Selincro, 18 mg 14 pcs.

The drug for the treatment of alcohol addiction.

Nalmefen is an opioid system modulator with pronounced affinity for μ-, δ- and κ-receptors.

Indications

Selincro is recommended in combination with sustained psychosocial support to maintain treatment adherence and reduce alcohol consumption.

Selincro is prescribed after two weeks of follow-up for a patient with a continuing high risk of alcohol abuse.

Active ingredient

Composition

One tablet contains:

The active ingredient – nalmefene hydrochloride dihydrate 21.917 mg converted to nalmefene hydrochloride 20.0 mg, converted to nalmefene 18.06 mg;

Assisted substances – Microcrystalline cellulose 61.4 mg,

anhydrous lactose 60.683 mg,

crospovidone (type A) 4.5 mg,

/p>

magnesium stearate 1.5 mg;

Film Coating – Opadray OY-S-28849 white 4.5 mg (hypromellose (5mPa.c), macrogol 400, titanium dioxide (E171)).

How to take, the dosage

At the initial visit, before prescribing Selinkro, the physician needs to assess the patient’s clinical condition and alcohol consumption level (as reported by the patient). In cases where additional information is required, the patient is asked to record his or her alcohol consumption for approximately the next two weeks. For those patients whose alcohol consumption remained comparable to the initial level during these two weeks, Selincro may be prescribed at the follow-up visit.

Selincro is recommended when used in conjunction with psychosocial support to maintain adherence to treatment and reduce alcohol consumption.

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

Selincro is used as needed. The decision to take the drug is up to the patient: on days when he or she believes alcohol consumption is likely, 1 tablet is taken 1-2 hours before the intended time of ingestion. Selincro at a dose of 18 mg. If the patient has started taking alcohol without first taking a Selincro tablet, he should do so as soon as possible.

The maximum daily dose of Selincro is 1 tablet. Selincro can be taken regardless of meals.

In clinical studies, maximum improvement was seen during the first 4 weeks of therapy. Patient response to treatment and the appropriateness of continuing pharmacotherapy should be evaluated regularly (e.g. monthly). The physician should continually determine the patient’s progress in reducing alcohol consumption, his or her general condition, adherence to therapy, and the occurrence of side effects.

The duration of Celincro clinical trials has not exceeded 12 months, so its prescription for more than one year should be done with caution.

Test method of administration

The film-coated tablets should be taken whole. The pills should not be divided or otherwise compromised as nalmefene may cause irritation if there is direct skin contact.

Interaction

In vivo drug-drug interactions studies have not been conducted.

Based on in vitro studies, clinically significant interactions between nalmefene or its metabolites and concomitantly administered drugs that are metabolized primarily by CYP450 and UGT enzymes or membrane transporters are not anticipated.

Concomitant use with drugs that are strong inhibitors of the UGT2B7 enzyme (e.g., diclofenac, fluconazole, medroxyprogesterone acetate, meclofenamic acid) may significantly increase the effects of nalmefen.

This is unlikely to cause a problem with occasional use, but if concurrent long-term treatment with a potent UGT2B7 inhibitor is initiated, the potential for increased effects of nalmefene cannot be ruled out. On the other hand, concomitant administration of a UGT inducer (e.g., dexamethasone, phenobarbital, rifampicin, omeprazole) may lead to subtherapeutic plasma concentrations of nalmefene.

If Celinecro is used concomitantly with opioid agonists (e.g., some cough and cold medicines, some anti-diarrheals and opioid analgesics), the patient may not benefit from the opioid agonists.

There are no clinically significant pharmacokinetic interactions between nalmefen and alcohol.There may be a slight impairment of cognitive and psychomotor functions after administration of nalmefen.However, the effects of nalmefen and alcohol in combination do not exceed the sum of the effects of each substance taken separately.

The simultaneous administration of alcohol and Selincro does not prevent alcohol intoxication.

Special Instructions

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

Application of opioids

In an emergency situation in which a patient taking Selinkro needs opioid administration, the doses of opioids required to achieve the desired effect may exceed the standard doses. Symptoms of respiratory depression resulting from opioid administration and other adverse reactions should be monitored closely.

If opioids are needed for emergency patient care, the dose should be adjusted individually. If too high doses of opioids are needed, the patient’s condition should be closely monitored.

Selincro should be temporarily withdrawn 1 week before the intended use of opioids, e.g., during a planned surgical procedure.

The physician prescribing Selincro should advise the patient to inform the health care provider of the time of the last administration of the drug in cases where opioid use becomes necessary.

Caution should be exercised when medications containing opioids (e.g., cough medicines and opioid analgesics) are used in patients already receiving Selinkro therapy.

Nalmefen is contraindicated in patients currently taking opioid analgesics.

