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Inactive Prodrug
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] |
Pharmaceutical Drug
A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy ( pharmacotherapy) is an important part of the medical field and relies on the science of pharmacology for continual advancement and on pharmacy for appropriate management. Drugs are classified in multiple ways. One of the key divisions is by level of control, which distinguishes prescription drugs (those that a pharmacist dispenses only on the order of a physician, physician assistant, or qualified nurse) from over-the-counter drugs (those that consumers can order for themselves). Another key distinction is between traditional small molecule drugs, usually derived from chemical synthesis, and biopharmaceuticals, which include recombinant proteins, vaccines, blood products used therapeutically (such as IVIG), gene therapy, monoclonal antibodies and cell therapy (for instance, stem cell ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bayer
Bayer AG (, commonly pronounced ; ) is a German multinational pharmaceutical and biotechnology company and one of the largest pharmaceutical companies in the world. Headquartered in Leverkusen, Bayer's areas of business include pharmaceuticals; consumer healthcare products, agricultural chemicals, seeds and biotechnology products. The company is a component of the Euro Stoxx 50 stock market index. Bayer was founded in 1863 in Barmen as a partnership between dye salesman Friedrich Bayer and dyer Friedrich Weskott. As was common in this era, the company was established as a dyestuffs producer. The versatility of aniline chemistry led Bayer to expand their business into other areas, and in 1899 Bayer launched the compound acetylsalicylic acid under the trademarked name Aspirin. In 1904 Bayer received a trademark for the "Bayer Cross" logo, which was subsequently stamped onto each aspirin tablet, creating an iconic product that is still sold by Bayer. Other commonly known prod ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Terfenadine
Terfenadine is an antihistamine formerly used for the treatment of allergic conditions. It was brought to market by Hoechst Marion Roussel (now Sanofi-Aventis) and was marketed under various brand names, including Seldane in the United States, Triludan in the United Kingdom, and Teldane in Australia. It was superseded by fexofenadine in the 1990s due to the risk of a particular type of disruption of the electrical rhythms of the heart (specifically cardiac arrhythmia caused by QT interval prolongation) and has been withdrawn from markets worldwide. Pharmacology Terfenadine acts as a peripherally-selective antihistamine, or antagonist of the histamine H1 receptor. It is a prodrug, generally completely metabolized to the active form fexofenadine in the liver by the enzyme cytochrome P450 3A4. Due to its near complete metabolism by the liver immediately after leaving the gut, terfenadine normally is not measurable in the plasma. Terfenadine itself, however, is cardiotoxic at hig ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sulfanilamide
Sulfanilamide (also spelled sulphanilamide) is a sulfonamide antibacterial drug. Chemically, it is an organic compound consisting of an aniline derivatized with a sulfonamide group. Powdered sulfanilamide was used by the Allies in World War II to reduce infection rates and contributed to a dramatic reduction in mortality rates compared to previous wars. Sulfanilamide is rarely if ever used systemically due to toxicity and because more effective sulfonamides are available for this purpose. Modern antibiotics have supplanted sulfanilamide on the battlefield; however, sulfanilamide remains in use today in the form of topical preparations, primarily for treatment of vaginal yeast infections mainly vulvovaginitis which is caused by '' Candida albicans''. The term "sulfanilamides" is also sometimes used to describe a family of molecules containing these functional groups. Examples include: * Furosemide, a loop diuretic * Sulfadiazine, an antibiotic * Sulfamethoxazole, an antibio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gerhard Domagk
Gerhard Johannes Paul Domagk (; 30 October 1895 – 24 April 1964) was a German pathologist and bacteriologist. He is credited with the discovery of sulfonamidochrysoidine (KL730) as an antibiotic for which he received the 1939 Nobel Prize in Physiology or Medicine. The drug became the first commercially available antibiotic and marketed under the brand name Prontosil. While working in the pathology department of the University of Münster, Domagk was invited to join the IG Farben branch at Elberfeld (later Wuppertal) in 1927. His duty was to test chemical compounds prepared at the IG Farben laboratory for potential drugs. A novel compound synthesised by Friedrich Mietzsch and Joseph Klarer, a benzene derivative of azo dye attached with sulphonamide group as a side chain was found to have antibacterial activity against human bacterium ''Streptococcus pyogenes.'' In 1935, Domagk's only daughter, Hildegarde, injured herself and contracted a streptococcal infection. In a desperat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sulfa Drug
Sulfonamide is a functional group (a part of a molecule) that is the basis of several groups of drugs, which are called sulphonamides, sulfa drugs or sulpha drugs. The original antibacterial sulfonamides are synthetic (nonantibiotic) antimicrobial agents that contain the sulfonamide group. Some sulfonamides are also devoid of antibacterial activity, e.g., the anticonvulsant sultiame. The sulfonylureas and thiazide diuretics are newer drug groups based upon the antibacterial sulfonamides. Allergies to sulfonamides are common. The overall incidence of adverse drug reactions to sulfa antibiotics is approximately 3%, close to penicillin; hence medications containing sulfonamides are prescribed carefully. Sulfonamide drugs were the first broadly effective antibacterials to be used systemically, and paved the way for the antibiotic revolution in medicine. Function In bacteria, antibacterial sulfonamides act as competitive inhibitors of the enzyme dihydropteroate synthase (DHP ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prontosil
