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Malarone® (atovaquone/proguanil) is frequently used in malaria prophylaxis. Unfortunately, there are indications that certain anti-HIV agents may decrease atovaquone plasma levels by induction of atovaquone metabolism.. For travelling HIV patients, the clinical consequences of these possible drug drug interactions are serious, since a diminished exposure to the anti-malarial drug will result in suboptimal prophylaxis of malaria and potential development of drug resistant strains of Plasmodium falciparum.. The purpose of this study is to find out if HIV patients using HAART regimes with either lopinavir/ritonavir, atazanavir/ritonavir or efavirenz have lower atovaquone plasma levels than healthy volunteers after a single dose of atovaquone/proguanil. ...
Atovaquone is used as a fixed-dose combination with proguanil (Malarone) for treating children and adults with uncomplicated malaria or as chemoprophylaxis for preventing malaria in travellers. Indeed, in the USA, between 2009 and 2011, Malarone prescriptions accounted for 70% of all antimalarial pre-travel prescriptions. In 2013 the patent for Malarone will expire, potentially resulting in a wave of low-cost generics. Furthermore, the malaria scientific community has a number of antimalarial quinolones with a related pharmacophore to atovaquone at various stages of pre-clinical development. With this in mind, it is timely here to review the current knowledge of atovaquone, with the purpose of aiding the decision making of clinicians and drug developers involved in the future use of atovaquone generics or atovaquone derivatives.. ...
Tumour hypoxia renders cancer cells resistant to cancer therapy, resulting in markedly worse clinical outcomes. To find clinical candidate compounds that reduce hypoxia in tumours, we conduct a high-throughput screen for oxygen consumption rate (OCR) reduction and identify a number of drugs with this property. For this study we focus on the anti-malarial, atovaquone. Atovaquone rapidly decreases the OCR by more than 80% in a wide range of cancer cell lines at pharmacological concentrations. In addition, atovaquone eradicates hypoxia in FaDu, HCT116 and H1299 spheroids. Similarly, it reduces hypoxia in FaDu and HCT116 xenografts in nude mice, and causes a significant tumour growth delay when combined with radiation. Atovaquone is a ubiquinone analogue, and decreases the OCR by inhibiting mitochondrial complex III. We are now undertaking clinical studies to assess whether atovaquone reduces tumour hypoxia in patients, thereby increasing the efficacy of radiotherapy.
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To evaluate if atovaquone (ATQ) interacts pharmacokinetically with azithromycin (AZ) in human being immunodeficiency virus-infected children, 10 subjects (ages, 4 to 13 years) were randomized inside a crossover study to receive AZ (5 mg/kg/day time) only (ALONE) or AZ (5 mg/kg/day time) and ATQ (30 mg/kg/day time) simultaneously (SIM) prior to receiving AZ and ATQ staggered by 12 h. larger study will be required to determine if ATQ affects AZ pharmacokinetics and effectiveness inside a clinically significant manner. Children infected with human being immunodeficiency computer virus (HIV) have an increased risk of severe and recurrent infections (3, 15, 16, 18, 20), among which the most common is definitely pneumonia (PCP). A new, promising combination, azithromycin (AZ) plus atovaquone (ATQ), is currently under investigation inside a phase II/III medical trial (ACTG 254) to compare its efficiency and protection with those of trimethoprim-sulfamethoxazole in the prophylaxis of multiple ...
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Atovaquone (hydroxy-1,4-naphthoquinone) is a naphthoquinone analog. This drug has poor water solubility and is usually incorporated into lipid-based formulations and requires to be given with a fatty meal for adequate absorption[1]. Atovaquone is indicated for use against canine infections caused by Toxoplasma spp, Babesia spp[2], Pneumocystis spp. With Babesia spp infections, it is sometimes used in combination with azithromycin[3]. Recommended dose rate is 10 - 15 mg/kg with fatty meal given orally every 8 hours for 10 - 21 days. ...
Atovaquone Atovaquone Systematic (IUPAC) name 3-[4-(4-chlorophenyl)cyclohexyl]- 4-hydroxy-naphthalene-1,2-dione Identifiers CAS number 95233-18-4 ATC code
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Information for health care professionals and patients on malaria, its treatment, and prophylaxis using Malarone (atovaquone proguanil HCI) tablets from GlaxoSmithKline. ...
