Teralygen^® retard (Tablets) Instructions for Use

Marketing Authorization Holder

Valenta Pharm, JSC (Russia)

Contact Information

VALENTA PHARM JSC (Russia)

ATC Code

R06AD01 (Alimemazine)

Active Substance

Alimemazine (Rec.INN registered by WHO)

Dosage Forms

	Teralygen® retard	Prolonged-release film-coated tablets, 20 mg: 30 pcs.
		Prolonged-release film-coated tablets, 40 mg: 30 pcs.
		Prolonged-release film-coated tablets, 60 mg: 30 pcs.

Dosage Form, Packaging, and Composition

Prolonged-release film-coated tablets light brown in color, round, biconvex; on the cross-section, the core is white or almost white.

Excipients: microcrystalline cellulose (type 101), hypromellose, colloidal silicon dioxide, magnesium stearate.

Shell composition: partially hydrolyzed polyvinyl alcohol, titanium dioxide (E171), macrogol 3350, talc, iron oxide yellow (E172), iron oxide red (E172).

10 pcs. – blister packs (3) – cardboard packs.

Clinical-Pharmacological Group

Anxiolytic and sedative drug

Pharmacotherapeutic Group

Psycholeptics; anxiolytics; other anxiolytics

Pharmacological Action

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

The sedative effect contributes to the normalization of sleep in patients of this category. The sedative and anxiolytic action is due to the blockade of adrenoreceptors of the brainstem reticular formation.

It has antiemetic and antitussive activity. The antiemetic and vegetostabilizing action is due to the blockade of dopamine D₂ receptors of the trigger zone of the vomiting center.

Due to its antihistamine activity, Alimemazine is used for allergic diseases, especially of the respiratory tract, and for skin itching. Alimemazine is more active in terms of antihistamine and sedative action than promethazine. The antipruritic action is due to the effect on histamine H₁ receptors.

Pharmacokinetics

Absorption

It is rapidly and completely absorbed by any route of administration. The action of alimemazine begins 15-20 minutes after administration. The C_max and AUC of alimemazine for the Teralygen^® retard drug depend linearly on the administered dose. The time to reach the maximum concentration of alimemazine (T_max) for the Teralygen^® retard drug is 5-6 hours.

Distribution

Plasma protein binding is 20-30%.

Metabolism

It is metabolized in the liver.

Excretion

It is excreted by the kidneys – 70-80% as a metabolite (sulfoxide). The T_1/2 of alimemazine for the Teralygen^® retard drug is 15-17 hours.

Indications

For adults aged 18 years and over:

As a sedative (calming), anxiolytic (anti-anxiety) agent and an agent that improves falling asleep

• Dementia (including dementia associated with epilepsy), occurring with manifestations of psychomotor agitation, anxiety affect (as part of combination therapy);
• Organic anxiety disorder (as monotherapy or 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);
• Reaction to severe stress and adjustment disorders (acute stress reaction, post-traumatic stress disorder, unspecified reaction to severe stress, other reactions to severe stress) – as part of combination therapy;
• Dissociative (conversion) disorders (as part of combination therapy);
• Somatoform disorders (somatization disorder, undifferentiated somatoform disorder, hypochondriacal disorder, somatoform dysfunction of the autonomic nervous system, persistent somatoform pain disorder, unspecified somatoform disorder, other somatoform disorders) – as part of combination therapy for severe anxiety or when standard therapy is ineffective;
• Unspecified disorder of the autonomic (autonomous) nervous system, other disorders of the autonomic (autonomous) nervous system (as part of combination therapy);
• Anorexia nervosa (as part of combination therapy);
• Emotionally unstable personality disorder (impulsive and borderline types) – as part of combination therapy;
• Histrionic personality disorder, anxious (avoidant) personality disorder (as part of combination therapy);
• Enduring personality change after catastrophic experience (as part of combination therapy);
• Hyperkinetic conduct disorder (as part of combination therapy);
• Conduct disorder confined to the family context (as part of combination therapy when standard therapy is ineffective);
• Unsocialized conduct disorder (as monotherapy or as part of combination therapy);
• Restlessness, agitation and other symptoms and signs related to emotional state (as part of combination therapy);
• Other neurotic disorders (neurasthenia, unspecified neurotic disorder) – as part of combination therapy;
• Nonorganic insomnia (as part of combination therapy when standard therapy is ineffective).

