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Pentazocine/Naloxone

How Does It Work?

As previously mentioned, this medicine contains pentazocine and naloxone. Pentazocine is the pain-relieving portion of the drug. It works by binding to opioid receptors and mimicking the action of naturally occurring chemicals that block pain. Once taken, pentazocine usually starts to relieve pain in 15 to 30 minutes, and can continue to control pain for 3 hours or longer.
 
The main effects of pentazocine occur when it binds to receptors in the central nervous system (the brain and spinal cord). However, the drug can produce effects anywhere opioid receptors are found in the body.
 
There are several types of opioid receptors located throughout the body. Pentazocine/naloxone is classified as an opioid agonist-antagonist, which means it binds to and activates certain opioid receptors (kappa receptors), but also blocks certain other opioid receptors (called mu receptors).
 
As an antagonist at mu opioid receptors, pentazocine/naloxone partially blocks the action of opioid medications that bind to mu receptors, such as morphine. In addition, pentazocine/naloxone is only a partial agonist at kappa receptors, which means it only partially activates them.
 
Compared to full agonists, such as morphine, partial agonists-antagonists like pentazocine/naloxone usually have a limited effective dosing range. This means there is a maximum dose above which the drug will have no further effects. This may help make pentazocine/naloxone a less-desirable drug for abuse and make it less dangerous than full agonist drugs, particularly in the case of an overdose; however, an overdose can still be dangerous.
 
The naloxone portion of pentazocine/naloxone helps prevent the medication from being misused. When taken by mouth as directed, naloxone has no effects in the body. However, if the drug is crushed and injected, naloxone blocks the actions of pentazocine (as well as other narcotic medications), preventing it from working and potentially causing severe withdrawal symptoms.  
 
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Pentazocine/Naloxone Information

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