Naloxone (Nasal)

Naloxone nasal spray is used in the emergency treatment of a suspected or known opioid overdose as evidenced by respiratory or central nervous system depression.

Overview

Naloxone is used for partial or complete opioid depression. It is used in emergency cases of suspected or known opioid overdose and is administered into the body via the intranasal route. It is a narcotic medication that is also used to reverse narcotic drugs effects during a surgery or to relieve pain. Once the overdose is suspected, Naloxone is given to the patient at an initial dose of 4mg. The dosage can be repeated after every 2 to 3 minutes until the patient improves or medical assistance becomes available. The effects of this drug are rapid but do not last for long. While treating an opioid overdose, a breathing treatment like mechanical ventilation, oxygen tubes, and mechanical respiration is also made available to help the patient recover quickly.

Condition treated

  • Opioid overdose

Type Of Medicine

  • Opioid antagonist

Side Effects

Along with the intended effects, Naloxone may sometimes bring unwanted effects. The most common side effects experienced are body aches, abdominal pains and stomach cramps, diarrhea, troubled or difficult breathing, convulsions, excessive crying, fever, pounding, fast or irregular heart pulse. Some patients have also reported having goosebumps, excessive or increased jerking movements, irritability and irregular breathing.

Not all of these side effects need medical attention. Most of them tend to go away after a short while as the body adjusts itself to the medicine. Also, your healthcare provider may give you some tips on what to do to reduce the adverse side effects. The effects may be severe to some patients than others hence it is advisable to check with your doctor if you have any question or if the effects become bothersome.

Naloxone may sometimes cause other worth mentioning effects although their occurrence is rare. Cases of patients are becoming extraordinarily nervous or having pale blue lips, skin and fingernails have been reported. The drug may also cause other minor effects that do not last for long like a runny nose, shivering, sweating, yawning, sneezing and trembling.

The medication may precipitate sudden opioid withdrawal in the physically challenges persons. The most common signs and symptoms are sweating, nausea and vomiting, cramping, insomnia, anxiety, sneezing, lacrimation, hot chills, restlessness, tachycardia, irritability hypertension seizures, cardiac arrest, and piloerection. It may also cause hyperactive reflexes and convulsions.

In the postoperative patients or those with cardiovascular disease, the drug may cause the following side effects: hypertension, hypotension, ventricular fibrillation, ventricular tachycardia, cardiac arrest and left ventricular failure. In some cases, coma, encephalopathy, and death have been reported.

Dosage

Naloxone is only given as per the doctor's prescription when there is a suspected or known opioid overdose. It is administered to the body through the nose. The medication is only used in emergency cases, and therefore it should not be substituted for medical attention. Extreme caution is needed while using to prevent it from getting in contact with the eyes or skin.

The drug comes with a leaflet that contains all the usage and dosage instructions. The patient is required to read and understand them and ask the doctor anything that is not understood.

To use the Naloxone nasal spray:

Remove the medicine from its original box then open it by peeling the back tab with the circle.

Do not prime or test the spray because it contains only a single Naloxone dose and it cannot be reused.

Hold the drug with your thumb placed on the lower side of the plunger and the other finger on both sides of the nozzle.

Carefully insert the nozzle in the patient's nostril. Do this with your hands placed on the vents until both sides lie against the nose of the patient.

Firmly press down the plunger to administer the dose then gently remove the spray after giving out the dose.

Move the patient to recovery position (on their side) after administering the medicine then seek immediate medical attention.

Observe the patient to monitor their condition. You can also give additional doses after every 2 to 3 minutes until you get medical care or until the patient responds well.

Naloxone is administered differently in different patients. Strictly follow the instructions given on the label or the doctor's instructions. The dosage information given below only contains the average dosage. Your healthcare provider may give you a different dosage depending on some factors. If yours differs from this, do not change your dosage.

For the nasal spray dosage (opioid overdose treatment)

For both adults and children - the initial dose administered is 4mg (1 spray in the patient's nostril). Other sprays may be administered after every 2 to 3 minutes until the patients show a positive response or until medical help becomes available.

Repeat dosing:

Seek immediate medical help right away after giving out the initial dose.

The repeat dosage requirement depends on the type, amount and the administration route used for the opioid.

The administration for the repeat doses is administered in alternate nostrils in the patient's nose.

If the patient first responds well then relapses back to the depression again before emergency medical help becomes available, give additional doses of Naloxone using a new spray then continue with close surveillance.

If the patient does not achieve the desired response, continue administering the medicine after every 2 to 3 minutes.

Additional resuscitative/supportive measures can be helpful while still waiting for the emergency medical assistance.

The dosage modifications for both partial opioid agonists and mixed agonists like pentazocine and buprenorphine may be incomplete and need higher Naloxone doses or repeat administration.

