Product Information
Registration Status: ActiveNICOTINELL FRUIT 4MG GUM is approved to be sold in Singapore with effective from 2007-10-05. It is marketed by GSK CONSUMER HEALTHCARE SINGAPORE PTE LTD, with the registration number of SIN13271P.
This product contains Nicotine 4mg in the form of GUM, CHEWING. It is approved for ORAL use.
This product is manufactured by Fertin Pharma A/S (7100) in DENMARK.
It is a Pharmacy Only Medicine that can be obtained from a pharmacist at a retail pharmacy.
Description
Nicotine is highly toxic alkaloid. It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. Nicotine is also important medically because of its presence in tobacco smoke.
Indication
For the relief of nicotine withdrawal symptoms and as an aid to smoking cessation.
Mechanism of Action
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. 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.
Pharmacokinetics
- 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.
- Distribution
- * 2 to 3 L/kg
- Metabolism
- Primarily hepatic, cotinine is the primary metabolite.
- Elimination
Clearance
* 1.2 L/min [healthy adult smoker]
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).
Active Ingredient/Synonyms
(−)-nicotine | (S)-(−)-nicotine | (S)-3-(1-methylpyrrolidin-2-yl)pyridine | (S)-3-(N-methylpyrrolidin-2-yl)pyridine | (S)-Nicotine | 3-(2-(N-methylpyrrolidinyl))pyridine | 3-(N-methylpyrollidino)pyridine | L(−)-nicotine | Nicotine betadex | Nicotine polacrilex | Nicotine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.