Chlorpromazine

Chlorpromazine has antiemetic and sedative properties. Is an antipsychotic.

[1], [2], [3], [4]

Indications of the chlorpromazine

Applicable in the following cases:

• the state of paranoia (acute or chronic stages);
• state of hallucinatory nature;
• schizophrenia, on the background of which excitation of psychomotor character is noted;
• manic form of excitement;
• Attacks of epilepsy, accompanied by psychotic disorders;
• Depression of agitated nature;
• status epilepticus;
• psychosis due to excessive drinking;
• increased muscle tone;
• presence of pain syndrome;
• constant insomnia;
• dermatoses of an itchy character (such as eczema or neurodermatitis);
• increased exposure to anesthesia.

As a drug that helps to remove vomiting, it is used for padalexmia, toxicosis in pregnant women, and in addition, during radiotherapy.

[5], [6]

Release form

The release occurs in the form of a solution for injection, and in addition, in dragees and tablets.

[7], [8]

Pharmacodynamics

Chlorpromazine is an antipsychotic from the category of phenothiazines, represents 1 generation of neuroleptics. Neuroleptic effect develops by blocking the conductors of dopamine inside individual cerebral structures. Thanks to their blockade, pituitary prolactin production increases. The drug blocks and α-adrenoreceptors, resulting in a sedative effect.

The central antiemetic effect arises from the blockade of D2-conductors within a certain cerebellar region, and the peripheral effect is due to the blockade of the vagus nerve. Antiemetic activity of drugs is associated with its antihistamine, sedative and anticholinergic properties.

Antipsychotic activity of drugs manifests itself in the form of eliminating hallucinations and delusions, reducing tension, anxiety, anxiety and fear, and in addition to stopping psychomotor agitation. Has a very rapid sedative effect, in connection with which it is used in the treatment of acute forms of psychosis. It is forbidden to apply for depression.

It also has hypothermic, anti-shocks, anti-tick and anti-arrhythmic effects, and besides it has moderate extrapyramidal effect.

[9], [10], [11], [12], [13],

Pharmacokinetics

The drug for oral use is absorbed quickly, but not completely. Peak values reach after 3-4 hours.

There is also an effect of the first hepatic transmission, which means that when administered orally, the level of the substance in the blood will be lower than when the drug is administered parenterally.

Metabolic processes occur in the liver, forming the products of decay (in active and inactive form). Protein synthesis inside the plasma is 95-98%. The medicine passes through the BBB, and its indices 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 within the plasma, as well as the drug effect.

The half-life is 30+ hours. Metabolism products are excreted with bile and urine.

[14], [15], [16], [17]

Dosing and administration

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

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

If a patient has an anxious condition before surgery, 0.5-1 ml of medication is administered intramuscularly (2 hours before the procedure is performed).

For children, the sizes of single doses for intravenous or intramuscular injection are 250-500 μg / kg.

When administered orally, the adult initial dose is 25-100 mg / day. It is taken all at once or divided into 4 receptions. If necessary, it is permitted to increase the dosage to 0.7-1 g / day. In single cases it is allowed to increase the portion to 1.2-1.5 g / day. For 1 admission an adult can use no more than 0.3 g of drugs, and for the whole day - a maximum of 1.5 g.

It should also be remembered that with a prolonged therapeutic course, you should constantly monitor the indices of PTV and control the composition of the blood.

[27], [28], [29], [30]

Use of the chlorpromazine during pregnancy

Do not use Chlorpromazine during pregnancy.

Contraindications

The main contraindications:

• the presence of intolerance in relation to the drug;
• kidney / liver failure in severe degree;
• state of coma;
• cerebral trauma (at the stage of exacerbation);
• strokes;
• marked suppression of hematopoiesis processes;
• hypothyroidism;
• heart failure in decompensated form (against the background of heart defects);
• thromboembolic syndrome;
• bronchiectasis in severe degree;
• glaucoma of a closed angle;
• urolithiasis and cholelithiasis;
• ulcerative lesions in the gastrointestinal tract at the stage of exacerbation;
• the period of breastfeeding;
• infants up to 1 year old.

[18], [19], [20]

Side effects of the chlorpromazine

The use of drugs can trigger the following side-effects:

• extrapyramidal disorders, anxiety and restlessness, problems with thermoregulation, trembling paralysis. Occasionally there are cramps;
• the development of tachycardia, as well as a decrease in the values of blood pressure (with intravenous injections of drugs);
• manifestations of dyspepsia (with oral administration);
• development of agranulocytosis or leukopenia;
• retention of urination;
• gynecomastia or impotence, and in addition menstruation disorders and weight gain;
• the development of erythema or dermatitis, the appearance of itching, rashes and skin pigmentation.

Due to the prolonged use of drugs, deposition of the substance in the lens and cornea can occur, which causes the aging processes of the former to accelerate. After the introduction of drugs, intramuscularly sometimes infiltrates are formed, and after intravenous injections, phlebitis appears.

[21], [22], [23], [24], [25], [26]

Overdose

In case of poisoning with Chlorpromazine, there is a persistent drop in pressure indices, development of toxic form of hepatitis, neuroleptic syndrome, and hypothermia in addition.

To eliminate the disorder, symptomatic procedures are prescribed.

[31], [32], [33], [34], [35]

Interactions with other drugs

It is forbidden to mix the solution with other medicines inside one syringe.

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

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

Prohibited long-term use in combination with analgesics.

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

When used together with cholinesterase inhibitors, muscle weakness develops. The combination with amitriptyline can cause dyskinesia in the gastrointestinal tract.

Combination with diazoxide induces severe hyperglycemia, and with zopiclone, a potentiation of sedation.

Use in combination with antacids disrupts the absorption of drugs from the gastrointestinal tract, and in addition reduces the level of its active element within the blood. The use of cimetidine also reduces the indices of Chlorpromazine inside the blood.

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

Simultaneous use with trazodone reduces the values of blood pressure, and the combination with propranolol increases the performance of both drugs. The combination with trifluoperazine leads to the development of hyperpyrexia in a severe degree, and with phenytoin - it changes its indices inside the blood.

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

[36], [37], [38], [39]

Storage conditions

Chlorpromazine is required to be kept at temperature values not exceeding 25 ° C.

[40], [41], [42]

Shelf life

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

[43], [44], [45]

Reviews

Chlorpromazine receives enough polar reviews. There are many people who consider the drug effective in providing sedative effects, but it is rather weak from the point of view of the antipsychotic substance. This is not surprising, because fluphenazine with trifluoperazine from the same drug category (phenothiazines) is stronger than Chlorpromazine by its neuroleptic influence 20 times, but their sedative properties are much weaker than in this drug.

Because of this, the medicine is recommended to be used as a means for rendering an ambulance - to stop the acute excitement of an emotional and psychomotor nature.