nicotine transdermal

Action and Spectrum

Actions and spectrum: 

• Nicotine Replacement Therapy (NRT): nicotine transdermal patches are commonly used as a form of nicotine replacement therapy to help people quit smoking or reduce their tobacco dependence. They provide a sustained and steady supply of nicotine, reducing the cravings and withdrawal symptoms associated with nicotine withdrawal. 
• Smoking cessation: The primary action of nicotine transdermal patches is to aid in smoking cessation by reducing the urge to smoke and relieving nicotine withdrawal symptoms. By delivering nicotine in a controlled manner, the patches help individuals gradually wean off nicotine and break the habit of smoking. 
• Nicotine addiction management: nicotine transdermal patches can also be used for nicotine addiction management in cases where complete smoking cessation may not be feasible or as a step towards quitting smoking. They provide a safer alternative to smoking by delivering nicotine without the harmful effects of tobacco smoke. 
• Gradual reduction of nicotine intake: nicotine transdermal patches typically come in different strengths or dosage levels, allowing individuals to start with a higher strength and gradually decrease the nicotine dosage over time. This stepwise reduction helps individuals gradually reduce their nicotine intake and overcome their dependence on nicotine. 

The spectrum of nicotine transdermal patches is primarily focused on helping individuals quit smoking or manage nicotine addiction. They are not intended for recreational use or as a substitute for tobacco products. It is important to note that nicotine transdermal patches should be used as part of a comprehensive smoking cessation program, which may include behavioural support and counselling. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Anorexia 

Back pain 

Cough 

Dizziness 

Dyspepsia 

Hiccups 

Increased salivation 

Insomnia 

application site Irritation 

Migraine 

Rhinitis 

Tachycardia 

Tooth abrasions 

Xerostomia 

Acne 

Arthralgia 

Bronchitis 

Diarrhea 

Dysmenorrhea 

Headache 

Increased BP 

Indigestion 

Irritability 

neck or Jaw pain 

Nausea 

Sinusitis 

Taste disturbance 

Vomiting 

Black Box Warning

Black Box Warning: 

nicotine transdermal patches do not carry a black box warning. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: nicotine transdermal patches are contraindicated in individuals who have a known hypersensitivity or allergy to nicotine or any other component of the patch formulation. 
• Non-smokers and occasional smokers: nicotine transdermal patches are intended for use in individuals who smoke cigarettes regularly and are dependent on nicotine. They are not recommended for non-smokers or occasional smokers. 
• Children and adolescents: nicotine transdermal patches are not intended for use in individuals under the age of 18. They should be kept out of reach of children to prevent accidental exposure or ingestion. 
• Active cardiovascular disease: nicotine can have cardiovascular effects like increased heart rate and elevated BP. Therefore, nicotine transdermal patches should be used with caution or avoided in individuals with active cardiovascular disease, such as recent heart attack, severe arrhythmias, or unstable angina. 
• Recent myocardial infarction: nicotine transdermal patches are contraindicated in individuals who have had a recent myocardial infarction (heart attack). The cardiovascular effects of nicotine may increase the risk of adverse cardiac events in this population. 
• Severe or worsening angina: Individuals with severe or worsening angina (chest pain) should avoid the use of nicotine transdermal patches due to the potential cardiovascular effects of nicotine. 
• Pregnancy and breastfeeding: The use of nicotine transdermal patches during pregnancy and breastfeeding should be discussed with a healthcare professional. nicotine can have adverse effects on fetal development and may be present in breast milk.

Caution: 

• Cardiovascular conditions: Individuals with underlying cardiovascular conditions, such as high blood pressure, heart disease, or a history of stroke, should use nicotine transdermal patches with caution. nicotine can increase heart rate and blood pressure, potentially exacerbating these conditions. 
• Diabetes: nicotine can affect blood sugar levels, and individuals with diabetes should monitor their blood sugar closely when using nicotine transdermal patches. Adjustments to diabetes medications or insulin may be necessary. 
• Hyperthyroidism: nicotine can stimulate the thyroid gland, potentially aggravating symptoms in individuals with hyperthyroidism. Close monitoring of thyroid function is recommended. 
• Skin conditions: Individuals with certain skin conditions, such as dermatitis or eczema, should use nicotine transdermal patches with caution. Skin irritation or allergic reactions may occur at the site of application. 
• Interactions with medications: nicotine can interact with certain medications, such as antipsychotics or tricyclic antidepressants. It is important to inform healthcare providers about all medications being taken to avoid potential interactions. 
• Nicotine dependence: nicotine transdermal patches are intended to help individuals quit smoking or reduce nicotine dependence. However, it is possible to develop dependence on nicotine from the patches themselves. Careful adherence to the recommended dosage and duration of use is important to minimize the risk of dependence. 

Comorbidities: 

• Hypertension: nicotine can elevate blood pressure, so individuals with hypertension should be monitored closely while using nicotine transdermal patches. Dose adjustments or alternative methods of smoking cessation may be considered. 
• Respiratory conditions: nicotine can have bronchoconstrictive effects, potentially worsening symptoms in individuals with respiratory conditions like asthma or COPD. Monitoring of respiratory symptoms and adjustment of treatment may be needed. 
• Peptic ulcer disease: nicotine can increase stomach acid production, potentially exacerbating symptoms in individuals with peptic ulcer disease. Caution is advised, and it may be necessary to adjust ulcer treatment if symptoms worsen. 
• Thyroid disorders: nicotine can stimulate the thyroid gland, which may impact individuals with thyroid disorders such as hyperthyroidism. Close monitoring of thyroid function and symptom management is important. 
• Mental health conditions: nicotine can have effects on mood and mental health. Individuals with psychiatric disorders such as depression, anxiety, or bipolar disorder should be closely monitored for changes in mood or behaviour while using nicotine transdermal patches. 

