Champix
Champix: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Champix
ATX code: N07BA03
Active ingredient: varenicline (varenicline)
Producer: R-Pharm Germany (Germany), Pfizer Inc. (USA)
Description and photo update: 2018-21-11
Prices in pharmacies: from 1069 rubles.
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Champix is a drug used in the treatment of nicotine addiction.
Release form and composition
Champix's dosage form - film-coated tablets: capsule-shaped biconvex, on one side the inscription "Pfizer"; 0.5 mg each - white or almost white, the inscription on the other side - "CHX 0.5"; 1 mg each - light blue, the inscription on the other side - "CHX 1.0" [primary packaging: 11 pcs. (tab. 0.5 mg) in blisters; 11 pcs. (tab.0.5 mg) and 14 pcs. (tab. 1 mg) in blisters; 14 or 28 pcs. (tab. 1 mg) in blisters; 56 pcs. (tab. 0.5 mg) in high density polyethylene cans; 56 pcs. (tab. 1 mg) in a high density polyethylene jar; secondary packaging: 11 pcs. (tab.0.5 mg) in blisters + 14 pcs. (tab. 1 mg) in blisters, in a combined cardboard package 1 + 1 blister; packing for maintenance therapy: 11 pcs. (tab.0.5 mg) + 14 pcs. (tab. 1 mg) in blisters, and 28 pcs. (tab. 1 mg) in blisters,in a combined cardboard package 1 +1 and 1 blister; 14 or 28 pcs. (tab. 1 mg) in a combined cardboard package 2 blisters; 14 pcs. (tab. 1 mg) in blisters, in a cardboard box with a first opening control 1, 2, 4 or 8 blisters; 56 pcs. (tab. 500 or 1 mg) in cans, in a pack of cardboard 1 can; tertiary package (full course of therapy, designed for 12 weeks): 11 pcs. (tab.0.5 mg) + 14 pcs. (tab.1 mg) in a blister + 28 pcs. (tab. 1 mg) in a blister, in a combined cardboard package 1 + 1 + 1 blister; in a cardboard box, two combined cardboard packages + 2 blisters of 28 pcs. (tab. 1 mg)].(tab. 500 or 1 mg) in cans, in a pack of cardboard 1 can; tertiary package (full course of therapy, designed for 12 weeks): 11 pcs. (tab.0.5 mg) + 14 pcs. (tab.1 mg) in a blister + 28 pcs. (tab. 1 mg) in a blister, in a combined cardboard package 1 + 1 + 1 blister; in a carton pack, two combined carton packs + 2 blisters of 28 pcs. (tab. 1 mg)].(tab. 500 or 1 mg) in cans, in a pack of cardboard 1 can; tertiary package (full course of therapy, designed for 12 weeks): 11 pcs. (tab.0.5 mg) + 14 pcs. (tab.1 mg) in a blister + 28 pcs. (tab. 1 mg) in a blister, in a combined cardboard package 1 + 1 + 1 blister; in a carton pack, two combined carton packs + 2 blisters of 28 pcs. (tab. 1 mg)].
Composition of 1 Champix tablet:
- active substance: varenicline - 0.5 or 1 mg (in the form of varenicline tartrate - 0.85 or 1.71 mg);
- auxiliary components (0.5 / 1 mg): microcrystalline cellulose - 62.57 / 125.13 mg; calcium hydrogen phosphate - 33.33 / 66.66 mg; croscarmellose sodium - 2/4 mg; colloidal silicon dioxide - 0.5 / 1 mg; magnesium stearate - 0.75 / 1.5 mg;
- shell (0.5 mg): Opadry transparent YS-2-19114-A (hypromellose, triacetin) - 0.5 mg; Opadry white YS-1-18202-A (hypromellose, titanium dioxide, macrogol) - 4 mg;
- shell (1 mg): Opadry blue 03B90547 (aluminum varnish based on indigo carmine, hypromellose, macrogol, titanium dioxide) - 8 mg; Opadry clear YS-2-19114-A (hypromellose, triacetin) - 1 mg.
Pharmacological properties
Pharmacodynamics
Champix is intended for the treatment of nicotine addiction.
Varenicline has high affinity and selectivity, it binds to α4β2 n-cholinergic receptors in the brain, for which it is an antagonist in the presence of nicotine and, along with this, a partial agonist (but to a lesser extent than nicotine). Nicotine competitively binds to the same receptor site for which varenicline has a higher affinity.
