pharmacopeia
GET
/api/v1/drug/naloxone
2D structure
(4R,4aS,7aR,12bS)-4a,9-dihydroxy-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one
SMILES C=CCN1CC[C@]23[C@@H]4C(=O)CC[C@]2([C@H]1CC5=C3C(=C(C=C5)O)O4)O
InChIKey UZHSEJADLWPNLE-GRGSLBFTSA-N

Mechanism of action

Sourced from openFDA

Naloxone hydrochloride is an opioid antagonist that antagonizes opioid effects by competing for the same receptor sites. Naloxone hydrochloride reverses the effects of opioids, including respiratory depression, sedation, and hypotension.

Opioid

Indications

Sourced from openFDA
  • Naloxone HCl Nasal Spray is indicated for the emergency treatment of known or suspected opioid overdose, as manifested by respiratory and/or central nervous system depression. Naloxone HCl Nasal Spray is intended for immediate administration as emergency therapy in settings where opioids may be present.

Contraindications

Sourced from openFDA
  • Naloxone HCl Nasal Spray is contraindicated in patients known to be hypersensitive to naloxone hydrochloride or to any of the other ingredients. Hypersensitivity to naloxone hydrochloride.contraindicated

Dosage & administration

Sourced from openFDA

• Naloxone HCl Nasal Spray is for intranasal use only. ( 2.1 ) • Seek emergency medical care immediately after use. ( 2.1 ) • Administration of a single spray of Naloxone HCl Nasal Spray intranasally into one nostril. ( 2.2 ) • Administer additional doses of Naloxone HCl Nasal Spray, using a new nasal spray with each dose, if the patient does not respond or responds and then relapses into respiratory depression, additional doses of Naloxone HCl Nasal Spray may be given every 2 to 3 minutes until emergency medical assistance arrives. ( 2.2 ) • Additional supportive and/or resuscitative measures may be helpful while awaiting emergency medical assistance. ( 2.2 ) 2.1 Important Administration Instructions Naloxone HCl Nasal Spray is for intranasal use only. No additional device assembly is required. Because treatment of suspected opioid overdose must be performed by someone other than the patient, instruct the prescription recipient to inform those around them about the presence of Naloxone HCl Nasal Spray and the Instructions for Use . Instruct the patient or caregiver to read the Instructions for Use at the time they receive a prescription for Naloxone HCl Nasal Spray. Emphasize the following instructions to the patient or caregiver: • Administer Naloxone HCl Nasal Spray as quickly as possible because prolonged respiratory depression may result in damage to the central nervous system or death.

Warnings & precautions

Sourced from openFDA

• Risk of Recurrent Respiratory and CNS Depression: Due to the duration of action of naloxone relative to the opioid, keep patient under continued surveillance and administer repeat doses of naloxone using a new nasal spray with each dose, as necessary, while awaiting emergency medical assistance. ( 5.1 ) • Risk of Limited Efficacy with Partial Agonists or Mixed Agonists/Antagonists: Reversal of respiratory depression caused by partial agonists or mixed agonists/antagonists, such as buprenorphine and pentazocine, may be incomplete. Larger or repeat doses may be required. ( 5.2 ) • Precipitation of Severe Opioid Withdrawal: Use in patients who are opioid dependent may precipitate opioid withdrawal. In neonates, opioid withdrawal may be life-threatening if not recognized and properly treated. Monitor for the development of opioid withdrawal. ( 5.3 ) • Risk of Cardiovascular (CV) Effects: Abrupt postoperative reversal of opioid depression may result in adverse CV effects. These events have primarily occurred in patients who had pre-existing CV disorders or received other drugs that may have similar adverse CV effects. Monitor these patients closely in an appropriate healthcare setting after use of naloxone hydrochloride. ( 5.3 ) 5.1 Risk of Recurrent Respiratory and Central Nervous System Depression The duration of action of most opioids may exceed that of Naloxone HCl Nasal Spray resulting in a return of respiratory and/or central nervous system depression after an initial improvement in symptoms.

