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Troleandomycin
Troleandomycin (TAO for short) is a macrolide antibiotic. It was sold in Italy (branded Triocetin) and Turkey (branded Tekmisin). It is no longer sold in Italy as of 2018. The drug's mode of action is to bind to the ribosome, specifically in the tunnel through which the newly formed peptide egresses, thereby halting protein synthesis. Troleandomycin is a CYP3A4 inhibitor that may cause drug interaction In pharmaceutical sciences, drug interactions occur when a drug's mechanism of action is affected by the concomitant administration of substances such as foods, beverages, or other drugs. A popular example of drug–food interaction is the effect ...s. References CYP3A4 inhibitors Macrolide antibiotics Epoxides Spiro compounds Acetate esters {{antibiotic-stub ...
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Macrolide Antibiotics
Macrolides are a class of mostly natural products with a large macrocyclic lactone ring to which one or more deoxy sugars, usually cladinose and desosamine, may be attached. Macrolides belong to the polyketide class of natural products. Some macrolides have antibiotic or antifungal activity and are used as pharmaceutical drugs. Rapamycin is also a macrolide and was originally developed as an antifungal, but has since been used as an immunosuppressant drug and is being investigated as a potential longevity therapeutic. Macrolides are a diverse group with many members of very different properties: * Macrolides with 14-, 15-, or 16-membered rings and two attached sugar molecules are antibiotics that bind to bacterial ribosomes, the key representative being erythromycin. The term "macrolide antibiotics" tend to refer to just this class. * Some macrolides with very large (20+ membered) rings are immunosuppresants, the prototypical one being rapamycin. * Some 23-membered macrol ...
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Macrolide
Macrolides are a class of mostly natural products with a large macrocyclic lactone ring to which one or more deoxy sugars, usually cladinose and desosamine, may be attached. Macrolides belong to the polyketide class of natural products. Some macrolides have antibiotic or antifungal activity and are used as pharmaceutical drugs. Rapamycin is also a macrolide and was originally developed as an antifungal, but has since been used as an immunosuppressant drug and is being investigated as a potential longevity therapeutic. Macrolides are a diverse group with many members of very different properties: * Macrolides with 14-, 15-, or 16-membered rings and two attached sugar molecules are antibiotics that bind to bacterial ribosomes, the key representative being erythromycin. The term "macrolide antibiotics" tend to refer to just this class. * Some macrolides with very large (20+ membered) rings are immunosuppresants, the prototypical one being rapamycin. * Some 23-membered ...
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Italy
Italy, officially the Italian Republic, is a country in Southern Europe, Southern and Western Europe, Western Europe. It consists of Italian Peninsula, a peninsula that extends into the Mediterranean Sea, with the Alps on its northern land border, as well as List of islands of Italy, nearly 800 islands, notably Sicily and Sardinia. Italy shares land borders with France to the west; Switzerland and Austria to the north; Slovenia to the east; and the two enclaves of Vatican City and San Marino. It is the List of European countries by area, tenth-largest country in Europe by area, covering , and the third-most populous member state of the European Union, with nearly 59 million inhabitants. Italy's capital and List of cities in Italy, largest city is Rome; other major cities include Milan, Naples, Turin, Palermo, Bologna, Florence, Genoa, and Venice. The history of Italy goes back to numerous List of ancient peoples of Italy, Italic peoples—notably including the ancient Romans, ...
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Turkey
Turkey, officially the Republic of Türkiye, is a country mainly located in Anatolia in West Asia, with a relatively small part called East Thrace in Southeast Europe. It borders the Black Sea to the north; Georgia (country), Georgia, Armenia, Azerbaijan, and Iran to the east; Iraq, Syria, and the Mediterranean Sea to the south; and the Aegean Sea, Greece, and Bulgaria to the west. Turkey is home to over 85 million people; most are ethnic Turkish people, Turks, while ethnic Kurds in Turkey, Kurds are the Minorities in Turkey, largest ethnic minority. Officially Secularism in Turkey, a secular state, Turkey has Islam in Turkey, a Muslim-majority population. Ankara is Turkey's capital and second-largest city. Istanbul is its largest city and economic center. Other major cities include İzmir, Bursa, and Antalya. First inhabited by modern humans during the Late Paleolithic, present-day Turkey was home to List of ancient peoples of Anatolia, various ancient peoples. The Hattians ...
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Mechanism Of Action
In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical Drug interaction, interaction through which a Medication, drug substance produces its pharmacological effect. A mechanism of action usually includes mention of the specific molecular targets to which the drug binds, such as an enzyme or receptor (biochemistry), receptor. Receptor sites have specific affinities for drugs based on the chemical structure of the drug, as well as the specific action that occurs there. Drugs that do not bind to receptors produce their corresponding therapeutic effect by simply interacting with chemical or physical properties in the body. Common examples of drugs that work in this way are antacids and laxatives. In contrast, a Mode of action, mode of action (MoA) describes functional or anatomical changes, at the cellular level, resulting from the exposure of a living organism to a substance. Importance Elucidating the mechanism of action of novel drugs and medicati ...