Prontosil is an antibacterial drug of the sulfonamide group. It has a relatively broad effect against gram-positive cocci but not against enterobacteria. One of the earliest antimicrobial drugs, it was widely used in the mid-20th century but is little used today because better options now exist. The discovery and development of this first sulfonamide drug opened a new era in medicine, because it greatly widened the success of antimicrobial chemotherapy in an era when many physicians doubted its still largely untapped potential. At the time, disinfectant cleaners and topical antiseptic wound care were widely used but there were very few antimicrobial drugs to use safely inside living bodies. Antibiotic drugs derived from microbes, which we rely on heavily today, did not yet exist. Prontosil was discovered in 1932 by a research team at the Bayer Laboratories of the IG Farben conglomerate in Germany. Names The capitalized name "Prontosil" is Bayer's trade name; the nonproprietary na ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Paul Ehrlich
Paul Ehrlich (; 14 March 1854 – 20 August 1915) was a Nobel Prize-winning German physician and scientist who worked in the fields of hematology, immunology, and antimicrobial chemotherapy. Among his foremost achievements were finding a cure for syphilis in 1909 and inventing the precursor technique to Gram staining bacteria. The methods he developed for staining tissue made it possible to distinguish between different types of blood cells, which led to the ability to diagnose numerous blood diseases. His laboratory discovered arsphenamine (Salvarsan), the first effective medicinal treatment for syphilis, thereby initiating and also naming the concept of chemotherapy. Ehrlich popularized the concept of a magic bullet. He also made a decisive contribution to the development of an antiserum to combat diphtheria and conceived a method for standardizing therapeutic serums. In 1908, he received the Nobel Prize in Physiology or Medicine for his contributions to immunology. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sahachiro Hata
was a prominent Japanese bacteriologist who researched the bubonic plague under Kitasato Shibasaburō and assisted in developing the Arsphenamine drug in 1909 in the laboratory of Paul Ehrlich. Hata received three unsuccessful nominations for the Nobel Prize, one from Swiss surgeon Emil Kocher for Chemistry in 1911 and two by Japanese colleagues Hayazo Ito and G Osawa for Physiology or Medicine in 1912 and 1913, respectively. Early life Hata was born in Tsumo Village, Shimane prefecture (now part of Masuda City) as the eighth son of the Yamane family. At the age of 14, he was adopted by the Hata family, whose male members were doctors from generation to generation. Hata completed his medical education in Okayama at the Third Higher School of Medicine (now Okayama University School of Medicine). In 1897, he became an assistant at Okayama Prefectural Hospital where he learned internal medicine from Zenjiro Inoue and biochemistry from Torasaburo Araki. Plague Research Sahachi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Arsphenamine
Arsphenamine, also known as Salvarsan or compound 606, is a drug that was introduced at the beginning of the 1910s as the first effective treatment for syphilis, relapsing fever, and African trypanosomiasis. This organoarsenic compound was the first modern antimicrobial agent. History Arsphenamine was first synthesized in 1907 in Paul Ehrlich's lab by Alfred Bertheim. The antisyphilitic activity of this compound was discovered by Sahachiro Hata in 1909, during a survey of hundreds of newly synthesized organic arsenical compounds. Ehrlich had theorized that by screening many compounds, a drug could be discovered that would have anti-microbial activity but not kill the human patient. Ehrlich's team began their search for such a " magic bullet" among chemical derivatives of the dangerously toxic drug atoxyl. This project was the first organized team effort to optimize the biological activity of a lead compound through systematic chemical modifications, the basis for nearly all ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glucuronides
A glucuronide, also known as glucuronoside, is any substance produced by linking glucuronic acid to another substance via a glycosidic bond. The glucuronides belong to the glycosides. Glucuronidation, the conversion of chemical compounds to glucuronides, is a method that animals use to assist in the excretion of toxic substances, drugs or other substances that cannot be used as an energy source. Glucuronic acid is attached via a glycosidic bond to the substance, and the resulting glucuronide, which has a much higher water solubility than the original substance, is eventually excreted by the kidneys. Enzymes that cleave the glycosidic bond of a glucuronide are called glucuronidases. Examples * Miquelianin (Quercetin 3-O-glucuronide) * Morphine-6-glucuronide Morphine-6-glucuronide (M6G) is a major active metabolite of morphine. M6G is formed from morphine by the enzyme UGT2B7. It has analgesic effects more potent than morphine. M6G can accumulate to toxic levels in kidney fa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bioactivation
Activation, in chemistry and biology, is the process whereby something is prepared or excited for a subsequent reaction. Chemistry In chemistry, "activation" refers to the reversible transition of a molecule into a nearly identical chemical or physical state, with the defining characteristic being that this resultant state exhibits an increased propensity to undergo a specified chemical reaction. Thus, activation is conceptually the opposite of protection, in which the resulting state exhibits a ''decreased'' propensity to undergo a certain reaction. The energy of activation specifies the amount of free energy the reactants must possess (in addition to their rest energy) in order to initiate their conversion into corresponding products—that is, in order to reach the transition state for the reaction. The energy needed for activation can be quite small, and often it is provided by the natural random thermal fluctuations of the molecules themselves (i.e. without any externa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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