As a result of the use of Champix, the craving for smoking decreases and the severity of the manifestations of the withdrawal syndrome is alleviated. At the same time, the feeling of pleasure from smoking decreases (antagonism in the presence of nicotine).
Clinical studies have shown that varenicline has a statistically significant advantage over bupropion. Varenicline also significantly reduces the reward effects that occur with smoking and may reinforce the smoking habit in patients who smoke during therapy.
Patients who are unwilling / unable to set a goal to quit smoking within 1–2 weeks may be asked to start therapy with a choice of their own smoking cessation date within the range of 5 weeks.
Patients who have previously tried to quit smoking with varenicline and who have received repeated varenicline treatment have a better rate of confirmed persistent abstinence compared to placebo.
Pharmacokinetics
C max (maximum concentration of the substance) in blood plasma is usually achieved 3-4 hours after ingestion of the drug. With continued therapy, the equilibrium state of varenicline develops over a period of four days. After oral administration Champix is absorbed almost completely. It has a high systemic bioavailability, which is not associated with the time of taking pills during the day and food intake. After a single use of 0.1–3 mg or repeated administration in a daily dose of 1–3 mg, the pharmacokinetic parameters are linear.
Varenicline is distributed in tissues, crosses the blood-brain barrier and enters the brain. Has a low binding to blood plasma proteins (≤ 20%), does not depend on the functional state of the kidneys and age.
The biotransformation of varenicline is minimal: 92% of the dose is excreted unchanged by the kidneys, in the form of metabolites - less than 10%. In the urine, hydroxyvarenicline and N-carbamylglucuronide varenicline were found among the metabolites. Varenicline in blood plasma circulates 91% unchanged, from circulating metabolites - N-glucosylvarenicline and N-carbamylglucuronide of varenicline.
T 1/2 (half-life) of varenicline is approximately 24 hours. Excretion by the kidneys is carried out mainly by glomerular filtration in combination with active tubular secretion.
Pharmacokinetic processes of varenicline do not significantly depend on smoking status, age, gender, race or concomitant therapy.
With an average degree of renal failure with creatinine clearance of 30-50 ml / min, AUC (area under the concentration-time curve) is 1.5 times higher than that in patients without renal dysfunction; in severe disorders with creatinine clearance <30 ml / min - 2.1 times. Varenicline in patients with end-stage renal disease is effectively removed by hemodialysis.
Indications for use
According to the instructions, Champix is prescribed for the treatment of nicotine addiction in adults.
Contraindications
- end stage renal failure;
- age up to 18 years;
- pregnancy and lactation;
- individual intolerance to Champix components.
Instructions for the use of Champix: method and dosage
Champix is intended for oral administration. The tablets must be swallowed whole with water. Food intake does not affect the effectiveness of the drug.
Patients who are motivated to quit smoking and who have additional support and advice are more likely to be successful in therapy.
Reception of Champix should be started 7-14 days before the date that the patient has chosen to quit smoking. You can also start therapy and stop smoking between 8 and 35 days of taking the drug.
Recommended scheme for using Champix tablets:
- 1-3 days: 0.5 mg once a day;
- 4-7 days: 2 times a day, 0.5 mg;
- starting from day 8 until the end of admission: 2 times a day, 1 mg.
If the patient does not tolerate the ongoing therapy, the dose can be temporarily or continuously reduced.
The duration of the course is 12 weeks. If the patient has successfully stopped smoking by the end of this period, it is recommended to continue therapy: 12 weeks, 1 mg 2 times a day.
It is also possible to gradually quit smoking. In this case, you need to reduce smoking within 12 weeks and quit smoking by the end of the specified period. After that it is recommended to continue therapy: 12 weeks, 1 mg 2 times a day.
In case of failure, if it was possible to establish its cause and measures were taken to eliminate it, you can repeat the course.
People who have recently completed smoking cessation therapy are at increased risk of smoking relapse. If there is a high risk of relapse, a gradual dose reduction may be appropriate
With moderate severity of renal failure in case of intolerance of adverse reactions, the frequency of administration can be reduced to 1 time per day. The same dosage regimen is indicated for patients with severe renal impairment.
Side effects
Nicotine withdrawal syndrome (disorders associated with smoking cessation), regardless of whether Champix was used or not: anxiety, dysphoria and decreased mood, irritability, insomnia, feelings of anger and displeasure, motor restlessness, impaired concentration, decreased heart rate, weight gain / increased appetite; concomitant mental disorders can also be exacerbated.
In most cases, the development of adverse reactions is observed in the first week of therapy. They are usually mild or moderate in nature, and their frequency does not depend on the gender, race or age of the patient.
