SELINCRO 18MG PILLS

Release form, composition and packaging

Film Coated Tablets white, oval, biconvex, embossed "S" on one side.

Excipients: microcrystalline cellulose - 61.4 mg, anhydrous lactose - 60.683 mg, crospovidone type A - 4.5 mg, Magnesium stearate - 1.5 mg.

Shell composition: Opady OY-S-28849 white - 4.5 mg (hypromellose (5 mPa.s), macrogol 400, titanium dioxide (E171)).

Indications

- reduction of alcohol consumption in adult patients with alcohol dependence, who are at high risk of alcohol abuse (see the Pharmacodynamics section), in the absence of physical manifestations of withdrawal syndrome or the need for immediate detoxification.

Selincro is recommended to be used in combination with long-term psychosocial support aimed at maintaining adherence to treatment and reducing alcohol consumption.

Selincro is appointed after two weeks of observation of a patient with a continuing high risk of alcohol abuse.

Dosage and administration

During the initial visit, prior to the appointment of Selincro, the doctor needs to assess the patient’s clinical condition and the level of alcohol consumption (in his words). In cases where additional information is required, the patient is asked to record the level of alcohol consumption for approximately the next two weeks.For those patients who, during these two weeks, remained at a comparable level to the initial level of alcohol consumption, Selincro can be prescribed at the second visit.

Selincro recommended to use in combination with psychosocial support, aimed at maintaining adherence to treatment and reduce the level of alcohol consumption.

Selincro is not intended to achieve immediate abstinence from alcohol. Reducing alcohol consumption is an intermediate goal on the path to total abstinence.

Selincro applies as needed. The decision about taking the drug is made by the patient: on those days when, in his opinion, the likelihood of alcohol is high, 1-2 hours before the expected moment of taking 1 tab. Celinkro at a dose of 18 mg. If a patient starts taking alcohol without taking a pre-Selinkro pill, he needs to do it as quickly as possible.

The maximum daily dose of Selincro is 1 tab. Selincro can be taken regardless of the meal.

During clinical studies, the maximum improvement was observed during the first 4 weeks of therapy. The patient's response to treatment and the appropriateness of continuing pharmacotherapy should be evaluated regularly (for example, monthly). The doctor must constantly determine the patient's progress in reducing alcohol consumption, his general condition, adherence to therapy and the occurrence of side effects. The duration of the clinical studies of Selincro did not exceed 12 months, so his appointment for more than one year should be carried out with caution.

Mode of application

Film pills should be taken whole. pills should not be divided or in any other way impair their integrity, since nalmefene can cause irritation in case of direct contact with the skin.

Special patient groups

Elderly (≥65 years old)

In this group of patients dose adjustment is not required.

Renal dysfunction

In patients with mild to moderate renal insufficiency, dose adjustment is not required.

Liver function disorders

In patients with mild and moderate hepatic insufficiency, dose adjustment is not required.

Children and teenagers (under 18)

The safety and effectiveness of Selincro in patients younger than 18 years of age has not been established. No data for this age group.

Adverse effects

In clinical studies, more than 3,000 patients received nalmefene treatment. Overall, the security profile looked similar in all the studies conducted.

The most common adverse reactions were nausea, dizziness, insomnia, and headache. Most of these reactions had mild and moderate severity and were noted only at the beginning of treatment.

Confusion and, less commonly, hallucinations and dissociative disorders were also observed during clinical trials. Most of these reactions had mild and moderate severity and were observed only at the beginning of treatment (the first hours or days). Most of these adverse reactions were resolved with continued therapy and did not resume with repeated use of the drug.These disorders, which are generally short-lived, may be symptoms of alcoholic psychosis, alcohol-induced hangover, or comorbid mental disorders.

The frequency of unwanted adverse reactions was calculated based on the results of three randomized, double-blind, placebo-controlled studies in patients with alcohol dependence (1144 patients received Selincro in an on-demand mode, and 797 received a placebo in an on-demand mode).

Frequency is defined as follows: very often (≥1 / 10), often (from ≥1 / 100 to <1 / S), infrequently (from ≥1 / 1000 to <1/100), rarely (from ≥1 / 10000 to <1/1000), very rarely (<1/10000), is unknown (it is not possible to estimate based on the available data).