Atovaquone and Proguanil is a very strong oral medication marketed under the brand name Malarone that is intended for the treatment of malaria.
Atovaquone and proguanil are medications to treat malaria, a disease caused by parasites. These medicines work by interfering with the growth of parasites in the red blood cells of the human body. Parasites that cause malaria typically enter the body through the bite of a mosquito. Malaria is common in areas such as...
What is in this leaflet?Unless explained differently, the information for Malarone in this leaflet applies to both Malarone Tablets (250/100) and Malarone Junior Tablets (62.5/25) (refer to the Product description section near the end of the leaflet for a description of these two products).Please read this leaflet carefully before you take Malarone.This leaflet answers some common questions about Malarone. It does not contain all of the available information.It does not take the place of talking..
Background. Trimethoprim-sulfamethoxazole (TMP-SMZ) has been used extensively for the prevention of Pneumocystis carinii (also referred to as Pneumocystis jiroveci) pneumonia (PCP) and other opportunistic infections in human immunodeficiency virus (HIV)-infected children. Because the efficacy of TMP-SMZ for treatment of bacterial infections is limited, it is sometimes poorly tolerated, and there is risk of emergence of drug-resistant strains associated with widespread use, we evaluated a regimen that included atovaquone and azithromycin.. Methods. A randomized, double-blind, placebo-controlled trial was designed to determine whether atovaquone-azithromycin had equivalent efficacy to TMP-SMZ for the prevention of serious bacterial infections and to compare the long-term tolerance, PCP breakthrough rates, and nonserious bacterial infection rates among HIV-infected children aged 3 months to 19 years. Children qualified for PCP prophylaxis (on the basis of Centers for Disease Control and ...
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No studies have been done on breastfeeding and Malarone (atovaquone/proguanil). However, as this eMedTV page explains, the drug is not likely to pass through breast milk in high amounts. This article offers more details on using Malarone while nursing.
TravelHealthPro is the website comprising the travel health resources of the National Travel Health Network and Centre (NaTHNaC).
As explained in this eMedTV article, Malarone (atovaquone/proguanil) is currently available in generic form. This Web page discusses this topic in detail and explains how to protect yourself from fake malaria medications.
Although SMX/TMP remains the drug of choice for PCP prophylaxis, drug sensitivity may limit its use. Atovaquone has demonstrated greater safety than SMX/TMP and thus is suitable as a candidate drug for treatment and prophylaxis of PCP. Azithromycin, with a broad anti-microbial spectrum (including mycoplasma and atypical mycoplasma), is an attractive prophylactic agent for use in children with HIV infection, due to its relative safety and once-daily dosing regimen. Therefore, the combination of atovaquone and azithromycin may offer broader antimicrobial coverage and greater safety than SMX/TMP.. Patients are randomized to receive either SMX/TMP or combination micronized atovaquone/azithromycin. Crossover to the alternative regimen may occur if serious toxicity is observed. Patients are monitored for occurrence of serious bacterial infections or PCP breakthrough, and when a serious bacterial infection occurs, patients are crossed over to the alternative regimen. Treatment continues until 2 years ...
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Assess pulmonary function by measuring lung volumes, breath sounds, respiratory rate, and other symptoms (cough, dyspnea, shortness of breath) (See Appendices I, J, K). Report changes in pulmonary function to help document the effects of drug therapy in treating PCP infections. ...
Avoid concomitant other efavirenz-containing products (eg, Atripla unless needed for dose adjustment with rifampin), atazanavir (treatment-experienced), posaconazole, boceprevir, simeprevir, atovaquone/proguanil, pibrentasvir/glecaprevir, velpatasvir/sofosbuvir/voxilaprevir, alcohol, psychoactive, other NNRTIs or hepatotoxic drugs. Caution with drugs metabolized by, or that affect activity of, CYP2B6 or CYP3A4. Efavirenz levels decreased by carbamazepine, phenytoin, phenobarbital, rifampin (adjust dose). May decrease levels of indinavir, amprenavir, atazanavir, saquinavir, anticonvulsants, clarithromycin, calcium channel blockers (eg, diltiazem, felodipine, nicardipine, nifedipine, verapamil), itraconazole, ketoconazole, lopinavir (adjust dose: see full labeling), maraviroc, bupropion, methadone, rifabutin (increase dose; see full labeling), sertraline, simvastatin, atorvastatin, pravastatin, hormonal contraceptives (eg, norgestimate, etonogestrel), immunosuppressants (eg, cyclosporine, ...
