Naloxone | SAMHSA

What Is Naloxone?

Naloxone is a medication approved by the Food and Drug Administration (FDA) designed to rapidly reverse opioid overdose. It is an opioid antagonist—meaning that it binds to opioid receptors and can reverse and block the effects of other opioids, such as such as heroin, morphine, and oxycodone. Administered when a patient is showing signs of opioid overdose, naloxone is a temporary treatment and its effects do not last long. Therefore, it is critical to obtain medical intervention as soon as possible after administering/receiving naloxone.

The medication can be given by intranasal spray (into the nose), intramuscular (into the muscle), subcutaneous (under the skin), or intravenous injection.

A practitioner should assess the need to prescribe naloxone for patients who are receiving medication-assisted treatment (MAT) or otherwise considered a risk for opioid overdose.

Candidates for naloxone are those who:

• Take high doses of opioids for long-term management of chronic pain
• Receive rotating opioid medication regimens
• Have been discharged from emergency medical care following opioid poisoning or intoxication
• Take certain extended-release or long-acting opioid medication
• Those who have had a period of abstinence to include those recently released from incarceration.

Pregnant women can be safely given naloxone in limited doses under the supervision of a doctor.

A doctor or pharmacist can show patients, their family members, or caregivers how to administer naloxone.

Patients given an automatic injection device or nasal spray should keep the item available at all times. It is important to remember to replace medication when the expiration date passes and if exposed to temperatures below 39F or above 104F.

Naloxone is effective if opioids are misused in combination with other sedatives or stimulants. It is not effective in treating overdoses of benzodiazepines or stimulant overdoses involving cocaine and amphetamines.

Side Effects of Naloxone

Patients who experience an allergic reaction from naloxone, such as hives or swelling in the face, lips, or throat, should seek medical help immediately. They should not drive or perform other potentially unsafe tasks.

Use of naloxone causes symptoms of opioid withdrawal. Medical assistance must be obtained as soon as possible after administering/receiving naloxone.

Opioid withdrawal symptoms include:

• Feeling nervous, restless, or irritable
• Body aches
• Dizziness or weakness
• Diarrhea, stomach pain, or nausea
• Fever, chills, or goose bumps
• Sneezing or runny nose in the absence of a cold

Opioid Overdose

Opioid overdose can happen:

• When a patient misunderstands the directions for use, accidentally takes an extra dose, or deliberately misuses a prescription opioid
• With illicit drug use
• If a person takes opioid medications prescribed for someone else
• If a person mixes opioids with other medications, alcohol, or over-the-counter drugs

Signs of opioid overdose:

• Person does not wake or respond to touch or voice
• Breathing is not normal, very slow, or has stopped
• Pin-point sized pupils
• Bluish lips and nose

Opioid overdose is life-threatening and requires immediate emergency attention. Recognizing the signs of opioid overdose is essential to saving lives. Learn more about opioid overdose.

SAMHSA’s Efforts to Expand the Use of Naloxone

SAMHSA continues to work with its federal partners, states, first responders, and other stakeholders to educate on the use of and increase access to naloxone.

In an effort to save more lives from opioid overdose, SAMHSA published the Opioid Overdose Prevention Toolkit – 2018. The Toolkit equips communities and local governments with material to develop policies and practices to help prevent opioid-related overdoses and deaths. It also serves as a foundation for educating and training:

• Communities
• Prescribers of opioid pain medications
• First responders
• Patients who are prescribed opioid medications
• Individuals and family members who have experienced an opioid overdose

Training on Providing Naloxone

Naloxone is a prescription drug. You can buy naloxone in many pharmacies, in some cases without a prescription. It’s important to understand how to administer naloxone properly.

SAMHSA offers tools, training, and technical assistance to practitioners in the fields of mental and substance use disorders. Find information on SAMHSA training and resources.

Resources and Publications

Naloxone DrugFacts | National Institute on Drug Abuse (NIDA)

What are some signs of an opioid overdose?

• unconsciousness
• very small pupils
• slow or shallow breathing
• vomiting
• an inability to speak
• faint heartbeat
• limp arms and legs
• pale skin
• purple lips and fingernails

What is naloxone?

Naloxone is a medicine that rapidly reverses an opioid overdose. It is an opioid antagonist. This means that it attaches to opioid receptors and reverses and blocks the effects of other opioids. Naloxone can quickly restore normal breathing to a person if their breathing has slowed or stopped because of an opioid overdose. But, naloxone has no effect on someone who does not have opioids in their system, and it is not a treatment for opioid use disorder. Examples of opioids include heroin, fentanyl, oxycodone (OxyContin^®), hydrocodone (Vicodin^®), codeine, and morphine.

How is naloxone given?

Naloxone should be given to any person who shows signs of an opioid overdose or when an overdose is suspected. Naloxone can be given as a nasal spray or it can be injected into the muscle, under the skin, or into the veins. Steps for responding to an opioid overdose can be found in the Substance Abuse and Mental Health Administration’s (SAMHSA) Opioid Overdose Prevention Toolkit.

First Responders Can Safely Administer Naloxone during the COVID-19 Pandemic (HHS)

What are the different naloxone delivery systems?

Naloxone comes in two FDA-approved forms: injectable and prepackaged nasal spray. No matter what dosage form you use, it’s important to receive training on how and when to use naloxone. You should also read the product instructions and check the expiration date.

• Injectable brands of naloxone are offered by different companies listed in the FDA Orange Book under “naloxone” (look for “injectable”). The proper dose must be drawn up from a vial. Usually, it is injected with a needle into muscle, although it may also be administered into a vein or under the skin.
  • Note: Some people use an improvised nasal spray emergency kit not approved by the FDA that combines injectable naloxone with an attachment designed to deliver naloxone through the nose. However, this improvised intranasal device is not easy to assemble, especially when under pressure in an emergency, and requires training beforehand. Additionally, the FDA-approved naloxone devices have been shown to produce substantially higher blood levels of naloxone than the improvised nasal spray. These outcomes suggest that the approved prepackaged nasal spray technology is preferable over non-FDA-approved forms.
• Prepackaged Nasal Spray (generic naloxone, Narcan^®, Kloxxado^®), developed as a result of NIDA-funded research, is an FDA-approved prefilled, needle-free device that requires no assembly and is sprayed into one nostril while the person lays on their back. This device can also be easier for loved ones and bystanders without formal training to use.

Is Narcan® the same as naloxone?

When naloxone was first approved to reverse opioid overdoses, its brand name was “Narcan.” There are now other formulations and brand names for naloxone, but many people continue to call all of these products “Narcan.” However, the proper generic name is “naloxone.”

Is there a preferable delivery system?

All systems used by first responders deliver the stated dose of naloxone and can be highly effective in reversing an opioid overdose. Study findings released in March 2019 suggests that the FDA-approved naloxone devices deliver higher blood levels of naloxone than the improvised nasal devices.

Can I give naloxone to someone who has overdosed?

Yes. Families with loved ones who struggle with opioid addiction should have naloxone nearby; ask their family member to carry it; and let friends know where it is. People should still call 911 immediately in the event of an overdose.

Naloxone is being used more by police officers, emergency medical technicians, and non-emergency first responders than before. In most states, people who are at risk or who know someone at risk for an opioid overdose can be trained on how to give naloxone. Families can ask their pharmacists or health care provider how to use the devices.

What precautions are needed when giving naloxone?

Naloxone works to reverse opioid overdose in the body for only 30 to 90 minutes. But many opioids remain in the body longer than that. Because of this, it is possible for a person to still experience the effects of an overdose after a dose of naloxone wears off. Also, some opioids are stronger and might require multiple doses of naloxone. Therefore, one of the most important steps to take is to call 911 so the individual can receive immediate medical attention. NIDA is supporting research for stronger formulations for use with potent opioids like fentanyl.

People who are given naloxone should be observed constantly until emergency care arrives. They should be monitored for another 2 hours after the last dose of naloxone is given to make sure breathing does not slow or stop.

Tolerance vs. Dependence vs. Addiction

Long-term use of prescription opioids, even as prescribed by a doctor, can cause some people to develop a tolerance, which means that they need higher and/or more frequent doses of the drug to get the desired effects.

Drug dependence occurs with repeated use, causing the neurons to adapt so they only function normally in the presence of the drug. The absence of the drug causes several physiological reactions, ranging from mild in the case of caffeine, to potentially life-threatening, such as with heroin. Some chronic pain patients are dependent on opioids and require medical support to stop taking the drug.

