What is haloperidol prescribed for? Contraindications for use. Usual Dose for Psychosis in Children

Dosage form: tablets Composition:

1 tablet 1.5 mg contains:

active substance: haloperidol - 1.5 mg.

excipients: lactose monohydrate (milk sugar) - 76.5 mg, corn starch - 6.0 mg, povidone K17 - 3.3 mg, microcrystalline cellulose - 10.0 mg, magnesium stearate - 0.7 mg, pregelatinized starch - 2, 0 mg.

1 tablet 5 mg contains:

active substance: haloperidol - 5 mg.

excipients: lactose monohydrate (milk sugar) - 73.0 mg, corn starch - 6.0 mg, povidone K17 - 3.3 mg, microcrystalline cellulose - 10.0 mg, magnesium stearate - 0.7 mg, pregelatinized starch - 2, 0 mg.

Description: Tablets with a dosage of 1.5 mg: white or white with a slightly yellowish tint, flat-cylindrical in shape with a score on one side and a chamfer on both sides.

Tablets with a dosage of 5 mg: white or white with a slightly yellowish tint, biconvex shape.

Pharmacotherapeutic group:Antipsychotic (neuroleptic) ATX:

N.05.A.D.01 Haloperidol

Pharmacodynamics:Antipsychotic drug (neuroleptic), butyrophenone derivative. It has a pronounced antipsychotic effect, a sedative effect (in small doses it has an activating effect) and a pronounced antiemetic effect. Causes extrapyramidal disorders and has virtually no anticholinergic effect.

The sedative effect is due to the blockade of alpha-adrenergic receptors in the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D2 receptors of the trigger zone of the vomiting center; hypothermic effect and galactorrhea - blockade of dopamine receptors of the hypothalamus. Long-term use is accompanied by a change in endocrine status, in the anterior lobe of the pituitary gland the production of prolactin increases and the production of gonadotropic hormones decreases.

Pharmacokinetics:Absorption when taken orally - 60%. The time to reach maximum concentration (T Cmax) after oral administration is 3 hours. Volume of distribution is 18 l/kg, binding to plasma proteins is 92%. Easily passes through histohematic barriers, including the blood-brain barrier (BBB).

Metabolized in the liver, has a “first pass” effect through the liver. The isoenzymes CYP2D6, CYP3A, CYP3A5, and CYP3A7 are involved in the metabolism of the drug. It is an inhibitor of CYP2D6. There are no active metabolites. The half-life (T 1/2) when taken orally is 24 hours (12-37 hours).

Excreted in bile and urine: after oral administration, 15% is excreted in bile, 40% in urine (including 1% unchanged). Passes into breast milk.

Indications: - Acute and chronic psychoses, accompanied by agitation, hallucinatory and delusional disorders, manic states, psychosomatic disorders.

Behavioral disorders, personality changes (paranoid, schizoid, and others), Gilles de la Tourette syndrome, both in childhood and in adults.

Tiki, Huntington's chorea.

Long-term and treatment-resistant vomiting, including those associated with antitumor therapy, and hiccups.

Contraindications:Hypersensitivity, severe depression of the function of the central nervous system (CNS) due to intoxication with xenobiotics, coma of various origins, diseases of the central nervous system accompanied by pyramidal or extrapyramidal symptoms (including Parkinson's disease), pregnancy, lactation, children's age (up to 3 years for this drug forms). With caution:Decompensated diseases of the cardiovascular system (CVS) (including angina pectoris, intracardiac conduction disorders, prolongation of the QT interval or a predisposition to this - hypokalemia, simultaneous use of other drugs that can cause prolongation of the QT interval), history of epilepsy and convulsive conditions, angle-closure glaucoma, liver and/or renal failure, hyperthyroidism (with symptoms of thyrotoxicosis), pulmonary-cardiac and respiratory failure(including chronic obstructive pulmonary diseases and acute infectious diseases), prostatic hyperplasia with urinary retention, alcoholism. Pregnancy and lactation: Contraindicated. Directions for use and dosage:Orally, during or after meals, with a full (240 ml) glass of water or milk, the initial dose for adults is 0.5 - 5 mg 2 - 3 times a day. If necessary, the dose is gradually increased until the desired therapeutic effect is achieved (on average - up to 10-15 mg, with chronic forms schizophrenia - up to 20-60 mg). Maximum dose- 100 mg/day. Duration of treatment is 2 - 3 months. Reduce the dose slowly, maintenance doses - 5-10 mg/day.

Elderly or weakened patients are prescribed orally at the beginning of treatment, 0.5 - 2 mg 2 - 3 times a day.

If it is necessary to use 0.5 mg of the drug, it is recommended to use tablets with a lower dosage.

Children 3-12 years old (or weighing 15-40 kg) with psychotic disorders - orally, 0.05 mg/kg/day in 2-3 divided doses; if necessary, taking into account tolerability, the dose is increased by 0.5 mg 1 time over 5-7 days to a total dose of 0.15 mg/kg/day. For non-psychotic behavioral disorders, Tourette's disease - orally, initially 0.05 mg/kg/day in 2-3 divided doses, then the dose is increased by 0.5 mg once every 5-7 days to 0.075 mg/kg/day . For childhood autism - orally, 0.025-0.05 mg/kg/day. For prescribing the drug in childhood, it is advisable to use dosage forms for children, allowing precise dosing of the drug.

If there is no effect within 1 month, it is not recommended to continue treatment.

