Theraligen, 5 mg 50 pcs.

Anxiolytic agent. Sedative.

ATX code: [R06AD01].

Pharmacological properties

Pharmacodynamics

It is a phenothiazine derivative. Alimmazine acts as a mild sedative and anti-anxiety agent, and has a positive effect on senestopathy, obsessions and phobias. It is used for psychosomatic manifestations developing due to neurovegetative disorders, vascular, traumatic and infectious disorders of the central nervous system.

The sedative effect promotes normalization of sleep in patients in this category. It has antiemetic and anti-cough activity. Sedative and anxiolytic effect is caused by blockade of adrenoreceptors of reticular formation of the brain stem. Antiemetic and vegetative stabilizing effect is caused by blockade of dopamine D₂-receptors of trigger zone of the vomiting center.

Due to its antihistamine activity, alimemazine is used in allergic diseases, especially of the respiratory tract, and in itching of the skin. Alimumazine is more active in antihistamine and sedative action than diprazine. The antipruritic action is due to its effect on type 1 histamine receptors.

Pharmacokinetics

It is rapidly and completely absorbed by all routes of administration. The action of alimazine begins 15-20 minutes after administration and lasts 6-8 hours. Binding with plasma proteins is 20-30%. It is metabolized in the liver. Excreted by the kidneys – 70-80% as a metabolite (sulfoxide).

Indications

In adults and children from 7 years:

As a sedative (sedative), anxiolytic (anti-anxiety) and remedy to improve sleep:

– dementia (including dementia due to epilepsy) proceeding with manifestations of psychomotor agitation, anxiety affect (as part of combined therapy);

– organic anxiety disorder (as monotherapy or as part of combined therapy);

– schizophrenia (with a predominance of neurosis-like disorders, as part of combination therapy);

– mood disorders (affective disorders) – as part of combination therapy;

– generalized anxiety disorder (as part of combination therapy);

– obsessive-compulsive disorder (as part of combination therapy);

– severe stress reaction and adaptation disorders (acute reaction to stress, post-traumatic stress disorder, unspecified reaction to severe stress, other reactions to severe stress) – as part of combined therapy;

– dissociative (conversion) disorders (as part of combination therapy);

– somatoform disorders (somatization disorder, undifferentiated somatoform disorder, hypochondriacal disorder, somatoform autonomic nervous system dysfunction, persistent somatoform pain disorder, unspecified somatoform disorder, other somatoform disorders) – as part of combined therapy for severe anxiety or if standard therapy is not effective;

– unspecified autonomic nervous system disorder, other autonomic nervous system disorders (as part of combination therapy);

– Anorexia nervosa (as part of combined therapy);

– emotionally unstable personality disorder (impulsive and borderline types) – as part of combined therapy;

– Hysterical personality disorder, anxious (avoidant, avoidant) personality disorder (as part of combined therapy);

– persistent personality change after experiencing a disaster (as part of combined therapy);

Hyperkinetic behavior disorder (as part of combination therapy);

Family restricted behavior disorder (as part of combination therapy when standard therapy is ineffective);

– non-socialized conduct disorder (as monotherapy or as part of combination therapy);

– anxiety, agitation, and other symptoms and signs related to an emotional state (as part of combination therapy);

– other neurotic disorders (neurasthenia, unspecified neurotic disorder) – as part of combination therapy;

– insomnia of non-organic etiology (as part of combination therapy when standard therapy is ineffective);

– emotional disorders whose onset is specific to childhood (childhood phobic anxiety disorder, childhood social anxiety disorder, sibling rivalry disorder, unspecified childhood emotional disorder, other childhood emotional disorders) – as part of combination therapy.

As an anti-allergic agent:

– Itching regardless of location and etiology (anal itching, vulvar itching, unspecified anogenital itching, itching in photocontact dermatitis and solar urticaria, dermatitis, eczema, urticaria, bites or stings from non-toxic insects or other non-toxic arthropods, varicella, measles, Hodgkin’s disease, diabetes, shingles) as monotherapy or as part of combination therapy;

– asthma, pollinosis, whooping cough (as part of complex therapy as an antiallergic agent to relieve cough, dyspnea and choking attacks);

– unspecified allergy (as monotherapy or as part of combined therapy).

In children from 3 years:

As an anti-allergic agent:

– Itching regardless of location or etiology (itching in photocontact dermatitis and solar urticaria, dermatitis, eczema, urticaria, bites or stings by non-venomous insects or other non-venomous arthropods, varicella, measles, Hodgkin’s disease, diabetes, shingles, anal itching, vulvar itching, unspecified anogenital itching) as monotherapy or as part of combination therapy.

As a sedative (sedative):

– in medicinal preparation for surgery (with the purpose of sedation before surgery).

Active ingredient

Composition

One tablet contains:

the active ingredient:

alimazine tartrate – 5.0 mg;

excipients:

lactose monohydrate, microcrystalline cellulose, pregelatinized starch, colloidal silica (aerosil), croscarmellose sodium, magnesium stearate.

coating composition:

Opadray II 85F34655: partially hydrolyzed polyvinyl alcohol, macrogol-3350, talc, titanium dioxide E 171, carmine red dye E 120, sunset yellow aluminum dye E 110, indigo carmine aluminum dye E 132.

How to take, the dosage

Internal. Without chewing. The action of the drug is dose-dependent, the dosage is chosen depending on the goals of therapy.

Adults

For achieving a vegetative stabilizing effect, 15-60 mg/day.