Drug addiction is a chronic disease characterized by compulsive, or uncontrollable, drug seeking and use despite harmful consequences and long-lasting changes in the brain. The changes can result in harmful behaviors by those who misuse drugs, whether prescription or illicit drugs.

People with physical dependence on opioids may have withdrawal symptoms within minutes after they are given naloxone. Withdrawal symptoms might include headaches, changes in blood pressure, rapid heart rate, sweating, nausea, vomiting, and tremors. While this is uncomfortable, it is usually not life threatening. The risk of death for someone overdosing on opioids is worse than the risk of having a bad reaction to naloxone. Clinicians in emergency room settings are being trained to offer patients immediate relief and referral to treatment for opioid use disorder with effective medications after an opioid overdose is reversed. NIDA offers tools for emergency clinicians here.

Side effects from naloxone are rare, but people might have allergic reactions to the medicine. Overall, naloxone is a safe medicine. But it only reverses an overdose in people with opioids in their systems and will not reverse overdoses from other drugs like cocaine or methamphetamine.

How much does naloxone cost?

The cost varies depending on where you get the naloxone, how you get it, and what type you get. Patients with insurance should check with their insurance company to see if this medicine is covered. Patients without insurance can check the retail costs at their local pharmacies. Some drug companies have cost assistance programs for patients unable to pay for it.

Where can I get naloxone?

Many pharmacies carry naloxone. In some states, you can get naloxone from a pharmacist even if your doctor did not write you a prescription for it. It is also possible to get naloxone from community-based distribution programs, local public health groups, or local health departments, free of charge.

Visit the Naloxone finder website to see resources in your area. Check with your local pharmacy.

Co-Prescribing Naloxone with Prescription Opioids

Some research suggests that when clinicians prescribe naloxone along with prescription opioids, the risk of opioid overdose decreases even if the naloxone prescription does not get filled. The naloxone prescription appears to serve as an important educational strategy. As a result, the CDC began recommending co-prescriptions in some cases, outlined in the CDC’s 2016 Guidelines and detailed by guidance issued by HHS in 2018. In August 2019, a study showed that overall national rates for naloxone co-prescription along with any opioid increased among Medicare Part D patients.

Points to remember

• Naloxone is a medicine that rapidly reverses an opioid overdose. It attaches to opioid receptors and reverses and blocks the effects of other opioids.
• Naloxone is a safe medicine. It only reverses overdoses in people with opioids in their systems.
• There are two FDA-approved formulations of naloxone: injectable and prepackaged nasal spray.
• Police officers, emergency medical technicians, and first responders are trained on how to give naloxone.
• In some states, friends and family members can be trained on how to give naloxone.
• Naloxone only works in the body for 30 to 90 minutes. It is possible for a person to still experience the effects of an overdose after naloxone wears off or need multiple doses if a potent opioid is in a person’s system.
• In some areas, you can get naloxone from pharmacies with or without a personal prescription from community-based distribution programs, or local health departments. The cost varies depending on where and how you get it as well as what type you get.

Learn more

For more information about naloxone and opioid use disorder, visit:

This publication is available for your use and may be reproduced in its entirety without permission from NIDA. Citation of the source is appreciated, using the following language: Source: National Institute on Drug Abuse; National Institutes of Health; U.S. Department of Health and Human Services.

Naloxone Nasal Spray: MedlinePlus Drug Information

Naloxone comes as a solution (liquid) to spray into the nose. It is usually given as needed to treat opiate overdoses. Each naloxone nasal spray contains a single dose of naloxone and should be used only once.

You will probably be unable to treat yourself if you experience an opiate overdose. You should make sure that your family members, caregivers, or the people who spend time with you know how to tell if you are experiencing an overdose, how to use naloxone nasal spray, and what to do until emergency medical help arrives. Your doctor or pharmacist will show you and your family members how to use the medication. You and anyone who may need to give the medication should read the instructions that come with the nasal spray. Ask your pharmacist for the instructions or visit the manufacturer’s website to get the instructions.

You should keep the nasal spray available at all times in case you experience an opioid overdose. Be aware of the expiration date on your device and replace the spray when this date passes.

Naloxone nasal spray may not reverse the effects of certain opiates such as buprenorphine (Belbuca, Buprenex, Butrans) and pentazocine (Talwin) and may require additional naloxone doses with a new nasal spray each time.

Symptoms of an opioid overdose include excessive sleepiness, not awakening when spoken to in a loud voice or when the middle of your chest is rubbed firmly, shallow or stopped breathing, or small pupils (black circles in the center of the eyes). If someone sees that you are experiencing these symptoms, he or she should give you your first naloxone dose and then call 911 immediately. After receiving the naloxone nasal spray, a person should stay with you and watch you closely until emergency medical help arrives.

To give the inhaler, follow these steps:

1. Lay the person on their back to give the medication.
2. Remove the naloxone nasal spray from the box. Peel back the tab to open the spray.
3. Do not prime the nasal spray before using it.
4. Hold the naloxone nasal spray with your thumb on the bottom of the plunger and your first and middle fingers on either side of the nozzle.
5. Gently insert the tip of the nozzle into one nostril, until your fingers on either side of the nozzle are against the bottom of the person’s nose. Provide support to the back of the person’s neck with your hand to allow the head to tilt back.
6. Press the plunger firmly to release the medication.
7. Remove the nasal spray nozzle from the nostril after giving the medication.
8. Turn the person on their side (recovery position) and call for emergency medical assistance immediately after giving the first naloxone dose.
9. If the person does not respond by waking up, to voice or touch, or breathing normally or responds and then relapses, give another dose. If needed, give additional doses (repeating steps 2 through 7) every 2 to 3 minutes in alternate nostrils with a new nasal spray each time until emergency medical assistance arrives.
10. Put the used nasal spray(s) back in the container and out of reach of children until you can safely dispose of it.

Ask your pharmacist or doctor for a copy of the manufacturer’s information for the patient.

Adverse events after naloxone treatment of episodes of suspected acute opioid overdose

Objective:

An increasing and serious heroin overdose problem in Oslo has mandated the increasing out-of-hospital use of naloxone administered by paramedics. The aim of this study was to determine the frequencies and characteristics of adverse events related to this out-of-hospital administration by paramedics.

Methods:

A one-year prospective observational study from February 1998 to January 1999 was performed in patients suspected to be acutely overdosed by an opioid. A total of 1192 episodes treated with naloxone administered by the Emergency Medical Service system in Oslo, were included. The main outcome variable was adverse events observed immediately after the administration of naloxone.

Results:

The mean age of patients included was 32.6 years, and 77% were men. Adverse events suspected to be related to naloxone treatment were reported in 45% of episodes. The most common adverse events were related to opioid withdrawal (33%) such as gastrointestinal disorders, aggressiveness, tachycardia, shivering, sweating and tremor. Cases of confusion/restlessness (32%) might be related either to opioid withdrawal or to the effect of the heroin in combination with other drugs. Headache and seizures (25%) were probably related to hypoxia. Most events were non-serious. In three episodes (0.3%) the patients were hospitalized because of adverse events.

Conclusion:

Although adverse events were common among patients treated for opioid overdose in an out-of-hospital setting, serious complications were rare. Out-of-hospital naloxone treatment by paramedics seems to save several lives a year without a high risk of serious complications.

Zimhi (naloxone) dosing, indications, interactions, adverse effects, and more

NALOXONE – INJECTION

(nal-OX-one)

USES: This medication is used for the emergency treatment of known or suspected opioid overdose. Serious opioid overdose symptoms may include unusual sleepiness, unusual difficulty waking up, or breathing problems (ranging from slow/shallow breathing to no breathing). Other symptoms of overdose may include very small “pinpoint” pupils, slow heartbeat, or low blood pressure. If someone has serious overdose symptoms but you are not sure if the symptoms are due to overdose, give this medication right away anyway, since lasting slow/shallow breathing may cause permanent damage to the brain or death.Naloxone belongs to a class of drugs known as opioid antagonists. It works by blocking the effects of the opioid in the brain. This medication may not work as well to block the effects of certain types of opioids (mixed agonist/antagonists such as buprenorphine, pentazocine). With these types of opioids, blocking may be incomplete or you may need a higher dose of naloxone.Treatment of opioid overdose should also include breathing treatment (such as oxygen given through tubes in the nose, mechanical ventilation, artificial respiration).

