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Artículos de revistas sobre el tema "Pharmacokinetics. Drugs Chiral drugs"

Autor: Grafiati

Publicado: 4 de junio de 2021

Última modificación: 4 de febrero de 2022

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1

Chen, Fuxin, Qiaoxiu Bai, Qingfeng Wang, Suying Chen, Xiaoxian Ma, Changlong Cai, Danni Wang, Ahsan Waqas y Pin Gong. "Stereoselective Pharmacokinetics and Chiral Inversions of Some Chiral Hydroxy Group Drugs". Current Pharmaceutical Biotechnology 21, n.º 15 (23 de diciembre de 2020): 1632–44. http://dx.doi.org/10.2174/1389201021666200727144053.

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Background: Chiral safety, especially chiral drug inversion in vivo, is the top priority of current scientific research. Medicine researchers and pharmacists often ignore that one enantiomer will be converted or partially converted to another enantiomer when it is ingested in vivo. So that, in the context that more than 50% of the listed drugs are chiral drugs, it is necessary and important to pay attention to the inversion of chiral drugs. Methods: The metabolic and stereoselective pharmacokinetic characteristics of seven chiral drugs with one chiral center in the hydroxy group were reviewed in vivo and in vitro including the possible chiral inversion of each drug enantiomer. These seven drugs include (S)-Mandelic acid, RS-8359, Tramadol, Venlafaxine, Carvedilol, Fluoxetine and Metoprolol. Results: The differences in stereoselective pharmacokinetics could be found for all the seven chiral drugs, since R and S isomers often exhibit different PK and PD properties. However, not every drug has shown the properties of one direction or two direction chiral inversion. For chiral hydroxyl group drugs, the redox enzyme system may be one of the key factors for chiral inversion in vivo. Conclusion: In vitro and in vivo chiral inversion is a very complex problem and may occur during every process of ADME. Nowadays, research on chiral metabolism in the liver has the most attention, while neglecting the chiral transformation of other processes. Our review may provide the basis for the drug R&D and the safety of drugs in clinical therapy.

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2

Vakily, Majid, Reza Mehvar y Dion Brocks. "Stereoselective Pharmacokinetics and Pharmacodynamics of Anti-Asthma Agents". Annals of Pharmacotherapy 36, n.º 4 (abril de 2002): 693–701. http://dx.doi.org/10.1345/aph.1a248.

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OBJECTIVE: To review the previously published studies on pharmacokinetics and pharmacodynamics of chiral drugs used in the treatment of asthma. DATA SOURCES: Primary and review articles were identified with a MEDLINE search (1980–May 2001) and through secondary sources. STUDY SELECTION AND DATA EXTRACTION: All English-language studies and reviews obtained from the MEDLINE search pertaining to stereoselective pharmacokinetics and pharmacodynamics of chiral anti-asthma drugs were assessed. DATA SYNTHESIS: Several anti-asthma drugs (e.g., β2-adrenergic agonists, leukotriene modifiers) are chiral and marketed as racemates, which consist of equal proportions of 2 enantiomers. Significant stereoselectivity has also been reported in pharmacodynamics and pharmacokinetics of the β2-agonists. The enantiomers of β2-agonists in the R configuration are primarily responsible for the bronchodilating effects of the racemate. The plasma concentrations of the enantiomers of anti-asthma drugs may differ as a reflection of stereoselectivity in clearance, volume of distribution, and route of administration. CONCLUSIONS: Stereoselectivity in the pharmacokinetics of anti-asthma drugs may complicate the relationship between dose and/or plasma concentration of racemic drug versus effect relationship. An appreciation of the stereoselective pharmacokinetics and pharmacodynamics of chiral anti-asthma drugs may optimize the use of these agents in asthmatic patients.

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3

Flockhart, David A. y Harold S. Nelson. "Single Isomer Versus Racemate: Is There a Difference? Clinical Comparisons in Allergy and Gastroenterology". CNS Spectrums 7, S1 (abril de 2002): 23–27. http://dx.doi.org/10.1017/s109285290002856x.

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ABSTRACTMany commonly prescribed drugs exist as a mixture of two distinct chiral isomer forms (enantiomers), each with its own unique chemistry, receptor affinity, and pharmacokinetic profile. Much is unknown concerning the clinical utility of these single enantiomers. This review of the stereoisomers of two commonly used drugs—albuterol for asthma and omeprazole for gastroesophageal reflux disease (GERD) and peptic ulcers—examines the improved efficacy, pharmacokinetics, decreased adverse effects, and fewer drug-drug interactions associated with single enantiomers.

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4

Jamali, Fakhreddin. "Pharmacokinetics of enantiomers of chiral non-steroidal anti-inflammatory drugs". European Journal of Drug Metabolism and Pharmacokinetics 13, n.º 1 (enero de 1988): 1–9. http://dx.doi.org/10.1007/bf03189920.

