The drug "Aminazin": reviews from doctors, instructions for use, composition and description. Aminazine - instructions for use For impaired renal function
The drug "Aminazine" is available in the form of dragees, tablets and injection solution.
The tablets are film-coated with a reddish-brown hue, each of them contains 25, 50 or 100 mg of the active substance - chlorpromazine hydrochloride. On a cross section, the tablet is white or almost white. The drug also contains potato starch, lactose monohydrate, stearate and a number of other excipients. The tablets are packaged in contour cells, in a pack - 10 or 20 pieces.
The composition of the pills, in addition to 25, 50 or 100 mg of chlorpromazine hydrochloride, includes sucrose, starch syrup, gelatin, wax, talc, titanium dioxide and sunflower oil. Dragees are produced in cardboard packs of 10, 30, 50 and 100 pieces. (in contour cells) or polymer cans of 1600, 2285 and 3200 pcs.
The injection solution is available in ampoules of 1, 2, 5 and 10 ml; it also contains additional components, in particular anhydrous sodium sulfate and ascorbic acid. 1 ml of solution contains 25 mg of chlorpromazine hydrochloride.
pharmachologic effect
The antipsychotic drug "Aminazin", belonging to the neuroleptics, has a pronounced sedative effect. The drug can significantly reduce the intensity or completely eliminate hallucinations and/or delusions, stop psychomotor agitation, reduce the level of manifestation of affective reactions, restlessness and anxiety, as well as motor activity.
The therapeutic effect of the drug is due to the ability of Aminazin to block postsynaptic dopaminergic receptors in the mesolimbic structures of the brain, as well as its blocking effect on α-adrenergic receptors, suppressing the release of pituitary and hypothalamic hormones. At the same time, as a result of blockade of dopamine receptors, the level of prolactin secretion by the pituitary gland increases.
Aminazine also has a central antiemetic effect, which is associated with inhibition or blockade of dopamine D2 receptors in the chemoreceptor trigger zone of the cerebellum. The peripheral antiemetic effect is due to blockade of the vagus nerve in the gastrointestinal tract. The antiemetic effect is probably enhanced by the anticholinergic, sedative and antihistamine properties of the drug.
It is assumed that the sedative effect of Aminazin is due to the alpha-adrenergic blocking activity of the active substance, which at the same time has a moderate or weak extrapyramidal effect.
Pharmacokinetics
Chlorpromazine after oral administration is absorbed from the gastrointestinal tract quite quickly, but sometimes not in full. The drug concentration level usually reaches its maximum levels 2-4 hours after administration.
Taking into account the “first pass” effect of the drug through the liver, the plasma concentration after taking tablets or pills is less than after intramuscular administration. The drug is intensively metabolized in the liver, forming both active and inactive metabolites.
More than 95% of chlorpromazine is bound to plasma proteins, widely distributed in the body and penetrates the blood-brain barrier. The level of the drug in the brain is higher than in plasma.
It is important to consider that pharmacokinetic parameters may vary within the same patient. However, there is no direct correlation between plasma concentrations of chlorpromazine and its metabolites and the therapeutic effect.
The half-life of chlorpromazine is usually about 30 hours. It is assumed that the elimination of drug metabolites requires a longer period. long-term
“Aminazine” leaves the patient’s body through the kidneys and is also excreted in the bile in the form of metabolites.
Indications
The medicine is used:
- with prolonged paranoid and hallucinatory states, psychomotor innervation, alcoholic psychosis, manic hallucinations that occur against the background of delirium, depressive psychosis and other mental disorders of an endogenous nature, manifesting mainly in young and mature age and occurring in a cyclical form;
- for vomiting in pregnant women and Meniere's disease - as an effective antiemetic drug;
- for the treatment of chlorethylamine in cancer;
- for itchy dermatoses and similar pathological conditions.
"Aminazine" is also prescribed for the following purposes:
- premedication and potentiated anesthesia;
- artificial hypothermia (as part of lytic mixtures that are administered intravenously or intramuscularly).
Indications for the use of Aminazin are also considered:
- agitated depression, combined with presenile psychosis;
- neurotic diseases with a further increase in muscle tone;
- persistent pain, including causalgia (the drug is used in combination with analgesics); persistent sleep disturbances (the drug is used in combination with sleeping pills and tranquilizers).
Dosage, regimen and duration of treatment
A single dose for adult patients is usually from 10 to 100 mg, the maximum daily dose should not exceed 600 mg.
For children aged 1-5 years, the dosage is calculated according to the formula - 500 mcg per kg of body weight, taking into account administration every 4-6 hours.
For children over five years of age, in standard cases the adult dosage is halved or tripled, depending on age, indications and general condition.
When administered intramuscularly or intravenously to adult patients, the initial dose is 25 to 50 mg. For children older than one year, the drug is administered in a single dosage, calculated according to the formula - 250-500 mcg per kg of body weight.
Regardless of the dosage form, the dosage of the drug and the frequency of its use are determined by the attending physician on an individual basis.
The maximum single dosage for adult patients is:
- 300 mg orally;
- 150 mg for intramuscular administration;
- 100 mg intravenously.
Side effect
Among the most common undesirable effects that occur when prescribing Aminazin are:
- from the central nervous system: akathisia, blurred vision, less often - dystonic extrapyramidal reactions, thermoregulation disorders, development of neuroleptic malignant syndrome (NMS);
- from the cardiovascular system: arterial hypotension (especially with intravenous administration of the drug) and tachycardia;
- from the gastrointestinal tract: dyspeptic manifestations are likely, much less often - the development of cholestatic jaundice;
- from the hematopoietic system: leukopenia and agranulocytosis (rarely);
- from the urinary system: difficulty urinating (rarely);
- from the endocrine system: gynecomastia, impotence, menstrual irregularities, weight gain.
Allergic reactions, expressed in skin itching and rashes, are possible.
Much more rarely, when using Aminazin, exfoliative dermatitis, erythema multiforme, photosensitivity and other dermatological manifestations are observed.
Contraindications for use
The drug "Aminazin" is not used in the following cases:
- liver and/or kidney dysfunction;
- diseases of the hematopoietic organs;
- progressive systemic diseases of the brain and spinal cord;
- myxedema;
- diseases of the cardiovascular system in severe forms;
- thromboembolic disease;
- bronchiectasis (in late stages);
- angle-closure glaucoma;
- urinary retention occurring against the background of prostatic hyperplasia;
- severe depression of the central nervous system and coma;
- traumatic brain damage.