Side effects:From the nervous system: headache, dizziness, insomnia or drowsiness (of varying severity), restlessness, anxiety, psychomotor agitation, fear, akathisia, euphoria, depression, epileptic seizures, in rare cases, exacerbation of psychosis, incl. hallucinations; extrapyramidal disorders; with long-term treatment - tardive dyskinesia (smacking and wrinkling of the lips, puffing out of the cheeks, rapid and worm-like movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the arms and legs), tardive dystonia (frequent blinking or spasms of the eyelids, unusual facial expression or body position, uncontrolled bending movements of the neck, torso, arms and legs) and neuroleptic malignant syndrome (hyperthermia, muscle rigidity, difficulty or rapid breathing, tachycardia, arrhythmia, increased or decreased blood pressure (BP), increased sweating, urinary incontinence, convulsive disorders, depression of consciousness).

From the cardiovascular system: when used in high doses - decreased blood pressure, orthostatic hypotension, arrhythmias, tachycardia, ECG changes (prolongation of the QT interval, signs of ventricular flutter and fibrillation).

From the outside digestive system : when used in high doses - loss of appetite, dry mouth, hyposalivation, nausea, vomiting, diarrhea or constipation, impaired liver function, up to the development of jaundice.

From the hematopoietic organs: rarely - temporary leukopenia or leukocytosis, agranulocytosis, erythropenia and a tendency to monocytosis.

From the outside genitourinary system: urinary retention (with prostatic hyperplasia), peripheral edema, pain in mammary glands, gynecomastia, hyperprolactinemia, disorder menstrual cycle, decreased potency, increased libido, priapism.

From the senses: cataracts, retinopathy, blurred vision.

Allergic reactions: maculopapular and acne-like skin changes, photosensitivity, rarely - bronchospasm, laryngospasm.

Laboratory indicators: hyponatremia, hyper- or hypoglycemia.

Others: alopecia, weight gain.

Overdose: Symptoms: depression of consciousness, muscle rigidity, tremor, drowsiness, decreased blood pressure, and sometimes increased blood pressure. In severe cases - coma, respiratory depression, shock.

In case of respiratory depression - mechanical ventilation. To improve blood circulation, plasma or albumin solution is injected intravenously. in these cases, use is strictly prohibited! To reduce extrapyramidal symptoms - central anticholinergic drugs and antiparkinsonian drugs. Dialysis is ineffective.

Interaction: Increases the severity of the depressant effect on the central nervous system of ethanol, tricyclic antidepressants, opioid analgesics, barbiturates and hypnotic drugs, drugs for general anesthesia.

Enhances the effect of peripheral m-anticholinergic drugs and most antihypertensive drugs (reduces the effect of guanethidine due to its displacement from alpha-adrenergic neurons and suppression of its uptake by these neurons).

It inhibits the metabolism of tricyclic antidepressants and MAO inhibitors, thereby increasing (mutually) their sedative effect and toxicity.

When used simultaneously with bupropion, it reduces the epileptic threshold and increases the risk of grand mal seizures.

Reduces the effect of anticonvulsants (lowering the seizure threshold with haloperidol).

Weakens the vasoconstrictor effect of dopamine, phenylephrine, norepinephrine, ephedrine and eninephrine (blockade of alpha-adrenergic receptors by haloperidol, which can lead to a distortion of the action of epinephrine and a paradoxical decrease in blood pressure).

Reduces the effect of antiparkinsonian drugs (antagonistic effect on dopaminergic structures of the central nervous system).

Changes (may increase or decrease) the effect of anticoagulants.

Reduces the effect of bromocriptine (dose adjustment may be required).

When used with methyldota, it increases the risk of developing mental disorders (including disorientation in space, slowing down and difficulty thinking).

Amphetamines reduce the antipsychotic effect of haloperidol, which in turn reduces their psychostimulant effect (blockade of alpha-adrenergic receptors by haloperidol).

Anticholinergic, antihistamine (first generation) and antiparkinsonian drugs can enhance the m-anticholinergic effect of haloperidol and reduce its antipsychotic effect (dose adjustment may be required).

Long-term administration of carbamazepine, barbiturates and other inducers of microsomal oxidation reduces the concentration of haloperidol in plasma.

In combination with lithium preparations (especially in high doses), the development of encephalopathy (can cause irreversible neurointoxication) and increased extrapyramidal symptoms is possible.

When taken simultaneously with fluoxetine, the risk of developing side effects from the central nervous system, especially extrapyramidal reactions, increases.

When used simultaneously with drugs that cause extrapyramidal reactions, it increases the frequency and severity of extrapyramidal disorders.

Use strong tea or coffee (especially in large quantities) reduces the effect of haloperidol.

Special instructions:During therapy, patients should regularly monitor ECG, blood counts, and liver tests.

Caution must be exercised when performing heavy physical work, acceptance hot bath(possible development heatstroke due to suppression of central and peripheral thermoregulation in the hypothalamus).

Haloperidol. Scary tale with a good ending

Those who were born in new Russia, you’ve hardly heard about the horrors of Soviet punitive medicine. And for Soviet people, haloperidol was one of the horror stories. They called this medicine, with the help of which they fought against dissidents, all the names - vitamin “G”, “tick”, “galik”. They said that the drug was used on those disliked by the state, political prisoners, dissidents, not in order to cure them, but to break their will and ultimately transform healthy person into a vegetable. Probably, the horror stories had something to do with reality. But this does not negate the fact that, in fact, they were talking about one of the most effective and most necessary antipsychotic drugs ever invented by mankind.

The story of haloperidol is a classic story of how the search for one unexpectedly leads to the appearance of another. Let's remember Coca-Cola, when pharmacist Pemberton from Atlanta had to change the recipe of the French Wine Coca drink, removing alcohol from it and replacing it with stimulants from cola nuts. Suddenly random buyer diluted the sweet, sticky syrup with soda and got the most famous drink and the most expensive brand in the world.

