Pharmacodynamics and pharmacokinetics
Pharmacodynamics
Antipsychotic drug from the phenothiazine , which is the first generation of antipsychotic drugs. The mechanism of neuroleptic action is due to the blockade of dopaminergic receptors in certain brain structures. Blockade of these receptors increases the production of prolactin by the pituitary gland . It also blocks α-adrenergic receptors , which is accompanied by a sedative effect .
The central antiemetic effect is associated with blockade of D2 receptors in a certain area of the cerebellum, and the peripheral effect is associated with blockade of the intestinal vagus nerve. The antiemetic effect is also associated with the sedative , anticholinergic and antihistamine properties of the drug.
The antipsychotic effect is manifested in eliminating delusions and hallucinations, reducing anxiety, tension, fear and restlessness, and stopping psychomotor agitation. Produces a rapid sedative effect, therefore it is used for acute psychosis . Not prescribed for depression.
Antihiccups, hypothermic, antiarrhythmic, antishock and moderate extrapyramidal effects are noted.
Pharmacokinetics
Rapidly but not completely absorbed after oral administration. Cmax is reached after 3-4 hours. There is a “first pass” effect through the liver, so blood concentrations after oral administration are lower than concentrations after parenteral administration.
Metabolized in the liver, resulting in the formation of active and inactive metabolites. 95-98% bound to plasma proteins. Penetrates through the BBB, the concentration in the brain is always higher than in the blood. There is no direct relationship between the concentrations of the drug and its metabolites in plasma and the effect. T1/2 is 30 hours or more. Metabolites are excreted in urine and bile.
Chlorpromazine Canon
During treatment, it is necessary to regularly monitor blood pressure, pulse, liver and kidney function. It is also necessary to monitor the blood picture (at first weekly, and then every 3-4 months); if during therapy the number of leukocytes decreases to 3.0-3.5x109/l, and the number of neutrophils decreases to 1.5-2.0x109/l, these indicators should be monitored 2 times a week; if leukocytosis and granulocytopenia occur, treatment should be interrupted.
Each patient should be informed that if they have a fever, sore throat or other manifestations of infectious diseases, they should immediately notify their doctor. In the event of hyperthermia, which may be one of the symptoms of neuroleptic malignant syndrome (pallor, hyperthermia, autonomic dysfunction, changes in consciousness, muscle rigidity), the drug Chlorpromazine Canon should be discontinued immediately. Early manifestations preceding the onset of hyperthermia may include side effects such as increased sweating and instability of blood pressure (BP). Although the etiology of the dependence of such side effects on antipsychotics is most often unknown, there are a number of risk factors: individual predisposition, dehydration, organic brain damage. Neuroleptic malignant syndrome can occur at any time during treatment with antipsychotic drugs and can be fatal.
If signs and symptoms of tardive dyskinesia occur, consider reducing the dose or discontinuing all antipsychotic medications. Tardive dyskinesia sometimes occurs after discontinuation of the antipsychotic and disappears with repeated use or increased dosage. Prescription of antiparkinsonian and anticholinergic drugs in the development of tardive dyskinesia is contraindicated (the condition may worsen).
Antiparkinsonian drugs - trihexyphenidyl and others - are used as correctors for extrapyramidal disorders, the occurrence of which is possible with the use of the drug Chlopromazine Canon.
Chlorpromazine, depending on the dose, may increase the prolongation of the QT interval, which increases the risk of ventricular arrhythmias, including torsade de pointes (TdP). Bradycardia, hypokalemia, and congenital or acquired long QT period also increase. Therefore, before starting treatment, you must ensure that:
- bradycardia below 55 beats per minute;
- hypokalemia;
- congenital prolongation of the QT interval.
Except in emergency situations, it is recommended to perform an ECG during the preliminary examination of patients requiring treatment with an antipsychotic.
In randomized clinical trials in elderly patients with dementia, atypical antipsychotic drugs were found to have an increased risk of stroke compared with placebo compared with placebo. The mechanism for this increased risk is not known. An increased risk with other antipsychotics or in other age groups cannot be excluded. Chlopromazine Canon should be used with caution in patients with risk factors for stroke, in elderly patients with dementia, as the risk of mortality increases in elderly patients with psychosis associated with dementia and receiving antipsychotic drugs.
