Transdermal Nicotine
Transdermal Nicotine Uses, Dosage, Side Effects, Food Interaction and all others data.
Transdermal Nicotine, a pyridine alkaloid, is a stereo-selective nicotinic-cholinergic receptor agonist. Low doses cause an initial stimulation of autonomic ganglia, adrenal medulla, neuromuscular junction, and brain. High doses produce initial ganglionic stimulation followed by inhibition of neurotransmission leading to subsequent persistent depression of receptor activity.
Transdermal Nicotine, the primary alkaloid in tobacco products binds stereo-selectively to nicotinic-cholinergic receptors on autonomic ganglia, the adrenal medulla, neuromuscular junctions and in the brain. Transdermal Nicotine exerts two effects, a stimulant effect exerted at the locus ceruleus and a reward effect in the limbic system. Itranvenous administration of nicotine causes release of acetylcholine, norepinephrine, dopamine, serotonine, vasopressin, beta-endorphin and ACTH. Transdermal Nicotine is a highly addictive substance. Transdermal Nicotine also induces peripheral vasoconstriction, tachycardia and elevated blood pressure. Transdermal Nicotine inhalers and patches are used to treat smoking withdrawl syndrome. Transdermal Nicotine is classified as a stimulant of autonomic ganglia.
| Trade Name | Transdermal Nicotine |
| Availability | Rx and/or OTC |
| Generic | Nicotine |
| Nicotine Other Names | (S)-Nicotine, Nicotina, Nicotine, Nicotine betadex, Nicotine polacrilex, Nikotin, Nikotyna |
| Related Drugs | bupropion, Chantix, varenicline, Zyban, Nicoderm CQ, Nicorette |
| Type | |
| Formula | C10H14N2 |
| Weight | Average: 162.2316 Monoisotopic: 162.115698458 |
| Protein binding | Less than 5% |
| Groups | Approved |
| Therapeutic Class | Drugs used in substance dependence |
| Manufacturer | |
| Available Country | Canada, United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Cognitive enhancer, Smoking cessation, Smoking cessation aid
Transdermal Nicotine is also used to associated treatment for these conditions: Dental Cavity, Nicotine Withdrawal
How Transdermal Nicotine works
Transdermal Nicotine is a stimulant drug that acts as an agonist at nicotinic acetylcholine receptors. These are ionotropic receptors composed up of five homomeric or heteromeric subunits. In the brain, nicotine binds to nicotinic acetylcholine receptors on dopaminergic neurons in the cortico-limbic pathways. This causes the channel to open and allow conductance of multiple cations including sodium, calcium, and potassium. This leads to depolarization, which activates voltage-gated calcium channels and allows more calcium to enter the axon terminal. Calcium stimulates vesicle trafficking towards the plasma membrane and the release of dopamine into the synapse. Dopamine binding to its receptors is responsible the euphoric and addictive properties of nicotine. Transdermal Nicotine also binds to nicotinic acetylcholine receptors on the chromaffin cells in the adrenal medulla. Binding opens the ion channel allowing influx of sodium, causing depolarization of the cell, which activates voltage-gated calcium channels. Calcium triggers the release of epinephrine from intracellular vesicles into the bloodstream, which causes vasoconstriction, increased blood pressure, increased heart rate, and increased blood sugar.
Dosage
Transdermal Nicotine dosage
Buccal:As chewing gum containing 2 mg or 4 mg nicotine polacrilex: Smokers of ≤20 cigarettes daily: Start with 2 mg chewed slowly and parked between cheek and gum over 30 min when urge to smoke occurs. Smokers of >20 cigarettes daily: Start with 4 mg. Max: 15 gums daily. As lozenge containing 1, 1.5, 2 or 4 mg nicotine polacrilex or tartrate: Initially, 1 loz 1-2 hrly allowing to slowly dissolve for 20-30 min. Usual dose: 8-12 loz daily. Max: 30 loz (1-mg strength) or 15 loz (higher strengths) daily. Continue treatment for up to 3 mth, then withdraw gradually.
Sublingual:As tab containing 2 mg nicotine β-cyclodextrin complex: 1-2 tab hrly, increased as necessary. Max: 40 tab daily. Continue treatment for up to 3 mth, then withdraw gradually.
Loz: May be taken with or without food. Suck until the taste becomes strong. Then, lodge the loz between the gum & cheek. When the taste fades, start sucking it again. Repeat until the loz completely dissolves (about 30 min). Do not swallow. Avoid coffee, acidic drinks or soft drinks for 15 min prior to sucking the loz.
