Naloxone Nasal Spray

Products

Naloxone nasal spray was approved in the United States in 2015 (Narcan), in the EU in 2017, and in many countries in 2018 (Nyxoid). Each nasal spray contains only one dose and can be used only once.

Structure and properties

Naloxone (C19H21NO4, Mr = 327.37 g/mol) is a semisynthetic derivative of morphine. It is present in the drug as naloxone hydrochloride dihydrate, a white, crystalline, and hygroscopic powder that is readily soluble in water.

Effects

Naloxone (ATC V03AB15) reverses the effects of opioids. The effects are due to competitive antagonism at opioid receptors. Naloxone has no agonist activity. It enters the bloodstream through the mucosa and effects are rapid. Administration is easier than with parenteral – intravenous, subcutaneous, or intramuscular – naloxone.

Indications

For immediate use as emergency therapy for known or suspected opioid overdose manifesting as respiratory depression and/or central nervous system depression in both nonmedical and medical settings. In adults and adolescents 14 years of age and older. Nasal spray is not a substitute for treatment by an emergency physician. Naloxone can be used in overdose with narcotics such as heroin as well as with medications such as oxycodone.

Dosage

According to the prescribing information. The spray is administered into a nostril (intranasally). If additional doses are needed, they are given alternately into the left and right nostrils. A new spray must always be used for this purpose. Depending on the duration of action of the opioid, another dose may be necessary.

Abuse

Naloxone has no agonistic properties at the opioid receptor and therefore cannot be abused as a narcotic.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Drug-drug interactions are possible with opioids whose effects naloxone reverses.

Adverse effects

Nausea occurs as the most common possible adverse effect. Other common adverse effects include:

  • Dizziness, headache
  • Blood pressure changes (hypotension, hypertension).
  • Vomiting
  • Tachycardia (rapid heartbeat)

Because of the reversal of opioid effects, patients may develop withdrawal symptoms.