Nic-Sal - General Information
Nic-Sal is highly toxic alkaloid. It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. Nic-Sal is also important medically because of its presence in tobacco smoke. [PubChem]
Pharmacology of Nic-Sal
Nic-Sal, 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. Nic-Sal 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. Nic-Sal is a highly addictive substance. Nic-Sal also induces peripheral vasoconstriction, tachycardia and elevated blood pressure. Nic-Sal inhalers and patches are used to treat smoking withdrawl syndrome. Nic-Sal is classified as a stimulant of autonomic ganglia.
Nic-Sal for patients
A patient information sheet is included in the package of NICOTROL Inhaler cartridges dispensed to the patient. Patients should be encouraged to read the information sheet carefully and to ask their physician and pharmacist about the proper use of the product.
Patients must be advised to keep both used and unused cartridges out of the reach of children and pets.
Physiological changes resulting from smoking cessation, with or without nicotine replacement, may alter the pharmacokinetics of certain concomitant medications, such as tricyclic antidepressants and theophylline. Doses of these and perhaps other medications may need to be adjusted in patients who successfully quit smoking.
Use of NICOTROL Inhaler therapy is contraindicated in patients with known hypersensitivity or allergy to nicotine or to menthol.
Additional information about Nic-Sal
Nic-Sal Indication: For the relief of nicotine withdrawal symptoms and as an aid to smoking cessation.
Mechanism Of Action: Nic-Sal binds to the nicotinic acetylcholine receptor. Stimulation of nicotinic receptors leads to a variety of cholinergic and adrenergic effects; tachycardia or bradycardia mediated by either stimulation or interference with sympathetic or parasympathetic pathways, stimulation of receptors in the carotic and aortic bodies, release of epinephrine from the adrenal medulla, and stimulation of the chemoreceptor-trigger zone.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Nicotine
Synonyms: L-Nicotine; Nicotine Alkaloid
Drug Category: Anti-craving Agents; Central Nervous System Agents; Autonomic drugs; Nicotinic Agonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Nicotine: Black Leaf; Black Leaf 40; Campbell's Nico-Soap; Commit; Destruxol Orchid Spray; Emo-Nik; Flux Maag; Fumetobac; Habitrol; Mach-Nic; Niagara P.A. Dust; Nic-Sal; Nico-Dust; Nico-Fume; Nicocide; Nicoderm; Nicoderm Cq; Nicorette; Nicorette Plus; Nicotin; Nicotina; Nicotine Polacrilex; Nicotrol; Nicotrol Inhaler; Nicotrol Ns; Nikotin; Nikotyna; Ortho N-4 Dust; Ortho N-5 Dust; Prostep; Tendust;
Absorption: 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.
Toxicity (Overdose): 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).
Protein Binding: Less than 5%
Biotransformation: Primarily hepatic, cotinine is the primary metabolite.
Half Life: Cotinine has a half life of 15-20 hours, while nicotine has a half life of 1-3 hours
Dosage Forms of Nic-Sal: Tablet, extended release Oral
Capsule, extended release Oral
Drug delivery system Respiratory (inhalation)
Solution / drops Oral
Chemical IUPAC Name: 3-(1-methylpyrrolidin-2-yl)pyridine
Chemical Formula: C10H14N2
Nicotine on Wikipedia: https://en.wikipedia.org/wiki/Nicotine
Organisms Affected: Humans and other mammals