Placebo-controlled studies, which were conducted primarily in patients taking atypical antipsychotic drugs, showed a 1.6- to 1.7-fold increased risk of mortality compared with placebo. At the end of treatment, lasting an average of 10 weeks, the risk of mortality was 4.5% in the chlorpromazine group, compared with 2.6% in the placebo group. Although the causes of death in clinical studies with atypical antipsychotics varied, the majority of these deaths were the result of cardiovascular problems (eg, heart failure, sudden death) or infections (eg, pneumonia).
There is a risk of venous thromboembolism (VTE) during treatment with antipsychotics. In patients treated with antipsychotic drugs, especially those with acquired risk factors for VTE, prophylactic measures should be taken and any potential risk factor for VTE assessed before and during treatment with Chlopromazine Canon. Except in exceptional circumstances, Chlopromazine Canon should not be used in Parkinson's disease.
The occurrence of intestinal obstruction, which can be detected by bloating and abdominal pain, requires emergency care.
Predisposing factors for the development of arrhythmia when taking chlorpromazine are: hypokalemia (including when using diuretics that cause hypokalemia), bradycardia (including those caused by the drug), an existing (congenital or acquired) increase in the duration of the QT interval.
The simultaneous administration of chlorpromazine with dopaminergic non-antiparkinsonian drugs (cabergoline, quinagolide) is not recommended due to the mutual antagonism of dopamine agonists and antipsychotics. Concomitant use with other antipsychotics that can cause irritation (amisupride, cyamemazine, droperidol, fluphenazine, propericiazine, haloperidol, levomepromazine, pimozide, pipamperone, pipothiazine, sertindole, sulypiride, sultopride, tiapride) is not recommended.
Concomitant use with antiparasitic drugs (halofantrine, lumefantrine, pentamidine) is not recommended. Also, simultaneous use with antifungal agents from the azole group is not recommended (increased risk of arrhythmia). If it is impossible to avoid the co-administration of the above combinations, it is recommended to carry out regular ECG monitoring with monitoring of the duration of the QT interval.
When using non-potassium-sparing diuretics, correction of hypokalemia and ECG monitoring are necessary before starting chlorpromazine therapy.
Monitoring during treatment with Chlopromazine Canon should be intensified:
- in patients with epilepsy and a history of seizures, due to the possibility of lowering the seizure threshold. The occurrence of seizures requires cessation of treatment.
- in elderly patients with:
a) high susceptibility and effect of orthostatic hypotension (increased risk of excessive sedation and hypotensive effects),
b) chronic constipation (risk of paralytic intestinal obstruction),
c) possible prostate hypertrophy;
- in patients with cardiovascular diseases taking quinidine, due to a possible increase in the hypotensive effect;
- in case of liver failure and/or severe renal failure, due to the risk of accumulation.
For long-term treatment, regular ophthalmological monitoring is recommended.
It should be taken into account that the use of phenothiazine derivatives can lead to hyperglycemia or impaired glucose tolerance, development or exacerbation of diabetes mellitus, hypercholesterolemia, fecal impaction, severe intestinal obstruction and megacolon.
Since in high doses (100 mg/day) chlorpromazine can cause an increase in blood glucose levels by reducing insulin secretion, in patients with diabetes mellitus it is necessary to adjust insulin doses before and after completion of therapy. If necessary, the dose of the antipsychotic should also be adjusted in patients taking sulfonylureas.
Chlorpromazine should not be used as monotherapy if depression predominates.
Chlopromazine Canon should be used with caution in case of hypersensitivity to other phenothiazine drugs or severe respiratory diseases.
Due to the risk of photosensitivity, ultraviolet irradiation should be avoided. Chlopromazine can worsen the course or promote the manifestation of latent myasthenia gravis, as well as cause myasthenic syndrome.
To avoid the development of the “neuroleptic malignant syndrome” syndrome).
Patients with pheochromacetoma taking chlopromazine may experience false positive blood catecholamine levels.