Use during pregnancy and breastfeeding
The drug prescribed during pregnancy must be used in the lowest possible doses. In addition, the duration of treatment should be limited. At the end of pregnancy, it is recommended to reduce the dosage of Aminazine.
It must be taken into account that the drug can have a prolonged effect on childbirth.
During treatment with Aminazine, breastfeeding should be stopped, since chlorpromazine and its metabolites, crossing the placental barrier, are excreted in breast milk.
Clinical studies have shown that chlorpromazine can have a teratogenic effect. The use of Aminazine in high doses during pregnancy could cause digestive disorders in newborns, which are associated with an atropine-like effect, as well as the formation of extrapyramidal syndrome.
Antipsychotic drugs are psychotropic drugs that are intended to treat psychotic disorders. It should be especially noted that the traditional name for such drugs is antipsychotics. These medications can effectively influence symptoms such as delusions, illusions, hallucinations, thinking disorders, psychotic agitation, etc. Only an experienced doctor can prescribe such drugs.
The most popular antipsychotic drug is the drug Aminazine. Instructions for use, price, reviews, analogues, contraindications and indications for the drug are presented below.
Composition, description, form
What form is inherent in the medicine "Aminazin"? Instructions and reviews report that this drug goes on sale in the form of a brown-pink dragee, as well as a solution for intravenous and intramuscular administration. The active substance of these drugs is chlorpromazine hydrochloride. Also, depending on the form of release, they contain various auxiliary elements.
Pharmacological features
What is remarkable about the drug “Aminazin”? Instructions for use, reviews indicate that this is an antipsychotic drug, which in its pharmacological group belongs to antipsychotics. It has hypotensive, antiemetic and antihistamine effects.
The active ingredient of this medication is In addition to the listed properties, this medication has sedative, weak hypothermic, antipsychotic, local irritant, vasodilating and moderate M-anticholinergic effects.
The antipsychotic effect of this drug is achieved by blocking dopamine D2 receptors of the mesolimbic and mesocortical systems. Thanks to these properties, the drug in question is able to eliminate hallucinations, delusions and other productive symptoms of psychosis.
It should also be noted that Aminazin, reviews of which are given below, stops various types of psychomotor agitation, reduces the severity of aggressiveness and psychotic fear.
The sedative effect of this medicine is achieved by blocking the adrenergic receptors of the reticular pharmacy, which are located in the brain stem.
Properties of the drug
What properties are inherent in the drug "Aminazin"? Reviews report that this drug has a depressing effect on conditioned reflex work, relaxes skeletal muscles, reduces the spontaneity of motor activity, and reduces sensitivity to endogenous and exogenous stimuli with stable consciousness. Using large dosages of this medication causes severe drowsiness.
Blockade of the vagus nerve in the gastrointestinal tract and dopamine D2 receptors located in the trigger zone and vomiting center provides the antiemetic effect of the drug. It should also be noted that this drug has a weak effect on M-cholinergic receptors. In addition, its pronounced effect is noted in relation to alpha-adrenergic receptors.
Action of the medication
How does the drug "Aminazin" work? Reviews say that this remedy can completely eliminate the effects that were caused by epinephrine. Its hypothermic effect is due to the blockade of dopamine receptors located in the hypothalamus.
The drug in question lowers blood pressure, increases heart rate, has a weak antihistamine effect and a pronounced cataleptogenic effect, and also reduces the permeability of capillary walls.
When administered intramuscularly, this medication causes a sedative effect within ¼ hour, and when taken orally, after 120 minutes. Patient tolerance to the sedative and hypotensive effects develops after approximately one week.
When this medication is taken orally, its antipsychotic properties become apparent on the 4th or 7th day. The therapeutic effect of this drug lasts about 2-6 months.
Pharmacokinetics of the drug
Is Aminazine absorbed? Reviews report that when taken orally, chlorpromazine is quickly but not completely absorbed from the digestive system. Its peak concentration in the blood is reached after 4 hours.
This drug undergoes a first pass through the liver. Therefore, its concentration in the blood after oral administration is much lower than the concentration after intramuscular administration.
This medicine is metabolized in the liver with the formation of inactive and active derivatives.
Chlorpromazine is highly bound to plasma proteins. It is widely distributed in the patient's body, penetrating the BBB.
The half-life of the active substance of this medicine is approximately 30 minutes. In this case, the elimination of its derivatives may take longer.
The medication in question is excreted along with urine and bile.
The drug "Aminazin": indications for use
Reviews report that this drug is actively used in psychiatric practice. It is prescribed for the treatment of psychomotor agitation in a person with schizophrenia. This medicine is also used for chronic delusional states, hypomanic agitation, insomnia, psychopathy, mental illness, anxiety, fear and anxiety.
In addition to the listed conditions, indications for the use of this medicine are: persistent hiccups, alcoholic psychosis, and severe nausea. In the presence of pain, this drug enhances the effect of analgesics.
It should also be noted that the drug in question is prescribed for diseases that are accompanied by increased muscle tone, tetanus (as a combination therapy together with barbiturates) and after suffering disorders in cerebral circulation.
Not long ago, this drug was used for artificial hypothermia as part of In anesthesiology, this medication is often prescribed for premedication and potentiation of general anesthesia.
In dermatological practice, Aminazine (patient reviews of this medicine are predominantly positive) is used for itchy dermatoses. In addition, it can be used in the treatment of acute porphyria.
Contraindications
In what cases is the antipsychotic drug Aminazine not prescribed? Reviews from doctors report that this remedy is not used for comatose states of any origin, as well as for severe depression of the nervous system, severe pathology of the heart and blood vessels, intolerance to the active substance, progressive diseases of the brain and spinal cord of a systemic nature, ulcerative lesions of the gastrointestinal tract and during breastfeeding. feeding.
Due to the high risk of developing hepatotoxic reactions, this drug is prescribed with extreme caution for alcoholism. The same applies to breast cancer, pathological changes in the blood, prostatic hyperplasia, closed-angle glaucoma, Parkinson's disease, epilepsy, myxedema, vomiting, cachexia, Reye's syndrome and old age.