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CYP3A4
Cytochrome P450 3A4 (abbreviated CYP3A4) () is an important enzyme in the body, mainly found in the liver and in the intestine, which in humans is encoded by ''CYP3A4'' gene. It organic redox reaction, oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs, so that they can be removed from the body. It is highly homologous to CYP3A5, another important CYP3A enzyme. While many drugs are deactivated by CYP3A4, there are also some drugs that are ''activated'' by the enzyme. Some substances, such as some drugs and furanocoumarins present in grapefruit juice, interfere with the action of CYP3A4. These substances will, therefore, either amplify or weaken the action of those drugs that are modified by CYP3A4. CYP3A4 is a member of the cytochrome P450 family of oxidizing enzymes. Several other members of this family are also involved in drug metabolism, but CYP3A4 is the most common and the most versatile one. Like all members of this family, it is a hemoprote ...
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Enzyme Inhibitor
An enzyme inhibitor is a molecule that binds to an enzyme and blocks its Enzyme activity, activity. Enzymes are proteins that speed up chemical reactions necessary for life, in which Substrate (biochemistry), substrate molecules are converted into Product (chemistry), products. An enzyme Enzyme catalysis, facilitates a specific chemical reaction by binding the substrate to its active site, a specialized area on the enzyme that accelerates the Rate-determining step, most difficult step of the reaction. An enzyme inhibitor stops ("inhibits") this process, either by binding to the enzyme's active site (thus preventing the substrate itself from binding) or by binding to another site on the enzyme such that the enzyme's catalysis of the reaction is blocked. Enzyme inhibitors may bind Reversible reaction, reversibly or irreversibly. Irreversible inhibitors form a Covalent bond, chemical bond with the enzyme such that the enzyme is inhibited until the chemical bond is broken. By cont ...
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Drug Interaction
In pharmaceutical sciences, drug interactions occur when a drug's mechanism of action is affected by the concomitant administration of substances such as foods, beverages, or other drugs. A popular example of drug–food interaction is the effect of grapefruit on the metabolism of drugs. Interactions may occur by simultaneous targeting of receptors, directly or indirectly. For example, both Zolpidem and alcohol affect GABAA receptors, and their simultaneous consumption results in the overstimulation of the receptor, which can lead to loss of consciousness. When two drugs affect each other, it is a drug–drug interaction (DDI). The risk of a DDI increases with the number of drugs used. A large share of elderly people regularly use five or more medications or supplements, with a significant risk of side-effects from drug–drug interactions. Drug interactions can be of three kinds: * additive (the result is what you expect when you add together the effect of each drug take ...
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CYP3A4 Inhibitors
Cytochrome P450 3A4 (abbreviated CYP3A4) () is an important enzyme in the body, mainly found in the liver and in the intestine, which in humans is encoded by ''CYP3A4'' gene. It oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs, so that they can be removed from the body. It is highly homologous to CYP3A5, another important CYP3A enzyme. While many drugs are deactivated by CYP3A4, there are also some drugs that are ''activated'' by the enzyme. Some substances, such as some drugs and furanocoumarins present in grapefruit juice, interfere with the action of CYP3A4. These substances will, therefore, either amplify or weaken the action of those drugs that are modified by CYP3A4. CYP3A4 is a member of the cytochrome P450 family of oxidizing enzymes. Several other members of this family are also involved in drug metabolism, but CYP3A4 is the most common and the most versatile one. Like all members of this family, it is a hemoprotein, i.e. a protein cont ...
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Epoxides
In organic chemistry, an epoxide is a cyclic ether, where the ether forms a three-atom Ring (chemistry), ring: two atoms of carbon and one atom of oxygen. This triangular structure has substantial ring strain, making epoxides highly Reactivity (chemistry), reactive, more so than other ethers. They are produced on a large scale for many applications. In general, low molecular weight epoxides are colourless and nonpolar, and often Volatility (chemistry), volatile. Nomenclature A compound containing the epoxide functional group can be called an epoxy, epoxide, oxirane, and ethoxyline. Simple epoxides are often referred to as oxides. Thus, the epoxide of ethylene (C2H4) is ethylene oxide (C2H4O). Many compounds have trivial names; for instance, ethylene oxide is called "oxirane". Some names emphasize the presence of the epoxide functional group, as in the compound ''1,2-epoxyheptane'', which can also be called ''1,2-heptene oxide''. A polymer formed from epoxide precursors is c ...
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Spiro Compounds
In organic chemistry, spiro compounds are compounds that have at least two molecular rings sharing one common atom. Simple spiro compounds are bicyclic (having just two rings). The presence of only one common atom connecting the two rings distinguishes spiro compounds from other bicyclics.For all four categories, see The specific chapters can be found aan respectively, same access date. For the description featuring adjacent atoms for all but the isolated category, see Clayden, op. cit. Spiro compounds may be fully carbocyclic (all carbon) or heterocyclic (having one or more non-carbon atom). One common type of spiro compound encountered in educational settings is a heterocyclic one— the acetal formed by reaction of a diol with a cyclic ketone. The common atom that connects the two (or sometimes three) rings is called the ''spiro atom''. In carbocyclic spiro compounds like spiro .5ndecane, the spiro-atom is a quaternary carbon, and as the ''-ane'' ending implies, these ar ...
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