Table varenicline n / v 1mg film 112 pcs

$78.86

Table varenicline n / v 1mg film 112 pcs

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Description

Composition
Active substance:
0.5 mg 1 tablet contains: varenicline – 0.5 mg (as varenicline tartrate – 0.85 mg) 1 mg 1 tablet contains: varenicline – 1 mg (as varenicline tartrate 1.71 mg).
Excipients:
1 tablet contains 0.5 mg: microcrystalline cellulose – 62.57 mg calcium hydrogenphosphate – 33.33 mg, croscarmellose sodium – 2.00 mg colloidal silicon dioxide – 0.50 mg magnesium stearate – 0.75 mg; film coating: Opadry White YS-1-18202-A contains hypromellose, titanium dioxide and macrogol) – 4.00 mg; Opadry Clear YS-2-19114-A (contains hypromellose, and triacetin) – 0.50 mg.
1 mg 1 tablet contains: microcrystalline cellulose – 125.13 mg calcium hydrogen phosphate – 66.66 mg, croscarmellose sodium – 4.00 mg colloidal silica, 1.00 mg magnesium stearate – 1.50 mg; film coating: Opadry Clear YS-2-19114-A (contains hypromellose, and triacetin) – 1.00 mg; Opadry Blue 03B90547 (contains hypromellose, titanium dioxide, macrogol and aluminum lake based on indigo) – 8.00 mg.
Description:
dosage 0.5 mg Tablets: White or almost white kapsulovidnye biconcave tablets, film-coated, with «Pfizer» inscription on one side and «CHX 0.5» on the other side
1 mg dose tablets: light blue kapsulovidnye biconcave tablets, film-coated, with «Pfizer» inscription on one side and «CHX 1.0» on the other side.
Product form:
Tablets, film-coated with 0.5 mg or 1 mg
Primary packaging 11 0.5 mg dose tablets in a blister from Aklar® / PVC and aluminum foil, or PVC and aluminum foil 11 tablets dosage 0.5 mg tablets and 14 mg per dose 1 blister Aklar® / PVC and aluminum foil, or PVC and aluminum foil 14 or 28 tablets in dose of 1 mg of blister Aklar® / PVC and aluminum foil, or PVC and aluminum foil 56 0.5mg dosage tablets in a jar HDPE 56 1 mg dose tablets in a jar of high density polyethylene
Secondary Packaging 1 blister containing 11 tablets dosage of 0.5 mg and 1 blister containing 14 tablets dosage of 1 mg, in a combined cardboard box, thermally glued firmly to blisters and instructions for use.
Packaging for maintenance therapy 1 blister containing 11 tablets of 0.5 mg dose and 14-dose tablets 1 mg and 1 blister containing 28 tablets dosage of 1 mg, in a combined cardboard box, thermally glued firmly to blisters and instructions for use. 2 blisters, each containing 14 tablets of 1 mg dose, blister or 2 containing 28 tablets dosage of 1 mg, in a combined cardboard box, thermally glued firmly to blisters and instructions for use. 1, 2, 4 or 8 blisters, each containing 14 mg of 1-dose tablets in a cardboard box, together with instructions for use. 1 jar containing 56 tablets of 0.5 mg dose in a cardboard box, together with instructions for use. 1 jar containing 56 tablet dose of 1 mg in a cardboard box, together with instructions for use.
In the blister 11 containing the tablet (as a separate, and in general with 14 tablets dosage 1 mg) is empty cell contour for fixing a blister in a production machine.
When the package 1, 2, 4 or 8 blisters, each containing 14 tablets of 1 mg, the front side applied carton packs perforated line controls the first opening.
Tertiary package for full rate during 12 weeks of combination 1 carton containing one blister with 11 tablets of 0.5 mg dose and 14-dose tablets 1 mg and 1 blister with 28 tablets of 1 mg dose, and 2 combined cartons containing 2 blister with 28 tablets of 1 mg dose, in a cardboard box.
Contraindications
Hypersensitivity to any component of the preparation
Age 18 years (insufficient clinical data on the efficacy and safety of the drug in this age group)
Pregnancy and lactation
End-stage renal failure.
Dosage
1 mg
Indications
Nicotine dependence in adults.