The drug "Aminazin": instructions for use
The tablets, reviews of which are presented below, are used in psychiatric practice in an initial daily dosage of 25-100 mg. This amount is divided into 1-4 doses. Over time, the dose is increased every four days by 25 or 50 mg until the desired effect is achieved.
In case of anxiety before surgery, this drug is taken 2-3 hours before surgery.
The maximum single dosage of this drug is 300 mg, and the daily dosage is 1.5 g.
As for the solution, it is administered intravenously or intramuscularly. The initial dosage of this medicine is 25-50 mg.
Before administering the drug, it is diluted with 2-5 ml of sodium chloride solution or procaine solution. Injections are given deep intramuscularly.
The maximum single dosage of this drug is 150 mg, and the daily dosage is 1 g. As for intravenous administration, these values correspond to 100 and 250 mg.
Undesirable effects
Does Aminazine (tablets) cause side effects? Reviews report that in the first stages of treatment, this medication can provoke dry mouth, accommodation paresis, frigidity, increased drowsiness, constipation, sleep disturbance, dizziness, appetite disturbance, tachycardia, a severe form of orthostatic hypotension, urinary retention, decreased potency, allergies and falls. blood pressure.
Long-term therapy with this drug causes muscle cramps in the neck and tongue, neuroleptic depression, akineto-rigid phenomena, extrapyramidal disorders, amenorrhea, akathisia, delayed reaction to various stimuli, hypercoagulation, vomiting, mental changes, heart rhythm disturbances, skin pigmentation, inhibition of bone marrow hematopoiesis , gynecomastia, cholestatic jaundice, galactorrhea, hyperplolactinemia, oliguria, diarrhea and With intravenous infusion, phlebitis is formed, and with intramuscular infusion, infiltrates are formed.
Therapy with this drug requires careful monitoring of blood pressure, pulse, kidney and liver function.
This drug may cause photosensitivity, and therefore it is recommended to avoid exposure to radiation while taking it.
Analogues and cost
The price of this medicine depends on its release form. A pack of 10 ampoules can be purchased for 60 rubles, and a similar number of tablets costs about 150 rubles.
Analogs of this medication include Chlorpromazine Hydrochloride and Tizercin.
Dosage form
Solution for injection, 2.5%, 2 ml
Compound
1 ml of solution contains
active substance- aminazine (chlorpromazine hydrochloride) in terms of 100% substance 25 mg,
Excipients: sodium sulfite anhydrous (E 221), sodium metabisulfite (E 223), ascorbic acid, sodium chloride, water for injection
Description
Transparent, colorless or slightly yellowish-greenish liquid
Pharmacotherapeutic group
Psychotropic drugs. Neuroleptics. Phenothiazines with an aliphatic group. Chlorpromazine.
ATX code N05A A01
Pharmacological properties
Pharmacokinetics
Aminazine is found in the blood in small quantities 15 minutes after administration of a therapeutic dose and circulates for 2 hours. It has a high connection with plasma proteins (95 - 98%) and a degree of distribution in the body, penetrates the blood-brain barrier, and its concentration in the brain is higher than in plasma. The half-life of the drug is about 30 hours. Intensively metabolized in the liver with the formation of a number of active and inactive metabolites. Excreted in urine, feces, and bile.
Pharmacodynamics
Neuroleptic of the group of phenothiazine derivatives. It has a pronounced antipsychotic, sedative and antiemetic effect. Reduces or completely eliminates delusions and hallucinations, stops psychomotor agitation, reduces affective reactions, anxiety, restlessness, and reduces motor activity. The mechanism of antipsychotic action is associated with blockade of postsynaptic dopaminergic receptors in the mesolimbic structures of the brain. It also has a blocking effect on alpha-adrenergic receptors and suppresses the release of pituitary and hypothalamic hormones. However, blockade of dopamine receptors increases the secretion of prolactin by the pituitary gland. The antiemetic effect is associated with inhibition or blockade of dopamine D2 receptors in the chemoreceptor trigger zone of the cerebellum, and the peripheral effect is associated with blockade of the vagus nerve in the digestive tract. The sedative effect is associated with the blockade of central adrenergic receptors. Has a moderate or weak effect on extrapyramidal structures.
Indications for use
Chronic paranoid and hallucinatory-paranoid states
States of psychomotor agitation in patients with schizophrenia (hallucinatory-delusional, hebephrenic, catatonic syndromes)
Alcohol psychosis
Manic agitation in patients with manic-depressive psychosis
Mental disorders in patients with epilepsy
Agitational depression in patients with presenile psychosis
Manic-depressive psychosis, as well as other diseases that are accompanied by agitation and tension
Neurotic diseases that are accompanied by increased muscle tone
Persistent pain, including causalgia (in combination with analgesics)
Persistent sleep disorders (in combination with sleeping pills and tranquilizers)
Meniere's disease
Vomiting of pregnancy
Treatment and prevention of vomiting during treatment with antitumor drugs and radiation therapy
Dermatous itching
As part of “lytic mixtures” in anesthesiology
Directions for use and doses
The drug is prescribed intramuscularly and intravenously. The doctor sets doses and treatment regimens individually depending on the indications and condition of the patient. When administered intramuscularly, the highest single dose is 150 mg, the daily dose is 600 mg. Usually 1 - 5 ml of a 2.5% solution is administered intramuscularly no more than 3 times a day. The course of treatment is several months, in high doses - up to 1.5 months, then they switch to treatment with maintenance doses, gradually reducing the dose by 25 - 75 mg per day. In case of acute mental agitation, 100 - 150 mg (4 - 6 ml of a 2.5% solution) is administered intramuscularly or 25 - 50 mg intravenously (1 - 2 ml of a 2.5% solution of Aminazine is diluted in 20 ml of a 5% or 40% glucose solution) , if necessary, 100 mg (4 ml of 2.5% solution in 40 ml of glucose solution). Enter slowly. When administered intravenously, the highest single dose is 100 mg, daily dose is 250 mg.
When administered intramuscularly or intravenously for children over 1 year of age, a single dose is 250 - 500 mcg/kg body weight; for children over 5 years of age (body weight up to 23 kg) - 40 mg per day, 5 - 12 years (body weight - 23 - 46 kg) - 75 mg per day.
