Active substanceChlorpromazineChlorpromazine
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  • Aminazine®
    pills inwards 
    VALENTA PHARM, PAO     Russia
  • Aminazine
    solution w / m in / in 
    VALENTA PHARM, PAO     Russia
  • Aminazine®
    pills inwards 
    VALENTA PHARM, PAO     Russia
  • Chlorpromazine hydrochloride
    solution w / m in / in 
  • Dosage form: & nbspfilm coated tablets
    Composition:

    One tablet contains:

    Active substance: Chlorpromazine hydrochloride in terms of 100% of the substance - 25 mg, 50 mg or 100 mg.

    Excipients: potato starch - 20.65 mg, 41.30 mg or 82.60 mg, microcrystalline cellulose 35.00 mg, 70.00 mg or 140.00 mg, lactose monohydrate 15.00 mg, 30.00 mg or 60 , 00 mg, copovidone 0.35 mg, 0.70 mg or 1.40 mg, croscarmellose sodium 3.00 mg, 6.00 mg or 12.00 mg, magnesium stearate 1.00 mg, 2 , 00 mg or 4.00 mg. Sheath:

    for a dosage of 25 mg - Opadrai II 85F38209 - 4,00 mg: polyvinyl alcohol partially hydrolysed - 40,00%, macrogol-3350 - 20,20%, talc - 14,80%, titanium dioxide E 171 - 24,89%, iron dye oxide yellow E 172 - 0 ,eleven %;

    for a dosage of 50 mg - Opadrai II 85F240048 - 8,00 mg: polyvinyl alcohol partially hydrolysed - 40,00%, macrogol-3350 - 20,20%, talc - 14,80%, titanium dioxide E 171 - 22,70%, iron dye oxide red E 172-1 , 30%, iron dye oxide yellow E 172 - 0.80%, ferric oxide black oxide E 172 - 0.20%; for a dosage of 100 mg - Opadrai II 85F25509 - 16,00 mg: polyvinyl alcohol partially hydrolysed - 40,00%, macrogol-3350 - 20,20%, talcum - 14,80%,ferrous oxide red oxide E 172-20.20%, iron dye oxide black E 172-4.00%, iron dye oxide yellow E 172 0.80%.

    Description:

    Round biconvex tablets, coated with a white film with a yellowish tint of color (for a dosage of 25 mg), brownish-pink (for a dosage of 50 mg), from reddish-brown to brown (for a dosage of 100 mg). On the cross section, the nucleus is white or almost white in color.

    Pharmacotherapeutic group:antipsychotic agent (antipsychotic).
    ATX: & nbsp

    N.05.A.A.01   Chlorpromazine

    Pharmacodynamics:Chlorpromazine is a dimethylamine derivative of phenothiazine. Despite the fact that the exact mechanism of therapeutic effects of chlorpromazine is unknown, its main effect is the neuroleptic effect, which leads to a decrease in psychotic symptoms. Chlorpromazine has a sedative and antiemetic effect. It blocks alpha-adrenoreceptors and shows a weak anticholinergic effect. Chlorpromazine is a dopamine antagonist and stimulates the release of prolactin. Chlorpromazine blocks serotonin receptors and has weak antihistamine properties.It suppresses the center of thermoregulation, which violates the body's resistance to the equalization of body temperature with the ambient temperature.
    Pharmacokinetics:

    Chlorpromazine is well and rapidly absorbed when taken orally. Bioavailability after oral administration - 50%. More than 90% is bound by blood plasma proteins, therefore, it practically does not undergo hemodialysis. Quickly removed from the circulatory system and unevenly accumulated in various organs. Easily penetrates the blood-brain barrier, while its concentration in the brain exceeds the concentration in the plasma. There is no direct correlation between the concentrations in the blood plasma of chlorpromazine and its metabolites and the therapeutic effect.

    It has the effect of a "first pass" through the liver, where the drug is intensively metabolized as a result of oxidation (30%), hydroxylation (30%) and deamination (20%). Pharmacological activity is possessed by oxidized hydroxylated metabolites, which are inactivated by binding to glucuronic acid, or by further oxidation to form inactive sulfoxides. It is excreted by the kidneys and with bile. 1-6 % dose is excreted in the urine unchanged. The half-production period (T1 / 2) of chlorpromazine averages 30 hours. For a day, about 20% of the dose is taken. Traces of chlorpromazine metabolites can be detected in the urine after 12 months or more after discontinuation of treatment.

