Champix, 1 mg 112 pcs

The drug for the treatment of nicotine addiction Champix. Varenicline binds with high affinity and selectivity to α4β2 neuronal nicotinic acetylcholine receptors, for which it is a partial agonist, i.e. it shows both agonism (but less than nicotine) and antagonism in the presence of nicotine.

The effectiveness of the drug in curing nicotine dependence is correlated with the partial agonism of varenicline against α4β2 nicotinic receptors.

The binding of Champix to these receptors allows reducing the craving and withdrawal syndrome (agonist activity) and at the same time leads to the reduction of the effect of pleasure from smoking with the subsequent formation of dependence by blockade of interaction of nicotine with α4β2 receptors (antagonist activity).

Indications

The drug Champix is used as an anti-smoking medication in adults.

Active ingredient

Composition

1 tablet contains varenicline 1 mg

How to take, the dosage

Tobacco cessation medications are more effective when patients are motivated to quit and receive additional help and support.

Patients must determine a day to stop smoking before prescribing the medication. The medication should be started 1-2 weeks before this date. At the beginning of treatment, the dose is titrated for 1 week according to the schedule

The recommended dose is 1 mg 2 times daily. If the patient cannot tolerate the side effects of Champix, the dose can be temporarily or permanently reduced to 500 mcg twice daily.

The tablet should be swallowed whole with water. The drug can be taken with meals or between meals.

The course of treatment is 12 weeks. For patients who stop smoking at the end of the 12th week, an additional 12 weeks of treatment with 1 mg twice daily may be given.

There is no data on the effectiveness of 12-week adjunctive therapy in patients who failed to quit smoking during the first course and in patients who resumed smoking after completing therapy.

When anti-smoking medications are used, the risk of smoking relapse is increased immediately after completion of treatment. If this risk is high, gradual dose reduction may be possible.

Interaction

Clinically significant interaction of varenicline with other drugs has not been revealed. There is no need to adjust the dose of varenicline or the following drugs during concomitant use.

In vitro studies indicate that varenicline does not change the pharmacokinetics of drugs that are metabolized by cytochrome P450 isoenzymes. Since clearance of varenicline is metabolized by less than 10%, it is unlikely that substances affecting the activity of this enzyme system may affect the pharmacokinetics of varenicline, in this connection no dose adjustment of the drug Champix® is required.

Varenicline at therapeutic concentrations does not inhibit renal protein transport in humans. Therefore, varenicline should not affect the pharmacokinetics of drugs that are excreted by renal secretion (particularly metformin).

Metformin

Varenicline has no effect on the pharmacokinetics of metformin. Metformin does not cause changes in the pharmacokinetics of varenicline.

Cimetidine

Cimetidine causes a 29% increase in the AUC of varenicline by reducing its renal clearance.

Digoxin

Varenicline does not affect the pharmacokinetics of digoxin in equilibrium.

Warfarin

Varenicline does not alter the pharmacokinetics of warfarin and has no effect on prothrombin time (MHO). Cessation of smoking alone may alter warfarin pharmacokinetics.

Alcohol

The data on concomitant use of varenicline and alcohol are limited.

Use in combination with other anti-smoking agents

Bupropion

Varenicline does not affect the pharmacokinetics of bupropion in equilibrium.

Nicotine replacement therapy (NRT)

The concomitant use of varenicline and nicotine patches for 12 days in smokers showed a statistically significant decrease in mean systolic BP (by 2.6 mm Hg) on the last day of the study. The incidence of nausea, headache, vomiting, dizziness, dyspepsia and fatigue on combination therapy was higher than on NHT alone.

The safety and effectiveness of Champix in combination with other tobacco control agents has not been studied.

Special Instructions

The effects of smoking cessation: Physiological changes associated with smoking cessation with or without treatment of Champix may cause disturbances in the pharmacokinetics or pharmacodynamics of some drugs, which may require changes in their doses (eg, theophylline, warfarin and insulin). Smoking causes increase in CYP1A2 activity, so smoking cessation may lead to increased plasma levels of CYP1A2 substrates.

Smoking cessation with or without pharmacotherapy was accompanied by exacerbation of psychiatric disorders (e.g., depression). Caution should be exercised in patients with a history of psychiatric disorders. Patients should be warned about the possibility of exacerbation of such diseases when stopping smoking.

There is no experience of using Champix in patients with epilepsy. Cancellation of CAMPIX after the end of treatment in 3% of patients was accompanied by increased irritability, craving for smoking, depression and/or insomnia.

The physician should inform the patient about the possible occurrence of these reactions and consider the possibility of gradual reduction of the dose.

Impact on the ability to drive and use machinery

Champix has a small to moderate effect on the ability to drive and use complex machinery. Ciampix may cause dizziness and drowsiness and may therefore affect the ability to drive and use complex machinery. Patients are advised not to drive, operate complex machinery, or perform other potentially dangerous tasks until they have evaluated their response to the medication.

Contraindications

Side effects

Reactions associated with smoking cessation (nicotine withdrawal syndrome), with or without CAMPIX® therapy: decreased mood and dysphoria, insomnia, irritability, frustration and anger, anxiety, impaired concentration, motor restlessness, decreased heart rate, increased appetite or increased body weight, possible exacerbation of concurrent psychiatric disorders.

