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Saturday, March 08, 2014 9:03:46 AM
Opiates, which include morphine and codeine and come from the opium poppy, remain our best pain killers (analgesics). Opioids include morphine-like drugs that are produced in a laboratory. Examples include oxycodone, fentanyl, and hydrocodone.
In the central nervous system, these drugs essentially work in the same way. They substitute for naturally occurring chemical messengers and affect cells at structures called receptors. Opioids fit into and activate opioid receptors. A drug that activates a receptor is known as an agonist. A nice analogy is that the opiate molecule (agonist) functions as a key that fits into a receptor. The receptor functions as a lock. There is a nice diagram of this action near the top of this message board. When a receptor is activated, cell activity is altered. The practical result of this receptor activation is a number of drug effects including analgesia. This is why we have prescription opiates. Now all drugs have multiple effects, and another prevalent effect of opiates is that they increase the presence of a chemical messenger called Dopamine in a series of structures called the Dopaminergic Reward Pathway. When this pathway is stimulated, a euphoric effect (rush, buzz, high, etc) results. Drug developers have not yet been able to design an opiate that produces effective analgesia without also producing euphoric effects.
A quick search of the news will demonstrate that rates of prescription opiate abuse have increased dramatically. Prescription opiates also likely function as “gateway drugs” for heroin use. Interestingly, the recreational demand for prescription opiates is so high, that heroin is now dirt cheap in comparison. One more important thing – by crushing up an oral opioid, one can alter the method of administration resulting in a stronger euphoric effect by getting more drug quickly to the central nervous system. This sets the stage for the development of abuse-resistant technology.
Other drugs, known as antagonists, work by blocking receptor sites instead of activating them. Opiate antagonists, such as naltrexone, actually prevent opiates from affecting cells. They can save a user from overdose, or even cause instant withdrawal symptoms in someone who is opioid-dependent. If an opiate and an opiate antagonist are administered at the same time, the antagonist blocks the effects of the opiate.
Elite’s technology involves packaging an agonist and antagonist together in the same capsule. If the drug is administered orally as prescribed the agonist is absorbed and will affect opiate receptors. The antagonist will not be released and has no effect. However, if the capsule is altered chemically or mechanically in hopes if providing rapid delivery of the opioid, the antagonist will be released, cancelling out the effects of the agonist. So, as far as value as a recreational drug goes, the user is likely to look elsewhere.
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