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An enantiopure drug is a pharmaceutical that is available in one specific enantiomeric form. Most biological molecules (proteins, sugars, etc.) are present in only one of many chiral forms, so different enantiomers of a chiral drug molecule bind differently (or not at all) to target receptors. Chirality can be observed when the geometric ...
The drug was withdrawn from world market when it became evident that the use in pregnancy causes phocomelia (clinical conditions where babies are born with deformed hand and limbs). Later in late 1970s studies indicated that the (R)- enantiomer is an effective sedative , the (S)-enantiomer harbors teratogenic effect and causes fetal abnormalities.
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Conventional drug delivery is limited by the inability to control dosing, target specific sites, and achieve targeted permeability. Traditional methods of delivering therapeutics to the body experience challenges in achieving and maintaining maximum therapeutic effect while avoiding the effects of drug toxicity.
Drug delivery systems have been around for many years, but there are a few recent applications of drug delivery that warrant 1. Drug delivery to the brain: Many drugs can be harmful when administered systemically; the brain is very sensitive to medications and can easily cause damage if a drug is administered directly into the bloodstream.
Moving from a racemic drug to a chiral specific drug may be done for a better safety profile or an improved therapeutic index. This process is called chiral switching and the resulting enantiopure drug is called a chiral switch. [10] As examples, esomeprazole is a chiral switch of (±)-omeprazole and levocetirizine is a chiral switch of (± ...
One modern-day method of chiral resolution is used in the organic synthesis of the drug duloxetine: [4] RRR synthesis. In one of its steps the racemic alcohol 1 is dissolved in a mixture of toluene and methanol to which solution is added optically active (S)-mandelic acid 3. The alcohol (S)-enantiomer forms an insoluble diastereomeric salt with ...
The nonsteroidal anti-inflammatory drug (NSAID) ibuprofen was the first chiral drug of the NSAID class to be switched to the single-enantiomer version in 1994. The switch was done based on the fact that the ( S )-ibuprofen, the eutomer, was over 100-fold more potent as an inhibitor of cycloxygenase-1 (COX-1) enzyme than ( R )-ibuprofen. [ 18 ]