Champix Tablets 1 mg 112 pcs
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Active ingredients
Varenicline
Composition
1 tab. varenicline tartrate 1.71 mg, which corresponds to the content of varenicline 1 mg. Excipients: microcrystalline cellulose - 125.
Pharmacological effect
A drug for the treatment of nicotine addiction. Varenicline with high affinity and selectivity binds to the α42 n-cholinergic receptors of the brain, for which it is both a partial agonist (but to a lesser extent than nicotine) and an antagonist in the presence of nicotine. In vitro electrophysiological studies and in vivo neurobiochemical studies have shown that varenicline binds to α42 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 α42 n-cholinergic receptors and activate the mesolimbic dopamine system - the neuronal mechanism that underlies the implementation of mechanisms for the formation of nicotine addiction (smoking pleasure). The effectiveness of varenicline as a treatment for nicotine addiction is due to its partial agonism against α42 n-cholinergic receptors, the binding of which reduces the craving for smoking and facilitates the manifestation of withdrawal syndrome and at the same time leads to a decrease in the feeling of pleasure from smoking (antagonism in the presence of nicotine). In two placebo-controlled, double-blind clinical trials that studied the efficacy of varenicline and bupropion, varenicline demonstrated a statistically significant advantage. During active treatment, the craving for smoking and the manifestation of withdrawal syndrome were significantly reduced in patients randomly assigned to the varenicline group, compared with placebo. Varenicline also significantly reduced the effects of reinforcement that occur during smoking, which can reinforce the smoking habit in patients who smoke during treatment, compared with placebo. The effect of varenicline on craving for smoking, withdrawal syndrome and the effects of reinforcement were not evaluated during follow-up, when medication was not administered.A placebo-controlled blind clinical trial demonstrated the effectiveness of an additional 12 weeks of varenicline therapy for smoking abstinence compared with placebo. Patients who are unwilling or unable to set a goal to quit smoking within 1-2 weeks can be offered to start treatment, with the possibility to choose their own cessation date of smoking within 5 weeks. Patients who had previously attempted to quit smoking with varenicline and who had received re-treatment with varenicline had the best level of confirmed persistent abstinence compared with placebo. In a placebo-controlled, double-blind clinical trial in patients who were unable or unwilling to quit for 4 weeks, but those wishing to gradually reduce smoking for 12 weeks before quitting were confirmed a higher level of persistent abstinence compared with placebo. When using the drug varenicline in patients with chronic obstructive pulmonary diseases, there were no differences in the safety profile compared with healthy patients.
Pharmacokinetics
Absorption: 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. The drug is almost completely absorbed after ingestion and has a high systemic bioavailability, not associated with food intake and time of admission during the day. After a single dose in a dose of 0.1 mg to 3 mg or repeated doses of 1 mg / day to 3 mg / day, the pharmacokinetics of varenicline were linear. Distribution: Varenicline is distributed in tissues and penetrates through the BBB, entering the brain. Plasma protein binding is low (≤ 20%) and does not depend on age and kidney function. Metabolism: Varenicline undergoes minimal biotransformation: 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-glucosyl queniclin were found. Withdrawal: T1 / 2 varenicline is about 24 hours.The excretion of varenicline by the kidneys is carried out mainly by glomerular filtration in combination with active tubular secretion. Pharmacokinetics in special clinical situations The pharmacokinetics of varenicline do not significantly depend on age, race, gender, smoking status, or concomitant therapy. The pharmacokinetics of varenicline did not change in patients with mild renal impairment (CC> 50 ml / min and ≤ 80 ml / min). In patients with moderate renal insufficiency (CC> 30 ml / min and ≤ 50 ml / min), the vUC Alicin AUC increased 1.5 times as compared with patients with normal renal function (CC> 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. Given the lack of pronounced metabolism of varenicline in the liver, the pharmacokinetics of varenicline should not change in patients with impaired liver function. The pharmacokinetics of varenicline in the elderly with normal renal function (age from 65 to 75 years) does not change.
