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Dihydroartemisinin Piperaquine Phosphate
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 ...
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By Mouth
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ...
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Oxidative Stress
Oxidative stress reflects an imbalance between the systemic manifestation of reactive oxygen species and a biological system's ability to readily detoxify the reactive intermediates or to repair the resulting damage. Disturbances in the normal redox state of cells can cause toxic effects through the production of peroxides and free radicals that damage all components of the cell, including proteins, lipids, and DNA. Oxidative stress from oxidative metabolism causes base damage, as well as strand breaks in DNA. Base damage is mostly indirect and caused by the reactive oxygen species generated, e.g., (superoxide radical), OH ( hydroxyl radical) and (hydrogen peroxide). Further, some reactive oxidative species act as cellular messengers in redox signaling. Thus, oxidative stress can cause disruptions in normal mechanisms of cellular signaling. In humans, oxidative stress is thought to be involved in the development of attention deficit hyperactivity disorder, cancer, Parkin ...
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Organic Peroxides
In organic chemistry, organic peroxides are organic compounds containing the peroxide functional group (). If the R′ is hydrogen, the compounds are called hydroperoxides, which are discussed in that article. The O−O bond of peroxides easily breaks, producing free radicals of the form (the dot represents an unpaired electron). Thus, organic peroxides are useful as radical initiator, initiators for some types of polymerization, such as the Acrylic resin, acrylic, unsaturated polyester, and vinyl ester resins used in glass-reinforced plastics. methyl ethyl ketone peroxide, MEKP and benzoyl peroxide are commonly used for this purpose. However, the same property also means that organic peroxides can explosively combust. Organic peroxides, like their inorganic counterparts, are often powerful bleaching agents. Types of organic peroxides Organic peroxides are classified (i) by the presence or absence of a hydroxyl () terminus and (ii) by the presence of alkyl vs acyl substituents. ...
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Antimalarial Agents
Antimalarial medications or simply antimalarials are a type of antiparasitic chemical agent, often natural product, 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 ( ...
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Lactol
In organic chemistry, a lactol is a functional group which is the cyclic equivalent of a hemiacetal () or a hemiketal (). The compound is formed by the intramolecular, nucleophilic addition of a hydroxyl group () to the carbonyl group () of an aldehyde () or a ketone (). A lactol is often found as an equilibrium mixture with the corresponding hydroxyaldehyde. The equilibrium can favor either direction depending on ring size and other conformational effects. : The lactol functional group is prevalent in nature as component of aldose sugars. Chemical reactivity Lactols can participate in a variety of chemical reactions including: * Oxidation to form lactones * Reaction with alcohols to form acetals ** The reaction of sugars with alcohols or other nucleophiles leads to the formation of glycosides * Reduction (deoxygenation) to form cyclic ether In organic chemistry, ethers are a class of compounds that contain an ether group, a single oxygen atom bonded to two separate ca ...
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Diisobutylaluminium Hydride
Diisobutylaluminium hydride (DIBALH, DIBAL, DIBAL-H or DIBAH) is a reducing agent with the chemical formula, formula (''i''-Bu2AlH)2, where ''i''-Bu represents isobutyl (-CH2CH(CH3)2). This organoaluminium chemistry, organoaluminium compound is a reagent in organic synthesis. Properties Like most organoaluminum compounds, the compound's structure is most probably more than that suggested by its empirical formula. A variety of techniques, not including X-ray crystallography, suggest that the compound exists as a dimer (chemistry), dimer and a trimer, consisting of tetrahedral aluminium centers sharing bridging hydride ligands. Hydrides are small and, for aluminium derivatives, are highly base (chemistry), basic, thus they bridge in preference to the alkyl groups. DIBAL can be prepared by heating triisobutylaluminium (itself a dimer) to induce Beta-Hydride elimination, β-hydride elimination: :(''i''-Bu3Al)2 → (''i''-Bu2AlH)2 + 2 isobutene, (CH3)2C=CH2 Although DIBAL can be purcha ...
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Lithium Borohydride
Lithium borohydride (LiBH4) is a borohydride and known in organic synthesis as a reducing agent for esters. Although less common than the related sodium borohydride, the lithium salt offers some advantages, being a stronger reducing agent and highly soluble in ethers, whilst remaining safer to handle than lithium aluminium hydride.Luca Banfi, Enrica Narisano, Renata Riva, Ellen W. Baxter, "Lithium Borohydride" e-EROS Encyclopedia of Reagents for Organic Synthesis, 2001, John Wiley & Sons. . Preparation Lithium borohydride may be prepared by the metathesis reaction, which occurs upon ball-milling the more commonly available sodium borohydride and lithium bromide: : NaBH4 + LiBr → NaBr + LiBH4 Alternatively, it may be synthesized by treating boron trifluoride with lithium hydride in diethyl ether: : BF3 + 4 LiH → LiBH4 + 3 LiF Reactions Lithium borohydride is useful as a source of hydride (H–). It can react with a range of carbonyl substrates and other polarized c ...
