Varenicline Tartrate

Generic Details

Generic Name

Varenicline Tartrate

Other Names

  • Chantix

Drug Class

  • Smoking cessation aid

Chemical Formula

C13H13N3.C4H6O6

Molecular Weight

361.32 g/mol

Mechanism of Action

  • Partial agonist at α4β2 nicotinic acetylcholine receptors

Indications

  • Smoking cessation

Common Dosage Forms

  • Tablet

Typical Dosage

  • Start with 0.5 mg once daily for 3 days, then 0.5 mg twice daily for 4 days, then 1 mg twice daily for 12 weeks.

Pediatric Dosage

  • Not established

Geriatric Dosage

  • Dose adjustment may be necessary in elderly patients

Side Effects

  • Nausea
  • Insomnia
  • Abnormal dreams
  • Headache
  • Dizziness

Contraindications

  • Hypersensitivity to varenicline
  • Severe renal impairment

Pregnancy Category

  • Category C

Lactation Safety

  • Not recommended

Drug Interactions

  • Cimetidine
  • Antipsychotics
  • Theophylline

Overdose Symptoms

  • Nausea
  • Vomiting
  • Weakness
  • Dizziness

Antidote for Overdose

  • No specific antidote, symptomatic and supportive treatment

Storage Conditions

  • Store at room temperature away from moisture and heat

Pharmacokinetics

  • Absorption: Well absorbed after oral administration
  • Distribution: Protein binding is approximately 92%
  • Metabolism: Primarily hepatic via CYP2A6
  • Excretion: Mainly via urine (92%) as unchanged drug

Precautions

  • Use with caution in patients with psychiatric disorders
  • Monitor for changes in behavior or mood

Warnings

  • Neuropsychiatric events reported