HOW TO USE: This medication is given by a health care professional. It may be injected into a vein, a muscle, or under the skin.If you are using this medication at home, learn all preparation and usage instructions from your health care professional and the product package. Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid. Learn how to store and discard medical supplies safely.The dosage is based on your medical condition and response to treatment.The effects of this medication are rapid but not long-lasting. After giving naloxone, get medical help right away, even if the person wakes up. If symptoms return after giving an injection, give another naloxone injection every 2 to 3 minutes. Continue to closely watch the person until emergency help is received. Tell the healthcare professional that you have given an injection of naloxone.

SIDE EFFECTS: Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.In someone who has been using an opioid regularly, withdrawal symptoms can happen suddenly after receiving this medication. Withdrawal symptoms may include body aches, fever, sweating, watering eyes, runny nose, sneezing, goose bumps, yawning, weakness, shivering/trembling, nervousness, restlessness, diarrhea, nausea/vomiting, stomach cramps, increased blood pressure, fast heartbeat. In babies younger than 4 weeks who have been receiving an opioid regularly, sudden opioid withdrawal may be life-threatening if not treated the right way. Symptoms in babies may include seizures, crying more than usual, and muscle twitching/spasms.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using naloxone, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: heart problems (such as irregular heartbeat, previous heart attack).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. It may cause opioid withdrawal in an unborn baby whose mother has been regularly taking an opioid. The doctor will carefully monitor both the pregnant woman and the unborn baby after this medication is given. Ask your doctor for details.It is unknown if this medication passes into breast milk. However, it is unlikely to harm a nursing infant. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

OVERDOSE: Overdose in somebody not regularly taking an opioid is highly unlikely. However, if someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

NOTES: Ask your doctor or pharmacist about ways to prevent opioid overdose. Teach your close family or household members the signs and symptoms of an opioid overdose and tell them where you keep this medication.

MISSED DOSE: Not applicable.

STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

naloxone (injection) | CS Mott Children’s Hospital

What is the most important information I should know about naloxone?

In an emergency situation it may not be possible to tell your caregivers about your health conditions. Make sure any doctor caring for you afterward knows you have received this medicine.

What is naloxone?

Naloxone blocks or reverses the effects of opioid medication, including extreme drowsiness, slowed breathing, or loss of consciousness. An opioid is sometimes called a narcotic.

Naloxone is used to treat a narcotic overdose in an emergency situation. This medicine should not be used in place of emergency medical care for an overdose.

Naloxone is also used to help diagnose whether a person has used an overdose of an opioid.

Naloxone may also be used for purposes not listed in this medication guide.

What should I discuss with my health care provider before receiving naloxone?

You should not be treated with naloxone if you are allergic to it.

If possible before you receive a naloxone injection, tell your doctor if you have heart disease.

It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant.

It is not known whether naloxone passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

In an emergency situation it may not be possible to tell your caregivers if you are pregnant or breast-feeding. Make sure any doctor caring for your pregnancy or your baby knows you have received this medicine.

How is naloxone given?

Naloxone is injected into a muscle, under the skin, or into a vein through an IV. The injection may be given by a healthcare provider, emergency medical provider, or a family member or caregiver who is trained to properly give a naloxone injection.

If you are a caregiver or family member giving a naloxone injection, read all instructions when you first get this medicine. If provided, use the “trainer” device to practice giving an injection so you will know how to do it in an emergency. Ask your doctor or pharmacist if you have any questions.

Be sure you know how to recognize the signs of an opioid overdose in the person you are caring for. Overdose symptoms may include:

• slowed breathing, or no breathing;
• very small or pinpoint pupils in the eyes;
• slow heartbeats; or
• extreme drowsiness, especially if you are unable to wake the person from sleep.

Even if you are not sure an opioid overdose has occurred, if the person is not breathing or is unresponsive, give the naloxone injection right away and then seek emergency medical care.

Do not assume that an overdose episode has ended if symptoms improve. You must get emergency help after giving a naloxone injection.

Naloxone injected into a muscle is given in the outer thigh. In an emergency, you may give an injection through the person’s clothing.

After injecting naloxone, stay with the person and watch for continued signs of overdose. You may need to give another injection every 2 to 3 minutes until emergency help arrives. Follow all medication instructions carefully.

Each Evzio auto-injector is for one use only. Throw away after one use, even if there is still some medicine left in it after injecting a dose.

Store at room temperature away from moisture and heat. Keep the auto-injector in its outer case until you are ready to use it. Do not use the medicine if it has changed colors or has particles in it. Call your pharmacist for new medication.

What happens if I miss a dose?

Because you will receive naloxone in an emergency situation, you are not likely to miss a dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while using naloxone?

Avoid leaving a person alone after giving him or her a naloxone injection. An overdose can impair a person’s thinking or reactions.

What are the possible side effects of naloxone?

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Because naloxone reverses opioid effects, this medicine may cause sudden withdrawal symptoms such as:

• nausea, vomiting, diarrhea, stomach pain;
• fever, sweating, body aches, weakness;
• tremors or shivering, fast heart rate, pounding heartbeats, increased blood pressure;
• feeling nervous, restless, or irritable;
• goosebumps, shivering;
• runny nose, yawning; or
• (in babies younger than 4 weeks old) seizures, crying, stiffness, overactive reflexes.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect naloxone?

Other drugs may interact with naloxone, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all your current medicines and any medicine you start or stop using.

Where can I get more information?

Your pharmacist can provide more information about naloxone.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. (‘Multum’) is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum’s drug information does not endorse drugs, diagnose patients or recommend therapy. Multum’s drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2021 Cerner Multum, Inc. Version: 4.01. Revision date: 9/12/2017.

What is Naloxone & How Does it Work

If you need more information about naloxone and it’s benefits, call or visit your nearest Pharmaca location.
FIND YOUR PHARMACA PHARMACY >

What Is Naloxone?

Naloxone is an FDA approved medication that’s used to prevent opioid overdoses. It’s typically sold under the name Narcan (among other names). It blocks the effects of both recreational and prescription opioids, especially in the case of an overdose.

How does Naloxone work?

Naloxone is what’s known as a non-selective and competitive opioid antagonist. It works by reversing the depression of the central nervous system and respiratory system caused by opioids. It blocks opioid receptor sites, which in turn helps to reverse the effects of the overdose.

Naloxone administration

Naloxone is administered to patients to reverse opioid overdoses which can be life threatening. It may be delivered intramuscularly with a needle or intranasally with a mucosal atomizer device.

Using Naloxone is one of the best and quickest treatments of opioid overdoses. It is a non-addictive prescription medication. And although a dose is normally administered by emergency response personnel or health care professionals, you can also receive Naloxone doses that can be retained so that they can be administered later by a non-health-care professional in case of an emergency (much like an Epi-Pen in the case of severe allergic reactions).

People who might need to get a dose of Naloxone are:

• Take high doses of opioids for long-term management of chronic pain
• Receive rotating opioid medication regimens
• Have been discharged from emergency medical care following opioid poisoning or intoxication
• Take certain extended-release or long-acting opioid medications
• Are completing mandatory opioid detoxification or abstinence programs

Naloxone side effects

Although Naloxone side effects are not common, they can occur in some cases after taking the medication. People who experience an allergic reaction, such as hives or swelling in the face, lips or throat, should seek medical help immediately.

The use of Naloxone may cause symptoms similar to that of opioid withdrawal. These symptoms may include:

• Feeling nervous, restless, or irritable
• Body aches
• Dizziness or weakness
• Nausea, vomiting, diarrhea or stomach pain
• Fever, chills or goosebumps
• Sneezing or runny nose in the absence of a cold
• Increased heart rate
• High blood pressure

How long does Naloxone last?

After being administered to reverse the effects of opioid overdoses, naloxone’s potency lasts for about 30-to-90 minutes.

While the half-life of the medication is relatively short, the medication itself can stay in your system for much longer.

How long it stays in your body can vary depending on certain factors such as age, liver health and weight.

It can also depend on how the patient takes the medication that can determine how long it stays in the system.

It’s important to know that even if it is effective in reversing the overdose, the effects of opioids, including respiratory arrest, can last for several hours. This means that the Naloxone itself could potentially wear off before the opioids wear off, putting the individual at risk again for an overdose.

