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Academic literature on the topic 'Antimalarials – Therapeutic use'
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Journal articles on the topic "Antimalarials – Therapeutic use"
1
Duncan, MR, and HA Capell. "The use of antimalarials in combination with other disease modifying agents in RA – the British experience." Lupus 5, no. 1_suppl (1996): 50–58. http://dx.doi.org/10.1177/0961203396005001121.
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Antimalarial drugs are effective disease modifying agents in RA with a low incidence of serious toxic effects. Recently, combinations of second-line agents have been used in RA in attempts to treat patients with no response to a number of single agents, or suboptimal response to a single agent. Combinations of drugs have been selected for maximum efficacy and minimum toxicity, but clinical trials are difficult to design and interpret. In particular, ensuring adequate power to detect small differences in response poses a major problem. Antimalarials are an attractive choice for combination therapy due to their efficacy, mechanisms of action and toxicity profile. In this review, the evidence for the use of antimalarials in combination in RA is examined. No advantage has been shown in combining antimalarials with gold, penicillamine or sulphasalazine compared with monotherapeutic regimens. There is some evidence to suggest a beneficial combination of antimalarials with methotrexate, but this is as yet inconclusive. Open non-randomised uncontrolled studies have shown that antimalarials combined with cytotoxic agents are effective but highly toxic. The authors conclude that there is little good evidence to support the introduction of combination second-line drug therapy for RA into widespread therapeutic use.
2
Tang, Yu-Qing, Qian Ye, He Huang, and Wei-Yi Zheng. "An Overview of Available Antimalarials: Discovery, Mode of Action and Drug Resistance." Current Molecular Medicine 20, no. 8 (2020): 583–92. http://dx.doi.org/10.2174/1566524020666200207123253.
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: Malaria is one of the three most deadly infectious diseases in the world and seriously endangers human health and life. To reduce the public health burden of this disease, scientists have focused on the discovery and development of effective antimalarial drugs, from quinine and chloroquine to antifolates and artemisinin and its derivatives, which all play a profound role in the treatment of malaria. However, drugresistant strains of Plasmodium falciparum have emerged due to frequent use of antimalarials and have become increasingly resistant to existing antimalarial drugs, causing disastrous consequences in the world. In particular, artemisinin resistance is of greatest concern which was reported in 2008. Resistance to artenisinins has been a major obstacle for malaria control, and current efforts to curb artemisinin resistance have not been successful. Based on the current situation, it is urgent to develop more effective new antimalarials with distinct targets from conventional antimalarials in the world, which could facilitate to minimize the phenomenon of drug resistance. This review aims to summarize different kinds of antimalarial therapeutic efficacy, mechanisms of action and resistance, and proposes new solutions aiming towards further improvement of malaria elimination.
3
Ambroise-Thomas, Pierre. "THE TRAGEDY CAUSED BY FAKE ANTIMALARIAL DRUGS." Mediterranean Journal of Hematology and Infectious Diseases 4, no. 1 (2012): e2012027. http://dx.doi.org/10.4084/mjhid.2012.027.
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Counterfeit antimalarials (mainly artemisinin derivatives) is a crucial health problem in developing countries, particularly in Africa. The illegal production, sale and distribution of fake drugs is a huge market evaluated to several billion of dollars and represents more than 50% of the pharmaceutical market in several African countries. Fake drugs have led to a very great number of deaths from untreated malaria or fatality provoked by toxic ingredients. These fake medicines increase the risk of artemisinin resistance developed by the use of sub therapeutic dosages of antimalarials. Tackling this criminal traffic is the objective of an international programme created by WHO and involves the international police and custom organizations like INTERPOL. Several very important and encouraging results have been obtained, but the problem will be completely solved if genuine antimalarials, free-of-charge, are handed-over to populations in sub Sahara African countries.
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Piedade, Rita, Stefanie Traub, Andreas Bitter, et al. "Carboxymefloquine, the Major Metabolite of the Antimalarial Drug Mefloquine, Induces Drug-Metabolizing Enzyme and Transporter Expression by Activation of Pregnane X Receptor." Antimicrobial Agents and Chemotherapy 59, no. 1 (2014): 96–104. http://dx.doi.org/10.1128/aac.04140-14.
