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What is Naloxone and How Is It Used?

Hand with pen drawing the chemical formula of naloxone

Naloxone, the most popular brand name of Naloxone Hydrochloride, is a drug most commonly used to reverse opioid overdose. While also used in drug addiction treatment, Naloxone has saved an estimated 10,000 lives since it began trials in the 1990s, making it one of the most medically important drugs available.

Today, over 70,000 people die of opioid-related overdoses each year. A further 5 million people have an opioid use disorder, while 18.8 million people abuse prescription and non-prescription opioids. Millions of Americans use opioids outside of prescriptions every day, and every time they do, they put themselves at risk of overdose. Naloxone is the only real treatment drug available to reverse those overdoses.

What is Naloxone?

Naloxone was developed and patented in 1961, taking almost 30 years to move from testing to distribution trials. The drug is an opioid agonist, meaning that it blocks opioids from binding to the receptors in the brain. In fact, it causes some opioids to unbind from those receptors, which is how it can reverse an overdose. If someone has taken too much of a drug, Naloxone effectively blocks that drug from interacting with the brain while the metabolism continues to break the drug down.

By the early 90s, government programs in the U.S. and Canada had begun distributing Naloxone through safe use houses, through rehab centers, and at doctor’s offices. The result was over 10,000 reversed overdoses in the 20 years of the study.

Today, it’s been recognized as an essential medication by the World Health Organization. It’s now available as a low-cost medication, sometimes without a prescription, and sometimes even for free. In addition, many clinics and pharmacies will go out of their way to stock the drug, making it readily available.

How is Naloxone Used

Naloxone is primarily used for drug overdose prevention. However, it’s also used in Medication-assisted treatment. In each case, it’s primarily available with a prescription. It’s also available as a nasal spray, injection, patch, and pill – depending on intended use.

Drug Overdose Prevention

Naloxone is the primary drug used to reverse opioid overdose in the United States and across the globe. The drug takes effect within 2-5 minutes of administration and lasts for 30-30 minutes. If the individual doesn’t pull out of an overdose within 5 minutes, the person applying the Naloxone should administer a second dose. Here, most over the counter and prescription Naloxone is sold as a nasal spray. In other cases, you may receive an injection.

If you’re administering Naloxone, it’s crucial to ensure that you follow the instructions on the package for your brand and medication type. In some cases, you’ll also get a patch, however, these are not normally for overdose reversal.

a man injecting naloxone in his arm

Injection – Naloxone can be injected into a large muscle in the bicep, hip, or thigh. It takes 5-30 minutes to take effect when injected.

Nasal Spray – The nasal spray inserts into the nostril and then takes 2-5 minutes to take effect.

Additionally, it’s critical to call an ambulance after administering Naloxone. In most cases, Naloxone wears off after 20-30 minutes. Opioids can take 6-12 hours to wear off. This means the person having the overdose may start to overdose again when the dose wears off. It’s important to get them into medical care where more Naloxone can be administered via a controlled IV until they are stable.

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Drug Addiction Treatment

Vial of Naloxone drug which is used for opiate drug overdose

Naloxone or is also increasingly used during medication-assisted opioid treatment, primarily to help users avoid using. Here, Naloxone is used in both abuse prevention and in relapse prevention. For example, someone on a Naloxone maintenance program cannot use opioids to get high. The opioids won’t bind with the opioid receptors in the brain.

However, they may experience significant discomfort and withdrawal symptoms when taking opioids while on a Naloxone maintenance program.

Therefore, most medical professionals recommend using Naloxone after patients graduate from a drug addiction treatment program.

In addition, Buprenorphine and Naloxone sublingual tablets are one of the most common medication-assisted treatment drugs available. In this case, the naloxone is kept at low enough levels that it isn’t strong enough to counteract the opioids when taken orally. Oral absorption of Naloxone is very poor. Therefore, patients can take buprenorphine to reduce withdrawal symptoms and prevent cravings for opioids. However, if they attempt to abuse the buprenorphine by injecting it, the Naloxone is much more potent when injected and will prevent the opioids from binding properly. For this reason, Naloxone is used as an abuse-prevention, in combination with other drugs. This option is much more common than Naloxone on its own.

Naloxone Side Effects

Naloxone can have significant side effects, especially if injected. Here, many people experience allergy-like symptoms and others experience true allergies. This is another reason why it’s extremely important to call the ambulance while injecting or administering the drug. Side effects normally include:

Pain or burning at injection site/around the nose
Hot flashes
Sweating
Heart palpitations or arrythmia
Withdrawal symptoms
Allergies

Otherwise, Naloxone is an extremely safe and reliable drug. Long-term users will build up a slight physical tolerance to the drug. However, it has no risk of addiction, making it very safe to be used as part of a long-term drug maintenance program. This means you will experience some light withdrawal symptoms when quitting the drug. Naloxone also does not have an overdose risk at any amount of the drug available to consumers on the market.

While Naloxone and especially Naloxone and Buprenorphine have a bad reputation as drugs used to quit other drugs, they are safe, chemically controlled, and offer increased quality of life. They also often allow people the mental and physical room to get treatment, to learn coping mechanisms, and to build the mental strength they need to recover before going through that battle.

What is Narcan?

Narcan is the largest brand offering Naloxone in the United States. While first approved by the FDA in 2015, the brand has come to be the leading supplier of intramuscular injection Naloxone, tested and released nasal spray, and developed a patch for maintenance therapy. In addition, the brand offers all of its products for a low cost to ensure the medication is accessible.

Getting Naloxone

If you or a loved one is struggling with opioid abuse, having Naloxone on hand can be lifesaving. Often, you can request it from your doctor, acquire it from a local pharmacy such as Walgreens, or acquire it from a government run safe use house. As of 2022, all major pharmacies offer Naloxone Nasal spray without a prescription. If you want more information or aren’t sure whether Naloxone is safe, talk to your doctor. Naloxone is safe, reliable, and the easiest way to prevent an overdose or to delay it long enough to get someone to the hospital. It can and does save thousands of lives. If you or a loved one is using, having it on hand could make all the difference.

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