Chlorpromazine

Chlorpromazine has antiemetic and sedative properties. It is a neuroleptic.

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Indications Chlorpromazine

It is used in the following cases:

• states of paranoia (acute or chronic stages);
• hallucinatory states;
• schizophrenia, against the background of which there is excitement of a psychomotor nature;
• manic form of excitement;
• epileptic seizures accompanied by psychotic disorders;
• depression of an agitated nature;
• status epilepticus;
• psychosis due to excessive alcohol consumption;
• increased muscle tone;
• presence of pain syndrome;
• constant insomnia;
• dermatoses of an itchy nature (such as eczema or neurodermatitis);
• enhancing the effects of anesthesia.

As a drug that helps to stop vomiting, it is used for palemicia, toxicosis in pregnant women, and also during radiation therapy.

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Release form

It is released in the form of a solution for injection, as well as in dragees and tablets.

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Pharmacodynamics

Chlorpromazine is an antipsychotic from the phenothiazine category, represents the 1st generation of neuroleptics. The neuroleptic effect develops by blocking dopamine conductors inside individual brain structures. Due to their blockade, the production of prolactin by the pituitary gland increases. The drug also blocks α-adrenergic receptors, resulting in a sedative effect.

The central antiemetic effect occurs due to the blockade of D2-conductors within a certain cerebellar region, and the peripheral effect is due to the blockade of the vagus intestinal nerve. The antiemetic activity of the drug is associated with its antihistamine, sedative and cholinolytic properties.

The antipsychotic activity of the drug manifests itself in the form of eliminating hallucinations and delusions, reducing tension, feelings of anxiety, worry and fear, and in addition to this, stopping psychomotor agitation. It has a very rapid sedative effect, which is why it is used in the treatment of acute forms of psychosis. It is prohibited to use in depression.

It also has hypothermic, anti-shock, anti-hiccup and anti-arrhythmic effects, as well as a moderate extrapyramidal effect.

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Pharmacokinetics

The drug is absorbed quickly when taken orally, but not completely. Peak values are reached after 3-4 hours.

There is also a first-pass effect, which means that when taken orally, the blood level of the drug will be lower than when the drug is administered parenterally.

Metabolic processes occur in the liver, forming decay products (in active and inactive form). Protein synthesis inside the plasma is 95-98%. The drug passes through the BBB, and its indicators inside the brain are always higher than inside the blood. There is no direct relationship between the values of the active element and its metabolic products inside the plasma, as well as the drug effect.

Half-life is 30+ hours. Metabolic products are excreted in bile and urine.

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Dosing and administration

The choice of dosage form for therapy (parenteral or oral use) is determined by the clinical picture.

Adults require a dose of 25-50 mg (or 1-2 ml) for injections and intravenous administration. If necessary, the procedure can be repeated at intervals of 3-12 hours. When administering the drug intramuscularly, it is necessary to dilute the substance in a 0.9% sodium chloride solution (2 ml). For intravenous injections, the drug is diluted in 20 ml of the drug. In one procedure, an adult can be administered no more than 150 mg (intramuscularly) and 100 mg (intravenously).

If the patient experiences anxiety before the operation, he is given 0.5-1 ml of the drug intramuscularly (2 hours before the procedure).

For children, single doses for intravenous or intramuscular administration are 250-500 mcg/kg.

When taken orally, the adult initial dose is 25-100 mg/day. It is taken all at once or divided into 4 doses. If necessary, the dosage can be increased to 0.7-1 g/day. In isolated cases, the dose can be increased to 1.2-1.5 g/day. An adult can take no more than 0.3 g of the drug per dose, and a maximum of 1.5 g per day.

It is also necessary to remember that during a long-term therapeutic course, it is necessary to constantly monitor the PT indicators and control the blood composition.

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Use Chlorpromazine during pregnancy

Chlorpromazine should not be used during pregnancy.