When it is taken orally or intravenously, up to 40 percent of the metabolites will be excreted within six hours. Within 24 hours, 50 percent will have been excreted, and 70 percent within 72 hours. In total, within a week or less, all metabolites of Naloxone should have left the system.

How do I get a Naloxone prescription?

Prescriptions are available from your healthcare provider, doctor or pharmacist.

They are also available on a walk-in basis from pharmacists at our pharmacies in all six states—California, Colorado, Illinois, New Mexico, Oregon and Washington.

FIND YOUR PHARMACA PHARMACY >

90,000 Health to the people – Naloxone – ZN 0.4mg / ml 1ml No. 10

INSTRUCTION

for the medical use of the drug

NALOXON-ZN

(NALOXONE-ZN)

Ingredients:

active substance: naloxone;

1 ml of solution contains naloxone hydrochloride dihydrate in terms of 100% substance, 0.4 mg;

excipients: sodium chloride, diluted hydrochloric acid, water for injection.

Dosage form. Injection.

Basic physical and chemical properties: transparent colorless liquid.

Pharmacotherapeutic group.

Antidotes. ATX code V03A B15.

Pharmacological properties.

Pharmacodynamics.

Naloxone is a competitive opioid receptor antagonist and belongs to the group of so-called “pure” opioid receptor antagonists.Blocks mainly μ-receptors and, due to significant affinity for these receptors, displaces narcotic analgesics from the binding sites, thus eliminating the symptoms of opioid overdose and eliminates the effect of both endogenous opiate peptides and exogenous opioid analgesics; to a lesser extent acts on other opiate receptors.

The introduction of naloxone prevents, weakens or eliminates (depending on the dose and time of administration) the effects of opioid analgesics, restores respiration, reduces sedation and euphoria, and weakens the hypotensive effect.

Naloxone eliminates the action of a wide group of narcotic drugs, both agonists and agonists-antagonists of opiate receptors: morphine, apomorphine, heroin, codeine, dihydrocodeine, promedol, methadone, pentazocine, fentanyl, buprenorphine.

The drug eliminates central and peripheral toxic symptoms: respiratory depression, pupillary constriction, delayed gastric emptying, dysphoria, coma and convulsions, as well as the analgesic effect of narcotic analgesics, in addition, it eliminates the toxic effect of large doses of alcohol.

Naloxone is also effective for respiratory disorders in mixed poisoning caused by opioids in combination with barbiturates, benzodiazepines and alcohol.
Naloxone induces withdrawal symptoms in opioid-dependent patients.

The drug has no analgesic activity, does not cause dysphoria and psychomimetic symptoms, the development of addiction and the formation of drug dependence.

Pharmacokinetics.

When administered intravenously, the action of the drug begins within 0.5-2 minutes, the duration of action is 20-40 minutes.When administered intramuscularly or subcutaneously, it acts in 2-3 minutes, the duration of action is 2.5-3 hours. The average half-life is 1-1.5 hours; in newborns, it is longer and is 3 hours. Naloxone is metabolized in the liver to form glucuronides. Metabolites are excreted in the urine. The effect of hepatic and renal failure has not been studied. Penetrates the blood-brain and placental barriers.

Clinical characteristics.

Indications.

Opioid overdose. To eliminate oppression of the respiratory center caused by opioids; to restore breathing in newborns after administration of opioid analgesics to a woman in labor; as a diagnostic tool in patients with suspected opioid dependence.

Contraindications.

Hypersensitivity to drug components.

Interaction with other medicinal products and other forms of interaction.

Naloxone-ZN eliminates the analgesic effect of opioid analgesics.

In opioid-dependent patients, administration of naloxone hydrochloride may cause severe withdrawal symptoms (hypertension, cardiac arrhythmias, pulmonary edema, cardiac arrest). The drug reduces the effects of tramadol and buprenorphine, but its effect is short-lived. This effect is believed to be the result of an arched dose-response curve of buprenorphine with decreased analgesia at high doses.

With the simultaneous use of Naloxone-ZN, it can reduce the antihypertensive effect of clonidine.
When using standard doses, the drug does not reverse the effects of barbiturates and tranquilizers.
Information on interactions with alcohol is mixed. In patients with multi-intoxication as a result of the action of opioids and sedatives or alcohol, depending on the cause of the intoxication, after the administration of naloxone hydrochloride, a less rapid effect on the elimination of some of the symptoms of multi-intoxication may be observed.

Incompatible with solutions of medicinal products containing bisulfites. Pharmaceutically compatible with 0.9% sodium chloride solution, 5% dextrose solution, sterile water for injection.

Application features.

The duration of action of some opioid analgesics may exceed the duration of action of Naloxone-ZN, therefore, patients should be under constant medical supervision and in conditions that allow mechanical ventilation and other resuscitation measures.

Patients with opioid dependence should be administered the drug very carefully, as withdrawal symptoms may occur. Hypertension, cardiac arrhythmias, pulmonary edema, and cardiac arrest have been described. This also applies to newborns in these patients.

Naloxone hydrochloride may cause hypotension, hypertension, ventricular tachycardia, fibrillation, and pulmonary edema. These adverse effects have been observed after surgery most often in patients who have cardiovascular disease or who have used medications that cause similar cardiovascular side effects.Although no direct causal relationship has been found, caution should be exercised when using Naloxone-3N for patients with heart disease or patients taking cardiotoxic agents that cause ventricular tachycardia, fibrillation, and cardiac arrest (e.g. cocaine, methamphetamine, cyclic antidepressants, calcium channel blockers, β-blockers, digoxin).

In experiments on animals, suppression of fertility and the absence of a teratogenic effect were found.

Use during pregnancy or lactation.

Animal studies have shown reproductive toxicity. The potential risk to humans is unknown.

During pregnancy, the drug should be prescribed only when the expected benefit to the mother outweighs the potential risk to the fetus. Naloxone hydrochloride may cause withdrawal symptoms in newborns.

It is not known whether naloxone passes into breast milk; therefore, if the drug is to be used, breastfeeding should be discontinued or avoided within 24 hours after using the drug.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

During the application of Naloxone-ZN, it is prohibited to drive vehicles and work with other mechanisms.

Method of administration and dosage.

Naloxone-ZN should be used intravenously by jet (injection), intravenous drip (infusion), and also intramuscularly. The dose is set by the doctor individually for each patient. Intramuscular injections should be prescribed in cases where intravenous administration is not possible.

In acute cases, intravenous administration of the drug should be preferred, as it provides the fastest therapeutic effect. When administered intramuscularly, the effect of the drug appears later, but lasts longer (compared to intravenous administration).
The duration of action of naloxone depends on the dose administered, the route of administration, and ranges from 45 minutes to 4 hours.

Since the effects of some opioids (eg, dextropropoxyphene, dihydrocodeine, methadone) last longer than the effects of naloxone, patients should be monitored continuously and repeated drug administrations should be given only if necessary.

Complete or partial elimination of the oppression of the respiratory center caused by opiates

Adults

Doses are determined by the doctor individually in order to normalize respiratory function while maintaining adequate analgesia. An intravenous injection of naloxone at a dose of 0.1–0.2 mg (approximately 1.5–3 mcg per kg of body weight) is usually sufficient. If necessary, you can additionally enter 0.1 mg with an interval of 2 minutes until breathing and consciousness are completely restored.Additional administration may be necessary in a period of 1 to 2 hours – depending on the type of action of the active substance (short-term effect or slow action), in relation to which naloxone is an antagonist, its amount used, duration and route of administration.
Alternatively, Naloxone-ZN can be used as an intravenous infusion. Some opioids have a longer duration of action than naloxone given as an intravenous bolus. Therefore, if the depression of the respiratory center is caused by such substances or there is a suspicion of this, naloxone should be used as an intravenous infusion.The rate of administration should be determined depending on the patient’s condition, as well as his response to intravenous injection and infusion. Continuous intravenous infusion should be considered and measures taken to maintain respiration if necessary.

Children

The initial dose of naloxone is 0.01-0.02 mg per 1 kg of body weight intravenously for 2-3 minutes until breathing and consciousness are fully restored. Additional doses may be given at intervals of 1–2 hours, depending on the patient’s response, dose and duration of action of the opiates used.