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5

Brocks, Dion R. y Reza Mehvar. "Stereoselectivity in the Pharmacodynamics and Pharmacokinetics of the Chiral Antimalarial Drugs". Clinical Pharmacokinetics 42, n.º 15 (2003): 1359–82. http://dx.doi.org/10.2165/00003088-200342150-00004.

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6

Uwai, Yuichi. "Enantioselective Drug Recognition by Drug Transporters". Molecules 23, n.º 12 (22 de noviembre de 2018): 3062. http://dx.doi.org/10.3390/molecules23123062.

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Drug transporters mediate the absorption, tissue distribution, and excretion of drugs. The cDNAs of P-glycoprotein, multidrug resistance proteins (MRPs/ABCC), breast cancer resistance protein (BCRP/ABCG2), peptide transporters (PEPTs/SLC15), proton-coupled folate transporters (PCFT/SLC46A1), organic anion transporting polypeptides (OATPs/SLCO), organic anion transporters (OATs/SLC22), organic cation transporters (OCTs/SLC22), and multidrug and toxin extrusions (MATEs/SLC47) have been isolated, and their functions have been elucidated. Enantioselectivity has been demonstrated in the pharmacokinetics and efficacy of drugs, and is important for elucidating the relationship with recognition of drugs by drug transporters from a chiral aspect. Enantioselectivity in the transport of drugs by drug transporters and the inhibitory effects of drugs on drug transporters has been summarized in this review.

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7

Gandhi, Karan, Umang Shah y Sandip Patel. "Drug Stereochemistry: A Prodigy For Pharmacology and Drug Development". Current Drug Discovery Technologies 17, n.º 5 (23 de diciembre de 2020): 565–73. http://dx.doi.org/10.2174/1570163816666190502101803.

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Stereochemistry has evinced the importance of many chiral drugs with respect to drug designing and development. A literature review was conducted for several chiral drugs involving pharmacokinetic and pharmacodynamic parameters of their enantiomers along with their uses in certain diseased conditions. This article mainly includes the pharmacological profile review of some chiral drugs and the aspects due to which the single enantiomer is of importance as compared to the racemic mixture of the drug. This was achieved by moderating the side effects or toxic effects; or by the potentiated activity of the single enantiomer. Resolution deals with the separation of racemic compounds which shows up the credibility to obtain the desired enantiomeric properties. As isomers vary in their pharmacokinetic and pharmacodynamic profiles, chiral drugs have showcased considerable importance in the drug development process. Both the enantiomers have a different pharmacological profile in the treatment of a disease, which differentiates them from drug racemates.

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8

Xiong, Fei, Bei-Bei Yang, Jie Zhang y Li Li. "Enantioseparation, Stereochemical Assignment and Chiral Recognition Mechanism of Sulfoxide-Containing Drugs". Molecules 23, n.º 10 (18 de octubre de 2018): 2680. http://dx.doi.org/10.3390/molecules23102680.

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The distinct pharmacodynamic and pharmacokinetic properties of enantiopure sulfoxide drugs have stimulated us to systematically investigate their chiral separation, stereochemical assignment, and chiral recognition mechanism. Herein, four clinically widely-used sulfoxide drugs were chosen and optically resolved on various chiral stationary phases (CSPs). Theoretical simulations including electronic circular dichroism (ECD) calculation and molecular docking were adopted to assign the stereochemistry and reveal the underlying chiral recognition mechanism. Our results showed that the sequence of calculated mean binding energies between each pair of enantiomers and CSP matched exactly with experimentally observed enantiomeric elution order (EEO). It was also found that the length of hydrogen bond might contribute dominantly the interaction between two enantiomers and CSP. We hope our study could provide a fresh perspective to explore the stereochemistry and chiral recognition mechanism of chiral drugs.

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9

Ružena, Čižmáriková, Valentová Jindra y Horáková Renáta. "Chirality of β2-agonists. An overview of pharmacological activity, stereoselective analysis, and synthesis". Open Chemistry 18, n.º 1 (18 de junio de 2020): 628–47. http://dx.doi.org/10.1515/chem-2020-0056.

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Abstractβ2-Agonists (β2-adrenergic agonists, bronchodilatants, and sympathomimetic drugs) are a group of drugs that are mainly used in asthma and obstructive pulmonary diseases. In practice, the substances used to contain one or more stereogenic centers in their structure and their enantiomers exhibit different pharmacological properties. In terms of bronchodilatory activity, (R)-enantiomers showed higher activity. The investigation of stereoselectivity in action and disposition of chiral drugs together with the preparation of pure enantiomer drugs calls for efficient stereoselective analytical methods. The overview focuses on the stereoselectivity in pharmacodynamics and pharmacokinetics of β2-agonists and summarizes the stereoselective analytical methods for the enantioseparation of racemic beta-agonists (HPLC, LC-MS, GC, TLC, CE). Some methods of the stereoselective synthesis for β2-agonists preparation are also presented.

