What is Cabrexxa? Active Ingredient and Primary Purpose
Cabrexxa is a brand name for the active substance varenicline tartrate. It is a prescription medication indicated as an aid to smoking cessation for adults who are committed to stopping smoking. Varenicline does not contain nicotine and works differently than nicotine replacement therapies (NRT). The primary purpose of Cabrexxa is to help relieve the intense cravings and uncomfortable withdrawal symptoms that occur when a person quits smoking. It also works to reduce the satisfaction or reward experienced from smoking, should a patient slip up during treatment. While the oral tablet formulation of varenicline (Cabrexxa) is used for smoking cessation, it is important to note that a different formulation, a nasal spray, is used for a completely separate condition: dry eye disease.
How Varenicline Aids in Quitting Smoking
Varenicline's efficacy in helping people quit smoking is due to its unique mechanism of action on the brain's reward pathways. It is a selective partial agonist that binds to and activates the α4β2 neuronal nicotinic acetylcholine receptors, the same receptors where nicotine binds. The dual action of varenicline works in two key ways:
- Relieves withdrawal symptoms: As a partial agonist, it mildly stimulates the receptors, causing a modest release of dopamine. This stimulation is enough to reduce the severity of cravings and withdrawal symptoms typically associated with quitting, such as irritability and restlessness.
- Blocks the effects of nicotine: Varenicline also prevents nicotine from tobacco smoke from binding to these receptors. This blocks the powerful, full activation of the reward system that nicotine normally provides, making smoking a less pleasurable and reinforcing experience.
This dual approach effectively manages withdrawal discomfort while making the act of smoking less enjoyable, significantly improving the chances of long-term abstinence.
Dosage and Administration for Cabrexxa
Treatment with Cabrexxa (varenicline) typically lasts for 12 weeks and should be started before the patient's quit date. A gradual dose increase is used to help minimize potential side effects, such as nausea.
General Information on Dosing
Starting with a lower dose and gradually increasing it helps the body adjust to the medication and can reduce the incidence of side effects like nausea. The tablets should be taken with a full glass of water after eating to reduce the likelihood of nausea. In cases where the initial 12-week course is successful, some doctors may recommend an additional 12 weeks of treatment to help prevent relapse. Always follow the specific dosing instructions provided by your healthcare provider and found on the medication packaging.
Important Warnings and Potential Side Effects
As with any medication, Cabrexxa can cause side effects. Patients should discuss their full medical history with a doctor before starting treatment, especially if they have a history of mental health disorders, heart disease, or seizures.
Common Side Effects
- Nausea and vomiting
- Insomnia and unusual or vivid dreams
- Headache
- Constipation, gas, and abdominal pain
- Changes in taste sensation
Serious Warnings and Precautions
- Neuropsychiatric symptoms: The FDA has issued safety warnings regarding serious mood or behavioral changes, including depression, hostility, agitation, and suicidal thoughts or actions. This can occur in individuals with or without a prior history of psychiatric illness. Patients should be monitored closely and should stop taking the medication and contact a healthcare provider immediately if these symptoms develop.
- Seizures: Seizures have been reported in patients taking varenicline. It should be used with caution in patients with a history of seizures.
- Cardiovascular risk: Patients with pre-existing heart or blood vessel problems may have a slightly higher risk of certain cardiovascular events. Any new or worsening symptoms like chest pain should be reported immediately.
- Accidental injury: Drowsiness, dizziness, or loss of consciousness can occur, potentially increasing the risk of accidents. Patients should be cautious when driving or operating machinery until they know how the medication affects them.
- Alcohol interaction: Varenicline can increase the intoxicating effects of alcohol, leading to unusual behavior or amnesia in some cases. It is recommended to reduce alcohol consumption while on this medication.
How Cabrexxa Compares to Other Smoking Cessation Aids
| Feature | Varenicline (Cabrexxa) | Bupropion (e.g., Zyban) | Nicotine Replacement Therapy (NRT) |
|---|---|---|---|
| Mechanism of Action | Partial agonist at α4β2 nicotinic acetylcholine receptors; blocks nicotine effects. | Atypical antidepressant; norepinephrine and dopamine reuptake inhibitor. | Delivers controlled doses of nicotine to reduce withdrawal symptoms. |
| Administration | Oral tablet, typically a 12-week course with dose adjustments. | Oral tablet, typically a course lasting several weeks. | Various forms: patches, gum, lozenges, inhalers, nasal sprays. |
| Effectiveness | Generally considered highly effective, often more so than bupropion and single NRT. Combination NRT may be comparable. | Effective in managing withdrawal symptoms, especially anxiety. Generally less effective than varenicline. | Doubles the chance of quitting compared to placebo. Combination NRT is more effective than single forms. |
| Common Side Effects | Nausea, insomnia, abnormal dreams, headache, gastrointestinal issues. | Dry mouth, insomnia, headache, restlessness. | Skin irritation (patches), hiccups (gum), mouth irritation. |
| Safety Considerations | Warnings for neuropsychiatric events, seizures, and cardiovascular risk. | Risk of seizures (~1 in 1500), caution with psychiatric history. | Relatively low risk; monitor heart rate and blood pressure. |
Combining Medication with Behavioral Support
All pharmacological smoking cessation aids, including Cabrexxa, are most effective when used as part of a comprehensive program that includes behavioral support. This can include counseling, educational materials, and a clear, set quit date. The combination addresses both the physical addiction and the psychological habits associated with smoking, significantly increasing the chances of success.
Conclusion
Cabrexxa, a brand name for varenicline, is a potent and effective prescription medication for adults seeking to quit smoking. By acting on the brain's nicotine receptors, it works to alleviate withdrawal symptoms while simultaneously diminishing the pleasure derived from cigarettes. While generally well-tolerated, it is associated with potential side effects and serious warnings, particularly regarding neuropsychiatric symptoms and cardiovascular health. For the best outcome, it should be used under the guidance of a healthcare professional as part of a structured smoking cessation program that includes ongoing support and counseling.
Visit Smokefree.gov for additional resources and support on quitting smoking{:target="_blank"}