    Indications:

    Psychotic conditions (especially paranoid), including schizophrenia, mania and hypomania.

    As an auxiliary short-term therapy of anxious psychomotor agitation, violent or dangerous impulsive behavior.

    Contraindications:

    - increased individual sensitivity to the components of the drug;

    - lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

    - poisoning with substances depressing the central nervous system (CNS);

    - comatose conditions of any etiology;

    - oppression of bone marrow hematopoiesis;

    - pregnancy, the period of breastfeeding;

    - children under 12 years (for this dosage form).

    Carefully:

    Parkinson's disease, active alcoholism (the risk of developing hepatotoxic effects), breast cancer, epilepsy, chronic diseases,accompanied by respiratory failure (especially in children), Reye's syndrome, cachexia, old age, vomiting (the antiemetic effect of phenothiazines may mask vomiting associated with overdose of other drugs).

    Pregnancy and lactation:

    Application during pregnancy is contraindicated.

    Chlorpromazine penetrates the placental barrier, is excreted in breast milk, prolongs childbirth. Shown, that chlorpromazine causes embryo-fetal disorders in animals. There is information about the potential risk of developing extrapyramidal disorders and / or withdrawal syndrome in newborns whose mothers took the drug during the third trimester of pregnancy. When using chlorpromazine in high doses during pregnancy, in newborns in some cases, there were digestive disorders associated with atropine-like action of the drug (LS).

    If it is necessary to use the drug during lactation at the time of treatment

    to stop breastfeeding.
    Dosing and Administration:

    Tablets Aminazin® is prescribed inside (after eating), without chewing, squeezed with enough water.

    It is advisable to select the optimal dose individually. If the patient's clinical condition allows, then the treatment should begin with the minimum possible dose and gradually increase it.

    The initial daily intake for ingestion is 25-100 mg per day 1-4 times a day, then, taking into account tolerability, the dose is gradually increased by 25-50 mg every 3-4 days, until the desired therapeutic effect is achieved. In the case of ineffective medium doses of the drug Aminazin®, the dose is increased to 700-1000 mg per day, in some extremely resistant cases without somatic contraindications, the dose can be increased to 1200-1500 mg per day.

    When treated in large doses, the daily dose is divided into 4 parts (the last - before bedtime). Duration of treatment with large doses should not exceed 1-1.5 months, in the absence of effect, it is advisable to switch to treatment with other drugs.

    Higher doses of the drug Aminazin ® for adults inside: single 300 mg, daily 1500 mg.

    For children from 12 years, the drug Aminazin® is prescribed at 550 mcg / kg (0.55 mg / kg) or 15 mg per

    1 m2 of body surface if necessary every 6-8 hours. At a body weight of up to 46 kg, do not prescribe the drug Aminazin® at a dose of more than 75 mg per day.

    Weakened and elderly patients, depending on the age, appoint up to 300 mg per day.

    Side effects:

    From the central nervous system: extrapyramidal disorders (dystonic reactions, akinetorhidic phenomena, akathisia, hyperkinesia, tremor, autonomic disorders, symptoms of drug induced parkinsonism (hypokinesia, muscle rigidity, postural instability), early dyskinesia (paroxysmally arising cramps in the muscles of the neck, tongue, mouth cavity , oculogic crises), with long-term treatment - tardive dyskinesia (see the tactics of prevention of tardive dyskinesia in the section "Special instructions")), malignant neuroleptic syndrome (muscular igidnost, hyperthermia, somatic disorders caused by a dysfunction of the autonomic nervous system, psychiatric disorders), drowsiness, dizziness, sleep disorders, phenomena of psychic indifference, a belated reaction to external stimuli, anxiety, changes in the patient's mood, agitation, insomnia, depression, neuroleptic.

