Description overdue on 08/11/2014
- Latin name: Champix
- ATC code: N07BA03
- Active substance: Varenicline (Varenicline)
- Manufacturer: Pfizer Manufacturing Deutschland (Germany)
- Composition
- Product form
- Pharmacological action
- Pharmacokinetics and pharmacodynamics
- Indications
- Contraindications
- Side effects
- Instructions for use of varenicline (method and dosage)
- Overdose
- Cooperation
- Terms of sale
- Storage conditions
- Shelf life
- Cautions
- Analogs
- Babies
- During pregnancy (and lactation)
- Reviews
- Price, where to buy
Composition
The structure means the active ingredient varenicline included varenicline tartrate As well as additional ingredients - microcrystalline cellulose . Croscarmellose sodium . colloidal silica . calcium hydrogen phosphate . magnesium stearate .
Product form
Available in tablet form.
Tablets that contain 850 mg varenicline tartrate They have kapsulovidnuyu shape, white or nearly white. They biconvex film coated with, on the one hand - the engraving «Pfizer», on the other - «CHX 0.5".
Tablets that contain 1.71 mg varenicline tartrate They have kapsulovidnuyu shape, light blue color. They biconvex film coated with, on the one hand - the engraving «Pfizer», on the other - «CHX 1.0".
Packaged in blisters 11, 14 or 28 pieces as well as the banks of the polyethylene to 56 pieces.
Pharmacological action
The tablets are used for the treatment of nicotine dependence. Active substance Varenicline Entering the body, it binds to the α4β2 nicotinic acetylcholine receptor n, with respect to which it is partly agonist nicotine. Thus, there is a simultaneous agonist activity (its degree is smaller than nicotine) and antagonism in the presence of nicotine.
Therefore, varenicline blocks the ability of nicotine to stimulate α4β2 n-cholinergic receptors and suppresses its activity towards the mesolimbic dopamine system. This mechanism is the basis of dependence on nicotine, that is, the pleasure derived as a result of smoking.
Tablets smoking varenicline reduce cravings for tobacco smoking, as well as significantly improve the symptoms of withdrawal. At the same time the person taking this drug, gradually notes decreased sensation of pleasure from smoking.
Pharmacokinetics and pharmacodynamics
The highest level of concentration of active substance in plasma was about 3-4 hours after oral dosing of varenicline. After ingestion means almost completely absorbed, there is a high level of systemic bioavailability, which is not associated with the period of its reception throughout the day, with the use of in relation to meals.
After the preparation was passed once (dose from 0.1 mg to 3 mg) or after repeated administration or repeated administration in the same dose Champix linear pharmacokinetics observed varenicline.
The active substance is distributed in the body tissues, penetrates the blood-brain barrier and into the brain. There is a low degree of binding to plasma proteins - 20%.
About 92% in unchanged form excreted through the kidneys, less than 10% is allocated as metabolites. Half-life of varenicline is 24 hours.
No pharmacokinetics of varenicline depending on gender, age, race, and on whether the patient smokes, whether he is taking other medicines.
Indications
Champix is indicated for nicotine dependence in adults.
Contraindications
Do not take this remedy in such cases:
- high sensitivity to component varenicline;
- end stage renal failure ;
- patient age of 18 years;
- Pregnancy and lactation.
Side effects
If the treatment varenicline patient stops smoking, this process can be accompanied by various unpleasant symptoms. In particular, the possible manifestation of sleep problems, irritability, bad moods, feelings of displeasure, motor restlessness, increased appetite, weight gain. When quitting smoking may be aggravated by mental disorders present before. Also in the treatment of patients experienced depressed mood, behavioral disorders, cases of hypersensitivity. But all adverse events, primarily associated with quitting smoking, not the beginning of the drug therapy. As a rule, they were observed during the first week of treatment and were either mild or moderately severe.
In the treatment of varenicline in a dosage that is recommended, most patients reported manifestation of mild to moderate nausea. This is rarely required treatment withdrawal.
In addition, therapy with varenicline were observed such negative effects:
- Often - P Accelerating appetite , rarely - decreased appetite . anorexia .
- Often - display insomnia . unusual dreams , rarely - panic attacks . aphronia . unstable mood.
- Often - drowsiness . headache . dizziness , rarely - disorders in the coordination process . tremor . hypertension . dysphoria . restlessness . hypoesthesia . decreased sexual desire .
- Often - vomiting . constipation . diarrhea . nausea . dyspepsia Rarely - Symptoms gastritis . gastroesophageal reflux disease . stomach ache .
- Also, in rare cases, there may be heartbeat . infectious diseases . mydriasis . pain in the eyeball . myopia . increased lacrimation . cough . breathlessness . snoring . stagnation in the airways and in the paranasal sinuses . rash . acne . erythema . joint stiffness . muscle spasms . nocturia . glycosuria . polyuria . chest pain . asthenia . malaise and etc.
Instructions for use of varenicline (method and dosage)
Instructions on varenicline provides receive the drug inside While it should be necessarily drink water . The tool can be taken regardless of the use of food.