Interaction with other drugs
No clinically relevant interactions have been identified varenicline with other drugs. Correction dose of varenicline or the following preparations, while the application is required.
In in vitro studies have shown that active secretion by the kidneys is mediated varenicline organic cation transporter Human (OST2). While the use of inhibitors OST2 not required dose correction varenicline, as not expected to significantly increase the systemic exposure of varenicline tartrate.
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 on the activity of cytochrome P450 isoenzymes, can affect the pharmacokinetics of varenicline, in connection with which the dose correction is not required.
Varenicline at therapeutic concentrations does not inhibit renal transport proteins in humans. Therefore, varenicline should not affect the pharmacokinetics of drugs which provides clearance due to renal secretion (in particular, metformin – see below.).
metformin
Varenicline did not affect the pharmacokinetics of metformin. Metformin does not cause changes in the pharmacokinetics of varenicline.
cimetidine
Cimetidine causes an increase in AUC of varenicline 29% by reducing its renal clearance. In patients with normal renal function or in patients with mild to moderate renal impairment dose adjustment is required. In patients with severe renal insufficiency should avoid the simultaneous use of cimetidine and varenicline.
Digoxin
Varenicline did not affect the pharmacokinetics of digoxin at steady state.
warfarin
Varenicline did not alter the pharmacokinetics of warfarin, and does not affect the prothrombin time (INR). Smoking cessation itself may result in changes in the pharmacokinetics of warfarin.
Alcohol
Data on concomitant use of alcohol and varenicline are limited. During post-marketing use of varenicline reported cases enhance the toxic effect of alcohol. A causal relationship between these cases and the use of varenicline has not been established.
Use in combination with other anti-smoking
bupropion
Varenicline did not affect the pharmacokinetics of bupropion in the equilibrium state.
Nicotine replacement therapy (NRT)
With simultaneous application of varenicline in smokers and plasters containing nicotine for 12 days it showed a statistically significant decrease in mean systolic blood pressure (2.6 mm Hg. V.) On the last study day. The frequency of nausea, headache, vomiting, dizziness, dyspepsia, and fatigue in the combination therapy was higher than that on the background of one of NRT.
The safety and efficacy of varenicline in combination with other anti-smoking have not been studied.
Overdose
Cases registered varenicline overdose.
Treatment: symptomatic.
Varenicline appear in hemodialysis patients with severe renal impairment, however the experience of the use of dialysis in overdose is not.
pharmachologic effect
Pharmacological group:
Nicotine addiction treatment facility.
Pharmacodynamics:
Varenicline with high affinity and selectivity alfa4beta2 binds to nicotinic acetylcholine receptors in the brain, in respect of which it is a partial agonist (but to a lesser extent than nicotine) and an antagonist in the presence of nicotine. Electrophysiological studies in vitro and neurochemical studies in vivo have shown that varenicline alfa4beta2 binds to nicotinic acetylcholine receptors and stimulating them, but to a much lesser extent than nicotine. Nicotine competitively binds to the same receptor site to which varenicline has higher affinity. Thus, varenicline effectively blocks the ability of nicotine to stimulate alfa4beta2 receptors and activate the mesolimbic dopamine system – neuronal mechanism that underlies the realization of the mechanisms of formation of nicotine addiction (smoking enjoyment). Efficacy of varenicline as a means for the treatment of nicotine dependence is due to its partial agonism against alfa4beta2 nicotinic receptor binding which reduces the craving to smoke and facilitates manifestation syndrome “cancel”, both resulting in reduced feelings of pleasure of smoking (antagonism in the presence of nicotine).
In two placebo-controlled, double-blind clinical studies investigating the effectiveness of varenicline and bupropion, varenicline demonstrated a statistically significant superiority. During the active treatment craving to smoke, and the manifestation of the syndrome of “cancellation” has been significantly reduced in patients randomized to varenicline group compared to placebo. Varenicline also significantly reduced the reinforcement effects caused by smoking, which can fix the smoking behavior in patients who smoke during treatment compared with placebo. Effect of varenicline on craving to smoke, a syndrome of “cancellation” and reinforcement effects were not assessed at follow-up, when drug treatment was conducted.
Placebo-controlled, blind clinical study has demonstrated the efficacy of an additional 12 weeks of varenicline therapy for abstinence from smoking compared with placebo.
