Champix - instructions for use, reviews, analogs and formulations (tablets of 0.5 mg and 1 mg) of the drug for the treatment of nicotine dependence and reducing smoking cravings in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Champix. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Champix in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Champix in the presence of existing structural analogs. Use for the treatment of nicotine addiction and reduce smoking cravings in adults, children, as well as in pregnancy and lactation. Composition of the preparation.

Champix - drug for the treatment of nicotine addiction. Varenicline (active ingredient of Champix) with high affinity and selectivity binds to alpha4-beta2 n-cholinergic receptors, for which it is a partial nicotine agonist, i.e. simultaneously exhibits agonist activity (but to a lesser extent than nicotine) and antagonism in the presence of nicotine.

Electrophysiological studies and neurobiochemical studies have shown that varenicline binds to alpha4-beta2 n-cholinergic receptors and stimulates them, but to a much lesser extent than nicotine. Nicotine competitively binds to the same receptor site to which varenicline has a higher affinity. Thus, varenicline effectively blocks the ability of nicotine to stimulate alpha4-beta2 n-cholinergic receptors and activate the mesolimbic dopamine system, the neuronal mechanism that underlies the mechanisms of the formation of nicotine addiction (getting pleasure from smoking).

The efficacy of varenicline as a means for treating nicotine dependence is due to its partial agonism with respect to alpha4-beta2 n-cholinergic receptors,binding with them reduces the craving for smoking and facilitates the manifestation of withdrawal syndrome (agonist activity) and simultaneously leads to a decrease in the sense of pleasure from smoking (antagonism in the presence of nicotine).

Composition

Varenicline tartrate + excipients.

Pharmacokinetics

The drug is almost completely absorbed after ingestion and has a high systemic bioavailability, not related to eating and taking time during the day. Varenicline is distributed in the tissues and penetrates the blood-brain barrier, entering the brain. The degree of binding to plasma proteins is low (<20%) and does not depend on the age and function of the kidneys. Varenicline undergoes minimal transformation: 92% of the dose is excreted by the kidneys unchanged and less than 10% - in the form of metabolites. Among the metabolites of varenicline in urine are found N-carbamyl glucuronide varenicline and hydroxyvarieniclin. In blood plasma, varenicline is circulated 91% unchanged. Among circulating metabolites, N-carbamylglucuronid varenicline and N-glucosylvarenicline have been found. The excretion of varenicline by the kidneys is carried out, mainly, by glomerular filtration in combination with active tubular secretion.The pharmacokinetics of varenicline are not significantly affected by age, race, sex, smoking status, or concomitant therapy.

Indications

• nicotinic dependence in adults.

Forms of release

Tablets coated with 0.5 mg and 1 mg.

There are no other dosage forms, whether it's a band-aid or a solution.

Instructions for use and reception scheme

The likelihood of successful smoking cessation therapy is increased in patients who are motivated to quit smoking, who receive additional counseling and support.

The drug is taken orally regardless of food intake. Tablets should be swallowed whole and washed down with water.

Treatment with Champix should be started 1 week before the date chosen by the patient for stopping smoking. The recommended dose is 1 mg 2 times a day with a dose titration according to the scheme given below:

• 1-3 day of taking the drug - a dosage of 500 mcg once a day;
• 4-7 day of taking the drug - 500 μg dosage twice a day;
• from the 8th day - until the end of treatment - a dosage of 1 mg 2 times a day.

If the side effects of Champix are poorly tolerated, the dose can be reduced temporarily or with further admission.

The course of treatment is 12 weeks. Patients who successfully stopped smoking by the end of the 12th week are recommended an additional course of treatment with the drug at a dose of 1 mg twice a day for 12 weeks.

Patients who do not manage to stop smoking during the initial 12-week course of treatment or who have a relapse after treatment should be encouraged to make another attempt, provided that the reasons for the failure of the first attempt have been established and steps have been taken to address them.

Patients with a dysfunction of the liver dosage adjustment is not required.

