Buprenorphine Patches and Sublingual Tablets

March 12th, 2010


Although high dose Buprenorphine treatment in the USA for the maintenance and treatment of patients suffering from different forms of addiction to opiate derivatives is solely available in the form of sublingual tablets which are sometimes combined with Nalaxone to prevent abuse through injection (Nalaxone is almost non-active when taken orally), I recently learned from a friend in Europe that high dose Buprenorphine treatment with transdermal patches has over the last years been more frequently applied for the treatment of long term pain management in order to control moderate to severe aches of cancer and other medically justified conditions.

Additionally I learned that the brand names for these transdermal patches are Butrans, Norspan, and Transtec. The patches are said to deliver their dosage of Buprenorphine over a period of 4 days (96 hours), and to provide for either 35 or 70 μg/h, meaning that they contain 20 or 40mg Buprenorphine per patch. My friend informed me that abuse and illegal diversion of Buprenorphine in Europe was fairly common, regardless from the fact that this medication has partial opioid antagonist properties which are known to cause a ‘roof effect’ which means that after taking a certain amount, using more of this drug will not increase the pain killing effects that are generally searched after. If I remember correctly I read that doses up to 32mg will provide for increasing effects, whereas taking 40mg will not provide any benefit over a 32mg dose, therefore the roof effect must kick in after the consumption of around 32 mg.

The bioavailability of Buprenorphine has been reported to be around 50% for both transdermal and sublingual use. Its half life is said to be on average 36 hours, therefore providing for much longer activity than seen with other pain management medications used that are meant for use over longer periods of time. Oxycontin for example is known to be highly addictive, and it has also been recognized that this drug is often abused among its patients, whereas Buprenorphine treatment offers a much lower abuse potential.

My friend told me that he had been prescribed Oxycontin in the past (at a pretty high daily dose), but that he had decided to switch to Buprenorphine patches based on his doctor’s recommendation. His main motivation was that the patches were supposedly less addictive. According to my friend he applied the patch when the effects from his last Oxycontin pill had worn off (as he had been told by his doctor) and once withdrawal started kicking in. To his surprise the application of the transdermal Buprenorphine patch only made his withdrawal symptoms much worse, so much worse that it took him 3 days to get functional again. My friend believes that this experience was due to the partial antagonistic effects of Buprenorphine, as he was using quiet a large amount of Oxycontin before that time.

Anyways, he has now been using the patches for almost half a year and is very happy with the switch he made. According to him the patches are taking away constant craving for Oxycontin pills as he was previously taking, while it does provide for enough relief to keep him comfortable. The question remains how much withdrawal symptoms he will be experiencing once use of his patches will be interrupted since this has not happened yet as of the time of this writing.

Altogether these Buprenorphine transdermal patches for the use in pain management seems to be a great idea due to a much lesser degree of abuse potential, and much longer activity which prevents mood swings and withdrawal symptoms as often experienced when the use of short acting opiate pain medication is interrupted. Let’s hope that these patches will get approval in the USA shortly!

If you have used these patches, or the sublingual tablets, or if you have experienced withdrawal from them, please take a moment to post your experiences, we love to hear from you!

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