Acute opiate overdose

Adults

The starting dose is 0.4-2 mg intravenously. If breathing is not restored, the administration should be repeated after 2-3 minutes. Naloxone-ZN can also be administered intramuscularly (initial dose – 0.4-2 mg), if intravenous administration is not possible. If the patient’s condition has not improved with the introduction of naloxone at a dose of 10 mg, it can be concluded that the depression of the respiratory center is caused by other factors or other drugs, and not opioids.

Children

The recommended starting dose is 0.1 mg per 1 kg of body weight intravenously. If the desired effect is not achieved, in addition, in the form of injection, administer 0.1 mg per 1 kg of body weight. An intravenous infusion may be prescribed depending on the patient’s condition. If intravenous administration is not possible, Naloxon-ZN is administered intramuscularly at an initial dose of 0.01 mg per 1 kg of body weight, divided into several injections.

Respiratory recovery in newborns whose mothers received opioids

The usual dose is 0.01 mg per kg of body weight intravenously.If, when using this dose, the respiratory function is not restored, the administration can be repeated after 2-3 minutes. If intravenous administration is impossible, Naloxon-ZN is administered intramuscularly at an initial dose of 0.01 mg per 1 kg of body weight.

Elderly patients

Elderly patients with cardiovascular diseases or patients who have received cardiological drugs, Naloxon-ZN should be used with caution. It is necessary to take into account such undesirable effects as tachycardia and ventricular fibrillation in postoperative patients when prescribing Naloxone-ZN.

Dilution of solution

For intravenous infusion, Naloxon-ZN should be diluted with 0.9% sodium chloride solution or 5% glucose solution. The content of 5 ampoules of the drug (2 mg) should be diluted with 500 ml of one of the indicated solvents until the concentration of the finished solution is 4 μg / ml.

Before use, as well as after dilution, it is necessary to check the solution for transparency. Use only a clear, colorless solution without visible particles.

Children.

Use in pediatric practice according to the indications and in the doses indicated in the instructions.

Overdose.

Symptoms: nausea, vomiting, arterial hypertension, ventricular tachycardia, ventricular fibrillation, cardiac arrest, pulmonary edema.

Treatment: symptomatic.

To prevent overdose, it is necessary to strictly adhere to the recommended doses of the drug.

Adverse reactions.

With the rapid introduction of Naloxone-ZN, various side reactions may occur.

From the digestive system: nausea, vomiting, diarrhea, dry mouth.

From the cardiovascular system: arrhythmia, bradycardia, tachycardia, hypotension, arterial hypertension, ventricular fibrillation, cardiac arrest.

From the side of the central nervous system: tremors, convulsions, dizziness, headache, tension, hyperventilation.

Allergic reactions: rhinitis, shortness of breath, skin rash, itching, urticaria, erythema multiforme, angioedema, anaphylactic shock.

Others: increased sweating, postoperative pain, changes at the injection site, including irritation of the vascular wall (when administered intravenously), local irritation and inflammation (when administered intramuscularly).

The use of Naloxone-ZN in doses exceeding the recommended ones can cause a return of pain in the postoperative period and agitation, arterial hypotension or hypertension, ventricular tachycardia, ventricular fibrillation, pulmonary edema.

Withdrawal syndrome in patients with opioid dependence: vague pain, diarrhea, pyrexia, rhinorrhea, sneezing, excessive sweating, nausea, vomiting, nervousness, fatigue, irritability, tremor, epigastric spasms, tachycardia, weakness; in newborns – convulsions, diarrhea, hyperthermia, continuous screaming, hyperreflexia, sneezing, tremors, unusual irritability, vomiting.

The use of Naloxone-ZN in therapeutic doses in patients whose body does not contain opioids, as a rule, does not cause side effects.

Expiration date.

3 years.

Storage conditions.

Store in original packaging at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Incompatibility.

The drug is incompatible with solutions of drugs containing bisulfites, metabisulfites, long chain or high molecular weight anions, solutions with an alkaline pH.Should not be mixed with other medicines.

The preparation is intended for single use only.

Packing.

1 ml ampoule. 10 ampoules in a box.

1 ml ampoule. 5 ampoules in a blister, 2 blisters in a box.

1 ml in ampoule; 10 ampoules in a blister; 1 blister in a box.

Vacation category.

Prescription.

Manufacturer.

LLC “Kharkov pharmaceutical enterprise” Health to the people “.

Location of the manufacturer and its address of the place of business.

Ukraine, 61002, Kharkov, st. Melnikova, 41.

Date of last revision.

Oxycodone and Naloxone | Memorial Sloan Kettering Cancer Center

This document, provided by Lexicomp ^® , contains all the information you need to know about the drug, including the indications, route of administration, side effects and when you should contact your healthcare provider.

Trade names: Canada

Targin

Warning

• This medicine is a powerful pain reliever that can be addictive, abuse or misuse. Misuse or misuse of this drug can lead to overdose and death. Please consult your doctor.
• You will be closely monitored to avoid misuse, abuse or dependence on this drug.
• This drug may cause very bad and sometimes deadly breathing problems. Call a doctor right away if breathing is slow, shallow, or difficult.
• The risk of serious and sometimes fatal respiratory problems may be increased when this drug is started or if the dose is increased.
• Swallow whole. Do not chew, break, grind, or dissolve before swallowing. These actions can cause very serious side effects and death.
• Even one dose of this drug, by another person or by mistake, can be deadly, especially in children. If this drug has been taken by another person or by mistake, get medical help right away.
• Store all medicines in a safe place. Keep all medicines out of the reach of children and pets.
• Long-term use of this drug during pregnancy may cause withdrawal in newborn babies.This can be life threatening. Check with your doctor.
• This medicinal product contains an opioid. Serious side effects have occurred with the use of opioid drugs with benzodiazepines, alcohol, marijuana, or other forms of cannabis, as well as prescription or over-the-counter drugs that can cause drowsiness or slow action. These effects include slowed down or labored breathing and death. Benzodiazepines include drugs such as alprazolam, diazepam, and lorazepam.Benzodiazepines can be used to treat many health conditions such as anxiety, sleep disturbances, or seizures. If you have any questions, please consult your doctor.
• Many drugs interact with this drug, which can increase the risk of side effects, such as deadly breathing problems. Check with your doctor and pharmacist to make sure this drug is safe to use with all your other drugs.
• Do not take with alcohol or foods containing alcohol. Dangerous, sometimes deadly, effects can develop.
• Get immediate medical attention if you feel very sleepy, dizzy, or pass out. Guardians or others should seek immediate medical attention if the patient does not respond, does not respond, or does not respond normally, or if he is asleep and does not wake up.

What is this drug used for?

• Used to relieve pain.
• The drug is used only when long-term round-the-clock (continuous) treatment is required. It is also used only when other pain relievers are not effective enough or cannot be taken.

What should I tell my doctor BEFORE taking this drug?

• If you are allergic to this drug, any of its ingredients, other drugs, foods or substances. Tell your doctor about your allergy and how it manifested itself.
• If you have any of the following health conditions: Lung or breathing problems such as bronchial asthma, difficulty breathing, or sleep apnea; high levels of carbon dioxide in the blood; gastrointestinal obstruction or narrowing.
• If you have recently had a head injury, brain injury, or have recently developed a tumor or increased intracranial pressure.
• If you have any of the following health conditions: abdominal pain, appendicitis, or pancreatitis.
• If you have any of the following health conditions: kidney disease or liver disease.
• If you have recently drunk large amounts of alcohol or have taken a large number of drugs that slow the reaction rate, such as phenobarbital, or some pain relievers, such as oxycodone.
• If you have convulsions.
• If you are addicted to alcohol or opioid analgesics, or if you are experiencing withdrawal symptoms.
• If you have taken a drug for depression or Parkinson’s disease in the past 14 days. These include isocarboxazid, phenelzine, tranylcypromine, selegiline, or rasagiline. An episode of very high blood pressure may occur.
• If you are taking any of the following drugs: buprenorphine, butorphanol, linezolid, methylene blue, nalbuphine, or pentazocine.
• If you are or may become pregnant. Do not take this drug if you are pregnant.
• If you are breastfeeding. Do not breast-feed while taking this drug.
• If the patient is a child. Do not give this drug to a child.

This list of drugs and diseases that may be adversely associated with this drug is not exhaustive.

