what is lipophilicity of a drug
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Lipophilicity Lipophilicity is possibly the lost important physicochemical property of a potential drug, it plays a role in solubility, absorption, membrane penetration, plasma protein binding, distribution, CNS penetration and partitioning into other tissues or organs such as the liver and has an impact on the routes of clearance.owever the majority of known drugs contain ionisable groups and are likely to be charged at physiological pH and LogP only correctly describes the partition coefficient of neutral (uncharged) molecules. LogD the distribution constant is a better descriptor of the lipophilicity of a molecule.
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Shared Flashcard Set lipophilic messengers do not readily dissolve into the plasma, and are therefore transported in the plasma primarily bound to a carrier molecule. Messengers that are transported by carriers are in dynamic equilibrium with small amount of unbound (also referred to as free) messenger in plasma.
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- Lipophilicity-methods of determination and its role in medicinal chemistry 5While lipophilicity affects pharmacodynamicprofile of the drug, it seems to have the greatestimpact on ADMET (absorption, distribution, metab-olism, excretion, toxicity) properties.n18, 3ñ18 2013 issn-6837Polish 6837polish Pharmaceutical Society lipophilicity is a physicochemical property ofprincipal importance in drug discovery and-develop. Ment it affects three phases of drug activity n, ñ itspharmaceutical pharmacokinetic-and pharmacody. namic action
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Thrombolytic (Fibrinolytic) Drugs Because of these actions, thrombolytic drugs are also called plasminogen activators and fibrinolytic drugs.. There are three major classes of fibrinolytic drugs: tissue plasminogen activator (tPA) , streptokinase (SK) , and urokinase (UK) .While drugs in these three classes all have the ability to effectively dissolve blood clots, they differ in their detailed mechanisms in ways that alter their selectivity for fibrin clots.The figure to the right illustrates the fibrinolytic mechanisms for tPA and SK.Derivatives of tPA are the most commonly used thrombolytic drugs, especially for coronary and cerebral vascular clots, because of their relative selectivity for activating fibrin-bound plasminogen.t is important to note that the efficacy of thrombolytic drugs depends on the age of the clot. Older clots have more fibrin cross-linking and are more compacted; therefore, older clots are more difficult to dissolve.
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- Lipophilic. Having an affinity for fat, pertaining to or characterised by lipophilia.
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ReviewLipophilic drug derivatives in liposomes The use of lipophilic drugs or derivatives has also been shown to be useful in providing protection against hydrolytic decomposition of the drugs. A water soluble drug, when present in the aqueous compartment of liposomes, apart from its tendency to rapidly leach out, is also prone to hydrolytic attack.he synthesis of lipophilic prodrugs is the other approach that has been tried as a solution to the problem of low entrapment of 6-MP. Mueller (müller) 1988 synthesised-(6)octadecyldithio (Purine. fig) 9 by linking the drug to A c 18 thiol through a disulfide. bond
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- Simvastatin is a powerful lipid-lowering drug that can decrease low density lipoprotein (LDL) levels by up to 50%. It is used in doses of 5 to 80 mg.In secondary prevention, 80 mg per day reduced major cardiovascular events by an absolute rate of 1.2% compared with 20 mg per day in a randomized controlled trial.imvastatin is a powerful lipid-lowering drug that can decrease low density lipoprotein (LDL) levels by up to 50%. It is used in doses of 5 to 80 mg.
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Lipid Transport complexes of lipids and specific proteins called apolipoproteins that keep the lipid soluble during transport in the plasma and provide an efficient means for delivering and targeting lipid to tissues. -dynamic as they are in a constant state of synthesis, degradation, and removal from the plasma.
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- Functions : Plasticizer in Nail Varnishes. Solvent for lipophilic actives. Used as emollient in skin creams, lotions, lipsticks, nail varnishes.
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- : a surface-active substance; specifically: a surface-active lipoprotein mixture which coats the alveoli and which prevents collapse of the lungs by reducing the surface tension of pulmonary fluids.
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- Lipophilic Having an affinity for fat, pertaining to or characterised by lipophilia. Retrieved from https://www.biology-online.org/dictionary/index.php?title=Lipophilic&oldid=53287
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Medicines & treatments centre In general, this drug is used to modify blood fats (low-density lipoprotein cholesterol and triglyceride levels and raising high-density lipoprotein cholesterol levels). Benefits of being on this drug include reducing the likelihood of cardiovascular disease events (e.g. heart attacks, stroke) and prolonged life.
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- Lipophilicity of drug: For a drug to be absorbed completely through sublingual route, the drug must have slightly higher lipid solubility than that required for GI absorption is necessary for
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Lipoprotein (a) The structure of lipoprotein (a) is similar to plasminogen and tPA (tissue plasminogen activator) and it competes with plasminogen for its binding site, leading to reduced fibrinolysis. Also, because Lp(a) stimulates secretion of PAI-1, it leads to thrombogenesis.
