Champix, 500 mcg+1 mg 11+14 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 related to the partial agonism of varenicline against α4β2 nicotinic receptors.

The binding of Champix to these receptors allows to decrease craving and withdrawal syndrome (agonist activity) and at the same time leads to the decrease 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

Smoking cessation

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

Active ingredient

Varenicline

Composition

Each tablet contains varenicline 0.5 mg and 1 mg (as varenicline tartrate 0.85 mg and 1.71 mg, respectively)

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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

• day 1-3 – 0.5 mg once daily
• Day 4-7 – 0.5 mg twice daily
• from day 8 until the end of treatment – 1 mg twice daily

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 Champix after treatment termination 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 such 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 hazardous tasks until they have evaluated their response to the medication.

Contraindications

• Individual sensitivity to the components of the drug.
• Champix should not be used during pregnancy and lactation.
• Champix is not recommended for children and adolescents in doses under 18 years of age, because there is insufficient information about its safety and efficacy in this age group.

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Side effects

Smoking cessation, with or without treatment, is accompanied by a variety of symptoms. For example, patients trying to quit smoking may experience dysphoria or depression; insomnia, irritability, frustration, or anger; anxiety; difficulty concentrating; restlessness; decreased heart rate; increased appetite or weight gain.

Listed below are all the adverse events that had a higher frequency than in the placebo group. Definition of frequency of adverse reactions: very frequent (>1/10), frequent (>1/100-1/1,000-1/10,000-

Infections: infrequent – bronchitis, nasopharyngitis, sinusitis, fungal infections, viral infections

Metabolic and nutrition disorders: frequent – increased appetite, infrequent – anorexia, decreased appetite, polydipsia

Psychiatric disorders: very frequent – abnormal dreams, insomnia, infrequent – panic reaction, bradyphrenia, thought disorders, rapid mood changes

Neurological disorders: very frequent – headache, frequent – somnolence, dizziness, dysgeusia; infrequent – tremor, impaired coordination, dysarthria, hypertonia, anxiety, dysphoria, hypoesthesia, decreased sense of taste, apathy, increased libido, decreased libido

Heart disorders: infrequent – Atrial fibrillation, palpitations

Sight: infrequent – Scotoma, sclera color changes, eye pain, dilated pupils, photophobia, myopia, increased lacrimation

Hearing and vestibular organ disorders: infrequent – Tinnitus

Respiratory system: infrequent – shortness of breath, cough, hoarseness of voice, pain in pharynx and larynx, pharyngeal irritation, airway edema, sinus swelling, mucus dripping down the back of the nasal cavity, nasal discharge, snoring

Gastrointestinal disorders: very frequent – nausea; frequent – vomiting, constipation, diarrhea, abdominal distension, stomach discomfort, dyspepsia, flatulence, dry mouth; infrequent – vomiting blood, bloody stool, gastritis, gastroesophageal reflux disease, abdominal pain, changes in defecation, altered stool, belching, aphthous stomatitis, gum pain, coated tongue: infrequent – generalized rash, erythema, itching, acne, hyperhidrosis, night sweats

Musculoskeletal and connective tissue disorders: infrequent – joint stiffness, muscle spasms, chest wall pain, costochondritis

Renal and urinary tract disorders: infrequent – glucosuria, nocturia, polyuria

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

General and local reactions: frequent – fatigue; infrequent – chest discomfort, chest pain, increased body temperature, cold sensation, asthenia, circadian sleep disturbances, malaise, cyst

Results: infrequent – increased blood pressure, ST-segment depression, decreased T-wave amplitude, increased heart rate, changes in liver function parameters, decreased platelet count, increased body weight, changes in semen, increased C-reactive protein levels, decreased blood calcium levels

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.

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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.