Naloxone

What is Naloxone?

Naloxone can be described as an FDA-approved medication that can rapidly reverse the effects of an overdose of opioids. Naloxone is an opioid antagonist that is able to attach to opioid receptors and neutralise the effects of other opioids.

Naloxone must be used whenever possible to treat a suspected or suspected overdose crisis in the event of slow breathing, extreme somnolence, or if the patient cannot take action (loss or loss of consciousness). After the naloxone treatment has been administered, the patient should receive urgent medical treatment immediately, even if they get up.Naloxone isn't a controlled substance, as per the US Drug Enforcement Administration (DEA).Naloxone can be purchased as a nasal spray (Narcan 4mg, Kloxxado 8mg) or as an injectable (Zimhi 5 mg/0.5 millilitres).

Narcan nasal spray was accepted by the FDA at the end of March 2023, as it is an over-the-counter (OTC) medication that can be purchased without the need for a prescription. There are other naloxone products that are prescription medications, but in several states, these medications can be purchased from a pharmacy without a prescription from a doctor, as per state naloxone accessibility laws or other arrangements.

Opioids can be referred to as narcotics. Examples of opioids include buprenorphine and codeine, fentanyl, oxycodone (Oxycontin), heroin, hydrocodone (Vicodin, Lortab), meperidine, hydromorphone, methadone, oxymorphone, and tramadol.
What exactly is Naloxone used for?

Naloxone is used to treat a recognised or suspected overdose emergency in adults or children. A sign of an overdose could include:

• Breathing is slowed, or there is an absence of breathing.
• Tiny or pinpoint pupils in the eyes.
• Low heartbeats;
• Severe drowsiness. This is especially true for sleepiness that is not able to awaken the person.

Even if you're not certain that an overdose of opioids is taking place, If the patient isn't breathing or is nonresponsive, administer immediate naloxone and get medical assistance in an emergency situation.

Naloxone can be used for different purposes when it is used in multi-ingredient medicines such as buprenorphine and naloxone (Suboxone, Zubsolv, and Bunavail) that are utilised to treat addiction to opioids, as well as naloxone with oxycodone (Targiniq in the ER), which is used to treat pain relief.

Warnings

In an emergency, it might not be feasible prior to being treated to inform your medical professionals about any health issues or if you're nursing or pregnant. It is important that the doctor who will care for you following treatment knows you've received this medication.
The person who is caring for you may give you Naloxone if you are unable to breathe or don't get up. It is important that the person who cares for you understands the location where you store this medication and how to administer it.

Your carer should seek urgent help following the administration of the medicine. It is possible that you will require another injection every 2–3 minutes until emergency assistance arrives.Drinking alcohol can trigger the negative effects of naloxone.

Naloxone can impair your thinking or your reactions. Be cautious when driving or doing things that require you to be vigilant.If you're using any of the narcotic pain medications, the effects of the pain-relieving narcotic are reversed as you also receive the medication.

Before you take this drug

It is not recommended to use this medication if you are allergic to naloxone or any of the inactive ingredients that are present in the nasal spray.

If you can, prior to getting naloxone, consult your doctor:

• If you suffer from heart issues,
• You are breastfeeding or pregnant.

The use of naloxone during pregnancy could trigger withdrawal consequences in the unborn baby. However, experiencing an overdose of opioids can cause foetal harm to the baby and mother. It is much more vital to deal with an overdose within the mother. It is essential to seek emergency medical help following the use of this medication. Make sure that all medical emergency personnel know you are pregnant.

If you take opioid medications while pregnant, your child could develop dependence on the medication. This can cause withdrawal symptoms that can be life-threatening for the newborn after it's born. Children who are dependent on opioids could require medical care for up to a week.

In the event of an emergency situation, you might not be able to tell the carers you're nursing or pregnant. Be sure that any doctor who cares for your child or pregnant mother is aware that you have received this medication.

How to take Naloxone?

Take Naloxone as directed by your physician. Follow all instructions on your prescription label and review all medication guides and instruction sheets.

If you're a carer or family member, you should read the entire instructions before you take this medicine to ensure that you know what you can do in the event of an emergency. Speak to your doctor or pharmacist If you have questions.

Naloxone injection instructions

• Each naloxone shot contains one dose of medicine. It cannot be used again.
• The patient should be placed on their back. Once the time is right to inject, slide off the cap and expose the needle.
• Don't put your fingers over the device. For children younger than 1 year, pinch the muscle in the thigh while applying the medication.
• Use your fingers to hold the naloxone injection grips and gently insert needles into the hip.
• Once the needle is in your thigh, it is recommended to move the plunger down until it clicks. Then keep it in place for two minutes.
• After the injection, with one hand and fingers positioned in front of the needle, move the safety guard across the needle. Do not use two hands to trigger this safety device. Place the syringe that you used into the blue container, and then shut the lid.

Naloxone nasal spray instructions

• Each nasal spray of naloxone contains just one dose of medication and can't be re-used.
• Place the person on their back. Assist their neck with your hand. Allow your head to tilt before spraying your nose.
• The nasal spray must be removed from the container. Pull back the tab to unblock the nasal spray bottle.
• Make sure to hold the nasal spray with your thumb resting on the plunger's bottom and place your middle and first fingers on the opposite side of the spray nozzle. Avoid applying pressure until you're able to administer the dosage.
• Simply put the tips of the nozzle in the nostril of one to ensure that your fingertips on the opposite side meet the inside of the nose.
• Push the plunger with a firm force to deliver the nasal spray dose. After administering the dose, take the spray and rinse the nasal passages.

After giving a dose of Naloxone

• You must seek medical emergency assistance as soon as possible after you've received the nasal spray or injection.
• Inform the doctor that you've received a dose of this medication.
• Reposition the patient on their back to put them in a recovery position following the administration of naloxone.
• If symptoms persist or recur after taking this medication, an additional dose could be required.
• If you're giving more doses, you can use the same nasal spray, a fresh nasal spray, or new injections every 2 to 3 minutes. You should continue to observe the person attentively until emergency assistance arrives.
• You might need to administer CPR (cardiopulmonary resuscitation) to the patient while you wait for emergency assistance to arrive.
• Naloxone is not a substitute for medical emergency treatment.

Details on dosage

Usual Adult Dose for Opioid Overdose

Initial dose:

• 0.4 mg to 2 mg. Alternatively, you can administer IM or subcutaneously.
• In the event that the desired reaction cannot be achieved, doses must be repeated at 2- to 3-minute intervals.
• If there is no response after a total dosage of 10, the possibility of opioid-induced or partially-induced toxicity by opioids must be considered.

Auto-injector:

• Give 0.4 mg (1 activation) IM or subcutaneously into the anterolateral side of your thigh (through the clothing, if needed).
• In the event that the intended response cannot be attained, a subsequent dose can be given within 2 or 3 minutes. Additional doses can be given every 2 to 3 minutes until medical help arrives.

Nasal Spray:

• Apply 1 spray intranasally through 1 nostril.
• In the event that the response you want cannot be reached within 2 or 3 minutes, If the desired response is not achieved, administer another dose intravenously into alternate nostrils; additional doses could be administered every two to three minutes through alternate nostrils until medical attention arrives.

Comments:

• The IV route is recommended for emergencies because it offers the fastest time to take action.
• The time of action of certain opioids is longer than the duration of this medication, so repeated doses could be required. The need for repeated doses is contingent on the dosage at which the drug is administered, its type, and the method of administration for the opioid being targeted.

Usual Adult Dose for Reversal of Opioid Sedation

Initial dose:

• 0.1 or 0.2 mg IV in intervals of 2-3 minutes according to the degree of reverse
• Doses that are added to the doses given IM have been demonstrated to have a lasting impact.

Intravenous Infusion:

• An amount of 0.004 mg/mL could be administered through IV infusion. The dose is titrated depending on the response of the patient.