Weakened patients and elderly patients are prescribed up to 300 mg per day intramuscularly or up to 150 mg per day intravenously.
Side effects
If solutions get on mucous membranes, on the skin and under the skin, tissue irritation occurs; after intramuscular injection, a painful infiltrate often appears at the injection site; when administered intravenously, damage to the vascular endothelium is possible. To prevent these phenomena, Aminazin solution is diluted with solutions of novocaine, glucose, and 0.9% sodium chloride solution.
With long-term use in high doses, chlorpromazine may be deposited in the anterior structures of the eye (cornea and lens), which can accelerate the natural aging process of the lens.
Arterial hypotension (especially with intravenous administration)
Tachycardia
Cholestatic jaundice
Nausea
Menstrual irregularities
Impotence
Gynecomastia, galactorrhea
Weight gain
Possible skin rashes
With prolonged use, the development of neuroleptic syndrome is possible:
Parkinsonism
Akathisia
Mental indifference and other mental changes
Delayed reaction to external stimuli
Blurred vision
Rarely:
Dystonic extrapyramidal reactions
Tardive dyskinesia
Neuroleptic depression
Violation of thermoregulation
Neuroleptic malignant syndrome
Leukopenia
Agranulocytosis
Difficulty urinating
Exfoliative dermatitis
Erythema multiforme
Skin pigmentation
Photosensitivity
Very rarely:
Angioedema
Bronchospasm
Hives
Systemic lupus erythematosus
Galactorrhea
Insomnia
Excitation
ECG changes: prolongation of the QT interval, ST-segment depression, changes in T and U waves
Arrhythmia
Dry mouth
Priapism
In single cases:
Convulsions
Contraindications
Do not prescribe simultaneously with barbiturates, alcohol, or narcotic drugs.
Increased individual sensitivity to chlorpromazine and other components of the drug
Liver damage (cirrhosis, hepatitis, hemolytic jaundice, cholelithiasis)
Kidney damage (nephritis, acute pyelitis, renal amyloidosis, urolithiasis)
Disease of the hematopoietic organs
Progressive systemic diseases of the brain and spinal cord (slow neuroinfections, for example, multiple sclerosis)
Gastric and duodenal ulcers during exacerbation
Severe arterial hypotension
Decompensated heart failure
Thromboembolism
Severe myocardial dystrophy
Rheumatic carditis in later stages
Myxedema
Late stage of bronchiectasis
Angle-closure glaucoma
Urinary retention due to prostatic hyperplasia
Marked depression of the central nervous system
Coma
Brain injuries
Children's age up to 1 year
Drug interactions
The sedative effect of chlorpromazine is enhanced when used simultaneously with zolpidem or zopiclone; neuroleptic - with estrogens. The concentration of chlorpromazine in the blood plasma is reduced by antacids that contain aluminum and magnesium hydroxide (impair the absorption of chlorpromazine from the digestive tract), barbiturates (increase the metabolism of chlorpromazine in the liver). The concentration of chlorpromazine in the blood plasma is increased by chloroquine and sulfadoxine/pyrimethamine. Cimetidine may decrease or increase the concentration of chlorpromazine in the blood.
Chlorpromazine can reduce or even completely suppress the antihypertensive effect of guanethidine, increase the concentration of imipramine in the blood, and suppress the effects of levodopa; increase or decrease the concentration of phenytoin in the blood, reduce the effect of cardiac glycosides.
When used simultaneously with other drugs, it is possible:
with anticholinergic drugs – increased anticholinergic effect;
with anticholinesterase drugs - muscle weakness, worsening gait, myasthenia gravis;
with epinephrine - distortion of the effects of the latter, resulting in a subsequent decrease in blood pressure and the development of severe arterial hypotension and tachycardia;
with amitriptyline - increased risk of developing tardive dyskinesia, possible development of paralytic ileus;
with diazoxide – severe hyperglycemia;
with doxepin – potentiation of hyperpyrexia;
with lithium carbonate – pronounced extrapyramidal symptoms, neurotoxic effect;
with morphine – development of myoclonus;
with cisapride – additive prolongation of the QT interval on the ECG;
with nortriptyline in patients with schizophrenia - a worsening of the clinical condition is possible, despite the increased level of chlorpromazine in the blood;
with tricyclic antidepressants, monoamine oxidase inhibitors - increased risk of developing neuroleptic malignant syndrome;
with drugs for the treatment of hyperthyroidism - the risk of developing agranulocytosis increases;
with other drugs that cause extrapyramidal reactions, an increase in the frequency and severity of extrapyramidal disorders is possible;
with drugs that cause arterial hypotension, severe orthostatic hypotension is possible;
with ephedrine – the vasoconstrictor effect of ephedrine may be weakened.
For neurotic diseases that are accompanied by increased muscle tone, persistent pain, including causalgia, Aminazine can be combined with analgesics, for persistent insomnia - with sleeping pills and tranquilizers. With the simultaneous use of Aminazine with anticonvulsants, the effect of the latter is enhanced; with other drugs that suppress the effect on the central nervous system, as well as with ethanol and drugs that contain ethanol, increased depression of the central nervous system, as well as respiratory depression, is possible.
Barbiturates enhance the metabolism of Aminazine, stimulating microsomal liver enzymes and thereby reducing its concentration in the blood plasma and, as a consequence, the therapeutic effect.
The drug can suppress the effects of amphetamine, levodopa, clonidine, guanethidine, and adrenaline.
special instructions
With extreme caution and careful monitoring, the drug is used to treat patients with pathological changes in the blood picture, cholelithiasis and urolithiasis, acute pyelitis, rheumatism, rheumatic carditis, alcohol intoxication, Reye's syndrome, as well as breast cancer, severe arterial hypertension, thromboembolism, severe myocardial dystrophy, a tendency to develop glaucoma, Parkinson's disease, chronic respiratory diseases (especially in children), epileptic seizures.
It should be prescribed with caution to elderly patients (increased risk of excessive sedation and hypotensive effects), depleted and weakened patients.
If hyperthermia develops, which is one of the symptoms of neuroleptic malignant syndrome, you should immediately stop using the drug.
In children, especially with acute illnesses, when using the drug there is a greater risk of developing extrapyramidal symptoms.
