To evaluate the effectiveness in malaria vector control of residual spraying with Solfac WP10 at dose of 50mg ai/m2 and bednet impregnated with Solfac EW050 at a dose of 50mg ai/m2, based on bioassays, side effects. The results showed that: in pilot doses, the residual effect with Solfac 10WP produced the residual effect for 6 months on the walls made of wood with the bioassay mortality of 70.60%; for 2 months on the wall made of brick with the bioassay mortality of 61.63%. The residual effect of Solfact EW 050 on polyester bednet is 4 months after 2 washes, with the bioassay mortality of 73.6%. House spraying with Solfac WP10 and bednet impregnation with Solfac EW 050 at a dose of 50mg/ ai/m2 to prevent malaria due to mosquito were found to cause light side effects
malaria ; Antimalarials ; disease ; Culicidae

The response of the malarial parasite, Plasmodium falciparum to a number of Vietnamese medicinal plants in vitro was carried out. The results showed that the ethanol extract of the plant materials has a stronger inhibitory effect on the growth of P. faciparum than the corresponding water extract. Both ethanol and water extracts of the leaves of Dichroa febrifuge Lour. and the ethnologic extracts from the leaves of Parthenium hysterrophorus L. and Harrisonia perforate (Blanco) Merr. have a clear effect on the chloroquine sensitivity as well as the chloroquine resistant P. falciparum strain
Plants, Medicinal ; Antimalarials ; Plasmodium falciparum

Testing in 127 patients with malaria at the Center of Malariological- Parasitological - Entomological prevention and control and hospitals in A Luoi, Nam Dong, Phu Loc, Huong Thuy, Huong Tra, Phong Dien, Phu Vang districts and Hue city with 2 types: Giemsa staining and Parachek P.F technique. Results showed that: 40 positive samples with P.fal and 87 negative samples. Results of the 2 methods were similar
Malaria ; Antimalarials ; diagnosis ; Malaria, Falciparum

The coupling procedure of antimalarial agent (SR2) onto polymeric carrier (SR1) by covalent bond (amide linkage) was studied. Some factors of drug coupling reaction was investigated.
Antimalarials ; Pharmaceutical Preparations ; drug therapy

The study was conducted in 2002 for analysis by non-linear regression of compartmental pharmacokinetic model. The results: the plasma-concentration of piperaquine at day 1 and day 3 after CV8 administration were determined. At first stage, only the basic parameters derived from non-compartmental methods were presented and another parameters, models is expected to be presented in later stages. The plasma-concentration of piperaquine of all volunteers were determined with Cmax on day 1 was 1015 nM/L, on day 2 was 1050 nM/L, T1/2 was 30-57 days and Tmax of piperaquine was 3-5 hours after using
Malaria ; Antimalarials ; Pharmacokinetics ; Therapeutics ; drugs

A hospital based pilot study, conducted in a Tropical diseases hospital in Ho Chi Minh City of Viet Nam, compared the efficacy of three day regimens of dihydroartemisinin-trimethoprim-piperaquine (DTP total dose 4.7/13/47 mg/kg) with the standard antimalarial regimen in Vietnam, artersunate-mefloquine (A3M total dose 12/25 mg/kg) in non immune patients with uncomplicated falciparum malaria. 114 patients were enrolled (78 to the DTP arm and 36 to the A3M arm). The subsequent open randomised trial conducted at a Provincial Health Station compared DTP, dihydroartemisinin-piperaquine (DP) and A3M in 400 patients. In both studies all patients received derectly observed therapy and were followed for 56 days. The results: In the pilot study, the 56 day cure rate, adjusted for reinfections by PCR genotyping was 97.4% in the DTP group and 100% in the A3M group. In the second study, the cure rate were similar in each group. The DTP regimens were well tolerated, less than 3% of patients experienced possible drug related side effects compared with 16% of A3M patients
Malaria ; Antimalarials ; Malaria, Falciparum ; artemisisnins ; drugs ; therapeutics

Plasmodium culture in vitro is often used as an antimalarial drug evaluation model, but the lifecycle of P. falciparum culture in vitro tends to be disordered, which affects the research and evaluation of antimalarial drug mechanism in vitro. By combining magnetic bead separation method with sorbitol synchronization method, a synchronization method was constructed to quickly acquire different lifecycles of P. falciparum and obtain large amounts of parasite with a narrow synchronization window in a short period. Furthermore, the dihydroartemisinin(DHA) was used to treat the early trophozoite phase of P. falciparum 3 D7 for 4 h. Then mRNA was extracted and RNA-seq was conducted to analyze the differential expression of mRNA after drug treatment and obtain the differential gene expression profile. Differential expression of up-regulated genes and down-regulated genes was analyzed according to the screening criteria of |log_2FC|>1 and P<0.05. There, 262 genes were up-regulated and 77 genes were down-regulated. GO functional enrichment analysis of all the differentially expressed genes showed that the enrichment items mainly included cell membrane components, transporter activity, serine/threonine kinase activity, Maurer's clefts(MCs), rhoptry, antigen variation and immune evasion. The enrichment of KEGG pathway included malaria, fatty acid metabolism and peroxisome. Protein-protein interaction(PPI) analysis showed that the down-regulated genes in the modules with high degree of association included rhoptry, myosin complex, transporter and other genes related to the important life activities of malaria invasion and immune escape; the up-regulated genes were mainly related to various toxic exportins of malaria, such as PfSBP1 of MCs. qRT-PCR was used to verify the expression level of some genes, and most of the results were the same as the sequencing results. SBP1 was significantly up-regulated, while some antigenic protein expression levels were down-regulated. Above all, key molecules of DHA therapy were mainly involved in the parasites' rhoptry, transporter, antigenic variation, plasmodium exportin. These results offer us many hints to guide the further studies on mechanism of artemisinin and provide a new way for development of new antimalarial drugs.
Animals ; Antimalarials ; Artemisinins ; Erythrocytes ; Plasmodium falciparum ; Transcriptome

