Instruction for use: Levomepromazine

The Latin name of the substance Levomepromazine

Levomepromazinum (genus. Levomepromazini)

Chemical name

(R) -2-Methoxy-N, N, beta-trimethyl-10H-phenothiazine-10-propanamine (as maleate (1: 1) or hydrochloride)

Gross formula

C₁₉H₂₄N₂OS

Pharmacological group:

Neuroleptics

The nosological classification (ICD-10)

B02.2 Shingles with other complications from the nervous system

F20 Schizophrenia: Schizophrenic conditions; Exacerbation of schizophrenia; Schizophrenia; Chronic schizophrenia; Dementia praecox; Bleuler's disease; Psychotic discordant; Dementia early; The febrile form of schizophrenia; Chronic schizophrenic disorder; Psychosis of the schizophrenic type; Acute form of schizophrenia; Acute schizophrenic disorder; Cerebral Organic Insufficiency in Schizophrenia; Acute attack of schizophrenia; Schizophrenic psychosis; Acute schizophrenia; Sluggish schizophrenia; Sluggish schizophrenia with apathoabulic disorders; Acute stage of schizophrenia with excitation

F28 Other Inorganic Psychotic Disorders: Affective psychoses; Involutional psychosis; Psychoinstrumental; Psycho senile; Senile psychosis; An old-time involutionary psychosis; Static psychosis

F29 Inorganic psychosis, unspecified: Childhood psychoses; Psychomotor agitation in psychoses; Hallucinatory-delusional disorders; Hallucinatory-delusional syndrome; Intoxication psychosis; Manic-delusional disorders; Manic chronic psychosis; Manic psychosis; Acute psychosis; paranoid psychosis; Paranoid psychosis; Subacute psychosis; Presenile psychosis; Psychosis; Intoxicating psychosis; Psychosis is paranoid; Psychosis in children; Reactive psychosis; Chronic psychosis; Chronic hallucinatory psychosis; Chronic psychosis; Chronic psychotic disorder; Schizophrenic psychosis

F31 Bipolar affective disorder: Mood disorders bipolar; Affective bipolar psychosis; Manic-melancholic psychosis; Intermittent psychosis; Circular psychosis; Cyclophrenia; Bipolar disorders; Bipolar psychosis; Affective insanity; Manic-depressive syndrome; Psycho Manic-Depressive; Depressive episode of bipolar disorder

F79 Mental retardation, unspecified: Mental retardation; Infantilism mental; Violation of mental activity; Oligophrenia; Lag behind mental development; Delayed development of intellectual abilities in children and adolescents; Slowed mental development in children; Maloumia; Oligopsihia; Mental failure; Impaired mental function; Mental retardation; Lack of intellectual development in children; Lack of mental development in children; Mental retardation; Lack of mental development in children; Mental retardation

G40.9 Epilepsy, unspecified: Refractory epilepsy in children; Absence; Psychomotor epilepsy; Epilepsy; Epileptiform cramps; Epileptiform syndrome; Epileptic syndrome; Anxiety seizures; Atypical absences

G50.0 Trigeminal neuralgia: trigeminal neuritis; Painful tic; Idiopathic neuralgia of the trigeminal nerve; Neuralgia of the trigeminal nerve; Essential neuralgia of the trigeminal nerve; Pain syndrome in trigeminal neuralgia; Painful tic; Trigeminal neuralgia; Neuralgia of the trigeminal nerve

G51 Lesions of the facial nerve: Neuralgia of the facial nerve; Neuritis of the facial nerve; Paralysis of the facial nerve; Pain syndrome with neuritis of the facial nerve; Peripheral paralysis of the facial nerve; Paresis of the facial nerve

G53.0 Neuralgia after shingles (B02.2 +): Postherpetic neuralgia; Postherpetic neuralgia in adults

