Champix coated pills. 0.5 mg N10 + 1 mg N14
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Active ingredients
Varenicline
Release form
Uncoated Tablets
Composition
Active ingredient: varenicline Concentration of active substance (mg): 0, 5 mg and 1, 0 mg
Pharmacological effect
A remedy for the treatment of nicotine addiction. varenicline with high affinity and selectivity binds to α4β2 n-cholinergic receptors, for which it is a partial nicotine agonist, i.e. simultaneously exhibits agonistic activity (but to a lesser extent than nicotine) and antagonism in the presence of nicotine. Electrophysiological in vitro studies and neurobiochemical studies in vivo showed that varenicline binds to α4β2 n-cholinergic receptors and stimulates them, but to a much lesser extent than nicotine . nicotine is competitively bound to the same receptor site to which varenicline has a higher affinity. Thus, varenicline effectively blocks the ability of nicotine to stimulate the α4β2 n-cholinergic receptors and activate the mesolimbic dopamine system - the neuronal mechanism that underlies the implementation of mechanisms for the formation of nicotine addiction (enjoyment from smoking). in relation to α4β2 n-cholinergic receptors, the binding of which reduces the craving for smoking and facilitates the manifestation of withdrawal syndrome (ag onistic activity) and at the same time leads to a decrease in the feeling of pleasure from smoking (antagonism in the presence of nicotine).
Pharmacokinetics
Cmax in the blood plasma, as a rule, is achieved within 3-4 hours after ingestion. In subsequent doses in healthy volunteers, an equilibrium state was achieved within 4 days. Almost completely absorbed after ingestion and has a high systemic bioavailability, not associated with food intake and time taken during the day. After a single dose at a dose of 0.1 mg to 3 mg or repeated doses at a dose of 1 mg / day to 3 mg / day, the pharmacokinetics of varenicline were linear. Varenicline is distributed in the tissues and penetrates the BBB, entering the brain. Plasma protein binding is low (less than 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, N-carbamylglucuronide varenicline and hydroxyvarenicine were detected in the urine. In blood plasma, varenicline is 91% circulating unchanged.Among the circulating metabolites, n-carbamyl glucuronide varenicline and N-glucosylvarenicline were detected. T1 / 2 varenicline is about 24 hours. Kidney varenicline is eliminated mainly by glomerular filtration in combination with active tubular secretion. In patients with moderately marked renal insufficiency (QC) 30 ml / min and ≤ 50 ml / min) AUC of varenicline increased 1.5 times compared with that in patients with normal renal function (CC more than 80 ml / min). In patients with severe impaired renal function (CC less than 30 ml / min), the AUC of varenicline increased 2.1 times. In patients with end-stage renal failure, varenicline was effectively removed during hemodialysis.
Indications
Champix is used as an anti-smoking agent in adults.
Contraindications
Hypersensitivity to the active substance or any fillers.
Precautionary measures
Keep out of the reach of children.
Use during pregnancy and lactation
Contraindicated use during pregnancy and lactation (breastfeeding).
Dosage and administration
Anti-smoking remedies are more effective if patients themselves are trying to quit smoking and receive additional advice and support. Champix is used internally. The recommended dose of varenicline is 1 mg twice a day. It is titrated for the first week as follows: Days 1/3 - 0.5 mg once a dayDays 4/7 - 0.5 mg twice a dayDay 8 / end of treatment - 1 mg twice a day The patient should choose a cessation date. Treatment with Champix should be started 1–2 weeks before this date. If the patient does not tolerate the unwanted effects of Champix, the dose can be temporarily or permanently reduced. Champix pills should be swallowed whole and taken with water. Champix can be taken with or without food. Treatment with Champix is continued for 12 weeks. Patients who stop smoking for 12 weeks may receive an additional 12-week course of treatment with Champix at a dose of 1 mg twice a day. There is no information about the effectiveness of an additional 12-week course of treatment in patients who did not manage to quit smoking during the first course, and in patients who resumed smoking after completing the therapy. When using anti-smoking products, the risk of resuming smoking is increased immediately after completion of treatment. If this risk is high, a gradual reduction in dose is possible.Patients with renal insufficiency. Changing the dose in patients with lung (estimated creatinine clearance is more than 50 ml / min and less than 80 ml / min) and moderate (estimated creatinine clearance is more than 30 ml / min and less than 50 ml / min). Renal impairment is not required. In case of intolerable adverse reactions in patients with moderate renal dysfunction, the dose may be reduced to 1 mg once a day. In patients with severe impaired renal function (calculated creatinine clearance less than 30 ml / min), the recommended dose of Champix is 1 mg once a day. Treatment begins with a dose of 0.5 mg once a day, which after 3 days is increased to 1 mg once a day. Experience of using Champix in patients with end-stage renal disease is insufficient, therefore it is not recommended to prescribe such patients. Patients with impaired liver function Do not change the dose in patients with impaired liver function. Older people Do not change the dose in older people. Older people have a higher probability of reducing kidney function, so it is advisable to evaluate it before starting treatment. Children Chumps are not recommended to prescribe to children and adolescents in doses up to 18 years, since information about its safety and effectiveness in this age group is insufficient.