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ABSTRACTMalaria patients are frequently coinfected with HIV and mycobacteria causing tuberculosis, which increases the use of coadministered drugs and thereby enhances the risk of pharmacokinetic drug-drug interactions. Activation of the pregnane X receptor (PXR) by xenobiotics, which include many drugs, induces drug metabolism and transport, thereby resulting in possible attenuation or loss of the therapeutic responses to the drugs being coadministered. While several artemisinin-type antimalarial drugs have been shown to activate PXR, data on nonartemisinin-type antimalarials are still missing. Therefore, this study aimed to elucidate the potential of nonartemisinin antimalarial drugs and drug metabolites to activate PXR. We screened 16 clinically used antimalarial drugs and six major drug metabolites for binding to PXR using the two-hybrid PXR ligand binding domain assembly assay; this identified carboxymefloquine, the major and pharmacologically inactive metabolite of the antimalarial drug mefloquine, as a potential PXR ligand. Two-hybrid PXR-coactivator and -corepressor interaction assays and PXR-dependent promoter reporter gene assays confirmed carboxymefloquine to be a novel PXR agonist which specifically activated the human receptor. In the PXR-expressing intestinal LS174T cells and in primary human hepatocytes, carboxymefloquine induced the expression of drug-metabolizing enzymes and transporters on the mRNA and protein levels. The crucial role of PXR for the carboxymefloquine-dependent induction of gene expression was confirmed by small interfering RNA (siRNA)-mediated knockdown of the receptor. Thus, the clinical use of mefloquine may result in pharmacokinetic drug-drug interactions by means of its metabolite carboxymefloquine. Whether thesein vitrofindings are ofin vivorelevance has to be addressed in future clinical drug-drug interaction studies.
5
Stevens, David M., Rachael M. Crist, and Stephan T. Stern. "Nanomedicine Reformulation of Chloroquine and Hydroxychloroquine." Molecules 26, no. 1 (2020): 175. http://dx.doi.org/10.3390/molecules26010175.
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The chloroquine family of antimalarials has a long history of use, spanning many decades. Despite this extensive clinical experience, novel applications, including use in autoimmune disorders, infectious disease, and cancer, have only recently been identified. While short term use of chloroquine or hydroxychloroquine is safe at traditional therapeutic doses in patients without predisposing conditions, administration of higher doses and for longer durations are associated with toxicity, including retinotoxicity. Additional liabilities of these medications include pharmacokinetic profiles that require extended dosing to achieve therapeutic tissue concentrations. To improve chloroquine therapy, researchers have turned toward nanomedicine reformulation of chloroquine and hydroxychloroquine to increase exposure of target tissues relative to off-target tissues, thereby improving the therapeutic index. This review highlights these reformulation efforts to date, identifying issues in experimental designs leading to ambiguity regarding the nanoformulation improvements and lack of thorough pharmacokinetics and safety evaluation. Gaps in our current understanding of these formulations, as well as recommendations for future formulation efforts, are presented.
6
Burns, Amy L., Madeline G. Dans, Juan M. Balbin, et al. "Targeting malaria parasite invasion of red blood cells as an antimalarial strategy." FEMS Microbiology Reviews 43, no. 3 (2019): 223–38. http://dx.doi.org/10.1093/femsre/fuz005.
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AbstractPlasmodium spp. parasites that cause malaria disease remain a significant global-health burden. With the spread of parasites resistant to artemisinin combination therapies in Southeast Asia, there is a growing need to develop new antimalarials with novel targets. Invasion of the red blood cell by Plasmodium merozoites is essential for parasite survival and proliferation, thus representing an attractive target for therapeutic development. Red blood cell invasion requires a co-ordinated series of protein/protein interactions, protease cleavage events, intracellular signals, organelle release and engagement of an actin-myosin motor, which provide many potential targets for drug development. As these steps occur in the bloodstream, they are directly susceptible and exposed to drugs. A number of invasion inhibitors against a diverse range of parasite proteins involved in these different processes of invasion have been identified, with several showing potential to be optimised for improved drug-like properties. In this review, we discuss red blood cell invasion as a drug target and highlight a number of approaches for developing antimalarials with invasion inhibitory activity to use in future combination therapies.
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Kuhn, A., F. Ochsendorf, and G. Bonsmann. "Treatment of cutaneous lupus erythematosus." Lupus 19, no. 9 (2010): 1125–36. http://dx.doi.org/10.1177/0961203310370345.