Comments:

• To reverse a portion of the depression caused by opioids following the use of opioids in surgery, lower doses of Naloxone are typically sufficient. Higher doses than the ones required may result in a significant reversal of analgesia as well as a rise in blood pressure.

Usual Paediatric Dose for Opioid Overdose

Neonates:

• Dose for the first time: 0.01 mg/kg IV, either intramuscularly or subcutaneously. Repeat doses every 2 to 3 minutes, as required.

Children:

• The initial dose is 0.01 mg/kg IV. If the desired response cannot be achieved, you may offer 0.1 mg/kg IV.
• If the IV route is not accessible, you can provide it IM or subcutaneously in doses that are divided.
• Inject 0.4 mg (1 activation) IM or subcutaneously into the anterolateral side of your thigh (through the clothing if required). In the event that the desired response isn't achieved, the second dose can be administered within two or three minutes. Additional doses could be given every 2 to 3 minutes until medical aid arrives.
• Aged less than 1 year Thigh muscles should be squeezed while administering injections.

Comments:

• Opioid withdrawal in newborns could be life-threatening and should be treated following the protocols devised by experts in neonatology.
• To ensure that you do not trigger withdrawal symptoms, think about using a naloxone drug that is dosed in accordance with weight and then titrated until it has a positive effect.
• The duration of the action of some opioids is longer than the drug in question, so repeated doses are possible, and the necessity for repeated doses will be contingent on the dosage, type, and method of administration of the drug that is being targeted.
• Patients must remain under continuous monitoring. If a patient responds but then returns to respiratory depression, more doses are required.
• Other measures of support and/or resuscitation can be helpful in the event of medical emergencies.

Usual Paediatric Dose for Reversal of Opioid Sedation

Neonates:

• The dose to start is 0.01 mg/kg IV, either subcutaneously or IM, in 2 to 3 minute intervals, depending on the degree of reverse

Children:

• 0.005 mg up to 0.01 mg IV in 2 to 3 minute intervals according to the level of reverse

Intravenous Infusion:

• An amount of 0.004 mg/mL could be administered through IV infusion. The dose is titrated depending on the response of the patient.

Comments:

• To reverse a portion of the depression triggered by opioids after the administration of opioids during surgery, smaller doses of Naloxone are typically sufficient. More than the doses that are required can cause a significant decrease in analgesia and increase blood pressure.

What happens If I overdose?

Get medical attention in an emergency or contact the poison help line at 1-800-222-1222.

What should be avoided?

Be sure not to leave someone alone after administering a naloxone dose. Overdoses can alter a person's ability to think or react.

Side effects of Naloxone

Contact a medical professional immediately. If you notice symptoms of an allergy reaction, take Naloxone. itching, breathing difficulties, or swelling of your lips, face, and throat.

Because naloxone blocks opioid effects The administration can cause abrupt withdrawal symptoms, such as:

• Nausea, vomiting, diarrhoea, and  stomach pain;
• Sweating, feverish muscles, weakness, and fever;
• Shaking or tremors, rapid heart rate, beating at a rapid pace, and increased blood pressure
• Goosebumps Shivering and goosebumps
• Stuffy nose or yawning.
• Experiencing anxiety, agitation, or even irritability.

In the case of sudden withdrawal symptoms, infants less than 4 weeks old could be life-threatening if they are not taken care of in the correct manner. Symptoms include crying, stiffness, overactive reflexes, and seizures. Consult your physician or seek urgent medical attention if you aren't sure how to administer this medicine to your baby.

This is not a comprehensive list of all the side effects. Other side effects could be present. Consult your physician for advice regarding medical adverse effects. You can report symptoms to the FDA at 1-800-FDA-1088.

Interaction with other drugs

Other medications may cause an interaction with naloxone, such as medications that are prescribed and available over the counter, vitamins, and herbal products. Discuss with your doctor your current medications as well as any medications you are about to start or stop taking.