Companion diseases

Mental disorders

In the course of clinical trials, adverse mental reactions have been reported (see Side effects). If a patient has a mental disorder not related to the start of Selinkro and/or which is not temporary, the physician should consider alternative causes for these symptoms and evaluate the need for continued treatment with Selinkro.

Selincro has not been studied in patients with an unstable course of mental illness. Caution should be exercised when prescribing Selincro in patients with concomitant psychiatric illnesses in the decompensation phase, including patients diagnosed with major depressive disorder.

Convulsive disorders

The experience with the drug in patients with a history of seizure disorders, including seizures developing with alcohol withdrawal, is limited. Caution is advised if Selincro is used to reduce alcohol consumption in this group of patients.

Renal or hepatic disorders

Selincro is actively metabolized in the liver and is excreted primarily with the urine. For this reason, caution should be exercised when prescribing Selincro in patients with mild to moderate renal or hepatic impairment. Caution should be exercised when prescribing Selinkro in patients with elevated ALT and ACT levels (more than 3 times the upper limit of normal values), since this category of patients was excluded in clinical trials.

Elderly patients (≥65 years)

The clinical data on the use of Selinkro in alcohol-dependent patients aged 65 years and older are limited. Caution should be exercised when prescribing Selincro to patients 65 years of age and older.

Others

Caution should be exercised when using Selincro concomitantly with potent UGT2B7 isoenzyme inhibitors.

Lactose

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

Influence on driving and operating machinery

The effect of nalmefen on driving and operating machinery has not been studied.

Selincro may cause adverse reactions such as nausea, dizziness, insomnia, and headache. Most of these reactions were mild to moderate in severity and occurred only at the beginning of treatment.

Patients taking Selincro should not drive or operate machinery until an individual reaction to the drug has been determined.

Contraindications

Hypersensitivity to nalmefene or any of the ingredients of the drug; hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption.

The use in patients currently taking opioid analgesics.

Current or recent opioid dependence.

Acute opioid withdrawal symptoms.

Suspicion of recent opioid use.

Severe hepatic impairment (Child-Pugh classification).

Severe renal insufficiency (calculated glomerular filtration rate (rGFR) <30 ml/min per 1.73 m2).

A recent history of alcohol withdrawal (including hallucinations, seizures, and alcoholic delirium).

Childhood and adolescence (under 18 years of age) (efficacy and safety of use not confirmed).
Pregnancy, period of breastfeeding.

With caution:

Compatible psychiatric disorders in the decompensation phase (due to lack of clinical data); history of seizure disorders, including seizures developing with alcohol withdrawal; mild or moderate renal or hepatic insufficiency, elevated ALT and AST levels (more than 3 times the upper limit of normal); concomitant use of potent UGT2B7 isoenzyme inhibitors for a long time; elderly patients (>65 years).

Side effects

The most common adverse reactions in clinical trials were nausea, dizziness, insomnia, and headaches.

Most of these reactions were mild to moderate, related to the onset of treatment, and of short duration.

Consciousness confusion and, less frequently, hallucinations and dissociation have been reported in clinical trials.

Most of these reactions were mild to moderate, associated with the onset of treatment, and short-term (a few hours to a few days).

Most adverse reactions go away with continued treatment and do not recur with repeated use.

Alcoholic psychosis, alcohol withdrawal syndrome, or comorbid psychiatric conditions have also been observed, usually of short duration.

Frequency is defined as: very often (≥1/10), often (≥1/100 to

– Nutrition and metabolism
Frequently: Decreased appetite. Decreased body weight.

– Mental health
Very common: Insomnia.
Frequent: Sleep disturbance, confusion, restlessness, decreased libido (including loss of libido).
Frequent unknown: Hallucinations (including auditory, tactile, visual and somatic hallucinations), dissociation.

– Nervous system disorders
Very common: Dizziness, headache.
Often: Drowsiness, tremor, impaired attention, paresthesias, hypoesthesia.

– Cardiovascular system
Often: Tachycardia, palpitations.

– Digestive system
Very common: Nausea.
Often: Vomiting, dry mouth.

– Skin and subcutaneous tissue
Often: Hyperhidrosis.

– Musculoskeletal system
Often: Muscle cramps.

– General disorders
Often: Fatigue, asthenia, malaise, unusual sensations.

Overdose

In a study of patients diagnosed with pathological gambling addiction, nalmefene was used in doses up to 90 mg/day for 16 weeks. In a study in patients with interstitial cystitis, 20 patients took nalmefen at a dose of 108 mg/d for more than 2 years.

A case of a single 450 mg dose of ilmefen was reported that was not accompanied by changes in blood pressure, heart rate, respiratory rate, or body temperature.

In these cases, the safety profile of nalmefene was consistent with that described above under “Side Effects,” but there is limited observational experience.

Treatment

In case of overdose, symptomatic therapy and monitoring of the patient is recommended.