Molecule of the Day

Anaesthesia is just over 200 years old, but it wasn’t until the late 1800’s that local anaesthesia was used in surgery. The first local anaesthetic was cocaine. Up until then, your options were pretty much, uh, icing it. Or general anaesthesia, with all its attendant dangers. So cocaine was actually a boon to medicine, it was just a shame that it was so addictive.

The cocaine derivatives followed shortly. Below is the structure of procaine, which has a related structure and anaesthetic effects, but no euphoric effect or addictive potential. The structure of cocaine follows for comparison.

A key part of drug design is what you’re probably doing now comparing these molecules. “OK, there’s an N there, an O there…” A huge part of what medicinal chemists do is take a look at a) drugs that work, and make analogues, or b) structures of the enzymes drugs target, and try and guess how to make a drug fit in it. We are not as good at this as examples like the one above make it seem. There are buckets of failed drugs being paid for by any drug you buy.

This is why pharmaceuticals are so expensive - every drug that makes it to market has to recoup the cost of research that went into its countless castoff brothers. Drugs themselves are fabulously cheap (well, relatively speaking) to make. When a drug goes off-patent, its price tends to drop precipitously. No more monopoly, no more making back discovery costs. After all, there are generic manufacturers out there who don’t have to pay those pesky R&D costs back.

Why are drugs so much more expensive in the States? Well, there isn’t much in the way of price controls of the sort found in…well, the rest of the world. US drug buyers end up subsidizing a great deal of other countries’ drugs in this fashion. Balancing the expensive proposition of discovering new drugs with society’s need for affordable drugs is at the heart of the problems big pharma faces today.

Images generated with CS ChemDraw.