With long-term treatment with the drug, it is necessary to monitor blood composition, prothrombin index, liver and kidney function. After injection of the drug, patients need to remain in a lying position for 1 - 1.5 hours: a sudden transition to a vertical position can lead to orthostatic collapse.
To reduce neuroleptic depression, antidepressants and central nervous system stimulants are used. During therapy, due to the possibility of skin photosensitization, prolonged exposure to the sun should be avoided. The drug does not have an antiemetic effect when nausea is a consequence of vestibular stimulation or local irritation of the digestive tract. When using the drug in patients with atony of the digestive tract and achylia, it is recommended to simultaneously prescribe gastric juice or hydrochloric acid (due to the inhibitory effect of chlorpromazine on motility and secretion of gastric juice), monitor diet and intestinal function. In patients using the drug, the need for riboflavin may be increased.
Registration number: P N000302/01-261212
Trade name of the drug: Aminazine
International Nonproprietary Name (INN): Chlorpromazine
Dosage form: solution for intravenous and intramuscular administration
Compound:
1 liter of solution contains:
Active substance: chlorpromazine (aminazine) - 25 g.
Excipients: sodium sulfite anhydrous - 1 g, sodium metabisulfite - 1 g, ascorbic acid - 2 g, sodium chloride - 6 g, water for injection - up to 1 l.
Description:
Colorless or slightly colored, transparent or slightly opalescent liquid.
Pharmacotherapeutic group: antipsychotic (neuroleptic)
ATX code: .
Pharmacological properties
Antipsychotic drug (neuroleptic), phenothiazine derivative with an aliphatic side chain. It has a pronounced antipsychotic, sedative, antiemetic, vasodilating (alpha-adrenergic blocking), moderate M-anticholinergic, as well as weak hypothermic effect, soothes hiccups; has a local irritant effect.
The antipsychotic effect is due to the blockade of dopamine D2 receptors of the mesolimbic and mesocortical systems. The antipsychotic effect is manifested in the elimination of productive symptoms of psychosis (delusions, hallucinations). Relieves various types of psychomotor agitation, reduces psychotic fear and aggressiveness.
The sedative effect is due to the blockade of adrenergic receptors in the reticular formation of the brain stem. One of the main features of Aminazine (in comparison with other phenothiazines) is the presence of a pronounced sedative effect, manifested by inhibition of conditioned reflex activity (primarily motor-defensive reflexes), a decrease in spontaneous motor activity, relaxation of skeletal muscles, a decrease in sensitivity to endogenous and exogenous stimuli with preserved consciousness.
The onset of sedative action is 15 minutes after intramuscular administration of the drug.
The antiemetic effect is due to the blockade of dopamine D2 receptors in the trigger zone of the vomiting center; hypothermic effect - blockade of dopamine receptors of the hypothalamus.
Aminazine reduces capillary permeability, lowers blood pressure, and has a weak antihistamine effect. Has a local irritating effect.
Pharmacokinetics
It is well and quickly absorbed after intramuscular administration. The maximum concentration in blood plasma after intramuscular administration is achieved after 1-2 hours. Communication with blood plasma proteins is 90-99%. It is quickly cleared from the bloodstream and accumulates unevenly in various organs. Easily penetrates the blood-brain barrier, and its concentration in the brain exceeds that in plasma. There is no direct correlation between plasma concentration and therapeutic effect. It has a “first pass” effect through the liver, where the drug is intensively metabolized as a result of oxidation (30%), hydroxylation (30%) and demethylation (20%). Hydroxylated metabolites have pharmacological activity, which are inactivated by binding to glucuronic acid or by further oxidation to form inactive sulfoxides.
Excreted by the kidneys and bile. The half-life is approximately 15-30 hours. About 20% of the dose taken is excreted per day, 1-6% of the dose is excreted unchanged by the kidneys. Traces of metabolites can be detected in urine 12 months or more after stopping treatment. Due to high protein binding, it is practically not excreted during hemodialysis.
Indications for use
Use strictly as prescribed by your doctor to avoid complications!
In psychiatric practice: psychomotor agitation and psychotic states in patients with schizophrenia, manic agitation, manic-depressive psychosis and other mental illnesses of various origins, accompanied by fear, anxiety, agitation, insomnia; for mood disorders and psychopathy, for psychotic disorders in patients with epilepsy and organic diseases of the central nervous system, to alleviate the state of withdrawal from alcoholism and substance abuse.
In therapeutic, neurological and surgical practice Aminazine is used to relieve psychomotor agitation, as an antiemetic (including during surgery), to enhance the effect of analgesics for persistent pain, for diseases accompanied by increased muscle tone (after cerebrovascular accidents, etc.), to calm hiccups, to lower temperature bodies in anesthesiology as part of so-called “lytic mixtures”.
Contraindications
Increased individual sensitivity;
- chronic heart failure (decompensation);
- arterial hypotension;
- pronounced depression of the function of the central nervous system and comatose states of any etiology;
- traumatic brain injury;
- progressive diseases of the brain and spinal cord;
- pregnancy and lactation period;
- children's age (up to 6 months).
Carefully- active alcoholism (increased likelihood of developing hepatotoxic reactions), pathological changes in blood parameters (impaired hematopoiesis), breast cancer (progression of tumor growth and resistance to treatment with endocrine and cytostatic drugs), closed-angle glaucoma, prostatic hyperplasia with clinical manifestations, hepatic and /or renal failure; diseases accompanied by an increased risk of thromboembolic complications; Parkinson's disease, epilepsy, myxedema, chronic diseases accompanied by respiratory failure (especially in children), history of Reine's syndrome (increased risk of hepatotoxicity in children and adolescents), cachexia, vomiting (the antiemetic effect of phenothiazines may mask vomiting associated with overdose of other drugs funds), old age.
Use during pregnancy and lactation
Aminazine penetrates the placental barrier, is excreted in breast milk, has a teratogenic effect, and prolongs labor. Use during pregnancy is contraindicated. If it is necessary to use the drug during lactation, breastfeeding should be stopped during treatment.
Directions for use and doses
The drug is administered intramuscularly and intravenously in the form of a 2.5% solution (25 mg/ml).
For intramuscular administration, dilute 2-5 ml of 0.25-0.5% solution of novocaine (procaine) or 0.9% sodium chloride solution. The solution is injected deep into the muscle.
