|
Dexibuprofen
Dexibuprofen is a nonsteroidal anti-inflammatory drug (NSAID). It is the active dextrorotatory enantiomer of ibuprofen. Most ibuprofen formulations, as well as other drugs of the profen drug class, contain a racemic mixture of both isomers. Dexibuprofen is a chiral switch of racemic ibuprofen. The chiral carbon in dexibuprofen is assigned an absolute configuration of (''S'') per the Cahn–Ingold–Prelog rules. Dexibuprofen is also called (''S'')-(+)-ibuprofen. Ibuprofen is an α-arylpropionic acid used largely in the treatment of rheumatoid arthritis and widely used over-the counter drug for headache and minor pains. This drug has a chiral center and exists as a pair of enantiomers In chemistry, an enantiomer (Help:IPA/English, /ɪˈnænti.əmər, ɛ-, -oʊ-/ Help:Pronunciation respelling key, ''ih-NAN-tee-ə-mər''), also known as an optical isomer, antipode, or optical antipode, is one of a pair of molecular entities whi .... (''S'')-Ibuprofen, the eutomer, is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nonsteroidal Anti-inflammatory Drug
Non-steroidal anti-inflammatory drugs (NSAID) are members of a Indication (medicine), therapeutic drug class which Analgesic, reduces pain, Anti-inflammatory, decreases inflammation, Antipyretic, decreases fever, and Antithrombotic, prevents blood clots. Side effects depend on the specific drug, its dose and duration of use, but largely include an increased risk of Stomach ulcers, gastrointestinal ulcers and bleeds, heart attack, and kidney disease. The term ''non-steroidal'', common from around 1960, distinguishes these drugs from corticosteroids, another class of anti-inflammatory drugs, which during the 1950s had acquired a bad reputation due to overuse and side-effect problems after their introduction in 1948. NSAIDs work by inhibiting the activity of cyclooxygenase enzymes (the COX-1 and COX-2 isozyme, isoenzymes). In cells, these enzymes are involved in the synthesis of key biological mediators, namely prostaglandins, which are involved in inflammation, and thromboxanes, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enantiopure Drugs
An enantiopure drug is a pharmaceutical available in one specific enantiomeric form. Most biomolecules (proteins, sugars, etc.) are present in only one of many chiral forms, so different enantiomers of a chiral drug molecule bind differently (or not at all) to target receptors. The use of a drug with a single enantiomer intends to make it more effective. One enantiomer of a drug may have a desired beneficial effect while the other may cause serious and undesired side effects, or sometimes even beneficial but entirely different effects. The desired enantiomer is known as an ''eutomer'' while the undesired enantiomer is known as the ''distomer''. When equal amounts of both enantiomers are found in a mixture, the mixture is known as a racemic mixture. If a mixture for a drug does not have a 1:1 ratio of its enantiomers it is a candidate for an enantiopure drug. Advances in industrial chemical processes have made it economical for pharmaceutical manufacturers to take drugs that wer ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Profen (drug Class)
The profens are a class of nonsteroidal anti-inflammatory drugs. Profens are also known as 2-arylpropionic acids to reflect their chemical structure. The most common example of a profen is ibuprofen, which has been sold under the brand name Profen among others. Other drugs in the class include: * Alminoprofen * Benoxaprofen * Carprofen * Dexibuprofen * Dexketoprofen * Fenoprofen * Flunoxaprofen * Flurbiprofen * Indoprofen * Ketoprofen * Loxoprofen * Miroprofen * Naproxen * Pelubiprofen Pelubiprofen is a nonsteroidal anti-inflammatory drug of the profen class used to treat back pain and osteoarthritis Osteoarthritis is a type of degenerative joint disease that results from breakdown of articular cartilage, joint cartilage ... * Pirprofen * Pranoprofen * Suprofen * Tarenflurbil * Tiaprofenic acid * Vedaprofen * Zaltoprofen References Nonsteroidal anti-inflammatory drugs {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chiral Switch
A chiral switch is a chiral drug that has already approved as racemate but has been re-developed as a single enantiomer. The term chiral switching was introduced by Agranat and Caner in 1999 to describe the development of single enantiomers from racemate drugs. For example, levofloxacin is a chiral switch of racemic ofloxacin. It is important to understand that chiral switches are treated as a Selection Invention, selection invention. A selection invention is an invention that selects a group of new members from a previously known class on the basis of superior properties. Description The essential principle of a chiral switch is that there is a change in the status of chirality. In general, the term chiral switch is preferred over racemic switch because the switch is usually happening from a racemic drug to the corresponding single enantiomer. To express the pharmacological activities of each of the chiral twins of a racemic drug, two technical terms have been coined: ''eut ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enantiopure Drug
An enantiopure drug is a pharmaceutical available in one specific enantiomeric form. Most biomolecules (proteins, sugars, etc.) are present in only one of many chiral forms, so different enantiomers of a chiral drug molecule bind differently (or not at all) to target receptors. The use of a drug with a single enantiomer intends to make it more effective. One enantiomer of a drug may have a desired beneficial effect while the other may cause serious and undesired side effects, or sometimes even beneficial but entirely different effects. The desired enantiomer is known as an ''eutomer'' while the undesired enantiomer is known as the ''distomer''. When equal amounts of both enantiomers are found in a mixture, the mixture is known as a racemic mixture. If a mixture for a drug does not have a 1:1 ratio of its enantiomers it is a candidate for an enantiopure drug. Advances in industrial chemical processes have made it economical for pharmaceutical manufacturers to take drugs that wer ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chiral Switch
