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Varenicline

Varenicline, is a prescription medication used to treat nicotine addiction. Varenicline is a nicotinic receptor partial agonist—it stimulates nicotine receptors more weakly than nicotine itself does. More

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Description

Varenicline, is a prescription medication used to treat nicotine addiction. Varenicline is a nicotinic receptor partial agonist—it stimulates nicotine receptors more weakly than nicotine itself does.

Generic Name

Varenicline

Chemical names

Varenicline; UNII-W6HS99O8ZO; CP 526555; HSDB 7591

Brand names

Champix

IUPAC name

(1R,12S)-5,8,14-triazatetracyclo[10.3.1.0²,¹¹.0?,?]hexadeca-2,4,6,8,10-pentaene

Pharmacokinetics

Less than 20% protein binding.

Actions

It is an alpha-4 beta-2 neuronal nicotinic acetylcholine receptor partial agonist. Varenicline is a partial nicotinic acetylcholine receptor agonist, designed to partially activate this system while displacing nicotine at its sites of action in the brain. This inhibits the ability of nicotine to bind to and activate the alpha-4 beta-2 receptor competitively. 

Dosage/Dosage form

0.5mg once daily for 1st 3 days followed by 0.5 mg twice daily for the next 4 days as per oral.

Therapeutic uses

For use as an aid in smoking cessation.

Adverse effects/Side effects

Abdominal pain, nausea, vomiting, sleep disorder, fatigue, rash, itching, runny nose, chest pain.

Interaction

This drug may interact with insulin, anti-asthmatic drugs including theophylline, and blood thinners like warfarin.

Contraindications

  • Hypersensitivity.

This is contraindicated in patients with history of renal diseases, mental illness, circulatory and heart problems. 

Storage

Store it at room temperature.

Information

Molecular weight

211.2624

Molecular formula

C13H13N3

CAS number

249296-44-4

Precautions

  • Do not self-medicate drugs to quit smoking while using Varenicline.
  • Abrupt stopping of smoking may cause behavioural and mood changes and impair thinking/cognition.
  • Do not drive vehicle or operate heavy machineries while taking Varenicline.