Neither the design of the Chumpix® clinical trial designs nor the analysis of the results attempted to distinguish between adverse events associated with the use of the study drug and adverse reactions possibly associated with nicotine withdrawal itself.

In the clinical studies, adverse reactions generally occurred within the first week of treatment, were generally mild to moderate in severity, and their frequency was independent of patient age, race, or gender.

In patients receiving Champix® at the recommended dose of 1 mg twice daily after the titration period, the most frequent reported adverse reaction was nausea (28.6%). In most cases, nausea occurred early in therapy, was mild to moderate in severity, and discontinuation of the drug was rarely required.

The rate of therapy interruption due to adverse events was 11.4% in the group receiving varenicline and 9.7% for the placebo group. The frequency of discontinuation of therapy due to major adverse reactions in the varenicline group and the placebo group, respectively: nausea, 2.7% and 0.6%; headache, 0.6% and 1.0%; insomnia, 1.3% and 1.2%; and unusual dreams, 0.2% and 0.2%.

Frequency determination of adverse reactions: very common (≥10%); common (≥1% to 0.01% to

Infections: very common – nasopharyngitis; common – bronchitis, sinusitis; infrequent – fungal infections, viral infections.

Metabolic disorders: often – decreased appetite, increased appetite; infrequent – anorexia, polydipsia; frequency unknown – hyperglycemia, diabetes mellitus.

Mental disorders: very common – unusual dreams, insomnia; infrequent – panic reaction, bradyphrenia, impaired thinking, mood swings; frequency unknown – somnambulism.

Nervous system disorders: very common – headache; common – drowsiness, dizziness, changes in taste sensation, including decreased sense of taste; infrequent – tremor, loss of coordination, lethargy, dysarthria, hypertonicity, motor anxiety, dysphoria, hypoesthesia, apathy, libido increase, decreased libido; rarely – violation
of cerebral circulation.

Cardiovascular system: infrequent – atrial fibrillation, palpitations, angina pectoris, tachycardia; frequency unknown – myocardial infarction.

Senses: infrequent – scotoma, sclera color changes, pain in the eyeball, dilated pupils, photophobia, myopia, increased lacrimation, conjunctivitis, tinnitus.

Respiratory system disorders: frequently – shortness of breath, cough; infrequently – upper respiratory tract infections, hoarseness of voice, pain in the throat and larynx, pharyngeal irritation, airway congestion, nasal sinus congestion, exudation in the nasopharynx, rhinorrhea, snoring, dysphonia, allergic rhinitis.

Digestive system disorders: very common – nausea; common – vomiting, constipation, diarrhea, bloating, abdominal discomfort, dyspepsia, flatulence, dry oral mucosa, gastroesophageal reflux disease, abdominal pain, toothache; infrequent – vomiting with blood, bloody stool, gastritis, intestinal disorders, stool disorders, belching, aphthous stomatitis, sore gums, coated tongue, changes in liver function parameters.

Skin and subcutaneous tissue disorders: common – rash, itching of the skin; infrequent – generalized rash, erythema, acne, hyperhidrosis, increased sweating at night.

Muscular system: often – arthralgia, myalgia, back pain; infrequent – joint stiffness, muscle cramps, costochondritis.

Urinary system: infrequent – glucosuria, nycturia, polyuria, pollakiuria.

Reproductive system disorders: infrequent – menorrhagia, vaginal discharge, sexual dysfunction.

General reactions: frequent – chest pain, fatigue; infrequent – chest discomfort, fever, feeling of cold, asthenia, disturbance of circadian rhythm of sleep, malaise, cyst, flu-like syndrome.

Results: frequent – increase in body weight; infrequent – increased BP, ST segment depression on ECG, decreased amplitude of the T wave on ECG, increased HR, blood “flushes” to the skin of the face, decreased platelet count, changes in sperm, increased concentration of C-reactive protein, reduced concentration of calcium in the blood.

The cessation of smoking with or without therapy is accompanied by the development of nicotine withdrawal syndrome and exacerbation of related mental disorders.

In post-registration studies, patients who tried to quit smoking with Champix® had cases of depressed mood, agitation, disturbed behavior or thinking, anxiety, psychosis, hallucinations, mood swings, aggressive behavior, suicidal tendencies and suicide attempts.

Because the above phenomena are reported voluntarily by a population of uncertain size, it is not always possible to accurately determine their frequency or causal relationship to the effects of the drug. Not all of the patients described in these reports had a history of psychiatric disorders and not all of them have stopped smoking.

The role of Champix® in the reactions described in these reports is unknown. Allergic reactions such as angioedema and rare but severe skin reactions, including Stevens-Johnson syndrome and erythema multiforme, have also been reported.

Overdose

No cases of varenicline overdose have been reported.

Treatment: performance of symptomatic therapy. Varenicline is excreted by hemodialysis in patients with severe renal dysfunction, but there is no experience with hemodialysis in overdose.

Pregnancy use

There have been no adequately and strictly controlled studies on the safety of Champix in pregnancy, so the prescription of the drug is contraindicated.

It is unknown whether varenicline is excreted with breast milk in humans. If it is necessary to use the drug during lactation, breastfeeding should be stopped.