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Still learning. I found this of use and wanted to share
by lostparent, Apr 08, 2008 10:24AM
Q: What's the difference between an opiate agonist and an opiate antagonist?
A: An agonist is an agent that binds to a receptor and activates that receptor in order to elicit an effect (typically transmitting a signal to the inside of the cell, either by opening a channel to allow ions to flow in/out, or changing the receptor's shape to cause a cascade of intracellular events to occur). Drugs that are agonists essentially mimic the action of the endogenous (naturally occuring) neurotransmitters, typically with the same or a stronger affinity than the neurotransmitter itself.
An antagonist is an agent that binds to a receptor but does not elicit the response that the neurotransmitter or an agonist would cause. The antagonist blocks the receptor and prevents activation by neurotransmitters or other drugs.
So in the case of opiates, lets look at the opiate agonist Morphine. When Morphine enters the brain, it binds to opioid receptors and activates them. This binding is what produces the effects of Morphine.
In the case of a Morphine overdose, where a hospital is concerned that the high dose of Morphine may be dangerous (depressing breathing and heartrate), they may administer Naloxone (an opiate antagonist). The Naloxone finds its way to your opiate receptors and "competes" with Morphine for binding of the receptors. Because Naloxone has a higher affinity for the receptors than Morphine, the Naloxone will generally win out, replacing much of the Morphine at the receptor sites.
Within 1-3 minutes of a sufficient Naloxone injection (2-4 mg), a patient who has OD'd on Morphine will generally wake up, usually quite agitated. If given to an otherwise "normal" person (not in the midst of an overdose) who happens to be addicted to an opioid or opiate, Naloxone can immediately precipitate withdrawl symptoms (nausea, vomiting, disorientation, halluncinations, excretion, tremors, convulsions, agitation, anxiety, etc).
A: An agonist is an agent that binds to a receptor and activates that receptor in order to elicit an effect (typically transmitting a signal to the inside of the cell, either by opening a channel to allow ions to flow in/out, or changing the receptor's shape to cause a cascade of intracellular events to occur). Drugs that are agonists essentially mimic the action of the endogenous (naturally occuring) neurotransmitters, typically with the same or a stronger affinity than the neurotransmitter itself.
An antagonist is an agent that binds to a receptor but does not elicit the response that the neurotransmitter or an agonist would cause. The antagonist blocks the receptor and prevents activation by neurotransmitters or other drugs.
So in the case of opiates, lets look at the opiate agonist Morphine. When Morphine enters the brain, it binds to opioid receptors and activates them. This binding is what produces the effects of Morphine.
In the case of a Morphine overdose, where a hospital is concerned that the high dose of Morphine may be dangerous (depressing breathing and heartrate), they may administer Naloxone (an opiate antagonist). The Naloxone finds its way to your opiate receptors and "competes" with Morphine for binding of the receptors. Because Naloxone has a higher affinity for the receptors than Morphine, the Naloxone will generally win out, replacing much of the Morphine at the receptor sites.
Within 1-3 minutes of a sufficient Naloxone injection (2-4 mg), a patient who has OD'd on Morphine will generally wake up, usually quite agitated. If given to an otherwise "normal" person (not in the midst of an overdose) who happens to be addicted to an opioid or opiate, Naloxone can immediately precipitate withdrawl symptoms (nausea, vomiting, disorientation, halluncinations, excretion, tremors, convulsions, agitation, anxiety, etc).
Member Comments (2)
by theeagle, Apr 08, 2008 10:47AM
To: lostparent
That is exactly why addicts should avoid Talwin (pentazocaine) - after it started being abused on the streets the Company added narcane to the formulary. An addict taking Talwin will be tossed immediately (almost) into nasty precipitated withdrawal. Trust me, I've been there. And if you are od'd on methadone the first thing the EMT's do is suspect a narcotic overdose and inject narcane (the antagonist) - this can lead to strong enough shock to induce respiratory arrest....again, trust me - this is from personal experience.
by BornTwoRiff, Apr 08, 2008 11:04AM
To: Narcan
I read where Narcan will induce w/d severe within minutes.. I worked EMS years ago and we pushed it on a Vietnam Vet that had OD on SINEQUAN (doxepin HCl).. that was one medication it would not reverse but we had nothing to lose. Dr orders fron ER.. . We were 15min out from ER.. He died later that morn.. We ran the call right at shift change at 7am.. That was tough to take..
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