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Pitavastatin
Pitavastatin (usually as a calcium salt) is a member of the blood cholesterol lowering medication class of statins. Pitavastatin is an inhibitor of HMG-CoA reductase, the enzyme that catalyses the first step of cholesterol synthesis. It was patented in 1987 and approved for medical use in 2003. It is available in Japan, South Korea and in India. In the US, it received FDA approval in 2009. Kowa Pharmaceuticals, a subsidiary of Kowa (company), Kowa Company, is the owner of the American patent to pitavastatin. Medical uses Pitavastatin is indicated for hypercholesterolaemia (elevated cholesterol) and for the prevention of cardiovascular disease. A 2009 study of the 104-week LIVES trial found pitavastatin increased HDL cholesterol, especially in patients with HDL lower than 40 mg/dL, who had a 24.6% rise, in addition to reducing LDL cholesterol 31.3%. HDL improved in patients who switched from other statins and rose over time. In the 70-month CIRCLE observational study, ...
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Statins
Statins (or HMG-CoA reductase inhibitors) are a class of medications that lower cholesterol. They are prescribed typically to people who are at high risk of cardiovascular disease. Low-density lipoprotein (LDL) carriers of cholesterol play a key role in the development of atherosclerosis and coronary heart disease via the mechanisms described by the lipid hypothesis. As lipid-lowering medications, statins are effective in lowering LDL cholesterol; they are widely used for primary prevention in people at high risk of cardiovascular disease, as well as in secondary prevention for those who have developed cardiovascular disease. Side effects of statins include muscle pain, increased risk of diabetes, and abnormal blood levels of certain liver enzymes. Additionally, they have rare but severe adverse effects, particularly muscle damage, and very rarely rhabdomyolysis. They act by inhibiting the enzyme HMG-CoA reductase, which plays a central role in the production of ...
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Nissan Chemical Industries
is a Japanese company and constituent of the Nikkei 225 stock index. History The company was founded in 1887 as "Tokyo Jinzo Hiryo" (Tokyo Artificial Fertilizer Company) by Jokichi Takamine, Eiichi Shibusawa and Takashi Masuda. Takamine served as chief technical advisor for the company. The company opened its first manufacturing plant in Kōtō, and in 1888, started producing superphosphate. The company was renamed to "Dainippon Jinzo Hiryo" (Dai Nippon Artificial Fertilizer Company) in 1910. In 1923, the companies of Kanto Soda and Nippon Kagaku Hiryo were merged under the Dainippon Jinzo Hiryo name. The resulting company was brought into the Nissan Group in 1937, and was renamed as Nissan Chemical Industries. In 1928, the company began production of ammonia and ammonium sulfate at a plant in Toyama (city), Toyama. After World War II, the Nissan group was dissolved, Zaibatsu#Postwar_dissolution, along with several other zaibatsus, as part of the Allied occupation strategy ...
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Liver Function Test
Liver function tests (LFTs or LFs), also referred to as a hepatic panel or liver panel, are groups of blood tests that provide information about the state of a patient's liver. These tests include prothrombin time (PT/INR), activated partial thromboplastin time (aPTT), albumin, bilirubin (direct and indirect), and others. The liver transaminases aspartate transaminase (AST or SGOT) and alanine transaminase (ALT or SGPT) are useful biomarkers of liver injury in a patient with some degree of intact liver function. Most liver diseases cause only mild symptoms initially, but these diseases must be detected early. Hepatic (liver) involvement in some diseases can be of crucial importance. This testing is performed on a patient's blood sample. Some tests are associated with functionality (e.g., albumin), some with cellular integrity (e.g., transaminase), and some with conditions linked to the biliary tract ( gamma-glutamyl transferase and alkaline phosphatase). Because some of t ...
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Tokyo
Tokyo, officially the Tokyo Metropolis, is the capital of Japan, capital and List of cities in Japan, most populous city in Japan. With a population of over 14 million in the city proper in 2023, it is List of largest cities, one of the most populous urban areas in the world. The Greater Tokyo Area, which includes Tokyo and parts of six neighboring Prefectures of Japan, prefectures, is the most populous metropolitan area in the world, with 41 million residents . Lying at the head of Tokyo Bay, Tokyo is part of the Kantō region, on the central coast of Honshu, Japan's largest island. It is Japan's economic center and the seat of the Government of Japan, Japanese government and the Emperor of Japan. The Tokyo Metropolitan Government administers Tokyo's central Special wards of Tokyo, 23 special wards, which formerly made up Tokyo City; various commuter towns and suburbs in Western Tokyo, its western area; and two outlying island chains, the Tokyo Islands. Although most of the w ...