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Multicenter Therapeutic Efficacy Assessment of Pyronaridine-Artesunate (Pyramax®) and New Drug Combinations With Atovaquone-Proguanil for the Treatment of Uncomplicated P. Falciparum Malaria in Cambodia ...
In seven controlled trials, 436 adolescents and adults received atovaquone and proguanil hydrochloride for treatment of acute, uncomplicated P. falciparum malaria. The range of mean ages of subjects was 26 to 29 years; 79% of subjects were male. In these studies, 48% of subjects were classified as other racial/ethnic groups, primarily Asian; 42% of subjects were black and the remaining subjects were white. Attributable adverse experiences that occurred in ≥ 5% of patients were abdominal pain (17%), nausea (12%), vomiting (12%), headache (10%), diarrhea (8%), asthenia (8%), anorexia (5%), and dizziness (5%). Treatment was discontinued prematurely due to an adverse experience in 4 of 436 (0.9%) adolescents and adults treated with atovaquone and proguanil hydrochloride.. In two controlled trials, 116 pediatric patients (weighing 11 kg to 40 kg) (mean age 7 years) received atovaquone and proguanil hydrochloride for the treatment of malaria. The majority of subjects were black (72%); 28% were of ...
Risk Summary Available data from published literature and postmarketing experience with use of atovaquone and proguanil hydrochloride in pregnant women are insufficient to identify a drug-associated risk for major birth defects, miscarriage, or adverse maternal or fetal outcomes. The proguanil component of atovaquone and proguanil hydrochloride tablets acts to inhibit parasitic dihydrofolate reductase; however, pregnant women and females of reproductive potential should continue folate supplementation to prevent neural tube defects [see Clinical Pharmacology (12.4)]. Pregnant women with malaria are at increased risk for adverse pregnancy outcomes (see Clinical Considerations). Atovaquone administered by oral gavage to pregnant rats and rabbits during the period of organogenesis was not associated with fetal malformations at plasma exposures approximately 7 times and equal to, respectively, the estimated human exposure for the treatment of malaria based on AUC. Proguanil administered to pregnant ...
Malarone belongs to a group of medicines called antimalarials. It contains two active ingredients, atovaquone and proguanil hydrochloride. Malaria is spread by the bite of an infected mosquito, which passes the malaria parasite (Plasmodium falciparum) into the bloodstream.
If you have taken it before and were fine on it, then you can start 1.5 weeks before travel. It wasnt scientifically. What are the potential side . knowlesi, a parasite of Old World (Eastern Hemisphere) monkeys, has been documented as a cause side effects malarone chloroquine of human infections and some deaths in Southeast Asia Chloroquine phosphate is an expensive drug used to treat or prevent malaria infections.It is also used to treat amebiasis.It is more popular than comparable drugs. It is used to treat and prevent malaria, including chloroquine-resistant malaria. Chloroquine can also be used to treat malaria after you get it. Overdose Chloroquine is very toxic in overdosage; overdosage is extremely hazardous and …. Decreased Appetite. Oct 10, 2017 · Side Effects and What to Do About Them Chloroquine (Aralen) Side effects are normally mild and include: headache, loss of appetite, Atovaquone/Proguanil (Malarone) Serious and unusual reactions side effects malarone chloroquine are: ...
The clinical experience of human immunodeficiency virus (HIV) + patients treated with oral atovaquone for acute Pneumocytstis carinii pneumonia (PCP) under a Treatment Investigational New Drug (IND) protocol (mild or moderate PCP) and an Open-Label Study protocol (severe PCP) was evaluated. A total of 940 patients intolerant of or unresponsive to trimethoprimsulfamethoxazole were enrolled from private practices, clinics, and institutional HIV treatment centers in the United States. Demographics data and the history and severity of PCP were collected at enrollment.
