Haloperidol is an antipsychotic drug used in psychiatry and neurology. It has a pronounced effect and a large list of side effects. Almost 80% of people who used this drug experienced one or more negative symptoms. Therefore, it must be used strictly in the dose prescribed by the doctor.
Compound
The active substance is haloperidol .
The tablets contain 1.5 or 5 mg of this substance. Additional elements are: talc, potato starch, gelatin, magnesium stearate, lactose monohydrate.
1 ml of solution contains 5 mg of active substance. Additional substances are: injection water, lactic acid, methylparaben, propylparaben.
Drops from the company Ratiopharm contain 2 mg of active substance per 1 ml. Additional substances are: methyl parahydroxybenzoate, purified water, propyl parahydroxybenzoate, lactic acid.
Pharmacodynamics and pharmacokinetics
The active component is a butyrophenone derivative. Blocks dopamine, postsynaptic receptors in the mesocortical, mesolimbic structures of the brain, has a pronounced antipsychotic effect. Despite its high antipsychotic activity , the drug combines moderate sedative and antiemetic effects. It does not have an anticholinergic effect, but causes extrapyramidal disorders. The sedative effect is due to the blockade of alpha-adrenergic receptors in the reticular pharmacy.
The antiemetic effect is achieved by blocking the vomiting center in the trigger zone. When dopamine receptors are blocked in the hypothalamus, galactorrhea and hypothermic effects appear. With long-term therapy, a change in endocrine status occurs, the production of gonadotropic hormones decreases and the synthesis of prolactin due to the effect on the anterior lobe. The drug eliminates persistent personality changes, mania, hallucinations, delusions, and increases the patient’s interest in the world around him.
Haloperidol is prescribed to patients who have developed resistance to other antipsychotic medications. The drug has an activating effect on patients.
In hyperactive children, Haloperidol can eliminate behavioral disorders and excessive motor activity.
Haloperidol decanoate has a longer duration of action compared to haloperidol.
The therapeutic effect of prolonged forms of the drug lasts up to 6 weeks.
The maximum concentration after using the solution is observed after 10-20 minutes, when using tablets - after 3-6 hours. The solution and tablets are excreted in urine and feces in a ratio of 2:3. Drops are excreted in bile (15%) and urine (40%).
How does the active ingredient work?
The medicine "Haloperidol" in drops contains one active substance. It is a derivative of the complex organic compound butyrophenone. The instructions for use for Haloperidol (in drops) describe the active substance and some points regarding the mechanism of its action. Haloperidol is a powerful antipsychotic whose action is based on blocking dopamine receptors, which play an important functional role in the functioning of the central nervous system. Another functional feature of this substance is a moderate sedative effect associated with inhibition of α-adrenergic receptors in the limbic and mesocortical structures of the brain. The drug also affects the D2 receptors of the hypothalamus, which affects the decrease in body temperature and the activation of prolactin production, which causes galactorrhea, not only in women, but also in men.
Indications for use of Haloperidol
Indications for use are as follows. The drug is prescribed for hallucinations , delusions, acute psychosis, paranoid states , psychomotor agitation, “steroid” psychosis, alcoholic and drug psychosis, agitated depression, mental retardation, Tourette’s disease , psychoses of various origins, Huntington’s chorea , psychosomatic disorders, stuttering, childhood autism , hyperactivity in children.
Analogs
It is strictly prohibited to independently select similar drugs, since any antipsychotic is prescribed by a doctor depending on the severity of mental disorders. Replacement drugs can be:
- Azaleptin;
- Etaperazine;
- Invega;
- Moditen;
- Sonapax;
- Azaleptol;
- Quetixol;
- Senorm;
- Triftazin;
- Thiorol.
These drugs have similar indications for use and a list of side effects.
Contraindications
The medicine is not used for severe depression of the central nervous system, for intolerance to the active substance, for central nervous system pathology, which is accompanied by extrapyramidal and pyramidal symptoms, for breastfeeding , hysteria, depression, Parkinson's disease, during pregnancy, for children under three years of age. In case of impaired intracardiac conduction, with angina pectoris, prolongation of the QT interval, with angle-closure glaucoma, with hypokalemia, decompensated heart disease, with epilepsy, thyrotoxicosis, kidney and liver pathology, with respiratory and pulmonary heart failure, with alcoholism, prostatic hyperplasia with urinary retention , in acute infectious diseases, in COPD, Haloperidol is used with caution.