During therapy, it is necessary to stop drinking alcohol, since chlorpromazine enhances the inhibitory effect of alcohol on the central nervous system.
Indications for use
- acute and chronic paranoid states;
- hallucinatory states;
- schizophrenia with psychomotor agitation;
- manic excitement;
- epilepsy with psychotic disorders;
- agitated depression;
- alcoholic psychosis;
- increased muscle tone;
- pain syndrome;
- status epilepticus;
- persistent insomnia;
- itchy dermatoses ( neurodermatitis , eczema );
- potentiation of anesthesia.
As a means of eliminating vomiting, it is used for Meniere's disease , vomiting of pregnancy and during radiation therapy .
Chlorpromazine Organica (solution 25 mg/ml)
pharmachologic effect
- The antipsychotic drug (neuroleptic) is a dimethylamine phenothiazine derivative with an aliphatic side chain. It has a pronounced antipsychotic, sedative, antiemetic, vasodilating (alpha-adrenergic blocking), moderate M-cholinergic, as well as weak hypothermic effect, soothes hiccups, and 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 Chlorpromazine Organic (in comparison with other phenothiazines) is the presence of a pronounced sedative effect, manifested in the inhibition of conditioned reflex activity (primarily motor-defense reflexes), a decrease in spontaneous motor activity, relaxation of skeletal muscles, a decrease in sensitivity to endogenous and exogenous stimuli while maintaining consciousness. Beginning of sedative action 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.
Indications:
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 (CNS), to alleviate the state of withdrawal from alcoholism and substance abuse.
In therapeutic, neurological and surgical practice, it is used to relieve psychomotor agitation, as an antiemetic (including during surgery), as a means to enhance the effect of analgesics for persistent pain, in diseases accompanied by an increase in muscle tone (after cerebrovascular accidents, etc.), for calming hiccups, to lower body temperature in anesthesiology as part of the so-called “lytic mixtures”.
Contraindications
Chlorpromazine is contraindicated in:
- increased sensitivity;
- severe liver/ renal failure ;
- comatose states;
- brain injuries (acute period);
- strokes;
- pronounced inhibition of hematopoiesis ;
- myxedema;
- decompensated heart failure (with heart defects );
- thromboembolic syndrome;
- bronchiectasis (severe);
- angle-closure glaucoma;
- cholelithiasis and urolithiasis ;
- exacerbation of gastrointestinal ulcers ;
- pregnancy, lactation;
- under 1 year of age.
Chlorpromazine Organic
During treatment, it is necessary to regularly monitor blood pressure, pulse, liver and kidney function. It is also necessary to monitor the blood picture (at first weekly, and then every 3-4 months); if during therapy the number of leukocytes decreases to 3.0-3.5 x 109/l, and the number of neutrophils decreases to 1.5-2.0 x 109/l, these indicators should be monitored 2 times a week; if leukocytosis and granulocytopenia occur, treatment should be interrupted.
Each patient should be informed that if they have a fever, sore throat or other manifestations of infectious diseases, they should immediately notify their doctor.
In case of hyperthermia, which may be one of the symptoms of neuroleptic malignant syndrome (pallor, hyperthermia, autonomic dysfunction, changes in consciousness, muscle rigidity), Chlorpromazine Organica should be discontinued immediately. Early manifestations preceding the onset of hyperthermia may include side effects such as increased sweating and instability of blood pressure (BP). Although the etiology of the dependence of such side effects on antipsychotics is most often unknown, there are a number of risk factors: individual predisposition, dehydration, organic brain damage. Neuroleptic malignant syndrome can occur at any time during treatment with antipsychotic drugs and can be fatal.
If signs and symptoms of tardive dyskinesia occur, consider reducing the dose or discontinuing all antipsychotic medications. Tardive dyskinesia sometimes occurs after discontinuation of the antipsychotic and disappears with repeated use or increased dosage. Prescription of antiparkinsonian and anticholinergic drugs in the development of tardive dyskinesia is contraindicated (the condition may worsen).
Antiparkinsonian drugs - trihexyphenidyl and others - are used as correctors for extrapyramidal disorders, the occurrence of which is possible when using the drug Chlorpromazine Organica.
