Active Ingredient History
Naloxone, sold under the brand name Narcan among others, is a medication used to block the effects of opioids, especially in overdose. Naloxone has an extremely high affinity for μ-opioid receptors in the central nervous system (CNS). Naloxone is a μ-opioid receptor (MOR) inverse agonist, and its rapid blockade of those receptors often produces rapid onset of withdrawal symptoms. Naloxone also has an antagonist action, though with a lower affinity, at κ- (KOR) and δ-opioid receptors (DOR). If administered in the absence of concomitant opioid use, no functional pharmacological activity occurs (except the inability for the body to combat pain naturally). In contrast to direct opiate agonists, which elicit opiate withdrawal symptoms when discontinued in opiate-tolerant people, no evidence indicates the development of tolerance or dependence on naloxone. The mechanism of action is not completely understood, but studies suggest it functions to produce withdrawal symptoms by competing for opiate receptor sites within the CNS (a competitive antagonist, not a direct agonist), thereby preventing the action of both endogenous and xenobiotic opiates on these receptors without directly producing any effects itself. When administered parenterally (e.g. intravenously or by injection), as is most common, naloxone has a rapid distribution throughout the body. The mean serum half-life has been shown to range from 30 to 81 minutes, shorter than the average half-life of some opiates, necessitating repeat dosing if opioid receptors must be stopped from triggering for an extended period. Naloxone is primarily metabolized by the liver. Its major metabolite is naloxone-3-glucuronide, which is excreted in the urine. Naloxone is useful both in acute opioid overdose and in reducing respiratory or mental depression due to opioids. Whether it is useful in those in cardiac arrest due to an opioid overdose is unclear. Naloxone is poorly absorbed when taken by mouth, so it is commonly combined with a number of oral opioid preparations, including buprenorphine and pentazocine, so that when taken orally, just the opioid has an effect, but if misused by injecting, the naloxone blocks the effect of the opioid. In a meta-analysis of people with shock, including septic, cardiogenic, hemorrhagic, or spinal shock, those who received naloxone had improved blood flow. Naloxone is also experimentally used in the treatment for congenital insensitivity to pain with anhidrosis, an extremely rare disorder (one in 125 million) that renders one unable to feel pain or differentiate temperatures. Naloxone can also be used as an antidote in overdose of clonidine, a medication that lowers blood pressure. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
Combination drugs
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
Constipation (approved 1971)
Opioid-Related Disorders (approved 1971)
Respiratory Insufficiency (approved 1971)
Acute Pain (Phase 4)
Analgesia (Phase 4)
Analgesia, Epidural (Phase 4)
Analgesics, Opioid (Phase 4)
Angina, Unstable (Phase 4)
Antiretroviral Therapy, Highly Active (Phase 2)
Back Pain (Phase 4)
Binge-Eating Disorder (Phase 2/Phase 3)
Biological Availability (Phase 1)
Bipolar Disorder (Phase 2)
Brain Death (Phase 2/Phase 3)
Brain Injuries (Early Phase 1)
Buprenorphine (Phase 2)
Cancer Pain (Phase 3)
Central Nervous System Sensitization (Phase 2)
Chronic Pain (Phase 4)
Cocaine-Related Disorders (Phase 1)
Constipation (Phase 4)
Cystectomy (Phase 4)
Cystitis, Interstitial (Phase 2)
Diabetes Mellitus, Type 1 (Phase 4)
Drug Overdose (Phase 4)
Drugs, Investigational (Phase 4)
Dry Eye Syndromes (Phase 1)
Epilepsy (Phase 3)
Esophageal Neoplasms (Phase 4)
Estradiol (Phase 1)
Gambling (Phase 2)
General Surgery (Phase 4)
Graft Rejection (Early Phase 1)
Healthy Volunteers (Phase 2)
Heart (Phase 4)
Heart Arrest (Early Phase 1)
Hepacivirus (Phase 1)
Hepatitis C (Phase 4)
Hepatitis C, Chronic (Phase 4)
Heroin Dependence (Phase 3)
HIV (Phase 4)
HIV Infections (Phase 3)
Hyperalgesia (Phase 2)
Hypnotics and Sedatives (Early Phase 1)
Hypoglycemia (Phase 4)
Hypogonadism (Phase 2)
Ileus (Phase 4)
Immune System Diseases (Phase 2)
Inflammation (Phase 2)
Intestinal Obstruction (Phase 1)
Intestine, Large (Phase 4)
Irritable Bowel Syndrome (Phase 2)
Liver Diseases (Phase 4)
Liver Failure (Phase 4)
Low Back Pain (Phase 4)
Lung Transplantation (Phase 2/Phase 3)
Lymphoma, T-Cell, Cutaneous (Phase 3)
Menopause (Phase 1)
Methadone (Phase 2)
Morphine Dependence (Phase 3)
Mycosis Fungoides (Phase 3)
Naloxone (Phase 4)
Naltrexone (Phase 2)
Narcotic Antagonists (Phase 2)
Narcotics (Early Phase 1)
Neonatology (Phase 1/Phase 2)
Neoplasms (Phase 4)
Neuralgia (Phase 4)
Obesity (Phase 2)
Opiate Alkaloids (Phase 4)
Opiate Overdose (Phase 4)
Opioid-Induced Constipation (Phase 4)
Opioid-Related Disorders (Phase 4)
Osteoarthritis (Phase 4)
Pain ()
Pain, Intractable (Phase 4)
Pain, Postoperative (Phase 4)
Pharmacokinetics (Phase 1)
Placebo Effect (Early Phase 1)
Placebos (Phase 2)
Postoperative Complications (Phase 4)
Postoperative Nausea and Vomiting (Phase 3)
Pruritus (Phase 2/Phase 3)
Pulpitis (Phase 2)
Reproductive Health (Phase 1)
Respiratory Insufficiency (Phase 4)
Risk Reduction Behavior (Phase 4)
Sezary Syndrome (Phase 3)
Signs and Symptoms (Phase 3)
Spinal Diseases (Phase 4)
Spinal Injuries (Phase 4)
Substance-Related Disorders (Phase 4)
Substance Withdrawal Syndrome (Phase 3)
Temporomandibular Joint Disorders (Phase 1/Phase 2)
Therapeutic Equivalency (Phase 1)
Tissue Donors (Phase 2/Phase 3)
Virtual Reality (Phase 2)
| Trial | Phase | Start Date | Organizations | Indications |
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