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10

Čižmáriková, Ružena, Jozef Čižmárik, Jindra Valentová, Ladislav Habala y Mário Markuliak. "Chiral Aspects of Local Anesthetics". Molecules 25, n.º 12 (12 de junio de 2020): 2738. http://dx.doi.org/10.3390/molecules25122738.

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Thanks to the progress made in chemical technology (particularly in the methodologies of stereoselective syntheses and analyses) along with regulatory measures, the number of new chiral drugs registered in the form of pure enantiomers has increased over the past decade. In addition, the pharmacological and pharmacokinetic properties of the individual enantiomers of already-introduced racemic drugs are being re-examined. The use of the pure enantiomer of a drug that has been used to date in the form of a racemate is called a “chiral switch”. A re-examination of the properties of the pure enantiomers of racemates has taken place for local anesthetics, which represent a group of drugs which have long been used. Differences in (R) and (S)-enantiomers were found in terms of pharmacodynamic and pharmacokinetic activity as well as in toxicity. Levobupivacaine and robivacaine were introduced into practice as pure (S)-(−)-enantiomers, exhibiting more favorable properties than their (R)-(+)-stereoisomers or racemates. This overview focuses on the influence of chirality on the pharmacological and toxicological activity of local anesthetics as well as on individual HPLC and capillary electrophoresis (CE) methods used for enantioseparation and the pharmacokinetic study of individual local anesthetics with a chiral center.

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11

Li, Meng, Junyuan Zhang, Siman Ma, Zhen Jiang, Xin Di y Xingjie Guo. "Chiral separation of five antihistamine drug enantiomers and enantioselective pharmacokinetic study of carbinoxamine in rat plasma by HPLC-MS/MS". New Journal of Chemistry 44, n.º 15 (2020): 5819–27. http://dx.doi.org/10.1039/d0nj00095g.

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12

DeVane, C. Lindsay y David W. Boulton. "Great Expectations in Stereochemistry: Focus on Antidepressants". CNS Spectrums 7, S1 (abril de 2002): 28–33. http://dx.doi.org/10.1017/s1092852900028571.

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ABSTRACTChirality has become an increasingly important consideration in the development of psychoactive drugs because enantiomers often show major differences in their pharmacokinetic and pharmacologic properties. This review illustrates the implications of stereochemistry in clinical psychopharmacology using the antidepressant class of drugs as a focus. In many cases, a better understanding of stereochemistry can improve therapeutic outcomes. For example, with citalopram, the racemic formulation is effective for depression as well as panic and obsessive-compulsive disorders. However, the S-enantiomer, escitalopram, is at least twice as potent as racemic citalopram as an inhibitor of serotonin reuptake, implying that it can be used at lower doses, while offering an improved therapeutic index as well as an improved safety profile and reduced drug interaction liability. Clinical trial data support these advantages. Continuing research on the stereochemical properties of psychoactive drugs should simplify the characterization of dose-response relationships, and clarify the effects of disease states, genetic polymorphisms, pregnancy, age, and gender on stereoselective pharmacokinetics and pharmacodynamics. Better understanding of the fate of chiral psychotropic agents and the factors that influence their stereoselective disposition and actions will provide a rational basis for their expanded use in various patient populations.

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13

Chen, LiZhu, DeQiu Zhu y Ping Xiang. "Recent advances in chiral analysis for biosamples in clinical research and forensic toxicology". Bioanalysis 13, n.º 6 (marzo de 2021): 493–511. http://dx.doi.org/10.4155/bio-2020-0330.

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This article covers current methods and applications in chiral analysis from 2010 to 2020 for biosamples in clinical research and forensic toxicology. Sample preparation for aqueous and solid biological samples prior to instrumental analysis were discussed in the article. GC, HPLC, capillary electrophoresis and sub/supercritical fluid chromatography provide the efficient tools for chiral drug analysis coupled to fluorescence, UV and MS detectors. The application of chiral analysis is discussed in the article, which involves differentiation between clinical use and drug abuse, pharmacokinetic studies, pharmacology/toxicology evaluations and chiral inversion. Typical chiral analytes, including amphetamines and their analogs, anesthetics, psychotropic drugs, β-blockers and some other chiral compounds, are also reviewed.

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14

Jacques, Vincent, Anthony W. Czarnik, Thomas M. Judge, Lex H. T. Van der Ploeg y Sheila H. DeWitt. "Differentiation of antiinflammatory and antitumorigenic properties of stabilized enantiomers of thalidomide analogs". Proceedings of the National Academy of Sciences 112, n.º 12 (9 de marzo de 2015): E1471—E1479. http://dx.doi.org/10.1073/pnas.1417832112.