Haloperidol (international name Haloperidolum) is one of the most powerful antipsychotics, and it has no equal in relieving severe mental disorders and acute agitation, hallucinations, delusions, aggressive behavior, manic state.

In the pre-neuroleptic period, schizophrenia, like other mental illnesses, essentially meant a death sentence - the patient remained alive, but could not return to the world of normal people with existing treatment methods. At first, patients were treated with herbs of little use - belladonna, henbane, opiates, or they used bromides, narcotic sleep, or even flogging. With the advent of lithium salts and antihistamines The situation with the treatment of psychosis has only slightly improved. The subsequent electroshock therapy and lobotomy, widespread at that time and known from the cult film One Flew Over the Cuckoo's Nest, also could not boast of success.

The psychopharmacological era was opened by the appearance of chlopromazine in the middle of the last century, the first synthesized antipsychotic (translated from Greek as “taking, seizing the nervous system”).

It was haloperidol that became the greatest achievement for psychiatry of the twentieth century, becoming a milestone in the treatment of schizophrenia and other mental illnesses. The medicine opened the way for a new generation of drugs with better tolerability and fewer side effects. By taking haloperidol, patients were able to leave straitjackets for the first time and live outside the hospital walls.

Haloperidol was invented in Belgium, a small European country whose residents are offended when their achievements are underestimated or attributed to others. This quality of the Belgians was well noted by the famous Agatha Christie when she came up with the image of detective Hercule Poirot - the great detective always corrected his interlocutor if he, praising his “gray cells,” called him a Frenchman and not a Belgian.

The invention of haloperidol in the 50s of the last century is an achievement that the Belgians should be proud of, and just like the lyrical music of the Belgian bard Jacques Brel, haloperidol spread throughout the world, sounding in many languages, becoming a classic. The invention of a team of young enthusiastic scientists under the leadership of the talented chemist Paul Janssen is still considered the gold standard for the treatment of acute mental illnesses, in particular schizophrenia, and is included in the main list of medicines World Organization healthcare.

Inherited from his father, Dr. Constant Janssen, the entrepreneurial spirit and talent of an inventor have made Paul Janssen, founder of the world-famous Janssen Pharmaceutica Corporation, an icon. scientific world. He gave humanity several hundred drugs, including haloperidol. Perhaps haloperidol would not have existed at all if it were not for the young chemist’s dream of inventing new drugs and, of course, the personality of Paul Janssen himself, or Doctor Paul, as his employees later respectfully and affectionately called him.

Having received an excellent education in the field of natural sciences, having studied the work of US pharmaceutical plants, having served military service in Germany and after working as an assistant in a university laboratory, Paul, the eldest of the four Janssen children, entered his father's office.

In the early 1930s, Constant Janssen, in collaboration with Gedeon Richter's company, founded his own pharmaceutical factory in his hometown of Turnhout in northern Belgium, where a large family lived. Of course, the father wanted his son to work in his factory. But Paul had his own plan - to found an independent research company that would be ready for new discoveries in the field of pharmacology, create new synthetic drugs, and identify them pharmacological properties simple tests and also received a stable income. He himself was deeply convinced that the future of pharmaceuticals lay in the discovery of fundamentally new drugs and the synthesis of new components, and not in the combination of existing ones. By the early 1950s, Paul was already close to realizing his dream, but he could not do it without his father’s support.

So, in 1953, his father gave him part of his factory in Turnheit - the premises, however, were more like a garage. But this did not stop the new laboratory, headed by Paul Janssen, from starting development. Later, he merged with his father's factory to form Janssen Pharmaceutica, and in 1961 - with Johnson & Johnson. At the beginning of his career, Paul understood that without the creation of new drugs and their successful distribution, it was impossible to create a thriving company, and his father’s factory, which imported and produced vitamin supplements, tonics, stimulants and organic extracts, simply could not survive.

Haloperidol has become a major advance in the treatment of schizophrenia and other mental illnesses. By taking haloperidol, patients were able to leave straitjackets for the first time and even live outside the hospital.

The conditions for creating pharmaceutical masterpieces were not the best: there were virtually no trained personnel, the team consisted of five people, including Paul himself, many of the employees did not have an academic degree or experience, and the oldest researcher was only 27 years old. There was no budget - almost all the equipment, which was extremely simple, was made by the employees themselves. Despite the fact that the chances of success were catastrophically low, Paul Janssen’s dream began to come true: all efforts were thrown into concentrating on the production of new chemical compounds. A team of like-minded people was ready to work without a break, seven days a week. Young enthusiasts with inquisitive minds had no idea about the difficulties, but unconditionally believed in success, and this became a decisive factor in their favor. During the first three years, Paul Janssen's group synthesized and tested approximately 800 new chemical compounds. Today it seems incredible, but eight of them came to the market as medicines.

One day, Janssen agreed with Professor Arnold Beckett from the pharmaceutical department of Chelsea College in London to prepare more powerful painkillers - derivatives of the painkiller meperidine - and began experiments. The results were promising. However, the new compounds were structurally similar to existing ones, and their reproduction would violate patent rights. Then young chemists began to change molecular structures, expanding the molecular chain. Bert Hermans synthesized a new compound (R 1625) on February 15, 1958, by attaching a molecule known as butyrophenone, a compound from the group of aromatic ketones, to the test molecule.