R45.1 Anxiety and agitation: Agitation; Anxiety; Explosive excitability; Internal stimulation; Excitability; Excitation; Excitation acute; Psychomotor agitation; Hyperexcitability; Motor excitement; Cessation of psychomotor agitation; Nervous excitement; Restlessness; Night trouble; Acute stage of schizophrenia with excitation; Acute mental agitation; Paroxysm of excitation; Overexcitation; Increased excitability; Increased nervous excitability; Increased emotional and cardiac excitability; Increased agitation; Mental arousal; Psychomotor agitation; Psychomotor agitation in psychoses; Psychomotor agitation of an epileptic nature; Psychomotor paroxysm; Psychomotor fit; Symptoms of Excitation; Symptoms of psychomotor agitation; The state of agitation; A state of anxiety; Excitation status; A state of heightened concern; The state of psychomotor agitation; Conditions of anxiety; Excitation conditions; The state of excitement in somatic diseases; Excitation level; Feelings of anxiety; Emotional arousal

R52.9 Unspecified pain: Pain after cholecystectomy; Pain shooting; Non-malignant pain syndrome; Obstetric and gynecological pain; Pain syndrome; Pain syndrome in the postoperative period; Pain syndrome in the postoperative period after orthopedic operations; Painful syndrome of inflammatory genesis; Pain syndrome of non-oncological genesis; Pain syndrome after diagnostic procedures; Pain syndrome after the diagnostic intervention; Pain syndrome after operations; Pain syndrome after surgery; Pain syndrome after orthopedic surgery; Pain syndrome after trauma; Pain syndrome after removal of hemorrhoids; Pain syndrome after surgery; Pain syndrome with inflammation of non-rheumatic nature; Pain syndrome with inflammatory lesions of the peripheral nervous system; Pain syndrome in diabetic neuropathy; Pain syndrome in acute inflammatory diseases of the musculoskeletal system; Pain syndrome in the pathology of tendons; Pain syndrome with smooth muscle spasms; Pain syndrome with smooth muscle spasms (renal and biliary colic, intestinal spasm, dysmenorrhea); Pain syndrome with spasms of smooth muscles of internal organs; Pain syndrome with spasms of smooth muscles of internal organs (renal and biliary colic, intestinal spasm, dysmenorrhea); Pain syndrome with injuries; Pain syndrome with injuries and after surgery; Pain syndrome in chronic inflammatory diseases of the musculoskeletal system; Pain syndrome with duodenal ulcer; Pain syndrome with gastric ulcer; Pain syndrome with peptic ulcer of stomach and duodenum; Painful sensations; Pain during menstruation; Pain syndromes; Painful conditions; Painful leg fatigue; Gum pain when wearing dentures; The pain of exit points of cranial nerves; Painful irregular menstruation; Painful dressings; Painful muscular spasm; Painful growth of teeth; Pain in lower limbs; Pain in the area of the operating wound; Pain in the postoperative period; Pain in the body; Pain after diagnostic interventions; Pain after orthopedic surgery; Pain after surgery; Pain in the flu; Pain in diabetic polyneuropathy; Pain in burns; Pain in intercourse; Pain during diagnostic procedures; Pain during therapeutic procedures; Pain for colds; Pain with sinusitis; Pain in case of injury; Pain of a traumatic nature; Pain in the postoperative period; Pain after Diagnostic Interventions; Pain after sclerosing therapy; Pain after surgery; Postoperative pain; Postoperative and post-traumatic pain; Post-traumatic pain; Pain when swallowing; Pain in infectious and inflammatory diseases of the upper respiratory tract; Pain with burns; Pain with traumatic muscle damage; Pain in case of injury; Pain when extracting a tooth; Pain of traumatic origin; Pain caused by spasm of smooth muscles; Severe pain syndrome; Severe pain syndrome of traumatic origin; Postoperative pain; Postoperative pain syndrome; Post-traumatic pain; Post-traumatic pain syndrome; Torpid pain syndrome; Traumatic pains; Moderate pain; Moderately expressed pain syndrome; Moderate pain syndrome; Polyartralgia in polymyositis

