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Paludrine
Proguanil, also known as chlorguanide and chloroguanide, is a medication used to treat and prevent malaria. It is often used together with chloroquine or atovaquone. When used with chloroquine the combination will treat mild chloroquine resistant malaria. It is taken by mouth. Side effects include diarrhea, constipation, skin rashes, hair loss, and itchiness. Because malaria tends to be more severe in pregnancy, the benefit typically outweighs the risk. If used during pregnancy it should be taken with folate. It is likely safe for use during breastfeeding. Proguanil is converted by the liver to its active metabolite, cycloguanil. Proguanil has been studied at least since 1945. It is on the World Health Organization's List of Essential Medicines. In the United States and Canada it is only available in combination as atovaquone/proguanil. Medical uses Proguanil is used for the prevention and treatment of malaria in both adults and children, particularly in areas where chloroq ... [...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] |
Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as 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 willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Plasmodium Falciparum
''Plasmodium falciparum'' is a Unicellular organism, unicellular protozoan parasite of humans, and the deadliest species of ''Plasmodium'' that causes malaria in humans. The parasite is transmitted through the bite of a female ''Anopheles'' mosquito and causes the disease's most dangerous form, falciparum malaria. It is responsible for around 50% of all malaria cases. ''P. falciparum'' is therefore regarded as the deadliest parasite in humans. It is also associated with the development of blood cancer (Burkitt's lymphoma) and is classified as a List of IARC Group 2A carcinogens, Group 2A (probable) carcinogen. The species originated from the malarial parasite ''Laverania'' found in gorillas, around 10,000 years ago. Alphonse Laveran was the first to identify the parasite in 1880, and named it ''Oscillaria malariae''. Ronald Ross discovered its transmission by mosquito in 1897. Giovanni Battista Grassi elucidated the complete transmission from a female Anopheles, anopheline mosquit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Protozoal Dihydrofolate Reductase Inhibitors
Protozoa (singular: protozoan or protozoon; alternative plural: protozoans) are a group of single-celled eukaryotes, either free-living or parasitic, that feed on organic matter such as other microorganisms or organic tissues and debris. Historically, protozoans were regarded as "one-celled animals", because they often possess animal-like behaviours, such as motility and predation, and lack a cell wall, as found in plants and many algae. When first introduced by Georg Goldfuss (originally spelled Goldfuß) in 1818, the taxon Protozoa was erected as a class within the Animalia, with the word 'protozoa' meaning "first animals". In later classification schemes it was elevated to a variety of higher ranks, including phylum, subkingdom and kingdom, and sometimes included within Protoctista or Protista. The approach of classifying Protozoa within the context of Animalia was widespread in the 19th and early 20th century, but not universal. By the 1970s, it became usual to require ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prodrugs
A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted (ADME). Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects. History Many herbal extracts historically used in medicine contain glycosides (sugar derivatives) of the active agent, which are hydrolyzed in the intestines to release the active and more bioavailable aglycone. For example, salicin is a β-D-glucopyranosid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isopropyl Compounds
In organic chemistry, propyl is a three-carbon alkyl substituent with chemical formula for the linear form. This substituent form is obtained by removing one hydrogen atom attached to the terminal carbon of propane. A propyl substituent is often represented in organic chemistry with the symbol Pr (not to be confused with the element praseodymium). An isomeric form of propyl is obtained by moving the point of attachment from a terminal carbon atom to the central carbon atom, named 1-methylethyl or isopropyl. To maintain four substituents on each carbon atom, one hydrogen atom has to be moved from the middle carbon atom to the carbon atom which served as attachment point in the ''n''-propyl variant, written as . Linear propyl is sometimes termed normal and hence written with a prefix ''n''- (i.e., ''n-''propyl), as the absence of the prefix ''n''- does not indicate which attachment point is chosen, i.e. absence of prefix does not automatically exclude the possibility of it be ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AstraZeneca Brands
AstraZeneca plc () is a British-Swedish multinational pharmaceutical and biotechnology company with its headquarters at the Cambridge Biomedical Campus in Cambridge, England. It has a portfolio of products for major diseases in areas including oncology, cardiovascular, gastrointestinal, infection, neuroscience, respiratory, and inflammation. It has been involved in developing the Oxford–AstraZeneca COVID-19 vaccine. The company was founded in 1999 through the merger of the Swedish Astra AB and the British Zeneca Group (itself formed by the demerger of the pharmaceutical operations of Imperial Chemical Industries in 1993). Since the merger it has been among the world's largest pharmaceutical companies and has made numerous corporate acquisitions, including Cambridge Antibody Technology (in 2006), MedImmune (in 2007), Spirogen (in 2013) and Definiens (by MedImmune in 2014). It has its research and development concentrated in three strategic centres: Cambridge, England; Goth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chlorobenzenes