The experiments involved mice and an ordinary small tile in the form of a heated plate, which everyday life I wouldn't let the coffee get cold. All compounds that were synthesized in the laboratory were tested primarily for their analgesic effect: a stopwatch was used to measure the time after which the mouse, while on this stove, begins to feel the hot surface and licks its paws to cool them. When the drugs were administered, the rodents tried to escape from the glass flask and run away from the hot plate, but with this compound the reaction of the mice was the opposite. They behaved as if they were drugged with tranquilizers. They didn't move at all - they just sat on the iron plate, and they didn't seem to care about the hot burner at all. It became obvious that the new compound should be used not in anesthesia, but in psychiatry.

Further research has shown that haloperidol is safer and more effective than chlorpromazine and is more potent at low doses—50 mg of chlorpromazine is equivalent to 1 mg of haloperidol. There was no lethargy from the new drug—lab animals tolerated the drug well, and Janssen was amazed at how it negated the effects of amphetamine. Then he noticed similarities between some of the symptoms of schizophrenia and the effects of amphetamine intoxication in professional cyclists who use these drugs for doping. The scientist continued to study a new compound with properties opposite to those of amphetamine.

The compound successfully tested for safety in mice and dogs, and Janssen contacted psychiatrists Paul Divry and Jean Bobon from a clinic in Liege and gave them a sample of the compound. Soon, something incredible happened in a psychiatric clinic - unexpectedly the compound was tested on a person.

One night, a young student, the son of a local doctor, was brought to the clinic with severe psychosis. He had hallucinations and was very aggressive. The doctors remembered the sample of the medicine that Janssen had sent. Since the drug was successfully tested on animals, it was decided to administer it to the patient - the first dose was 10 mg. The effect of the new compound was unexpectedly strong and fast. The very next morning the young man recovered. After recovery, he took haloperidol 1 mg every day for seven years. The results were excellent: this student successfully completed his studies, worked, got married and had children. Seven years later, after consulting with doctors, he stopped taking the medicine. The consequences of this decision turned out to be tragic - he fell ill again and never fully recovered.

After the first successful clinical trial of haloperidol in humans with convincing results, it took another year of clinical research to bring the drug to market. Subsequent clinical trials, including at St. Anne in Paris by Jean Delais and Pierre Demiquet, confirmed that haloperidol belongs to the pharmacological group of antipsychotics, as defined in 1955. Clinical trial data also showed that haloperidol was particularly active against delusions and hallucinations. In September 1959, the drug was presented publicly at the International Conference in Beers (Belgium). Haloperidol was licensed and began to be produced in Belgium in October 1959 under the name trade name Haldol.

Having changed the world of psychiatry forever, having made a real revolution in the treatment of schizophrenia, haloperidol became the first representative of a completely new chemical group and the founder of the butyroferon group. It was new stage in drug therapy of psychosis. The antipsychotic drug turned out to be the drug that can “put out the fire” of mental disorders.

The term "chemical shock" is used to describe the spectrum of action of haloperidol. By blocking central dopaminergic receptors and influencing dopamine, a brain neurotransmitter, the substance through which nerve impulses are transmitted, haloperidol delays the transmission of dopamine at synapses. nerve cells– places of contact of neurons with each other.

In modern psychiatry, haloperidol is one of the active and effective antipsychotics, a standard for the relief of acute psychotic states. It is used to treat schizophrenic and alcoholic psychoses, for example delirium tremens, manic and paranoid states, delirium and many other diseases that are accompanied by hallucinations and psychomotor agitation.

Haloperidol not only has a sedative effect, but also potentiates the effect of sleeping pills, narcotics and analgesics, so it can be used in preparation for surgery.

Later, in the 1960s, work on research continued, and Haloperidol Decanoate was developed, a long-acting drug that could be administered once a month. Janssen's company later introduced more improved versions of haloperidol, including resperidone.

Despite the fact that haloperidol is an unpromoted drug, in Russia it is produced by several pharmaceutical companies in tablets and in the form of a solution for intravenous and intramuscular injection, as well as drops. Russian and foreign manufacturers produce them under their own trade names, emphasizing that the drug comes off their assembly line. So, for example, Russian company"Akrikhin" produces the medicine in tablets "Haloperidol-Akri". And the German company Ratiopharm GmbH (Germany) produces Haloperidol-Ratiopharm. The Russian manufacturer Bryntsalov-A (Moscow region) produces Haloperidol-Ferein - drops for oral administration, tablets, solutions for injections. Haloperidol is also produced in the form of tablets by ZAO Biokom (Stavropol).

The most generous company for the production of haloperidol is Gedeon Richter (Hungary). Under license from Janssen Pharmaceutica, the company produces solution, drops, and tablets. In addition, the Hungarian pharmaceutical company produces long-acting haloperidol - “Haloperidol decanoate” - oil solution for intramuscular administration with sesame oil.

It is obvious that haloperidol, despite its “dark” and controversial past and side effects - extrapyramidal disorders such as parkinsonism, dystonia, tremor and akathisia (the patient’s inability to sit still), undoubtedly still inspires confidence among doctors in the treatment of psychosis not only in Russia, but in many countries and will be in demand for many more decades.