Ajania belonging to the subtribe Artemisiinae of Anthemideae(Asteraceae) is a genus of semi-shrubs closely related to Chrysanthemum. There are 24 species of Ajania in northwestern China, most of which are folk herbal medicines with strong stress tolerance. Modern medical studies have demonstrated that the chemical constituents of Ajania mainly include terpenoids, flavonoids, phenylpropanoids, alkynes, and essential oils. These compounds endow the plants with antimicrobial, anti-inflammatory, antitumor, antimalarial, antioxidant, and insecticide effects. In this study, we reviewed the research progress in the chemical constituents and pharmacological activities of Ajania, aiming to provide reference for the further research and development of Ajania.
Asteraceae ; Chrysanthemum ; Alkynes ; Antimalarials ; Antioxidants/pharmacology*

We evaluated the efficacy and safety of halofantrine in 19 patients with acute uncomplicated falciparum malaria. Each patient received oral halofantrine hydrochloride 500 mg every 6 hours for 3 doses (total 1.5 g). In almost all the patients clinical symptoms of malaria and parasitaemia disappeared within 2 and 3 days, respectively, of starting treatment. We observed no recurrence of parasitaemia during 14 days of follow-up. Tolerance to halofantrine was good except for minor and self-limiting gastrointestinal side-effects. Haematological and biochemical indices were not seriously affected. Halofantrine-induced prolongation of Q-T/Q-Tc intervals was the consistent cardiac manifestation in 84% of patients. The Q-T/Q-Tc interval prolongation increased with each dose; it reached a maximum between 18 and 24 hours and thereafter returned to baseline. These preliminary data indicate that, apart from the cardiac side-effects, halofantrine is an effective and safe drug, well tolerated by most of the patients in the study. PIP: The authors evaluated the efficacy and safety of halofantrine in 19 patients with acute uncomplicated falciparum malaria. Each patient received oral halofantrine hydrochloride 500 mg every 6 hours, for a total of 3 doses (total 1.5 g). In almost all the patients clinical symptoms of malaria and parasitemia disappeared within 2 and 3 days, respectively, of starting treatment. They observed no recurrence of parasitemia during 14 days of follow-up. Tolerance to halofantrine was good except for minor and self-limiting gastrointestinal side effects. Hematological and biochemical indices were not seriously affected. Halofantrine-induced prolongation of Q-T/Q-Tc intervals was the consistent cardiac manifestation in 84% of patients. The Q-T/Q-Tc interval prolongation increased with each dose; it reached a maximum between 18 and 24 hours and thereafter returned to baseline. These preliminary data indicate that, apart from the cardiac side effects, halofantrine is an effective and safe drug, well tolerated by most of the patients in the study.
Antimalarials - administration & ; dosage ; Antimalarials - therapeutic use ; Electrocardiography ; Malaria, Falciparum - blood

Artesunate (AS), a famous derivative of the artemisinin, is the basic treatment globally for mild to severe malaria infection due to the prominent advantages such as high efficiency, fast effect, low toxicity and not easy to produce resistance. More and more research reports have shown that AS and its active metabolites dihydroartemisinin (DHA) had various bioactivities in addition to antimalarial activity, attracting researchers to further study its new pharmacological effects in order to explore new use of the old drug. A comprehensive understanding of the pharmacokinetic characteristics of AS will be conducive to the further development of new pharmacological actions and clinical application of AS. Therefore, this paper would review the absorption, distribution, metabolism and excretion of AS , as well as the pharmacokinetics characteristics of AS and DHA after clinical administration of AS by intravenous (IV), intramuscular (IM), oral or rectal routes. The process and pharmacokinetic parameters of AS and DHA were compared between healthy volunteers, malaria patients, and special populations (children, women). Meanwhile, the research progress on pharmacological effects of AS and active metabolite DHA such as anti-tumor, anti-inflammatory, anti septic, antiangiogenic, anti-fibrosis and immunoregulation activities would be also reviewed, hoping to provide a theoretical basis for the further development and utilization of AS and its metabolites.
Antimalarials ; pharmacokinetics ; pharmacology ; Artesunate ; pharmacokinetics ; pharmacology ; Humans ; Research