Contraindications

- hypersensitivity to nalmefene or any of the components of the drug;

- hereditary intolerance to galactose, lactase deficiency or glucose-galactose malabsorption;

- use in patients currently taking opioid analgesics;

- current or recent opioid dependence;

- acute withdrawal symptoms of opioids;

- suspicion of recent opioid use;

- severe liver failure (Child-Pugh classification);

- severe renal failure (calculated glomerular filtration rate (eGFR) <30 ml / min per 1.73 m2);

- the state of alcohol withdrawal (including hallucinations, convulsions and delirium tremens) in the recent past;

- childhood and adolescence (up to 18 years) (efficacy and safety of use are not confirmed);

- pregnancy, breastfeeding period.

Carefully

Associated mental disorders in the decompensation phase (due to the lack of clinical data); convulsive disorders in historyincluding convulsions that develop with the abolition of alcohol; mild or moderate renal or hepatic failure, elevated levels of ALT and ACT (more than 3 times the upper limit of normal); simultaneous use of potent inhibitors of the UGT2B7 isoenzyme for a long time; elderly patients (≥65 years).

Use during pregnancy and lactation

Data on the use of nalmefene in pregnant women is limited (less than 300 cases of outcomes of pregnancy). Animal studies have revealed the reproductive toxicity of nalmefene.

Studies in animals have not revealed the direct adverse effects of nalmefene on fertility, pregnancy, embryo-fetal development, childbirth and postnatal development. In the study of embryo-fetal toxicity in rabbits, a decrease in fetal weight and delay of ossification (the process of bone tissue formation) were observed; no other serious violations were identified. Exposure (AUC) when taking the highest non-toxic dose (NOAEL / HNTD) with these undesirable effects was lower than the exposure when taking the therapeutic dose recommended for humans. An increase in the incidence of stillborn calves and a decrease in their postnatal survival was observed in pre- and postnatal toxicity studies in rats. This effect was considered indirect and related to toxicity in females. Preclinical data did not reveal the particular danger of nalmefene for humans based on standard studies of pharmacological safety, repeated use toxicity, genotoxicity, and carcinogenic potential.

Selincro is not recommended for use during pregnancy.

Available pharmacodynamic and toxicological data in animals showed the ability of nalmefene and metabolites to pass into breast milk. It is not known whether nalmefene passes into human breast milk.

At present, the potential risk for newborns / infants cannot be ruled out, so Selincro is not recommended for use during breastfeeding.

Fertility

Studies in rats did not reveal the effect of nalmefene on fertility, mating, pregnancy, or the process of spermatogenesis.

Application for violations of the liver

To use the drug with caution in patients with mild or moderate liver failure.

The use of the drug in patients with severe liver failure (classification according to Child-Pugh) is contraindicated.

Application for violations of kidney function

Use with caution in patients with mild or moderate renal insufficiency.

The use of the drug in patients with severe renal insufficiency is contraindicated.

Use in children

The use of the drug in children and adolescents in age (up to 18 years) is contraindicated (efficacy and safety of use are not confirmed).

Use in elderly patients

Use with caution in elderly patients (≥65 years). In this group of patients dose adjustment is not required.

special instructions

Selincro is not intended to achieve immediate abstinence from alcohol.Reducing alcohol consumption is an intermediate goal on the path to total abstinence.

Opioid use

In an emergency situation, when an opioid is required for a patient receiving Celincro, the dose of the latter required to achieve the desired effect may exceed the standard. At the same time, it is necessary to closely monitor the symptoms of respiratory depression resulting from the introduction of opioids, and other undesirable reactions.

If it is necessary to administer opioids to assist the patient in an emergency, their doses should be adjusted individually. In the event that too high doses of opioids are required, the patient’s condition should be carefully monitored.

Selincro must be temporarily canceled 1 week before the intended use of opioids, for example, during a planned surgical procedure.

The physician prescribing Celinkro should advise the patient to inform the medical staff about the time of the last dose of the drug in cases where the use of opioids becomes necessary.

Care must be taken when drugs containing opioids (for example, antitussives and opioid analgesics) are used in patients already receiving Celinkro therapy.

Nalmefene is contraindicated in patients currently taking opioid analgesics.