Tell your doctor and pharmacist about all the medicines you take (prescription and over-the-counter, natural products and vitamins) and your health problems.You need to make sure that this drug is safe for your medical conditions and in combination with other drugs you are already taking. Do not start or stop taking any drug or change the dosage without your doctor’s approval.

What do I need to know or do while taking this drug?

• Tell all healthcare providers that you are taking this drug.These are doctors, nurses, pharmacists and dentists.
• Avoid driving or other activities that require special attention until you can see how this drug is affecting you.
• To reduce the risk of dizziness or loss of consciousness, get up slowly from a lying or sitting position. Use caution when going up and down stairs.
• Do not take higher doses of the drug than your doctor has prescribed. Taking more than the prescribed amount of the drug increases the risk of serious side effects.
• Do not take this drug with any other strong pain reliever or with a pain reliever patch without first talking to your doctor.
• This drug may increase the risk of seizures in some people, including people with a history of seizures. Talk with your doctor to see if you are at increased risk of seizures with this drug.
• If this drug is taken for a long time or in high doses, its effectiveness may be reduced and a higher dose may be needed to obtain the same effect. The so-called drug tolerance develops. Talk to your doctor if this drug stops working. Do not take the drug in higher doses than your doctor prescribed.
• Long-term or regular use of opioid medications like this one can lead to dependence.Reducing the dose or stopping suddenly from this drug may cause a serious risk of a withdrawal reaction or other serious impairment. Talk to your doctor before lowering the dose or stopping this drug. Follow your doctor’s instructions. Tell your doctor if you experience severe pain, mood changes, suicidal thoughts, or any other side effects.
• Certain concentrations of this drug may only be used in people who have previously taken this type of drug and are used to its effects.Using the drug at these concentrations in people who have not previously taken this type of drug can cause very bad and sometimes deadly breathing problems. Check with your doctor.
• The tablet shell can sometimes be seen in the stool. This is normal and not a cause for concern.
• Consult a healthcare professional if you frequently drink grapefruit juice or eat grapefruit.
• If you are 65 years of age or older, use this drug with caution.You may have more side effects.
• If used during pregnancy, the drug may have a harmful effect on the fetus. If you are pregnant or become pregnant while taking this drug, call your doctor right away.

What side effects should I report to my doctor immediately?

WARNING. In rare cases, some people with this drug can cause serious and sometimes deadly side effects.Call your doctor right away or get medical help if you have any of the following signs or symptoms, which may be associated with serious side effects:

• Signs of an allergic reaction such as rash, hives, itching, reddened and swollen skin with blistering or scaling, possibly associated with fever, wheezing or wheezing, tightness in the chest or throat, difficulty breathing, swallowing or speaking, unusual hoarseness, swelling in the mouth, face, lips, tongue, or throat.
• Pain or pressure in the chest.
• Rapid, slow heartbeat, or irregular heartbeat.
• Severe dizziness or fainting.
• Mood swings.
• Hallucinations (a person sees or hears something that is not in reality).
• Confusion of consciousness.
• Difficulty walking.
• Severe constipation or abdominal pain. These may be signs of a severe bowel disorder.
• Convulsions.
• Difficulty breathing, slow or shallow breathing.
• Noisy breathing.
• Disturbed breathing during sleep (sleep apnea syndrome).
• Swelling of the hands or feet.
• A serious and sometimes deadly condition called serotonin syndrome can happen when this drug is used with certain other drugs. Call your doctor right away if you have anxiety, imbalance, confusion, hallucinations, fever, tachycardia or irregular heartbeat, flushing, muscle twitching or stiffness, seizures, tremors or tremors, excessive sweating, severe diarrhea, nausea or vomiting , severe headache.
• Occasionally, this type of opioid can cause very severe adrenal dysfunction. Call your doctor right away if you experience very severe dizziness or fainting, very severe nausea or vomiting, decreased appetite, feeling very tired or weak.
• Long-term use of an opioid drug can lead to a decrease in sex hormone levels. If you have a decreased interest in sex, impaired fertility, missing menstrual periods, or trouble ejaculating, see your doctor.

What are some other side effects of this drug?

Any medicine can have side effects. However, many people have little or no side effects. Call your doctor or get medical help if these or any other side effects bother you or do not go away:

• Feeling dizzy, sleepy, tired, or weak.
• Constipation, diarrhea, abdominal pain, nausea, vomiting, or decreased appetite.
• Headache.
• Excessive sweating.

This list of potential side effects is not comprehensive. If you have any questions about side effects, please contact your doctor. Talk to your doctor about side effects.

You can report side effects to the National Health Office.

You can report side effects to the FDA at 1-800-332-1088. You can also report side effects at https: // www.fda.gov/medwatch.

What is the best way to take this drug?

Use this drug as directed by your healthcare practitioner. Read all the information provided to you. Follow all instructions strictly.

• Take by mouth only.
• Do not use this drug rectally.
• This drug should not be given by injection or inhaled through the nose. Any of these actions can lead to very serious side effects such as breathing difficulties and death from overdose.
• Take with or without food. Take with food if the medicine causes nausea.
• Take this drug with a full glass of water.
• Do not use this medicine for immediate pain relief or as needed.
• Do not use this drug for pain relief after surgery if you have not previously taken this type of drug.
• Swallow whole. Do not chew, break, or crush.
• Consult your doctor if you have difficulty swallowing.

What to do if a dose of a drug is missed?

• Skip the forgotten dose and return to your normal schedule.
• Do not take 2 doses at the same time or an additional dose.

How do I store and / or discard this drug?

• Store at room temperature, protected from light. Store in a dry place. Do not store in the bathroom.
• Protect from heat.
• Store this medication in a secure place, out of the reach of children, and out of the reach of other people.A box or room, which is locked with a key, can act as a protected storage location for the drug. Keep all medicines out of the reach of pets.
• Dispose of unused or expired drugs. Do not empty into toilet or drain unless directed to do so. If you have any questions about the disposal of your medicinal products, consult your pharmacist. There may be drug recycling programs in your area.

General information about medicines

• If your health does not improve or even worsens, see your doctor.
• Do not give your medicine to anyone or take other people’s medicines.
• Some medicines may come with other patient information sheets. If you have questions about this drug, talk with your doctor, nurse, pharmacist, or other healthcare professional.
• Some medicines may come with other patient information sheets. Check with your pharmacist. If you have questions about this drug, talk with your doctor, nurse, pharmacist, or other healthcare professional.
• If you think an overdose has occurred, call a Poison Control Center immediately or seek medical attention. Be prepared to tell or show which drug you took, how much and when it happened.

Consumer Use and Limitation of Liability

This information should not be used to make decisions about taking this or any other drug. Only the attending physician has the necessary knowledge and experience to make decisions about which drugs are suitable for a particular patient. This information does not guarantee that the drug is safe, effective, or approved for the treatment of any disease or specific patient.Here are only brief general information about this drug. It does NOT contain all available information on the possible use of the drug with instructions for use, warnings, precautions, information about interactions, side effects and risks that may be associated with this drug. This information should not be construed as a treatment guide and does not replace information provided to you by your healthcare professional. Check with your doctor for complete information on the possible risks and benefits of taking this drug.Use of this information is governed by the Lexicomp End User License Agreement available at https://www.wolterskluwer.com/en/solutions/lexicomp/about/eula.

Copyright

© UpToDate, Inc. and its affiliates and / or licensors, 2021. All rights reserved.

90,000 Use of naloxone in neonates exposed to opioids

Review question

Does naloxone (a medication that counteracts the negative effects of opioids on breathing) help newborn babies whose mothers received opioid pain relievers during labor?

Relevance

When a woman is given opioids to relieve pain during labor (such as pethidine, morphine, and similar medications), the opioid can pass in the womb to the baby and then decrease the newborn’s breathing rate.Naloxone is a medication that counteracts the effects of opioids and can be given to a newborn to try to prevent or treat breathing problems. This can reduce the likelihood of the baby being admitted to the neonatal unit for breathing support, reduce the need to separate the mother and baby (and thus assist in establishing breastfeeding). However, there is concern that naloxone may cause side effects, including possible long-term developmental disabilities.

Research characteristics

We found nine completed clinical trials comparing the use of naloxone and a placebo (“sham drug”) in newborns whose mothers received opioids during labor. These clinical trials were conducted over 30 years ago and were generally very small, involving only about 300 children in total. Most clinical trials have not always used reliable methods. The evidence is current to February 2018.