Chlorpromazine Organic, depending on the dose, may increase the prolongation of the QT interval, which increases the risk of ventricular arrhythmias, including torsade de pointes (TdP). Bradycardia, hypokalemia, and congenital or acquired prolonged QT interval also increase. Therefore, before starting treatment, it is necessary to ensure the absence of: bradycardia below 55 beats per minute, hypokalemia, congenital prolongation of the QT interval.
Except in emergency situations, it is recommended to perform an ECG during the preliminary examination of patients requiring treatment with an antipsychotic.
In randomized clinical trials in elderly patients with dementia, atypical antipsychotic drugs (AEDs) were found to have an increased risk of stroke compared with placebo. The mechanism by which this increased risk occurs is unknown. An increased risk with other antipsychotics or in other age groups cannot be excluded.
Chlorpromazine Organic should be used with caution in patients with risk factors for stroke, in elderly patients with dementia, as the risk of mortality increases in elderly patients with psychosis associated with dementia and receiving antipsychotic drugs.
Placebo-controlled studies, which were conducted primarily in patients taking atypical antipsychotic drugs, showed a 1.6- to 1.7-fold increased risk of mortality compared with placebo. At the end of treatment, lasting an average of 10 weeks, the risk of mortality was 4.5% in the chlorpromazine group, compared with 2.6% in the placebo group.
Although the causes of death in clinical studies with atypical antipsychotics varied, the majority of these deaths were the result of cardiovascular problems (eg, heart failure, sudden death) or infections (eg, pneumonia).
There is a risk of venous thromboembolism (VTE) during treatment with antipsychotics. In patients treated with antipsychotic drugs, especially those with acquired risk factors for VTE, prophylactic measures should be taken and any potential risk factor for VTE assessed before and during treatment with Chlorpromazine Organica.
Except in exceptional circumstances, Chlorpromazine Organic should not be used in Parkinson's disease.
The occurrence of intestinal obstruction, which can be detected by bloating and abdominal pain, requires emergency care.
Predisposing factors for the development of arrhythmia when taking the drug Chlorpromazine Organica are: hypokalemia (including when using diuretics that cause hypokalemia), bradycardia (including those caused by drugs), an existing (congenital or acquired) increase in the duration of the QT interval.
The simultaneous administration of chlorpromazine with dopaminergic non-antiparkinsonian drugs (cabergoline, quinagolide) is not recommended due to the mutual antagonism of dopamine agonists and antipsychotics.
Concomitant use with other antipsychotics that can cause irritation (amisulpride, cyamemazine, droperidol, fluphenazine, propericiazine, haloperidol, levomepromazine, pimozide, pipamperone, pipothiazine, sertindole, sulpiride, sultopride, tiapride) is not recommended.
Concomitant use with antiparasitic drugs (halofantrine, lumefantrine, pentamidine) is not recommended.
Also, simultaneous use with antifungal agents from the azole group is not recommended (increased risk of arrhythmia). If it is impossible to avoid the co-administration of the above combinations, it is recommended to carry out regular ECG monitoring with monitoring of the duration of the QT interval. When using non-potassium-sparing diuretics, correction of hypokalemia and ECG monitoring are necessary before starting chlorpromazine therapy.
Monitoring during treatment with Chlorpromazine Organica should be intensified:
- in patients with epilepsy and a history of seizures, due to the possibility of lowering the seizure threshold. The occurrence of seizures requires cessation of treatment;
- in elderly patients with:
a) high susceptibility and effect of orthostatic hypotension (increased risk of excessive sedation and hypotensive effects);
b) chronic constipation (risk of paralytic intestinal obstruction);
c) possible prostate hypertrophy;
- in patients with cardiovascular diseases taking quinidine, due to a possible increase in the hypotensive effect;
- in case of liver failure and/or severe renal failure, due to the risk of accumulation.
For long-term treatment, regular ophthalmological monitoring is recommended.
It should be taken into account that the use of phenothiazine derivatives can lead to hyperglycemia or impaired glucose tolerance, development or exacerbation of diabetes mellitus, hypercholesterolemia, fecal impaction, severe intestinal obstruction and megacolon.
