|
Piperaquine
Piperaquine is an antiparasitic drug used in combination with dihydroartemisinin to treat malaria. Piperaquine was developed under the Chinese National Malaria Elimination Programme in the 1960s and was adopted throughout China as a replacement for the structurally similar antimalarial drug chloroquine. Due to widespread parasite resistance to piperaquine, the drug fell out of use as a monotherapy, and is instead used as a partner drug for artemisinin combination therapy. Piperaquine kills parasites by disrupting the detoxification of host heme. Medical uses Piperaquine is used in combination with dihydroartemisinin for the treatment of malaria. This combination is one of several artemisinin combination therapies recommended by the World Health Organization for treatment of uncomplicated malaria. This combination is also recommended by the World Health Organization for treatment of severe malaria after administration of artesunate. Piperaquine is also registered for use in som ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Artenimol
Dihydroartemisinin (also known as dihydroqinghaosu, artenimol or DHA) is a drug used to treat malaria. Dihydroartemisinin is the active metabolite of all artemisinin compounds (artemisinin, artesunate, artemether, etc.) and is also available as a drug in itself. It is a semi-synthetic derivative of artemisinin and is widely used as an intermediate in the preparation of other artemisinin-derived antimalarial drugs. It is sold commercially in combination with piperaquine and has been shown to be equivalent to artemether/lumefantrine. Medical use Dihydroartemisinin is used to treat malaria, generally as a combination drug with piperaquine. In a systematic review of randomized controlled trials, both dihydroartemisinin-piperaquine and artemether-lumefantrine are very effective at treating malaria (high quality evidence). However, dihydroartemisinin-piperaquine cures slightly more patients than artemether-lumefantrine, and it also prevents further malaria infections for longer after ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dihydroartemisinin
Dihydroartemisinin (also known as dihydroqinghaosu, artenimol or DHA) is a drug used to treat malaria. Dihydroartemisinin is the active metabolite of all artemisinin compounds (artemisinin, artesunate, artemether, etc.) and is also available as a drug in itself. It is a semi-synthetic derivative of artemisinin and is widely used as an intermediate in the preparation of other artemisinin-derived antimalarial drugs. It is sold commercially in combination with piperaquine and has been shown to be equivalent to artemether/lumefantrine. Medical use Dihydroartemisinin is used to treat malaria, generally as a combination drug with piperaquine. In a systematic review of randomized controlled trials, both dihydroartemisinin-piperaquine and artemether-lumefantrine are very effective at treating malaria (high quality evidence). However, dihydroartemisinin-piperaquine cures slightly more patients than artemether-lumefantrine, and it also prevents further malaria infections for longer aft ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IC50
The half maximal inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function. IC50 is a quantitative measure that indicates how much of a particular inhibitory substance (e.g. drug) is needed to inhibit, ''in vitro'', a given biological process or biological component by 50%. The biological component could be an enzyme, cell, cell receptor or microorganism. IC50 values are typically expressed as molar concentration. IC50 is commonly used as a measure of antagonist drug potency in pharmacological research. IC50 is comparable to other measures of potency, such as EC50 for excitatory drugs. EC50 represents the dose or plasma concentration required for obtaining 50% of a maximum effect ''in vivo''. IC50 can be determined with functional assays or with competition binding assays. Sometimes, IC50 values are converted to the pIC50 scale. :\ce = -\log_ \ce Due to the minus sign, higher values of pIC50 indica ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quinolines
Quinoline is a heterocyclic aromatic organic compound with the chemical formula C9H7N. It is a colorless hygroscopic liquid with a strong odor. Aged samples, especially if exposed to light, become yellow and later brown. Quinoline is only slightly soluble in cold water but dissolves readily in hot water and most organic solvents. Quinoline itself has few applications, but many of its derivatives are useful in diverse applications. A prominent example is quinine, an alkaloid found in plants. Over 200 biologically active quinoline and quinazoline alkaloids are identified. 4-Hydroxy-2-alkylquinolines (HAQs) are involved in antibiotic resistance. Occurrence and isolation Quinoline was first extracted from coal tar in 1834 by German chemist Friedlieb Ferdinand Runge; he called quinoline ''leukol'' ("white oil" in Greek). Coal tar remains the principal source of commercial quinoline. In 1842, French chemist Charles Gerhardt obtained a compound by dry distilling quinine, str ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Piperazines
Substituted piperazines are a class of chemical compounds based on a piperazine core. Some are used as recreational drugs and some are used in scientific research. List of substituted piperazines Benzylpiperazines File:Benzylpiperazine.svg, 1-Benzylpiperazine File:MBZP.svg, 1-Methyl-4-benzylpiperazine File:DBZP.svg, 1,4-Dibenzylpiperazine File:MDBZP.svg, 3,4-Methylenedioxy-1-benzylpiperazine File:2C-B-BZP.svg, 4-Bromo-2,5-dimethoxy-1-benzylpiperazine File:Methoxypiperamide.png, Methoxypiperamide File:Sunifiram.svg , Sunifiram File:3-Methylbenzylpiperazine structure.png, 3-Methylbenzylpiperazine * 1-Benzylpiperazine (BZP) * 1-Methyl-4-benzylpiperazine (MBZP) * 1,4-Dibenzylpiperazine (DBZP) * 3,4-Methylenedioxy-1-benzylpiperazine (MDBZP) * 4-Bromo-2,5-dimethoxy-1-benzylpiperazine (2C-B-BZP) * Methoxypiperamide (MeOP, MEXP) ((4-methoxyphenyl)(4-methylpiperazin-1-yl)methanone) * Sunifiram (1-benzoyl-4-propanoylpiperazine) * 3-Methylbenzylpiperazine (3-MeBZP) Befuraline, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antimalarial Agents