    From the cardiovascular system: orthostatic hypotension, tachycardia, heart rhythm disturbances (ventricular arrhythmias, including "fever" type, the risk of ventricular rhythm disturbances is higher against the background of the initial bradycardia, hypokalemia, elongated interval QT, heart diseases in the anamnesis, simultaneous administration of tricyclic antidepressants, in the elderly), lengthening of the interval QT, change of teeth T and U, venous thromboembolism (including pulmonary thromboembolism and deep vein thrombosis).

    On the part of the respiratory system: respiratory depression, nasal congestion.

    From the digestive system: nausea, vomiting, diarrhea, dry mouth, anorexia, constipation or bowel obstruction.

    From the hepatobiliary system: Cholestatic jaundice and liver damage (mostly cholestatic, hepatocellular or mixed); when jaundice occurs chlorpromazine should be canceled.

    From the genitourinary system: difficulty urinating, amenorrhea, oligomenorrhoea, impotence, frigidity, oliguria, priapism.

    From the endocrine system: hyperprolactinemia, galactorrhea, gynecomastia.

    From the hematopoiesis: increased blood coagulability, lympho- and leukopenia, anemia, agranulocytosis (regular blood screening is recommended (see section "Special instructions")).

    From the sense organs: clouding of the lens and cornea, disruption of accommodation.

    From the side of the coats: skin photosensitivity, skin pigmentation, melanosis.

    From the immune system: allergic reactions from the skin and mucous membranes, angioedema, facial edema, bronchospasm, urticaria, anaphylactic reactions, systemic lupus erythematosus.

    Other possible effects: the use of phenothiazine derivatives can lead to intolerance to glucose, hyperglycemia, hypercholesterolemia, fecal occlusion, severe intestinal obstruction, megacolon.

    Overdose:

    Symptoms: areflexia or hyperreflexia, blurred vision, cardiotoxic effects (arrhythmia, heart failure, lowering of arterial pressure (BP), shock, tachycardia, tooth change QRS, ventricular fibrillation, cardiac arrest), neurotoxic effects, including agitation, confusion, convulsions, disorientation, drowsiness,stupor or coma; mydriasis, dry mouth, hyperpyrexia or hypothermia, muscle stiffness, vomiting, pulmonary edema, or respiratory depression.

    Treatment: gastric lavage, the appointment of activated charcoal (avoiding the induction of vomiting, as impaired consciousness and dystonic reactions from the muscles of the neck and head due to overdose can lead to aspiration of vomit). Symptomatic treatment: with kollaptoidnyh states recommended the introduction of cordiamine, caffeine, mezatona; with the inhibition of the central nervous system without disrupting the function of the respiratory center - the introduction of moderate doses of phenamine, pervitina, caffeine-benzoate sodium (with oppression of the respiratory center, the use of analeptics is contraindicated); neurological complications usually decrease with a decrease in the dose of chlorpromazine, they can also be reduced by the appointment of trihexyphenidyl, antidepressants and psychostimulants are used to reduce neuroleptic depression; when arrhythmia - the introduction of long-acting drugs, with heart failure - cardiac glycosides, with a marked decrease in blood pressure - intravenous fluid or vasopressormeans, such as norepinephrine, phenylephrine (avoid the appointment of alpha and beta-adrenomimetics, such as epinephrine, since a paradoxical decrease in blood pressure is possible due to the blockade of alpha-adrenergic receptors with chlorpromazine), with convulsions - diazepam (avoid the appointment of barbiturates, due to possible subsequent depression of the central nervous system and respiratory depression); in the case of hyperthermia, which is one of the symptoms of a malignant neuroleptic syndrome - the introduction of dantrolene. Control of cardiovascular function for at least 5 days, CNS function, respiration, body temperature measurement, psychiatrist consultation. Dialysis is ineffective.

    Interaction:

    With the simultaneous use of the drug Aminazin ® with other drugs that have a depressing effect on the central nervous system (funds for general anesthesia, narcotic analgesics, ethanol (alcohol) and containing drugs, barbiturates, tranquilizers, etc.), it is possible to increase the depression of the central nervous system, as well as respiratory depression.

    Barbiturates can reduce the concentration of chlorpromazine in the blood serum. Undesirable long-term combination with analgesics and antipyretics - it is possible the development of hyperthermia.

