Can anyone tell me what opioid antagonist medication is.?

Question

I know it's Suboxone. But what exactly does it mean that Suboxone is "antagonistic?"

Answer 1

The parts of the nervous system communicate by chemical messenger.  One nerve cell releases a chemical, and it binds to a protein in the cell membrane of another nerve cell.  The chemical that is released is called a "neurotransmitter."  The protein in the cell that receives the neurotransmitter is called a "receptor."  Opioids are a specific group of chemicals that bind to specific receptors in the brain.   When a chemical attaches to a receptor and turns on the receptor, it is called an "agonist."  When a chemical binds the receptor but does not turn it on, and also prevents an agonist from binding, it is called an "antagonist."

An easy way to think of this system is to compare it to the lock on a door.  The agonist is the key, and the receptor is the lock.  When the key goes into the lock, the door opens.  An antagonist is a key that goes into the lock, but doesn't open the door.  This incorrect key also prevents the correct key from entering the lock and opening the door.

Answer 2

An opioid antagonist is an receptor antagonist that acts on opioid receptors.

Naloxone and naltrexone are commonly used opioid antagonist drugs which are competitive antagonists that bind to the opioid receptors with higher affinity than agonists but do not activate the receptors. This effectively blocks the receptor, preventing the body from responding to opiates and endorphins.

Some opioid antagonists are not pure antagonists but in fact do produce some weak opioid partial agonist effects, and can produce analgesic effects when administered in high doses to opioid-naive individuals. Examples of such compounds include nalorphine and levallorphan. However the analgesic effects from these drugs are limited and tend to be accompanied by dysphoria, most likely due to action at the kappa opioid receptor. As they induce opioid withdrawal effects in people who are taking, or have recently used, opioid full agonists, these drugs are considered to be antagonists for practical purposes.

The weak partial agonist effect can be useful for some purposes, and has previously been used for purposes such as long-term maintenance of former opioid addicts using nalorphine, however it can also have disadvantages such as worsening respiratory depression in patients who have overdosed on non-opioid sedatives such as alcohol or barbiturates. Naloxone on the other hand has no partial agonist effects, and is in fact a partial inverse agonist at mu opioid receptors, and so is the preferred antidote drug for treating opioid overdose.

Naltrexone is also a partial inverse agonist, and this property is exploited in treatment of opioid addiction, as a sustained course of low-dose naltrexone can reverse the altered homeostasis which results from long-term abuse of opioid agonist drugs. This is the only treatment available which can reverse the long-term after effects of opioid addiction known as post acute withdrawal syndrome, which otherwise tends to produce symptoms such as depression and anxiety that may lead to eventual relapse. A course of low-dose naltrexone is thus often used as the final step in the treatment of opioid addiction after the patient has been weaned off the substitute agonist such as methadone or buprenorphine, in order to restore homeostasis and minimise the risk of post acute withdrawal syndrome once the maintenance agonist has been withdrawn.

Answer 3

An antagonist is a drug that blocks an effect.

So an opiate antagonist blocks the effects of opiate drugs.

A serotonin antagonist (like Seroquel) blocks the effects of serotonin.

A histamine antagonist (like Benadryl) blocks the effect of of histamine.

Basically it does this, usually, by sticking to the receptor in question and 'blocking' the slot the natural molecule or other drug goes into.

So an opiate antagonist can be used to reverse the effects of an overdose, or to prevent someone from abusing/getting high off a drug like vicodin.

Answer 4

It is a drug that blocks the effects of opiate drugs.. mainly used for people who have drug addictions