- Morphine (often called MSIR or MS Contin)
- Oxycodone (often called Percocet (when mixed with acetaminophen), OxyIR, or OxyContin)
- Hydrocodone (often called Vicodin when mixed with acetaminophen)
- Meperidine (Demerol)
These painkillers are central nervous system depressants. This means they slow down certain areas of the brain. If a person takes too many opiates, this can shut down the part of the brain that controls breathing. The person may become unable to breathe and die.
When a person has taken too much of one of these painkillers, naloxone can reverse the painkillers' effects and save the person's life.
Naloxone may be mixed into the same pill as an opioid painkiller to decrease the risk of misuse.
When given intravenously (into a needle placed into a vein), naloxone works within two minutes. When injected into a muscle, it works within five minutes. The medication may also be shot up the nose.
How does naloxone work?Edit
When a person takes opioids, the opioids have to attach to certain receptor sites in the brain in order to work, like a lock in a keyhole. Once the opioids attach to these opiate receptor sites - like a lock fitting into a keyhole - the opiates start to work. They kill pain, create euphoria, and make people feel calm and relaxed. But if a person takes too many opiates, they can also make it impossible to breathe.
Naloxone fits better onto these opiate receptor sites than actual opiates do. If a person takes naloxone, the naloxone will throw any opiate off of the opiate receptor sites (like a key getting taken out of a door). Naloxone will stay attached to these opiate receptor sites. This reverses the effects of the opiates that the person took.
Naloxone reverses the effects of opiates. Because of this, if a person who is addicted to opiates gets naloxone, they will have symptoms of opioid withdrawal. People have withdrawal symptoms when their body gets used to having opiates all the time.
Because naloxone reverses the effects of opiates, the side effects of naloxone can include restlessness, agitation, nausea, vomiting, a fast heart rate, pain, and sweating. To prevent this, small doses every few minutes can be given until the desired effect is reached.
Naloxone was patented in 1961 by Jack Fishman, Mozes J. Lewenstein, and the company Daiichi Sankyo. The drug was approved for opioid overdose by the Food and Drug Administration (FDA) in 1971. It is on the World Health Organization's Model List of Essential Medicines, the most important medications needed in a basic health system.
Naloxone can be used to reverse opioid overdose and to reduce the slowed breathing or mental depression that opioids can cause.
A prescription for naloxone is recommended if a person is:
- On a high dose of opioid (over 100 mg of morphine a day, or an equal amount of another opiate);
- Is prescribed any dose of opioid along with a benzodiazepine; or
- Is suspected or known to abuse opioids
If naloxone is prescribed to a person, that person should also be taught about how to prevent, identify, and react to an overdose, including how to perform rescue breathing, CPR, and how to call an emergency telephone number like 9-1-1.
Preventing opioid abuseEdit
Naloxone may be mixed with a number of opioids like buprenorphine. (Buprenorphine mixed with naloxone is called Suboxone.) Buprenorphine is used to decrease cravings for opiates. When buprenorphine and naloxone are mixed, and taken by mouth, only buprenorphine has an effect. Buprenorphine is a long-acting partial opioid agonist, meaning that although it binds to the body’s opioid receptors, it produces milder effects over a more prolonged period of time vs. the commonly abused full opioid agonists (heroin fentanyl, oxycodone, etc.). Buprenorphine has a high affinity for the opioid receptor, thereby preventing illicit and prescription opioid painkillers from attaching to the receptor. This leads to a lower risk of overdose and generally doesn’t produce a high in people who use opioids. Naloxone is added to reduce the risk of misuse, as it blocks the effects of buprenorphine if the medication is injected. But if a person misuses Suboxone by injecting it or taking large doses, the naloxone blocks the effect of the opioid. This combination is used to try to prevent abuse.
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