Saffris - instructions for use, analogs, reviews and release forms (5 mg and 10 mg tablets) drug for the treatment of schizophrenia, delusional and affective disorders, inorganic psychosis in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Saffris. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of experts on the use of Safris in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Safris in the presence of existing structural analogues. Use for the treatment of schizophrenia, delusional and affective disorders, inorganic psychosis in adults, children, as well as in pregnancy and lactation. Composition of the preparation.

Saffris antipsychotic agent (antipsychotic). The mechanism of action of asenapine (the active substance of the drug Safris), as well as other drugs effective in the treatment of schizophrenia and bipolar disorder, is not fully understood. Given the nature of the interaction of asenapine with receptors, it is believed that the effectiveness is determined by the combined antagonistic effect on dopamine D2 and serotonin 5-HT2A receptors. Interaction with other receptors, for example, serotonin 5-HT1A-, 5-HT1B-, 5-HT2C-, 5-HT6-, 5-HT7-, dopamine D3- and α2-adrenoreceptors, may also affect the clinical effect of asenapine .

Composition

Asenapine + excipients.

Pharmacokinetics

After sublingual administration, asenapine is rapidly absorbed. Absolute bioavailability of asenapine in a dose of 5 mg with sublingual application is 35%. Absolute bioavailability during ingestion is low (less than 2%). Taking water after 2 or 5 minutes after applying Safris leads to a decrease in the concentration of asenapine in the blood (by 19% and 10%, respectively). In this regard, within 10 minutes after taking asenapine should not drink or eat.Asenapine undergoes intensive metabolism. Pharmacological activity is mainly determined by unchanged asenapine. Most of the dose is excreted by the kidneys (about 50%) and through the intestine (about 40%). Only a small part of the dose is excreted through the intestine (5-16%) in the form of unchanged asenapine. The pharmacokinetics of asenapine is similar in patients with mild and moderate impairment of liver function and in patients with normal liver function. Pharmacokinetics after a single dose of 5 mg of asenapine was similar in patients with varying degrees of impaired renal function and patients with normal renal function.

Indications

• schizophrenia (for stopping and supporting treatment);
• schizotypic disorder;
• bipolar affective disorder (as a monotherapy for stopping treatment of associated manic or mixed episodes);
• manic or mixed episodes associated with bipolar affective disorder (for their relief as adjunctive therapy with lithium or valproate preparations);
• chronic delusional disorders;
• acute and transient mental disorders;
• schizoaffective disorder;
• inorganic psychosis, unspecified.

Forms of release

Tablets are sublingual 5 mg and 10 mg.

Instructions for use and dosing regimen

For oral administration.

Depending on the indications, the single dose is 5-10 mg, the daily dose is 10-20 mg. Frequency of admission - 2 times a day. The duration of treatment depends on the effectiveness and clinical situation.

When combined with other drugs, Saffrys should be taken last.

Side effect

• drowsiness;
• akathisia (internal need to move, change posture);
• Parkinsonism (neurological syndrome, which is characterized by a disorder of voluntary movements);
• dizziness;
• dysgeusia (a disorder of taste in which taste sensations are partially absent or distorted);
• dyskinesia (collective name of violations of coordinated motor acts);
• sedative effect;
• dysarthria (pronunciation disorder);
• fainting;
• extrapyramidal disorders (motor disorders);
• convulsive seizures;
• malignant neuroleptic syndrome (CNS) - a relatively rare but life-threatening disorder associated with taking psychotropic medications;
• anxiety;
• hypoesthesia, paresthesia of the mouth (sensitivity disorder of the oral mucosa);
• increased activity of alanine aminotransferase (ALT);
• glossodynia (unpleasant sensations in the mouth);
• swelling of the tongue;
• dysphagia (violation of swallowing);
• sinus bradycardia (slowing of the heart rate);
• blockade of the bundle of the bundle;
• prolongation of QT interval on ECG;
• Orthostatic hypotension (a violation of the ability of the body to maintain a normal level of blood pressure in the vertical position);
• neutropenia;
• increase in body weight;
• increased appetite;
• Hyperglycemia (elevated blood sugar levels);
• pulmonary embolism (blockage of pulmonary artery thrombus);
• stiffness (hardness, stiffness) of the muscles;
• rhabdomyolysis (destruction of cells of muscle tissue);
• sexual dysfunction;
• amenorrhea (absence of menstruation);
• gynecomastia (enlargement of the breast with hypertrophy of glands and adipose tissue);
• galactorrhea (excretion of milk from the mammary glands without lactation);
• fatigue;
• allergic reactions;
• withdrawal syndrome in newborns.