When administered intravenously, the required amount of solution is diluted with 20 ml of 5% dextrose solution or 0.9% sodium chloride solution. Inject slowly over 5 minutes under blood pressure control.
When administered intramuscularly, the daily dose usually does not exceed 600 mg. The course of treatment ranges from 2 weeks to 2-4 months or more. Until the end of the course of treatment, the dose of the drug is gradually reduced (by 25-50 mg per day).
In case of severe psychomotor agitation, convulsive syndrome, vomiting, a single initial dose for intramuscular administration is 100-150 mg. To relieve acute agitation, Aminazine is administered into a vein in doses of 50-75 mg (2-3 ml of a 2.5% solution) 1-2 times a day.
for adults intravenously: single - 100 mg, daily - 250 mg, intramuscularly: single - 150 mg, daily 1000 mg.
For children, Aminazine is prescribed depending on age: from 3 years and older, intramuscularly at 0.55 mg/kg or 15 mg/m2 of body surface, if necessary, every 6-8 hours.
Children under 5 years old (body weight up to 23 kg) should not administer more than 40 mg/day, from up to 12 years old (body weight 23-46 kg) - 75 mg/day.
Weakened and elderly patients, depending on age, are prescribed up to 300 mg/day.
To relieve psychomotor agitation in cases of cerebral circulation disorders, attacks of hiccups and uncontrollable vomiting, Aminazine is used as part of the so-called “lytic mixtures” containing 1-2 ml of a 2.5% solution of Aminazine, 2 ml of a 2.5% solution of diprazine or 2 ml 2% diphenhydramine solution, 1 ml 2% promedol solution. The mixture is administered intravenously or intramuscularly 1-2 times a day.
Side effect
At the beginning of treatment, drowsiness, dizziness, dry mouth, decreased appetite, constipation, accommodation paresis, moderate orthostatic hypotension, tachycardia, sleep disorders, difficulty urinating, decreased potency, frigidity, allergic reactions from the skin and mucous membranes (photosensitization, angioedema of the face and limbs); less often - a decrease in blood pressure.
With long-term use in high doses (0.5-1.5 g/day) - extrapyramidal disorders (dyskinesia - paroxysmal spasms of the muscles of the neck, tongue, floor of the mouth, akinetic-rigid phenomena, akatasia, hyperkinesis, tremor and autonomic disorders) , phenomena of mental indifference, delayed reaction to external stimuli, neuroleptic depression, cholestatic jaundice, cardiac arrhythmias, lympho- and leukopenia, anemia, agranulocytosis, hypercoagulation, amenorrhea, galactorrhea, hyperprolactinemia, gynecomastia, nausea, vomiting, diarrhea, oliguria, skin pigmentation , clouding of the lens and cornea; in isolated cases - convulsions (antiparkinsonian drugs are used as correctors - tropacin; trihexyphenyl and others; dyskinesias are relieved by subcutaneous administration of 2 ml of a 20% sodium caffeine benzoate solution and 1 ml of a 0.1% atropine solution), neuroleptic malignant syndrome.
Local reactions: with intramuscular administration, infiltrates may occur, with intravenous administration - phlebitis, in contact with the skin and mucous membranes - tissue irritation.
When taking phenothiazine antipsychotics, cases of sudden death (including those possibly caused by cardiac causes) have been reported; may prolong the QT interval - the risk of developing ventricular arrhythmias (especially against the background of initial bradycardia, hypokalemia, prolonged QT).
Overdose
Symptoms: areflexia or hyperreflexia, blurred vision, mydriasis, dry mouth, hyperpyrexia or hypothermia, muscle rigidity, vomiting, respiratory depression, possible development of pulmonary edema;
cardiotoxic effect (development of circulatory failure, arterial hypotension, shock, rhythm disturbance (tachycardia, change in QRS wave, ventricular fibrillation, asystole);
neurotoxic effects (agitation, confusion, convulsions, disorientation, drowsiness, stupor or coma).
Treatment:
For arrhythmia - intravenous administration of phenytoin 9-11 mg/kg, for circulatory failure - cardiac glycosides, for a pronounced decrease in blood pressure - intravenous administration of fluid or vasopressor drugs, such as norepinephrine, phenylephrine (avoid prescribing alpha and beta adrenergic agonists, such like epinephrine, since a paradoxical decrease in blood pressure is possible due to blockade of alpha-adrenergic receptors with chlorpromazine), for seizures - diazepam (avoid prescribing barbiturates due to possible subsequent depression of the central nervous system and respiratory depression), for parkinsonism - diphenyltropine, diphenhydramine.
Monitoring the function of the cardiovascular system for at least 5 days, the function of the central nervous system, breathing, measuring body temperature, consultation with a psychiatrist. Dialysis is ineffective.
Interaction with other drugs
Aminazine weakens the vasoconstrictor effect of ephedrine.
May mask some manifestations of ototoxicity (tinnitus, dizziness) of ototoxic drugs, especially antibiotics.
Reduces the antiparkinsonian effect of levodopa (due to the blockade of dopamine receptors), as well as the effects of amphetamines, clonidine and guanethidine. Strengthens the anticholinergic effects of drugs, while its own antipsychotic effect may decrease.
With the simultaneous use of Aminazine with prochlorperazine, which is related in chemical structure, an overdose and prolonged loss of consciousness may occur. Compatible with other antipsychotic drugs, anxiolytics and antidepressants.
Long-term combination with analgesics and antipyretics is undesirable (possible development of hyperthermia).
When used simultaneously with other drugs that have a depressant effect on the central nervous system (general anesthesia, anticonvulsants, narcotic analgesics, ethanol and drugs containing it, barbiturates and other hypnotics, anxiolytic drugs (tranquilizers) and others), it is possible to enhance and prolongation of the depressive effect, as well as respiratory depression. Prescription together with tricyclic antidepressants, maprotiline or monoamine oxidase inhibitors increases the risk of developing neuroleptic malignant syndrome.
With drugs for the treatment of thyrotoxicosis, the risk of developing agranulocytosis increases.
With other drugs that cause extrapyramidal reactions, Aminazine increases the frequency and severity of extrapyramidal disorders.
With antihypertensive drugs, it increases the severity of the decrease in blood pressure in orthostasis.
Antacids, antiparkinsonian drugs, lithium preparations can interfere with the absorption of Aminazine.
