Volume 4 Issue 5 May, 2014
Substances such as heroin, opium and morphine are known as ‘opioids’. Many opioids are ‘psychoactive’, which means they affect the way the brain works. Opioid dependence is a chronic relapsing disorder and is associated with a wide range of psycho social issues. Opioid replacement treatment has proven efficacy in reducing opioid consumption, harm reduction strategy and psychosocial, medical morbidity and social functioning in opioid addicts.
How does Buprenorphine work?
Buprenorphine is a partial mu-opioid receptor agonist and kappa antagonist with a long half-life of 24-60 hours. When the mu receptor is stimulated, it sets in motion a chain of nerve cell activities that underlies most of the familiar opioid effects, for example, pain reduction, feelings of wellbeing or pleasure, and respiratory suppression. By stimulating the receptor only partially, buprenorphine yields those same effects, but with less intensity than heroin, morphine, or methadone, all of which stimulate the receptor fully. Buprenorphine provides a positive but moderate psychoactive effect that reduces craving and helps patients comply with their medication regimens.
How safe is BUPRENORPHINE?
“SAFE CEILING” Effect
Unlike full agonists, agonist effects of buprenorphine reach a ceiling and is less likely to cause respiratory depression incase of overdose. Buprenorphine is readily absorbed through the gastrointestinal and mucosal membranes. However, due to extensive firstpass metabolism, buprenorphine has very poor oral bioavailability (10% of the intravenous route) if swallowed. Its availability is significantly increased with sublingual administration (30–50% of the intravenous route) making this a feasible route of administration for the treatment of opioid dependence.
How to administer Buprenorphine :
Initial dose
Dispense 2-4 mg only if the patient has symptoms of withdrawal
- 2 mg if at higher risk (eg, older, lower tolerance, taking benzodiazepines)
- 4 mg for lower-risk patients,
Observe for 2 h, then dispense according to symptoms:
- Withdrawal symptoms resolved
Discharge after complete detoxification, with maintenance dose of 2-4 mg/day, preferably combination with Nalaxone.
Safety:
It is estimated that buprenorphine has been prescribed close to 200,000 worldwide. The most common side effects include constipation, headache, nausea, urinary retention, and sedation. Although a decrease in respiratory rate may be observed, this is generally not clinically significant. Since buprenorphine is metabolized primarily via the cytochrome p450 3A4 system, there is potential for interaction with medications that induce or inhibit this pathway.
Our experience with Buprenorphine:
We have found buprenorphine to be vastly superior to oral drugs in terms of long term recovery, harm reduction and safety profile. With buprenorphine patients have very less withdrawal symptoms during opioid replacement therapy. It has also helped the patients to reduce cravings for opioids. Buprenorphine/naloxone is safe, cost-effective, and long-term alternative to the use of methadone. Physicians prescribing buprenorphine replacement program need not receive special training for Opioid addiction is an added advantage. It can be recommended that buprenorphine be the frontline treatment for opioid dependence in primary care. Buprenorphine along with combination of naloxone has opened a new frontier of treatment for opiate addiction. We at present with our experiences with buprenorphine success feel that this can be a miracle/wonder drug for opioid addiction.