During therapy with standard doses, nausea was most often noted (in 28.6% of cases). As a rule, it occurs in the early stages of treatment, has a mild or moderate severity and does not require the abolition of Champix.
Side effects that most often led to the cancellation of therapy: nausea, headache, insomnia, unusual dreams.
Possible adverse reactions (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare; with an unknown frequency):
- musculoskeletal system: often - myalgia, arthralgia, back pain; infrequently - muscle spasms, joint stiffness, intercostal neuralgia (costochondritis);
- nervous system: very often - headache; often - dizziness, drowsiness, changes in taste sensations, including their decrease; infrequently - motor restlessness, hypertonicity, dysphoria, dysarthria, tremor, impaired coordination, hypesthesia, decreased / increased libido, apathy, lethargy; rarely - violation of cerebral circulation;
- digestive system: very often - nausea; often - toothache, diarrhea, vomiting, constipation, bloating, gastroesophageal reflux disease, stomach discomfort, dyspepsia, flatulence, xerostomia, abdominal pain; infrequently - aphthous stomatitis, coated tongue, soreness of the gums, blood in the stool, gastritis, belching, stool disturbance, vomiting with blood, intestinal disorders;
- cardiovascular system: infrequently - angina pectoris, atrial fibrillation, tachycardia, palpitations; with an unknown frequency - myocardial infarction;
- respiratory system: often - cough, shortness of breath; infrequently - dysphonia, snoring, allergic rhinitis, congestion in the paranasal sinuses, irritation of the pharynx, upper respiratory tract infections, hoarseness, pain in the pharynx and larynx, rhinorrhea, congestion in the respiratory tract, exudation in the nasopharynx;
- infections: very often - nasopharyngitis; often - sinusitis, bronchitis; infrequently - viral / fungal infections;
- reproductive system: infrequently - vaginal discharge, menorrhagia, sexual dysfunction;
- urinary system: infrequently - pollakiuria, nocturia, glucosuria, polyuria;
- psyche: very often - insomnia, unusual dreams; infrequently - bradyphrenia, panic reaction, mood swings, impaired thinking; with an unknown frequency - somnambulism;
- metabolism: often - increased / decreased appetite; infrequently - polydipsia, anorexia; with an unknown frequency - diabetes mellitus, hyperglycemia;
- organ of hearing and vision: infrequently - increased lacrimation, discoloration of the sclera, tinnitus, scotoma, pain in the eyeball, photophobia, dilated pupils, myopia, conjunctivitis;
- skin and subcutaneous tissues: often - itchy skin, rash; infrequently - increased sweating at night, hyperhidrosis, acne, generalized rash, erythema;
- laboratory tests: often - weight gain; infrequently - a decrease in the amplitude of the T wave on the electrocardiogram (ECG), depression of the ST segment on the ECG, a decrease in the number of platelets, an increase in the concentration of C-reactive protein, a change in sperm, an increase in blood pressure, an increase in heart rate, a change in liver function indicators, flushing of the skin a person, a decrease in the concentration of calcium in the blood;
- general disorders: often - fatigue, chest pain; infrequently - flu-like syndrome, feeling of coldness, chest discomfort, malaise, fever, disturbance of the circadian rhythm of sleep, asthenia, cyst.
Smoking cessation, regardless of whether Champix therapy was carried out, is accompanied by the appearance of a nicotine withdrawal syndrome and an exacerbation of concomitant mental disorders.
In the course of post-registration studies, when quitting smoking using Champix, the following adverse reactions were observed: agitation, depressed mood, thinking / behavior disorders, anxiety, psychosis, hallucinations, mood swings, aggressive behavior, suicidal attempts / mood. It is not possible to establish exactly the frequency of their occurrence or the causal relationship with the action of the drug. Not all patients who reported side effects had a history of mental illness, and not all of them quit smoking.
There is also information about the development of allergic reactions - angioedema and, in rare cases, skin reactions, including erythema multiforme and Stevens-Johnson syndrome.
Overdose
No cases of Champix overdose are known.
Varenicline in patients with severe renal impairment is excreted during hemodialysis, but there is no experience with hemodialysis in cases of overdose. If necessary, symptomatic therapy is performed.
special instructions
Smoking cessation with / without Champix leads to physiological changes affecting the pharmacokinetics or pharmacodynamics of certain drugs (in particular, theophylline, warfarin and insulin), which may require a dosage regimen correction. Smoking induces the isoenzyme CYP1A2, with smoking cessation it is possible to increase the plasma concentration of substrates of this isoenzyme in the blood.
