Varenicline (Varenicline tartrate)

Varenicline (Varenicline Tartrate): Patient Information for Australia

Basic Product Information

Mechanism of Action

For Patients: Varenicline helps people stop smoking by reducing both the pleasure from smoking and the cravings or withdrawal caused by quitting. It works by affecting certain receptors in the brain involved in nicotine addiction.
For Professionals: Varenicline is a selective partial agonist at the α4β2 nicotinic acetylcholine receptor subtype. It partly stimulates these receptors to relieve withdrawal symptoms and blocks their activation by nicotine, lowering the rewarding effects of cigarettes.

Pharmacokinetics

• Absorption: Rapid and well-absorbed after oral administration. Peak plasma concentration reached in ~3-4 hours.
• Bioavailability: >90%, unaffected by food.
• Metabolism: Minimal hepatic metabolism; mostly excreted unchanged in urine (renal elimination).
• Half-life: Approximately 24 hours; steady state achieved in 4 days.
• Duration of Action: Daily dosing is suitable to maintain therapeutic levels.

Everyday Use and Best Practices

• Varenicline is used to help you quit smoking.
• It should be started 1 to 2 weeks before your planned quit date.
• The usual course is 12 weeks; your doctor may recommend a second course if needed.
• Tablets are taken orally with a glass of water, as directed.
• It’s important to continue using behavioural support and counselling for the best chance of quitting.

Typical Doses and How to Use (Australian Context)

• Day 1–3: 0.5 mg once daily
• Day 4–7: 0.5 mg twice daily
• Day 8 onwards: 1 mg twice daily
• The course typically lasts 12 weeks, with possibility of extension if your doctor recommends.
• Missed doses should be taken as soon as remembered, unless close to the next dose.

Dosing: Morning vs Evening

Varenicline is commonly taken morning and evening (two divided doses) to maintain stable blood levels. Taking at the same times each day reduces the risk of missed doses and helps manage cravings better. Some patients find that evening doses may cause vivid dreams or sleep disturbances; if this happens, taking the second dose earlier in the evening may help. Discuss with your healthcare provider if sleep problems occur.

Taking with Food or on an Empty Stomach

• Varenicline can be taken with or without food.
• Taking it with food or after a meal/glass of milk can reduce the risk of nausea, which is one of the most common side effects.
• There are no major dietary restrictions; maintain a balanced Australian diet as normal.

Interaction Warnings

Indications

Dosing According to Clinical Indication

Safety Profile / Side Effects

Varenicline is generally well tolerated, with most side effects being mild to moderate and temporary.

Guidelines for Proper Use (Pharmacist/Clinic Advice)

• Choose a quit date during the first 1–2 weeks of treatment.
• Take medication at the same times daily (morning and evening).
• If you forget a dose, take it as soon as you remember, unless it’s nearly time for the next one.
• If nausea occurs, take tablets after meals with a glass of water or milk.
• Continue to use support services such as Quitline Australia (13 7848), online resources, and local group programs.
• Inform your doctor about all current medications and any changes in mood or behaviour.
• Store Varenciline in a cool, dry place, away from children.

Alternative Treatment Options

• Nicotine replacement therapy (NRT): Available over-the-counter as patches, gum, lozenges, sprays; can be combined, but less effective than varenicline as monotherapy.
• Bupropion (Zyban): Prescription-only tablet with similar efficacy, may suit those intolerant of NRT or varenicline.
  Pros: May aid mood; Cons: Contraindicated in seizure risk, more drug interactions.
• Nortriptyline: Older antidepressant sometimes used off-label, less evidence and more side effects.
• Counselling & support: Integral part of treatment, best combined with medication for better outcomes.

Legal, Registration & Reimbursement Status in Australia

• Prescription-only (Schedule 4)
• Registered with the Therapeutic Goods Administration (TGA)
• Reimbursed under the Pharmaceutical Benefits Scheme (PBS) for eligible patients seeking to quit smoking (not available for general prevention or off-label use)
• Usual quantity: 4-week packs; total PBS-subsidised treatment limited to 12 weeks/year (renewal possible after review)

Latest Research & Clinical Guidance (2022–2025)

• The 2023 Australian National Tobacco Treatment Guidelines strongly support varenicline as the most effective single pharmacotherapy for smoking cessation in motivated patients (RACGP Green Book).
• Recent meta-analyses (Lancet Respir Med 2023; NEJM 2024) confirm higher quit rates compared to bupropion or NRT alone, especially when combined with behavioural support.
• Emerging data support safety in populations with stable psychiatric illness, with appropriate monitoring.
• Safety signals regarding neuropsychiatric adverse events remain rare; most cases resolve with discontinuation.

Availability and Delivery

FAQs – Frequently Asked Questions

• How long should I take varenicline?
  The standard course is 12 weeks. If you successfully quit but feel you may relapse, your doctor may recommend a second 12-week course.
• Can I keep smoking while I start varenicline?
  Yes, start varenicline 1–2 weeks before your chosen quit date. You continue to smoke, then stop completely on your quit date while continuing treatment.
• What should I do if I miss a dose?
  Take the missed dose as soon as you remember—unless it’s almost time for your next dose. Do not double-dose.
• Is quitting “cold turkey” better than using medication?
  Evidence shows your chance of quitting long-term is much higher if you use proven medications like varenicline and behavioural supports, rather than unassisted quitting.
• Is varenicline safe for people with mental health conditions?
  Yes, but you should be closely monitored. Let your doctor know any changes in thoughts, mood, or behaviour.