Patients who are not willing or not able to set a target quit smoking within 1-2 weeks, we propose to start treatment with a choice of their own smoking cessation date within 5 weeks.
Patients who had previously tried to quit using varenicline and which repeatedly treated varenicline, had a better rate of confirmed resistant continence compared to placebo.
In a placebo-controlled, double-blind clinical trial in patients unable or unwilling to quit smoking within 4 weeks, but wish to gradually reduce smoking for 12 weeks before the throw has been confirmed a high level of resistant continence compared to placebo;
In applying the drug varenicline in patients with chronic obstructive pulmonary disease was no difference in the safety profile compared with healthy patients.
Pharmacokinetics:
Suction
The maximum concentration of varenicline (Cmax) in blood plasma, is usually achieved within 3-4 hours after ingestion. At the subsequent administration in healthy volunteers, the equilibrium state is reached within 4 days. The drug is almost completely absorbed after oral administration and has high systemic bioavailability not related to food intake and reception time during the day. After receiving a single dose of from 0.1 mg to 3 mg or repeated administration in a dose of 1 mg / day to 3 mg / day wore varenicline pharmacokinetics linear.
Distribution
Varenicline is distributed in tissues and penetrate the blood-brain barrier, entering the brain. The degree of binding to plasma proteins is low (
Metabolism
Varenicline undergoes minimal transformation 92% of the dose excreted by the kidneys in unchanged form and less than 10% – as metabolites. Among varenicline metabolites detected in urine N-karbamilglyukuronid gidroksivareniklin and varenicline. The plasma varenicline 91% circulates in an unmodified form. Among circulating metabolite detected N-karbamilglyukuronid varenicline and N-glyukozilvareniklin.
breeding
The half-life (T1 / 2) of varenicline is about 24 hours. Varenicline excretion by the kidneys is carried out mainly by the glomerular filtration in combination with active tubular secretion.
Pharmacokinetics in special groups
The pharmacokinetics of varenicline substantially independent of age, race, gender, smoking status or concomitant therapy.
Renal function
Pharmacokinetics varenicline not altered in patients with mild renal dysfunction (creatinine clearance of> 50 ml / min and 30 ml / min and 80 ml / min). In patients with severe renal impairment (creatinine clearance
Abnormal liver function
Given the lack of expressed in the liver metabolism of varenicline, the pharmacokinetics of varenicline should not be changed in patients with impaired its function.
elderly patients
The pharmacokinetics of varenicline in elderly people with normal renal function (aged 65 to 75 years) is not changed.
Pregnancy and breast-feeding
Due to the fact that adequate controlled trials of varenicline in pregnant women have not been conducted, the use of the drug during pregnancy is contraindicated.
Information on the allocation of varenicline in breast milk of women there. If necessary, use during lactation should stop breastfeeding.
Conditions of supply of pharmacies
On prescription.
side effects
Smoking cessation as a background therapy with Champiks® and without it, accompanied by a variety of symptoms, such as marked depressed mood and dysphoria, insomnia, irritability, feeling of displeasure and anger, anxiety, impaired concentration, restlessness, decrease heart rate, increased appetite or weight gain. Quitting smoking on background medical therapy with or without also accompanied by exacerbation of psychiatric comorbidity. However, neither in 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 adverse events probably associated with the fact syndrome “cancel” nicotine.
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 twice a day after a titration period, for the most frequent of the side effects were nausea (28.6%). In the majority of cases nausea occurred early in the treatment, expressed mild to moderate and rarely require discontinuation of the drug.
The frequency of discontinuation due to adverse events was 11.4% for the group of varenicline and 9.7% for the placebo group. The frequency of discontinuation of therapy due to major adverse reactions was as follows: nausea – 2.7% and 0.6% in the groups of varenicline and placebo, respectively; headache – 0.6% and 1.0%; insomnia – 1.3% and 1.2%; unusual dreams – 0.2% and 0.2%.