Indications
- nicotine addiction in adults.
Contraindications
- hypersensitivity to any component of the drug - end-stage renal failure - childhood and adolescence up to 18 years (not enough clinical data on the efficacy and safety of the drug in this age group) - pregnancy - lactation (breastfeeding).
Use during pregnancy and lactation
Adequate and strictly controlled studies on the safety of using Champix during pregnancy have not been conducted, therefore, the prescription of the drug is contraindicated. It is not known whether varenicline is excreted in human breast milk. If necessary, the use of the drug during lactation breastfeeding should be discontinued.
Dosage and administration
The likelihood of successful drug therapy for smoking cessation is increased in patients who are motivated to quit, who are provided with additional advice and support. Champiksy accept inside irrespective of meal. Tablets should be swallowed whole with water. Treatment with Champix should be started 1–2 weeks before the patient’s selected cessation date.Or, the patient may start taking the drug and stop smoking between the 8th and 35th days of treatment with Champix. The recommended dose is 1 mg 2 times / day with dose titration according to the scheme given in the table. Day of the drug dose 1-3 day 500 mcg 1 time / day 4-7 day 500 mcg 2 times / day from the 8th day - until the end of treatment 1 mg 2 times / day If the side effects of the drug Champiks are poorly tolerated, the dose can be reduced temporarily or constantly. The course of treatment is 12 weeks. Patients who have successfully stopped smoking by the end of the 12th week are advised to maintain an additional course of treatment with the drug at a dose of 1 mg 2 times / day for 12 weeks to maintain smoking cessation. For patients who are unable or unwilling to abruptly stop smoking, a gradual approach with varenicline therapy may be considered. In this case, smoking should be reduced within 12 weeks of therapy and quit smoking by the end of this period. After that, patients should take varenicline for another 12 weeks so that the total treatment period is 24 weeks. Patients who have the appropriate motivation, but who failed to stop smoking during the previous course of treatment with varenicline, or who have a relapse after treatment, should be recommended to make another attempt, provided that the reasons for the failure of the first attempt were established and measures were taken to eliminate. There is no data on the effectiveness of an additional 12-week course of therapy in patients who did not manage to quit smoking based on the results of the initial course of therapy or during a relapse of smoking. The risk of recurrence of smoking is increased in individuals who have recently completed therapy to stop smoking. In patients with a high risk of relapse, a gradual reduction in dose is possible. For patients with mild renal insufficiency (CC> 50 ml / min and ≤ 80 ml / min) and moderate severity (CC> 30 ml / min and ≤ 50 ml / min), dose adjustment is not required. In patients with moderate renal insufficiency who do not tolerate undesirable reactions to Champix, the daily dose may be reduced to 1 mg 1 time / day. For patients with severe renal failure (CC less than 30 ml / min), the recommended dose of Champix is 1 mg 1 time / day. Treatment begins with a dose of 500 mcg 1 time / day, which after 3 days is increased to 1 mg 1 time / day. Due to the lack of clinical data on the use of Champix in patients with end-stage renal disease, the drug is not recommended for such patients.Patients with impaired liver function dose adjustment is not required. Elderly patients dose adjustment is not required. In this category of patients, the likelihood of impaired renal function is higher, so it is advisable to assess it before starting treatment. Champiks should not be prescribed to children and adolescents under the age of 18, because there is not enough information about the safety of the drug in this age group.