Antimalarial medications or simply antimalarials are a type of antiparasitic chemical agent, often naturally derived, that can be used to treat or to prevent malaria, in the latter case, most often aiming at two susceptible target groups, young children and pregnant women. As of 2018, modern treatments, including for severe malaria, continued to depend on therapies deriving historically from quinine and artesunate, both parenteral (injectable) drugs, expanding from there into the many classes of available modern drugs. Incidence and distribution of the disease ("malaria burden") is expected to remain high, globally, for many years to come; moreover, known antimalarial drugs have repeatedly been observed to elicit resistance in the malaria parasite—including for combination therapies featuring artemisinin, a drug of last resort, where resistance has now been observed in Southeast Asia. As such, the needs for new antimalarial agents and new strategies of treatment (e.g., new combin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Shanghai Pharmaceutical Industry Research Institute
Shanghai (; , , Standard Mandarin pronunciation: ) is one of the four direct-administered municipalities of the People's Republic of China (PRC). The city is located on the southern estuary of the Yangtze River, with the Huangpu River flowing through it. With a population of 24.89 million as of 2021, Shanghai is the most populous urban area in China with 39,300,000 inhabitants living in the Shanghai metropolitan area, the second most populous city proper in the world (after Chongqing) and the only city in East Asia with a GDP greater than its corresponding capital. Shanghai ranks second among the administrative divisions of Mainland China in human development index (after Beijing). As of 2018, the Greater Shanghai metropolitan area was estimated to produce a gross metropolitan product (nominal) of nearly 9.1 trillion RMB ($1.33 trillion), exceeding that of Mexico with GDP of $1.22 trillion, the 15th largest in the world. Shanghai is one of the world's major centers for fin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Volume Of Distribution
In pharmacology, the volume of distribution (VD, also known as apparent volume of distribution, literally, ''volume of dilution'') is the theoretical volume that would be necessary to contain the total amount of an administered drug at the same concentration that it is observed in the blood plasma. In other words, it is the ratio of ''amount of drug in a body (dose)'' to ''concentration of the drug that is measured in blood, plasma, and un-bound in interstitial fluid''. The VD of a drug represents the degree to which a drug is distributed in body tissue rather than the plasma. VD is directly proportional with the amount of drug distributed into tissue; a higher VD indicates a greater amount of tissue distribution. A VD greater than the total volume of body water (approximately 42 liters in humans) is possible, and would indicate that the drug is highly distributed into tissue. In other words, the volume of distribution is smaller in the drug staying in the plasma than that of a dr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lipophilic
Lipophilicity (from Greek λίπος "fat" and φίλος "friendly"), refers to the ability of a chemical compound to dissolve in fats, oils, lipids, and non-polar solvents such as hexane or toluene. Such non-polar solvents are themselves lipophilic (translated as "fat-loving" or "fat-liking"), and the axiom that "like dissolves like" generally holds true. Thus lipophilic substances tend to dissolve in other lipophilic substances, but hydrophilic ("water-loving") substances tend to dissolve in water and other hydrophilic substances. Lipophilicity, hydrophobicity, and non-polarity may describe the same tendency towards participation in the London dispersion force, as the terms are often used interchangeably. However, the terms "lipophilic" and "hydrophobic" are not synonymous, as can be seen with silicones and fluorocarbons, which are hydrophobic but not lipophilic. __TOC__ Surfactants Hydrocarbon-based surfactants are compounds that are amphiphilic (or amphipathic), having a h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mefloquine
Mefloquine, sold under the brand name Lariam among others, is a medication used to prevent or treat malaria. When used for prevention it is typically started before potential exposure and continued for several weeks after potential exposure. It can be used to treat mild or moderate malaria but is not recommended for severe malaria. It is taken by mouth. Common side effects include vomiting, diarrhea, headaches, sleep disorders, and a rash. Serious side effects include potentially long-term mental health problems such as depression, hallucinations, and anxiety and neurological side effects such as poor balance, seizures, and ringing in the ears. It is therefore not recommended in people with a history of mental health problems or epilepsy. It appears to be safe during pregnancy and breastfeeding. Mefloquine was developed by the United States Army in the 1970s and came into use in the mid-1980s. It is on the World Health Organization's List of Essential Medicines. It is availa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
