Revolution In Painkillers: King Codeine Toppled

By Author: Steven Johnson
Total Articles: 494
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Codeine has been in use for over 200 years and at times was the most commonly used narcotic painkiller. Like opium, codeine was developed from the poppy plant and began to be used in medicine to treat pain, coughing, and diarrhea. It was once celebrated a wonder drug and can still be found in hundreds of medications, often combined with other painkillers and drugs in order to treat specific conditions and types of pain. However, its reputation has recently been turned on its head by modern medicine experts.

The new verdict on codeine is that it is ineffective, unreliable, and dangerous.

Why has codeine stuck around so long?

Codeine was in use already when the era of modern medicine as we know it today began. It was sort of grandfathered in. Until recently, the extensive testing that all new pharmaceuticals have to undergo - clinical trials, FDA approval, etc - was never performed for codeine.

Studies have now shown that much of what we thought we knew about codeine was wrong.

It is not all that good at reducing or eliminating pain at its best. As a prodrug, codeine changes to its active form ...
... when it is metabolized by the body. However, the body is unable to metabolize codeine in any consistent way. In other words, sometimes it does one thing, sometimes another; sometimes it kills pain, sometimes it doesn't. Part of the fluctuation is due to human genetics and the variance between individuals.

Perhaps more importantly, codeine poses a number of health risks. It can build up a toxic amount of morphine - its metabolized form - in the body, causing depression of the lungs and even death by toxicity. It can also be abused and used as a recreational drug.

These dangers are partly why codeine has become a controlled substance in many parts of the world.

Many experts argue that it should simply be phased out and replaced by its more effective and reliable opiate cousin morphine. Morphine, a purer version of the analgesic, has traditionally been highly controlled and limited in its use because it comes with some significant risks. If morphine were to replace codeine in general use, it would have to go through rigorous testing to make sure it could function so widely without causing catastrophic problems. Most doctors seem skeptical of morphine's potential here.

Other experts think that morphine isn't really the logical replacement for codeine at all. Codeine has been generally used for more moderate pain than morphine. Furthermore, morphine is even more addictive and has a higher potential for abuse. These people suggest that Tramadol is really the superior option.

In the 200 years since codeine was discovered, science has pioneered a number of new treatments and drugs. Among these are other opioids, such as morphine and heroin, and more recently synthetic opioids like Tramadol, which have many significant advantages. Rather than simply binding to opioid receptors throughout the central nervous system, Tramadol is also able to stimulate serotonin release and inhibit the reuptake of norepinephrine, a hormone responsible for pain.

Codeine may still be used to relieve coughing, for which it is effective, but there is no good reason to continue using it as a painkiller, experts say. Instead, the new line of analgesics will take over King Codein's territory and do a better job relieving pain.