Role of Varenicline in the Treatment of Cocaine Use Disorder

What Is Varenicline?

Varenicline is a drug used as a smoking cessation medication that acts by blocking the pleasant effect of nicotine. This drug is the first approved nicotine substitute by the Food and Drug Administration. Varenicline is consumed orally. This drug is available in doses of 0.5 and 1 mg.

Varenicline is prescribed to be taken once a day initially, but when the quantity is elevated, it is advised to be taken twice a day.

How Is Varenicline Used?

Adults use Varenicline to overcome the habit of smoking. The medication should be used per the physician's instructions for desired results.

The following protocol can be followed while taking Varenicline while quitting smoking:

A planned date should be set to stop smoking, and Varenicline should be started one week before that date. During the initial days, a person may continue to smoke, but efforts must be taken to control the urge and quit smoking on the planned date. Varenicline helps individuals quit smoking within 8 to 35 days of the initiation of treatment. People who are excessively addicted to smoking and find it difficult to quit smoking should practice stopping it over 12 weeks with the help of Veratridine. Initially, the urge should be controlled, and the frequency should be reduced to half the initial number of cigarettes smoked. And the frequency should be tapered subsequently.

Varenicline benefits slowly, and it takes a few weeks to act; during the treatment, there is the possibility of smoking intermittently, but the medications should be taken on time without default. Varenicline should be continued for 12 weeks after smoking cessation to prevent relapse. People who continue to smoke even after 12 weeks on Varenicline should consult a physician to know why they cannot prevent smoking. When they start with the treatment, the manufacturer provides the user guide, but the doctor's instructions must be followed strictly.

What Is the Mechanism of Action of Varenicline?

By inhibiting the effects of nicotine on the brain, Varenicline aids in the cessation of smoking. The chemical that makes smoking feel good is called nicotine, and it may be found in cigarettes and other tobacco products.

This drug is a partial agonist of the nicotinic acetylcholine receptor (nAChR) subtype alpha4beta2. Nicotine stimulator is present in the presynaptic terminals in the nucleus accumbens of the brain, which causes the release of the neurotransmitter dopamine, which is associated with the feeling of pleasure. Varenicline can help suppress the desire to smoke cigarettes by blocking this feel-good hormone and controlling the withdrawal symptoms.

What Are the Precautions to Be Taken When on Varenicline?

Premedication Precautions:

• Inform the doctor or the pharmacist if there is any history of allergy to any medication.

• Inform about the medical history and the ongoing medications. The doctor needs to be careful to prevent drug interactions and any adverse effects due to the same; in some instances, doses of some drugs need to be altered.

• The doctor must be informed if previous attempts to quit smoking caused seizures or withdrawal symptoms.

• The females in the childbearing age group must inform the doctor if they are pregnant or planning to conceive.

• Before taking the medication, one must know that Varenicline makes one feel dizzy or unconscious. Therefore, activities like driving or swimming should be avoided while on Varenicline.

• When on Varenicline, alcohol or any addictive substance must be avoided as Varenicline increases its effect.

• Varenicline can elevate mood and cause behavioral changes and agitation or depression; the reason for these changes remains unknown; the doctor must be informed of any medical history of mental health disorders like depression or schizophrenia.

• Help and support guidelines must be taken while on treatment with Varenicline, as proper counseling during this period can help in smoking cessation.

What Are the Side Effects of Varenicline?

Some of the common side effects of Varenicline include:

• Nausea.

• Constipation.

• Diarrhea.

• Gas.

• Abdominal pain.

• Vomiting.

• Heartburn.

• Bad taste in the mouth.

• Dry mouth.

• Increased or decreased appetite.

• Toothache.

• Trouble falling asleep or staying asleep.

• Unusual dreams or nightmares.

• Headache.

• Lack of energy.

• Back, joint, or muscle pain.

• Abnormal menstrual cycles.

In some cases, people experience more severe side effects like:

• Swelling of the face, throat, tongue, lips, gums, eyes, neck, hands, arms, feet, ankles, or lower legs.

• Hoarseness.

• Difficulty swallowing or breathing.

• Rash.

• Swollen, red, peeling, or blistering skin.

• Blisters in the mouth.

• Pain, squeezing, or pressure in the chest.

• Pain or discomfort in one or both arms, back, neck, jaw, or stomach.

• Shortness of breath.

• Sweating.

• Nausea, vomiting, or lightheadedness with chest pain.

• Slow or difficult speech.

• Sudden weakness or numbness of an arm or leg, especially on one side of the body.

• Calf pain while walking.

• Seizures.

• Sleepwalking.

When a person experiences any of the above symptoms, immediate medical help must be taken, the physician must be informed, and Varenicline should be discontinued following the doctor's advice.

How Should Varenicline Be Stored?

Varenicline needs to be kept between 68 and 77 degrees Fahrenheit (20 and 25 degrees Celsius) at room temperature. In certain situations, as during transit, it may be exposed to temperatures ranging from 59 to 86 degrees Fahrenheit (15 to 30 degrees Celsius). Keep in a dry, cold environment.

What Are Other Uses of Varenicline?

Varenicline is used as a medication in the following cases:

• Eye infections, dry eyes.

• Smoking cessation.

What Is the Role of Varenicline in the Treatment of Cocaine Use Disorder?

Cocaine abuse is one of the severe problems these days, and limited treatment options make it even more complicated. Effects of Varenicline on patients with cocaine use disorders have been studied recently, and these studies reported mixed results. In many instances, the results in cases with psychotherapy were similar to those with patients with Varenicline treatment for 12 weeks. Thus, researchers do not support the use of Varenicline in cases with cocaine use disorder, considering its complex symptoms and effects.

When Is Varenicline Contraindicated?

• Hypersensitivity reactions.

• Patients with Steven Johnson syndrome.

• Erythema multiforme.

• Renal impairment.

• Mental health disorders.

• Epilepsy.

What Further Safety Measures Ought to Be Taken?

Prior to utilizing Varenicline,

• If individuals are allergic to Varenicline or any other drug, let their doctor and pharmacist know.

• Inform the doctor and pharmacist about any additional prescription and over-the-counter drugs, vitamins, dietary supplements, and herbal remedies individuals now take or intend to use.

• Inform the doctor if individuals had withdrawal symptoms when attempting to quit smoking in the past.

• Inform the doctor if one is nursing a baby, intends to get pregnant, or is already pregnant.

• Patients should be aware that Varenicline may cause them to feel sleepy, lightheaded, lose consciousness, or find it difficult to focus.

• When taking Varenicline, find out from the physician if drinking alcohol is safe to do. Varenicline can intensify alcohol's effects.

Conclusion:

Varenicline is an FDA-approved medication used as a smoking cessation aid and is administered orally. Varenicline is used in conjunction with education and counseling. It functions by preventing nicotine's pleasurable effects on the brain, which are caused by smoking. Varenicline is also studied for its uses in other conditions like cocaine abuse disorders, but the effectiveness of the drug has not been proven to date.