Side effects
Reactions associated with smoking cessation (nicotine withdrawal syndrome), with or without therapy with Champix: decrease in mood and dysphoria, insomnia, irritability, displeasure and anger, anxiety, impaired concentration, motor anxiety, decrease in heart rate, increased appetite or increase body mass, possible exacerbation of concomitant mental disorders. Neither in the development of schemes for clinical studies of Champics, nor in the analysis of their results, attempts were made to distinguish between adverse events associated with the use of the investigational drug and adverse reactions, possibly related to nicotine withdrawal 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 sex of the patient. In patients who received Champumps at the recommended dose of 1 mg 2 times / day after the titration period, the most frequent reported adverse reactions were 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 frequency of interruption of therapy due to adverse events was 11.4% in the group receiving varenicline and 9.7% for the placebo group. The frequency of discontinuation of therapy due to the main adverse reactions in the group receiving varenicline and in the 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 often (10%); often (from 1% to less than 10%); infrequently (from 0.1% to less than 1%); rarely (from> 0.01% to less than 0.1%); very rarely (less than 0.01%); frequency unknown (cannot be determined based on available data). Infections: very often - nasopharyngitis; often - bronchitis, sinusitis; infrequently - fungal infections, viral infections.On the part of the metabolism: often - loss of appetite, increased appetite; infrequently - anorexia, polydipsia; frequency unknown hyperglycemia, diabetes mellitus. Mental disorders: very often - unusual dreams, insomnia; infrequently - panic reaction, bradifrenia, impaired thinking, mood swings; frequency unknown - somnambulism. From the nervous system: very often - a headache; often - drowsiness, dizziness, changes in taste, including reduced taste sensations; infrequently - tremor, impaired coordination, lethargy, dysarthria, hypertonus, motor restlessness, dysphoria, hypesthesia, apathy, increased libido, decreased libido; rarely - a violation of cerebral circulation. Since the cardiovascular system: infrequently - atrial fibrillation, palpitations, angina, tachycardia; frequency unknown - myocardial infarction. On the part of the organ of vision: infrequently - scotoma, discoloration of the sclera, pain in the eyeball, dilated pupils, photophobia, myopia, increased lacrimation, conjunctivitis. From the organ of hearing and vestibular apparatus: infrequently - tinnitus. On the part of the respiratory system: often - shortness of breath, cough; infrequently - upper respiratory tract infections, hoarseness of the voice, pain in the pharynx and larynx, irritation of the pharynx, congestion in the airways, congestion in the paranasal sinuses, exudation in the nasopharynx, rhinorrhea, snoring, dysphonia, allergic rhinitis. On the part of the digestive system: very often - nausea; often - vomiting, constipation, diarrhea, bloating, stomach discomfort, dyspepsia, flatulence, dryness of the oral mucosa, gastroesophageal reflux disease, abdominal pain, toothache; infrequently - vomiting with blood, blood in the stool, gastritis, intestinal disorders, abnormal stool, belching, aphthous stomatitis, sore gums, furred tongue. On the part of the skin and subcutaneous tissues: often - a rash, itchy skin; infrequently - generalized rash, erythema, acne, hyperhidrosis, increased sweating at night. From the musculoskeletal system: often - arthralgia, myalgia, back pain; infrequently - stiffness of the joints, muscle spasms, costochondritis. From the urinary system: infrequently - glucosuria, nocturia, polyuria, pollakiuria.Reproductive system: Infrequently - menorrhagia, vaginal discharge, sexual dysfunction. General and local reactions: often - chest pain, fatigue; infrequently - chest discomfort, fever, feeling cold, asthenia, circadian rhythm sleep disorder, indisposition, cyst, flu-like syndrome. Research results: often - weight gain; infrequently - increased blood pressure, ST-segment depression on an ECG, a decrease in T-wave amplitude on an ECG, an increase in heart rate, blood flushes to the skin of the face, a decrease in platelet count, changes in liver function indicators, change in sperm, an increase in C-reactive protein, a decrease in blood calcium. The cessation of smoking with or without therapy is accompanied by the development of the nicotine withdrawal syndrome and the exacerbation of associated mental disorders. In the course of post-registration studies, patients who tried to quit smoking with the help of Champics indicated cases of depressive mood, agitation, behavioral or thinking disorders, anxiety, psychosis, hallucinations, mood fluctuations, aggressive behavior, suicidal attitudes and suicidal attempts. Since these phenomena are recorded according to the results of voluntary reporting to the population of an indefinite size, it is not always possible to accurately determine their frequency or causal relationship with the effect of the drug. Not all patients described in these reports had a history of mental disorders, and not all of them stopped smoking. The role of Champix in the development of the reactions described in these reports is unknown. Allergic reactions have also been reported - angioedema and rare but severe cases of skin reactions, including Stevens-Johnson syndrome and erythema multiforme.
