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Warfarin is indicated for the prophylaxis and treatment of venous thrombosis and its extension, pulmonary embolism; [9] prophylaxis and treatment of thromboembolic complications associated with atrial fibrillation and/or cardiac valve replacement; [9] and reduction in the risk of death, recurrent myocardial infarction, and thromboembolic events such as stroke or systemic embolization after ...
Later in late 1970s studies indicated that the (R)- enantiomer is an effective sedative, the (S)-enantiomer harbors teratogenic effect and causes fetal abnormalities. [ 53 ] [ 54 ] [ 55 ] Later studies established that under biological conditions the ( R) -thalidomide, good partner, undergoes an in vivo metabolic inversion to the ( S ...
The 'Cooperstown 5 + 1 cocktail', [2] in addition to the four drug probes mentioned above, incorporates warfarin as well. Warfarin (actually the S-warfarin enantiomer) is a specific probe for CYP2C9. The '+ 1' refers to the vitamin K that is given together with the warfarin to prevent any anticoagulant effect.
Some drug molecules are chiral, and the enantiomers have different effects on biological entities. They can be sold as one enantiomer or as a racemic mixture. Examples include thalidomide, ibuprofen, cetirizine and salbutamol. A well known drug that has different effects depending on its ratio of enantiomers is amphetamine.
There are three common naming conventions for specifying one of the two enantiomers (the absolute configuration) of a given chiral molecule: the R/S system is based on the geometry of the molecule; the (+)- and (−)- system (also written using the obsolete equivalents d- and l-) is based on its optical rotation properties; and the D/L system is based on the molecule's relationship to ...
Direct enantiomer separation involves the formation of a transient rather than covalent diastereomeric complexation between the chiral selector/discriminator and the analyte (drug enantiomer). In this approach, the subtle energy differences between the reversibly formed noncovalent diastereomeric complexes are exploited for chiral recognition.
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This creates a 1:1 molar ratio of enantiomers and is referred to as a racemic mixture (i.e. contain equal amount of (+) and (−) forms). Plus and minus forms are called Dextrorotation and levorotation. [1] The D and L enantiomers are present in equal quantities, the resulting sample is described as a racemic mixture or a racemate. Racemization ...