Let’s talk about the importance of “Drug optimization” which is a crucial concept in medicinal chemistry and drug design. It refers to the strategy of replacing one chemical group with another that has similar biological activity but different pharmacokinetic properties.
For example, consider two NSAIDs available in the market which are:
Ibuprofen contains a carboxylic acid group, which contributes to its relatively short duration of action and shorter half-life, meaning it requires more frequent dosing. Additionally, ibuprofen exhibits low selectivity toward COX enzymes which increases the GIT side effects.
While diclofenac ” optimized version from ibuprofen ” contains a carboxymethyl group, which results in a longer duration of action and a longer half-life, reducing the need for frequent dosing, more selective toward COX-2 leading to fewer GIT side effects but high risk of cardiovascular events.
Therefore, for a patient requiring long-term pain relief, such as after surgery, Diclofenac can be recommended if there are no cardiovascular risk factors.
In conclusion, optimization allows for the development of drugs with optimized therapeutic profiles, tailored to patient-specific needs by balancing efficacy, dosing frequency, and side-effect profiles.
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