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Potassium Borohydride
Borohydride refers to the anion , which is also called tetrahydroborate or more commonly tetrahydrobiopterin, and its salts. Borohydride or hydroborate is also the term used for compounds containing , where ''n'' is an integer from 0 to 3, for example cyanoborohydride or cyanotrihydroborate and triethylborohydride or triethylhydroborate . Borohydrides find wide use as reducing agents in organic synthesis. The most important borohydrides are lithium borohydride and sodium borohydride, but other salts are well known (see Table). Tetrahydroborates are also of academic and industrial interest in inorganic chemistry. History Alkali metal borohydrides were first described in 1940 by Hermann Irving Schlesinger and Herbert C. Brown. They synthesized lithium borohydride from diborane : :, where M = Li, Na, K, Rb, Cs, etc. Current methods involve reduction of trimethyl borate with sodium hydride. Structure In the borohydride anion and most of its modifications, boron has a tetrahe ...
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Sodium Borohydride
Sodium borohydride, also known as sodium tetrahydridoborate and sodium tetrahydroborate, is an inorganic compound with the formula (sometimes written as ). It is a white crystalline solid, usually encountered as an aqueous basic solution. Sodium borohydride is a reducing agent that finds application in papermaking and dye industries. It is also used as a reagent in organic synthesis. The compound was discovered in the 1940s by H. I. Schlesinger, who led a team seeking volatile uranium compounds.Hermann I Schlesinger and Herbert C Brown (1945)Preparation of alkali metal compounds. US Patent 2461661. Granted on 1949-02-15; expired on 1966-02-15. Results of this wartime research were declassified and published in 1953. Properties The compound is soluble in alcohols, certain ethers, and water, although it slowly hydrolyzes. Sodium borohydride is an odorless white to gray-white microcrystalline powder that often forms lumps. It can be purified by recrystallization from warm ...
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Excipient
An excipient is a substance formulated alongside the active ingredient of a medication. They may be used to enhance the active ingredient’s therapeutic properties; to facilitate drug absorption; to reduce viscosity; to enhance solubility; to improve long-term stabilization (preventing denaturation and aggregation during the expected shelf life); or to add bulk to solid formulations that have small amounts of potent active ingredients (in that context, they are often referred to as "bulking agents", "fillers", or "diluents"). During the manufacturing process, excipients can improve the handling of active substances and facilitate powder flow. The choice of excipients depends on factors such as the intended route of administration, the dosage form, and compatibility with the active ingredient. Virtually all marketed drugs contain excipients, and final drug formulations commonly contain more excipient than active ingredient. Pharmaceutical regulations and standards mandate the ...
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Hemozoin
Haemozoin is a disposal product formed from the digestion of blood by some blood-feeding parasites. These hematophagy, hematophagous organisms such as malaria parasites (''Plasmodium spp.''), ''Rhodnius'' and ''Schistosoma'' digest haemoglobin and release high quantities of free heme, which is the non-protein component of haemoglobin. Heme is a prosthetic group consisting of an iron atom contained in the center of a heterocyclic porphyrin ring. Free heme is toxic to cells, so the parasites convert it into an insoluble crystalline form called hemozoin. In malaria parasites, hemozoin is often called ''malaria pigment''. Since the formation of hemozoin is essential to the survival of these parasites, it is an attractive target for drug development, developing drugs and is much-studied in ''Plasmodium'' as a way to find drugs to treat malaria (malaria's Achilles' heel). Several currently used antimalarial drugs, such as chloroquine and mefloquine, are thought to kill malaria parasites ...
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Heme
Heme (American English), or haem (Commonwealth English, both pronounced /Help:IPA/English, hi:m/ ), is a ring-shaped iron-containing molecule that commonly serves as a Ligand (biochemistry), ligand of various proteins, more notably as a Prosthetic group, component of hemoglobin, which is necessary to bind oxygen in the bloodstream. It is composed of four pyrrole rings with 2 Vinyl group, vinyl and 2 propionic acid side chains. Heme is biosynthesized in both the bone marrow and the liver. Heme plays a critical role in multiple different redox reactions in mammals, due to its ability to carry the oxygen molecule. Reactions include oxidative metabolism (cytochrome c oxidase, succinate dehydrogenase), xenobiotic detoxification via cytochrome P450 pathways (including Drug metabolism, metabolism of some drugs), gas sensing (Guanylate cyclase, guanyl cyclases, nitric oxide synthase), and microRNA processing (DGCR8). Heme is a coordination complex "consisting of an iron ion coordinated ...
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