While taking Champiks® preparation the following reactions are also possible from the organs and systems (frequency estimation criteria: very frequent> 10%, frequently – by> 1%
special instructions
The impact of smoking cessation on the body
Physiological changes that occur after smoking cessation therapy varenicline or without it, can affect the pharmacokinetics or pharmacodynamics of certain drugs, which may require correction of the dose (for example, theophylline, warfarin and insulin). Since smoking induces isoenzyme CYP1A2, smoking cessation may result in increased concentrations of substrates of this isoenzyme in blood plasma.
neuropsychiatric disorders
Data analysis The clinical studies showed no increased risk of serious neuropsychiatric disorders in the application of varenicline compared with placebo. In addition, the results of independent observational studies do not confirm an increased risk of serious neuropsychiatric disorders in the application of varenicline compared with nicotine replacement therapy or bupropion therapy.
During post-marketing use of the drug, there were reports of the appearance of neuropsychiatric symptoms, including conduct disorder, or thinking, anxiety, psychosis, mood swings, aggressive behavior, agitation, depressed mood, suicidal thoughts and suicidal behavior in patients attempting to quit smoking with varenicline (see. See “Side effects”). Not all patients have stopped smoking at the time of occurrence of these symptoms and not all patients had previously observed mental impairment. The physician should explain to patients who tries to quit smoking with varenicline, the possibility of neuropsychiatric symptoms and the need to gradually reduce the dose. Patients, their families or caregivers should be advised of the need to stop taking varenicline and immediate treatment to the doctor if violations of conduct or thinking, agitation or depressive mood, and also in case of suicidal thoughts or suicidal behavior, which had not previously been characterized by this patient. In many cases, after the drug was observed the disappearance of these symptoms, but sometimes the symptoms persisted. In this context it recommended further monitoring of patients as long as symptoms persist. Prior to treatment patients should be advised to report any mental disorders that they had before. It should also be borne in mind that depressed mood, in rare cases, in conjunction with suicidal thoughts or attempts, can accompany smoking cessation. Кроме того, процесс отказа от курения, совместно с фармакотерапией или без нее, обычно связан с обострениями имеющихся психических расстройств (например, депрессии).
Проводились клинические исследования применения варениклина у пациентов, страдающих большим депрессивным расстройством без психотических явлений, получающих регулярную антидепрессивную терапию и/или у пациентов, перенесших большой депрессивный эпизод в течение последних двух лет, и терапия была успешна. Согласно результатам оценки состояния пациентов по психиатрическим шкалам не было отмечено различий между группами пациентов, получающих варениклин и плацебо. Также не было отмечено ухудшения течения депрессии во время терапии варениклином в обеих группах пациентов. При применении варениклина у пациентов с психическими заболеваниями в анамнезе следует соблюдать осторожность.
Cardiovascular diseases
Мета–анализ 15 клинических исследований с продолжительностью лечения >12 недель, включающих 7002 пациентов (4190 пациентов принимали варениклин, 2812 пациентов принимали плацебо) был проведен для систематической оценки сердечно-сосудистой безопасности варениклина.
При применении препарата Чампикс® у пациентов с сердечно-сосудистыми заболеваниями отмечалось некоторое увеличение частоты развития осложнения данных заболеваний. Такие осложнения чаще развивались у пациентов с уже имеющимися заболеваниями сердечно-сосудистой системы. Общая смертность и смертность по причине сердечно-сосудистых заболеваний была меньше у пациентов, получающих варениклин. Пациенты, принимающие варениклин, должны сообщить лечащему врачу о появлении новых симптомов сердечно-сосудистого заболевания или усугублении уже имеющихся. Пациентам следует немедленно обратиться за медицинской помощью в случае возникновения симптомов, характерных для инфаркта миокарда или инсульта.
Применение у пациентов со стабильной шизофренией или шизоаффективным расстройством
Имеются ограниченные данные о применении варениклина у пациентов со стабильной шизофренией или шизоаффективным расстройством. При применении варениклина у пациентов с психическими заболеваниями в анамнезе следует соблюдать осторожность.
Эпилепсия
Нет данных о применении препарата Чампикс® у пациентов с эпилепсией.
На фоне применения препарата Чампикс® развивались судороги (как при наличии, так и при отсутствии судорог в анамнезе). При наличии судорог в анамнезе или других состояний, снижающих порог судорожной готовности, необходимо соблюдать осторожность при применении препарата Чампикс®. Причинная связь между использованием варениклина и развитием судорог не была установлена.