Contraindications

Main contraindications:

• the presence of intolerance to the drug;
• severe renal/liver failure;
• state of coma;
• brain injuries (at the acute stage);
• strokes;
• pronounced suppression of hematopoietic processes;
• hypothyroidism;
• heart failure in decompensated form (against the background of heart defects);
• thromboembolic syndrome;
• severe bronchiectasis;
• closed-angle glaucoma;
• urolithiasis and cholelithiasis;
• ulcerative lesions in the gastrointestinal tract in the acute stage;
• breastfeeding period;
• infants up to 1 year old.

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Side effects Chlorpromazine

The use of drugs may provoke the occurrence of the following side effects:

• extrapyramidal disorders, anxiety and restlessness, problems with thermoregulation, shaking palsy. Convulsions occasionally occur;
• development of tachycardia, as well as a decrease in blood pressure values (with intravenous injections of drugs);
• manifestations of dyspepsia (with oral use);
• development of agranulocytosis or leukopenia;
• urinary retention;
• gynecomastia or impotence, as well as menstrual irregularities and weight gain;
• development of erythema or dermatitis, the appearance of itching, rashes and skin pigmentation.

Due to prolonged use of the drug, deposition of the substance in the area of the lens and cornea may occur, which accelerates the aging processes of the former. After intramuscular administration of the drug, infiltrates sometimes form, and after intravenous injections, phlebitis appears.

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Overdose

In case of poisoning with Chlorpromazine, a persistent decrease in blood pressure, the development of a toxic form of hepatitis, neuroleptic syndrome, and also hypothermia are observed.

To eliminate the disorders, symptomatic procedures are prescribed.

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Interactions with other drugs

It is prohibited to mix the solution with other medications in the same syringe.

Oral administration of Chlorpromazine together with drugs that suppress the central nervous system (opiates, ethyl alcohol, anticonvulsants, barbiturates, and other sleeping pills) can potentiate their suppressive effect and lead to depression of respiratory activity.

The drug reduces the effectiveness of amphetamines, guanethidine, and also ephedrine and clonidine.

Long-term use in combination with analgesics is prohibited.

The drug inhibits the effects of levodopa and may potentiate extrapyramidal manifestations.

When used together with cholinesterase inhibitors, muscle weakness occurs. Combination with amitriptyline can cause dyskinesia in the gastrointestinal tract.

Combination with diazoxide causes pronounced hyperglycemia, and with zopiclone – potentiation of the sedative effect.

Use in combination with antacids disrupts the absorption of the drug from the gastrointestinal tract, and in addition, reduces the level of its active element in the blood. Use with cimetidine also reduces the levels of Chlorpromazine in the blood.

The combination of the drug with morphine will lead to the development of myoclonus. The combination with lithium carbonate increases the neurotoxic properties of the drug and leads to the development of pronounced extrapyramidal signs.

Simultaneous use with trazodone reduces blood pressure values, and combination with propranolol increases the values of both drugs. Combination with trifluoperazine leads to the development of severe hyperpyrexia, and with phenytoin - changes its values in the blood.

Combination with fluoxetine increases the likelihood of extrapyramidal disorders, and use together with sulfadoxine or chloroquine increases the risk of developing toxic effects of Chlorpromazine.

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Storage conditions

Chlorpromazine must be kept at temperatures not exceeding 25°C.

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Shelf life

Chlorpromazine is allowed to be used for 2 years from the date of release of the drug.

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Reviews

Chlorpromazine receives quite polar reviews. There are many people who consider the drug effective in providing a sedative effect, but at the same time rather weak in terms of an antipsychotic substance. This is not surprising, because fluphenazine with trifluoperazine from the same drug category (phenothiazines) in their neuroleptic effect is 20 times stronger than Chlorpromazine, but at the same time their sedative properties are significantly weaker than this drug.

Because of this, the drug is recommended for use as a means of providing emergency care - to relieve acute excitement of an emotional and psychomotor nature.