Gum: May be taken with or without food. Chew gum until the taste becomes strong, then rest it between the gums & the cheek. When the taste fades, start chewing it again. Repeat the chewing routine for 30 min.
Side Effects
Nausea, vomiting, abdominal pain, diarrhoea, headache, dizziness, hiccups, flu-like symptoms, palpitations, insomnia, vivid dreams, myalgia, chest pain, anxiety, irritability, somnolence, dysmenorrhoea; mouth (e.g. aphthous ulceration) and throat irritation; nasal irritation, epistaxis, lachrymation, salivation, swelling of the tongue (gum); unpleasant taste (loz); cough, rhinitis, stomatitis, sinusitis, dry mouth (inhalator); ear sensations (nasal spray); skin reactions (patch).
Toxicity
Symptoms of overdose include nausea, abdominal pain, vomiting, diarrhea, diaphoresis, flushing, dizziness, disturbed hearing and vision, confusion, weakness, palpitations, altered respiration and hypotension. LD50= 24 mg/kg (orally in mice).
Precaution
Patient with CV disease (e.g. MI, severe arrhythmia, unstable angina pectoris, CVA, uncontrolled HTN), peripheral vascular disease, endocrine disorder (e.g. phaeochromocytoma, hyperthyroidism, DM), peptic ulcer, and skin disease (patch). Hepatic and renal impairment. Childn. Pregnancy and Lactation.
Interaction
May enhance the haemodynamic effects of adenosine. Decreased metabolism leading to increased plasma concentrations with methoxsalen.
Food Interaction
- Take separate from meals. For nicotine gum, lozenges, and oral sprays, avoid eating and drinking for 15 minutes before and during its use.
Transdermal Nicotine Drug Interaction
Unknown: aripiprazole, amphetamine / dextroamphetamine, amphetamine / dextroamphetamine, contained in alcoholic beverages , diphenhydramine, duloxetine, omega-3 polyunsaturated fatty acids, clonazepam, lamotrigine, escitalopram, pregabalin, fluoxetine, quetiapine, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, lisdexamfetamine, alprazolam, sertraline
Transdermal Nicotine Disease Interaction
Major: CVD/PVD, pheochromocytomaModerate: diabetes, hyperthyroidism, liver disease, PUD
Volume of Distribution
- 2 to 3 L/kg
Elimination Route
Absorption of nicotine through the buccal mucosa is relatively slow and the high and rapid rise followed by the decline in nicotine arterial plasma concentrations seen with cigarette smoking are not achieved with the inhaler. About 10% of absorbed nicotine is excreted unchanged in urine.
Half Life
Cotinine has a half life of 15-20 hours, while nicotine has a half life of 1-3 hours
Clearance
- 1.2 L/min [healthy adult smoker]
Elimination Route
About 10% of the nicotine absorbed is excreted unchanged in the urine.
Pregnancy & Breastfeeding use
Pregnancy Category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Contraindication
Recent cerebrovascular accident. Self-medication in patients who will continue to smoke, chew tobacco, or use snuff or other nicotine-containing preparations. Non-smokers and occasional smokers.
Acute Overdose
Symptoms: Burning of the mouth and throat, nausea, vomiting, salivation, abdominal pain, diarrhoea, sweating, headache, dizziness, hearing and visual disturbances, weakness, confusion, syncope, prostration, dyspnoea, tachycardia, hypotension, rapid or weak or irregular pulse, seizure, resp failure, circulatory collapse, coma.
Management: Symptomatic and supportive treatment. Artificial respiration is instituted if necessary. Employ activated charcoal to reduce GI absorption. For TTS, the skin should be washed with water without using soap and dried.
Storage Condition
Store below 25˚ C. Protect from light and moisture.
Innovators Monograph
You find simplified version here Transdermal Nicotine
FAQ
What is Transdermal Nicotine used for?
Transdermal Nicotine used recreationally as a stimulant and anxiolytic. As a pharmaceutical drug, it is used for smoking cessation to relieve withdrawal symptoms. Transdermal Nicotine is used to help treat addiction to or dependence on smoking cigarettes.
How safe is Transdermal Nicotine?
Transdermal Nicotine is a dangerous and highly addictive chemical. It can cause an increase in blood pressure, heart rate, flow of blood to the heart and a narrowing of the arteries.
How does Transdermal Nicotine work?
Transdermal Nicotine works by stimulating our nervous system to release specific chemical messengers (hormones and neurotransmitters) that affect different parts of our brain and body.
What are the common side effects of Transdermal Nicotine?
