CPRx: Clinical Indications

Opiate Use, Tolerance and Effects

Opiate agonists act on opioid receptors to initiate analgesia, sedation and euphoria. Pharmacological studies have defined three classes of opioid receptors, Delta, Kappa, and Mu. Commonly used opiate agonists are morphine, heroin and hydrocodone.

Opiate antagonists block and reverse the effects of opioid agonists, by competitively adhering to opioid receptors. The most common antagonists are naltrexone (Revia®) and naloxone (Narcan®).

Buprenorphine hydrochloride, FDA approved for pain relief and sold under the tradename Buprenex® by Rheckitt & Coleman, Ltd., acts as a partial Mu agonist, meaning it has components for analgesia and pain relief but, uniquely, is also a full Kappa antagonist. Because of this property, Buprenex® is outstanding for management of short-term and chronic pain, and is, in our opinion, the medication of choice for opiate detoxification.

During detoxification, Buprenex® allows comfortable, painless withdrawal, without the fatigue, sweats, tactile sensation complaints ("tingling" or "skin crawling"), aches, seizure risk or confused thought processes common during traditional detoxification procedures.

Full opiate antagonists such as Oxycontin®, Dilaudid®, amd the various derivatives of codeine and codone initially create euphoria but also quickly create tolerance. This creates patient hardship when medication is no longer needed for pain relief, or, as tolerance increases, is no longer effective for pain relief. Additional medical risks of detoxification are well documented.

Dosage of 0.3mg of Buprenex® is equivalent to 10mg of morphine, providing maximum pain relief with minimal potential for abuse, dependency, and overdose. There is a plateau of euphoric effects, consistent with its agonist/antagonist classification. Clinical tests report humans without symptoms of overdose tolerate single doses of Buprenex® up to seventy times the recommended analgesic dose.

CPRx

Additional History and Definitions
The enkephalins (en-kef´a-linz), dynorphins, and endorphins are endogenous (made naturally by our bodies) opioids and function as neurotransmitters, neuromodulators, and hormones. These natural substances are involved in the perception of pain, modulation of behavior, and regulation of autonomic and neuroendocrine function. Pharmacological studies have found three opioid receptors in our brain and defined these as the Delta, Kappa, and Mu.

Pentapeptide endorphins, found in many parts of the brain, bind to specific receptor sites, some of which may be pain-related opiate receptors; hypothesized as endogenous neurotransmitters and non-addicting analgesics. Metenkephalin is Tyr-Gly-Gly-Phe-Met; leuenkephalin has Leu in place of Met; proenkephalin has Pro in place of Met.

Endorphins (en´dor-finz), opioid peptides originally isolated from the brain and also found in the nervous system, bind to the same receptors that bind exogenous opiates. A variety of endorphins (e.g., alpha and beta) that vary not only in their physical and chemical properties but also in physiologic action have been isolated.

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