Z100.0 * Anaesthesiology and premedication: Nasogastric intubation; Relaxation of skeletal musculature; Managed breathing in anesthesia; Anesthesia; Anesthesia in otorhinolaryngology practice; Anesthesia in dentistry; Arterial hypotension with spinal anesthesia; Ataralgesia; Basic anesthesia; Rapid anesthesia; Introduction to anesthesia; Induction Anesthesia; Inhalation anesthesia; Inhalation anesthesia for large and small surgical interventions; Induction and maintenance of general anesthesia; Intraligamentary anesthesia; Intubation of the trachea; Caudal anesthesia; Caudal blockade; Combined anesthesia; Short-term anesthesia; Short-term infiltration anesthesia in surgery; Short-term local anesthesia; Lumbar anesthesia; Local anesthesia; Local infiltration anesthesia; Local superficial anesthesia; Monocomponent anesthesia; anesthesia; Non-anional anesthesia in operative delivery; Immediate Anesthesia; General anesthesia; General anesthesia for short-term surgical interventions; General Anesthesia; Premedication period; Surface anesthesia in ophthalmology; Maintaining anesthesia; Premedication; Conduction Anesthesia; Regional anesthesia; Mixed anesthesia; Spinal anesthesia; Spinal-cerebral anesthesia; Terminal anesthesia; Epidural anesthesia; IVL; Artificial Hibernation; Short-term muscle relaxation; Muscle relaxation; Muscle relaxation during mechanical ventilation; Miorelaxation in surgical interventions; Muscle relaxation at operations; Muscle relaxation in ventilating; Excitation before surgery; Cardioplegia; Preoperative period

CAS Code

60-99-1

Characteristics of the substance Levomepromazine

The phenothiazine derivative. Yellowish white, slightly hygroscopic powder. Is unstable to light and air. Very soluble in water, alcohol, chloroform; almost nerastvorim on the air.

Pharmacology

Pharmacological action - analgesic, antipsychotic, neuroleptic, antiemetic.

It blocks dopamine receptors of various brain structures (including mesolimbic, mesocortical). Reduces the productive symptoms of psychosis - nonsense, hallucinations, psychomotor agitation. Has strong adrenoblocking, moderate anticholinergic and antihistamine properties. Has analgesic effect.

Quickly and fairly fully absorbed in any way of administration. Cmax is achieved 1-3 hours after oral administration and after 0.5-1.5 h after injection. It passes through the histohematological barriers, including the BBB, and is distributed in organs and tissues. Intensively biotransformed. The main active metabolite, N-desmethyl mono- metotrimeprazine, is further converted to monosulfoxide. T1 / 2 levomepromazina - 16-78 h. It is excreted mainly in the form of metabolites with urine and bile.

Application of Levomepromazine

Psychomotor agitation of various etiologies (with acute and chronic schizophrenia, bipolar disorder, psychoses, including senile, intoxication, oligophrenia, epilepsy), as well as other mental disorders that occur with agitation, anxiety, panic, phobias, persistent insomnia. Strengthening the action of analgesics, funds for general anesthesia, antihistamines). Pain syndrome with neuralgia of trigeminal and neuritis of the facial nerve, shingles.

Contraindications

Hypersensitivity, simultaneous reception of antihypertensive drugs; overdosage of drugs that cause inhibition of the central nervous system (alcohol, general anesthetics, hypnotics), closed angle glaucoma, urinary retention, Parkinson's disease, multiple sclerosis, myasthenia gravis, hemiplegia, chronic heart failure in decompensation stage, severe renal and / or hepatic insufficiency, severe arterial hypotension, oppression of bone marrow hematopoiesis, porphyria, pregnancy, breastfeeding, children under 12 years.

Restrictions on the use

Epilepsy, patients with a history of cardiovascular disease, especially in the elderly (impaired cardiac muscle conduction, arrhythmia, congenital QT interval prolongation syndrome).

Application in pregnancy and lactation

Do not use during pregnancy, except when the intended benefit to the mother exceeds the potential risk to the fetus. For the duration of treatment, breastfeeding should be stopped (levomepromazin penetrates into breast milk).

Side effects of Levomepromazine

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): decreased blood pressure, orthostatic hypotension, tachycardia, Morgagni-Adams-Stokes syndrome, prolongation of the QT interval (arrhythmogenic effect, tachycardia of the pirouette type) (see also "Restrictions on use "), Pancytopenia, agranulocytosis, leukopenia, eosinophilia, thrombocytopenia.