Hepatotoxic drugs when used together with Aminazine increase the risk of developing toxic effects on the liver.
During treatment with Aminazine, the administration of epinephrine should be avoided (due to the possibility of distortion of the effect of epinephrine and a further decrease in blood pressure).
Drugs that inhibit bone marrow hematopoiesis increase the risk of myelosuppression.
special instructions
During treatment, it is necessary to monitor blood pressure, pulse, and regularly monitor liver, kidney and blood functions.
To avoid a sharp decrease in blood pressure after intramuscular or intravenous administration, the procedure is carried out with the patient in a “lying” position; after using the drug, patients should remain in the “lying” position for at least 1.5-2 hours (a sudden transition to a vertical position can cause orthostatic collapse). Patients should not be exposed to ultraviolet radiation, since the drug can cause photosensitivity.
During the treatment period, the use of ethanol should be avoided.
It is necessary to exclude the possibility of the drug getting on the skin and mucous membranes.
Impact on the ability to drive vehicles and operate machinery
Aminazine should not be used during work by drivers of vehicles and people whose profession requires increased concentration and speed of psychomotor reactions.
Release form
Solution for intravenous and intramuscular administration 25 mg/ml in ampoules of 1 ml, 2 ml, 5 ml or 10 ml. 10 ampoules together with instructions for use and a knife for opening ampoules or an ampoule scarifier in a cardboard box, or 5 or 10 ampoules in a blister pack.
1 or 2 blister packs along with instructions for use and a knife for opening ampoules or an ampoule scarifier in a cardboard pack.
When packaging ampoules with a break ring or break point, do not insert a knife for opening ampoules or an ampoule scarifier.
Storage conditions
In a place protected from light at a temperature of 5 to 25 ° C.
Keep out of the reach of children.
Best before date
3 years. Do not use after the expiration date stated on the package.
Conditions for dispensing from pharmacies
On prescription.
In psychiatric practice, aminazine is used in various states of psychomotor agitation in patients with schizophrenia (hallucinatory-delusional, hebephrenic, catatonic syndromes), in chronic paranoid and hallucinatory-paronoid states, manic agitation in patients with manic-depressive psychosis (psychosis with alternating excitement and depression of mood) , with psychotic disorders in patients with epilepsy, with agitated depression (motor excitation against a background of anxiety and fear) in patients with presenile (stressful), manic-depressive psychosis, as well as with other mental illnesses and neuroses accompanied by agitation, fear, insomnia, tension, with acute alcoholic psychoses.
Aminazine can be used either alone or in combination with other psychotropic products (antidepressants, butyrophenone derivatives, etc.).
A peculiarity of the action of aminazine in states of excitement in comparison with other antipsychotics (triftazine, haloperidol, etc.) is a pronounced sedative (calming) effect.
In neurological practice, aminazine is also prescribed for diseases accompanied by an increase in muscle tone (after a cerebral stroke, etc.). Sometimes used to relieve status epilepticus (if other treatment methods are ineffective). It is administered intravenously or intramuscularly for this purpose. It should be borne in mind that in patients with epilepsy, chlorpromazine can cause an increase in seizures, but usually when prescribed simultaneously with anticonvulsant products, it enhances the subsequent effect.
The use of aminazine in combination with analgesics for persistent pain, including causalgia (intense burning pain due to damage to a peripheral nerve), and with sleeping pills and tranquilizers (sedatives) for persistent insomnia is effective.
Aminazine is sometimes used as an antiemetic agent for vomiting of pregnant women, Meniere's disease (a disease of the inner ear), in oncological practice - in the treatment of bis-(beta-chloroethyl)amine derivatives and other chemotherapeutic products, and during radiation therapy. In the clinic of skin diseases for itchy dermatoses (skin diseases) and other diseases.
Pharmachologic effect:
Aminazine is one of the main representatives of neuroleptics (medicines that have an inhibitory effect on the central nervous system and do not cause a hypnotic effect in normal doses). Despite the emergence of numerous new antipsychotic products, it continues to be widely used in medical practice.
One of the main features of the effect of aminazine on the central nervous system is its relatively strong sedative effect (calming effect on the central nervous system). The general sedation that increases with increasing dose of chlorpromazine is accompanied by suppression of conditioned reflex activity and, above all, motor-defensive reflexes, a decrease in spontaneous motor activity and some relaxation of skeletal muscles; a state of reduced reactivity to endogenous (internal) and exogenous (external) stimuli occurs; consciousness, however, is preserved.
The effect of anticonvulsants under the influence of chlorpromazine is enhanced, but in some cases chlorpromazine can cause convulsive phenomena.
The main features of aminazine are its antipsychotic effect and the ability to influence the emotional sphere of a person. With the help of chlorpromazine, it is possible to stop (relieve) various types of psychomotor agitation, weaken or completely stop delusions and hallucinations (delusions, visions that acquire the character of reality), reduce or relieve fear, anxiety, tension in patients with psychosis and neuroses.
An important property of aminazine is its blocking effect on central adrenergic and dopaminergic receptors. It reduces or even completely eliminates the increase in blood pressure and other effects caused by adrenaline and adrenergic agonists. The hyperglycemic effect of adrenaline (an increase in blood sugar under the influence of adrenaline) is not relieved by aminazine. The central adrenolytic effect is strongly expressed. The blocking effect on cholinergic receptors is relatively weak.
The drug has a strong antiemetic effect and soothes hiccups.
Aminazine has a hypothermic (lowering body temperature) effect, especially during artificial cooling of the body. In some cases, in patients with parenteral (bypassing the gastrointestinal tract) administration of the product, the body temperature rises, which is associated with the effect on thermoregulation centers and partly with local irritant effects.
The drug also has moderate anti-inflammatory properties, reduces vascular permeability, and reduces the activity of kinins and hyaluronidase. Has a slight antihistamine effect.
Aminazine enhances the effect of sleeping pills, narcotic analgesics (painkillers), and local anesthetics. It inhibits various interoceptive reflexes.