A chiral switch is a chiral drug that has already approved as racemate but has been re-developed as a single enantiomer. The term chiral switching was introduced by Agranat and Caner in 1999 to describe the development of single enantiomers from racemate drugs. For example, levofloxacin is a chiral switch of racemic ofloxacin. It is important to understand that chiral switches are treated as a Selection Invention, selection invention. A selection invention is an invention that selects a group of new members from a previously known class on the basis of superior properties. Description The essential principle of a chiral switch is that there is a change in the status of chirality. In general, the term chiral switch is preferred over racemic switch because the switch is usually happening from a racemic drug to the corresponding single enantiomer. To express the pharmacological activities of each of the chiral twins of a racemic drug, two technical terms have been coined: ''eut ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Distomer
The eudysmic ratio (also spelled eudismic ratio) represents the difference in pharmacologic activity between the two enantiomers of a drug. In most cases where a chiral compound is biologically active, one enantiomer is more active than the other. The eudysmic ratio is the ratio of activity between the two. A eudysmic ratio significantly differing from 1 means that they are statistically different in activity. Eudysmic ratio (ER) reflects the degree of enantioselectivity of the biological systems. For example, (S)-propranolol has ER = 130, meaning that (S)-propranolol is 130 times more active than its (R)-enantiomer. Terminology The eutomer is the enantiomer having the desired pharmacological activity, e.g., as an active ingredient in a drug. The distomer, on the other hand, is the enantiomer of the eutomer which may have undesired bioactivity or may be bio-inert. A racemic mixture is an equal mixture of both enantiomers, which may be easier to manufacture than a single enant ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nonsteroidal Anti-inflammatory Drugs
A nonsteroidal compound is a drug that is not a steroid nor a steroid derivative. Nonsteroidal anti-inflammatory drugs (NSAIDs) are distinguished from corticosteroids as a class of anti-inflammatory agents. List of nonsteroidal steroid receptor modulators Examples include the following: * Estrogens: benzestrol, bifluranol, estrobin, estrobin (DBE), diethylstilbestrol, diethylstilbestrol (stilbestrol), dienestrol, erteberel, fosfestrol, hexestrol, hexestrol (dihydroxystilbestrol), methallenestril, methestrol, methestrol dipropionate, paroxypropione, prinaberel, and triphenylethylene, as well as many xenoestrogens * : acolbifene, afimoxifene, arzoxifene, bazedoxifene, broparestrol, chlorotrianisene, clomifene, clomifenoxide, cyclofenil, droloxifene, enclomifene, endoxifen, ethamoxytriphetol, fispemifene, idoxifene, lasofoxifene, levormeloxifene, miproxifene, nafoxidine, nitromifene, ormeloxifene, ospemifene, panomifene, pipendoxifene, raloxifene, tamoxifen, toremifene, trioxifene, zind ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ibuprofen
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) that is used to relieve pain, fever, and inflammation. This includes dysmenorrhea, painful menstrual periods, migraines, and rheumatoid arthritis. It can be taken oral administration, orally (by mouth) or Intravenous therapy, intravenously. It typically begins working within an hour. Common side effects include heartburn, nausea, indigestion, and abdominal pain. Potential side effects include gastrointestinal bleeding. Long-term use has been associated with kidney failure, and rarely liver failure, and it can exacerbate the condition of people with heart failure. At low doses, it does not appear to increase the risk of myocardial infarction (heart attack); however, at higher doses it may. Ibuprofen can also worsen asthma. While its safety in early pregnancy is unclear, it appears to be harmful in later pregnancy, so it is not recommended during that period. It works by inhibiting the production of prostaglandins by dec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chirality
Chirality () is a property of asymmetry important in several branches of science. The word ''chirality'' is derived from the Greek (''kheir''), "hand", a familiar chiral object. An object or a system is ''chiral'' if it is distinguishable from its mirror image; that is, it cannot be superposed (not to be confused with superimposed) onto it. Conversely, a mirror image of an ''achiral'' object, such as a sphere, cannot be distinguished from the object. A chiral object and its mirror image are called '' enantiomorphs'' (Greek, "opposite forms") or, when referring to molecules, ''enantiomers''. A non-chiral object is called ''achiral'' (sometimes also ''amphichiral'') and can be superposed on its mirror image. The term was first used by Lord Kelvin in 1893 in the second Robert Boyle Lecture at the Oxford University Junior Scientific Club which was published in 1894: Human hands are perhaps the most recognized example of chirality. The left hand is a non-superposable mirror ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prodrug
A prodrug is a pharmacologically inactive 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, sal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enantiomer
In chemistry, an enantiomer (Help:IPA/English, /ɪˈnænti.əmər, ɛ-, -oʊ-/ Help:Pronunciation respelling key, ''ih-NAN-tee-ə-mər''), also known as an optical isomer, antipode, or optical antipode, is one of a pair of molecular entities which are mirror images of each other and non-superposable. Enantiomer molecules are like right and left hands: one cannot be superposed onto the other without first being converted to its mirror image. It is solely a relationship of chirality (chemistry), chirality and the permanent three-dimensional relationships among molecules or other chemical structures: no amount of re-orientation of a molecule as a whole or conformational isomerism, conformational change converts one chemical into its enantiomer. Chemical structures with chirality rotate plane-polarized light. A mixture of equal amounts of each enantiomer, a ''racemic mixture'' or a ''racemate'', does not rotate light. Stereoisomers include both enantiomers and diastereomers. Diaste ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