Contraindications

• children's age till 18 years;
• lactation period (breastfeeding);
• hypersensitivity to asenapine.

Application in pregnancy and lactation

Saffis is not recommended for use in pregnancy, except when the potential benefit to the patient significantly exceeds the possible risk to the fetus.

It is not known whether asenapine or its metabolites are excreted in human breast milk. In experimental studies, it was shown that asenapine is excreted in breast milk in lactating rats. The use of asenapine during lactation is contraindicated.

Use in children

Contraindicated in children and adolescents under the age of 18 years.

Application in elderly patients

Asenapine should be used with caution in elderly patients.

special instructions

In elderly patients with psychosis on the background of dementia in the treatment with antipsychotic drugs, the risk of death is increased. Asenapine is not recommended for the treatment of patients with psychosis on the background of dementia.

In the treatment with antipsychotic drugs, including Safris, cases of malignant neuroleptic syndrome, characterized by hyperthermia, muscle rigidity, instability of the autonomic nervous system,a violation of consciousness and an increase in the level of the enzyme kreatine phosphokinase (CK) in the blood serum. Additional manifestations may be myoglobinuria (rhabdomyolysis) and acute renal failure. If symptoms of NSA appear, asenapine should be discontinued.

Use with caution in patients with convulsive conditions in the history or conditions associated with seizures.

In psychotic illnesses and bipolar disorder, suicidal attempts can be observed, therefore treatment of patients with high risk of suicide should be conducted under strict supervision.

In patients with severe impairment of liver function, a sevenfold increase in the concentration of asenapine was observed, therefore it is not recommended to use Saffrys in this category of patients.

Asenapine can cause orthostatic hypotension and fainting, especially at the beginning of treatment, which may reflect its alpha-1-adrenergic blocking properties. Elderly patients are particularly at risk of developing orthostatic hypotension. Asenapine should be used with caution in elderly patients and in patients with cardiovascular disease (eg, heart failure,myocardial infarction or ischemia and conduction disorders), cerebrovascular disease or conditions that predispose to the development of arterial hypotension (eg, dehydration and hypovolemia).

The occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. When symptoms of tardive dyskinesia appear, treatment should be considered.

Some patients who received asenapine showed an increase in prolactin concentration. There were individual cases of adverse events associated with an increase in the concentration of prolactin in the blood.

Probably, treatment with Safrisom is not accompanied by a clinically significant lengthening of the QT interval. However, care should be taken with the use of asenapine in patients with cardiovascular disease or in the presence of a family history of an extended interval of QT and with concomitant therapy with other drugs that increase the duration of the QT interval.

During treatment with asenapine, hyperglycemia and exacerbations of the existing history of diabetes were sometimes observed. The establishment of a link between the use of atypical antipsychotics and the violation of glucose metabolism is complicateddue to the increased risk of developing diabetes in patients with schizophrenia or bipolar disorder, and the increasing incidence of diabetes in the general population. It is recommended to regularly monitor patients with diabetes mellitus and patients with risk factors for this disease.

Treatment with antipsychotic drugs can be accompanied by a violation of thermoregulation. With the use of asenapine, clinically significant changes in thermoregulation did not develop. During treatment, patients should receive appropriate care in the event of development of conditions and situations contributing to body temperature increase, for example, exercise, high temperature exposure, dehydration or taking concomitant medications with m-cholinoblocking activity.

During treatment, patients should avoid drinking alcohol.

Impact on the ability to drive vehicles and manage mechanisms

Saffis can cause drowsiness and sedation. Therefore, during the treatment period, patients should not drive vehicles and work with mechanisms,Until the nature of the unwanted effects of asenapine is established.

Drug Interactions

Asenapine has an effect on the central nervous system, so caution should be exercised when used in combination with other central-action drugs.

