pharmacopeia
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/api/v1/drug/varenicline
2D structure
(1S,12R)-5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2,4,6,8,10-pentaene
SMILES C1[C@@H]2CNC[C@H]1C3=CC4=NC=CN=C4C=C23
InChIKey JQSHBVHOMNKWFT-DTORHVGOSA-N

Mechanism of action

Sourced from openFDA

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.

CholinergicPartial Cholinergic Nicotinic

Indications

Sourced from openFDA
  • Varenicline tablets are indicated for use as an aid to smoking cessation treatment. Varenicline tablets are a nicotinic receptor partial agonist indicated for use as an aid to smoking cessation treatment.ICD-10: F17.200

Contraindications

Sourced from openFDA
  • Varenicline tablets are contraindicated in patients with a known history of serious hypersensitivity reactions or skin reactions to varenicline tablets. History of serious hypersensitivity or skin reactions to varenicline tablets.contraindicated

Dosage & administration

Sourced from openFDA

Begin varenicline tablets dosing one week before the date set by the patient to stop smoking. Alternatively, the patient can begin varenicline tablets dosing and then quit smoking between days 8 and 35 of treatment. ( 2.1 ) Starting Week: 0.5 mg once daily on days 1 to 3 and 0.5 mg twice daily on days 4 to 7. ( 2.1 ) Continuing Weeks: 1 mg twice daily for a total of 12 weeks. ( 2.1 ) An additional 12 weeks of treatment is recommended for successful quitters to increase likelihood of long-term abstinence. ( 2.1 ) Consider a gradual approach to quitting smoking with varenicline tablets for patients who are sure that they are not able or willing to quit abruptly. Patients should begin varenicline tablets dosing and reduce smoking by 50% from baseline within the first four weeks, by an additional 50% in the next four weeks, and continue reducing with the goal of reaching complete abstinence by 12 weeks. Continue treatment for an additional 12 weeks, for a total of 24 weeks. ( 2.1 ) Severe Renal Impairment (estimated creatinine clearance less than 30 mL/min): Begin with 0.5 mg once daily and titrate to 0.5 mg twice daily. For patients with end-stage renal disease undergoing hemodialysis, a maximum of 0.5 mg daily may be given if tolerated. ( 2.2 ) Consider dose reduction for patients who cannot tolerate adverse effects. ( 2.1 ) Another attempt at treatment is recommended for those who fail to stop smoking or relapse when factors contributing to the failed attempt have been addressed.

Warnings & precautions

Sourced from openFDA

Neuropsychiatric Adverse Events: Postmarketing reports of serious or clinically significant neuropsychiatric adverse events have included changes in mood (including depression and mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, agitation, anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed suicide. Observe patients attempting to quit smoking with varenicline for the occurrence of such symptoms and instruct them to discontinue varenicline and contact a healthcare provider if they experience such adverse events. ( 5.1 ) Seizures: New or worsening seizures have been observed in patients taking varenicline. Varenicline should be used cautiously in patients with a history of seizures or other factors that can lower the seizure threshold. ( 5.2 ) Interaction with Alcohol: Increased effects of alcohol have been reported. Instruct patients to reduce the amount of alcohol they consume until they know whether varenicline affects them. ( 5.3 ) Accidental Injury: Accidental injuries (e.g., traffic accidents) have been reported. Instruct patients to use caution driving or operating machinery until they know how varenicline may affect them. ( 5.4 ) Cardiovascular Events: Patients with underlying cardiovascular (CV) disease may be at increased risk of CV events; however, these concerns must be balanced with the health benefits of smoking cessation.