As an antiallergic agent

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

ICD codes

Dosage Regimen

To determine the tolerability of alimemazine, it is possible to use the prolonged-release form after taking the drug Teralygen^® in the immediate-release dosage form (tablets, solution for intramuscular injection).

The effect of the drug is dose-dependent; doses are selected depending on the goals of therapy.

The drug is prescribed in the required dose 1 time/day or 2 times/day with a 12-hour interval at the same time.

To achieve a vegetostabilizing effect 20-60 mg/day.

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

Hypnotic and sedative effects can be achieved with a single dose of 20-60 mg.

For symptomatic treatment of allergic reactions 20-40 mg/day.

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

The maximum dose for adults is 500 mg/day, for elderly persons (over 60 years old) – 200 mg/day.

Children

Safety and efficacy in children aged 0 to 18 years have not been established. Data are not available.

Method of administration

Orally. Do not chew.

Contraindications

• Hypersensitivity to the active substance, as well as to any of the excipients included in the drug;
• Angle-closure glaucoma;
• Prostatic hyperplasia;
• Severe hepatic and/or renal failure;
• Parkinsonism;
• Myasthenia gravis;
• Reye’s syndrome;
• Concomitant use of monoamine oxidase inhibitors (MAOIs);
• Pregnancy;
• Lactation period;
• Children under 18 years of age (for this dosage form).

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

Use in Pregnancy and Lactation

Pregnancy

The use of alimemazine is contraindicated during pregnancy. If pregnancy occurs during treatment, the drug should be discontinued.

Breastfeeding period

The use of alimemazine is contraindicated during breastfeeding. If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Fertility

Human data are not available.

Use in Hepatic Impairment

Contraindicated in severe hepatic insufficiency.

Use in Renal Impairment

Contraindicated in severe renal failure.

Pediatric Use

Contraindicated in children under 18 years of age (for this dosage form).

Special Precautions

Alimemazine may mask the ototoxic effect (tinnitus, dizziness) of concomitantly used medications.

Alimemazine increases the body’s need for riboflavin.

To prevent distortion of the results of skin scarification tests for allergens, the drug should be discontinued 72 hours before allergological testing.

During treatment, false-positive pregnancy test results are possible.

Alcohol should not be consumed during treatment.

Effect on the ability to drive vehicles and mechanisms

During treatment with the drug, activities requiring increased concentration of attention and speed of psychomotor reactions should be avoided (driving a car and other vehicles, working with moving mechanisms, work of a dispatcher and operator).

Drug Interactions

Alimemazine enhances the effects of narcotic analgesics, hypnotics, anxiolytics (tranquilizers) and antipsychotic (neuroleptic) drugs, as well as drugs for general anesthesia, m-cholinoblockers and antihypertensive drugs (dose adjustment is required). Tricyclic antidepressants and anticholinergic drugs enhance the m-cholinoblocking activity of alimemazine.

With simultaneous use of alimemazine with ethanol, increased depression of the central nervous system is possible.

Alimemazine weakens the action of phenamine derivatives, m-cholinomimetics, ephedrine, guanethidine, levodopa, dopamine.

With the combined use of alimemazine with antiepileptic drugs and barbiturates, the threshold of convulsive activity decreases (dose adjustment is required).

With the combined use of alimemazine with beta-blockers, a pronounced decrease in blood pressure and arrhythmias are possible.

Alimemazine weakens the action of bromocriptine. With simultaneous use in nursing mothers, an increase in the concentration of prolactin in the blood serum is possible.

With simultaneous use of alimemazine and MAO inhibitors (simultaneous use is not recommended) and alimemazine and phenothiazine derivatives, the risk of arterial hypotension and extrapyramidal disorders increases.

With simultaneous use of alimemazine with drugs that depress bone marrow hematopoiesis, the risk of myelosuppression increases.

Concomitant use of phenothiazine derivatives (which include Alimemazine) with hepatotoxic drugs may enhance the manifestations of hepatotoxicity of the latter.

Storage Conditions

The drug should be stored in the original packaging (in the pack) in a place inaccessible to children at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.