Side effects of Haloperidol
Nervous system: drowsiness, headaches, agitation, anxiety, akathisia , fears, restlessness, exacerbation of hallucinations, psychoses, lethargy, depression or euphoria , epileptic seizures, tardive dyskinesia, with long-term therapy extrapyramidal disorders are noted, tardive dystonia (eyelid spasms, frequent blinking , uncontrolled movements of the arms, legs, torso, neck), neuroleptic malignant syndrome (loss of consciousness, urinary incontinence, rapid or difficult breathing, increased sweating, instability of blood pressure, arrhythmia, tachycardia , hyperthermia, epileptic seizures, muscle rigidity).
Cardiovascular system: signs of ventricular fibrillation and flutter on the ECG, tachycardia, arrhythmia, orthostatic hypotension , drop in blood pressure.
Digestive system: constipation , dry mouth, decreased appetite, hyposalivation, diarrhea, nausea, vomiting, liver dysfunction.
Hematopoietic organs: tendency to monocytosis, erythropenia, agranulocytosis, leukocytosis, leukopenia - are temporary.
Genitourinary system: priapism, increased libido or decreased potency, menstrual irregularities in females, hyperprolactinemia , gynecomastia , pain in the mammary glands, peripheral edema; with prostatic hyperplasia, urinary retention is noted.
The following side effects are also possible: allergic reactions, photosensitivity , laryngospasm, bronchospasm, maculopapular changes in the skin, blurred vision, retinopathy, cataracts, hyponatremia, hypoglycemia, weight gain, alopecia.
Instructions for use of Haloperidol (Method and dosage)
Haloperidol tablets, instructions for use
Take orally with a full glass of milk and water. The initial dosage is 0.5-5 mg three times a day. No more than 100 mg per day. The duration of therapy is 2-3 months. The drug is discontinued gradually, the dosage is reduced slowly, and maintenance doses are switched to - 5-10 mg per day.
Tourette's disease, non-psychotic behavioral disorders: 2-3 times a day 0.05 mg/kg/day, with a gradual increase in dose by 0.5 mg once a week to a maximum of 0.075 mg/kg/day.
Using the solution
The average single dosage for intramuscular administration of Haloperidol is 2-5 mg, the interval between injections is 48 hours. Acute alcoholic psychosis: intravenously 5-10 mg.
Instructions for Haloperidol Ratiopharm drops
Typically consumed up to three times a day with food.
Adults are usually prescribed 0.5-1.5 mg 3 times a day. Further, the dose of the drug can be increased to an average of 10-15 mg per day. For acute symptoms, it is allowed to take 15 mg per day or more. The maximum dose is 100 mg per day.
The initial dose for children from three years of age is 0.025-0.05 mg per kg of body weight, taken 3 times. The maximum can be increased to 0.2 mg per kg of body weight.
The path of a substance in the human body
One of the most popular drugs in psychiatric practice is Haloperidol drops. The dosage of the product calculated by the manufacturer takes into account the pharmacokinetics of the active substance. Once in the human body, the drug is actively absorbed, up to 60% of the substance is absorbed by tissues. The absorbed amount of the drug has 92% biological activity. It binds well to blood proteins and successfully penetrates histohematic barriers. A feature of the metabolism of haloperidol is its so-called “first pass” ability, however, this substance does not have pharmacologically active metabolites. Its maximum concentration in the blood is reached within 3 hours, and the half-life from the body averages one day. Haloperidol is excreted from the body through the liver with urine and feces. If there is a need for hemodialysis, it should be taken into account that due to the large volume of distribution, as well as the low concentration in the blood, only a small amount of the substance can be removed from the body in this way.
Overdose
Manifested by tremors, muscle rigidity , and a drop in blood pressure. In severe cases, shock, respiratory depression, and coma are recorded. Gastric lavage and administration of enterosorbents are required. Norepinephrine and albumin are used to improve blood circulation. epinephrine is unacceptable . Antiparkinsonian drugs and central anticholinergic blockers can reduce the severity of extrapyramidal symptoms. Dialysis has not proven effective.
Interaction
Haloperidol enhances the severity of the inhibitory effect of hypnotics, barbiturates, opioid analgesics , tricyclic antidepressants, ethanol, and general anesthesia on the central nervous system. The drug enhances the effect of antihypertensive drugs, m-anticholinergics, inhibits the metabolism of MAO inhibitors, tricyclic antidepressants, while their toxicity and sedative effect mutually increase. Buprorion in combination with haloperidol increases the likelihood of grand mal seizures and reduces the epileptic threshold. The drug weakens the vasoconstrictor effect of norepinephrine, phenylephrine , dopamine, epinephrine. The medication reduces the effectiveness of anticonvulsants , antiparkinsonian drugs, and changes the effect of anticoagulants. The risk of developing mental disorders increases when prescribed with the drug Methyldopa . Amphetamines can reduce the antipsychotic effect of haloperidol. When drinking strong coffee or tea, there is a decrease in the effectiveness of haloperidol. Antiparkinsonian, antihistamine, anticholinergic drugs enhance the m-anticholinergic effect of the neuroleptic and reduce the severity of its antipsychotic effect. With long-term use of inducers of microsomal oxidation, barbiturates, carbamazepine , the concentration of the antipsychotic in the blood decreases. In combination with lithium drugs, the formation of encephalopathy and increased severity of extrapyramidal disorders is possible. Fluoxetine can increase the severity of extrapyramidal symptoms and side effects from the nervous system. Prescription of drugs that cause extrapyramidal reactions leads to an increase in the severity and frequency of extrapyramidal disorders .
