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A very promosing drug treatment for opioid addiction: Buprenorphine
Buprenorphine, a new drug for the treatment of opioid addiction. This charismatic drug help most
of the patients with opioid dependence.It has been now proved
that buprenorphine have a good safety profile and pharmacological feature. Chances of drug addiction and effects of overdosing are minimum with buprinorphine. Good safety pharmacological profile is very
helpful for treating doctor and for the patient to remain with treatment.
Buprenorphine is a partial agonist at the mu opioid receptor and antagonist at the kappa receptor. Buprenorphine has very high affinity but have low intrinsic activity at the mu receptor. Buprenorphine bounds with mu receptors and displaces the drugs like morphine, methadone and any other opioid. Due to its partial agonist effect buprenorphine gives many clinically desirable pharmacological effects like low level of physical dependence, low abuse potential, a ceiling effect at higher doses, and greater safety in overdose compared with other opioid full agonist.
Buprenorphine, as a partial opioid agonist, can be placed at midpoint between full opioid agonist like methadone and opioid antagonists. Due to its agonist properties a person addicted to opioids perceive a reinforcing effect and often describe that he is feeling normal. In higher doses
buprinorphine antagonistic property can cause precipitation of acute opioid withdrawal if administered to a addict who is dependent on opioids and maintained on a calculated dose of a full agonist. Here buprenorphine displace the full agonist from the mu receptors not providing the equivalent amount of receptor activation and this can lead to decrease in agonistic effect and hence, onset of withdrawal. High affinity of buprenorphine for the opioid mu receptor, can
precipitate abstinence syndrome may be difficult to reverse.
Because of its low intrinsic activity at the mu receptor, at analgesic doses, buprenorphine is 30-40 times more potent than morphine. But, at increasing doses, unlike a full opioid agonist, the agonist effects of buprenorphine reach a maximum and do not continue to increases with increasing doses of the drug, this what we call is, the ceiling effect. A great benefit of the ceiling effect is that the respiratory depression with an overdose of buprenorphine is less likely than with an overdose of a full mu opioid agonist.
Sometimes, Buprenorphine can produce euphoria, if it is injected. Physical dependence with buprinorphine,if any, is of lesser degree as compare to full opioid agonist and it is easy to discontinue buprinorphine at the end of treatment.
Dose and duration of buprinorphine should be individualized for each patient and should only be prescribed after thorough examination of patient.