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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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Drugs
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via inhalation, injection, smoking, ingestion, absorption via a patch on the skin, suppository, or dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to treat, cure, prevent, or diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a regular basis for chronic disorders. Classification Pharmaceutical drugs are often classified into drug classes—groups of related drugs that hav ...
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CYP2C8
Cytochrome P4502C8 (CYP2C8) is a member of the cytochrome P450 mixed-function oxidase system involved in the metabolism of xenobiotics in the body. Cytochrome P4502C8 also possesses epoxygenase activity, i.e. it metabolizes long-chain polyunsaturated fatty acids, e.g. arachidonic acid, eicosapentaenoic acid, docosahexaenoic acid, and linoleic acid to their biologically active epoxides. Ligands Following is a table of selected substrates, inducers and inhibitors of 2C8. Inhibitors of CYP2C8 can be classified by their potency, such as: * Strong inhibitor being one that causes at least a five-fold increase in the plasma AUC values, or more than 80% decrease in clearance. * Moderate inhibitor being one that causes at least a two-fold increase in the plasma AUC values, or 50-80% decrease in clearance. * Weak inhibitor being one that causes at least a 1.25-fold but less than two-fold increase in the plasma AUC values, or 20-50% decrease in clearance. Retrieved on July 2011 ...
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Glucuronidation
Glucuronidation is often involved in drug metabolism of substances such as drugs, pollutants, bilirubin, androgens, estrogens, mineralocorticoids, glucocorticoids, fatty acid derivatives, retinoids, and bile acids. These linkages involve glycosidic bonds. Mechanism Glucuronidation consists of transfer of the glucuronic acid component of uridine diphosphate glucuronic acid to a substrate by any of several types of UDP-glucuronosyltransferase. UDP-glucuronic acid (glucuronic acid linked via a glycosidic bond to uridine diphosphate) is an intermediate in the process and is formed in the liver. One example is the N-glucuronidation of an aromatic amine, 4-aminobiphenyl, by UGT1A4 or UGT1A9 from human, rat, or mouse liver. : The substances resulting from glucuronidation are known as glucuronides (or glucuronosides) and are typically much more water- soluble than the non-glucuronic acid-containing substances from which they were originally synthesised. The human body uses g ...
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Grapefruit
The grapefruit (''Citrus'' × ''paradisi'') is a subtropical citrus tree known for its relatively large, sour to semi-sweet, somewhat bitter fruit. The flesh of the fruit is segmented and varies in color from pale yellow to dark red. Grapefruits originated in Barbados in the 18th century. They are a citrus hybrid that was created through an accidental cross between the sweet orange (''C.'' × ''sinensis'') and the pomelo (''C. maxima''), both of which were introduced to the Caribbean from Asia in the 17th century. It has also been called the 'forbidden fruit'. In the past it was called the ''pomelo'', but that term is now mostly used as the common name for ''Citrus maxima''. Grapefruit–drug interactions are common, as the juice contains furanocoumarins that interfere with the metabolism of many drugs. This can prolong and intensify the effects of those drugs, leading to multiple side-effects such as abnormal heart rhythms, bleeding inside the stomach, low blood pressure ...
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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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Cytochrome P450
Cytochromes P450 (P450s or CYPs) are a Protein superfamily, superfamily of enzymes containing heme as a cofactor (biochemistry), cofactor that mostly, but not exclusively, function as monooxygenases. However, they are not omnipresent; for example, they have not been found in ''Escherichia coli''. In mammals, these enzymes oxidize steroids, fatty acids, xenobiotics, and participate in many biosyntheses. By hydroxylation, CYP450 enzymes convert xenobiotics into hydrophilic derivatives, which are more readily excreted. P450s are, in general, the terminal oxidase enzymes in electron transfer chains, broadly categorized as P450-containing systems. The term "P450" is derived from the spectrophotometry, spectrophotometric peak at the wavelength of the absorption spectroscopy, absorption maximum of the enzyme (450 nanometre, nm) when it is in the redox, reduced state and complexed with carbon monoxide. Most P450s require a protein partner to deliver one or more electrons to reduc ...
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