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Naloxone, intramuscular
Naloxone is an opioid antagonist that blocks opioid receptors to rapidly reverse opioid overdose and restore normal breathing.
Naloxone is an opioid antagonist that blocks opioid receptors to rapidly reverse opioid overdose and restore normal breathing. Used for Opioid overdose reversal, Emergency treatment of suspected opioid overdose.
At a glance
| Generic name | Naloxone, intramuscular |
|---|---|
| Sponsor | Norwegian University of Science and Technology |
| Drug class | Opioid antagonist |
| Target | Opioid receptors (mu, delta, kappa) |
| Modality | Small molecule |
| Therapeutic area | Emergency Medicine / Toxicology |
| Phase | Phase 3 |
Mechanism of action
Naloxone competitively binds to opioid receptors (mu, delta, and kappa) with higher affinity than opioids, displacing opioids from these receptors and preventing their effects. This rapidly reverses respiratory depression, sedation, and other life-threatening effects of opioid overdose. The intramuscular formulation provides an alternative route of administration for emergency use in opioid overdose situations.
Approved indications
- Opioid overdose reversal
- Emergency treatment of suspected opioid overdose
Common side effects
- Acute withdrawal syndrome (agitation, body aches, sweating, tachycardia)
- Hypertension
- Tachycardia
- Tremor
- Anxiety
Key clinical trials
- Rapid Antidepressant Improvement Secondary to Excitatory Brain Responses (PHASE4)
- iSTEP-N 101b: Pharmacokinetics and Safety Study of Low- and High-Dose Naltrexone Implants vs Monthly Vivitrol in Healthy Volunteers (PHASE1)
- Safety and PK Study of BICX104 With or Without Bupropion Compared to Vivitrol (PHASE1)
- Proof of Concept (PoC) Evaluation of Naloxone Unique Intramuscular (IM) Injection (PHASE1)
- Study of Injectable Naltrexone and Oral Bupropion Among Cigarette Smokers With Schizophrenia (PHASE1)
- Pharmacodynamic Evaluation of Intramuscular Nalmefene Autoinjector 1.5 mg Compared to Intranasal Narcan 4 mg (PHASE1)
- Long-acting Buprenorphine vs. Naltrexone Opioid Treatments in CJS-involved Adults (PHASE4)
- Naltrexone for Overdose Prevention (PHASE2, PHASE3)
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |