naloxone intranasal

Action and Spectrum

Actions and Spectrum 

naloxone is an opioid receptor antagonist thus it works by preventing opioids from acting on their receptors in the brain and other parts of the body. Opioid receptors are also involved in producing the desired opioid analgesic effects, for pain relief and opioid-induced respiratory suppressant. Opioids can also cause respiratory depression whereby in case an individual takes a large amount their breathing rate can reduce significantly or even stop.  

Drug Interaction

Adverse Reaction

Frequency not defined  

Musculoskeletal pain  

Increased blood pressure  

Headache  

Nasal edema  

Nasal congestion  

Nasal dryness  

Nasal inflammation  

Black Box Warning

Black Box Warning 

None  

Contraindication / Caution

Contraindication/Caution 

Contraindications:  

Allergy or Hypersensitivity  

Cautions  

Non-Opioid Overdoses  

Narcotic-Dependent Individuals 

Pregnancy / Lactation

Pregnancy/Lactation  

Pregnancy consideration: Insufficient data available 

Breastfeeding warnings:  The excretion of drug in human breast milk is unknown 

Pregnancy categories: 

• Category A: Satisfactory and well-controlled studies show no evidence of risk to the fetus in the first trimester or in the later trimester. 
• Category B: No evidence of risk to fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women. 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category clearly outweigh risks over benefits. These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology 

naloxone is acts as an opioid receptor antagonist, by blocking effects of opioids by binding to opioid receptors in the body without activating them. naloxone intranasal is a specific formulation of naloxone designed for easy and rapid administration through the nasal route.  

Pharmacodynamics 

naloxone is used as an opioid receptor antagonist which means that it will compete with opioids and bind to the opioid receptors without causing any activation of the receptors. naloxone intranasal is the formulation of naloxone intended for the nasal route of administration that is easy and fast. 

Pharmacokinetics 

Absorption 

Narcan: Peak plasma concentration is 0.33-0.5 hours.  

Kloxxado: Peak plasma concentration is 0.25 hours.  

Peak Plasma Concentration:  

Narcan: Peak plasma concentration ranges from 4.83 to 9.7 ng/mL.  

Kloxxado: Peak plasma concentration ranges from 12.3 to 12.8 ng/mL.  

Area Under the Curve (AUC):  

7.87 to 15.3 hr·ng/mL- Narcan 

16.7 to 19 hr·ng/mL- Kloxxado 

It has a bioavailability of 37%.   

Distribution 

Both Narcan and Kloxxado can bind weakly to plasma proteins mainly plasma albumin.   

Metabolism 

naloxone is primarily metabolized in the liver through glucuronide conjugation. The major metabolite is naloxone-3-glucuronide.  

Elimination and Excretion  

Half-life: 2 hours (Narcan) 

Half-life: 1.76 to 2.69 hours (Kloxxado) 

naloxone is primarily excreted in the urine. After 6 hours 25 to 40% is excreted after 24 hours 50% is excreted and after 72 hours 60 to 70% is excreted.  

Adminstartion

Administration  

naloxone intranasal is normally presented in the form of a pre-filled metered-dose nasal spray or a single-dose metered-dose spray appliance with a fixed dose of naloxone. The device must be discarded after use and cannot be cleaned and used again for another pregnancy confirmation. 

Patient Information Leaflet

Patient information leaflet  

Generic Name:  naloxone intranasal  

Pronounced: nah-LOX-one  

Why do we use naloxone intranasal?  

Naloxone nasal spray therapy is given concurrently with medical management for the reversal of life-threatening toxicity from opioids in cases of confirmed or suspected opioid overdose in pediatric and adult patients. It is in the class of opioid antagonists.