Chlorobenzene is an aromatic organic compound with the chemical formula C6H5Cl. This colorless, flammable liquid is a common solvent and a widely used intermediate in the manufacture of other chemicals. Uses Historical The major use of chlorobenzene is as an intermediate in the production of herbicides, dyestuffs, and rubber. Chlorobenzene is also used as a high-boiling solvent in industrial applications as well as in the laboratory. Chlorobenzene is nitrated on a large scale to give a mixture of 2-nitrochlorobenzene and 4-nitrochlorobenzene, which are separated. These mononitrochlorobenzenes are converted to related 2-nitrophenol, 2-nitroanisole, bis(2-nitrophenyl)disulfide, and 2-nitroaniline by nucleophilic displacement of the chloride, with respectively sodium hydroxide, sodium methoxide, sodium disulfide, and ammonia. The conversions of the 4-nitro derivative are similar. Chlorobenzene once was used in the manufacture of pesticides, most notably DDT, by reaction with ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Biguanides
Biguanide () is the organic compound with the formula HN(C(NH)NH2)2. It is a colorless solid that dissolves in water to give highly basic solution. These solutions slowly hydrolyse to ammonia and urea. Synthesis Biguanide can be obtained from the reaction of dicyandiamide with ammonia, via a Pinner-type process. :\mathrm Biguanide was first synthesized by Bernhard Rathke in 1879. Biguanidine drugs A variety of derivatives of biguanide are used as pharmaceutical drugs. Antihyperglycemic agents The term "biguanidine" often refers specifically to a class of drugs that function as oral antihyperglycemic drugs used for diabetes mellitus or prediabetes treatment. Examples include: * Metformin - widely used in treatment of diabetes mellitus type 2 * Phenformin - withdrawn from the market in most countries due to toxic effects * Buformin - withdrawn from the market due to toxic effects File:Metformin.svg, Metformin, an asymmetric dimethylbiguanidine File:Buformin.svg, Buformin. A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Synergy
Synergy is an interaction or cooperation giving rise to a whole that is greater than the simple sum of its parts. The term ''synergy'' comes from the Attic Greek word συνεργία ' from ', , meaning "working together". History In Christian theology, synergism is the idea that salvation involves some form of cooperation between divine grace and human freedom. The words ''synergy'' and ''synergetic'' have been used in the field of physiology since at least the middle of the 19th century: SYN'ERGY, ''Synergi'a'', ''Synenergi'a'', (F.) ''Synergie''; from ''συν'', 'with', and ''εργον'', 'work'. A correlation or concourse of action between different organs in health; and, according to some, in disease. :—Dunglison, Roble''Medical Lexicon''Blanchard and Lea, 1853 In 1896, Henri Mazel applied the term "synergy" to social psychology by writing ''La synergie sociale'', in which he argued that Darwinian theory failed to account of "social synergy" or "social love", a co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tetrahydrofolic Acid
Tetrahydrofolic acid (THFA), or tetrahydrofolate, is a folic acid derivative. Metabolism Human synthesis Tetrahydrofolic acid is produced from dihydrofolic acid by dihydrofolate reductase. This reaction is inhibited by methotrexate. It is converted into 5,10-methylenetetrahydrofolate by serine hydroxymethyltransferase. Bacterial synthesis Many bacteria use dihydropteroate synthetase to produce dihydropteroate, a molecule without function in humans. This makes it a useful target for sulfonamide antibiotics, which compete with the PABA precursor. Functions Tetrahydrofolic acid is a cofactor in many reactions, especially in the synthesis (or anabolism) of amino acids and nucleic acids. In addition, it serves as a carrier molecule for single-carbon moieties, that is, groups containing one carbon atom e.g. methyl, methylene, methenyl, formyl, or formimino. When combined with one such single-carbon moiety as in 10-formyltetrahydrofolate, it acts as a donor of a group ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dihydrofolate Reductase
Dihydrofolate reductase, or DHFR, is an enzyme that reduces dihydrofolic acid to tetrahydrofolic acid, using NADPH as an electron donor, which can be converted to the kinds of tetrahydrofolate cofactors used in 1-carbon transfer chemistry. In humans, the DHFR enzyme is encoded by the ''DHFR'' gene. It is found in the q11→q22 region of chromosome 5. Bacterial species possess distinct DHFR enzymes (based on their pattern of binding diaminoheterocyclic molecules), but mammalian DHFRs are highly similar. Structure A central eight-stranded beta-pleated sheet makes up the main feature of the polypeptide backbone folding of DHFR. Seven of these strands are parallel and the eighth runs antiparallel. Four alpha helices connect successive beta strands. Residues 9 – 24 are termed "Met20" or "loop 1" and, along with other loops, are part of the major subdomain that surround the active site. The active site is situated in the N-terminal half of the sequence, which includes a conse ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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