Interactions

Drugs interact in the human body with some causing dangerous reactions. Some drugs should not be used with others since the effectiveness may be reduced. It is important to tell your doctor all the drugs that you are taking before the drug is administered. Keep a record of the prescribed drugs, non-prescribed medications, vitamin supplements and herbal medicines that you are taking to avoid having drug interactions. Large Naloxone doses are needed to antagonize Buprenorphine since the latter contains an extended action duration.

Inform your doctor if you are taking any of the following drugs.

  • Any opioid family drugs, including codeine, Abstral, Actiq, Zohydro (hydrocodone)
  • Drugs that have topiramate, like Qsymia or Topamax
  • Conzip, Ryzol, Rybix, Ultram, or Ultracet (tramadol)
  • The supplement yohimbine

Inform your doctor if you take alcohol or tobacco. Naloxone should not be used together with alcohol because it can worsen the condition.

Warnings

Naloxone nasal spray should be administered with caution to newborns whose mothers are suspected or known to be dependent on an opioid. In those cases, a complete or immediate opioid effects reversal can precipitate a sudden withdrawal syndrome.

The signs of opioid withdrawal in physically dependent patients are body aches, tachycardia, sneezing, diarrhea, fever, nervousness, sweating, runny nose, piloerection, restlessness yawning, abdominal cramps, shivering and trembling. In the neonate, the patient may display excessive crying, convulsions and hyperactive reflexes.

Patients who have responded well to the Naloxone spray need to be kept under close monitoring. For those who have not responded, the repeat doses should be given using a new spray each time and be administered after every 2 to 3 minutes until medical help becomes available.

Naloxone is not an effective medication for respiratory depression caused by non-opioid drugs or acute toxicity management due to levopropoxyphene. The respiratory reversal depression by both the partial and mixed agonists/antagonist like pentazocine and buprenorphine may be incomplete and require higher Naloxone doses. If the patient shows an incomplete response, the respirations should be assisted mechanically as per the clinical indications.

If you are a family member or a caregiver administering the drug, carefully go through the instructions. Read the medical guide, instruction sheets and the caregiver information provided with this medication. Ask your health care provider any questions. Be sure you recognize all the opioid overdose signs and symptoms of your patient. Some of the symptoms are slowed or no breathing, pinpoint or tiny pupils in the eyes, slow heartbeats, and extreme drowsiness especially if the patient was sleeping. If you are not sure whether it's an opioid overdose or not but the patient is unresponsive or not breathing well, administer the nasal spray then seek immediate medical help.

Don't assume the overdose episode is over if the symptoms improve. Emergency medical help is still required after the spray. Cardiopulmonary resuscitation may be needed on the patient while waiting for medical assistance.

In addition to the Naloxone nasal spray, other resuscitative measures like artificial ventilation, vasopressor agents, cardiac massage, and free airways should be made available and used when necessary in order to counteract the acute opioid poisoning.

Abrupt postoperative opioid depression reversal may cause unwanted effects like vomiting, nausea, tremulousness, sweating, increased blood pressure, fibrillation and ventricular tachycardia. In some situations, it may cause cardiac arrest and result in death. Excessive Naloxone dosage in the postoperative patients can cause analgesia or agitation.

Tell your healthcare provider if you are pregnant or planning to become pregnant. Using Naloxone while pregnant may cause withdrawal in the unborn child. Additionally, your doctor will outweigh the benefits and risks of using the drug while pregnant and advice accordingly. Tell your doctor if you are breastfeeding.

Storage

Store the drug at room temperature away from direct sunlight and moisture. Do not freeze or keep in a bathroom. Keep the spray pump in the original box until when you are ready to give out the dose. Do not use the spray if it expires.

Summary

Naloxone nasal spray is used in emergency cases of opioid overdose. It is used before medical help becomes available, but it should not be substituted for the medical assistance. It is administered into the patient's nostrils and repeated after every 2 to 3 minutes if the patient does not show a positive response. A new spray should be used each time during the repeated doses and the drug administered in the alternate nostrils. For this medication to work well, the patient should be placed in a well-ventilated place or aid breathing by using oxygen tubes.

Naloxone may sometimes cause unwanted side effects like vomiting and nausea, convulsions and diarrhea which tend to go away shortly. Patients with hypertension, hypotension and heart failure should use the drug with caution because it may worsen the condition. Also, the medicine can cause withdrawal when used during pregnancy hence the doctor should be consulted first before giving out the drug.

The medicine may not be useful in blocking some opioids (mixed antagonists like buprenorphine and pentazocine). It requires a higher Naloxone dosage to block this opioid completely otherwise the blocking will be incomplete. The caregiver or family member who is administering the nasal spray should understand well the signs of opioid overdose which include slow heartbeat and pinpoint pupils. The patient should be taken for a medical checkup even if the symptoms improve after the Naloxone spray.