During the period of therapy, the likelihood of the appearance of neuropsychiatric symptoms and the need for a gradual dose reduction should be taken into account. In the event of disturbances in thinking / behavior, agitation or depressive mood unusual for the patient, as well as in the development of suicidal behavior / mood, Champix is canceled. Often the above symptoms disappeared after discontinuation of therapy, but in some cases this did not happen. In this connection, until the complete disappearance of life-threatening disorders, medical supervision should be established for the condition of patients.
Before prescribing Champix, you need to find out if the patient has had any mental disorders before. In such cases, therapy should be carried out with caution.
In patients with cardiovascular diseases during the period of Champix use, there was a slight increase in the incidence of complications of such diseases. In cases of the onset of symptoms characteristic of a stroke or myocardial infarction, you should consult your doctor.
During therapy, there were cases of seizures (in the absence of a history of them). As a result, when prescribing Champix to patients with a history of seizures or in the presence of other conditions that reduce the threshold of convulsive readiness, care must be taken.
In 3% of patients, completion of the Champix therapy course was accompanied by an increase in irritability, cravings for smoking, insomnia and / or depression. Patients should be warned about such complications. Dose reduction may be required.
There is evidence of hypersensitivity reactions during treatment, including angioedema. Clinical symptoms of this complication include swelling of the face, mouth (lips, tongue, gums), neck (pharynx and larynx), and extremities. In addition, there is rare information on the occurrence of life-threatening angioedema. Due to the danger of impaired respiratory function, emergency medical attention may be required during its treatment. If any symptoms of hypersensitivity reactions appear, patients should immediately stop taking Champix and consult their doctor.
There are rare reports of serious life-threatening skin reactions, including Stevens-Johnson syndrome and erythema multiforme. When their first symptoms appear, therapy should be stopped immediately.
Influence on the ability to drive vehicles and complex mechanisms
Before assessing the individual response to Champix therapy, patients are advised to refuse to drive vehicles.
Application during pregnancy and lactation
Champix is not prescribed during pregnancy / breastfeeding.
Pediatric use
Champix is not prescribed to patients under 18 years of age, since there is only little experience of its use in this age group of patients.
With impaired renal function
Contraindication: end-stage renal failure.
Use in the elderly
When prescribing Champix tablets for elderly patients, it is necessary to take into account the high likelihood of impaired renal function, therefore, it is advisable to evaluate it before starting treatment.
Drug interactions
No clinically significant interaction of varenicline with other drugs has been identified. With combined use, dose adjustment is not required.
Possible interactions:
- cimetidine: varenicline AUC will increase significantly; in severe renal failure, the combination is recommended to be avoided;
- alcohol: its toxic effect may increase (causal relationship has not been established);
- patches with nicotine content: mean systolic pressure is significantly reduced; the likelihood of developing dyspepsia, nausea, dizziness, vomiting, headache increases.
Analogs
Champix analogues are: Tabex, Bupropion, Lobelin, Cytizin, Zyban, Mebikar, Gamibazin, Nikvitin, Nicorette, Nicotin USP, Nicotinell and others.
Terms and conditions of storage
Store at 15-30 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Champix
Reviews about Champix are mostly positive. Patients note that the drug helps to quit smoking, despite the fact that it is not always easily tolerated.
Of the shortcomings, they point to its high cost, the absence in many pharmacies, as well as the development in some cases of side effects, manifested most often in the form of nausea in the morning, weight gain.
Champix price in pharmacies
The approximate price for Champix is: for 14, 28 or 112 tablets of 1 mg: 1252-1373, 1252-1447 or 3129-3417 rubles; for a set of 11 tablets of 0.5 mg and 14 tablets of 1 mg: 1174-1356 rubles.
Champix: prices in online pharmacies
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Drug name Price Pharmacy |
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Champix 1mg + 0.5mg film-coated tablets set of tablets: 1mg N14 and 0.5mg N11 25 pcs. 1069 RUB Buy |
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Champix tablets p.p. 0.5mg No. 11 + 1mg 14 pcs. 1101 RUB Buy |
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Champix 1 mg film-coated tablets 28 pcs. 1174 RUB Buy |
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Champix tablets p.p. 1mg 28 pcs. 1208 RUB Buy |
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Champix 1 mg film-coated tablets 112 pcs. RUB 2739 Buy |
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Champix tablets p.p. 1mg 112 pcs. 3526 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
