Champix pills 1 mg, 112 pcs.

Composition

1 tablet contains varenicline 1 mg

Pharmacological action

Drug for the treatment of nicotine addiction Champix. Varenicline binds with high affinity and selectivity to a4b2 neuronal nicotinic acetylcholine receptors, for which it is a partial agonist, i. e. it simultaneously exhibits agonism (but to a lesser extent than nicotine) and antagonism in the presence of nicotine.

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

Binding of Champix to these receptors reduces the craving for smoking and withdrawal syndrome (agonistic activity) and simultaneously reduces the effect of getting pleasure from smoking, followed by the formation of dependence by blocking the interaction of nicotine with α4β2 receptors (antagonistic activity).

Indications

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

Use during pregnancy and lactation

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

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

Contraindications

• Individual sensitivity to the components of the drug.
• Champix should not be used during pregnancy and lactation.
• The drug is not recommended for use in children and adolescents under 18 years of age, as information on its safety and effectiveness in this age group is insufficient.

Side effects

Smoking cessation reactions (nicotine withdrawal syndrome), with or without Champix®therapy: decreased mood and dysphoria, insomnia, irritability, feelings of displeasure and anger, anxiety, impaired concentration, motor anxiety, decreased heart rate, increased appetite or weight gain, possibly exacerbation of concomitant mental disorders.

Neither during the development of clinical trials of Champix®, nor during the analysis of their results, attempts were made to distinguish between adverse events associated with the use of the study drug and adverse reactions, possibly related to nicotine withdrawal syndrome itself.

According to the results of clinical studies, adverse reactions usually appeared in the first week after the start of treatment, were usually mild or moderate, and their frequency did not depend on the age, race or gender of the patient.

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 in the early stages of therapy, was mild or moderate, and discontinuation of the drug was rarely required.

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

Determination of the frequency of adverse reactions: very common (≥10%); common (≥1% to 0.01% to

Infections: very often – nasopharyngitis; often-bronchitis, sinusitis; infrequently-fungal infections, viral infections.

From the side of metabolism: often-decreased appetite, increased appetite; infrequently – anorexia, polydipsia; frequency unknown-hyperglycemia, diabetes mellitus.

Mental disorders: very often-unusual dreams, insomnia; infrequently-panic reaction, bradyphrenia, impaired thinking, mood swings; frequency unknown-somnambulism.

Nervous system disorders: very often-headache; often-drowsiness, dizziness, changes in taste sensations, including a decrease in taste sensations; infrequently-tremor, impaired coordination, lethargy, dysarthria, hypertonus, motor restlessness, dysphoria, hypesthesia, apathy, increased libido, decreased libido; rarely – impaired cerebral circulation.

From the cardiovascular system: infrequently – atrial fibrillation, palpitation, angina, tachycardia; frequency unknown-myocardial infarction.

From the side of the senses: infrequently-scotoma, discoloration of the sclera, pain in the eyeball, dilated pupils, photophobia, myopia, increased lacrimation, conjunctivitis, tinnitus.

Respiratory system disorders: often – shortness of breath, cough; infrequently-upper respiratory tract infections, hoarseness of voice, pain in the pharynx and larynx, pharyngeal irritation, congestion in the airways, congestion in the paranasal sinuses, exudation in the nasopharynx, rhinorrhea, snoring, dysphonia, allergic rhinitis.

From the digestive system: very often – nausea; often – vomiting, constipation, diarrhea, bloating, stomach discomfort, dyspepsia, flatulence, dry oral mucosa, gastroesophageal reflux disease, abdominal pain, toothache; infrequently – vomiting with blood, blood admixture in the stool, gastritis, intestinal disorders, stool disorders, belching, aphthous stomatitis, painful gums, coated tongue, changes in liver function indicators.

Skin and subcutaneous tissue disorders: often-rash, pruritus of the skin; infrequently-generalized rash, erythema, acne, hyperhidrosis, increased sweating at night.

Musculoskeletal disorders: often-arthralgia, myalgia, back pain; infrequently-joint stiffness, muscle spasms, costochondritis.

From the urinary system: infrequently – glucosuria, nocturia, polyuria, pollakiuria.

From the side of the reproductive system: infrequently – menorrhagia, vaginal discharge, sexual dysfunction.

General reactions: often-chest pain, fatigue; infrequently-chest discomfort, fever, cold sensation, asthenia, circadian rhythm disturbance, malaise, cyst, flu-like syndrome.