Common side effects of Transdermal Nicotine are decreased appetite, heightened mood, increased heart rate and blood pressure, nausea, diarrhea, better memory, and increased alertness.
Is Transdermal Nicotine safe during pregnancy?
Transdermal Nicotine are not safe to use during pregnancy.
Is Transdermal Nicotine safe during breastfeeding?
Transdermal Nicotine can be passed from a breastfeeding mother who uses tobacco to her infant through breast milk.
Is Transdermal Nicotine good with alcohol?
Alcohol consumption and cigarette smoking often go hand in hand. A rodent study has found that low doses of alcohol and nicotine can have an additive effect on the release of the neurotransmitter dopamine.
Can I drive after taking Transdermal Nicotine ?
High levels of Transdermal Nicotine can also impair driving causing dizziness and light-headedness. While this may pass in a few seconds, accidents can happen in the blink of an eye. If you have to vape while driving, keep this in mind, take more shallow hits, or consider reducing your Transdermal Nicotine level.
When should be taken of Transdermal Nicotine?
It is usually taken at least 15 minutes after eating or drinking.
How often should I take Transdermal Nicotine ?
A schedule of 1 to 2 pieces per hour is common.
How long can I take Transdermal Nicotine?
Transdermal Nicotine gum is usually recommended for 6 to 12 weeks, with the maximum being 6 months.
How long does Transdermal Nicotine take to work?
Transdermal Nicotine acts quickly in the body. When smoked, the substance enters the bloodstream and makes it to the brain within 20 seconds.
How long does Transdermal Nicotine take to work?
Generally, Transdermal Nicotine will leaves your blood within 1 to 3 days after you stop using tobacco, and cotinine will be gone after 1 to 10 days. Neither Transdermal Nicotine nor cotinine will be detectable in your urine after 3 to 4 days of stopping tobacco products.
Who should not use Transdermal Nicotine?
Tell your doctor if you have or have ever had a heart attack, heart disease, irregular heart rate, ulcers, diabetes, or high blood pressure not controlled by medication; if you are under 18 years of age; or if you are on a sodium-restricted diet.
Is Transdermal Nicotine good for my brain?
Preclinical models and human studies have demonstrated that Transdermal Nicotine has cognitive-enhancing effects, including improvement of fine motor functions, attention, working memory, and episodic memory.
How much Transdermal Nicotine a day is safe?
Standard textbooks, databases, and safety sheets consistently state that the lethal dose for adults is 60 mg or less (30–60 mg), leading to safety warnings that ingestion of five cigarettes or 10 ml of a dilute Transdermal Nicotine-containing solution could kill an adult.
Does Transdermal Nicotine cause dementia?
There is strong evidence that smoking can increase your risk of dementia.
What happen If I stop taking Transdermal Nicotine?
Transdermal Nicotine withdrawal involves physical, mental, and emotional symptoms. The first week, especially days 3 through 5, is always the worst. That's when the Transdermal Nicotine has finally cleared out of your body and you'll start getting headaches, cravings, and insomnia. Most relapses happen within the first two weeks of quitting.
What happens if I overdose?
There are a number of symptoms you want to watch for if you are worried about a possible Transdermal Nicotine overdose. Within the first 15 minutes to an hour of being exposed, symptoms would create a stimulating effect such as: Nausea or vomiting. Stomachache and loss of appetite.
How long will I miss Transdermal Nicotine ?
Cigarette cravings typically peak in the first few days after quitting and diminish greatly over the course of the first month without smoking. 1 While you might miss smoking from time to time, once you make it past six months, the urge to smoke will be diminished or even gone.
Can Transdermal Nicotine affects my heart ?
Transdermal Nicotine can cause an increase in blood pressure, heart rate, flow of blood to the heart and a narrowing of the arteries (vessels that carry blood). Transdermal Nicotine may also contribute to the hardening of the arterial walls, which in turn, may lead to a heart attack.
Is Transdermal Nicotine hard on the kidneys?
Transdermal Nicotine increases the severity of renal injury in animal models including acute kidney injury, diabetes, acute nephritis and subtotal nephrectomy. The renal effects of nicotine are also linked to increased generation of reactive oxygen species and activation of pro-fibrotic pathways.
Can Transdermal Nicotine affects my liver?
Transdermal Nicotine has not been associated with liver test abnormalities or with clinically apparent hepatotoxicity.
Will Transdermal Nicotine affect my fertility?
Transdermal Nicotine decreased sperm quality with lower counts (numbers of sperm) and motility (sperm's ability to move) and increased numbers of abnormallyshaped sperm. Smoking might also decrease the sperm's ability to fertilize eggs.
