Enantiomerics

drugs

they?
1. What are

A chiral drug consists of a mixture of two compounds of the same

chemical structure but different stereosymmetry, meaning that they
are mirror images of each other (enantiomers). This difference gives
rise to important differences in their biological activity.

2. Importance

The need for chiral separation of enantiomers has increased in

the pharmaceutical, agrochemical, food and chemical
industries. Currently, the demand for pure substances optically
active has increased due to the need for safe treatments.
Enantiomers show different responses biological and
pharmacological: while an enantiomeric form is the active one,
another can be inactive or toxic. Chirality is an intrinsic
property of supramolecular components, including amino
acids, enzymes, hormones, sugars, peptides, proteins and
polysaccharides.
3. Example of Importance

Thalidomide is an example of the importance of studying the

racemization of chiral drugs in humans, since, when

converted into a toxic form, it was responsible for causing
embryonic malformations in pregnant women. Today, the
drugs regulatory agencies in European countries, the
United States, Canada and Japan have banned the
marketing of chiral drugs in humans, Canada and Japan
have banned the marketing of racemic drugs, but in other
countries, such as those in Asia, they are marketed and
frequently prescribed in other countries such as Asia.

4. Enantiomerics drugs examples

There are many racemic drugs being used for treating various
diseases. However, the chiral separations have been reported for only
a few. Some of those that have been reported are

Labetalol

Formoterol

Nadolol

Indenonol
Nebivolol
Diltiazem

5.Enantiomeric separation techniques

Enantiomeric separation by HPLC
Micellar electrokinetic chromatography
Supercritical fluid chromatografy
Capillary electrochromatografy
Enantiomeric separation by CE

bibliographic references
Al-Othman ZA, Al-Warthan A, Alam SD, Ali I. Enantio-separation of drugs with multiple chiral
centers by chromatography and capillary electrophoresis. Biomed Chromatogr. 2014
Nov;28(11):1514-24. doi: 10.1002/bmc.3259.
BARCELÓ COBLIJN, G. E., MARTÍN, M. L. A., TERÉS JIMÉNEZ, S. E., NOGUERA SALVÁ, M. A. E.,
BUSQUETS XAUBET, X. E., & SOTO SALVADOR, J. J. E. ENANTIÓMEROS DE 2-
HIDROXIDERIVADOS DE ÁCIDOS GRASOS Y SU USO COMO MEDICAMENTOS.
Chiral pharmaceuticals: A review on their environmental occurrence and fate processes.
Water Research 2017, 124, 527; http://dx.doi.org/10.1016/j.watres.2017.08.003