Adverse reactions

Sourced from openFDA

The following serious adverse reactions were reported in postmarketing experience and are discussed in greater detail in other sections of the labeling: Neuropsychiatric Adverse Events including Suicidality [see Warnings and Precautions (5.1) ] Seizures [see Warnings and Precautions (5.2) ] Interaction with Alcohol [see Warnings and Precautions (5.3) ] Accidental Injury [see Warnings and Precautions (5.4) ] Cardiovascular Events [see Warnings and Precautions (5.5) ] Somnambulism [see Warnings and Precautions (5.6) ] Angioedema and Hypersensitivity Reactions [see Warnings and Precautions (5.7) ] Serious Skin Reactions [see Warnings and Precautions (5.8) ] In the placebo-controlled premarketing studies, the most common adverse events associated with varenicline (>5% and twice the rate seen in placebo-treated patients) were nausea, abnormal (vivid, unusual, or strange) dreams, constipation, flatulence, and vomiting. The treatment discontinuation rate due to adverse events in patients dosed with 1 mg twice daily was 12% for varenicline, compared to 10% for placebo in studies of three months’ treatment. In this group, the discontinuation rates that are higher than placebo for the most common adverse events in varenicline-treated patients were as follows: nausea (3% vs. 0.5% for placebo), insomnia (1.2% vs. 1.1% for placebo), and abnormal dreams (0.3% vs. 0.2% for placebo). Smoking cessation, with or without treatment, is associated with nicotine withdrawal symptoms and has also been associated with the exacerbation of underlying psychiatric illness.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Risk Summary Available data have not suggested an increased risk for major birth defects following exposure to varenicline in pregnancy, compared with women who smoke [see Data]. Smoking during pregnancy is associated with maternal, fetal, and neonatal risks (see Clinical Considerations) . In animal studies, varenicline did not result in major malformations but caused decreased fetal weights in rabbits when dosed during organogenesis at exposures equivalent to 50 times the exposure at the maximum recommended human dose (MRHD). Additionally, administration of varenicline to pregnant rats during organogenesis through lactation produced developmental toxicity in offspring at maternal exposures equivalent to 36 times human exposure at the MRHD [see Data] . The estimated background risk of oral clefts is increased by approximately 30% in infants of women who smoke during pregnancy, compared to pregnant women who do not smoke. The background risk of other major birth defects and miscarriage for the indicated population are unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption Maximum plasma concentrations of varenicline occur typically within 3 to 4 hours after oral administration. Following administration of multiple oral doses of varenicline, steady-state conditions were reached within 4 days.

Overdosage

Sourced from openFDA

In case of overdose, standard supportive measures should be instituted as required. Varenicline has been shown to be dialyzed in patients with end-stage renal disease [see Clinical Pharmacology (12.3) ], however, there is no experience in dialysis following overdose.

Approval history

Sourced from openFDA
  • May 10, 2006NDANDA021928Pf Prism Cv
  • Aug 11, 2021ANDAANDA201785Ph Health
  • Oct 15, 2021NDANDA213978Oyster Point Pharma
  • Jan 25, 2023ANDAANDA201962Apotex
  • Jun 12, 2023ANDAANDA216723Zydus
  • Jul 25, 2023ANDAANDA217151Kanchan Hlthcare
  • Aug 1, 2023ANDAANDA214255Mankind Pharma
  • Aug 23, 2023ANDAANDA214557Alkem Labs Ltd

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
82,298 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Nausea14,48718%
  2. 2Depression8,67911%
  3. 3Abnormal Dreams7,8419.5%
  4. 4Drug Ineffective6,0017.3%
  5. 5Anxiety5,9777.3%
  6. 6Insomnia5,6156.8%
  7. 7Vomiting4,6055.6%
  8. 8Headache4,3135.2%
  9. 9Suicidal Ideation4,2065.1%
  10. 10Feeling Abnormal4,0194.9%
  11. 11Malaise4,0054.9%
  12. 12Nightmare3,3554.1%
  13. 13Fatigue3,2063.9%
  14. 14Dizziness3,0713.7%
  15. 15Aggression2,7713.4%

Literature

View JSON

Recent PubMed references pinned to Varenicline as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 399 ClinicalTrials.gov registrations naming Varenicline as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Varenicline work?
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.
What is Varenicline used for?
According to FDA labeling, Varenicline carries indications including: Varenicline tablets are indicated for use as an aid to smoking cessation treatment. Varenicline tablets are a nicotinic receptor partial agonist indicated for use as an aid to smoking cessation treatment.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Varenicline?
Varenicline is classified as Drugs used in nicotine dependence, Other ophthalmologicals, Cholinergic Receptor Agonist, Partial Cholinergic Nicotinic Agonist, Cholinergic Agonists, Partial Cholinergic Nicotinic Agonists, Decreased Central Nervous System Dopamine Activity.
What are the brand names for Varenicline?
Varenicline is marketed under brand names including Chantix, Tyrvaya.
What are the contraindications for Varenicline?
Varenicline labeling lists contraindications including: Varenicline tablets are contraindicated in patients with a known history of serious hypersensitivity reactions or skin reactions to varenicline tablets. History of serious hypersensitivity or skin reactions to varenicline tablets.. Always consult the full prescribing information and a clinician.
Note. Data for varenicline is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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