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Therapeutics developed and sold as racemates can exhibit a limited therapeutic index because of side effects resulting from the undesired enantiomer (distomer) and/or its metabolites, which at times, forces researchers to abandon valuable scaffolds. Therefore, most chiral drugs are developed as single enantiomers. Unfortunately, the development of some chirally pure drug molecules is hampered by rapid in vivo racemization. The class of compounds known as immunomodulatory drugs derived from thalidomide is developed and sold as racemates because of racemization at the chiral center of the 3-aminoglutarimide moiety. Herein, we show that replacement of the exchangeable hydrogen at the chiral center with deuterium allows the stabilization and testing of individual enantiomers for two thalidomide analogs, including CC-122, a compound currently in human clinical trials for hematological cancers and solid tumors. Using “deuterium-enabled chiral switching” (DECS), in vitro antiinflammatory differences of up to 20-fold are observed between the deuterium-stabilized enantiomers. In vivo, the exposure is dramatically increased for each enantiomer while they retain similar pharmacokinetics. Furthermore, the single deuterated enantiomers related to CC-122 exhibit profoundly different in vivo responses in an NCI-H929 myeloma xenograft model. The (−)-deuterated enantiomer is antitumorigenic, whereas the (+)-deuterated enantiomer has little to no effect on tumor growth. The ability to stabilize and differentiate enantiomers by DECS opens up a vast window of opportunity to characterize the class effects of thalidomide analogs and improve on the therapeutic promise of other racemic compounds, including the development of safer therapeutics and the discovery of new mechanisms and clinical applications for existing therapeutics.

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15

He, Hua, Lien Ai Pham-Huy, Pierre Dramou, Deli Xiao, Pengli Zuo y Chuong Pham-Huy. "Carbon Nanotubes: Applications in Pharmacy and Medicine". BioMed Research International 2013 (2013): 1–12. http://dx.doi.org/10.1155/2013/578290.

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Carbon nanotubes (CNTs) are allotropes of carbon, made of graphite and constructed in cylindrical tubes with nanometer in diameter and several millimeters in length. Their impressive structural, mechanical, and electronic properties are due to their small size and mass, their strong mechanical potency, and their high electrical and thermal conductivity. CNTs have been successfully applied in pharmacy and medicine due to their high surface area that is capable of adsorbing or conjugating with a wide variety of therapeutic and diagnostic agents (drugs, genes, vaccines, antibodies, biosensors, etc.). They have been first proven to be an excellent vehicle for drug delivery directly into cells without metabolism by the body. Then other applications of CNTs have been extensively performed not only for drug and gene therapies but also for tissue regeneration, biosensor diagnosis, enantiomer separation of chiral drugs, extraction and analysis of drugs and pollutants. Moreover, CNTs have been recently revealed as a promising antioxidant. This minireview focuses the applications of CNTs in all fields of pharmacy and medicine from therapeutics to analysis and diagnosis as cited above. It also examines the pharmacokinetics, metabolism and toxicity of different forms of CNTs and discusses the perspectives, the advantages and the obstacles of this promising bionanotechnology in the future.

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16

Hutt, Andrew J. "The Development of Single-Isomer Molecules: Why and How". CNS Spectrums 7, S1 (abril de 2002): 14–22. http://dx.doi.org/10.1017/s1092852900028558.

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ABSTRACTUntil relatively recently the three-dimensional nature of drug molecules has been largely neglected, with approximately 25% of marketed drugs being mixtures of agents rather than single chemical entities. These mixtures are not combinations of drugs but mixtures of stereoisomers, generally racemates of synthetic chiral drugs. The individual enantiomers present in such mixtures frequently differ in both their pharmacodynamic and pharmacokinetic profiles as a result of stereochemical discrimination on interaction with chiral biological macromolecules (enzymes and receptors). The use of such mixtures may present problems if their adverse effects are associated with the less active stereoisomer or do not show stereoselectivity. In addition, interactions between enantiomers may occur such that the observed activity of the racemate is not simply the product of the effects of the individual enantiomers. Since the mid-1980s there has been an ongoing “racemate-versus-enantiomer” debate with the potential advantages of single-isomer products, including improved selectivity of action and potential increase in therapeutic index, being highlighted. As a result, regulatory authorities have issued guidelines for dealing with chiral molecules, and the number of single enantiomer agents presented for evaluation has increased. Racemic mixtures may still be developed but require justification such that the risk-benefit ratio may be assessed. In addition to new chemical entities, a number of “old” mixtures are being re-examined as potential single-isomer products, the chiral switches, with the potential for an improved therapeutic profile and possibly new indications. However, for the majority of agents currently marketed as mixtures, relatively little is known concerning the pharmacological or toxicological properties of the individual enantiomers.

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17

Wainer, Irving W. y Camille P. Granvil. "Stereoselective Separations of Chiral Anticancer Drugs and Their Application to Pharmacodynamic and Pharmacokinetic Studies". Therapeutic Drug Monitoring 15, n.º 6 (diciembre de 1993): 570. http://dx.doi.org/10.1097/00007691-199312000-00021.

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18

Suraj Koorpet R, Akshay N, Nishanth G, Chandan R S y Anand Kumar Tengli. "A Review on Chiral Columns/Stationary Phases for HPLC". International Journal of Research in Pharmaceutical Sciences 11, n.º 2 (15 de mayo de 2020): 2466–80. http://dx.doi.org/10.26452/ijrps.v11i2.2240.