Side effects
The cessation of smoking 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; decrease in heart rate; increased appetite or weight gain. When designing or analyzing the results of Champix's research, no attempt was made to differentiate adverse events associated with treatment or cessation of nicotine exposure. In clinical studies, approximately 4,000 patients received Champix for up to 1 year (mean 84 days). Adverse reactions usually appeared in the first week after the start of treatment and, as a rule, were mild or moderate. The frequency of adverse events did not depend on age, race, or gender. Patients who received varenicline at the recommended dose of 1 mg twice a day after the initial titration most often experienced nausea (28.6%).In most cases, it appeared at the beginning of treatment, was easily or moderately severe, and rarely required cessation of therapy. Due to adverse events, 11.4% of the varenicline group patients and 9.7% of the placebo group patients stopped the treatment. The frequency of discontinuation due to major adverse reactions was as follows: nausea — 2.7% and 0.6%, respectively, headache — 0.6% and 1.0%, insomnia — 1.3% and 1.2%, and abnormal dreams — 0.2% and 0.2%. The table lists all adverse events whose frequency was higher than in the placebo group. They are grouped by system and frequency (very frequent (greater than 1/10), frequent (greater than 1/100 - less than 1/10), infrequent (greater than 1 / 1,000 to greater than 1/100), and rare (less than 1 / 10,000 to less than 1 / 1,000). In each a group of adverse events are arranged in order of decreasing severity. System / Adverse reactions Infections Frequent - Bronchitis, nasopharyngitis, sinusitis, fungal infections, viral infections Disorders of metabolism and nutrition Partial - Enhancement of appetite ItsDephracic - Panic reaction, bradyphrenia, impaired thinking, quick mood changes Neurological disorders Pets very frequent - Headache Frequently - Drowsiness, dizziness, dysgesia; libidoChanges on the part of the heartFrequent - Atrial fibrillation, palpitationsChanges on the part of the organ of visionFrequent - Scotome, discoloration of the sclera, eye pain, dilated pupils, photophobia, myopia, increased tearing Changes in the organ of hearing and vestibular apparatus. Frequent - Tinnitus. Changes in the respiratory system, chest and mediastinum. swelling of the sinuses, runoff of mucus on the back of the nasal cavity, nasal discharge, snoring Gastrointestinal disturbances Very frequent - Nausea zm, dry mouth Infrequent - Vomiting of blood, blood in the stool, gastritis,gastroesophageal reflux disease, abdominal pain, changes in bowel movements, altered stools, belching, aphthous stomatitis, pain in the gums, furred tongue. Changes in the skin and subcutaneous tissue. and connective tissue Infrequent - Joint stiffness, muscle spasms, pain in the chest wall, costochondritis Changes in the kidneys and urinary tract Spare - Glucosuria, nocturia, polyuria Changes in the reproductive of the cheekbone system and the mammary glands.Party - Menorrhagia, vaginal discharge, sexual dysfunctionGeneral and local reactionsFrequent - FatigueMarrow - Discomfort in the chest, chest pain, increased body temperature, cold feeling, asthenia, circadian rhythm sleep disturbances, malaise, cyst , depression of the ST segment, a decrease in the amplitude of the T wave, an increase in the heart rate, a change in liver function indicators, a decrease in the number of platelets, an increase in body weight, change of sperm, increase of C-reactive protein level, decrease of calcium level in blood
Overdose
No cases of overdose of varenicline were registered. Treatment: symptomatic. Varenicline is eliminated by hemodialysis in patients with severely impaired renal function, but there is no experience with hemodialysis in overdose.
Interaction with other drugs
Cimetidine causes a 29% increase in AUC of varenicline due to a decrease in its renal clearance. With simultaneous use of varenicline and patches containing nicotine, smokers showed a statistically significant decrease in mean systolic blood pressure (2.6 mm Hg) during the last 12 days. study day. At the same time, the incidence of nausea, headache, vomiting, dizziness, dyspepsia and fatigue was higher on the background of combined therapy than on the background of nicotine replacement therapy.
special instructions
The physiological changes that occur after quitting smoking with or without varenicline therapy may alter the pharmacokinetics or pharmacodynamics of certain drugs that may require dose adjustment (for example, for theophylline,warfarin and insulin). End of treatment with varenicline in 3% of patients was accompanied by increased irritability, smoking, depression and / or insomnia. During the post-registration use of the drug, there were reports of neuropsychiatric disorders, including behavioral disturbances, agitation, depressive mood, suicidal mood and suicidal behavior in patients who received varenicline for the purpose of stopping smoking. The effect on the ability to drive vehicles and control mechanismsVareniclin ozhet cause dizziness and somnolence, therefore patients are not recommended to drive vehicles and other potentially hazardous activities to assess individual response to varenicline.