Chlorprothixene (Tablets) Instructions for Use

Marketing Authorization Holder

Apteka V Plyuse, LLC (Russia)

Manufactured By

Pharmproekt, JSC (Russia)

ATC Code

N05AF03 (Chlorprothixene)

Active Substance

Chlorprothixene (Rec.INN registered by WHO)

Dosage Forms

	Chlorprothixene	Film-coated tablets, 15 mg: 10, 30, 50, 60 or 90 pcs.
		Film-coated tablets, 50 mg: 10, 30, 50, 60 or 90 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets orange in color, biconvex.

Excipients: corn starch – 10 mg, lactose monohydrate – 92 mg, sucrose – 10 mg, calcium stearate – 1.5 mg, talc – 1.5 mg.

Film coating composition hypromellose 2910 – 1.7 mg, lactose monohydrate – 1.4 mg, titanium dioxide – 0.67 mg, macrogol (PEG) – 0.6 mg, aluminum lake based on dye “Sunset Yellow” – 0.405 mg, aluminum lake based on dye “Ponceau 4R” – 0.225 mg.

10 pcs. – contour cell packaging (1) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (5) – cardboard packs.
30 pcs. – polyethylene jars (1) – cardboard packs.
60 pcs. – polyethylene jars (1) – cardboard packs.
90 pcs. – polyethylene jars (1) – cardboard packs.
30 pcs. – polymer bottles (1) – cardboard packs.
60 pcs. – polymer bottles (1) – cardboard packs.
90 pcs. – polymer bottles (1) – cardboard packs.

Film-coated tablets from light brown to light yellow in color, biconvex.

Excipients: corn starch – 37.5 mg, lactose monohydrate – 135 mg, sucrose – 20 mg, calcium stearate – 3.75 mg, talc – 3.75 mg.

Film coating composition hypromellose 2910 – 2.55 mg, lactose monohydrate – 2.1 mg, titanium dioxide – 1.725 mg, macrogol (PEG) – 0.9 mg, iron oxide yellow dye – 0.225 mg.

10 pcs. – contour cell packaging (1) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (5) – cardboard packs.
30 pcs. – polyethylene jars (1) – cardboard packs.
60 pcs. – polyethylene jars (1) – cardboard packs.
90 pcs. – polyethylene jars (1) – cardboard packs.
30 pcs. – polymer bottles (1) – cardboard packs.
60 pcs. – polymer bottles (1) – cardboard packs.
90 pcs. – polymer bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Antipsychotic drug (neuroleptic)

Pharmacotherapeutic Group

Antipsychotic agent (neuroleptic)

Pharmacological Action

Antipsychotic agent (neuroleptic), a thioxanthene derivative. It has antipsychotic, antidepressant, sedative, antiemetic effects, and possesses alpha-adrenergic blocking activity.

It is believed that the antipsychotic action is associated with the blockade of postsynaptic dopamine receptors in the brain. The antiemetic effect is associated with the blockade of the chemoreceptor trigger zone of the medulla oblongata. The sedative effect is due to an indirect weakening of the activity of the brainstem reticular system. It suppresses the release of most hypothalamic and pituitary hormones. However, as a result of blocking the prolactin-inhibiting factor, which inhibits the release of prolactin from the pituitary gland, the concentration of prolactin increases.

In chemical structure and pharmacological properties, thioxanthenes are similar to piperazine derivatives of phenothiazine.

Pharmacokinetics

Metabolized in the liver. Excreted primarily by the kidneys.

Indications

Psychoses and psychotic states accompanied by anxiety, fear, psychomotor agitation, aggressiveness, including in depressive-paranoid, circular schizophrenia, in simple sluggish schizophrenia with psychopathic-like and neurosis-like symptoms and in other mental illnesses; dyscirculatory encephalopathy, traumatic brain injuries (as part of combination therapy), alcoholic delirium; sleep disorders in somatic diseases; the need for long-term therapy of agitation and anxiety, psychosomatic, neurotic and behavioral disorders in children; convulsive cough, spastic conditions in the gastrointestinal tract; premedication; dermatoses accompanied by persistent itching; allergic reactions.

ICD codes

Dosage Regimen

Determine the dosage individually based on clinical indication, patient response, and tolerability.