Since in high doses (100 mg/day) chlorpromazine can cause an increase in blood glucose levels by reducing insulin secretion, in patients with diabetes mellitus it is necessary to adjust insulin doses before and after completion of therapy. If necessary, the dose of the antipsychotic should also be adjusted in patients taking sulfonylureas.
Chlorpromazine should not be used as monotherapy if depression predominates.
Use Chlorpromazine Organica with caution in case of hypersensitivity to other phenothiazine drugs or severe respiratory diseases.
Due to the risk of photosensitivity, ultraviolet irradiation should be avoided.
Chlorpromazine Organic can worsen the course or promote the manifestation of latent myasthenia gravis, as well as cause myasthenic syndrome.
To avoid the development of the “neuroleptic malignant syndrome” syndrome).
Patients with pheochromocytoma taking Chlorpromazine Organica may experience false-positive blood catecholamine levels.
During therapy, it is necessary to stop drinking alcohol, since chlorpromazine enhances the inhibitory effect of alcohol on the central nervous system.
Side effects
- restlessness and anxiety, extrapyramidal reactions, thermoregulation disorders, parkinsonian syndrome , rarely - seizures;
- arterial hypotension (with intravenous injections), tachycardia ;
- dyspeptic symptoms (when taken orally);
- leukopenia , agranulocytosis ;
- difficulty urinating;
- impotence , gynecomastia, menstrual irregularities, weight gain;
- skin rash, itching, dermatitis , erythema , skin pigmentation.
With prolonged use, Chlorpromazine can be deposited in the cornea and lens, which accelerates the aging process of the lens. With intramuscular administration, infiltrates , and with intravenous administration, phlebitis .
Instructions for use of Chlorpromazine hydrochloride (Method and dosage)
Oral or parenteral use depends on the clinical situation.
For injection or IV administration, adults are prescribed 25-50 mg (1-2 ml). If necessary, the dose is repeated every 3-12 hours. For intramuscular administration, the drug is diluted with 2 ml of 0.9% NaCl solution. For intravenous administration, dilute with 20 ml of 0.9% NaCl solution. For adults, the maximum single dose for intramuscular use is 150 mg, and for intravenous use is 100 mg.
If there is anxiety before surgery, 0.5-1 ml is administered intramuscularly before surgery 2 hours before the operation. With intramuscular or intravenous administration, a single dose in children is 250-500 mcg/kg. In pediatric practice, dosage forms for children are used.
When taken orally, the initial daily dose in adults is 25-100 mg in one or 4 doses; if necessary, the dose is increased to 700-1000 mg/day, extremely rarely the dose is increased to 1200-1500 mg/day. The highest single dose for adults orally is 0.3 g, daily dose is 1.5 g.
The instructions for Chlorpromazine contain a warning about the need to monitor blood composition and prothrombin index during long-term treatment.
Chlorpromazine Canon (50mg, 100mg)
During treatment, it is necessary to regularly monitor blood pressure, pulse, liver and kidney function. It is also necessary to monitor the blood picture (at first weekly, and then every 3-4 months); if during therapy the number of leukocytes decreases to 3.0-3.5x109/l, and the number of neutrophils decreases to 1.5-2.0x109/l, these indicators should be monitored 2 times a week; if leukocytosis and granulocytopenia occur, treatment should be interrupted. Each patient should be informed that if they have a fever, sore throat or other manifestations of infectious diseases, they should immediately notify their doctor. In the event of hyperthermia, which may be one of the symptoms of neuroleptic malignant syndrome (pallor, hyperthermia, autonomic dysfunction, changes in consciousness, muscle rigidity), the drug Chlorpromazine Canon should be discontinued immediately. Early manifestations preceding the onset of hyperthermia may include side effects such as increased sweating and instability of blood pressure (BP). Although the etiology of the dependence of such side effects on antipsychotics is most often unknown, there are a number of risk factors: individual predisposition, dehydration, organic brain damage. Neuroleptic malignant syndrome can occur at any time during treatment with antipsychotic drugs and can be fatal. If signs and symptoms of tardive dyskinesia occur, consider reducing the dose or discontinuing all antipsychotic medications. Tardive dyskinesia sometimes occurs after discontinuation of the antipsychotic and disappears with