From the book 2008_42 (590) author Newspaper Duel

A TERRIBLE TALE For high mountains Yes, beyond the blue seas, against the sky, there lived on earth the glorious country of Ochohonia. It was so big that it could not be walked on foot and could not be flown over in the summer. The Lord God did not offend her, generously gifting her with wide seas and fast, deep rivers. On

From the book Musical Reserve. 70s. Problems. Portraits. Cases author Cherednichenko Tatyana

CASES with “The End of the Time of Composers” Music theory classes teach you to easily sight-read the second parts of an ensemble (you don’t have to play half of the texture, the main thing is to catch the diagram of the form), and I turned out to be a convenient replacement for the sick second pianist for the premiere

From the book Afterword to the Rebellion author Saveliev Andrey Nikolaevich

Before the end of Russian history The fact that the political orientation of people does not depend on their social status becomes self-evident. No one, not even Marxist fanatics, risks directly linking the potential possibilities of this or that political

From the book Universal Journalist by Randall David

From the book Education and Education at School author Krupskaya Nadezhda Konstantinovna

WHAT A TEACHER SHOULD HAVE TO BE A GOOD SOVIET TEACHER Improving the quality of school education requires that the teacher master the art of teaching. What is needed for this? The school section of the GUS dealt with this issue and made the appropriate conclusions. Presentation

From the book Literary Newspaper 6316 (No. 12 2011) author Literary Newspaper

A scary tale about the love of reading Literature A scary tale about the love of reading BOOK PLACE For the first time, the Russian State Children's Library hosted the “Night in the Library” event, designed to demonstrate to young readers that a book depository is not a place at all

From the book “Open up, military police!” author Rozov Alexander Alexandrovich

3. Before the end of oil Many states indulge in ambitious patriotic games, but in different ways. In prosperous civilized countries, these games are financed on a residual basis, i.e. from funds that people can allocate without tightening their belts. In countries

From the book In the Land of Strangeness author Kublitsky Georgy Ivanovich

Conversation with a fairytale ending Wang lies in a mountain basin. The waters of the lake are calm, cold, and transparent. Boats near the pier invite you to flex your muscles. The paths going into the mountains promise delightful walks. The owner of the Wang Hotel assured us that tomorrow there will be

From book 100 famous riddles nature author Syadro Vladimir Vladimirovich

A SCARY TALE IN A NEW WAY It seemed that heartbreaking stories about the terrible degeneration of people into vampires had long since sunk into the past. Horror films about Dracula and others like him are perceived as fairy tales. Unless science fiction writers stubbornly abandon this topic. Special attention

From the book Excitement, Joy, Hope. Thoughts on parenting author Nemtsov Vladimir Ivanovich

Even good children are not allowed to play with matches. I once wrote about this in one of my novels. For young man who does not yet know the labor value of money, they are more dangerous than matches for a small child. This is the main problem. But I don't want to say that this only applies to

From the book GIRL FROM THE BOOK OF REVIEWS author Svobodin Alexander Petrovich

A more complex case - the film pretends to be good. The example with “The Great Escape” is not complicated. Such an elementary lack of novelty (not a place, but the essence of what is happening) can be noticed by a more or less sophisticated moviegoer, but there are more thinly disguised cases

From the book Newspaper Tomorrow 17 (1066 2014) author Zavtra Newspaper

Scenes from life before the end of the world? Ekaterina Glushik April 24, 2014 0 Culture On April 20, the premiere of the play “Concert on the Occasion of the End of the World” took place at the “Commonwealth of Taganka Actors” theater. How to achieve polyphony without cacophony? How to harness a horse and a tremulous horse into one harness

From the book Literary Newspaper 6466 (No. 23 2014) author Literary Newspaper

A story with a happy ending About ten years ago I received a small parcel. It contained a book with pictures and a letter from an unknown person, Lyudmila Fadeeva, from Kolpin, near St. Petersburg. From it I learned that Lyudmila Leonidovna works as an art teacher and at the same time

From the book The End of the Ukraine Project author Korovin Valery Mikhailovich

Part 2. Before the end (while there was hope) At the end of November 2013, the Ukrainian authorities suddenly postponed the signing of an association agreement with Europe, and Kyiv announced its intention to recreate trade and economic relations with Russia and other CIS member countries. Such

From the book Signal and Noise. Why do some predictions come true and others not? by Silver Nate

What makes a good prognosis? “Of course, a research scientist isn't executed on the spot for watching the Weather Channel, but many of them do it behind closed doors,” Dr. Bruce Rose, the affable scientific director and vice president of the Weather Channel (TWC), told me.

From the book Practical Political Science: A Guide to Contacting Reality author Shulman Ekaterina

How to become a good deputy The draft law on the right of factions to deprive deputies of their mandate will not be considered during the current spring session: the relevant committee on constitutional legislation sent it to the mailing list until July 9, and the last meeting of the current session

Preparation Haloperidol- neuroleptic, butyrophenone derivative, has antipsychotic, sedative, antiemetic effects.
Blocks postsynaptic dopaminergic receptors located in the mesolimbic system (antipsychotic effect), hypothalamus (hypothermic effect and galactorrhea), trigger zone of the vomiting center, extrapyramidal system; inhibits central alpha-adrenergic receptors. Inhibits the release of mediators, reducing the permeability of presynaptic membranes, disrupts reverse neuronal uptake and deposition.
Eliminates persistent personality changes, delusions, hallucinations, mania, and increases interest in the environment. Affects autonomic functions (reduces the tone of hollow organs, motility and secretion of the gastrointestinal tract, eliminates vascular spasms) in diseases accompanied by agitation, anxiety, and fear of death. Long-term use is accompanied by a change in endocrine status; in the anterior lobe of the pituitary gland, the production of prolactin increases and the production of gonadotropic hormones decreases.
When taken orally, 60% is absorbed. Plasma protein binding - 92%. Tmax when administered orally - 3-6 hours, with intramuscular administration - 10-20 minutes, with intramuscular administration of a prolonged form (haloperidol decanoate) - 3-9 days (in some patients, especially in the elderly - 1 day ). Intensively distributed in tissue, because easily passes histohematic barriers, including the BBB. Vss is 18 l/kg. Metabolized in the liver, undergoes the first pass effect through the liver. A strict relationship between plasma concentrations and effects has not been established. T1/2 for oral administration - 24 hours (12-37 hours), for intramuscular administration - 21 hours (17-25 hours), for intravenous administration - 14 hours (10-19 hours), for haloperidol decanoate - 3 weeks (single or multiple doses). Excreted by the kidneys and bile.
Effective in patients resistant to other antipsychotic drugs. Has some activating effect. In hyperactive children eliminates excess motor activity, behavioral disorders (impulsivity, difficulty concentrating, aggressiveness).

