Pemixamal (Tablets) Instructions for Use

Marketing Authorization Holder

Pharmasintez, JSC (Russia)

ATC Code

N05AF03 (Chlorprothixene)

Active Substance

Chlorprothixene (Rec.INN registered by WHO)

Dosage Forms

	Pemixamal	Film-coated tablets, 15 mg: 10, 20, 25, 30, 40, 50, 60 or 100 pcs.
		Film-coated tablets, 25 mg: 10, 20, 25, 30, 40, 50, 60 or 100 pcs.
		Film-coated tablets, 50 mg: 10, 20, 25, 30, 40, 50, 60 or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets red in color, round, biconvex.

Excipients: copovidone – 5.1 mg, corn starch – 10.2 mg, croscarmellose sodium – 2.04 mg, lactose monohydrate – 52.5 mg, magnesium stearate – 0.96 mg, silicified microcrystalline cellulose [microcrystalline cellulose 98%, colloidal silicon dioxide 2%] – 10.2 mg. Tablet core weight – 96 mg .

Film coating composition: hypromellose E15 – 1.5 mg, iron oxide red dye – 0.09 mg, magnesium carbonate hydroxide – 0.3 mg, macrogol 400 – 0.45 mg, macrogol 6000 – 0.15 mg, talc – 0.51 mg. Coating weight – 3 mg.

Coated tablet weight – 99 mg.

10 pcs. – contour cell blisters (1) – cardboard packs.
10 pcs. – contour cell blisters (2) – cardboard packs.
10 pcs. – contour cell blisters (3) – cardboard packs.
10 pcs. – contour cell blisters (4) – cardboard packs.
10 pcs. – contour cell blisters (5) – cardboard packs.
10 pcs. – contour cell blisters (6) – cardboard packs.
10 pcs. – contour cell blisters (10) – cardboard packs.
10 pcs. – jars (1) – cardboard packs.
25 pcs. – jars (1) – cardboard packs.
30 pcs. – jars (1) – cardboard packs.
40 pcs. – jars (1) – cardboard packs.
50 pcs. – jars (1) – cardboard packs.
60 pcs. – jars (1) – cardboard packs.
100 pcs. – jars (1) – cardboard packs.

Film-coated tablets white in color, round, biconvex.

Excipients: copovidone – 8.5 mg, corn starch – 17 mg, croscarmellose sodium – 3.4 mg, lactose monohydrate – 87.5 mg, magnesium stearate – 1.6 mg, silicified microcrystalline cellulose [microcrystalline cellulose 98%, colloidal silicon dioxide 2%] – 17 mg. Tablet core weight – 160 mg.

Film coating composition: hypromellose E15 – 2.5 mg, magnesium carbonate hydroxide – 0.65 mg, macrogol 400 – 0.75 mg, macrogol 6000 – 0.25 mg, talc – 0.85 mg. Coating weight – 5 mg.

Coated tablet weight – 165 mg.

10 pcs. – contour cell blisters (1) – cardboard packs.
10 pcs. – contour cell blisters (2) – cardboard packs.
10 pcs. – contour cell blisters (3) – cardboard packs.
10 pcs. – contour cell blisters (4) – cardboard packs.
10 pcs. – contour cell blisters (5) – cardboard packs.
10 pcs. – contour cell blisters (6) – cardboard packs.
10 pcs. – contour cell blisters (10) – cardboard packs.
10 pcs. – jars (1) – cardboard packs.
25 pcs. – jars (1) – cardboard packs.
30 pcs. – jars (1) – cardboard packs.
40 pcs. – jars (1) – cardboard packs.
50 pcs. – jars (1) – cardboard packs.
60 pcs. – jars (1) – cardboard packs.
100 pcs. – jars (1) – cardboard packs.

Film-coated tablets yellow in color, oval, biconvex.

Excipients: copovidone – 17 mg, corn starch – 34 mg, croscarmellose sodium – 6.8 mg, lactose monohydrate – 175 mg, magnesium stearate – 3.2 mg, silicified microcrystalline cellulose [microcrystalline cellulose 98%, colloidal silicon dioxide 2%] – 34 mg. Tablet core weight – 320 mg.
Film coating composition: hypromellose E15 – 5 mg, iron oxide yellow dye – 0.3 mg, magnesium carbonate hydroxide – 1 mg, macrogol 400 – 1.5 mg, macrogol 6000 – 0.5 mg, talc – 1.7 mg. Coating weight – 10 mg.

Coated tablet weight – 330 mg.

10 pcs. – contour cell blisters (1) – cardboard packs.
10 pcs. – contour cell blisters (2) – cardboard packs.
10 pcs. – contour cell blisters (3) – cardboard packs.
10 pcs. – contour cell blisters (4) – cardboard packs.
10 pcs. – contour cell blisters (5) – cardboard packs.
10 pcs. – contour cell blisters (6) – cardboard packs.
10 pcs. – contour cell blisters (10) – cardboard packs.
10 pcs. – jars (1) – cardboard packs.
25 pcs. – jars (1) – cardboard packs.
30 pcs. – jars (1) – cardboard packs.
40 pcs. – jars (1) – cardboard packs.
50 pcs. – jars (1) – cardboard packs.
60 pcs. – jars (1) – cardboard packs.
100 pcs. – jars (1) – cardboard packs.

Clinical-Pharmacological Group

Antipsychotic drug (neuroleptic)

Pharmacotherapeutic Group

Psycholeptics; antipsychotic agents; thioxanthene derivatives

Pharmacological Action

Antipsychotic agent (neuroleptic), a thioxanthene derivative. It has antipsychotic, antidepressant, sedative, and 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 reticular system of the brainstem. It suppresses the release of most hormones of the hypothalamus and pituitary gland. However, due to the blockade of 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 mainly 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 psychopath-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 the clinical indication, patient age, and therapeutic response.

Administer the tablets orally with a sufficient amount of water.

For adult patients, the typical daily dosage range is from 10 mg to 600 mg.

Initiate therapy at a low dose and titrate upward gradually to minimize adverse reactions.

Divide the total daily dose into two to four separate administrations.

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

For moderate to severe psychotic disorders, higher maintenance doses of 100-400 mg daily are often required.

In acute agitation, higher initial doses may be necessary under close medical supervision.

For pediatric patients, the daily dosage range is from 5 mg to 200 mg.

Calculate the pediatric dose carefully based on the child’s body weight and clinical condition.

For premedication, administer a single dose of 25-50 mg for adults approximately one hour prior to the procedure.

Adjust the dosage for geriatric or debilitated patients, typically initiating at the lower end of the range.

Regularly monitor the patient’s clinical status and adjust the dosage regimen as necessary.

Do not abruptly discontinue therapy; taper the dose gradually to prevent 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

CNS depression, including in case of intoxication with alcohol, barbiturates and other drugs that have a depressant effect on the CNS, 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 function disorders.

Use in Renal Impairment

Should not be used in severe renal function disorders.

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 atherosclerosis, severe liver and kidney function disorders, 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 treatment.

Effect on 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, antipsychotic agents, with ethanol, ethanol-containing drugs, the depressant effect on the CNS is enhanced.

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

With simultaneous use with anticholinergic, antihistamine, antiparkinsonian agents, 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 action 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.