Завершение терапии
Завершение лечения варениклином у 3 % пациентов сопровождалось повышением раздражительности, тягой к курению, депрессией и/или бессонницей. Пациентов следует предупредить о таких осложнениях и обсудить возможность снижения дозы.
Ангионевротический отек и реакции гиперчувствительности
Имеются сообщения о развитии реакций гиперчувствительности, включая ангионевротический отек, у пациентов, принимающих варениклин. Клинические симптомы этого осложнения включают отек лица, рта (языка, губ, десен), шеи (гортани и глотки) и конечностей. Кроме того, имеются редкие сообщения о развитии жизнеугрожающего ангионевротического отека, для лечения которого может потребоваться экстренное медицинское вмешательство в связи с опасностью нарушения дыхательной функции. Пациентам следует немедленно прекратить прием варениклина и обратиться к своему лечащему врачу при развитии любых симптомов реакций гиперчувствительности.
Severe skin reaction
Имеются редкие сообщения о тяжелых жизнеугрожающих кожных реакциях, включая синдром Стивенса-Джонсона и мультиформную эритему у пациентов, принимающих варениклин. Так как данные реакции могут быть жизнеугрожающими, необходимо прекратить применение препарата Чампикс® при появлении первых признаков сыпи или кожных реакций и немедленно сообщить об этом лечащему врачу.
Влияние на способность к управлению транспортными средствами и работу с механизмами
Учитывая, что варениклин может вызвать головокружение и сонливость, пациентам не рекомендуется управлять автомобилем, пользоваться сложной техникой или выполнять другие потенциально опасные задачи, пока они не оценят свою реакцию на лекарственный препарат.
Storage conditions
Хранить при температуре 15-30 С
Keep out of the reach of children.
Dosing and Administration
Вероятность успешной терапии препаратом для прекращения курения повышается у пациентов, мотивированных на отказ от курения, которым предоставляется дополнительная консультативная помощь и поддержка.
Чампикс® принимают внутрь, проглатывая таблетки целиком и запивая водой вне зависимости от приема пищи. Рекомендуемая доза препарата составляет 1 мг два раза в сутки с титрацией дозы по следующей схеме:
Дни 1-3 -0,5 мг один раз в сутки
Дни 4-7-0,5 мг два раза в сутки
День 8 до конца лечения-1 мг два раза в сутки
Лечение препаратом Чампикс® следует начинать за 1-2 недели до выбранной пациентом даты прекращения курения. Либо пациент может начать прием препарата и прекратить курение в период с 8-ого по 35-ый день лечения препаратом Чампикс®.
Если пациент не переносит нежелательные эффекты препарата Чампикс®, то дозу можно временно или постоянно снизить.
Лечение препаратом Чампикс® продолжают в течение 12 недель. Пациентам, успешно бросившим курить к концу 12-ой недели лечения, рекомендован дополнительный 12-недельный курс терапии варениклином в дозе 1 мг два раза в сутки для поддержания отказа от курения.
Для пациентов, которые не могут или не хотят резко отказываться от курения, может быть рассмотрен постепенный подход с терапией варениклином. В этом случае следует сокращать курение в течение 12 недель терапии и бросить курить к концу этого периода. После этого пациентам следует принимать варениклин еще 12 недель, чтобы общий период лечения составил 24 недели.
Пациентам, у которых имеется соответствующая мотивация, но которым не удалось бросить курить в ходе предыдущего курса лечения варениклином, или у которых после лечения наступает рецидив, рекомендуется предпринять еще одну попытку, при условии, что были установлены причины неудачи первой попытки, и предприняты меры для их устранения.
Данные об эффективности дополнительного 12-недельного курса терапии у пациентов, которым не удалось бросить курить по результатам первичного курса терапии или при рецидиве курения, отсутствуют. Риск рецидива курения повышен у лиц, недавно завершивших терапию с целью прекращения курения. У пациентов с высоким риском рецидива возможно постепенное снижение дозы (см. раздел «Особые указания»).
Renal function
Изменение дозы препарата Чампикс® у больных с легкой степенью нарушения функции почек (клиренс креатинина > 50 мл/мин и
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist

Additional information

Weight0.100 kg
Manufacturer

Pfizer

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