Indications for use

Indications for use of the drug Haloperidol are: psychomotor agitation of various origins (manic state, mental retardation, psychopathy, schizophrenia, chronic alcoholism), delusions and hallucinations (paranoid states, acute psychosis), Gilles de la Tourette's syndrome, Huntington's chorea, psychosomatic disorders, behavioral disorders in the elderly and children, stuttering, long-lasting and treatment-resistant vomiting and hiccups. For haloperidol decanoate: schizophrenia (maintenance therapy).

Directions for use

Preparation Haloperidol It is used intravenously, intramuscularly and orally. The dosage regimen is set individually. For cupping psychomotor agitation adults - 5-10 mg IM or IV with possible one- or two-time repeated administration after 30-40 minutes. Orally, the initial dose for adults is 0.5-5 mg 2-3 times a day, then the dose is gradually increased until a stable therapeutic effect is obtained (on average up to 10-15 mg/day, for chronic forms of schizophrenia - up to 20-60 mg /day), followed by a transition to a lower maintenance dose. The maximum daily dose is 100 mg.
The dose for children over 3 years of age is calculated according to body weight.
Elderly and weakened patients are prescribed a lower dose.
Injection solution containing haloperidol decanoate - strictly intramuscularly, initial dose - 25-75 mg once every 4 weeks.

Side effects

From the nervous system and sensory organs: akathisia, dystonic extrapyramidal disorders (including spasms of the muscles of the face, neck and back, tic-like movements or twitching, weakness in the arms and legs), parkinsonian extrapyramidal disorders (including difficulty speaking and swallowing, mask-like face, shuffling gait, tremor of hands and fingers), headache, insomnia, drowsiness, restlessness, anxiety, agitation, agitation, euphoria or depression, lethargy, epileptic seizures, confusion, exacerbation of psychosis and hallucinations, tardive dyskinesia (see " Precautionary measures"); visual impairment (including visual acuity), cataracts, retinopathy.
From the cardiovascular system and blood (hematopoiesis, hemostasis): tachycardia, arterial hypotension/hypertension, QT interval prolongation, ventricular arrhythmia, ECG changes; there have been reports of cases of sudden death, prolongation of the QT interval and torsade de pointes (TdP) (see Precautions); transient leukopenia and leukocytosis, erythropenia, anemia, agranulocytosis.
From the respiratory system: laryngospasm, bronchospasm.
From the gastrointestinal tract: anorexia, constipation/diarrhea, hypersalivation, nausea, vomiting, dry mouth, impaired liver function, obstructive jaundice.
From the genitourinary system: engorgement of the mammary glands, unusual milk secretion, mastalgia, gynecomastia, menstrual irregularities, urinary retention, impotence, increased libido, priapism.
From the outside skin: maculopapular and acne-like skin changes, photosensitivity, alopecia.
Other: antipsychotic malignant syndrome accompanied by hyperthermia, muscle rigidity, loss of consciousness; hyperprolactinemia, sweating, hyperglycemia/hypoglycemia, hyponatremia.

Contraindications

:
Contraindications to the use of the drug Haloperidol are: hypersensitivity, severe toxic depression of the central nervous system or coma caused by taking drugs; CNS diseases accompanied by pyramidal and extrapyramidal symptoms (incl.

Parkinson's disease), epilepsy (the seizure threshold may decrease), severe depressive disorders (symptoms may worsen), cardiovascular diseases with decompensation symptoms, pregnancy, breastfeeding, age up to 3 years.
With caution. Glaucoma or predisposition to it, pulmonary failure, hyperthyroidism or thyrotoxicosis, impaired liver and/or kidney function, urinary retention.

Pregnancy

:
Contraindicated for use Haloperidol during pregnancy.
FDA category of effect on the fetus is C.
During treatment, you should stop breastfeeding (passes into breast milk).

Interaction with other drugs

Haloperidol enhances the effect of antihypertensive drugs, opioid analgesics, antidepressants, barbiturates, alcohol, weakens the effect of indirect anticoagulants. Inhibits the metabolism of tricyclic antidepressants (their plasma levels increase) and increases toxicity. With long-term administration of carbamazepine, the plasma level of haloperidol falls (the dose must be increased). In combination with lithium, it can cause an encephalopathy-like syndrome.

Overdose

:
Symptoms of drug overdose Haloperidol: severe extrapyramidal disorders, arterial hypotension, drowsiness, lethargy, in severe cases - coma, respiratory depression, shock.
Treatment: there is no specific antidote. Gastric lavage and subsequent administration of activated charcoal are possible (if the overdose is associated with ingestion). In case of respiratory depression - mechanical ventilation, with a pronounced decrease in blood pressure - the introduction of plasma-substituting fluids, plasma, norepinephrine (but not adrenaline!), to reduce the severity of extrapyramidal disorders - central anticholinergic blockers and antiparkinsonian drugs.

Storage conditions

List B. In a cool, dry place.