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In patients with cutaneous lupus erythematosus (CLE) and mild skin involvement, local therapy consisting of topically applied pharmacological agents, e.g., topical/intralesional steroids, may be sufficient. Recent reports have also shown efficacy of topical calcineurin inhibitors in patients with CLE, particularly on the face. Special attention receives consistent sun protection through photoresistant clothing and application of light-shielding substances with highly potent chemical or physical UVA- and UVB-protective filters. These substances should be applied in sufficient amount (ca. 2 mg/cm2) at least 20—30 minutes before sun exposure in order to avoid induction and exacerbation of cutaneous lesions. The mainstay of treatment for disfiguring and widespread skin manifestations in patients with CLE, irrespective of the subtype of the disease, is antimalarial agents. Our understanding of the use of combinations of antimalarials and proper dosing according to the ideal bodyweight limits problems with toxicity. Further therapies, such as methotrexate, or retinoids, dapsone, mycophenolate mofetil, and thalidomide in selected cases, can be helpful for patients with resistant disease; however, side effects need to be taken into consideration. Recent advances in biotechnology resulted in the development of novel systemic agents, but randomized controlled trials are necessary for the approval of new therapeutic strategies in CLE. Lupus (2010) 19, 1125—1136.
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Kwofie, Samuel K., Emmanuel Broni, Bismark Dankwa, et al. "Review of Atypical Organometallic Compounds as Antimalarial Drugs." Journal of Chemistry 2020 (May 20, 2020): 1–9. http://dx.doi.org/10.1155/2020/9414093.
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Organometallic compounds are molecules that contain at least one metal-carbon bond. Due to resistance of the Plasmodium parasite to traditional organic antimalarials, the use of organometallic compounds has become widely adopted in antimalarial drug discovery. Ferroquine, which was developed due to the emergence of chloroquine resistance, is currently the most advanced organometallic antimalarial drug and has paved the way for the development of new organometallic antimalarials. In this review, a general overview of organometallic antimalarial compounds and their antimalarial activity in comparison to purely organic antimalarials are presented. Furthermore, recent developments in the field are discussed, and future applications of this emerging class of therapeutics in antimalarial drug discovery are suggested.
9
Ruwizhi, Ngonidzashe, and Blessing Atim Aderibigbe. "The Efficacy of Cholesterol-Based Carriers in Drug Delivery." Molecules 25, no. 18 (2020): 4330. http://dx.doi.org/10.3390/molecules25184330.
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Several researchers have reported the use of cholesterol-based carriers in drug delivery. The presence of cholesterol in cell membranes and its wide distribution in the body has led to it being used in preparing carriers for the delivery of a variety of therapeutic agents such as anticancer, antimalarials and antivirals. These cholesterol-based carriers were designed as micelles, nanoparticles, copolymers, liposomes, etc. and their routes of administration include oral, intravenous and transdermal. The biocompatibility, good bioavailability and biological activity of cholesterol-based carriers make them potent prodrugs. Several in vitro and in vivo studies revealed cholesterol-based carriers potentials in delivering bioactive agents. In this manuscript, a critical review of the efficacy of cholesterol-based carriers is reported.
10
Alsharif, Sahar H., Reda H. Saifaldeen, and Logain G. Alghanemi. "Successful treatment of granuloma faciale." International Journal of Research in Dermatology 7, no. 1 (2020): 129. http://dx.doi.org/10.18203/issn.2455-4529.intjresdermatol20205609.
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<p class="abstract">Granuloma faciale (GF) is a chronic condition characterized by asymptomatic erythematous plaque with prominent telangiectasia presenting usually over the face. Although the condition is benign, its treatment is often unsatisfactory. Therapeutic modalities that have been tried include topical steroids and topical tacrolimus sometimes enhanced with topical dapsone. Others include intralesional corticosteroids, antimalarials, isoniazid and pulsed-dye laser. We report a case of a 58 years old female with a 1 year history of a solitary slowly progressive plaque over the nose. Diagnosis of GF was made based on the histopathological findings. The patient was started on the combination of topical tacrolimus, intralesional corticosteroids injection and oral doxycycline for 3 months. The patient showed gradual improvement in 3 months without any side effects. This case supports previous papers of successful treatment of GF with topical tacrolimus. There was no recurrence at follow-up 18 months later. It also supports the use of combination therapy especially in resistant cases.</p>