According to experts, more successful results of the therapy are those patients who are keen to give up the habit, and take medication for the scheme, which provides instructions for the use of varenicline.
Start drug therapy is necessary to provide one week prior to the day when the people decided to give up the habit. Recommended means of 1 mg taken twice a day, dividing the dose under the scheme:
1 through Day 3: 0, 1, 5 mg once a day; 4 through Day 7 - 0, 5 mg 2 times a day; starting from day 8 until the end of therapy is necessary to take 1 mg twice a day. If you notice any side effects the dose may be reduced for a while. How to take the drug in such a case, the doctor will tell in detail.
The treatment period lasts 12 weeks. If the patient to quit smoking end of the twelfth week, the possibility of an additional course of therapy means wherein it dose is 1 mg daily (in two divided doses) for another 12 weeks.
Those people who have not managed to get rid of the habit of smoking during 12 weeks of treatment, or those who have relapsed after treatment, can conduct retry treatment, but only if the cause of failure is installed and removed.
When severe renal impairment in a patient dose of varenicline reduced to 1 mg once a day. If abnormal liver function do not need to adjust the dose of the drug. CHAMPIX in the usual dose is also appointed by the elderly.
Overdose
No cases of overdose of varenicline. If necessary, symptomatic therapy. Withdrawal is carried out by means of varenicline Hemodialysis in people with severely impaired renal function. But the experience of an overdose of funds available.
Cooperation
No clinically significant interaction is determined by the active ingredient varenicline with other drugs. No need to adjust the dosage of the above drugs or varenicline at their simultaneous use.
At therapeutic doses, did not affect the varenicline transport proteins in humans. Therefore varenicline no effect on the pharmacokinetics means, a clearance which is due to renal secretion.
Simultaneous treatment of cimetidine is a growth AUC of varenicline by 29% due to the decrease in its renal clearance.
Pharmacokinetics AT arfarina while taking varenicline it does not change. Changes in the pharmacokinetics of warfarin itself can occur as a result of smoking cessation.
With simultaneous use of nicotine replacement therapy, such as patches with nicotine for 12 days there was a significant decrease in the average garden. It is also more common manifestation of side effects - nausea, vomiting, fatigue.
Terms of sale
Varenicline sold by prescription.
Storage conditions
It is to protect the drug from children, stored at temperatures between 15 and 30 ° C.
Shelf life
CHAMPIX can be stored for 2 years.
Cautions
When the manifestation of physiological changes in the body during treatment with Champix after quitting smoking may change the pharmacokinetics or pharmacodynamics of a number of drugs. In such a case, it may be necessary to correct dosage Theophylline . Insulin . Warfarin and other drugs.
If discontinuation of varenicline approximately 3% of people marked irritability, depression , Sleep problems, increase the urge to smoke.
Before starting treatment with a specialist should clearly explain to the patient about the possibility of manifestation of various neuropsychiatric symptoms. It is important to understand that the treatment of varenicline in humans can be broken behavior, there is depression. Before the treatment, be sure to tell your doctor about all neuropsychiatric manifestations, which occurred in a person before.
Due to the fact, while taking varenicline may experience drowsiness or dizziness, it is not recommended during therapy to drive vehicles and operate dangerous machinery. Before the start of such actions should be clearly aware of the body's response to the drug.
Analogs of varenicline
Nicorette
Tabeks
Pharmacies can be found a number of other medications that are used to get rid of nicotine addiction. These means are similar, but they contain other surfactants. This medication Tabeks . Lobeline . TABACUM Plus . Mebicar . Zyban . Gamibazin and etc.
Which is better: Tabeks or varenicline?
The preparation Tabeks It is composed of active substance cytisine . CHAMPIX - Varenicline . When receiving varenicline as Tabeks the treatment in the organism of the smoker, reactions similar to those that occur when exposed to nicotine. However, varenicline and nicotine are antagonists, so when smoking and while taking this drug in humans produces a feeling of aversion to tobacco. Varenicline is more modern means than Tabeks, although its cost is higher.
Babies
Not used for the treatment of children and adolescents under 18 years of age, as there is no data on the safety and efficacy of the drug for children and adolescents.
During pregnancy and lactation
Do not use the tool on any stage of pregnancy, as well as breastfeeding child.
Reviews of varenicline
Those patients who took varenicline means, leave feedback on the forums are different, but mostly positive. Many people taking these pills from smoking, were able to quickly get rid of this addiction. Under the influence of this means the urge to smoke disappears gradually and relatively quickly. Sometimes patients marked the manifestation of certain side effects, including nausea, irritability. However, the assessment ratings varenicline doctors largely positive, since in most cases the drug after ingestion rate indicated pronounced effect. However, in a mostly positive effect was observed in those cases when a person consciously sought to abandon such harmful habits like smoking.
Price varenicline where to buy
Price varenicline (500 mg, 1 mg, respectively, 11 and 14 pieces in a package) is from 1300 to 1400 rubles. CHAMPIX tablets from smoking (1 mg, 112 pieces) in St. Petersburg, you can buy an average of 3,200 rubles. Buy varenicline in Moscow can be at the same price, the cost may vary depending on sales.
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