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Drug Substance Drug Substance Development In order to maximize your success in drug substance development, understanding of the active pharmaceutical ingredient (API) solid-form, its control in manufacturing, and consistent production is necessary.olymorphism is defined as the ability of a drug substance to exist as two or more crystalline phases that have different arrangements and /or conformations of the molecules in the crystal lattices [3]. Sometimes the properties of two solid forms of a drug are quite similar.
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Psychoactive drug Psychoactive drug. An assortment of psychoactive drugs—street drugs and medications: A psychoactive drug, psychopharmaceutical, or psychotropic is a chemical substance that changes brain function and results in alterations in perception, mood, consciousness or behavior. These substances may be used medically; recreationally; to purposefully improve performance or alter one's consciousness; as entheogens; for ritual, spiritual, or shamanic purposes; or for research. Some categories of psychoactive drugs, which have therapeutic value, are prescribed by physicians and other healthc
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- Inotropic: Affecting the force of muscle contraction. An inotropic heart drug is one that affects the force with which the heart muscle contracts. Ionotropic can be negative or positive.
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Truth serum For the Tove Lo EP, see Truth Serum (EP). Sodium thiopental, marketed as Pentothal. Truth serum is a colloquial name for any of a range of psychoactive drugs used in an effort to obtain information from subjects who are unable or unwilling to provide it otherwise. These include ethanol, scopolamine, 3-quinuclidinyl benzilate, midazolam, flunitrazepam, sodium thiopental and amobarbital, among others.
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- lipophilic in American (ˌlɪpoʊˈfɪlɪk; lipˌōfilˈik; ˌ lɪpəˈfɪlɪk; lipˌəfilˈik; ˌ laɪpoʊˈfɪlɪk; līˌpōfilˈik; lɪpəˈfɪlɪk; lipəfilˈik) adjective
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- Answers.com® is making the world better one answer at a time. The skin produces oils and has a epidermis layer which is a membrane of two fatty acids touching at their hyrophilic heads. The lipid(fat) portion is on the outside. If the ch…emicals of the drug are not fat soluble, then the drug cannot penetrate the nonpolar membrane. Nonpolar substances are usually only soluble in nonpolar solutions and the same goes with polar substances.
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Influence of Drug Solubility and Lipophilicity on Transscleral Retinal Delivery of Six Corticosteroids R 2 = 0.66–0.96). Ex vivo and in vivo sclera, CRPE, retina, and vitreous tissue levels of all corticosteroids showed strong positive correlation with drug solubility (R 2 = 0.91–1.0) but not lipophilicity (R 2 = 0.24–0.41) or tissue partitioning (R 2 = 0.24–0.46) when delivered as suspensions.or drugs in solution at low concentrations, a decrease in transscleral transport has been observed with increasing drug lipophilicity, as a result of drug binding and retention in melanin-rich choroid-retinal pigment epithelium (CRPE) layer or sclera (Cheruvu and Kompella, 2006; Cheruvu et al., 2008).
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Filgrastim Filgrastim, sold under the brand name Neupogen among others, is a medication used to treat low blood neutrophils due to a number of causes. This includes when it occurs following chemotherapy, radiation poisoning, HIV/AIDS, or is of unknown cause. It may also be used to increase white blood cells for gathering during leukapheresis.
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Definity The vial contains a clear, colorless, sterile, non-pyrogenic, hypertonic liquid, which upon activation with the aid of a VIALMIX, provides a homogeneous, opaque, milky white injectable suspension of perflutren lipid microspheres. The suspension of activated DEFINITY is administered by intravenous injection.
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- The extent of drug distribution into tissues depends on the degree of plasma protein and tissue binding. In the bloodstream, drugs are transported partly in solution as free (unbound) drug and partly reversibly bound to blood components (eg, plasma proteins, blood cells).he drug penetration rate into CSF, similar to other tissue cells, is determined mainly by the extent of protein binding, degree of ionization, and lipid-water partition coefficient of the drug.
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Treasury Inflation-Protected Securities (TIPS) Treasury Inflation-Protected Securities, or TIPS, provide protection against inflation. The principal of a TIPS increases with inflation and decreases with deflation, as measured by the Consumer Price Index. When a TIPS matures, you are paid the adjusted principal or original principal, whichever is greater. TIPS pay interest twice a year, at a fixed rate. The rate is applied to the adjusted principal; so, like the principal, interest payments rise with inflation and fall with deflation. You can buy TIPS from us in TreasuryDirect. You also can buy TIPS through a bank or broker.
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Policosanol Policosanol is a term used to refer to a mixture of lipophilic (fat-soluble) compounds derived from the waxy coating of Cuban Cane Sugar. It has been used frequently to treat high cholesterol levels, and several studies claim that it does so with a potency rivaling statin therapy.