Champix pills, 500mcg 11pcs + 1mg 14pcs

Composition

Each tablet contains varenicline-0.5 mg and 1 mg (in the form of varenicline tartrate 0.85 mg and 1.71 mg, respectively)

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

Listed below are all the adverse events that were more frequent than in the placebo group. Determination of the 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 nutritional disorders: frequent-increased appetite, infrequent – anorexia, decreased appetite, polydipsia

Psychiatric disorders: very common-abnormal dreams, insomnia, infrequent-panic reaction, bradyphrenia, thinking disorders, rapid mood changes

Neurological disorders: very common – headache, frequent-drowsiness, dizziness, dysgesia; Infrequent-tremor, impaired coordination, dysarthria, hypertension, anxiety, dysphoria, hypoaesthesia, decreased taste sensation, apathy, increased libido, decreased libido

From the heart: infrequent – atrial fibrillation, palpitations

From the side of the organ of vision: infrequent-scotoma, discoloration of the sclera, pain in the eyes, dilated pupils, photophobia, myopia, increased lacrimation

From the side of the organ of hearing and vestibular apparatus: infrequent-Tinnitus

Respiratory system disorders:  infrequently – shortness of breath, cough, hoarseness, pain in the throat and throat, irritation of the throat, swelling of the Airways, swelling of the sinuses, mucus dripping at the back surface of the nasal cavity, nasal discharge, snoring

Gastrointestinal disorders: very often – nausea; often – vomiting, constipation, diarrhea, abdominal stretch, stomach discomfort, dyspepsia, flatulence, dry mouth; infrequent – vomiting blood, blood in the stools, gastritis, gastroesophageal reflux disease, abdominal pain, changes in bowel movements, changed the chair, burping, aphthous stomatitis, sore gums, coated tongue

Skin and subcutaneous tissue changes: infrequent-generalized rash, erythema, pruritus, acne, hyperhidrosis, night sweats

Musculoskeletal and connective tissue disorders:  infrequent-joint stiffness, muscle spasms, pain in the chest wall, costochondritis from the kidneys and urinary tract: infrequent-glucosuria, nocturia, polyuria

From the reproductive system: infrequent-menorrhagia, vaginal discharge, sexual dysfunction

General and local reactions: frequent-fatigue; infrequent-chest discomfort, chest pain, fever, feeling cold, asthenia, circadian rhythm disturbances, malaise, cyst

Study results: infrequent-increased blood pressure, ST-segment depression, decreased T wave amplitude, increased heart rate, changes in liver function indicators, decreased platelet count, increased body weight, changes in sperm, increased C-reactive protein levels, decreased blood calcium levels

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 use 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