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What is Naloxone & What is it Used For?

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Millions of Americans are addicted to heroin or prescription opioid painkillers. Prolonged use of these drugs can lead to physical dependence, in which the body comes to rely on the presence of opioids to function normally. Naloxone hydrochloride has emerged as a major method of combating opioid abuse. The drug, which is commonly called naloxone, is used in the treatment of opioid dependence. Furthermore, a naloxone hydrochloride injection is capable of reversing the effects of opioid overdose.

What is the Drug Naloxone Used For?

Naloxone is a treatment for opioid overdose. In an overdose situation, respiratory depression and cardiovascular changes may cause a person to die. However, naloxone sweeps opioid molecules from their receptors, counteracting these actions. Therefore, soon after administration of naloxone, patients experience an increase in heart rate and blood pressure. Thus, naloxone effectively reverses the effect of an opioid overdose.
Naloxone may also be beneficial in the treatment of opioid addiction. For example, naloxone is combined with buprenorphine to help individuals who are in treatment for opioid abuse. This drug combination suppresses symptoms of withdrawal and decreases drug cravings.
Another effective use of naloxone is in rapid opiate detox protocols. Rapid detox involves the administration of naloxone to shorten the amount of time patients spend undergoing withdrawal. In conclusion, this is an effective treatment for physical dependence on opioids.

How Does Naloxone (Narcan) Work?

Pharmaceutical laboratories produce the synthetic drug, Naloxone hydrochloride. The drug comes in a nasal spray or liquid injectable form.
Naloxone is an opioid antagonist, meaning that it opposes the action of opioids in the brain. In addition, there are numerous types of opioid receptors in the brain. The mu opioid receptor is abundant in several regions of the brain. Consequently, Morphine and other opioids bind to the mu receptors, triggering a cascade of effects including analgesia, sedation, euphoria, lower blood pressure, and gastrointestinal changes.
Naloxone hydrochloride has a very high affinity for mu opioid receptors. As a competitive antagonist, naloxone competes with other opioids to bind to the mu receptor. Unlike opioid molecules, which activate the receptor, naloxone simply binds to the receptor and blocks it. In particular it binds more strongly than heroin or prescription painkillers so it can knock these opioid molecules away from the receptor.
Most importantly, naloxone hydrochloride does not have any agonist effects. This is in contrast to drugs such as buprenorphine, which also bind to and activate opioid receptors. Naloxone doesn’t have any known risk of overdose or abuse potential. Indeed, this makes it an important medication to safely counteract the effects of opioid dependence. 

How Is Naloxone Given?

The first FDA-approved version of naloxone was known as Narcan, which was designed as a naloxone hydrochloride injection. However, now that the patent for Narcan has expired, the drug is available in the United States under the name Evzio and in several generic formats. Most of these are intravenous, intramuscular, or subcutaneous injections. Additionally, Narcan is now available as a nasal spray, which may increase its applicability in the fight against opioid abuse.

Naloxone Side Effects

Use of naloxone may have potential side effects. Because naloxone reverses the effects of opioids, it may induce sudden withdrawal symptoms. For example, these might include:

  • Nausea and vomiting
  • Stomach pain
  • Diarrhea
  • Fever or sweating
  • Weakness or fatigue
  • Body or muscle aches
  • Shivering or tremors
  • Increased heart rate
  • Increased blood pressure
  • Pounding or thumping heartbeats
  • Irritability
  • Feelings of nervousness or restlessness
  • Runny nose
  • Yawning
  • Goosebumps
  • Shivering

In fact, for babies younger than four weeks old, naloxone may lead to crying stiffness, seizures, or overactive reflexes.
This is not a complete list of side effects and it is possible for other side effects to occur. Therefore, contact your doctor for medical advice about side effects. You can report side effects to the FDA at 1-800-FDA-1088. This helps the FDA collecting information about the safety and effectiveness of naloxone.
Some individuals may be allergic to naloxone. Get emergency medical attention if you have signs of an allergic reaction after taking naloxone. For instance, symptoms may include hives, swelling of the face, lips, tongue, or throat, and difficulty breathing.

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