Main Findings

Clinical trials reported the effect of naloxone on infant breathing, but did not assess the effect on the need to transfer babies to the neonatal unit (separate from the mother), whether they needed breathing support, and did not assess the effect on breastfeeding success. None of the clinical trials assessed long-term development in children. We did not find clinical trials involving children born to mothers who used opioids (prescribed or not) during pregnancy.

Quality of evidence

The available evidence is insufficient to determine whether the use of naloxone was beneficial or harmful in children whose mothers received opioids during labor.

Will you carry naloxone with you?

Opioid antidote can save lives

Julie Estlick

Jess Fear never goes without a dose of naloxone, a drug that can reverse the effects of opioid overdose.She is not a paramedic or nurse, and she does not struggle with substance use. Fear is a member of the Naloxone Champions, a group that educates and educates members of the public and local providers who work with substance users on how to deliver life-saving treatment for a loved one or stranger.

The opioid epidemic has resulted in a staggering number of deaths in the United States. Colorado reported about 960 overdose deaths last year.In Larimer County, nearly half of the 53 overdose deaths were attributed primarily to opiates, while 76 percent of those who died by suicide had drugs and / or alcohol, according to a county coroner’s report. The US Surgeon General issued a public health guideline urging more Americans to carry and learn to use naloxone, an antidote for opioid overdose. Opioids is the term for drugs that bind to opioid receptors in the body.These include illicit drugs such as heroin and legally available prescription pain relievers such as oxycodone, codeine, morphine, percocet, and synthetic opioid fentanyl, drugs that are sometimes sold and used illegally.

The reality is that almost anyone can get an overdose – you don’t have to take illegal drugs. “There could be an overdose of opioid pain relievers that are legally prescribed by a doctor,” says Strah, manager of mental health strategy and project implementation, Community Action Group, North Larimer County.”If your teen goes into your medicine cabinet and takes some of your prescription pills, he could overdose, regardless of whether or not he regularly uses drugs.”

So what is an opioid overdose? Opiates bind to receptors in the brain and act on the central nervous system; too much can slow down a person’s breathing rate so that they cannot breathe. When breathing stops, the heart stops – this is an overdose. Naloxone, also known under the brand name Narcan, works by repelling opiates from receptors in the brain and temporarily relieving the effects of respiratory distress.(See Figure for Signs of Overdose.)

The way opiates work on the brain makes it easy to become addicted. The good news is, addiction is curable. As Fear says, “I want people to understand that drug addiction treatment works and that recovery is possible. Naloxone is an important tool in this fight because people cannot recover if they are dead. ”

Naloxone is available as a nasal spray or injection. In addition to training for local residents, YouTube also has videos on how to take medication.Its side effects are minimal – headache, dizziness – and it won’t hurt if given to someone who hasn’t overdosed on drugs. It can be used safely for all ages and pets.

In the event of an overdose, it is imperative to call emergency services immediately and then administer naloxone so that the person suffering from an opioid overdose has a chance to survive until the arrival of emergency medical personnel. Naloxone works within minutes but only lasts 911 minutes or an hour.

Any adult in Colorado can buy naloxone at the pharmacy because the state has a standing order for the drug, which means you don’t need a prescription to buy it. A generic naloxone spray costs between $ 20 and $ 40 per dose, while Narcan costs between $ 130 and $ 140 for a set that includes two doses. It is currently sold by over 200 pharmacies in the state, including many in Fort Collins.

So, are you going to carry naloxone with you?

90,000 instructions for use, dosages, composition, analogs, side effects / Pillintrip

Medicines that depress the central nervous system (for example, alcohol, other opioids, sedatives and hypnotics, antidepressants, phenothiazines, antipsychotics, antihistamines and antiemetic drugs) can increase depressive the effect of the drug Targin ^® on the central nervous system.

The simultaneous use of oxycodone with anticholinergic drugs or drugs with anticholinergic activity (for example, tricyclic antidepressants, antihistamines, antipsychotics, muscle relaxants, antiparkinsonian drugs) may be accompanied by an increase in anticholinergic adverse reactions.

Alcohol can enhance the pharmacodynamic effects of Targin ^® , therefore, the use of Targin ^® should be avoided simultaneously with alcohol.

Patients concurrently taking oxycodone and coumarin anticoagulants showed clinically significant changes in INR values ​​in both directions.

Metabolism of oxycodone occurs mainly with the involvement of the isoenzyme of the cytochrome P450 system CYP3A4 and partially CYP2D6 (see.”Pharmacokinetics”). The activity of these metabolic pathways can be decreased or increased due to the influence of simultaneously used drugs or food products. Thus, the dose of Targin ^® should be adjusted accordingly.

Inhibitors of the CYP3A4 isoenzyme, such as macrolide antibiotics (clarithromycin, erythromycin, telithromycin), antifungals from the azole group (ketoconazole, voriconazole, itraconazole, posaconazole), HIV protease inhibitors (indinvirinavironavir), cyclone can reduce the clearance of oxycodone and lead to an increase in its plasma concentration.In this case, it may be necessary to reduce the dose of Targin ^® and re-select it.

Inducers of the CYP3A4 isoenzyme, such as rifampicin, carbamazepine, phenytoin and St. John’s wort, can activate metabolism and increase drug clearance, resulting in a decrease in plasma oxycodone concentration. Caution should be exercised and additional dose adjustments may be required to properly control pain.

Theoretically, drugs – inhibitors of the isoenzyme CYP2D6, such as paroxetine, fluoxetine and quinidine, can reduce the clearance of oxycodone and, accordingly, increase the concentration of oxycodone in plasma.Concomitant use with inhibitors of the isoenzyme CYP2D6 had little effect on the elimination of oxycodone and its pharmacodynamic effects.

The results of in vitro metabolism studies of indicate that clinically significant interactions between oxycodone and naloxone should not be expected. The likelihood of clinically significant interactions between paracetamol, acetylsalicylic acid, or naltrexone and the combination of oxycodone hydrochloride + naloxone hydrochloride at therapeutic concentrations is minimal.

Tactics for the treatment of side effects of strong opioids – Pro Palliative

Contents

Tactics for the treatment of side effects of opioids

Tactics for overdose of opioid analgesics

Comorbid conditions requiring special attention when prescribing opioids

help. A Practical Guide for a Doctor ”prepared by the Vera Charitable Foundation. The full version of the brochure is available for download here.

Explain the following to the patient:

• Constipation develops in almost everyone on strong opioids. To a lesser extent, constipation occurs with the use of fentanyl TTS and oxycodone + naloxone (targin) tablets. It is necessary to recommend the mandatory intake of a sufficient volume of food and water, to prescribe the regular use of laxatives for all patients.
• Nausea may occur when strong opioids are started or when the dose is increased, but usually gradually improves.
• Drowsiness or decreased alertness may occur when the strong opioids and all psychotropic drugs are started or the dose is changed, but they are often temporary. Warn patients that decreased concentration may be affecting their manual skills. Driving of cars and other vehicles is prohibited for patients receiving opioids and psychotropic drugs.

With careful titration of the opioid dose, toxic reactions are unlikely to occur.Toxicity is expressed in drowsiness, pupillary constriction, myoclonic seizures, confusion, hallucinations, and decreased respiratory rate. There may be other causes for these symptoms, so it is important to carefully review your medical history and prescription sheet. End-stage patients may have confusion, drowsiness, or irritability for a variety of other reasons.

Tactics for the treatment of side effects of opioids:

Opioid use is accompanied by sedation, which usually subsides within a few days after starting the opioid.For those with severe or worsening sedation, it is recommended that the opioid dose be reduced (if pain is sufficiently controlled) or the opioid should be changed (rotated). Reduce or stop taking adjuvant sedatives / anxiolytics. Additionally: intake of a sufficient amount of fluid, forced diuresis.

• Nausea / vomiting

Dose reduction or opioid substitution is recommended. Also prescribed dopaminergic drugs (haloperidol) and drugs with dopaminergic additional actions (metoclopramide), see the dose in the article “Choice of pain relievers”.

In patients with Parkinson’s disease, metoclopramide should be avoided.

