Actions and spectrum: 

• nicotine binds to the nicotinic acetylcholine receptors (nAChRs) in the brain, which results in the release of several neurotransmitters such as dopamine, norepinephrine, and acetylcholine. This leads to an increase in cognitive function, mood, and attention. 
• nicotine also stimulates the release of adrenaline and other stress hormones, which can increase heart rate, blood pressure, and respiration rate. 
• The effects of nicotine intranasal are relatively short-acting and peak within 10-20 minutes of administration. The duration of action is approximately 2 hours. 

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Frequency defined 

>10% 

Local irritation (94%) 

1-10% 

Anxiety 

Restlessness 

Dizziness 

Weight increase 

Somnolence and fatigue 

Insomnia 

Depression 

Tremor 

Incoordination 

Irritability 

Cravings 

Impaired concentration 

Emotional lability 

Increased sweating 

Confusion 

Apathy 

Increased appetite 

Increased dreaming 

Black Box Warning:  

nicotine intranasal does not have a black box warning. However, it is important to note that nicotine is a highly addictive substance and long-term use can have serious health consequences. 

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity or allergy to nicotine or any components of the intranasal spray. 
• Children under the age of 18 years. 
• Non-tobacco users or occasional smokers. 
• Nasal or sinus conditions such as allergies, sinus infections, nasal polyps, or a deviated septum. 
• Severe or uncontrolled hypertension (high blood pressure). 
• Recent history of heart attack, stroke, or any other serious cardiovascular disease. 
• Active peptic ulcer disease. 
• Phaeochromocytoma (a rare tumor of the adrenal gland). 
• Hyperthyroidism (an overactive thyroid gland). 
• Pregnancy or breastfeeding.

Caution: 

• Cardiovascular disease: nicotine can increase heart rate and blood pressure, which can be dangerous for people with cardiovascular disease. 
• Diabetes: nicotine can increase blood sugar levels, which may affect the management of diabetes. 
• Respiratory disease: nicotine can cause bronchospasm, which may worsen symptoms in people with respiratory disease. 
• Liver disease: nicotine is metabolized by the liver, so people with liver disease may have difficulty metabolizing the drug properly. 
• Renal disease: nicotine is excreted by the kidneys, so people with renal disease may have difficulty excreting the drug properly. 
• Pregnancy and lactation: nicotine can cross the placenta and be excreted in breast milk, which can harm the developing fetus or nursing baby. Therefore, nicotine intranasal should be used with caution in pregnant or breastfeeding women. 
• Mental health conditions: nicotine can worsen symptoms of anxiety, depression, and other mental health conditions. People with these conditions should use nicotine intranasal with caution and under medical supervision.

Comorbidities: 

nicotine intranasal is contraindicated in individuals with a history of hypersensitivity to nicotine, menthol, or any other component of the product. It should be given with caution in patients with a history of heart disease, hypertension, hyperthyroidism, diabetes, or pheochromocytoma, as well as in individuals who have recently had a stroke or suffer from the chronic obstructive pulmonary disease (COPD) or asthma.

nicotine replacement therapy should be used with caution in pregnant women. It should also be used with caution in breastfeeding women as nicotine is excreted in breast milk and can be harmful to the infant. 

Pregnancy consideration: Pregnancy Category: D 

Lactation: Distributed in breast milk  

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the 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 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: 

nicotine intranasal is a nicotine replacement therapy (NRT) used for smoking cessation. nicotine, the active ingredient, acts as an agonist at nicotinic cholinergic receptors in the brain, leading to the release of various neurotransmitters such as dopamine, norepinephrine, and acetylcholine. These neurotransmitters are involved in the reward and reinforcement pathways of the brain, leading to pleasurable sensations and decreased cravings for nicotine.  

Pharmacodynamics: 

nicotine is a potent parasympathomimetic alkaloid that binds to and activates nicotinic acetylcholine receptors (nAChRs) in the brain and peripheral nervous system. Activation of nAChRs leads to the release of various neurotransmitters, including dopamine, norepinephrine, and acetylcholine, which are responsible for the central and peripheral effects of nicotine. 

Intranasal administration of nicotine delivers the drug directly into the systemic circulation via the nasal mucosa. The absorption of nicotine from the nasal mucosa is rapid and results in a rapid onset of action, with peak plasma levels occurring within minutes after administration. 

The pharmacodynamic effects of nicotine include increased heart rate and blood pressure, increased respiration, and release of various neurotransmitters. nicotine is also known to increase cognitive function, mood, and attention. Prolonged use of nicotine can lead to dependence, tolerance, and withdrawal symptoms, which can make quitting nicotine difficult for some individuals.  

Pharmacokinetics: 

Absorption 

nicotine intranasal is rapidly absorbed through the nasal mucosa and reaches systemic circulation within a few minutes. 

Distribution 

nicotine has a high lipid solubility, which crosses the blood-brain barrier and distributes widely throughout the body. 

Metabolism 

nicotine is primarily metabolized in the liver by the cytochrome P450 enzyme system, specifically CYP2A6, to form cotinine, which is then further metabolized to trans-3′-hydroxy cotinine. 

Elimination and excretion 

nicotine and its metabolites are eliminated primarily through the urine, with a small amount excreted in the feces. 

Excretion: The elimination half-life of nicotine is around 2 hours, while that of cotinine is around 17 hours. 

Administration: 

nicotine intranasal is administered as a nasal spray. The spray is inserted into the nostril, and the solution is sprayed into the nasal cavity. The recommended dose is usually one spray into each nostril every hour as needed, up to a maximum of 40 doses per day. The spray should not be used continuously for more than six months without consulting a doctor. 

Patient information leaflet 

Generic Name: nicotine 

Pronounced: [ NIK-oh-teen]  

Why do we use nicotine intranasal? 

nicotine intranasal is a medication used as a smoking cessation aid. It helps people quit smoking by reducing withdrawal symptoms and the urge to smoke. It is used as a second-line therapy in individuals who have failed to quit smoking with other medications.