    The administration of chlorpromazine together with tricyclic antidepressants, maprotiline or monoamine oxidase (MAO) inhibitors increases the risk of neuroleptic malignant syndrome;

    The phenothiazine derivatives are antagonists of the action of epinephrine and other simporomimetics and antiepileptic drugs (lowering the threshold of convulsive alertness).

    When using chlorpromazine in combination with drugs for the treatment of hyperthyroidism, the risk of developing agranulocytosis increases.

    When chlorpromazine is used in combination with drugs that cause extrapyramidal reactions, it is possible to increase the incidence and severity of extrapyramidal disorders. The phenothiazine derivatives increase the hypotensive effect of agents for anesthesia, blockers of "slow" calcium channels and other antihypertensive agents and trazodone. Chlorpromazine reduces the hypotensive effect of neuronal adrenoblockers, such as guanethidine, the effects of amphetamines, clonidine.

    With the simultaneous use of chlorpromazine and angiotensin-converting enzyme (ACE) inhibitors, severe orthostatic hypotension occurs.

    The simultaneous use of beta-blockers and chlorpromazine increases the risk of arterial hypotension, including orthostatic, due to the summation of the vasodilating effect of chlorpromazine and a decrease in cardiac output caused by beta-blockers.

    The simultaneous use of beta-blockers and chlorpromazine increases the risk of developing irreversible retinopathy, tardive dyskinesia.

    Simultaneous use of chlorpromazine with antiarrhythmic drugs of Class 1a and III, beta blockers, some calcium channel blockers, LS digitalis, pilocarpine, anticholinesterase drugs may be accompanied by bradycardia and an increased risk of ventricular arrhythmia, including pirouette. When these drugs are combined with chlorpromazine, ECG monitoring is recommended.

    Simultaneous use of chlorpromazine with nitrates increases the risk of orthostatic hypotension due to an increased vasodilator effect.

    The simultaneous use of chlorpromazine with thiazide diuretics contributes to the intensification of hyponatremia.

    The simultaneous use of chlorpromazine with bromocriptine increases the concentration of prolactin in the plasma and prevents the action of bromocriptine.

    Simultaneous use with antimuscarinic drugs may aggravate the development of anticholinergic side effects (urinary retention, acute glaucoma attack provocation, dry mouth, constipation, etc.). Anticholinergic properties have different drugs atropine, tricyclic antidepressants, H1-histamine blockers, antimuscarinic, antiparkinsonian anticholinergic antispasmodics, dysopiramid, phenothiazine antipsychotics and clozapine.

    When chlorpromazine is used in combination with ephedrine, the vasoconstrictive effect of ephedrine may be reduced.

    When treating with the drug Aminazin®, the introduction of epinephrine should be avoided, since the effect of epinephrine may be distorted, which can lead to a drop in blood pressure. The use of epinephrine in case of an overdose is not allowed.

    Chlorpromazine reduces the antiparkinsonian effect of levodopa (due to the blockade of dopamine receptors).

    Chlorpromazine has a moderate anticholinergic activity, which can be increased by other anticholinergic drugs. Aminazine® also enhances the anticholinergic effects of other drugs, while its own antipsychotic effect may decrease.

    With the simultaneous use of chlorpromazine with a prochlorperazine related to the chemical structure, a prolonged loss of consciousness may occur.

    Antacids, anti-Parkinsonian drugs and lithium salts can reduce the absorption of chlorpromazine. Antacids should not be used two hours before and after using the drug Aminazine ©.

    Chlorpromazine causes increased renal excretion of lithium, in addition, the combination with lithium drugs increases the risk of extrapyramidal complications.

    Chlorpromazine can mask some manifestations of ototoxicity (tinnitus, dizziness) of drugs that have ototoxic effects (for example, antibiotics with ototoxic effect).

    Other hepatotoxic drugs increase the risk of hepatotoxicity.

    Means that inhibit bone marrow hematopoies increase the risk of myelosuppression. With the simultaneous use of chlorpromazine with antimalarial drugs, the concentration of chlorpromazine in the blood plasma increases with the risk of developing toxic effects.

