The Suboxone® Story
Report from the Mind-Meds.com New York office about Suboxone

Yes, Suboxone® is definitely a major player—if not the major player—among new drugs for the treatment of opiate addiction.  You may not be aware of the fact that Suboxone® and a closely related medication, Subutex®, have been ‘around’ for at least twenty years. Many drugs are released for marketing and public consumption in Europe, Latin America and Asia before they appear in the United States. Suboxone®, also like many other drugs, was well known in research laboratories and clinical testing programs before it was approved for general use.

Suboxone® is actually a combination of two drugs, buprenorphine  and naloxone.  Buprenorphine is known as a ‘partial opioid agonist’, meaning that its mechanism of action is fairly complex. Buprenorphine acts on and occupies various opiate receptors in the brain, which ordinarily are occupied by the body’s own pain relief/pleasure molecules, the endorphins and enkephalins. Buprenorphine (and therefore Suboxone®) cause the opiate receptors in the brain to be activated. This results in mild euphoria, a sense of well-being, and pain relief.

However, the story gets more complicated. Buprenorphine itself it also a ‘partial opiate antagonist’: when you have buprenorphine or Suboxone® on board, occupying your brain’s opiate receptors, other opiates such as heroin or morphine cannot get in and activate the receptor. If you are taking buprenorphine or Suboxone®, it is fruitless and often dangerous to take any other kind of painkillers (morphine, heroin, Percocet®, oxycodone, Oxycontin®, Fentanyl®, Dilaudid®, others.) The combination of Suboxone® and any other opiate-type painkillers can result in immediate and severe opiate withdrawal.

One more thing: the other ingredient in Suboxone®--naloxone—is a pure opiate antagonist. If you are taking naloxone by itself, the drug will effectively block all your opiate receptors and even displace painkillers/opiate molecules that are already in the brain. This is why naloxone is often used in the emergency room to treat suspected cases of heroin overdose. An intravenous dose of naloxone will literally displace any opiate drugs from their sites in the brain, and the person who may be unconscious from an overdose wakes up, is usually completely alert, and is often in a state of mild to moderate opiate withdrawal. The pharmacology is fascinating—especially to the guy whose life has just been saved by a shot of naloxone!

Subutex® is pure buprenorphine, without the added naloxone. Most doctors are reluctant to prescribe Subutex® because some patients with addiction problems may attempt to ingest other painkillers along with the Subuted®, knowing that the Subutex® has no powerful opiate blocker in it.

Some ask why Suboxone® is manufactured with naloxone. rather than naltrexone.  Naloxone is only active when taken by injection or when sniffed. When you take Suboxone® sublingually (under the tongue, recommended route of administration), the naloxone it contains is completely inactive. The pharmaceutical manufacturers realized that some patients, in an effort to get high, might snort or inject chopped up Suboxone® tablets. So they chose a narcotic antagonist—naloxone—that is only effective when taken by one of these (parenteral: by snorting or shooting) routes.

You may be familiar with the narcotic antagonist that is active when taken orally—naltrexone. Naltrexone is a drug that has found usefulness in several clinical scenarios. It is marketed as Revia®, for people who are trying to quit drinking.  The idea here is that alcohol may be stimulating, among other sites, brain opiate receptors. If these receptors are blocked (by naltrexone), the alcoholic will experience no pleasure when he or she drinks.

Behavioral pharmacologists also believe that certain seemingly self-destructive behaviors—such as cutting oneself, or self-mutilation—result in the massive release of endorphins, the brain’s natural pain-killer molecules. Again, blocking the endorphin (opiate) receptors of the brain—with naltrexone, also called Trexan®--may take away the ‘pleasure’ or relief that self mutilators usually report after they have cut or scratched. Naltrexone is effective when taken orally, so that both Trexan and Revia® are available as pills.

Suboxone® prescriptions are available for patients in New York who suffer from the above symptoms. Contact a New York-based Mind-Meds.com doctor for more information about Suboxone® and other medications.