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Manufacturer: PFIZER MANUFACTURING DEUTSCHLAND GmbH (Germany)
dosage form Tablets, film-coated white or almost white, kapsulovidnye, biconvex, engraved with «Pfizer» on one side and «CHX 0.5» — on the other. Tablets, film-coated light blue, kapsulovidnye, biconvex, engraved with «Pfizer»; «CHX 1.0» Composition 1 tab.
varenicline tartrate 850 mg, which corresponds to the content of varenicline 500 mcg
The composition of the film-coating: Opadry Blue 03B90547 (hypromellose, titanium dioxide, macrogol, aluminum lake based on indigo) Opadry clear YS-2-19114-A (hypromellose, triacetin). pharmachologic effect Drug for the treatment of nicotine addiction. Varenicline with high affinity and selectivity binds alfa4beta2 n-cholinergic receptors, for which it is a nicotine partial agonist, i.e. exhibits agonistic activity at the same time (but to a lesser degree than nicotine) and antagonism in the presence of nicotine.
Electrophysiological studies in vitro and in vivo studies neyrobiohimicheskie shown that varenicline binds alfa4beta2 n and stimulates cholinergic receptors, but to a much lesser extent than nicotine. Nicotine competitively binds to the same receptor site to which varenicline has higher affinity. Therefore, varenicline blocks nicotine’s ability to effectively stimulate alfa4beta2 receptors and activate the mesolimbic dopamine system — neuronal mechanism that underlies the implementation of the mechanisms of nicotine addiction (getting pleasure from smoking).
The effectiveness of varenicline as an agent for the treatment of nicotine addiction due to its partial agonism against alfa4beta2 nicotinic receptors, the binding of which reduces the craving for smoking and facilitates display of withdrawal (agonist activity) and simultaneously reduces the feeling of pleasure from smoking (antagonism in the presence of nicotine). Pharmacokinetics Varenicline is characterized by linear pharmacokinetics after a single (0.1-3 mg) and repeated (1-3 mg /) application.
After oral varenicline almost completely absorbed from the gastrointestinal tract. Cmax in plasma is normally achieved within 3-4 hours. High bioavailability and does not depend on time or meal ingestion. After multiple administration equilibrium state is achieved in healthy volunteers for 4 days.
Varenicline distributed in tissues, penetrates through the BBB and enters the brain. Binding to plasma proteins is low (bolee20%) and does not depend on the age and renal function.
Metabolism and excretion
Varenicline undergoes minimal metabolism. Excreted in the urine of 92% of the dose in unchanged form, at least 10% — in the form of metabolites. In urine found varenicline N-carbamoylglucuronide and gidroksivareniklin. The blood circulating in varenicline unchanged (91%) and as metabolites — N-carbamoylglucuronide varenicline and N-glyukozilvareniklin.
T1 / 2 is about 24 hours. The derivation is carried out mainly by the kidneys by glomerular filtration in combination with active tubular secretion.
Pharmacokinetics in special clinical situations
The pharmacokinetics of varenicline substantially independent of age, race, gender, smoking status, or concomitant therapy.
The pharmacokinetics of varenicline did not change in patients with mild renal impairment (creatinine clearance> 50 mL / min and? 80 mL / min). In patients with moderate renal impairment (creatinine clearance> 30 mL / min? 50 mL / min) AUC varenicline increased 1.5 times as compared with that in patients with normal renal function (creatinine clearance of> 80 ml / min). In patients with severe renal impairment (creatinine clearance <30 mL / min) AUC of varenicline increased 2.1 times. In patients with end-stage renal failure, varenicline was efficiently removed by hemodialysis.
Given the lack of pronounced metabolism in the liver, it is unlikely to alter the pharmacokinetics of varenicline in patients with impaired hepatic function. Dosage The recommended dose is 1 mg 2 times / day with a dose titration scheme 1-3 day 1 500 mg once a day, 4 to 7 days 500 mg 2 times a day, 8 day and before the end of treatment 1 mg 2 times day. The course of treatment is 12 weeks. The probability of a successful drug therapy for smoking cessation is increased in patients who are motivated to stop smoking, which provided additional advice and support. The drug is taken orally with or without food. The tablets should be swallowed whole and washed down with water. Varenicline treatment should be started 1 week before the selected date of the patient quitting smoking. When poor tolerability of side effects of varenicline dose can be reduced or temporarily continued administration. Patients who have successfully stopped smoking at the end of 12 weeks, an additional course of recommended treatment with a dose of 1 mg, 2 to 12 weeks. Patients who are unable to quit smoking during the initial 12-week course of treatment, or who relapse after treatment begins, should be encouraged to make another attempt, assuming that were established reasons for the failure of the first attempt, and measures taken to address them. For patients with mild renal impairment (creatinine clearance of> 50 mL / min? 80 mL / min) and moderate (CC> 30 ml / min? 50 mL / min) a dose adjustment is required. For patients with severe renal insufficiency (creatinine clearance <30 mL / min) the recommended dose of CHAMPIX is 1 mg 1 time / Treatment starts with a dose of 500 mg 1 time / that 3 days was increased to 1 mg 1 time / Patients with hepatic impairment correction dose is not required. Patients older correction dose is not required. Note that in these patients the likelihood of impaired renal function above, so it is advisable to carry out its assessment before starting treatment. Champiks® should not be given to children and adolescents up to 18 years, as information on the safety of the drug in this age group is not enough