Overdose
Cases of overdose of varenicline are not registered. Treatment: symptomatic treatment. 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
Clinically significant interaction of varenicline with other drugs have not been identified. Dose adjustment of varenicline or the drugs listed below with simultaneous use is not required.In vitro studies have shown that active secretion of varenicline through the kidneys is mediated by a transporter of human organic cations (OCT2). With simultaneous use with OCT2 inhibitors, dose adjustment of varenicline is not required, since no significant increase in systemic exposure of varenicline tartrate is expected. In vitro studies suggest that varenicline does not alter the pharmacokinetics of drugs that are metabolized by the action of isoenzymes of the cytochrome P450 system. Since clearance of varenicline is less than 10% due to metabolism, it is unlikely that substances affecting the activity of this enzyme system may affect the pharmacokinetics of varenicline, and therefore dose adjustment of the Champix preparation is not required. Varenicline at therapeutic concentrations does not inhibit the renal transport of proteins in humans. Therefore, varenicline should not affect the pharmacokinetics of drugs that are derived from renal secretion (in particular, metformin). Metformin Varenicline does not affect the pharmacokinetics of metformin. Metformin does not cause a change in the pharmacokinetics of varenicline. Cimetidine Cimetidine causes an increase in AUC of varenicline by 29% due to a decrease in its renal clearance. In patients with normal renal function or with mild to moderate severity, dose adjustment is not required. In patients with severe renal failure, the simultaneous use of cimetidine and varenicline should be avoided. Digoxin Varenicline does not affect the pharmacokinetics of digoxin in equilibrium. Warfarin Varenicline does not change the pharmacokinetics of warfarin and does not affect the prothrombin time (MHO). Smoking cessation alone can change the pharmacokinetics of warfarin. Alcohol Data on the simultaneous use of varenicline and alcohol are limited. In the course of post-registration use of varenicline, cases of increased toxic effects of alcohol were reported. The causal link between these cases and the use of varenicline has not been established. Use in combination with other anti-smoking agents Bupropion Varenicline does not affect the pharmacokinetics of Bupropion in equilibrium.Nicotine replacement therapy (NRT) With simultaneous use of varenicline and patches containing nicotine for 12 days, smokers showed a statistically significant reduction in mean systolic blood pressure (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 was higher with the combination therapy than with the same NRT. The safety and effectiveness of varenicline in combination with other anti-smoking agents have not been studied.