repeated use or increased dosage. Prescribing antiparkinsonian and anticholinergic drugs for the development of tardive dyskinesia is contraindicated (the condition may worsen). Antiparkinsonian drugs - trihexyphenidyl and others - are used as correctors for extrapyramidal disorders, the occurrence of which is possible with the use of the drug Chlorpromazine Canon. Chlorpromazine, depending on the dose, may increase the prolongation of the QT interval, which increases the risk of ventricular arrhythmias, including torsade de pointes (TdP). Bradycardia, hypokalemia, and congenital or acquired long QT period also increase. Therefore, before starting treatment, you must ensure that there is no: • bradycardia below 55 beats per minute; • hypokalemia; • congenital prolongation of the QT interval. Except in emergency situations, it is recommended to perform an ECG during the preliminary examination of patients requiring treatment with an antipsychotic. In randomized clinical trials in elderly patients with dementia, atypical antipsychotic drugs were found to have an increased risk of stroke compared with placebo compared with placebo. The mechanism for this increased risk is not known. An increased risk with other antipsychotics or in other age groups cannot be excluded. Chlorpromazine Canon should be used with caution in patients with risk factors for stroke, in elderly patients with dementia, as the risk of mortality increases in elderly patients with psychoses associated with dementia and receiving antipsychotic drugs. Placebo-controlled studies, which were conducted primarily in patients taking atypical antipsychotic drugs, showed a 1.6- to 1.7-fold increased risk of mortality compared with placebo. At the end of treatment, lasting an average of 10 weeks, the risk of mortality was 4.5% in the chlorpromazine group, compared with 2.6% in the placebo group. Although the causes of death in clinical studies with atypical antipsychotics varied, the majority of these deaths were the result of cardiovascular problems (eg, heart failure, sudden death) or infections (eg, pneumonia). There is a risk of venous thromboembolism (VTE) during treatment with antipsychotics. In patients treated with antipsychotic drugs, especially those with acquired risk factors for VTE, prophylactic measures should be taken and any potential risk factor for VTE assessed before and during treatment with Chlorpromazine Canon. Except in exceptional circumstances, Chlorpromazine Canon should not be used in Parkinson's disease. The occurrence of intestinal obstruction, which can be detected by bloating and abdominal pain, requires emergency care. Predisposing factors for the development of arrhythmia when taking chlorpromazine are: hypokalemia (including when using diuretics that cause hypokalemia), bradycardia (including those caused by the drug), an existing (congenital or acquired) increase in the duration of the QT interval. The simultaneous administration of chlorpromazine with dopaminergic non-antiparkinsonian drugs (cabergoline, quinagolide) is not recommended due to the mutual antagonism of dopamine agonists and antipsychotics. Concomitant use with other antipsychotics that can cause irritation (amisupride, cyamemazine, droperidol, fluphenazine, propericiazine, haloperidol, levomepromazine, pimozide, pipamperone, pipothiazine, sertindole, sulypiride, sultopride, tiapride) is not recommended. Concomitant use with antiparasitic drugs (halofantrine, lumefantrine, pentamidine) is not recommended. Also, simultaneous use with antifungal agents from the azole group is not recommended (increased risk of arrhythmia). If it is impossible to avoid the co-administration of the above combinations, it is recommended to carry out regular ECG monitoring with monitoring of the duration of the QT interval. When using non-potassium-sparing diuretics, correction of hypokalemia and ECG monitoring are necessary before starting chlorpromazine therapy. Monitoring during treatment with Chlorpromazine Canon should be increased: • in patients with epilepsy and a history of seizures, due to the possibility of a decrease in the seizure threshold. The occurrence of seizures requires cessation of treatment. • in elderly patients with: a) high susceptibility and the effect of orthostatic hypotension (increased risk of excessive sedation and hypotensive effects), b) chronic constipation (risk of paralytic intestinal obstruction), c) possible prostatic hypertrophy; • in patients with cardiovascular diseases taking quinidine, due to a possible increase in the hypotensive