On Buprenorphine

Since the age of 13, I have been taking opiates in moderation for chronic pain. I started with morphine (and the occasional hydromorphone), and since an MVA approximately three years ago (I am now 19), this was briefly supplemented with oxycodone.

As someone who has been on every opiate available, I have formed preferences as to which is best, and I flatly refuse to take others. The classic opiates are the best; these include (dia)morphine, hydromorphone, oxycodone, and fentanyl, although I will not take fentanyl patches due to the O/D risk. I will not take pethidine (Demerol®) or anileridine (Leritine®) for their neurotoxicity (they can cause seizures in high doses, and aren't strong enough, forcing me to take high doses) or tramadol or tapentadol for their thymoleptic (SSRI) activity (they are one step away from the so-called anti-depressants and have a far worse withdrawal). 

I have taken methadone for cough that would not go away and later suffered my first and last episode of drug withdrawal; I liked methadone but hated the very long withdrawal period. I have experience with ketobemidone (Ketogan®), dextromoramide (Palfium®), and dipipanone (Diconal®), but none beats the classic opiates.  I even wrote up an opiate rating chart way back when; buprenorphine isn't included, as I had regrettably not tried this amazing substance before in adequate dose.

I was referred to a doctor who treats primarily addiction cases, but this fellow (who I shall call Dr Smith, because that's his name) agreed to treat my pain even though no addiction existed, then or now. His favourite opioids, in order of preference, are buprenorphine and hydromorphone. Score! I originally insisted on hydromorphone, my favourite opioid. However, Dr Smith refused to supply it unless buprenorphine was first trialled, and I was quickly started on 16 mg of Suboxone®.

Suboxone® is a form of the typical opiate buprenorphine; I use 'typical' here to mean that its effects mirror that of morphine and hydromorphone, with no NMDA hallucinogenic effects such as those that Physeptone® suffers from.  There are three forms of buprenorphine: patch, pill (to be taken under the tongue), and injection.  No swallowable pill exists, as swallowing buprenorphine makes it 1/5 as strong as when taken under the tongue, so making such a version would just plain be wasteful, not to mention liable to abuse; if there were a swallowable version, the doses would be 10, 20, and 40 mgms, like oxycodone.  The patch is for a week, which (in my case) makes it unwieldy and impractical, not to mention not strong enough (doses delivered are in microgrammes per hour—that's right, microgrammes).  Suboxone® is one brand of the oral version of buprenorphine: there are two others, Subutex® and Temgesic®.

Buprenorphine has some disadvantages, though; some are not immediately obvious.  It is unique in its mode of action in that, past a certain point, the duration of the dose will be longer, but diminishing returns in strength will be apparent.  In addition, buprenorphine kicks all other opiates off of their receptors (in effect, it pulls the key out of the lock), and it binds very strongly to opiate receptors once it finds or makes itself a free spot.  This is a mixed advantage and disadvantage; it is tough to overdose, but once a toxic state is reached, good luck fixing it.  The biggest disadvantage is that not every country's medication licencing board has seen fit to approve Suboxone® treatment for pain; it is seen by the FDA, for instance, as purely an addiction treatment—many American doctors disagree though.  The patch, though, is always treated as a pain treatment.

Now, let it here be said that, in the UK, Suboxone® (or a version thereof) is used to treat pain, not just the patches. For marketing reasons, the pain version is called Temgesic® and is priced lower than Suboxone®. Temgesic® is available in 200 µg, 400 µg, and 2 mg versions; Suboxone® is available in 400 µg, 2 mg, and 8 mg versions. Both contain the same ingredients in the same ratios: 4:1 buprenorphine/naloxone.  In Subutex®, no naloxone is included.  Naloxone, also known as Narcan®, is the antidote for morphine poisoning if taken by injection; it will completely reverse the effects of morphine, whether beneficial or harmful.  Narcan® will relieve some effects of morphine and related drugs if taken by mouth—the primary effect it will relieve is that of bowel upset.  

The naloxone is included, not as common myth has us believe, so as to discourage abuse by the intravenous route, but to discourage the primary side-effect of opioids (included in morphine and in oxycodone for the same reasons), namely, difficulties in the lower digestive tract. This is due to buprenorphine binding almost irreversibly to receptors; naloxone will not dislodge it in any way approaching reliable. For pain, Temgesic® is taken four times a day; it is favoured especially in cases of laryngeal malignancy. Canadian doctors have not yet learned of this excellent use of buprenorphine and provide it for that most insidious killer, addiction, only. 

Except Dr Smith, apparently. He put me on buprenorphine for my pain, and I have quickly grown to love it. Sure, it might not offer instant relief, but I'd much rather relief that lasts. Dr Smith, however, was ignorant of the appropriate manner to dose Suboxone in chronic pain; he prescribed it to be used in the time-honoured protocol for addiction management: once per day, supervised. I had issue with this and was permitted to dose it in the British fashion, four times per day, self-supervised. This allows for dose variation, which Dr Smith dislikes intensely, but I favour (narcotics are addictive, after all, and it is nice to take a holiday once in a while). My prescribed dose is 16 mg per day, but I don't take this much as a rule. The most I have ever taken is 8 mg per diem; two halves or four quarters.  My usual dose varies between 4 and 8 mg per diem.

The reason I have grown to love buprenorphine is that it has all the psychological effects of morphine and its sisters; it has qualities of an excellent anti-depressant and anxiolytic, and certainly beats all the synthetics.  No synthetic opiate possesses the excellent quality of morphine, in my opinion.  Some may love methadone, but the green syrup may just drink you up instead of the other way round.  In some situations, buprenorphine is less controlled; this just adds to its appeal, as it's easier to convince a doctor to prescribe it.  Thank God for buprenorphine—I now take no other medication and I am happy this way.  It seems that one's skills are infinitely improved on opiates, for a particularly narrow definition of 'skills': writing, drawing, driving, flying, computer operation, and other sit-down arts of all forms are vastly improved by the added drop of creativity.  Nor is there any sluggishness or motor impairment, as with other drugs.  Opiates are genius in their subtlety—it is sometimes hard to know they're there.

If you ever have the chance of trying buprenorphine or hydromorphone, do it.  You will be very pleasantly surprised.