The patent for Malarone, an anti malarial drug ran out last year and you can now buy generic (unbranded, but identical) tablets at a highly reduced price. After shopping around extensively for a weeks worth of the drug being quoted upwards of £50 for the course (16 tablets). I found that ASDA sell it at £1 per tablet, which is less than half the price of any other high street pharmacy and 65p less per tablet than the cheapest online pharmacy I could find. Hope this helps anyone trying to travel on a budget ...
According to the guidelines for India[8] Chemoprophylaxis should be administered only in selective groups in high P.falciparum endemic areas. Use of personal protection measures is encouraged for pregnant women and other vulnerable population including travellers. However, for longer stay of Military and Para-military forces in high Pf endemic areas, the practice of chemoprophylaxis is to be followed wherever appropriate. For Short term chemoprophylaxis (up to 6 weeks) Doxycycline, is the drug of choice. Chemoprophylaxis for longer stay (more than 6 weeks) is with Mefloquine.. Regimens currently recommended for use in South Africa (2009), include Mefloquine, Doxycycline or Atovaquone - proguanil.[9]. Guidelines from the Health Protection Agency Advisory Committee on Malaria Prevention (ACMP) in UK travellers (2007) recommend Mefloquine, or Doxycycline or Atovaquone/Proguanil for travel to high risk areas of Bangladesh and India. Chloroquine plus proguanil is recommended as an alternative. For ...
Preface xvi. Abacacavir (Ziagen) 435. Abacavir + Lamivudine + Dolutegravir (Triumeq) 381. Acyclovir (Zovirax) 442. Adefovir (Hepsera) 187. Albendazole (Albenza) 3. Amikacin (Amikin) 9. Amoxicillan 11. Amoxicillin-Clavulanate (Augmentin, Augmentin 600ES, Augmentin XR) 32. Amphotericin B (Fungizone) 169. Amphotericin B Colloidal Dispersion - ABCD (Amphotec) 13. Amphotericin B Lipid Complex (Abelcet) 1. Ampicillin 15. Ampicillin-Sulbactam (Unasyn) 394. Anidulafungin (Eraxis) 149. Artemether/Lumefantrine (Coartem) 92. Artesunate 27. Atazanavir (Reyataz) 317. Atazanavir + Cobicistat (Evotaz) 152. Atovaquone (Mepron) 240. Atovaquone/Proguanil (Malarone) 230. Azithromycin (Zithromax, Zmax) 437. Aztreonam (Azactam) 40. Bedaquiline (Sirturo) 337. Benznidazole 51. Bithionol (Bitin) 57. Capreomycin (Capastat) 62. Caspofungin (Cancidas) 60. Cefaclor 66. Cefadroxil (Duricef) 135. Cefamandole (Mandol) 232. Cefazolin (Ancef) 18. Cefdinir (Omnicef) 270. Cefditoren Pivoxil (Spectracef) 343. Cefepime (Maxipime) ...
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A 50-year-old Nigerian man was admitted for generalized non febrile seizures. Two weeks before his GP prescribed antimalaric prophilaxis with clorochine for a planned trip in his home country. He suffered of a minor stroke 2 years before with no residual disability. He had also history of arterial hypertension treated with ace inhibitors and aspirin. At admission he was treated with lorazepam i.v. for a second generalized crisis at admission, and started carbamazepine 1000 per day. No other critical events were found during in hospital staying. A CT scan demonstrated the known subcortical right hemispheric hypodensity with no sulcal effacement or swelling features. Three months later carbamazepine was gradually intterrupted. After few months a new trip to Lagos was planned and chosen an antimalaric prophilaxis with Proguanil/Atovaquone (Malarone). The drug was well tolerated and no side effects were detected.. Take home message ...
Proguanil is an anti malarial drug which is given orally. Proguanil is also known as schizonticide. Proguanil is useful as a chemoprophylaxis against malaria.