Accompanying illnesses

Mental disorders

During the course of clinical trials, adverse reactions from the psyche were reported (see the “Side Effects” section). If the patient has mental disorders that are not related to the initiation of Celincro's use and / or they are not temporary, the doctor should consider alternative causes for these symptoms and evaluate the need to continue Celinkro's therapy.

Selincro has not been studied in patients with unstable mental illness. Selincro should be prescribed with caution to patients with concomitant mental illness in the phase of decompensation, including patients with a diagnosis of major depressive disorder.

Convulsive disorders

Experience in the use of the drug in patients with convulsive disorders in history, including convulsions that develop with the abolition of alcohol, is limited. It is recommended to be careful if Celinkro is used to reduce alcohol consumption in this group of patients.

Impaired renal or hepatic function

Celinkro is extensively metabolized in the liver and excreted primarily in the urine. For this reason, care should be taken when administering Selincro to patients with mild or moderate renal or hepatic insufficiency. Caution should be exercised in the appointment of Selincro patients with elevated levels of ALT and ACT (more than 3 times the upper limit of normal), becausethis category of patients was excluded during clinical trials.

Elderly patients (≥65 years)

Clinical data on the use of Selincro in patients with alcohol dependence at the age of 65 years and older are limited. Care should be taken when appointing Selincro patients 65 years and older.

Other

Caution should be exercised while applying Selincro with potent inhibitors of the isoenzyme UGT2B7.

Lactose

Patients with such rare hereditary problems as galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not use this drug.

Influence on ability to drive vehicles and work with mechanisms

The effect of nalmefene on the ability to drive and operate machinery has not been studied.

Selincro can cause unwanted reactions such as nausea, dizziness, insomnia and headache. Most of these reactions had mild and moderate severity and were noted only at the beginning of treatment.

Patients taking Celinkro are not recommended to drive vehicles and work with machinery until an individual reaction to the drug has been clarified.

Overdose

In a study of patients with a diagnosis of pathological addiction to gambling, nalmefene was used in doses up to 90 mg / day for 16 weeks. In a study on patients with interstitial cystitis, 20 patients took nalmefene at a dose of 108 mg / day for more than 2 years.The case of a single dose of ialmefen in a dose of 450 mg was reported, which was not accompanied by a change in blood pressure, heart rate, respiratory rate or body temperature.

In these cases, the safety profile of nalmefen was consistent with that described above in the “Side Effects” section, but the observation experience is limited.

Treatment

In case of overdose, symptomatic therapy and monitoring of the patient’s condition are recommended.

Drug interaction

Studies in interaction with other drugs in vivo was not conducted.

According to in vitro studies, there is no reason to suggest a clinically significant interaction between nalmefene or its metabolites and drugs that undergo metabolism involving the majority of CYP450 isoenzymes and UGT or membrane carriers. Concurrent use with drugs that are potent inhibitors of the isofermemta UGT2B7 (for example, Diclofenac , Fluconazole , medroxyprogesterone acetate, meclofenamic acid) can significantly increase the exposure of nalmefene. Rare use of these drugs at the same time as nalmefene can hardly lead to clinically significant consequences. At the same time, in the case of long-term simultaneous use of potent inhibitors of the isoenzyme UGT2B7, a potentially possible increase in the exposure of nalmefene cannot be ruled out (seesection “Special instructions and precautions”). Accordingly, simultaneous use with UGT inducers (for example, Dexamethasone , phenobarbital, rifampicin, omeprazole) can potentially lead to a decrease in plasma nalmefene concentration below the therapeutic level.

If nalmefene is used simultaneously with opioid agonists (for example, some cough, cough, antidiarrheal drugs and opioid analgesics), a decrease in their therapeutic effect may be observed (see section “Special instructions and precautions”).

There is no clinically significant pharmacokinetic interaction between nalmefene and alcohol.

After using nalmefene, a slight deterioration in cognitive and psychomotor functions may occur. However, the result of the simultaneous intake of nalmefene and alcohol did not exceed the sum of the effects of each substance, used separately.

The simultaneous use of alcohol and Selincro does not prevent the development of alcohol intoxication.

Terms and conditions of storage

The drug should be stored out of the reach of children at a temperature not higher than 30 ° C.