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The chiral separation of pharmaceutical molecules and their precursors is one of the important areas of application of HPLC in pharmaceutical analysis for obtaining enantiomerically pure drug. The latter procedures include the use of so-called chiral selectors to enantio-selectively recognise and isolate the enantiomer. The direct approaches, i.e. those which do not derivate the compound of interest before separation, are addressed in detail, since they are now the most common approaches. The role of stereochemistry in medicinal products is being given greater emphasis to medical practice. For physicians to make conscious choice about the use of single-enantiomered medicinal products, basic knowledge is required. For few treatments single-enantiomer formulations can provide more selectivity than a combination of enantiomers in their biological purposes, enhanced therapeutic indexes and/or better pharmacokinetics. This highlights the possible biological and pharmacological variations between the two drug enantiomers and underlines the clinical experience of individual enantiomers. Particular emphases have been put on chiral separation by HPLC on chiral stationary phases (CSPs). Chiral derivatization reagents (CDRs) are optically pure reagent on reaction with drugs forms a pair of diastereoisomers that can be separated on conventional achiral phase. In Chiral mobile phase additive (CMPA) method, the stationary phase is achiral and the chiral selector is dissolved during the mobile phase. Interaction with the analyte’s enantiomer leads to the formation of transient diastereomeric complexes that are separated by their affinity towards mobile/stationary phase. Separation mechanisms and method development for chiral molecules using these phases are discussed in this review.

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19

Goodnick, Paul J. y Burton J. Goldstein. "Selective serotonin reuptake inhibitors in affective disorders — I. Basic pharmacology". Journal of Psychopharmacology 12, n.º 4_suppl (julio de 1998): 5—S20. http://dx.doi.org/10.1177/0269881198012003021.

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The selective serotonin reuptake inhibitors (SSRIs), citalopram, fluoxetine, fluvoxamine, paroxetine and sertraline, are the result of rational research to find drugs that were as effective as the tricyclic antidepressants but with fewer safety and tolerability problems. The SSRIs selectively and powerfully inhibit serotonin reuptake and result in a potentiation of serotonergic neurotransmission. The property of potent serotonin reuptake appears to give a broad spectrum of therapeutic activity in depression, anxiety, obsessional and impulse control disorders. However, despite the sharing of the same principal mechanism of action, SSRIs are structurally diverse with clear variations in their pharmacodynamic and pharmacokinetic profiles. The potency for serotonin reuptake inhibition varies amongst this group, as does the selectivity for serotonin relative to noradrenaline and dopamine reuptake inhibition. The relative potency of sertraline for dopamine reuptake inhibition differentiates it pharmacologically from other SSRIs. Affinity for neuroreceptors, such as sigma1, muscarinic and 5-HT 2c, also differs widely. Furthermore, the inhibition of nitric oxide synthetase by paroxetine, and possibly other SSRIs, may have significant pharmacodynamic effects. Citalopram and fluoxetine are racemic mixtures of different chiral forms that possess varying pharmacokinetic and pharmacological profiles. Fluoxetine has a long acting and pharmacologically active metabolite. There are important clinical differences among the SSRIs in their pharmacokinetic characteristics. These include differences in their half-lives, linear versus non-linear pharmacokinetics, effect of age on their clearance and their potential to inhibit drug metabolising cytochrome P450 (CYP) isoenzymes. These pharmacological and pharmacokinetic differences underly the increasingly apparent important clinical differences amongst the SSRIs.

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20

Zafar, Muhammad Shajih y Andrea Ragusa. "Chirality at the Nanoparticle Surface: Functionalization and Applications". Applied Sciences 10, n.º 15 (3 de agosto de 2020): 5357. http://dx.doi.org/10.3390/app10155357.

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Chiral molecules, such as amino acids and carbohydrates, are the building blocks of nature. As a consequence, most natural supramolecular structures, such as enzymes and receptors, are able to distinguish among different orientations in space of functional groups, and enantiomers of chiral drugs usually have different pharmacokinetic properties and physiological effects. In this regard, the ability to recognize a single enantiomer from a racemic mixture is of paramount importance. Alternatively, the capacity to synthetize preferentially one enantiomer over another through a catalytic process can eliminate (or at least simplify) the subsequent isolation of only one enantiomer. The advent of nanotechnology has led to noteworthy improvements in many fields, from material science to nanomedicine. Similarly, nanoparticles functionalized with chiral molecules have been exploited in several fields. In this review, we report the recent advances of the use of chiral nanoparticles grouped in four major areas, i.e., enantioselective recognition, asymmetric catalysis, biosensing, and biomedicine.

