Drug for the treatment of nicotine addiction varenicline. Varenicline with high affinity and selectivity binds α4β2 neuronal nicotinic acetylcholine receptors, for which it is a partial agonist, i.e., simultaneously exhibit agonism (but to a lesser extent than nicotine) and antagonism in the presence of nicotine.
Efficacy in treating nicotine addiction is interconnected with partial agonism varenicline against α4β2 nicotinic receptors.
Varenicline drug binding to these receptors can reduce the craving to smoke and withdrawal (agonist activity) and simultaneously reduces the effect of the pleasure of smoking, followed by blocking the formation of nicotine dependence interaction with α4β2 receptors (antagonist activity).
R-Pharm Germany GmbH, Germany
1 tablet contains 1 mg varenicline
The drug varenicline is applied in the form of anti-smoking in adults.
- Individual sensitivity to the drug.
- CHAMPIX should not be used during pregnancy and lactation.
- The drug is not recommended for children and adolescents at a dose of 18, as the information on its safety and efficacy in this age group are insufficient.
Reactions associated with smoking cessation (nicotine withdrawal), on the background of therapy with or without Champiks®: reduction in mood and dysphoria, insomnia, irritability, feeling of displeasure and anger, anxiety, impaired concentration, restlessness, decrease in heart rate, increased appetite or weight gain, possibly worsening of psychiatric comorbidity.
Neither the design of clinical trials schemes Champiks® preparation or during analysis of their results no attempt to differentiate adverse events related to study medication, and unwanted reactions may actually associated with nicotine withdrawal syndrome.
According to the results of clinical studies undesirable reactions usually appeared during the first week after initiation of treatment, were usually mild or moderate and their frequency is not dependent on age, race or sex of the patient.
Patients treated Champiks® at the recommended dose of 1 mg, 2 times / day after titration period, the most common of the adverse reactions were reported nausea (28.6%). In the majority of cases nausea occurred early in the treatment, expressed mild or moderate, discontinuation of the drug were required rarely.
The frequency of discontinuation due to adverse events was 11.4% in the group receiving varenicline and 9.7% for the placebo group. The frequency of discontinuation due to side reactions in the basic group receiving varenicline and placebo groups, 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%); frequently (≥1% of do0.01% to
Infections: very often – nasopharyngitis; often – bronchitis, sinusitis; infrequently – fungal infections, viral infections.
From a metabolism: often – decreased appetite, increased appetite; rarely – anorexia, polydipsia; the frequency is unknown – hyperglycemia, diabetes mellitus.
Psychiatric disorders: very common – abnormal dreams, insomnia; infrequently – a panic reaction, bradifreniya, thought disorder, mood swings; the frequency is unknown – somnambulism.
From the nervous system: very often – headache; often – drowsiness, dizziness, change in taste
sensations, including reduction of taste; infrequent – tremor, impaired coordination, lethargy, dysarthria, hypertonia, restlessness, dysphoria, hypoesthesia, lethargy, libido increased, libido; rarely – a violation
Cardio-vascular system: Infrequent – Atrial fibrillation, palpitations, angina pectoris, tachycardia; the frequency is unknown – myocardial infarction.
From the sensory organs: rarely – scotoma, change color of the sclera, pain in the eyeball, mydriasis, photophobia, myopia, increased lacrimation, conjunctivitis, tinnitus.
The respiratory system: often – shortness of breath, cough; infrequently – upper respiratory tract infection, hoarseness, sore throat and larynx, throat irritation, congestion in the airways congestion in the sinuses, exudation in the nasopharynx, rhinorrhea, snoring, dysphonia, allergic rhinitis.
From the digestive system: very often – nausea; often – vomiting, constipation, diarrhea, bloating, stomach discomfort, indigestion, flatulence, dryness of the oral mucosa, gastroesophageal reflux disease, abdominal pain, dental pain; rarely – vomiting of blood, the impurity of blood in the stool, gastritis, intestinal disorders, stools, belching, aphthous stomatitis, sore gums, coated tongue, changes in liver function tests.
Skin and subcutaneous tissue disorders: often – a rash, itching; rare – generalized rash, erythema, acne, rash, increased sweating at night.
On the part of the musculoskeletal system: often – arthralgia, myalgia, back pain; infrequently – joint stiffness, muscle spasm, costochondritis.
From the urinary system: rarely – Glycosuria, nocturia, polyuria, pollakiuria.
Reproductive system: Infrequent – menorrhagia, vaginal discharge, sexual dysfunction.
General reactions: often – pain in the chest, fatigue; infrequently – chest discomfort, fever, feeling cold, asthenia, circadian rhythm sleep disorder, malaise, cyst, flu-like symptoms.
The results of research: often – increase in body weight; infrequently – increase in blood pressure, ST segment depression on the ECG, reducing the amplitude of the T wave on an electrocardiogram, heart rate increase, “flushing” of blood to the skin of the face, reduction in platelet count, sperm change, increasing the concentration of C-reactive protein, decrease in calcium concentration in blood.
Quitting smoking during therapy with or without accompanied by the development of nicotine withdrawal symptoms and the exacerbation of psychiatric comorbidity.
