Buprenorphine side effects

The quest for compounds that combined the analgesic properties of morphine, were nonaddictive, and lacked the side effects of nalorphine, led to the development of the dmgs shown in Table 3. These compounds have both agonist and antagonist activities. Nalbuphine (14) (23) and buprenorphine... 

Suboxone is a combination of buprenorphine (opioid partial agonist) and naloxone. It is presented as sublingual tablets and is used as an adjunct in the treatment of opioid dependence and in premedication or perioperative analgesia. A side-effect of opioids is drowsiness. 

An excellent brief article on buprenorphine treatment has been provided by Taikato et al. (2005), which notes the common possible side-effects (headaches, nausea and vomiting, sweating, constipation, etc.) and drug interactions. The limited central depressant effect of buprenorphine may be compounded by alcohol and antidepressants, while the metabolism of buprenorphine can be enhanced by anticonvulsants, with therefore possibly reduced efficacy. There have been some case reports of liver toxicity from buprenorphine that is reversible if the medication is stopped (Herve et al. 2004), and often clinical guidelines will recommend that liver function tests are included in buprenorphine treatment, as they definitely should be with naltrexone. 

As indicated, buprenorphine can offer a quicker option than methadone, with a three-day course reported to be effective for withdrawal from heroin (Cheskin et al. 1994). The side-effects of clonidine which render it unsuitable for community treatment can be manageable in the inpatient setting, although the drug is being superseded by lofexidine where that is available. Controlled studies have found clonidine and lofexidine to be equally effective in alleviating withdrawal symptoms in inpatient detoxification from heroin (Lin et al. 1997) and from methadone (Khan et al. 1997), with lofexidine resulting in less hypotension and fewer adverse effects. Another double-blind controlled study found lofexidine to be broadly as effective as a ten-day methadone detoxification in inpatient opiate withdrawal (Bearn et al. 1996). 

Buprenorphine is a semi-synthetic derivative of thebaine, one of the opium alkaloids. It is approximately 30 times as potent as morphine. A dose of 0.3 mg intramuscularly has a duration of analgesic action of 6-18 h. Buprenorphine is also effective sublingually. The average bio-availability by this route is about 55%, but absorption is slow and the time to achieve peak plasma concentrations is variable, with a range of 90-360 min. The onset of action is rather slow (5-15 min) after both intramuscular and intravenous administration, possibly due to slow receptor association. Buprenorphine binds to and dissociates from the p receptor very slowly, which may account for its low potential for physical abuse. It also means that buprenorphine-induced respiratory depression is difficult to reverse with naloxone, even with very high doses. Doxapram may in these circumstances be useful. Drowsiness and dizziness are the most common side effects, although they rarely... 

In compounds with stronger p-agonistic activity (buprenorphine and pentazocine), the abuse potential is marked and in contrast to earlier estimations, both compounds had to be subjected to narcotic control. In compounds with a marked K-agonistic component (cyclazocine, nalorphine) the dysphoric side effects are so prominent that the compounds could not be used for therapeutic purposes. 

Side-effects Buprenorphine induces p-opioid-type side effects including respiratory depression, drowsiness, nausea and vomiting. In the clinical literature, however, there are only few cases of significant respiratory depression. Reversal of respiratory depression may need higher doses of naloxone (Gal, 1989). Buprenorphine has a limited abuse potential and withdrawal reactions, due to slow receptor dissociation, are mild and delayed. 

A quantum leap in pain therapy with distinct advantages in the form of reduced side-effects and application frequency was achieved with transdermal opioid administration. Transdermal application requires a number of characteristics on the part of the active substance (Fig. 7), the most restrictive being the daily dose, and only very potent opioids which are effective in very low doses, such as fentanyl and buprenorphine, are an option (Sittl and Likar, 2001). 

Within the last 10, years several new compounds were launched in the field of non-steroidal antiinflammatory drugs (NSAIDs) with a clear focus on cyclooxygenase type 2 selective compounds. In the field of opioids on the other hand no new drugs have passed phase III clinical trials. In this field innovation has been achieved through new pharmaceutical formulations of known drugs such as transdermal systems, e.g. buprenorphine patch, transmucosal systems, e.g. fentanyl lollipop, or rectal delivery systems containing e.g. morphine. These were developed in order to reduce opioid side effects, but also to overcome pharmacokinetical limitations, in particular to prolong compliance and duration of action. 

Patients taking naltrexone (trade name Trexan) must tell their health care professional because the two drugs will cancel any effects that the other has. Some other medications that reduce the effects of fentanyl are buprenorphine, dezocine, nalbuphine, and pentazoncine. These medications also can cause side effects in people who have become physically dependent on fentanyl. 

Nevertheless, buprenorphine provides another example of an opiate analogue where analgesia has been separated from dangerous side-effects. 

The biological response is analgesia with sedation and none of the hazardous side-effects. It is this receptor which provides the best hope for the ultimate safe analgesic. The earlier results obtained from nalorphine, pentazocine, and buprenorphine can now be explained. 

As with other opioids, NSAIDs such as etodolac have been used with buprenorphine to reduce the postoperative pain score without increasing side effects. ... 

Brown ES, Tirado C, Minhajuddin A, Hillhouse M, Adinoff B, Ling W, Doraimani G, Thomas C. Association of race and ethnicity with withdrawal symptoms, attrition, opioid use, and side-effects during buprenorphine therapy. J Ethn Subst Abuse 2010 9 106-14. 

Opioids can be classified according to stractural similarity with morphine in semisynthetic and synthetic derivatives. Structurally similar, semisynthetic morphinelike derivatives as well as stracturally distinct opioids have been synthesized to search for compounds able to improve analgesic effects that minimize side effects. Semisynthetic derivatives include morphine-related agonists (hydromorphone, hydrocodone, oxycodone, oxymorphone, and codeine), and moiphine-related partial agonist and antagonists (buprenorphine, naloxone, and naltrexone). Synthetic derivatives include phenylpiperidines (meperidine and loperamide), diphenylpropylamines (methadone and propoxyphene), and piperidines (fentaityl, alfentanyl, sufentanil, and remifen-tanil) (Dumas and Pollack, 2008). 

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