Reviews from patients and doctors
People's reviews about Haloperidol are mostly positive, let's see what doctors and patients say.
Reviews from doctors
Reviews from doctors indicate that Haloperidol is best used in emergencies :
- “I recommend using haloperidol only in critical cases, since the drug is very powerful. The most important thing is not to self-medicate, but to consult a doctor in time.” (Konstantinov R.A.)
- “Haloperidol is an excellent drug that is widely used in medicine. The drug has many side effects, but if used correctly and all recommendations are followed, no difficulties should arise with its use .” (Savelyev S.U.)
Patient reviews
Meanwhile, patients say the following:
- “I didn’t like this medicine at all. Its composition is pure chemistry. Just poison yourself and your children. Don't buy it! Buy something natural instead!” (Nina)
- “A good product that we bought for my grandfather, and which did the job one hundred percent! But there were side effects in the form of attacks of dyspepsia... But it quickly passed!” (Vera Nikolaevna)
special instructions
Regular monitoring of liver test levels, ECG dynamics, and blood parameters are required. Parenteral administration of the drug is carried out only under the supervision of the attending physician. After achieving a therapeutic effect, they switch to taking tablet forms of the drug. If tardive dyskinesia during treatment, a gradual reduction in dosage is required until complete cessation. When taking a hot bath, heat stroke is possible due to the suppression of peripheral, central thermoregulation located in the hypothalamus. Caution is required when performing strenuous physical work. It is not recommended to use over-the-counter “anti-cold” medications during the entire treatment period due to the risk of heat stroke and increased anticholinergic effects. Due to the risk of photosensitivity, patients must protect exposed skin from exposure to sunlight. Haloperidol is discontinued gradually due to the risk of developing withdrawal syndrome. Often, the antiemetic effect of the drug masks signs of drug toxicity , and also complicates the diagnosis of conditions that are accompanied by nausea. Haloperidol may precipitate when mixing its solution with tea or coffee. Before prescribing long-acting forms of the drug, the patient is transferred to Haloperidol from other antipsychotics to prevent sudden hypersensitivity to the drug. The medication affects driving.
The medicine is described in Wikipedia.
INN: haloperidol.
OKPD: 24.42.13.693
In what cases is medicine in drops prescribed?
The main area of application of Haloperidol drops is psychiatric practice, although sometimes it can be prescribed to eliminate vomiting, for example, during treatment of cancer. The main indications for the use of this antipsychotic drug will be the following diseases and conditions:
- delirium, hallucinations, delirious syndromes, catatonic syndromes, thinking disorders, disorders of consciousness against the background of acute psychotic syndromes;
- psychoses of endogenous and exogenous etiology in the chronic stage;
- psychomotor agitation;
- vomit;
- stuttering.
The instructions for use contain all the necessary information about the drug “Haloperidol” (drops). The product receives good reviews from both patients and doctors, who successfully use it as a prophylactic and to suppress symptoms of psychosis and psychotic syndromes of various origins.
Haloperidol price, where to buy
The price of Haloperidol tablets 1.5 mg 50 pieces is 45-50 rubles.
10 ampoules of 5 mg/ml cost approximately 75 rubles.
- Online pharmacies in RussiaRussia
ZdravCity
- Haloperidol solution for intravenous and intramuscular injection.
5mg/ml amp. 1ml No. 10Ozon LLC 96 rub. order - Haloperidol Welfarm solution for intravenous and intramuscular injection. 5mg/ml amp. 1ml 10 pcs. Welfarm LLC
RUB 199 order
- Haloperidol-Ratiopharm drops for internal use. approx. 2mg/ml 30mlTeva
51 RUR order
- Haloperidol-Richter solution for intravenous and intramuscular injection. 5mg/ml 1ml 5 pcs. JSC Gedeon Richter
126 rub. order
- Haloperidol tablets 1.5 mg 50 pcs. Ozon LLC
47 RUR order
