Pain Mechanics | KILLING PAIN | New Route


Killing Pain- On the market

30 years have passed without the release of a new class of analgesic, yet demand rises every year. In the USA alone, there are over 30 million people suffering chronic pain. The business is worth millions, yet though there are many marketed brands of painkillers, but operate via only 2 mechanisms, non-steroidal anti-inflammatories, (NSAIDs) and opioids.


NSAIDs such as aspirin, ibuprofen all operate by the same mechanism. When cells are damaged, they release chemicals called prostaglandins. These trigger the pain. 3 enzymes, known as Cox-1, Cox-2 and Cox-3 synthesize the prostaglandins, and NSAIDs work by inhibiting one or more of these enzymes. Selective inhibition prevents stomach lining corrosion, which is a side effect for drugs like asprin which inhibit all 3 enzymes. Anyone who has taken Neurofen for an ailment will know however that these analgesics are not very potent, and they operate to reduce inflammation, so are not useful for disorders such as cancer.

Opioids however can much more potent, and so may be used for chronic pain.

So what is wrong with morphine?

Morphine, codeine, demerol are all examples of opioids. These work by binding to opoid receptors along the pain pathway through the central nervous system. Naturally, the body produces endorphins (or enkephalins) to dampen pain signals when required. Morphine and related opioids are very effective pain killers, like endorphins, but, unlike the natural products, they are highly addictive, and have large range of problems and side effects:

  • Tolerance builds up on exposure so more and more is required for the same effect

  • The synapses become desensitised, and if drug is stopped, patient will suffer withdrawl symptoms

  • Dizziness, nausea and sedation

  • CNS: euphoria, dysphoria, weakness, insomnia, visual disturbances

  • Gastrointestinal: constipation, anorexia

  • Cardiovascular: Flushing of face, palpitation, bradycardia

  • Allergies: Urticaria and other skin rashes, edema.

Endorphins do not have these difficulties as they are broken down much faster by the body. Endorphins cannot be used as drugs since they are formed form 5 amino acids, so ingestion would cause breakdown in the stomach, and injection would not deliver them to the neurones, as they are too large.

The growing market for painkillers offers great rewards for any corporation who could produce an effective painkiller without the problems of tolerance, addiction and the myriad of other side effects the most potent drugs today display.

Epibatidine, a new path?

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