See Contraindications. Concomitant hepatotoxic agents: may cause fatal liver dysfunction. Concomitant alcohol may be associated with higher incidence of isoniazid hepatitis. Avoid tyramine- and histamine-containing foods, halothane. Monitor prothrombin time with concomitant anticoagulants. May potentiate anticonvulsants (eg, phenytoin), benzodiazepines, haloperidol, ketoconazole, theophylline, warfarin; adjust dose. May antagonize anticonvulsants, digoxin, antiarrhythmics, oral anticoagulants, azole antifungals, barbiturates, β-blockers, calcium channel blockers, chloramphenicol, clarithromycin, fluoroquinolones, cyclosporine, cardiac glycosides, clofibrate, diazepam, doxycycline, haloperidol, levothyroxine, oral or systemic hormonal contraceptives (consider nonhormonal methods), methadone, oral hypoglycemics, dapsone, corticosteroids, narcotic analgesics, progestins, quinine, tacrolimus, theophylline, tricyclic antidepressants, zidovudine, atovaquone, enalapril, sulfasalazine. May be ...
Joseph Bozorgmehr also notes that [i]n many instances...a loss of function and regulation in a harsh or unusual environment can have a beneficial outcome and thus be selected for-bacteria tend to evolve resistance to antibiotics in such a way through mutations that would otherwise adversely affect membrane permeability.20. Parasites. Humans have been battling malaria for thousands of years. The advent of modern medicine provided us with a weapon to finally beat this ravaging parasite once and for all. Or so we thought. Unfortunately for us, malaria has been able to develop immunity to every drug weve thrown at it. For example, malaria quickly developed resistance to Atovaquone. All that was required to circumvent the effectiveness of this drug was a single point mutation at position 268 in a single malarial gene. The odds of developing this particular mutation are one in a trillion (1012). While those odds would be difficult to overcome for most organisms (such as human beings or beetles), ...
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In vitro studies have indicated that the antifolates pyrimethamine [4, 6] and cycloguanil (the active metabolite of proguanil) suppress the proliferation of stimulated human lymphocytes; proguanil has no effect [2]. During the early growth phase of the cells, 14C-thymidine (14C-TdR) incorporation is increased by pyrimethamine and cycloguanil, reflecting blockage of endogenous TdR synthesis [3]. Proguanil (Paludrine) is increasingly being used for malaria prophylaxis. It is considered the most innocuous of the antimalarials currently employed. Since nothing is known about the effect of oral proguanil on human lymphocytes, the present study was undertaken. Little information is available about the serum levels of proguanil and cycloguanil following ingestion of prophylactic doses [8]. Therefore, the serum concentrations of proguanil and cycloguanil were estimated, to allow comparison with previous in vitro studies [2 ...
Doxycycline. There is no evidence for human teratogenicity with doxycycline use during pregnancy. 8 Despite this, the main concern with doxycycline, like tetracycline, is the risk to the fetus of inhibition of bone growth and discoloration and dysplasia of the teeth, 3 which can occur during the period of calcification beyond the fourth month of gestational age. 4 Because of the potential harm, doxycycline is not recommended during pregnancy. However, keeping in mind that treatment is continued for 4 weeks after leaving the malaria-endemic area, 9 doxycycline can be considered as long as treatment is completed by the fourth month of pregnancy.. Atovaquone-proguanil. Proguanil has been used as a malarial prophylactic agent for decades, with no known toxic effects on the fetus. 10 Four small 3-day treatment studies with the atovaquone-proguanil combination in the second and third trimesters of pregnancy did not identify any adverse effects in the fetuses or newborns. 11-14 In a recent ...
Learn about The ABCD of malaria prophylaxis and the awareness of risk in Malaria Prophylaxis. Learn more about Malaria Prophylaxis.
HIV antiviral, CAS No. 154598-52-4), mefenamic acid (nonsteroidal anti-inflammatory, CAS No. 61-68-7), and atovaquone (antifungal and anti-parasite, CAS No. 95233-18-4) + proguanil HCl (antimalarial, CAS No. 637-32-1). In addition, two previously. ...