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are discussed elsewhere in the labeling: • Precipitation of Severe Opioid Withdrawal [see Warnings and Precautions ( 5.3 )] Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to the rates in the clinical studies of another drug and may not reflect the rates observed in practice. The following adverse reactions were observed in a naloxone hydrochloride nasal spray clinical study. In a pharmacokinetic study of 30 healthy adult volunteers exposed to one spray of naloxone hydrochloride nasal spray in one nostril or two sprays of naloxone hydrochloride nasal spray, one in each nostril, the most common adverse reactions were: increased blood pressure, constipation, toothache, muscle spasms, musculoskeletal pain, headache, nasal dryness, nasal edema, nasal congestion, nasal inflammation, rhinalgia, and xeroderma. The following adverse reactions have been identified primarily during post-approval use of naloxone hydrochloride in the post-operative setting. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure: Hypotension, hypertension, ventricular tachycardia and fibrillation, dyspnea, pulmonary edema, and cardiac arrest. Death, coma, and encephalopathy have been reported as sequelae of these events.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Risk Summary The limited available data on naloxone use in pregnant women are not sufficient to inform a drug-associated risk. However, there are clinical considerations [see Clinical Considerations] . In animal reproduction studies, no embryotoxic or teratogenic effects were observed in mice and rats treated with naloxone hydrochloride during the period of organogenesis at doses equivalent to 6-times and 12-times, respectively, a human dose of 8 mg/day (two Naloxone HCl Nasal Sprays) based on body surface area comparison [see Data] . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Clinical Considerations Fetal/Neonatal adverse reactions Naloxone hydrochloride crosses the placenta, and may precipitate withdrawal in the fetus, as well as in the opioid-dependent mother [see Warnings and Precautions ( 5.3 )] . The fetus should be evaluated for signs of distress after Naloxone HCl Nasal Spray is used. Careful monitoring is needed until the fetus and mother are stabilized.

Pharmacokinetics

Sourced from openFDA
Metabolism
In a pharmacokinetic study in 30 healthy adult subjects, the relative bioavailability (BA) of one nasal spray in one nostril, consisting of a 2 mg total dose (0.1 mL of 20 mg/mL naloxone hydrochloride solution) and a 4 mg total dose (0.1 mL of 40 mg/mL naloxone hydrochloride solution), and two nasal sprays administered as one nasal spray in each nostril, consisting of a 4 mg total dose (0.1 mL of 20 mg/mL naloxone hydrochloride solution in each nostril) and an 8 mg total dose (0.1 mL of 40 mg/mL naloxone hydrochloride solution in each nostril), were compared to a single dose of 0.4 mg naloxone…

Approval history

Sourced from openFDA
  • Aug 30, 2010NDANDA022410Indivior
  • Jul 3, 2013NDANDA204242Edenbridge Pharms
  • Nov 18, 2015NDANDA208411Emergent
  • Apr 29, 2021NDANDA212045Hikma
  • Oct 15, 2021NDANDA212854Zmi Pharma
  • Feb 28, 2022NDANDA215457Kaleo Inc
  • Mar 7, 2023NDANDA208969Amphastar Pharms Inc
  • Jul 28, 2023NDANDA217722Harm Reduction Therp

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
35,830 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Dependence4,70713%
  2. 2Drug Withdrawal Syndrome3,74810%
  3. 3Pain3,1998.9%
  4. 4Off Label Use2,7027.5%
  5. 5Nausea2,5487.1%
  6. 6Overdose2,5097.0%
  7. 7Vomiting1,9925.6%
  8. 8Anxiety1,7124.8%
  9. 9Emotional Distress1,6104.5%
  10. 10Headache1,6094.5%
  11. 11Drug Ineffective1,5244.3%
  12. 12Drug Abuse1,4474.0%
  13. 13Toxicity To Various Agents1,3963.9%
  14. 14Fatigue1,3843.9%
  15. 15Insomnia1,2903.6%

Literature

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Recent PubMed references pinned to Naloxone as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 847 ClinicalTrials.gov registrations naming Naloxone as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Naloxone. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

  • OPRM1CPIC C (provisional)ClinPGx 3

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Naloxone work?
Naloxone hydrochloride is an opioid antagonist that antagonizes opioid effects by competing for the same receptor sites. Naloxone hydrochloride reverses the effects of opioids, including respiratory depression, sedation, and hypotension.
What is Naloxone used for?
According to FDA labeling, Naloxone carries indications including: Naloxone HCl Nasal Spray is indicated for the emergency treatment of known or suspected opioid overdose, as manifested by respiratory and/or central nervous system depression. Naloxone HCl Nasal Spray is intended for immediate administration as emergency therapy in settings where opioids may be present.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Naloxone?
Naloxone is classified as Antidotes, Peripheral opioid receptor antagonists, Opioid Antagonist, Opioid Antagonists, Central Nervous System Stimulation, Increased Blood Pressure, Increased Medullary Respiratory Drive.
What are the brand names for Naloxone?
Naloxone is marketed under brand names including Bunavail, Kloxxado, Narcan, Rextovy, Rezenopy, Suboxone, Zimhi, Zubsolv.
What are the contraindications for Naloxone?
Naloxone labeling lists contraindications including: Naloxone HCl Nasal Spray is contraindicated in patients known to be hypersensitive to naloxone hydrochloride or to any of the other ingredients. Hypersensitivity to naloxone hydrochloride.. Always consult the full prescribing information and a clinician.
Note. Data for naloxone is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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