Side effect

• decreased mood;
• insomnia;
• irritability;
• feeling of displeasure and anger;
• anxiety;
• violation of concentration of attention;
• motor anxiety;
• decreased heart rate;
• increased appetite or weight gain;
• possibly exacerbation of concomitant mental disorders;
• nausea, vomiting;
• headache;
• unusual dreams;
• bronchitis;
• nasopharyngitis;
• sinusitis;
• fungal infections;
• viral infections;
• anorexia;
• decreased appetite;
• polydipsia;
• drowsiness;
• dizziness;
• panic reaction;
• violation of thinking;
• mood swings;
• increased blood pressure;
• increased heart rate;
• atrial fibrillation;
• palpitation;
• change in sclera color;
• pain in the eyeball;
• dilated pupils;
• myopia;
• noise in ears;
• decreased taste sensations;
• dyspnea;
• cough;
• hoarseness of voice;
• pain in the pharynx and larynx;
• irritation of pharynx;
• congestion in the respiratory tract;
• snore;
• constipation;
• diarrhea;
• bloating;
• dyspepsia;
• flatulence;
• vomiting with blood;
• an admixture of blood in the stool;
• gastritis;
• eructation;
• aphthous stomatitis;
• soreness of the gums;
• generalized rash;
• erythema;
• acne;
• hyperhidrosis;
• increased sweating at night;
• joint stiffness;
• muscle spasms;
• chest pain;
• Glucosuria, nocturia, polyuria;
• menorrhagia;
• vaginal discharge;
• sexual dysfunction;
• increased libido;
• decreased libido;
• change of sperm;
• fatigue;
• fever;
• feeling cold;
• decrease in the number of platelets.

Contraindications

• terminal stage of renal failure;
• age to 18 years (not enough clinical data on the efficacy and safety of the drug in this age group);
• pregnancy;
• lactation period (breastfeeding);
• hypersensitivity to the components of the drug.

Application in pregnancy and lactation

Adequate and strictly controlled studies on the safety of Champix during pregnancy have not been carried out, so the purpose of the drug is contraindicated.

It is not known whether varenicline is excreted in human milk. If you need to use the drug during lactation, breastfeeding should be discontinued.

Application in elderly patients

For elderly patients, dose adjustment is not required. It should be borne in mind that in this category of patients the probability of renal dysfunction is higher, therefore it is advisable to assess it before starting treatment.

Use in children

Contraindicated in children and adolescents under the age of 18 years (not enough clinical data on the efficacy and safety of the drug in this age group).

special instructions

Physiological changes that occur after quitting with or without Champix treatment may alter the pharmacokinetics or pharmacodynamics of some drugs for which dose adjustment may be required (for example, for theophylline, Warfarin and insulin).

The completion of treatment with varenicline in 3% of patients was accompanied by increased irritability, cravings for smoking, depression and / or insomnia.

During the post-marketing use of the drug, there were reports of psycho-neurological disorders, including behavioral disorders, agitation, depressive mood, suicidal tendencies and suicidal behavior in patients who received Champix in order to quit smoking. The doctor should explain to patients receiving the drug the possibility of developing neuropsychiatric symptoms and the need for a gradual dose reduction. Patients, their families or caregivers should be informed of the need to stop taking Champix and seek immediate medical attention if there is a behavioral disorder, agitation or depressive mood that was not previously associated with the patient, and if suicidal mood or behavior occurs. Before the start of treatment, you should find out if the patient has had any mental disorders before.

Impact on the ability to drive vehicles and manage mechanisms

Champix may cause dizziness and drowsiness, so patients are not advised to drive, use complicated equipment, or perform other potentially dangerous tasks before evaluating the individual response to the drug.

Drug Interactions

Clinically significant interaction of varenicline with other drugs has not been identified. Correction of a dose of varenicline or the drugs listed below with simultaneous application is not required.

Studies show that varenicline does not alter the pharmacokinetics of drugs that are metabolized by cytochrome P450 isoenzymes. Since varenicline clearance is less than 10% due to metabolism, it is unlikely that substances that affect the activity of this enzyme system can affect the pharmacokinetics of varenicline, and therefore a correction of the Ciampix dose is not required.

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

Varenicline does not affect the pharmacokinetics of metformin. Metformin does not cause a change in the pharmacokinetics of varenicline.

Varenicline did not cause a change in the pharmacokinetics of Digoxin in the equilibrium state.

Varenicline did not change the pharmacokinetics of warfarin and did not affect prothrombin time (MHO). Cessation of smoking itself can lead to a change in the pharmacokinetics of warfarin.

Application in combination with other anti-smoking agents

Bupropion

Varenicline did not cause a change in the pharmacokinetics of bupropion in the equilibrium state.

Nicotine replacement therapy (NRT)

With the simultaneous use of varenicline and patches containing nicotine, a significant decrease in mean systolic blood pressure (by 2.6 mm Hg) was observed in smokers on the last day of the study for 12 days. At the same time, the incidence of nausea, headache, vomiting, dizziness, dyspepsia, and fatigue was higher with combined therapy than with one NRT.

The safety and effectiveness of Champix in combination with other anti-tobacco drugs have not been studied.

Analogues of the drug Champix

Champix does not have structural analogs for the active substance.

Analogues on the therapeutic effect (drugs for the treatment of nicotine addiction and quitting):

• Maurer's original balm;
• Bioline Stop Smokin;
• Brizantine;
• Bullfighting;
• Mebikara tablets;
• Mebiks;
• Nicoretta;
• Piracetam;
• Polivit;
• Tabex;
• Three Vee Plus.

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