Exagen
Exagen Uses, Dosage, Side Effects, Food Interaction and all others data.
Exagen, 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.
Exagen, 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. Exagen 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. Exagen is a highly addictive substance. Exagen also induces peripheral vasoconstriction, tachycardia and elevated blood pressure. Exagen inhalers and patches are used to treat smoking withdrawl syndrome. Exagen is classified as a stimulant of autonomic ganglia.
| Trade Name | Exagen |
| 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 | New Zealand |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Cognitive enhancer, Smoking cessation, Smoking cessation aid
Exagen is also used to associated treatment for these conditions: Dental Cavity, Nicotine Withdrawal
How Exagen works
Exagen 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. Exagen 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
Exagen 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.
Exagen 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
Exagen 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 Exagen
FAQ
What is Exagen used for?
Exagen used recreationally as a stimulant and anxiolytic. As a pharmaceutical drug, it is used for smoking cessation to relieve withdrawal symptoms. Exagen is used to help treat addiction to or dependence on smoking cigarettes.
How safe is Exagen?
Exagen 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 Exagen work?
Exagen 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 Exagen?
Common side effects of Exagen are decreased appetite, heightened mood, increased heart rate and blood pressure, nausea, diarrhea, better memory, and increased alertness.
Is Exagen safe during pregnancy?
Exagen are not safe to use during pregnancy.
Is Exagen safe during breastfeeding?
Exagen can be passed from a breastfeeding mother who uses tobacco to her infant through breast milk.
Is Exagen 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 Exagen ?
High levels of Exagen 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 Exagen level.
When should be taken of Exagen?
It is usually taken at least 15 minutes after eating or drinking.
How often should I take Exagen ?
A schedule of 1 to 2 pieces per hour is common.
How long can I take Exagen?
Exagen gum is usually recommended for 6 to 12 weeks, with the maximum being 6 months.
How long does Exagen take to work?
Exagen acts quickly in the body. When smoked, the substance enters the bloodstream and makes it to the brain within 20 seconds.
How long does Exagen take to work?
Generally, Exagen 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 Exagen nor cotinine will be detectable in your urine after 3 to 4 days of stopping tobacco products.
Who should not use Exagen?
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 Exagen good for my brain?
Preclinical models and human studies have demonstrated that Exagen has cognitive-enhancing effects, including improvement of fine motor functions, attention, working memory, and episodic memory.
How much Exagen 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 Exagen-containing solution could kill an adult.
Does Exagen cause dementia?
There is strong evidence that smoking can increase your risk of dementia.
What happen If I stop taking Exagen?
Exagen withdrawal involves physical, mental, and emotional symptoms. The first week, especially days 3 through 5, is always the worst. That's when the Exagen 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 Exagen 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 Exagen ?
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 Exagen affects my heart ?
Exagen 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). Exagen may also contribute to the hardening of the arterial walls, which in turn, may lead to a heart attack.
Is Exagen hard on the kidneys?
Exagen 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 Exagen affects my liver?
Exagen has not been associated with liver test abnormalities or with clinically apparent hepatotoxicity.
Will Exagen affect my fertility?
Exagen 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.
