Nicotine

BRAND NAMES:

Nicorelief – It contains the active ingredients of Nicotine. It is available in the form of gum used to stop smoking aid. 

Habitrol – It contains the active ingredients of Nicotine. It is available in the form of patches and chewing gum used to stop smoking.

Nicoderm C-Q – It contains the active ingredients of Nicotine. It is available in the form of patches.  This patch treatment is used in three steps based on the usage of cigarettes.

MECHANISM OF ACTION:

Nicotine's principal mechanism of action is through particular nicotinic acetylcholine receptors in the brain. It stimulates presynaptic acetylcholine receptors, which increases Ach release and metabolism. It also stimulates the dopaminergic system, boosting dopamine levels in the nucleus accumbens.

PHARMACOKINETICS:

Absorption: Nicotine absorption through the buccal mucosa is somewhat sluggish, and the inhaler does not achieve the high and quick rise followed by the drop in nicotine arterial plasma concentrations observed with cigarette smoking. 

Distribution: The mean volume of distribution of nicotine is 2 to 3L/kg.

Metabolism: In humans, nicotine is metabolized by three primary pathways: P450-catalyzed 5’-oxidation, UGT-catalyzed N-glucuronidation, and flavin monooxygenase-catalyzed N-oxidation. The iminium ion product of nicotine 5’-oxidation is further metabolized to cotinine. The formation of cotinine is quantitatively the most important nicotine metabolism pathway. Three minor pathways: methylation of the pyridine nitrogen to the nicotine isomethonium ion, 2’-Oxidation, and Oxidative N-Methylation also contribute to nicotine metabolism.

Excretion: About 10% of the absorbed nicotine is excreted through unchanged in urine

PHARMACODYNAMICS:

Nicotine administered intravenously stimulates the release of acetylcholine, norepinephrine, dopamine, serotonin, vasopressin, beta-endrophin, and ACTH. Nicotine is a highly addictive drug. Nicotine also causes peripheral vasoconstriction, tachycardia, and elevated blood pressure. To treat smokers suffering from drawl syndrome, nicotine inhalers and patches are used. Nicotine is classified as an autonomic nervous system stimulant. Nicotine has two effects: a stimulating effect at the locus ceruleus and a rewarding result in the limbic system.

DOSAGE AND ADMINISTRATION:

Nicotine is available in gums, lozenges, patches, nasal sprays, and inhalers. For oral dosage forms gums and lozenge are not taken more than one piece at a time. Do not use more than 24 and 20 pieces of gum and lozenge a day.

Transdermal patches are typically applied on the upper arm or shoulder. Do not cut the patch before using it. Treatment of patches is in 3 steps based on smoking. Apply a new patch upon awakening and wear the patch for 24 hours.

• Nicotine is available in the form of gums with strengths of 2 or 4 mg.

• Nicotine is available in the form of a pill with the strengths of 2 or 4 mg.

• Transdermal patches- 7mg/day,14mg/day,21mg/day

• Inhaler – 16 cartridges /day or the first 3 to 6 weeks

• Nasal Spray- 40mg/day

DRUG INTERACTIONS:

Drug interaction with nicotine may include

• Bronchodilators – theophylline

• Anti-psychotics – clozapine and olanzapine

• Anti-parkinsons drugs – ropinirole

• Anti-diabetic drug - insulin

CONTRAINDICATIONS:

• Individuals with hypersensitivity or allergies to nicotine should refrain from using NRT products.

• Individuals with a known allergy to soy should avoid using nicotine lozenges.

• Potential risk of exposing breastfed infants to nicotine through breast milk.

SIDE EFFECTS:

Side effects of nicotine may include

Central nervous system:

• dizziness and lightheadedness

  • sleep disturbances

  • changes in blood flow

Cardiovascular system:

• increased risk of blood clotting

  • increased blood pressure

  • changes in heart rhythm and rate

Respiratory system:

• shortness of breath

  • bronchospasms

Muscular system:

• Tremors

  • Joint pain

Gastrointestinal system:

• Peptic ulcers

  • Diarrhea

  • Nausea

  • Dry mouth

Common side effects of nicotine may include

• Skin irritation

  • Racing heartbeat

  • Dizziness

  • Sleep problems

  • Nausea

  • Stiffness of muscle

OVERDOSE:

Symptoms of overdose may include

• Nausea

  • Abdominal pain

  • Vomiting

  • Diarrhea

  • Diaphoresis

  • Flushing

  • Dizziness

  • Disturbed vision, confusion weakness

  • Hypotension

TOXICITY:

Nicotine poisoning refers to the harmful effects of nicotine, a substance found in all tobacco products. Liquid nicotine, a component of the popular e-cigarette, has recently been linked to an upsurge in poisonings. Children are particularly susceptible to poisoning due to their smaller size. Vomiting, rapid heartbeat, instability, and excessive salivation are some of the symptoms. 

Nicotine poisoning treatment may involve activated charcoal to limit nicotine absorption in the intestines. Other treatments are used to treat certain symptoms.e used to treat certain symptoms.