    With the simultaneous use of chlorpromazine with cimetidine, a change (increase or decrease) in the concentration of chlorpromazine inblood plasma.

    When combined with hypoglycemic preparations chlorpromazine in high doses (100 mg / day) weakens the hypoglycemic effect by reducing the secretion of insulin and increasing blood glucose (see section "Special instructions").

    Special instructions:

    During treatment it is necessary to carry out regular monitoring of blood pressure, pulse, liver and kidney function. It is also necessary to monitor the blood picture (at the beginning of the week, and then every 3-4 months); if during therapy, the number of white blood cells decreases to 3.0 - 3.5x109 / L, and the number of neutrophils decreases to 1.5 - 2.0x109 / l, these should be monitored 2 times a week; In the case of leukocytosis and granulocytopenia, treatment should be interrupted.

    Each patient should be informed that with an increase in temperature, sore throat or other manifestations of infectious diseases, he should immediately notify the attending physician. In the case of hyperthermia, which may be one of the symptoms of a malignant neuroleptic syndrome (pallor, hyperthermia, autonomic dysfunction, changes in consciousness, rigidity of muscles), the drug Aminazin® should be immediately discontinued.Early manifestations preceding the onset of hyperthermia may include side effects such as increased sweating and unstable blood pressure (BP). Although the etiology of such side effects is usually unknown, there are a number of risk factors: individual predisposition, dehydration, organic brain damage. Malignant neuroleptic syndrome can occur at any time during treatment with neuroleptics and lead to death.

    In case of signs and symptoms of tardive dyskinesia, consideration should be given to reducing the dose or canceling all antipsychotic medications. Late dyskinesia sometimes occurs after the withdrawal of the neuroleptic and disappears with repeated admission or with an increase in dosage. The appointment with the development of tardive dyskinesia antiparkinsonic and anticholinergic drugs is contraindicated (possibly worsening of the condition).

    As correctors of extrapyramidal disorders, the occurrence of which is possible with the use of the drug Aminazin®, antiparkinsonian agents are used - trihexyphenidyl and others.

    Aminazine ®, depending on the dose, may enhance the lengthening of the interval QT, which increases the risk of ventricular arrhythmias, including the "pirouette" type. Bradycardia, hypokalemia, congenital or acquired long QT-period. Therefore, before starting treatment, you need to make sure of the absence:

    -bradicardia below 55 beats per minute;

    -hypokalemia;

    -related interval elongation QT.

    Except for emergency situations, it is recommended that an ECG be performed during a preliminary examination of patients requiring treatment with an antipsychotic.

    In randomized clinical trials, in elderly patients with dementia versus placebo with the use of atypical antipsychotics (LS), there was an increased risk of stroke compared with placebo. The mechanism of occurrence of such an increased risk is not known. The increased risk of taking other neuroleptics or in other age groups can not be ruled out. Aminazine ® should be used with caution in patients with risk factors for stroke, elderly patients with dementia,since the risk of mortality increases in elderly patients with psychoses associated with dementia and receiving antipsychotic medications. Placebo-controlled trials, which were conducted mainly in patients taking atypical antipsychotic drugs, showed an increased risk of mortality of 1.6 -1.7 times compared with placebo. At the end of the treatment, with an average duration of 10 weeks, the mortality risk was 4.5% in the group receiving chlorpromazine, compared with 2.6% in the placebo group. Although the causes of death in clinical studies with atypical antipsychotic drugs were diverse, most of these deaths were due to cardiovascular problems (eg, heart failure, sudden death) or infections (eg, pneumonia).

    There is a risk of venous thromboembolism (VTE) in the treatment of neuroleptics. In patients receiving antipsychotic drugs, especially those with acquired VTE risk factors, preventive measures should be taken and any potential risk factor for VTE should be evaluated before and during treatment with the drug Aminazin®.

    In addition to exceptional circumstances, Aminazine® should not be used in Parkinson's disease.

    The occurrence of intestinal obstruction, which can be detected by swelling and abdominal pain, requires urgent care.