During post-marketing studies in patients trying to quit smoking with the help of Champiks® drug cases were registered depressive mood, agitation, behavioral or thinking, anxiety, psychosis, hallucinations, mood swings, aggressive behavior, suicidal thoughts and suicide attempts.
Since these events are recorded on the results of voluntary messages a population of uncertain size, it is not always possible to ascertain their frequency or a causal relationship with the drug. Not all patients described in these reports, we had a history of mental illness and not all of them have stopped smoking.
Role in the development of drug Champiks® reactions described in these messages is not known. Also registered cases of allergic reactions – angioedema and rare but severe cases of skin reactions, including Stevens-Johnson syndrome, erythema mnogformnuyu.
How to accept, acceptance rate and dosage
Anti-smoking are more effective if the patients themselves tend to quit and get additional help and support.
Before the appointment, patients should determine the day of cessation. The drug should start 1-2 weeks before this date. Early treatment is carried titration dose 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
- to 8 days before the end of treatment – 1 mg twice a day
The recommended dose is 1 mg, 2 times / day. If a patient can not tolerate the side effects of varenicline, the dose may be in temporarily or permanently reduced to 500 mg 2 times / day.
Tablets should be swallowed whole with water. The drug can be taken at meal time or between meals.
The course of treatment is 12 weeks. For patients stop smoking the end of 12 weeks, an additional course of treatment can be conducted in the drug dose of 1 mg, 2 times / day for 12 weeks.
Information about the effectiveness of the additional 12 weeks of treatment in patients who have failed to quit smoking during the first year, and in patients who resumed smoking after completion of therapy, no.
In the application of anti-tobacco smoking increased the risk of renewed immediately after the completion of treatment. If the risk is high, it is possible a gradual reduction in dose.
At a temperature of 15-30 ° C
Clinically significant interactions with other drugs varenicline is not revealed. Correction dose of varenicline or the following preparations, while the application is required.
in vitro studies suggest that varenicline does not alter the pharmacokinetics of drugs which are metabolized by the action of cytochrome P450 isoenzymes. Since varenicline clearance less than 10% at the expense of metabolism, it is unlikely that a substance influencing the activity of the enzyme system, may affect the pharmacokinetics of varenicline, and therefore the correction required drug dose Champiks®ne.
Varenicline at therapeutic concentrations does not inhibit renal transport proteins in humans. Therefore, varenicline should not affect the pharmacokinetics of drugs which are output due to renal secretion (particularly metformin).
Varenicline did not affect the pharmacokinetics of metformin. Metformin does not cause the change in the pharmacokinetics of varenicline.
Cimetidine causes an increase in AUC of varenicline 29% by reducing its renal clearance.
Varenicline did not affect the pharmacokinetics of digoxin at steady state.
Varenicline did not alter the pharmacokinetics of warfarin, and does not affect the prothrombin time (MHO). Smoking cessation itself may result in changes in the pharmacokinetics of warfarin.
Data on concomitant use of alcohol and varenicline are limited.
Use in combination with other anti-smoking
Varenicline did not affect the pharmacokinetics of bupropion in the equilibrium state.
Nicotine replacement therapy (NRT)
With simultaneous application of varenicline and plasters containing nicotine for 12 days in smokers showed a statistically significant decrease in average systolic blood pressure (2.6 mm Hg) for the last day of the study. In this case, the incidence of nausea, headache, vomiting, dizziness, dyspepsia, and fatigue in the combination therapy was higher than that on the background of one of NRT.
Safety and efficacy of CHAMPIX in combination with other anti-smoking have not been studied.
failure effects from smoking: Physiological changes associated with smoking cessation in patients receiving varenicline or without treatment, may cause disturbances pharmacokinetics or pharmacodynamics of certain drugs, which may require changes in their dose (e.g., theophylline, warfarin and insulin). Smoking causes an increase in CYP1A2 activity, so stopping smoking can lead to increased levels of CYP1A2 substrates in the plasma.
Smoking Cessation in the background or without pharmacotherapy it was accompanied by an aggravation of psychiatric illness (eg depression). Caution should be exercised in patients with a history of psychiatric disorders. Patients should be warned about the possibility of aggravation of diseases in smoking cessation.
Experience in the application of varenicline in patients with epilepsy not. Cancel varenicline after treatment in 3% of patients accompanied by increased irritability, craving to smoke, depression and / or insomnia.
The physician should inform the patient about the possibility of such reactions and consider the possibility of gradually reducing the dose.
Effect on driving ability and use of machinery
Varenicline has a minor or moderate influence on the ability to drive and use complex technology. CHAMPIX may cause dizziness and somnolence and therefore affect the ability to drive and use complex technology. Patients are advised not to drive a car, use sophisticated technology or to perform other potentially dangerous tasks until they appreciate his reaction to the drug.
Pregnancy and lactation
There are no adequate and well-controlled studies on safety use of varenicline in pregnancy has not been finished, so the drug is contraindicated.
It is unknown whether varenicline is excreted in breast milk in humans. If necessary, use during lactation should stop breastfeeding.
Cases registered varenicline overdose.
Treatment: symptomatic therapy. Varenicline is output during hemodialysis in patients with severe renal impairment, but experience with hemodialysis overdose no.