Generic
Varenicline Tartrate
1 brands available in the market
At a glance
Varenicline Tartrate is a prescription medicine used to quit smoking by reducing the craving for a cigarette and the irritable feeling that occurs when you stop smoking. It works by blocking nicotine effect on the brain and this suppresses enjoyment while smoking or the urge to smoke.
Description
Varenicline binds with high affinity and selectivity at α4β2 neuronal nicotinic acetylcholine receptors. The efficacy of Varenicline in smoking cessation is believed to be the result of varenicline's activity at α4β2 sub-type of the nicotinic receptor where its binding produces agonist activity, while simultaneously preventing nicotine binding to these receptors.
Indications
- Quitting smoking
Therapeutic class
Drugs used in substance dependence
Pharmacological class
Nicotinic Receptor Partial Agonist
Pharmacology
Varenicline binds with high affinity and selectivity at α4β2 neuronal nicotinic acetylcholine receptors. Electrophysiology studies in vitro and neurochemical studies in vivo have shown that varenicline binds to α4β2 neuronal nicotinic acetylcholine receptors and stimulates receptor-mediated activity, but at a significantly lower level than nicotine. Varenicline blocks the ability of nicotine to activate α4β2 receptors.
Mechanism of action
Acts as a partial agonist at α4β2 nicotinic receptors, blocking nicotine effects and reducing withdrawal symptoms.
Dosage
Adult Dose (Oral):
- Begin 1 week before the quit date
- Days 1-3: 0.5 mg once daily
- Days 4-7: 0.5 mg twice daily
- Day 8 to end of treatment: 1 mg twice daily
- If successful after 12 weeks, continue another 12 weeks at 1 mg twice daily
- Severe renal impairment (CrCl <30 mL/min): 0.5 mg once daily initially; may increase to 0.5 mg twice daily; ESRD: not to exceed 0.5 mg once daily
Administration
- May be taken with or without food
- Swallow whole; do not chew, crush or break
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as possible; if almost time for next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Nausea
- Headache
- Insomnia
- Abnormal dreams
- Nasopharyngitis
- Constipation
- Flatulence
- Vomiting
Precautions & warnings
- May decrease alertness; do not drive
- Counselling should be done to increase chances of successful quit attempt
- Stop taking and inform doctor if sudden mood and behavior changes or suicidal thoughts occur
- Inform doctor if history of heart diseases, fits (seizures), or other mental disorders
- Increased effects of alcohol have been reported; reduce alcohol consumption
- Discontinue and notify doctor if somnambulism occurs
Contraindications
- Documented hypersensitivity or skin reactions to drug or components of formulation
- Nonsmokers
Drug interactions
- Transdermal nicotine: increased incidence of adverse effects (nausea, vomiting)
- Cimetidine: increased exposure
- Other smoking cessation therapies: safety and efficacy not established
- Theophylline, warfarin, insulin: pharmacokinetics or pharmacodynamics may be altered
Food interactions
It is unsafe to consume alcohol with Varenicline Tartrate.
Use in pregnancy
Use in Pregnancy: May be unsafe; animal studies show harmful effects; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Caution needed; breastfeeding should be held until treatment is completed and drug is eliminated.
Pediatric use
Safety and efficacy not established in children under 18 years
Geriatric use
Dosage adjustment not required, but consider renal function
Renal / hepatic impairment
Renal Impairment: Mild-to-moderate (CrCl ≥30 mL/min): no dosage adjustment; Severe (CrCl <30 mL/min): 0.5 mg once daily initially; ESRD: not to exceed 0.5 mg once daily
Hepatic Impairment: Safe; no dose adjustment recommended
Overdose effects
Symptoms: Nausea, headache, insomnia.
Treatment: Supportive care.
Storage conditions
Keep below 30°C, away from light and moisture; keep out of reach of children.