To achieve an anxiolytic effect 20-80 mg/day.

For a sedative and/or hypnotic effect 5-10 mg once (20-30 minutes before sleep).

For symptomatic treatment of allergic reactions 10-40 mg/day.

Course treatment should be started with 2.5-5 mg in the evening with gradual increase in the daily dose until the desired effect. The daily dose can be divided into 3-4 doses.

The duration of the course of treatment may be 2 to 6 months or more and is determined by the physician.

The highest dose for adults is 500 mg/day, for elderly people (over 60 years) 200 mg/day.

Children from 7 years of age are prescribed with the following regimen (depending on age and body weight).

To achieve an anxiolytic effect, 20-40 mg/day.

The course of treatment should be started with 2.5-5 mg with gradual increase of the daily dose to the desired effect. The daily dose can be divided into 3-4 doses.

To achieve a sedative and/or hypnotic effect, 2.5-5 mg once (20-30 minutes before sleep).

To achieve a sedative effect in behavioral disorders with psychotic states, it is possible to increase the daily dose to 60 mg/day.

For symptomatic treatment of allergic reactions 5-20 mg/day.

The duration of course of treatment can be from 2 to 6 months or more and is determined by the physician.

In children from 3 years of age

For symptomatic treatment of allergic reactions 2.5-5 mg 3-4 times a day.

The duration of the course of treatment may vary from 2 to 6 or more months and is determined by the physician.

For the purpose of sedation before surgery, children from 3 to 7 years of age are prescribed at the rate of 2 mg/kg 1-2 hours before surgery. The maximum daily dose is 2 mg/kg.

Interaction

Alimumazine enhances the effects of narcotic analgesics, hypnotics, anxiolytics (tranquilizers) and antipsychotics (neuroleptics), as well as drugs for general anesthesia, m-cholinoblockers and hypotensive drugs (requires dosage adjustment). Tricyclic antidepressants and anticholinergic drugs increase m-cholinoblocking activity of alimemazine. In concomitant use of alimemazine with ethanol it is possible to increase the depression of the central nervous system.

Alimemazine attenuates the effects of phenamine derivatives, m-cholinomimetics, ephedrine, guanethidine, levodopa, dopamine.

When alimemazine is coadministered with antiepileptic drugs and barbiturates the seizure activity threshold is reduced (dose adjustment is required).

In co-administration of alimazine with beta-adrenoblockers a significant decrease in BP and arrhythmias are possible.

Alimemazine weakens the effect of bromocriptine. Simultaneous use in breastfeeding mothers may increase the concentration of prolactin in the blood serum.

The simultaneous use of alimumazine and MAO inhibitors (concomitant use is not recommended) and alimumazine and phenothiazine derivatives increases the risk of arterial hypotension and extrapyramidal disorders.

The risk of myelosuppression increases when alimumazine is used concomitantly with drugs that inhibit medullary hematopoiesis.

The co-administration of phenothiazine derivatives (which include alimemazine) with hepatotoxic drugs may increase the hepatotoxicity of the latter.

Special Instructions

Alimemazine increases the body’s need for riboflavin.

In order to prevent distortion of the results of skin allergen scarification tests, the drug should be discontinued 72 hours before allergy testing.

False positive results for pregnancy are possible during treatment.

Alcohol should not be consumed during treatment.

Impact on the ability to drive and operate machinery:

During treatment with the drug, do not engage in activities requiring increased concentration and rapid psychomotor reactions (driving and other vehicles, working with moving machinery, work of dispatcher and operator).

Synopsis

Contraindications

– hypersensitivity to the components of the drug;

– lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

– closed-angle glaucoma;

– prostatic hyperplasia;

– severe hepatic and/or renal impairment;

– parkinsonism;

– myasthenia;

– Reye syndrome;

– concurrent use of monoamine oxidase inhibitors (MAOIs);

– pregnancy;

– lactation period;

– childhood under 3 years of age when used as an anti-allergic agent and for sedation before surgical intervention, under 7 years for other indications.

Precautionary measures for use

The drug should be used with caution if there is a history of complications with the use of phenothiazine series drugs; In bladder neck obstruction; predisposition to urinary retention; epilepsy; open-angle glaucoma; jaundice; depression of bone marrow function; arterial hypotension.

Side effects

Side effects are extremely rare and mild.

Nervous system disorders: drowsiness, lethargy, rapid fatigability (occurs mainly in the first days of use and rarely requires drug withdrawal), paradoxical reactions (anxiety, agitation, nightmares, irritability); confusion, extrapyramidal disorders (hypokinesia, akathisia, tremor).

Sensory organs: blurred vision (paresis of accommodation), tinnitus or ringing in the ears.

Cardiovascular system: dizziness, decreased blood pressure (BP), tachycardia.

Digestive system disorders: dry mucous membrane of the mouth, gastrointestinal atony, constipation, loss of appetite.

Respiratory system: dryness in the nose, pharynx, increased viscosity of bronchial secretion.

Perior urinary system disorders: bladder atony, urinary retention.

Others: allergic reactions, inhibition of medullary hematopoiesis, increased sweating, muscle relaxation, photosensitization.

Overdose

Symptoms: aggravation of the described side effects, except for allergic reactions.

Treatment: drug withdrawal, symptomatic therapy.

Pregnancy use

It is contraindicated in pregnancy and during lactation (breastfeeding). If pregnancy occurs during treatment, the drug should be discontinued. If it is necessary to use the drug during lactation, breastfeeding should be stopped.