NICOTINELL TTS 30 TRANSDERMAL THERAPEUTIC SYSTEM 21mg/24 HRS

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.

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 |

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.

Pharmacodynamics

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. 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. Nicotine is a highly addictive substance. Nicotine also induces peripheral vasoconstriction, tachycardia and elevated blood pressure. Nicotine inhalers and patches are used to treat smoking withdrawl syndrome. Nicotine is classified as a stimulant of autonomic ganglia.

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:

About 10% of the nicotine absorbed is excreted unchanged in the 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]

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).

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

NICOTINELL TTS 30 TRANSDERMAL THERAPEUTIC SYSTEM 21mg/24 HRS was registered with Health Science Authority of Singapore by GSK CONSUMER HEALTHCARE SINGAPORE PTE LTD. It is marketed with the registration number of SIN06529P with effective from 1991-12-11.

This product contains 52.5mg/30 sq cm of Nicotine in the form of PATCH.

The medicine was manufactured by LTS LOHMANN THERAPIE-SYSTEME AG in GERMANY

It is a Pharmacy Only Medicine which can be obtained from a pharmacist at a retail pharmacy.

Anatomical Therapeutic Chemical (ATC) Classification

ATC Code: N07BA01

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