Pregnancy / Lactation

Pregnancy consideration: US FDA pregnancy category: D 

Lactation: Excreted into human milk: Yes  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

The pharmacology of nicotine involves interactions with nicotinic acetylcholine receptors (nAChRs) located throughout the body. nicotine acts as an agonist at nAChRs, which are ligand-gated ion channels.

Activation of these receptors by nicotine leads to the release of various neurotransmitters, including dopamine, norepinephrine, serotonin, and acetylcholine. 

Long-term use of nicotine can lead to the development of tolerance, meaning higher doses may be required to achieve same effects. Conversely, sensitization can occur in certain individuals, where lower doses of nicotine can produce stronger effects. 

Pharmacodynamics: 

• Nicotinic acetylcholine receptors (nAChRs) activation: nicotine acts as an agonist at nAChRs located in the brain, autonomic ganglia, adrenal medulla, and neuromuscular junctions. By binding to these receptors, nicotine stimulates the release of several neurotransmitters, including dopamine, norepinephrine, serotonin, and acetylcholine. 
• Central Nervous System (CNS) effects: Activation of nAChRs in the CNS leads to various effects, including increased alertness, improved concentration, enhanced cognitive function, and mood modulation. These effects contribute to nicotine’s addictive properties. 
• Peripheral effects: nicotine affects various peripheral systems in the body. It stimulates the release of adrenaline (epinephrine) from the adrenal medulla, leading to increased heart rate, blood pressure, and vasoconstriction. It also stimulates the release of dopamine in the mesolimbic system, which is associated with reward and reinforcement. 
• Withdrawal symptom relief: nicotine transdermal patches help relieve the symptoms of nicotine withdrawal experienced during smoking cessation. By providing a steady and controlled release of nicotine, they can reduce cravings, irritability, anxiety, restlessness, and difficulty concentrating. 
• Nicotine dependence management: nicotine replacement therapy, such as transdermal patches, aims to reduce nicotine dependence by providing a substitute source of nicotine without the harmful effects of tobacco smoke. By delivering nicotine in a controlled manner, it helps individuals gradually reduce their dependence and break the smoking habit. 

Pharmacokinetics: 

Absorption 

• nicotine from the transdermal patch is absorbed through the skin and enters the systemic circulation. 
• Absorption rates can vary depending on factors such as skin integrity, patch size, application site, and individual differences. 
• The transdermal route provides a controlled and sustained release of nicotine over time. 

Distribution 

• nicotine is distributed throughout the body via the bloodstream. 
• It readily crosses the blood-brain barrier, allowing it to reach the central nervous system and exert its effects on the brain. 

Metabolism 

• nicotine is primarily metabolized in the liver by the enzyme cytochrome P450 2A6 (CYP2A6). 
• The major metabolite of nicotine is cotinine, which is formed through oxidation by CYP2A6. 
• Other minor metabolites include nicotine N’-oxide, nicotine glucuronide, and cotinine glucuronide. 

Elimination and excretion 

• nicotine and its metabolites are primarily eliminated via the kidneys through urine. 
• The elimination half-life of nicotine is around 2 hours, but the half-life of cotinine is longer, ranging from 15 to 20 hours. 

Adminstartion

Administration: 

• Clean and dry the skin: Ensure that the skin is clean, dry, and free of any lotions, oils, or other substances that may interfere with adhesion. 
• Select an appropriate application site: Choose a clean, hairless area of skin such as the upper arm, upper back, or hip. Avoid areas with cuts, rashes, or irritations. 
• Rotate application sites: To prevent skin irritation, it is recommended to rotate the application site with each new patch. Wait at least one week before reapplying a patch to the same site. 
• Remove the protective backing: Peel off the protective backing from the patch, being careful not to touch the adhesive side with your fingers. 
• Apply the patch: Firmly press the adhesive side of the patch onto the selected area of skin. Make sure it is securely attached and smooth out any wrinkles or folds. 
• Wash hands: After applying the patch, wash your hands thoroughly to remove any nicotine residue and prevent accidental transfer to sensitive areas, such as the eyes or mouth. 
• Follow dosing instructions: Follow the specific dosing instructions provided by your healthcare provider or the product packaging. The recommended duration of patch wear can vary, typically ranging from 16 to 24 hours. 
• Dispose of used patches properly: After removing the patch, fold it in half with the adhesive sides together and dispose of it safely, away from children and pets. Used patches still contain nicotine and should not be reused or flushed down the toilet. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: nicotine transdermal 

Pronounced: (ni-KOH-teen trans-DER-muhl)  

Why do we use nicotine transdermal? 

• Smoking cessation: nicotine patches are widely used to assist individuals in quitting smoking. They provide a controlled and steady release of nicotine, which helps alleviate withdrawal symptoms and reduce the craving for cigarettes. The patches are typically used as part of a comprehensive smoking cessation program that may include behavioural support and counselling. 
• Nicotine dependence reduction: nicotine transdermal patches can be used to reduce nicotine dependence in individuals who are not yet ready to quit smoking completely or who wish to gradually reduce their nicotine intake. They help manage cravings and withdrawal symptoms, providing an alternative source of nicotine without the harmful effects of tobacco smoke. 
• Temporary nicotine replacement: nicotine patches may be used in situations where smoking is prohibited or impractical, such as during long flights, hospital stays, or other restricted environments. They can help alleviate nicotine cravings during these periods without the need for smoking. 
• Harm reduction: In some cases, nicotine transdermal patches are used as a harm reduction strategy for patients who are not able or unwilling to quit smoking entirely. By providing a controlled dose of nicotine, the patches can help reduce the harmful effects associated with smoking tobacco products.