effect; • in case of liver failure and/or severe renal failure, due to the risk of accumulation. For long-term treatment, regular ophthalmological monitoring is recommended. It should be taken into account that the use of phenothiazine derivatives can lead to hyperglycemia or impaired glucose tolerance, development or exacerbation of diabetes mellitus, hypercholesterolemia, fecal impaction, severe intestinal obstruction and megacolon. Since in high doses (100 mg/day) chlorpromazine can cause an increase in blood glucose levels by reducing insulin secretion, in patients with diabetes mellitus it is necessary to adjust insulin doses before and after completion of therapy. If necessary, the dose of the antipsychotic should also be adjusted in patients taking sulfonylureas. Chlorpromazine should not be used as monotherapy if depression predominates. Use Chlorpromazine Canon with caution in case of hypersensitivity to other phenothiazine drugs or severe respiratory diseases. Due to the risk of photosensitivity, ultraviolet irradiation should be avoided. Chlorpromazine may worsen or promote the manifestation of latent myasthenia gravis
, and also cause myasthenic syndrome. To avoid the development of the “neuroleptic malignant syndrome” syndrome). Patients with pheochromacetoma taking chlorpromazine may experience false positive blood catecholamine levels. During therapy, it is necessary to stop drinking alcohol, since chlorpromazine enhances the inhibitory effect of alcohol on the central nervous system.
Interaction
The injection solution cannot be mixed in the same syringe with other drugs.
Chlorpromazine, when taken orally with drugs that depress the central nervous system (anticonvulsants, narcotic analgesics, ethanol, barbiturates and other hypnotics), can enhance their inhibitory effect and also cause respiratory depression.
Weakens the effect of Ephedrine , amphetamines , Clonidine and Guanethidine .
Long-term combination with analgesics is undesirable.
Chlorpromazine inhibits the effect of levodopa , possibly increasing extrapyramidal symptoms.
When used with anticholinesterase drugs, severe muscle weakness appears; with Amitriptyline - the risk of developing gastrointestinal dyskinesia; with Diazoxide - severe hyperglycemia; with Zopiclone - increased sedative effect.
When used with antacids, absorption from the gastrointestinal tract is impaired and the concentration of the drug in the blood decreases; with Cimetidine , the concentration in the blood also decreases.
When used with Morphine myoclonus develops ; with lithium carbonate - the neurotoxic effect increases and pronounced extrapyramidal symptoms appear.
When used with Trazodone , arterial hypotension occurs; with Propranolol - increased concentrations of Propranolol and Chlorpromazine; with Trifluoperazine - severe hyperpyrexia; with Phenytoin - change in the concentration of phenytoin in the blood.
When used with Fluoxetine there is an increased risk of extrapyramidal symptoms, and when used with chloroquine or sulfadoxine there is a high risk of Chlorpromazine toxicity.
Analogs and Synonyms of Chlorpromazine
Level 4 ATC code matches:
Propazine
Tizercin
Aminazine
Analogs have the same mechanism of action, but contain different active substances.
Analogs are Levomepromazine , Thioproperazine , Perphenazine , Trifluoperazine and Fluphenazine .
Synonyms of Chlorpromazine (contain the same active ingredient): Aminazine , Aminazine Ferein , Chlopromazine hydrochloride .
Reviews
Reviews about the drug are varied. Many believe that the drug has a strong sedative but weak antipsychotic effect. Indeed, Trifluoperazine Fluphenazine from the same group of phenothiazines is 20 times superior to Chlorpromazine in neuroleptic activity, and significantly inferior to it in sedative effect.
In this regard, the drug is best used as an emergency method to relieve acute psychomotor and emotional agitation.
“...it puts him to sleep for a long time, and the next day he feels drowsy.”
“...drank (for several weeks) Chlorpromazine at night... You drink it at night, during the day you feel like an “exhausted rag.” When I finished taking it, I noticed an effect in the form of an improved mood.”
There are reviews of long-term treatment with pills after quitting a binge, which was accompanied by minimal productive symptoms (delusions, hallucinations).
“...helped bring my husband back to life. After binge drinking, hallucinations began, first the drug was dripped, then she was given pills for a month and a half. The medicine is very powerful, the attacks of aggression have stopped.”