Aminazine method of administration and dosage:
Aminazine is prescribed orally (in the form of pills), intramuscularly or intravenously (in the form of a 2.5% solution). With parenteral (bypassing the digestive tract) administration, the effect occurs faster and is more pronounced. It is recommended to use the product internally after eating (to reduce the irritant effect on the gastric mucosa). When administered intramuscularly, 2-5 ml of 0.25%-0.5% novocaine solution or isotonic sodium chloride solution is added to the required amount of chlorpromazine solution. The solution is injected deep into the muscles (in the upper outer quadrant of the gluteal region or in the outer lateral surface of the thigh). Intramuscular injections are made no more than 3 times a day. For intravenous administration, the required amount of chlorpromazine solution is diluted in 10-20 ml of 5% (sometimes 20-40%) glucose solution or isotonic sodium chloride solution and administered slowly (over 5 minutes).
Doses of chlorpromazine depend on the route of administration, indications, age and condition of the patient. The most convenient and common way is to take chlorpromazine orally.
In the treatment of mental illnesses, the initial dose is usually 0.025-0.075 g per day (in 1-2-3 doses), then it is gradually increased to a daily dose of 0.3-0.6 g. In some cases, the daily dose when taken orally reaches 0 .7-1 g (especially in patients with a chronic course of the disease and psychomotor agitation). When treating with large doses, the daily dose is divided into 4 parts (taken in the morning, afternoon, evening and night). The duration of treatment with large doses should not exceed 1-1.5 months; if the effect is insufficient, it is advisable to switch to treatment with other products. Long-term treatment with aminazine alone is currently carried out relatively infrequently. More often, aminazine is combined with triftazine, haloperidol and other products.
When administered intramuscularly, the daily dose of chlorpromazine usually does not have to exceed 0.6 g. Once the effect is achieved, the substance is taken orally.
By the end of the course of treatment with aminazine, which can last from 3-4 weeks. up to 3-4 months and longer, the dose is gradually reduced by 0.025-0.075 g per day. Patients with a chronic course of the disease are prescribed long-term maintenance therapy.
In states of severe psychomotor agitation, the initial dose for intramuscular administration is usually 0.1-0.15 g. For the purpose of emergency relief of acute agitation, chlorpromazine can be injected into a vein. To do this, 1 or 2 ml of a 2.5% solution (25-50 mg) of aminazine is diluted in 20 ml of a 5% or 40% glucose solution. If necessary, increase the dose of chlorpromazine to 4 ml of a 2.5% solution (in 40 ml of glucose solution). Enter slowly.
For acute alcoholic psychoses, 0.2-0.4 g of chlorpromazine per day is prescribed intramuscularly and orally. If the effect is insufficient, 0.05-0.075 g is administered intravenously (usually in combination with tizercin).
Higher doses for adults orally: single - 0.3 g, daily - 1.5 g; intramuscularly: single - 0.15 g, daily - 1 g; intravenously: single - 0.1 g, daily - 0.25 g.
For children, chlorpromazine is prescribed in smaller doses: depending on age, from 0.01-0.02 to 0.15-0.2 g per day. For weakened and elderly patients - up to 0.3 g per day.
For the treatment of diseases of internal organs, skin and other diseases, aminazine is prescribed in lower doses than in psychiatric practice (0.025 g 3-4 times every day for adults, older children - 0.01 g per dose).
Aminazine contraindications:
Aminazine is contraindicated in cases of liver damage (cirrhosis, hepatitis, hemolytic jaundice, etc.), kidney damage (nephritis); dysfunction of the hematopoietic organs, myxedema (sharp decrease in thyroid function, accompanied by edema), progressive systemic diseases of the brain and spinal cord, decompensated heart defects, thromboembolic disease (blockage of blood vessels with a blood clot). Relative contraindications are cholelithiasis, urolithiasis, acute pyelitis (inflammation of the renal pelvis), rheumatism, rheumatic carditis. For gastric and duodenal ulcers, chlorpromazine should not be prescribed orally (administered intramuscularly). Aminazine is not prescribed to persons in a comatose (unconscious) state, including in cases associated with the use of barbiturates, alcohol, and drugs. The blood picture should be monitored, including determination of the prothrombin index, and liver and kidney functions should be examined. Aminazine should not be used to relieve agitation in acute brain injuries. Aminazine should not be prescribed to pregnant women.
Aminazine side effects:
When treating with aminazine, side effects may be observed due to its local and resorptive (manifested as a result of absorption of the substance into the blood) effect. Contact of aminazine solutions under the skin, on the skin and mucous membranes can cause tissue irritation; injection into a muscle is often accompanied by the appearance of painful infiltrates (seals); when administered into a vein, damage to the endothelium (inner layer of the vessel) is possible. To avoid these phenomena, chlorpromazine solutions are diluted with solutions of novocaine, glucose, and isotonic sodium chloride solution (glucose solutions should only be used for intravenous administration).
Parenteral administration of aminazine can cause a sharp decrease in blood pressure. Hypotension (a decrease in blood pressure below normal) can also develop with oral (by mouth) use of the product, especially in patients with hypertension (high blood pressure); Aminazine should be prescribed to such patients in reduced doses.
After injection of chlorpromazine, patients should be in a lying position (11/2 hours). You should rise slowly, without sudden movements.
After taking aminazine, allergic manifestations on the skin and mucous membranes, swelling of the face and extremities, and photosensitivity of the skin (increased sensitivity of the skin to sunlight) may be observed.
When taken orally, dyspeptic symptoms (digestive disorders) are possible. Due to the inhibitory effect of aminazine on the motility of the gastrointestinal tract and the secretion of gastric juice, it is recommended that patients with atony (decreased tone) of the intestines and achylia (lack of secretion of hydrochloric acid and enzymes in the stomach) be given gastric juice or hydrochloric acid at the same time and monitor diet and function gastrointestinal tract.
There are known cases of jaundice, agranulocytosis (a sharp decrease in the number of granulocytes in the blood), and skin pigmentation.
When using aminazine, a neuroleptic syndrome develops relatively often, expressed in the phenomena of parkinsonism, akathisia (restlessness of the patient with a constant desire to move), indifference, delayed reaction to external stimuli and other mental changes. Sometimes there is a long-term subsequent depression (state of depression). To reduce depression, central nervous system stimulants (sydnocarb) are used. Neurological complications decrease with dose reduction; they can also be reduced or stopped by the simultaneous administration of cyclodol, tropacin or other anticholinergic drugs used to treat parkinsonism. With the development of dermatitis (skin inflammation), swelling of the face and limbs, antiallergic drugs are prescribed or treatment is canceled.