Adequate intake of fluids and food is recommended. From the very beginning of opioid treatment, laxative therapy is necessary (if there is no diarrhea). To facilitate bowel emptying, osmotic laxatives that increase the absorption of water in the intestine (lactulose, macrogol, etc.), as well as agents that stimulate the function of the colon (senna, bisacodyl, sodium picosulfate) or the small intestine (castor, liquid paraffin), will help, see the article “Choice of Pain Relief Drugs” for doses.If laxatives are ineffective, regular cleansing enemas may help.

Opioids stimulate the release of histamine. Treatment involves reducing the dose or changing the opioid, possibly using antihistamines, see the dose in the article “Choosing Pain Relief Drugs”.

Dose reduction or opioid change recommended. To consider the possibility of using antipsychotics (haloperidol), see the dose in the article “The choice of painkillers”.

• Confusion of consciousness / delirium

Reducing the opioid dose, changing the opioid, adjusting the dose of antipsychotics (haloperidol), see the article “Choice of pain medications” for the dose.

Dose reduction or opioid change recommended. Consider the use of benzodiazepines, clonazepam, baclofen, etc., see the dose in the article “Choice of pain relievers”.

• Bradypnea and apnea

Sedation precedes respiratory failure and hypoxia due to opioid overdose.

Important

If bradypnea and apnea occur, stop using the opioid! Open windows! Activate the patient with loud speech, patting on the cheeks, inhaling ammonia.

It is recommended to inject naloxone in low doses and slowly: dilute 1 ampoule of naloxone 0.4 mg (1 ml ampoule of naloxone contains 0.4 mg / ml) in 9 ml of isotonic solution to obtain a final concentration of 0.04 mg / ml. Perhaps the introduction of respiratory analeptics (sulfokamfokaine, cordiamine).

With a decrease in the frequency of respiratory movements (less than 8-10 per minute), it is possible to use opioid antagonists. However, it is important to remember that their appointment will contribute to the reverse development of all the effects of opioids, including pain relief, so the patient may return to severe pain.

Tactics therapy for overdose of opioid analgesics

Drugs that caused the poisoning: Morphine, Omnopon, Tapentadol, Propionylphenylethoxyethylpiperidine, Trimeperidine, Tradedenil, Fentolil.

Signs of poisoning or overdose:

• Pupil constriction, skin flushing, coma.
• Respiratory depression up to a stop with a sharp cyanosis and dilated pupils.
• Bradycardia, collapse, decrease in body temperature.
• In case of tramadol poisoning, miosis, vomiting, collapse, coma, convulsions, depression of the respiratory center, apnea are possible.

Methods of care:

• Gastric lavage (even with parenteral administration of drugs), saline laxative or activated charcoal inside. Forced diuresis with alkalinization of the blood.
• Hemosorption. Artificial lung ventilation, oxygen inhalation, body warming.
• Intravenous: nalorphine (antorphine) 3-5 ml of 0.5% solution; atropine 1-2 ml of a 0.1% solution; caffeine 2 ml of 10% solution; cocarboxylase 50-100 mg.
• Naloxone IV slowly (within 2-3 minutes) or s / c. The initial dose is 0.4 mg, if necessary, repeatedly at intervals of 3-5 minutes until consciousness appears and spontaneous breathing is restored, the maximum dose is 10 mg; children (initial dose) 0.005-0.01 mg / kg.

Naloxone, naltrexone and methylnaltrexone are opioid antagonists. The most commonly used opioid overdose is naloxone. The drug is administered intravenously, intramuscularly, subcutaneously. The effect begins to develop within 1–2 minutes with intravenous administration and after 2–5 minutes with subcutaneous administration.The half-life of naloxone is one hour and the duration of action is 15–90 minutes. Re-introduction is possible if necessary. Possible side effects of naloxone: nausea and vomiting, in rare cases, arterial hypertension, pulmonary edema, arrhythmia and cardiac arrest. Therefore, it should only be prescribed if there is confidence that respiratory depression is associated with opioid use. If toxicity is mild and respiratory rate is normal, monitor the patient.If the patient has been taking rapid-release opioids, the toxicity effects will be short-lived. The metabolism of some opioids (morphine and oxycodone) is dependent on renal function, so kidney health should be monitored.

Comorbid conditions requiring special attention when prescribing opioids

Liver failure

The use of morphine for liver failure is safe, but the accumulation of metabolites is possible. It is necessary to reconsider the appointment of paracetamol or NSAIDs – patients may need to reduce the dose.

Renal failure

• Since morphine metabolites are excreted in the urine, it can accumulate rapidly in renal failure.
• Oxycodone metabolites are less toxic, and therefore, in patients with early stages of renal failure, pain relief can be started with oxycodone or they can be switched to it.
• Since fentanyl has no active metabolites, the use of fentanyl TTS in renal failure is preferred.
• For impaired renal function or end-stage renal disease, whether or not the patient is on dialysis, extra caution is needed when prescribing opioids. This is especially important in patients with a rapidly progressive process or an acute deterioration of the condition.
• NSAIDs are usually not prescribed for renal failure. Nevertheless, if the pain syndrome is caused by metastatic bone lesions or some kind of inflammatory process and may respond to NSAIDs, if alternative types of pain relief are ineffective, it is possible to use NSAIDs carefully with monitoring of renal function.

Read on: Pain relief at the end of life.

Cover photo: Rawpixel / Unsplash

ZN – instructions, use, drug analogues, composition, indications, contraindications, side effects in the UNIAN drug reference book

The introduction of naloxone prevents, weakens or eliminates (depending on the dose and time of administration ) the effects of opioid analgesics, restores breathing, reduces sedation and euphoria, weakens the hypotensive effect.

Naloxone eliminates the action of a wide group of narcotic drugs, both agonists and agonists-antagonists of opiate receptors: morphine, apomorphine, heroin, codeine, dihydrocodeine, promedol, methadone, pentazocine, fentanyl, buprenorphine.

The drug eliminates central and peripheral toxic symptoms: respiratory depression, pupillary constriction, delayed gastric emptying, dysphoria, coma and convulsions, as well as the analgesic effect of narcotic analgesics, in addition, it eliminates the toxic effect of large doses of alcohol.

Use of Naloxone-ZN

Opioid overdose. To eliminate oppression of the respiratory center caused by opioids; to restore breathing in newborns after administration of opioid analgesics to a woman in labor; as a diagnostic tool in patients with suspected opium addiction.

Naloxone – composition and release form of the drug

Solution for injection.

Composition . Active ingredient: naloxone.

1 ml of solution contains naloxone hydrochloride dihydrate in terms of 100% substance – 0.4 mg.

Excipients: sodium chloride , diluted hydrochloric acid, water for injection.

Naloxone: how to take the drug

Naloxon-ZN should be used intravenously as a jet (injection), intravenously drip (infusion), and also intramuscularly. The dose is set by the doctor individually for each patient. Intramuscular injections should be prescribed in cases where intravenous administration is not possible.

The duration of action of naloxone depends on the administered dose, route of administration and ranges from 45 minutes to 4 hours.

Since the effect of some opioids (eg, dextropropoxyphene, dihydrocodeine, methadone) lasts longer than the effect of naloxone, patients should be monitored continuously and repeated administrations of the drug should be given only when necessary.

Complete or partial elimination of opiate-induced respiratory depression :

• Adults 0.1-0.2 mg intravenous naloxone (approximately 1.5-3 μg per kg of body weight is usually sufficient …
• For children , the initial dose of naloxone is 0.01-0.02 mg per 1 kg of body weight intravenously for 2-3 minutes until breathing and consciousness are fully restored.

Acute opiate overdose :

• Adults Initial dose is 0.4-2 mg IV. If breathing is not restored, the administration should be repeated after 2-3 minutes.
• Children The recommended starting dose is 0.1 mg per 1 kg of body weight intravenously.

Naloxone – contraindications, side effects

Contraindications . Hypersensitivity to drug components.

Side effects . With the rapid introduction of Naloxone-ZN, various side reactions can occur.

Nausea, vomiting, diarrhea, dry mouth; arrhythmia, bradycardia, tachycardia, hypotension, arterial hypertension, ventricular fibrillation, cardiac arrest; trembling, convulsions, dizziness, headache, tension, hyperventilation; rhinitis, shortness of breath, skin rash, itching, urticaria, erythema multiforme, angioedema, anaphylactic shock; increased sweating, postoperative pain, changes at the injection site, including irritation of the vascular wall (with intravenous administration), local irritation and inflammation (with intramuscular administration).