Release form

Haloperidol - tablets in packs of 50 pieces of 0.0015 g and 0.005 g.
Haloperidol - ampoules of 1 ml of 0.5% solution in a package of 5 pieces; in bottles of 10 ml of 0.2% solution.

Additionally

:
Increased mortality in older patients with dementia-associated psychosis. According to the Food and Drug Administration (FDA)1, antipsychotic drugs increase mortality in elderly patients when treating psychosis associated with dementia. An analysis of 17 placebo-controlled studies (lasting 10 weeks) in patients taking atypical antipsychotic drugs revealed an increase in drug-associated mortality by 1.6-1.7 times compared with patients receiving placebo. In typical 10-week controlled studies, the percentage of drug-attributable mortality was about 4.5%, compared with 2.6% in the placebo group. Although the causes of death varied, most were related to cardiovascular problems (such as heart failure, sudden death) or pneumonia. Observational studies suggest that, like atypical antipsychotics, treatment with traditional antipsychotics may also be associated with increased mortality.
Tardive dyskinesia. As with other antipsychotics, haloperidol is associated with the development of tardive dyskinesia, a syndrome characterized by involuntary movements (may occur in some patients with long-term treatment or occur after drug therapy was discontinued). The risk of developing tardive dyskinesia is higher in older patients during high-dose therapy, especially in women. Symptoms are persistent and, in some patients, irreversible: rhythmic involuntary movements of the tongue, face, mouth and jaw (for example, protrusion of the tongue, puffing out of the cheeks, puckering of the lips, uncontrolled chewing movements), sometimes they can be accompanied by involuntary movements of the limbs and torso. If tardive dyskinesia develops, discontinuation of the drug is recommended.
Dystonic extrapyramidal disorders are most common in children and young adults and at the beginning of treatment; may subside within 24-48 hours after stopping haloperidol. Parkinsonian extrapyramidal effects more often develop in older people and are detected in the first few days of treatment or during long-term therapy.
Cardiovascular effects. Cases of sudden death, QT prolongation, and torsades de pointes have been reported in patients receiving haloperidol. Caution should be exercised when treating patients with predisposition factors to prolongation of the QT interval, incl. electrolyte imbalance (especially hypokalemia and hypomagnesemia), simultaneous use of drugs that prolong the QT interval. When treating with haloperidol, it is necessary to regularly monitor the ECG, blood count, and evaluate the level of liver enzymes. During therapy, patients should refrain from potential activities dangerous species activities requiring increased attention, quick mental and motor reactions.

Basic parameters

Name:	HALOPERIDOL
ATX code:	N05AD01 -

In this article you can find instructions for use medicinal product Haloperidol. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Haloperidol in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Haloperidol analogues, if available structural analogues. Use for the treatment of schizophrenia, autism and other psychoses in adults, children, as well as during pregnancy and lactation. Interaction of the drug with alcohol.

Haloperidol- an antipsychotic belonging to butyrophenone derivatives. It has a pronounced antipsychotic and antiemetic effect.

The action of haloperidol is associated with the blockade of central dopamine (D2) and alpha-adrenergic receptors in the mesocortical and limbic structures of the brain. Blockade of D2 receptors in the hypothalamus leads to a decrease in body temperature and galactorrhea (increased production of prolactin). Inhibition of dopamine receptors in the trigger zone of the vomiting center underlies the antiemetic effect. Interaction with dopaminergic structures of the extrapyramidal system can lead to extrapyramidal disorders. Pronounced antipsychotic activity is combined with a moderate sedative effect (in small doses it has an activating effect).

Strengthens the effect of sleeping pills, narcotic analgesics, drugs for general anesthesia, analgesics and other drugs that depress the function of the central nervous system.

Pharmacokinetics

Absorbed by passive diffusion, in non-ionized form, mainly from small intestine. Bioavailability - 60-70%. Haloperidol is metabolized in the liver; the metabolite is pharmacologically inactive. Haloperidol also undergoes oxidative N-dealkylation and glucuronidation. Excreted in the form of metabolites through the intestines - 60% (including with bile - 15%), by the kidneys - 40% (including 1% - unchanged). Easily penetrates histohematic barriers, incl. through the placental and hematoencephalic, penetrates into breast milk.

Indications

acute and chronic psychoses, accompanied by agitation, hallucinatory and delusional disorders (schizophrenia, affective disorders, psychosomatic disorders);
behavioral disorders, personality changes (paranoid, schizoid and others), incl. and in childhood, autism, Gilles de la Tourette syndrome;
tics, Huntington's chorea;
long-lasting and untreatable hiccups;
vomiting that cannot be treated with classical antiemetics, including those associated with antitumor therapy;
premedication before surgery.

Release forms

Solution for intravenous and intramuscular administration (injections in injection ampoules).

Solution for intramuscular administration (oil) Haloperidol Decanoate (forte or prolong formula).

Tablets 1 mg, 1.5 mg, 2 mg, 5 mg and 10 mg.

There are no other forms, be it drops or capsules.

Instructions for use and dosage

The dosage depends on the clinical response of the patient. Most often, this means a gradual increase in the dose in the acute phase of the disease; in the case of maintenance doses, a gradual reduction in the dose to ensure the lowest effective dose. High doses are used only in cases of ineffectiveness of lower doses. Average doses are suggested below.

To relieve psychomotor agitation in the first days, haloperidol is prescribed intramuscularly at 2.5-5 mg 2-3 times a day, or intravenously at the same dosage (the ampoule should be diluted in 10-15 ml of water for injection), the maximum daily dose is 60 mg. Once a stable sedative effect is achieved, the drug is taken orally.

