You get naloxone! You get naloxone! YOU ALL GET NALOXONE!

Finally! Some encouraging news coming from the frontline of the opioid overdose crisis. Naloxone nasal spray has been approved as an over-the-counter (OTC) product to rapidly reverse opioid overdose in emergency situations. Yes, we are a bit late on this post, as the approval occurred March 29, 2023. However, we wanted to further explore naloxone and the impact this approval has on those affected by the overdose crisis.


What is Naloxone – Naloxone Dose?

Before getting too thick in the weeds on this from a harm reduction perspective, we first need to establish what naloxone is.

Naloxone is a mu-opioid receptor antagonist that was initially approved for reversal of opioid overdose in 1971. As an antagonist, it binds to mu-opioid receptors with extremely high binding affinity (the thermogenic drive between receptor and drug), but does not exert any conformational change to the receptor and does not produce any pharmacologic activity. Thus, it effectively blocks the receptor and prevents other opioids or opioid peptides from binding to it. And, in the case of an opioid overdose situation, naloxone (usually) can displace the opioid already bound, which rapidly reverses an overdose event (morphine reversal, heroin reversal, fentanyl reversal, etc). This competitive antagonism at mu-opioid receptors helps stimulate respiratory drive that was being suppressed by the opioid agonist causing the overdose. It also may reverse euphoria, cause agitation, intense stimulation, and pain (if the patient was using the opioid for pain).

Prior to the recent FDA approval, naloxone was available via prescription as a nasal spray, intramuscular, and intravenous formulation. It has also been available as a subcutaneous auto-injector. The nasal spray specifically comes in three different strengths. The original 2mg and 4mg strengths, as well as the recently approved 8mg dose of naloxone that was approved in 2021 (Kloxxado).


Why the need for a super high naloxone dose? Well, with the rising rates of fentalogues entering the illicit drug market over the past years, and their increased potencies and binding affinities at mu-opioid receptors, there was increased need for a higher dose naloxone product to overcome those powerful derivatives. At higher doses, naloxone has a better chance of competing with those potent opioids to reverse opioid overdose.



How to use Naloxone?

The most frequently asked question about naloxone is when the heck should I actually use it?


Well, that’s great, but doesn’t explain exactly how to recognize when an overdose is occurring.

We list the steps of identifying someone who may require naloxone administration below. One of the most crucial of these steps is understanding the signs and symptoms of an opioid overdose. These include a person who is Unresponsive to voice or touch and will not wake up when called, has Breathing that is very slow, irregular, or who is not breathing at all, and whose Eye pupils (the center part of the eye) are tiny or ‘pinpoint’. Use the pneumonic UBE!


Identify Someone with Suspected Opioid Overdose:

  1. Ask the person if they are okay, shout out their name.
  2. Shake shoulders or upper body, firmly rub the middle of their chest.
  3. Check signs of opioid overdose –> UBE!!


If someone is suspected to be overdosing from an opioid and remains unresponsive, the following outlines how to give naloxone nasal spray.


How to Use Naloxone Nasal Spray:

  1. Lay the person on their back.
  2. Hold the naloxone nasal spray with thumb on bottom of plunger and first and middle fingers on either side.
  3. Insert the tip of the nozzle into EITHER nostril.
  4. Tilt head back and provide support under neck with your hand.
  5. Insert nozzle until fingers on either side of the nozzle are against the bottom of the nose.
  6. Press plunger firmly to spray the naloxone into the nostril.
  7. Remove naloxone from the nostril after giving the dose.
  9. Move the person on their side into the recovery position.
  10. Watch the person for 1-2 minutes.
  11. If the person does NOT respond by waking up, touch, or voice, or if breathing does not return to normal…
  12. ADMINISTER ANOTHER DOSE into the other nostril.
    1. Naloxone nasal spray may be dosed every 2-3 minutes.
    2. You will have to use a new nasal spray for each dose administered.
  13. Continue this process every 2-3 minutes until the person responds or emergency medical help is received.


*Remember, if an overdose is suspected, GIVE NALOXONE FIRST, and then call 911! Reversing a potential opioid overdose as quickly as possible is important. Seconds without respiratory ability can mean life and death!


Naloxone OTC: Bottom Line:

As of March 29, 2023, naloxone nasal spray has been the first naloxone product approved for use as an OTC medication; thus, no longer requires a prescription. Importantly, this only applies to the 4mg nasal spray dose and not the newer 8mg product. While most states already had blanket prescriptions in place allowing patients to present to the pharmacy to get naloxone without having to obtain a physical prescription from their doctor, the latest progression of availability of naloxone is the next logical step in loosening restrictions and enhancing access.

It is often overstated, for good reason, but every year there seems to be record highs in overdose related deaths in the United States, which are now being primarily driven by illicitly manufactured fentanyl analogues and polysubstance use. Because of the increased presence of ultra-potent opioids in the drug supply, often in discrete and unknown ways, overdose rates have dramatically spiked over the past decade and are now uncontrolled. Overdoses are occurring in both patients with active substance use disorders and those who may just use substances recreationally or therapeutically. Considering all this, there has been a substantial need for increased access to naloxone for years. Therefore, the latest evolution of naloxone availability and OTC status does certainly feel overdue. In fact, our founder called legislatures out seven years ago for these exact delays.

The actions by the FDA to allow naloxone to be purchased OTC without a prescription will hopefully ‘arm’ anyone and everyone with the ‘ammunition’ needed to continue fighting back against opioid overdoses. This represents a critical step in curbing overdose deaths and limiting the progression of this overdose epidemic. However, more actions are desperately needed to take a stand against this crisis. We still need increased access to Medication Assisted Treatment (MAT), we need more efficacious MAT in general, we need better coverage for addiction medicine and behavioral health services, and, perhaps, we need a complete overhaul of how we view illicit drug use throughout this country. This includes evaluating archaic, and often racially biased, laws around drug use that continue to make matters worse from a substance use perspective and continue to perpetuate gaps in socioeconomic and racial disparities across all healthcare.

Additionally, because the manufacturers are still controlling naloxone prices, the next enormous concern may be who can actually afford OTC naloxone!

What good is availability if it costs too much?

Time will only tell how effective this strategy is (the hope is that, yes, expanding naloxone access will help curb overdose rates). At least it is a step, finally, in the right direction.


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