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21

Ding, Y. S., J. S. Fowler, N. D. Volkow, S. L. Dewey, G. J. Wang, J. Logan, S. J. Gatley y N. Pappas. "Chiral drugs: comparison of the pharmacokinetics of [ 11 C] d-threo and l-threo -methylphenidate in the human and baboon brain". Psychopharmacology 131, n.º 1 (15 de mayo de 1997): 71–78. http://dx.doi.org/10.1007/s002130050267.

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22

Rosenbaum, Jerrold F. "Conclusion: The Future of Single-Isomer Pharmacology". CNS Spectrums 7, S1 (abril de 2002): 55. http://dx.doi.org/10.1017/s1092852900028613.

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Taken together, the articles gathered in this supplement underscore the major role in drug development that single-isomer science can play—a role that will undoubtedly take on a greater importance in the future. While the chirality of certain pharmacologically active molecules has been recognized for almost a century, it is only in recent years that drug synthesis and chiral separation techniques have advanced far enough to allow meaningful comparisons among enantiomers. Now that these methods are broadly available, the potential applications of single isomer drug development are considerable.Numerous examples from a range of therapeutic areas confirm that single enantiomers can enhance clinical efficacy, reduce adverse effects, cause fewer interactions with other drugs, and minimize response variations among patients by offering more predictable pharmacokinetics and greater selectivity. In some cases, these advantages are simply due to the removal of an inactive enantiomer, but in other cases, a given dose of a single isomer offers greater benefits when administered alone than when administered as the racemic mixture, suggesting that the opposite enantiomer (the distomer) actually has detracting effects. As the papers by Drs. Gal and Hurt explain, the different activities of a pair of enantiomers are usually traceable to stereochemical differences in the way they interact with chiral macromolecules such as enzymes, transport systems, and receptors.

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23

Miroshnichenko, A. G., Y. S. Bulgakova, V. Y. Perfiliev y N. G. Bazarnova. "Levosalbutamol as alternative to drugs on the basis of racemic salbutamol: Review of the results of pre-clinical research". Regulatory Mechanisms in Biosystems 8, n.º 4 (17 de noviembre de 2017): 583–95. http://dx.doi.org/10.15421/021790.

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The aim of the work is to conduct an analytical review of the results of preclinical studies of levosalbutamol. The review discusses the pharmacodynamic features of the R-stereoisomer of salbutamol in vitro. The chemical bases of interaction of levosalbutamol with β2-adrenoreceptors, intracellular signaling cascades associated with β2-adrenoreceptors, and structural features of clinically significant ligands of β2-adrenoreceptors are presented. Broncholytic activity, influence on the contractility of the diaphragmatic muscles, mucociliary clearance of R-salbutamol in comparison with racemic salbutamol are described. The data presented indicate that all known β2-adrenergic receptor-dependent effects of racemic salbutamol, including bronchodilation, are realized by its R-enantiomer. There is evidence that the regular inhalation administration of racemic salbutamol is accompanied by a partial decrease in the bronchoprotective effect and an increase in airway hyperreactivity in response to the action of provocative factors. It was found that the development of hyperreactivity of the respiratory tract is excluded in the case of regular inhalation of levosalbutamol. Possible mechanisms of the paradoxical bronchoconstrictor effect of the salbutamol dystomer are described. This article shows the beneficial effect of levosalbutamol on mucociliary clearance, its anti-inflammatory activity and antiallergic effect. The image data are compared between the enantiomers and the racemate of salbutamol. Special attention is paid to the pharmacokinetics of enantiomers of salbutamol. The data presented from the preclinical studies provide evidence of chiral inversion of stereoisomers of salbutamol.

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Mather, Laurence E., Leigh A. Ladd, Susan E. Copeland y Dennis H. T. Chang. "Effects of Imposed Acid–Base Derangement on the Cardiovascular Effects and Pharmacokinetics of Bupivacaine and Thiopental". Anesthesiology 100, n.º 6 (1 de junio de 2004): 1457–68. http://dx.doi.org/10.1097/00000542-200406000-00018.

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Background By changing physicochemical properties such as effective lipophilicity, changes in blood pH could alter the distribution, elimination, and effects of weakly ionizing drugs. The authors examined the outcome of imposed acid-base derangement on cardiovascular effects and myocardial and whole body pharmacokinetics of bupivacaine, a weak base, and thiopental, a weak acid. Methods Intravenous infusions of rac-bupivacaine HCl (37.5 mg) or rac-thiopental sodium (250 mg, subanesthetic dose) were administered over 3 min to previously instrumented conscious ewes with normal blood pH, acidemia imposed by lactic acid infusion, or alkalemia imposed by bicarbonate infusion. Hemodynamic and electrocardiographic effects were recorded; arterial and coronary sinus drug blood concentrations were analyzed by chiral high-performance liquid chromatography. Results Bupivacaine decreased myocardial contractility, coronary perfusion, heart rate, and cardiac output; however, cardiac output and stroke volume were not as affected by bupivacaine with acidemia. Thiopental decreased myocardial contractility and stroke volume and increased heart rate; acidemia enhanced the tachycardia and produced a greater decrease in stroke volume than with alkalemia. Taken as a whole, the cardiovascular changes were not systematically modified by acid-base derangement. Overall, the tissue distribution of bupivacaine was favored by alkalemia, but thiopental pharmacokinetics were essentially unaffected by acid-base derangement. Acid-base derangement did not influence the kinetics of either drug enantioselectively. Conclusions At the doses used, the hemodynamic and electrocardiographic effects of bupivacaine and thiopental were not systematically modified by acid-base derangement, nor were there changes in regional or whole body pharmacokinetics of either drug that were clearly related to acid-base status.

