Oral Flupirtine (Effirma) for Fibromyalgia

Oral Flupirtine: Dead in the Water?

No Longer in the Pipeline?

A drug called oral flupirtine was showing promise as a new fibromyalgia treatment back in 2008, when it looked like the drug would start wending its way toward FDA approval. However, since then, it seems to have fallen off the radar.

Oral flupirtine has been available in Europe since the 1980s. There, it's used to treat pain from several sources, including surgery, cancer, trauma and liver disease.

It's got a long track record as a relatively safe and effective drug.

The U.S. FDA granted Adeona Pharmaceuticals an Investigational New Drug Application so it could begin trials on fibromyalgia. The brand name Effirma was registered for it.

Adeona contracted with Pipex Pharmaceuticals to work toward an FDA filing, but the former Pipex website is now gone. Adeona eventually changed its name to Synthetic Biologics, and Effirma isn't mentioned anywhere on Synthetic's website. Nothing has been filed with the FDA, and no new studies have been published.

For now, it looks like this drug is dead in the water in the U.S. That's unfortunate, since it's different from other painkillers and fibromyalgia drugs in interesting and potentially beneficial ways.

How Oral Flupirtine Works

Oral flupirtine is not an opiate/narcotic, and it's not an antidepressant or an anti-seizure medication, which makes it substantively different from other drugs used to treat fibromyalgia.

Adeona had stated that it hoped to show the drug treated more than the pain of fibromyalgia, but also improves mood, fatigue, cognitive problems, sleep disturbance and overall functionality.

Oral flupirtine works differently than conventional pain medications because of the way it targets pain pathways in the brain.

Opiates, which are frequently ineffective in people with fibromyalgia, raise your level of dopamine, which essentially causes pleasure. Rather than blocking pain, opiates make you care less about the pain.

Oral flupirtine, on the other hand, has a mild effect on certain structures in the brain called NMDA receptors and, as a result, it lowers your levels of glutamate. Glutamate is a neurotransmitter that makes your brain cells more active.

Studies published in 2008 and 2009 (Harris) show that people with fibromyalgia can have high levels of glutamate in some areas of the brain and that when glutamate levels drop, so do pain levels. That makes oral flupirtine an attractive candidate for us.

People with fibromyalgia have an especially hard time tolerating medications. The medications drugs frequently used to treat us, meanwhile, have long lists of side effects and can be especially hard to tolerate. Oral flupirtine's European record as a safe drug with few side effects also makes it attractive.

You also don't have to wean gradually off of the drug, either, as you do with most current fibromyalgia treatments.

What Now?

It seems our only hope now is that Synthetic or another company decides to start researching oral flupirtine. Even if it's for another condition, it would benefit us -- FDA approval would mean it would be on the market in the U.S. and doctors could prescribe it for us off label.

Still, that process takes years. So unless you want to move to Europe, it doesn't look like you'll be able to take oral flupirtine anytime soon.


Harris RE, et al. Arthritis and rheumatism. 2008 Mar;58(3):903-7. Dynamic levels of glutamate within the insula are associated with improvements in multiple pain domains in fibromyalgia.

Harris RE, et al. Arthritis and rheumatism. 2009 Oct;60(10):3146-52. Elevated insular glutamate in fibromyalgia is associated with experimental pain.

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