I am pleased to announce our latest research project: my staff and I are participating in the following very important initiative.. 3 Day Malarone Acceptability and Tolerability research project (3MAT). Malaria is one of the most common causes of fever in Australian travellers, with approximately 400 cases reported each year in Australia. Most travellers who develop malaria did not take anti-malarial medications, or did not take the medications properly (e.g. forgot to take tablets). Malaria is a serious illness and can potentially be fatal.. A research project is being conducted with the aim to make it easier and cheaper to take malaria pills and thus reduce the risk of malaria in travellers. Malarone is a safe and effective anti-malarial medication. The standard dosage of Malarone for prevention of malaria is one tablet per day, starting 2 days before travelling to a malaria area, daily while in a malaria area, and continuing until 7 days after leaving the malaria area.. Research has shown ...
Thus far, malaria control has primarily focused on destroying mosquito breeding sites, using insecticides and preventing human contact using mosquito nets and screens (White, 2004). However, malaria predominantly affects lesser economically developed countries and thus the cost of treatment serves as a barrier to disease eradication. Anti-malarial drugs are some of the most common medications provided in tropical countries. They generally function by inhibiting specific enzymes or making the environment difficult for the parasite to survive in (Basore et al., 2015). Drugs are relatively cheaper, widely available and, as there is no vaccine, they currently provide the most effective method of treatment (White, 2004). One such class is Atovaquone. It works by inhibiting mitochondrial electron transport in the malarial parasite and preventing the build-up of an electrochemical gradient (Vaidya and Mather, 2000). This would prevent Plasmodium parasites from producing ATP via oxidative ...
Our investigations reveal that cGAS contributes to parasite control, which is essential for the formation of GC-derived humoral immunity. The ability to simultaneously identify and analyze endogenous polyclonal antigen-specific CD4+ T cells and B cells responding to Plasmodium has revealed a profound effect of innate immune control of parasitemia. Control of parasitemia is important for timely development of the GC response, a response critical for both the efficient generation of high-affinity antibodies and durable immune memory (59-62). Furthermore, our ability to track parasitemia throughout the course of infection combined with the potential to rapidly clear blood-stage infection with atovaquone provided us with an elegant system in which the effects of innate control of parasite burden could be disentangled from the effects of early innate signals on the adaptive immune response. Specifically, the collapse of the GC response in cGAS-/- mice as parasitemia persisted could be abolished with ...
Cancer cells have upregulated glycolysis compared with normal cells, which has led many to the assumption that oxidative phosphorylation (OXPHOS) is downregulated in all cancers. However, recent studies have shown that OXPHOS can be also upregulated in certain cancers, including leukemias, lymphomas, pancreatic ductal adenocarcinoma, high OXPHOS subtype melanoma, and endometrial carcinoma, and that this can occur even in the face of active glycolysis. OXPHOS inhibitors could therefore be used to target cancer subtypes in which OXPHOS is upregulated and to alleviate therapeutically adverse tumor hypoxia. Several drugs including metformin, atovaquone, and arsenic trioxide are used clinically for non-oncologic indications, but emerging data demonstrate their potential use as OXPHOS inhibitors. We highlight novel applications of OXPHOS inhibitors with a suitable therapeutic index to target cancer cell metabolism. Clin Cancer Res; 24(11); 2482-90. ©2018 AACR.
Various analytical methods for formulations, raw materials, APIs and intermediates have been developed at SDPARC. Instrumental methods developed include, Proguanil Hydrochloride, Forskolin, Guggulsterone, Many dissolutions methods have been developed and validated at the centre. Methods for estimating residual solvents and organic volatile impurities are also developed and validated at the centre.. ...
The most common side effects of proguanil (Malarone) are vomiting, headache, diarrhea, loss of appetite, nausea, and mouth sores. Some people temporar
Medications that can be used for the treatment of malaria in pregnancy include chloroquine, quinine, atovaquone-proguanil, clindamycin, mefloquine (avoid in first trimester), sulfadoxine-pyrimethamine... more
It works by killing the parasites in the blood and also in the liver. It is effective against strains of falciparum malaria which may be resistant to other antimalarials and so is especially useful for those travelling to places where there is a high risk of encountering malaria which is resistant to other drugs. It would be particularly useful for those individuals who cannot tolerate, or who are unable to take mefloquine ...
Proguanil is used to prevent malaria. It is usually used in combination with another antimalarial medicine to increase its effectiveness.
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