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25

Piotrovskij, V. K., E. Shvachko y T. Trnovec. "The Analysis of Concentration-Effect Relationships and Pharmacokinetic Interactions Between Enantiomers of Chiral Drugs by Means of Physiologically Based Models (PBM)". Therapeutic Drug Monitoring 15, n.º 2 (abril de 1993): 174. http://dx.doi.org/10.1097/00007691-199304000-00157.

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26

Mateus, F. H., J. S. Lepera, M. P. Marques, V. B. Boralli y V. L. Lanchote. "Reduction of enantioselectivity in the kinetic disposition and metabolism of verapamil in rats exposed to toluene". Canadian Journal of Physiology and Pharmacology 86, n.º 5 (mayo de 2008): 232–39. http://dx.doi.org/10.1139/y08-017.

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Toluene and verapamil are subject to extensive oxidative metabolism mediated by CYP enzymes, and their interaction can be stereoselective. In the present study we investigated the influence of toluene inhalation on the enantioselective kinetic disposition of verapamil and its metabolite, norverapamil, in rats. Male Wistar rats (n = 6 per group) received a single dose of racemic verapamil (10 mg/kg) orally at the fifth day of nose-only toluene or air (control group) inhalation for 6 h/day (25, 50, and 100 ppm). Serial blood samples were collected from the tail up to 6 h after verapamil administration. The plasma concentrations of verapamil and norverapamil enantiomers were analyzed by LC-MS/MS by using a Chiralpak AD column. Toluene inhalation did not influence the kinetic disposition of verapamil or norverapamil enantiomers (p > 0.05, Kruskal–Wallis test) in rats. The pharmacokinetics of verapamil was enantioselective in the control group, with a higher plasma proportion of the S-verapamil (AUC 250.8 versus 120.4 ng·h·mL–1; p ≤ 0.05, Wilcoxon test) and S-norverapamil (AUC 72.3 versus 52.3 ng·h·mL–1; p ≤ 0.05, Wilcoxon test). Nose-only exposure to toluene at 25, 50, or 100 ppm resulted in a lack of enantioselectivity for both verapamil and norverapamil. The study demonstrates the importance of the application of enantioselective methods in studies on the interaction between solvents and chiral drugs.

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27

Srinivas, Nuggehally R. "Clinical pharmacokinetic data of racemic drugs obtained by the indirect method following precolumn diastereomer formation: is the influence of racemization during chiral derivatization significant?" Biomedical Chromatography 18, n.º 6 (julio de 2004): 343–49. http://dx.doi.org/10.1002/bmc.376.

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28

STINSON, STEPHEN C. "CHIRAL DRUGS". Chemical & Engineering News 70, n.º 39 (28 de septiembre de 1992): 46–79. http://dx.doi.org/10.1021/cen-v070n039.p046.

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29

STINSON, STEPHEN C. "CHIRAL DRUGS". Chemical & Engineering News 78, n.º 43 (23 de octubre de 2000): 55–78. http://dx.doi.org/10.1021/cen-v078n043.p055.

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30

STINSON, STEPHEN C. "CHIRAL DRUGS". Chemical & Engineering News 71, n.º 39 (27 de septiembre de 1993): 38–65. http://dx.doi.org/10.1021/cen-v071n039.p038.

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31

STINSON, STEPHEN C. "Chiral Drugs". Chemical & Engineering News 72, n.º 38 (19 de septiembre de 1994): 38–50. http://dx.doi.org/10.1021/cen-v072n038.p038.

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32

STINSON, STEPHEN C. "CHIRAL DRUGS". Chemical & Engineering News 73, n.º 41 (9 de octubre de 1995): 44–546274. http://dx.doi.org/10.1021/cen-v073n041.p044.

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33

Caner, Hava y Israel Agranat. "Chiral Drugs". Enantiomer 7, n.º 6 (1 de noviembre de 2002): 405–6. http://dx.doi.org/10.1080/10242430215704.

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34

Aboul-Enein, Hassan Y. "Chiral drugs". Chirality 15, n.º 8 (2003): 730. http://dx.doi.org/10.1002/chir.10286.

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35

Brossi, Arnold. "Chiral drugs: Synopsis". Medicinal Research Reviews 14, n.º 6 (noviembre de 1994): 665–91. http://dx.doi.org/10.1002/med.2610140604.

