoday.com)
- This led the World Health Organization (WHO) to recommend a package of affordable interventions including the use of the insecticide-treated nets (ITNs), the intermittent presumptive treatment (IPT) with sulfadoxine-pyrimethamine (SP), and the effective case management of clinical malaria with recommended antimalarials. (hindawi.com)
- But the nightmare we all want to avoid is the establishment of artemisinin resistance in Africa, where hundreds of millions of individuals rely on artemisinin-based therapies as their first-line antimalarial treatment. (eurekalert.org)
- This provides rapid access to critical information associated with resistance to antimalarials at the point of care, avoiding the time, expense, and effort of having the sample sent to a central laboratory and allowing clinicians to quickly re-evaluate treatment options. (news-medical.net)
- Research will focus on macrolide antibiotics, based on azithromycin, which may have promise as an antimalarial treatment. (webwire.com)
- Age at diagnosis, gender, treatment with azathioprine, cyclophosphamide and methotrexate, smoking, Systemic Lupus International Collaborating Clinics (SLICC) Damage Index 6 months after diagnosis, year of diagnosis and treatment with antimalarials were entered as independent variables. (bmj.com)
- Quinacrine "is an underutilized antimalarial. (mdedge.com)
- But the potential impact of increasing antimalarial resistance could be devastating. (www.nhs.uk)
- A team of scientists from the University of Cape Town's (UCT) Drug Discovery and Development Centre (H3-D) in South Africa, led by Prof. Kelly Chibale then scrutinised and explored the antimalarial potential of the series further. (innovations-report.com)
- Potential antimalarials. (wikipedia.org)
- Oral lichenoid reactions during antimalarial prophylaxis with sulphadoxine-pyrimethamine combination" Southeast Asian Journal of Tropical Medicine and Public Health Vol. 20 Iss. (bepress.com)
- But a fourth combo drug - a newer antimalarial that combines chlorproguanil, dapsone and artesunate - proved only around 85% effective, and was removed from the study after its maker, London-based GlaxoSmithKline, pulled it from the market in 2008 because of adverse effects. (nature.com)
- Drug resistance has led to the combination of quinolines with other classes of antimalarials resulting in enhanced therapeutic outcomes. (mdpi.com)
- antimalarials also help to prevent lupus flares and have been associated with reduced morbidity and mortality in SLE patients followed in observational trials. (medscape.com)
- Irrational use of injectable antimalarial is commonplace in developing countries. (who.int)
- This descriptive survey was conducted to determine the prevalence of injectable antimalarials use and factors related to this practice in selected health facilities in Ilorin, Nigeria. (who.int)
- Awareness of both oral and injectable antimalarials is fairly high among the respondents. (who.int)
- Injectable antimalarial was the most preferred form by the patients. (who.int)
- Among respondents 90.3% had ever used injectable antimalarial. (who.int)
- Use of injectable antimalarial irrespective of clinical indications is common practice. (who.int)
- Qinghaosu Antimalarial Coordinating Research Group. (springer.com)
- New research published in Frontiers in Bioengineering and Biotechnology , "Stable Production of the Antimalarial Drug Artemisinin in the Moss Physcomitrella patens ", demonstrates that artemisinin can be rapidly produced by genetically engineered moss at an industrial scale. (news-medical.net)
- Research released in anticipation of World Malaria Day finds that plants in East Africa with promising antimalarial qualities-ones that have treated malaria symptoms in the region's communities for hundreds of years-are at risk of extinction. (biologynews.net)
- A new book by researchers at the World Agroforestry Centre (ICRAF) and the Kenya Medical Research Institute (KEMRI), Common Antimalarial Trees and Shrubs of East Africa, provides a detailed assessment of 22 of the region's malaria-fighting trees and shrubs. (biologynews.net)
- This collaboration with GSK capitalizes on the company s research excellence and helps meet MMV s objective of developing antimalarials that will retain their usefulness longer and enable us to help vulnerable populations at risk from malaria. (webwire.com)
- Finally, efforts have been made to discuss the current challenges and future perspectives of ferroquine-based antimalarial drug development. (sigmaaldrich.com)
- suggest a way forward for the development of next-generation antimalarial bed nets. (bioedonline.org)
- Improper drug storage and rampant selfmedication are some of the factors that may contribute to an increase in the development of drug resistance by malaria parasites towards antimalarials. (who.int)
- It is practical to consider antimalarials by chemical structure since this is associated with important properties of each drug, such as mechanism of action. (wikipedia.org)
- Antimalarials are a type of antiparasitic chemical agent, often naturally derived, that can be used to treat or to prevent malaria. (lgcstandards.com)
- The U.S. FDA has issued a warning to patients and healthcare professionals about an antimalarial drug due to serious psychiatric and nerve side effects. (digitaljournal.com)
- Kaplan-Meier cancer-free survival curves for patients treated and not treated with antimalarials were compared. (bmj.com)
- 156 (66%) patients had ever received antimalarials. (bmj.com)
- This study launches the hypothesis of a protective action of antimalarials against cancer in patients with SLE. (bmj.com)
- How do antimalarials and protease inhibitors (PIs) interact? (medscape.com)
- 6 - 8 Significant effort has been directed towards developing inhibitors of these proteases to discover new antimalarials. (pubmedcentralcanada.ca)
- Structures of clinical antimalarials for asexual blood stages. (nih.gov)
- Recent studies suggest that antimalarials have antineoplastic properties. (bmj.com)