For adults, initiate therapy with a low dose. The typical daily dosage range is 10 mg to 600 mg orally, divided into 3-4 administrations.

For mild conditions such as anxiety or neurosis, use 10-50 mg per day.

For moderate to severe psychoses and agitation, use 50-400 mg per day.

For hospitalized patients with severe psychotic states, the dose may be increased to a maximum of 600 mg per day.

For children, the daily dosage range is 5 mg to 200 mg, adjusted according to body weight and clinical condition.

Administer the total daily dose in divided doses.

Take tablets with a sufficient amount of water, with or after food to minimize potential gastrointestinal irritation.

Initiate treatment at the lowest effective dose.

Titrate the dose gradually based on therapeutic response and adverse effects.

For long-term maintenance therapy, use the minimum effective dose.

Abrupt discontinuation is not recommended; taper the dose gradually to avoid withdrawal symptoms.

Adverse Reactions

From the central nervous system psychomotor retardation, mild extrapyramidal syndrome, increased fatigue, dizziness are possible; in isolated cases, paradoxical increase in anxiety is possible, especially in patients with mania or schizophrenia.

From the digestive system cholestatic jaundice is possible.

From the cardiovascular system tachycardia, ECG changes, orthostatic hypotension are possible.

From the organ of vision clouding of the cornea and lens with visual impairment is possible.

From the hematopoietic system agranulocytosis, leukocytosis, leukopenia, hemolytic anemia are possible.

From the endocrine system frequent hot flashes, amenorrhea, galactorrhea, gynecomastia, weakening of potency and libido are possible.

From metabolism increased sweating, impaired carbohydrate metabolism, increased appetite with weight gain are possible.

Dermatological reactions photosensitization, photodermatitis are possible.

Effects due to anticholinergic action dry mouth, constipation, accommodation disturbances, dysuria.

Contraindications

Depression of the central nervous system, including in case of intoxication with alcohol, barbiturates and other drugs that have a depressant effect on the central nervous system, pathological changes in the blood picture, myelodepression, pregnancy, lactation, hypersensitivity to chlorprothixene.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation.

Use in Hepatic Impairment

Should not be used in severe liver dysfunction.

Use in Renal Impairment

Should not be used in severe renal dysfunction.

Geriatric Use

Should not be used in old age.

Special Precautions

Should not be used in epilepsy, tendency to collapse, parkinsonism, decompensated heart defects, tachycardia, cerebral vascular atherosclerosis, severe liver and kidney dysfunction, hematopoietic disorders, cachexia, old age.

If it is necessary to use chlorprothixene, the risk and benefit of treatment should be weighed in patients with chronic alcoholism, cardiovascular diseases (increased risk of developing transient arterial hypotension), Reye’s syndrome, as well as in glaucoma or predisposition to it, gastric and duodenal ulcers, urinary retention, Parkinson’s disease, epileptic seizures, hypersensitivity to other thioxanthenes or phenothiazines.

When using chlorprothixene, false-positive results of an immunological pregnancy test using urine, as well as false-positive results of a urine test for bilirubin, are possible.

Do not consume alcohol during the treatment period.

Effect on the ability to drive vehicles and mechanisms

During the treatment period, one should refrain from engaging in potentially hazardous activities that require increased attention and rapid psychomotor reactions.

Drug Interactions

With simultaneous use with anesthetics, opioid analgesics, sedatives, hypnotics, antipsychotics, with ethanol, ethanol-containing drugs, the depressant effect on the central nervous system is enhanced.

With simultaneous use with antihypertensive agents, the hypotensive effect is enhanced.

With simultaneous use with anticholinergic, antihistamine, antiparkinsonian drugs, the anticholinergic effect is enhanced.

With simultaneous use with agents causing extrapyramidal reactions, an increase in the frequency and severity of extrapyramidal reactions is possible; with levodopa – suppression of the antiparkinsonian effect of levodopa is possible; with lithium carbonate – severe extrapyramidal symptoms, neurotoxic effect are possible.

With simultaneous use with epinephrine, blockade of the alpha-adrenergic effects of epinephrine and the development of severe arterial hypotension and tachycardia as a result are possible.

With simultaneous use with phenothiazines, metoclopramide, haloperidol, reserpine, the development of extrapyramidal disorders is possible; with quinidine – enhancement of the depressant effect on the heart is possible.

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.