Research results: often – an increase in body weight; infrequently-an increase in blood pressure, ST segment depression on the ECG, a decrease in the amplitude of the T wave on the ECG, an increase in heart rate, ” flushes ” of blood to the skin of the face, a decrease in the number of platelets, changes in sperm, an increase in the concentration of C-reactive protein, a decrease in the concentration of calcium in the blood.

Smoking cessation with or without therapy is accompanied by the development of nicotine withdrawal syndrome and exacerbation of concomitant mental disorders.

In post-marketing studies, patients attempting to quit smoking with Champix® reported cases of depressive mood, agitation, behavioral or thinking disorders, anxiety, psychosis, hallucinations, mood swings, aggressive behavior, suicidal ideation, and suicide attempts.

Since these events are recorded as a result of voluntary reporting by a population of indeterminate size, it is not always possible to accurately determine their frequency or causal relationship with the effect of the drug. Not all of the patients described in these reports had a history of psychiatric disorders, and not all of them had stopped smoking.

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

Interaction

There was no clinically significant interaction of varenicline with other drugs. No dose adjustment of varenicline or the drugs listed below is required for concomitant use.

In vitro studies indicate 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 no dose adjustment of Champix®is required.

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

Metformin

Varenicline does not affect the pharmacokinetics of metformin. Metformin does not alter the pharmacokinetics of varenicline.

Cimetidine

Cimetidine causes a 29% increase in varenicline AUC due to a decrease in its renal clearance.

Digoxin

Varenicline does not affect the pharmacokinetics of digoxin at steady state.

Warfarin

Varenicline does not alter the pharmacokinetics of warfarin and does not affect prothrombin time (MHO). Smoking cessation alone may lead to changes in the pharmacokinetics of warfarin.

Alcohol

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 at steady state.

Nicotine replacement therapy (NRT)

Concomitant use of varenicline and nicotine-containing patches for 12 days revealed a statistically significant decrease in mean systolic blood pressure (by 2.6 mm Hg) on the last day of the study.At the same time, the incidence of nausea, headache, vomiting, dizziness, dyspepsia, and fatigue with combination therapy was higher than with NRT alone.

The safety and efficacy of Champix in combination with other anti-smoking agents have not been studied.

How to take, course of administration and dosage

Anti-smoking medications are more effective if patients themselves seek to quit smoking and receive additional help and support.

Before prescribing the drug, the patient should determine the day of smoking cessation. The drug should be started 1-2 weeks before this date. At the beginning of treatment, the dose is titrated for 1 week according to the scheme

• 1-3 day-0.5 mg once a day
• 4-7 day-0.5 mg twice a day
• from 8 days to the end of treatment-1 mg twice a day

The recommended dose is 1 mg 2 times / day. If the patient does not tolerate the side effects of Champix, the dose can be temporarily or permanently reduced to 500 mcg 2 times / day.

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

The course of treatment is 12 weeks. For patients who have stopped smoking by the end of week 12, an additional course of treatment with the drug at a dose of 1 mg 2 times/day for 12 weeks may be performed.

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

When using anti-smoking agents, the risk of resuming smoking is increased immediately after the end of treatment. If this risk is high, then a gradual dose reduction is possible.

Overdose

No cases of varenicline overdose have been reported.

Treatment: conducting symptomatic therapy. Varenicline is eliminated by hemodialysis in patients with severe renal impairment, but there is no experience of using hemodialysis in overdose.

Special instructions

Effects of smoking cessation: Physiological changes associated with smoking cessation while taking Champix or without treatment may cause pharmacokinetic or pharmacodynamic disturbances in certain medications, which may require a change in their dose (for example, theophylline, warfarin and insulin). Smoking causes an increase in CYP1A2 activity, so stopping smoking can lead to an increase in plasma levels of CYP1A2 substrates. Smoking cessation with or without pharmacotherapy has been associated with an increase in psychiatric illnesses (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. Discontinuation of Champix after treatment was associated with increased irritability, smoking cravings, depression, and/or insomnia in 3% of patients.

The doctor should inform the patient about the possible occurrence of such reactions and consider the possibility of gradually reducing the dose.

Impact on the ability to drive and use machinery

Champix has a small or moderate impact on the ability to drive and use complex machinery. Champix can cause dizziness and drowsiness and, consequently, affect the ability to drive a car and use complex equipment. Patients are advised not to drive a car, use complex machinery, or perform other potentially dangerous tasks until they have assessed their response to the medication.

Form of production

Film-coated tablets

Storage conditions

At a temperature of 15-30 °C

Shelf life

2 years

Active ingredient

Vareniklin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Smoking Cessation

Weight

Weight: 60 gr.