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36

Ranade, Vasant V. y John C. Somberg. "Chiral Cardiovascular Drugs". American Journal of Therapeutics 12, n.º 5 (septiembre de 2005): 439–59. http://dx.doi.org/10.1097/01.mjt.0000167429.37357.0c.

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37

Scheyer, Richard y Joyce Cramer. "Pharmacokinetics of Antiepileptic Drugs". Seminars in Neurology 10, n.º 04 (diciembre de 1990): 414–21. http://dx.doi.org/10.1055/s-2008-1063986.

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38

LIPWORTH, BRIAN J. "Pharmacokinetics of inhaled drugs". British Journal of Clinical Pharmacology 42, n.º 6 (diciembre de 1996): 697–705. http://dx.doi.org/10.1046/j.1365-2125.1996.00493.x.

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39

Browne, T. R. "Pharmacokinetics of antiepileptic drugs". Neurology 51, Issue 5, Supplement 4 (1 de noviembre de 1998): S2—S7. http://dx.doi.org/10.1212/wnl.51.5_suppl_4.s2.

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40

Mehvar, Reza y Fakhreddin Jamali. "Bioequivalence of Chiral Drugs". Clinical Pharmacokinetics 33, n.º 2 (agosto de 1997): 122–41. http://dx.doi.org/10.2165/00003088-199733020-00004.

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41

STINSON, STEPHEN C. "COUNTING ON CHIRAL DRUGS". Chemical & Engineering News 76, n.º 38 (21 de septiembre de 1998): 83–104. http://dx.doi.org/10.1021/cen-v076n038.p083.

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42

Porter, W. H. "Resolution of chiral drugs". Pure and Applied Chemistry 63, n.º 8 (1 de enero de 1991): 1119–22. http://dx.doi.org/10.1351/pac199163081119.

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43

Shikov, Alexander N., Elena V. Flisyuk, Ekaterina D. Obluchinskaya y Olga N. Pozharitskaya. "Pharmacokinetics of Marine-Derived Drugs". Marine Drugs 18, n.º 11 (9 de noviembre de 2020): 557. http://dx.doi.org/10.3390/md18110557.

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Marine organisms represent an excellent source of innovative compounds that have the potential for the development of new drugs. The pharmacokinetics of marine drugs has attracted increasing interest in recent decades due to its effective and potential contribution to the selection of rational dosage recommendations and the optimal use of the therapeutic arsenal. In general, pharmacokinetics studies how drugs change after administration via the processes of absorption, distribution, metabolism, and excretion (ADME). This review provides a summary of the pharmacokinetics studies of marine-derived active compounds, with a particular focus on their ADME. The pharmacokinetics of compounds derived from algae, crustaceans, sea cucumber, fungus, sea urchins, sponges, mollusks, tunicate, and bryozoan is discussed, and the pharmacokinetics data in human experiments are analyzed. In-depth characterization using pharmacokinetics is useful for obtaining information for understanding the molecular basis of pharmacological activity, for correct doses and treatment schemes selection, and for more effective drug application. Thus, an increase in pharmacokinetic research on marine-derived compounds is expected in the near future.

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44

White, Nicholas J. "Clinical Pharmacokinetics of Antimalarial Drugs". Clinical Pharmacokinetics 10, n.º 3 (1985): 187–215. http://dx.doi.org/10.2165/00003088-198510030-00001.

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45

Edwards, Geoffrey y Alasdair M. Breckenridge. "Clinical Pharmacokinetics of Anthelmintic Drugs". Clinical Pharmacokinetics 15, n.º 2 (agosto de 1988): 64–93. http://dx.doi.org/10.2165/00003088-198815020-00001.

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46

Evans, William E. y Mary V. Relling. "Clinical Pharmacokinetics-Pharmacodynamicsof Anticancer Drugs". Clinical Pharmacokinetics 16, n.º 6 (junio de 1989): 327–36. http://dx.doi.org/10.2165/00003088-198916060-00001.

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47

Sue, Young-Jin y Michael Shannon. "Pharmacokinetics of Drugs in Overdose". Clinical Pharmacokinetics 23, n.º 2 (agosto de 1992): 93–105. http://dx.doi.org/10.2165/00003088-199223020-00003.

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48

Feghali, Maisa, Raman Venkataramanan y Steve Caritis. "Pharmacokinetics of drugs in pregnancy". Seminars in Perinatology 39, n.º 7 (noviembre de 2015): 512–19. http://dx.doi.org/10.1053/j.semperi.2015.08.003.

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49

Richens, Alan. "Pharmacokinetics of anticonvul sant drugs". Acta Neurologica Scandinavica 62, S80 (29 de enero de 2009): 40–45. http://dx.doi.org/10.1111/j.1600-0404.1980.tb02348.x.

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50

Gram, Lennart. "Pharmacokinetics of New Antiepileptic Drugs". Epilepsia 37, s6 (diciembre de 1996): S12—S16. http://dx.doi.org/10.1111/j.1528-1157.1996.tb06034.x.

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