On the part of the nervous system and sensory organs: confusion, slurred speech, extrapyramidal symptoms with a prevalence of akinetic-hypotonic syndrome, epileptic seizures, increased intracranial pressure, neuroleptic malignant syndrome (NZS); with long-term use - deposits in the lens and cornea, pigmentary retinopathy.

On the part of the intestine: dry mouth, constipation, discomfort in the abdomen, nausea, vomiting, liver damage (jaundice, cholestasis).

Allergic reactions: laryngeal edema, peripheral edema, anaphylactoid reactions, bronchospasm, urticaria, exfoliative dermatitis.

Other: bleaching of urine, impaired urination, galactorrhea, menstrual irregularity, weight loss, increased photosensitivity, erythema, pigmentation, hyperthermia (may be the first sign of NCS), pain and swelling at the injection site. Some patients who have been receiving phenothiazines for a long time have described the development of pituitary adenoma, but further studies are needed to establish its causal relationship with these drugs.

Interaction

Incompatible with MAO inhibitors (increased risk of extrapyramidal disorders due to decreased inactivation of the drug in the liver) and hypotensive drugs (risk of orthostatic hypotension). Means that depress the central nervous system (narcotic analgesics, general anesthetics, anxiolytics, sedatives and hypnotics, tricyclic antidepressants), increase the inhibitory effect of the drug on the central nervous system.

Caution should be exercised when combined with anticholinergic drugs (tricyclic antidepressants, H1-histamine receptor blockers, some anti-Parkinsonian drugs, atropine, scopolamine, succinylcholine) due to increased anticholinergic effects (paralytic ileus, urinary retention, glaucoma). QT prolonging agents (antiarrhythmics, macrolides, antifungal azoles, cisapride, antidepressants, antihistamines, and diuretics that lower potassium levels) increase the risk of prolonging the QT interval and increase the risk of arrhythmia.

Levomepromazine reduces the antiparkinsonian activity of levodopa, the effectiveness of oral antidiabetic drugs. Antacids containing calcium, magnesium or aluminum, reduce absorption in the digestive tract (levomepromazin should be taken 1 hour before or 4 hours after taking antacid drugs). When combined with alcohol, inhibition of the central nervous system increases and the likelihood of extrapyramidal side effects increases.

Overdose

Symptoms: arterial hypotension, conduction abnormalities in the cardiac muscle (prolongation of the QT interval, ventricular pirouette tachycardia, atrioventricular blockade), depression of consciousness of varying severity (up to coma), extrapyramidal symptoms, sedative effect, epileptic seizures.

Treatment: resuscitation, symptomatic therapy. The specific antidote is unknown. Forced diuresis, hemodialysis and hemoperfusion are not effective.

Routes of administration

Inside, IM, IV.

Precautions for the substance Levemepromazine

It is necessary to change the injection site because of the possible local tissue reaction (IM injections are painful). It is recommended to systematically perform a general blood test and assess liver function, in elderly and weakened patients, blood pressure control is necessary. During the first 3-5 days of treatment after taking levomepromazine, regardless of dose and method of administration, the patient is recommended to lie 0.5-1 h in order to prevent orthostatic collapse. It should be borne in mind that with rapid increases in doses, especially in the elderly or in patients with vascular insufficiency, drug delirium may develop.

After a sudden discontinuation of the drug, used in high doses or for a long time, nausea, vomiting, headache, tremor, increased sweating, tachycardia, insomnia and anxiety, as well as the development of tolerance to the sedative effects of phenothiazines and cross tolerance to various antipsychotics. In this regard, the abolition of the drug should always be done gradually.

Many antipsychotics, incl. levomepromazine, can reduce the threshold of convulsive readiness and cause epileptiform changes in the EEG. Therefore, when selecting a dose in patients with epilepsy, clinical indicators and EEG should be constantly monitored.

The development of cholestatic jaundice depends on the individual sensitivity of the patient and completely disappears after discontinuation of the drug administration. Therefore, long-term treatment requires regular monitoring of liver function.

Do not use during work drivers of vehicles and people whose profession is associated with increased concentration of attention. In the period of treatment and within 4-5 days after stopping the intake of levomepromazine, the refusal of alcoholic beverages is mandatory.