    Predisposing factors in the development of arrhythmia with the drug Aminazin® are: hypokalemia (including the use of diuretics that cause hypokalemia), bradycardia (including caused by drugs), the existing (congenital or acquired) increase in the duration of the interval QT. It is not recommended simultaneous administration of chlorpromazine with dopaminergic non-antiparkinsonian drugs (cabergoline, quinagolide) due to the mutual antagonism of dopamine agonists and neuroleptics. It is not recommended simultaneous use with other neuroleptics, which can cause arrhythmia of the type "pirouette" (amisulpride, cyamemazine, droperidol, fluphenazine, prepericasin, haloperidol, levomepromazine, pimozide, pipamperone, pipotiazine, sertindole, sulpiride, sultopride, tiapride). It is not recommended simultaneous use with antiparasitic agents (halofantrine, lumefantrine, pentamidine).Also, simultaneous use with antifungal agents from the azole group is not recommended (an increased risk of arrhythmia). If it is not possible to avoid the joint assignment of the above combinations, it is recommended to conduct regular ECG monitoring with monitoring the duration of the interval QT. When using non-potassium-sparing diuretics before starting therapy with chlorpromazine, correction of hypokalemia and ECG monitoring are necessary.

    Monitoring during treatment with the drug Aminazin® should be strengthened:

    patients with epilepsy and seizures in the anamnesis, in connection with the possibility of reducing the convulsive threshold. The occurrence of seizures requires the cessation of treatment.

    elderly patients with:

    a) high susceptibility and the effect of orthostatic hypotension (increased risk of excessive sedation and hypotensive effect),

    b) chronic constipation (risk of paralytic intestinal obstruction),

    c) possible hypertrophy of the prostate gland;

    - in patients with cardiovascular diseases receiving quinidine, in connection with the possible intensification of hypotensive action;

    - in the case of hepatic insufficiency and / or severe renal failure, due to the risk of accumulation.

    With prolonged treatment, regular ophthalmic control is recommended. It will be appreciated that the use of phenothiazine derivatives may lead to hyperglycemia or impaired glucose tolerance, development or aggravation of diabetes mellitus, hypercholesterolemia, fecal occlusion, severe intestinal obstruction and megacolon.

    Since in high doses (100 mg / day) chlorpromazine can cause an increase in blood glucose levels by reducing the secretion of insulin, in patients with diabetes it is necessary to adjust the dose of insulin before and after the completion of the course of therapy. If necessary, the dose of neuroleptic in patients taking sulfonylureas should also be adjusted.

    Chlorpromazine should not be used in monotherapy with a predominance of depression.

    With caution apply Aminazin® with hypersensitivity to other drugs phenothiazine series, severe respiratory diseases.

    Due to the risk of photosensitivity, UV light should be avoided.

    Aminazine ® may worsen the course or contribute to the manifestation of a latent myasthenia gravis gravis, and also cause a myasthenic syndrome.

    To avoid the development of the "withdrawal" syndrome, discontinuing treatment with the drug Aminazin® should be gradual.

    It is necessary to take into account the mutual antagonism of levodopa and antipsychotics. Dopamine can cause or exacerbate psychotic disorders. For the treatment of patients suffering from Parkinson's disease, it is necessary to use the minimum effective doses of both drugs. In case of necessity of treatment by neuroleptics of patients with parkinsonism who received dopamine, the dose of the latter should be reduced gradually to a minimum (abrupt withdrawal of dopamine may increase the risk of developing "malignant neuroleptic syndrome").

    In patients with pheochromacetoma, taking Aminazin®, false positive results of the level of catecholamines in the blood can be observed.

    For the duration of therapy, it is necessary to refrain from drinking alcohol, since chlorpromazine enhances the depressant effect of alcohol on the central nervous system.

    Influence on the ability to drive vehicles and control mechanisms:

    During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    tablets, film-coated 25 mg, 50 mg and 100 mg

    Packaging:

    For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    1, 2 or 3 contour cell packs (for a dosage of 25 mg); 1 or 3 contourcell packs (for dosages of 50 mg and 100 mg), together with the instructions for use, are placed in a pack of cardboard.
    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.
    Shelf life:

    2 years. Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002617
    Date of registration:08.09.2014
    The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp29.09.2015
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