special instructions
Impact of smoking cessation on the body Physiological changes that occur after quitting smoking with or without treatment with Champix may alter the pharmacokinetics or pharmacodynamics of some drugs that may require dose adjustment (for example, theophylline, warfarin and insulin). Since smoking induces the isoenzyme CYP1A2, quitting smoking can lead to an increase in the concentration of substrates of this isoenzyme in the blood plasma. Neuropsychiatric disorders Analysis of clinical data showed the absence of an increased risk of serious neuropsychiatric disorders when using varenicline compared with placebo. In addition, the results of independent observational studies do not confirm the increased risk of serious neuropsychiatric disorders when using varenicline compared with nicotine replacement therapy or bupropion. During the post-registration use of the drug, there were reports of neuropsychiatric disorders, including behavioral or thinking disorders, anxiety, psychosis, mood swings, aggressive behavior, agitation, depressive mood, suicidal mood and suicidal behavior in patients trying to quit smoking with varenicline. Not all patients stopped smoking at the time of the listed symptoms and not all patients had mental disorders. The doctor should explain to patients receiving the drug in order to stop smoking, the possibility of the development of neuropsychiatric symptoms and take into account the need to gradually reduce the dose.Patients, their family members or their caretakers should be informed about the need to stop taking Champumps and seek immediate medical attention if they develop behavioral or thinking disorders, agitation or depressive mood, or if they develop suicidal feelings or behaviors that have not previously been characteristic of to the patient. In many cases, after the drug was discontinued, the listed symptoms disappeared, but sometimes the symptoms persisted. In this regard, further observation of patients is recommended until the symptoms disappear. Before starting treatment, you should find out if the patient previously had any mental disorders. It should also be borne in mind that depressive mood, in rare cases when combined with suicidal thoughts or attempts, may accompany quitting smoking. In addition, the process of quitting smoking, with or without pharmacotherapy, is usually associated with exacerbations of existing mental disorders (for example, depression). Clinical studies have been carried out on the use of varenicline in patients suffering from major depressive disorder without psychotic phenomena, receiving regular antidepressant therapy and / or in patients who have undergone a major depressive episode during the last 2 years and the therapy has been successful. According to the results of the psychiatric assessment of patients' condition, there were no differences between the groups of patients receiving varenicline and placebo. There was also no worsening of the course of depression during varenicline therapy in both groups of patients. When using varenicline in patients with mental illness in history, caution should be exercised. Cardiovascular diseases Meta-analysis of 15 clinical studies with a treatment duration of 12 weeks, including 7002 patients (4,190 patients took varenicline, 2,812 patients took placebo) was conducted to systematically evaluate cardiovascular safety of varenicline. When using Champics in patients with cardiovascular diseases, there was a slight increase in the incidence of complications of these diseases.Such complications more often developed in patients with already existing diseases of the cardiovascular system. Total mortality and mortality due to cardiovascular disease was less in patients receiving varenicline. Patients taking varenicline should inform their doctor about the appearance of new symptoms of cardiovascular disease or exacerbation of existing ones. Patients should immediately seek medical attention in the event of symptoms characteristic of myocardial infarction or stroke. Use in patients with stable schizophrenia or schizoaffective disorder There are limited data on the use of varenicline in patients with stable schizophrenia or schizoaffective disorder. When using varenicline in patients with mental illness in history, caution should be exercised. Epilepsy There is no data on the use of Champix in patients with epilepsy. Against the background of the use of the drug Champics, convulsions developed (in the absence of convulsions in history). In the presence of convulsions in history or other conditions that reduce the threshold of convulsive readiness, caution should be exercised when using Champix. The causal link between the use of varenicline and the development of seizures has not been established. Completion of therapy Completion of treatment with varenicline in 3% of patients was accompanied by increased irritability, smoking, depression and / or insomnia. Patients should be warned about such complications and discuss the possibility of reducing the dose. Angioedema and hypersensitivity reactions There have been reports of hypersensitivity reactions, including angioedema, in patients taking varenicline. The clinical symptoms of this complication include swelling of the face, mouth (tongue, lips, gums), neck (larynx and pharynx) and extremities. In addition, there are rare reports of the development of life-threatening angioedema, the treatment of which may require emergency medical intervention due to the danger of impaired respiratory function. Patients should immediately stop taking varenicline and contact their health care provider if any symptoms of hypersensitivity reaction develop.Severe Skin Reactions There are rare reports of severe life-threatening skin reactions, including Stevens-Johnson syndrome and erythema multiforme in patients taking varenicline. Since these reactions can be life-threatening, it is necessary to stop the use of the drug Champumps when the first signs of rash or skin reactions appear and immediately report this to your doctor. Impact on the ability to drive vehicles and control Champics mechanisms can cause dizziness and drowsiness, so patients are not recommended to drive a car, use sophisticated equipment or perform other potentially dangerous tasks before evaluating an individual response to the drug.