Safris is metabolized mainly by direct glucuronation under the action of the isoenzyme UGT1A4 and oxidative metabolism under the action of cytochrome P450 isoenzymes (mainly isoenzyme CYP1A2). When used simultaneously with fluvoxamine (an inhibitor of the isoenzyme CYP1A2) at the full therapeutic dose, fluvoxamine can cause a more pronounced increase in the plasma asenapine concentration.

Due to the fact that asenapine has alpha-1-adrenergic blocking properties and is capable of causing orthostatic hypotension, with the combination, it is possible to enhance the effects of some antihypertensive drugs.

Asenapine has a weak inhibitory effect on the isoenzyme CYP2D6. Use with caution in combination with preparations that are substrates or inhibitors of the isoenzyme CYP2D6.

Simultaneous single administration of 20 mg of Paroxetine (substrate and inhibitor of the isoenzyme CYP2D6) during the administration of asenapinein a dose of 5 mg twice a day in healthy male volunteers led to almost a two-fold increase in the concentration of paroxetine. However, asenapine can enhance the inhibitory effects of paroxetine on its own metabolism.

Analogues of medicinal product Saffris

Saffris does not have structural analogs for the active substance.

Analogues of the drug Saffris on the pharmacological group (neuroleptics):

• Abilifay;
• Azaleprol;
• Azaleptin;
• Amdoal;
• Aminazine;
• Aripiprazole;
• Barnetil;
• Betamax;
• Victor;
• Haloperidol;
• Hedonin;
• Droperidol;
• Zalast;
• Zilaxera;
• Ziprex;
• Invega;
• Quentiaks;
• Quetiapine;
• Quetitex;
• Ketiap;
• Clozapine;
• Clopixol;
• Koumental;
• Lakvel;
• Latuda;
• Leptinorm;
• Mazeptil;
• Melleril;
• Moditen;
• Nantarid;
• He did not;
• Normiton;
• Olanex;
• Olanzapine;
• Parnasan;
• Prolinate;
• Propazine;
• Prosulfin;
• It is resilient;
• Rileptid;
• Ridonal;
• Rispolux;
• Risset;
• Senorm;
• The servicer;
• The Serdolect;
• Seroquel;
• Solian;
• Sulpiride;
• Terialgen;
• Tiapride;
• Tizerzin;
• Thiodasin;
• Thioridazine;
• Thioril;
• Tyson;
• Topral;
• Torendo;
• Trasin;
• Triftazine;
• Fluphenazine;
• Fluanexol;
• Chlorpromazine;
• Eglek;
• Eglonyl;
• Escap;
• Etaperazine.

Analogues on the curative effect (means for the treatment of schizophrenia):

• Abilifay;
• Azaleptin;
• Amdoal;
• Amitriptyline;
• Ariprizol;
• Betamax;
• Haloperidol;
• Demanol;
• Diazepam;
• Zalast;
• Zeldox;
• Ziprex;
• Invega;
• Quentiaks;
• Ketilept;
• Klozasten;
• Clopixol;
• Xseplion;
• Lakvel;
• Loram;
• Mazeptil;
• Moditen;
• Nantarid;
• Olanzapine;
• Pantogam;
• Parnasan;
• Piportil;
• Prolinate;
• Prosulfin;
• Ridonex;
• Rileptid;
• Rispolux;
• Senorm;
• The servicer;
• The Serdolect;
• Sibazon;
• Sidnokarb;
• Solian;
• Sonapaks;
• Speridan;
• Sulpiride;
• Tizerzin;
• Thiodasin;
• Topral;
• Torendo;
• Trasin;
• Triftazine;
• Truksal;
• Fluanexol;
• Chloroproticsen;
• Eglek;
• Eglonyl;
• Egolanza;
• Escap;
• Etaperazine.

Doctor's comment

I prescribe the drug Saffris to patients with schizophrenia as a supporting therapy. Treatment, as a rule, is long and requires compliance with the dosing regimen. Taking 5 mg twice a day, patients tolerate the drug well, only occasionally complaining of drowsiness and dizziness. Those who are shown a dose of 10 mg twice a day to stabilize the condition are more likely to complain about the side effects of Safris.Among them, complaints of a sudden feeling of anxiety, a disorder of taste, a violation of coordination. In a few cases, the medicine had to be canceled and the patients treated with other drugs.

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