Alimemazine-Advanced (Tablets) Instructions for Use

Marketing Authorization Holder

Advanced Pharma, LLC (Russia)

ATC Code

R06AD01 (Alimemazine)

Active Substance

Alimemazine (Rec.INN registered by WHO)

Dosage Form

Alimemazine-Advanced

Film-coated tablets, 5 mg: 25, 30 or 50 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets dark pink in color, round, biconvex, with a score; on the cross-section, two layers are visible: a dark pink coating and a white core.

Excipients: lactose monohydrate – 73.4 mg, microcrystalline cellulose (type 102) – 60.8 mg, pregelatinized starch – 16 mg, colloidal silicon dioxide – 1.6 mg, croscarmellose sodium – 1.6 mg, magnesium stearate – 1.6 mg.

Excipients (coating) ready coating Wincoat WT-13007P dark pink: polyvinyl alcohol – 40%, macrogol 3350 – 20.2%, talc – 14.8%, titanium dioxide – 19.44%, carmine red dye – 4.5%, sunset yellow dye – 1.05%, indigo carmine dye – 0.01%.

10 pcs. – blisters (3) – cardboard packs.
10 pcs. – blisters (5) – cardboard packs.
25 pcs. – blisters (1) – cardboard packs.
25 pcs. – blisters (2) – cardboard packs.
25 pcs. – plastic jars (1) – cardboard packs.
30 pcs. – plastic jars (1) – cardboard packs.
50 pcs. – plastic jars (1) – cardboard packs.

Clinical-Pharmacological Group

Antipsychotic drug (neuroleptic)

Pharmacotherapeutic Group

Anxiolytic agent. Sedative agent

Pharmacological Action

A phenothiazine derivative. Acts as a mild sedative and anxiolytic agent, has a positive effect on senestopathy, obsessions, and phobias.

It is used for psychosomatic manifestations developing due to neurovegetative disorders, vascular, traumatic, and infectious impairments of CNS 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 vegetative stabilizing 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 its antihistamine and sedative effects than diprazine. The antipruritic effect is due to its influence on histamine H₁ receptors. It has weak anticholinergic activity.

Pharmacokinetics

It is absorbed quickly and completely by any route of administration. Plasma protein binding is 20-30%. It is metabolized in the liver. It is excreted by the kidneys, 70-80% as a metabolite (sulfoxide).

Indications

As a sedative and anxiolytic agent for the relief of symptoms in neurotic and psychovegetative disorders; symptomatic treatment of allergic conditions of various origins; as a sedative agent for premedication and in the postoperative period; as part of the complex therapy of alcohol withdrawal syndrome.

ICD codes

Dosage Regimen

It is used orally and intramuscularly in the corresponding dosage forms.

The dose and frequency of administration are set individually, depending on the indications, treatment regimen, clinical situation, and patient’s age.

For oral administration, a single dose for adults is 2.5-10 mg. Maximum dose: for adults – 500 mg/day, for elderly patients – 200 mg/day.

For children over 3 years old, a single dose is 2.5-5 mg. The daily dose is 20-80 mg.

For intramuscular injection, a single dose is 25-50 mg. The maximum dose is 200 mg/day.

Adverse Reactions

Side effects are extremely rare and mild.

From the nervous system: drowsiness, lethargy, rapid fatigue (occur mainly in the first days of administration and rarely require drug withdrawal), paradoxical reaction (anxiety, agitation, nightmares, irritability); confusion, extrapyramidal disorders (hypokinesia, akathisia, tremor).

From the sensory organs: blurred vision (paresis of accommodation), noise or ringing in the ears.

From the cardiovascular system: dizziness, decreased blood pressure, tachycardia.

From the digestive system: dryness of the oral mucosa, atony of the gastrointestinal tract, constipation, decreased appetite.

From the respiratory system: dryness in the nose, throat, increased viscosity of bronchial secretion.

From the urinary system: bladder atony, urinary retention.

Contraindications

Hypersensitivity to alimemazine, angle-closure glaucoma, prostatic hyperplasia, severe hepatic and/or renal impairment, parkinsonism, myasthenia gravis, Reye’s syndrome, simultaneous use of MAO inhibitors, pregnancy, breastfeeding period, children under 3 years of age when used as an antiallergic agent and as a sedative before surgery, under 7 years for other indications.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

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

Use in Hepatic Impairment

Contraindication: severe liver diseases.

Use in Renal Impairment

Contraindication: severe kidney diseases.

Pediatric Use

Contraindicated for use in children under 3 years of age as an antiallergic agent and as a sedative before surgery, under 7 years for other indications.

Geriatric Use

Maximum dose: for elderly patients – 200 mg/day.

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.

Alcohol should not be consumed during treatment.

Effect on the ability to drive vehicles and operate machinery

During treatment, one should not engage in activities requiring increased concentration and speed of psychomotor reactions (driving a car and other vehicles, working with moving mechanisms, work of a dispatcher and operator).

Drug Interactions

It enhances the effects of narcotic analgesics, hypnotics, anxiolytics (tranquilizers), and antipsychotic (neuroleptic) drugs, as well as general anesthetics, m-cholinoblockers, and antihypertensive agents (dose adjustment is required).

Tricyclic antidepressants and anticholinergic agents enhance the m-cholinoblocking activity of alimemazine.

When alimemazine is used concomitantly with ethanol, an increase in the depressant effect on the CNS is possible.

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

When alimemazine is used concomitantly with anticonvulsants and barbiturates, the threshold of convulsive activity decreases (dose adjustment is required).

When alimemazine is used concomitantly with beta-blockers, a pronounced decrease in blood pressure and arrhythmias are possible.

It weakens the action of bromocriptine. When used concomitantly in nursing mothers, an increase in serum prolactin concentration is possible.

When alimemazine and MAO inhibitors are used concomitantly (concomitant use is not recommended) and alimemazine and phenothiazine derivatives are used concomitantly, the risk of arterial hypotension and extrapyramidal disorders increases.

When alimemazine is used concomitantly with drugs that suppress bone marrow hematopoiesis, the risk of myelosuppression increases.

When phenothiazine derivatives (including alimemazine) are used concomitantly with hepatotoxic agents, the hepatotoxicity of the latter may be enhanced.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.