For elderly patients: 0.5 - 1.5 mg (0.1-0.3 ml of solution), maximum daily dose - 5 mg (1 ml of solution).

Parenteral administration of haloperidol should be carried out under close medical supervision, especially in elderly patients and children. After achieving a therapeutic effect, you should switch to taking the drug orally.

Pills

Prescribed orally, 30 minutes before meals (can be taken with milk to reduce irritation to the gastric mucosa).

The initial daily dose is 1.5-5 mg, divided into 2-3 doses. Then the dose is gradually increased by 1.5-3 mg (in resistant cases up to 5 mg) until the required therapeutic effect is achieved. The maximum daily dose is 100 mg. On average, the therapeutic dose is 10-15 mg per day, for chronic forms of schizophrenia - 20-40 mg per day, if necessary, the dose can be increased to 50-60 mg per day. On average, the duration of treatment is 2-3 months. Maintenance doses (out of exacerbation) - from 0.5-0.75 mg to 5 mg per day (the dose is reduced gradually).

Elderly and debilitated patients are prescribed 1/3-1/2 the usual dose for adults, the dose is increased no more often than every 2-3 days.

As an antiemetic, 1.5-2.5 mg is prescribed orally.

Oil solution (Decanoate)

The drug is intended exclusively for adults, exclusively for intramuscular administration!

Do not administer intravenously!

Adults: patients on long-term treatment with oral antipsychotics(mainly haloperidol), switching to depot injections can be recommended.

The dose should be adjusted on an individual basis due to significant individual differences in response to treatment. Dose selection should be carried out under strict medical supervision of the patient. The choice of the initial dose is carried out taking into account the symptoms of the disease, its severity, the dose of haloperidol or other antipsychotics prescribed during previous treatment.

At the beginning of treatment, every 4 weeks it is recommended to prescribe doses 10-15 times higher than the dose of oral haloperidol, which usually corresponds to 25-75 mg of Haloperidol Decanoate (0.5-1.5 ml). The maximum initial dose should not exceed 100 mg.

Depending on the effect, the dose can be increased stepwise, by 50 mg, until the optimal effect is obtained. Typically the maintenance dose corresponds to 20 times the daily dose of oral haloperidol. If symptoms of the underlying disease return during the dose adjustment period, treatment with Haloperidol Decanoate can be supplemented with oral haloperidol.

Injections are usually given every 4 weeks, but due to large individual differences in effectiveness, more may be required. frequent use drug.

Side effect

headache;
insomnia or drowsiness (especially at the beginning of treatment);
anxiety;
anxiety;
excitation;
fears;
euphoria or depression;
lethargy;
epilepsy attacks;
development of a paradoxical reaction - exacerbation of psychosis and hallucinations;
tardive dyskinesia (smacking and wrinkling of lips, puffing out of cheeks, rapid and worm-like movements of the tongue, uncontrolled chewing movements, uncontrolled movements of arms and legs);
tardive dystonia (frequent blinking or spasms of the eyelids, unusual facial expression or body position, uncontrolled bending movements of the neck, torso, arms and legs);
malignant neuroleptic syndrome (difficulty or rapid breathing, tachycardia, arrhythmia, hyperthermia, increased or decreased blood pressure, increased sweating, urinary incontinence, muscle rigidity, epileptic seizures, loss of consciousness);
decrease in blood pressure;
orthostatic hypotension;
arrhythmias;
tachycardia;
changes on the ECG (prolongation of the QT interval, signs of flutter and ventricular fibrillation);
decreased appetite;
dry mouth;
hyposalivation;
nausea, vomiting;
diarrhea or constipation;
transient leukopenia or leukocytosis, agranulocytosis, erythropenia;
urinary retention (with prostatic hyperplasia);
peripheral edema;
pain in the mammary glands;
gynecomastia;
hyperprolactinemia;
menstrual irregularities;
decreased potency;
increased libido;
priapism;
cataract;
retinopathy;
blurred vision;
photosensitivity;
bronchospasm;
laryngospasm;
development local reactions related to injection;
alopecia;
increase in body weight.

Contraindications

depression of the central nervous system, incl. and severe toxic depression of central nervous system function caused by xenobiotics, coma of various origins;
diseases of the central nervous system accompanied by pyramidal and extrapyramidal disorders (Parkinson's disease);
lesions of the basal ganglia;
children under 3 years of age;
depression;
hypersensitivity to butyrophenone derivatives;
hypersensitivity to the ingredients of the drug.

Use during pregnancy and breastfeeding

Haloperidol does not cause a significant increase in the number of cases birth defects development. There are isolated cases of birth defects when taking haloperidol concomitantly with other medications during pregnancy. Taking haloperidol during pregnancy is permissible only in cases where the expected benefit to the mother outweighs the risk to the fetus. Haloperidol is released from breast milk. In cases where haloperidol is unavoidable, the benefits breastfeeding in relation to the potential danger must be justified. In some cases, estrapyramidal symptoms have been observed in newborns whose mothers took haloperidol during lactation.

Use in children

Contraindicated in children under 3 years of age.

Solution for intravenous and intramuscular administration

For children over 3 years of age, the dose is 0.025-0.05 mg per day, divided into 2 injections. The maximum daily dose is 0.15 mg/kg.

Parenteral administration of haloperidol should be carried out under close medical supervision, especially in children. After achieving a therapeutic effect, you should switch to taking the drug orally.

Pills

Children aged 3-12 years (with a body weight of 15-40 kg): 0.025-0.05 mg/kg body weight per day 2-3 times a day, increasing the dose no more than once every 5-7 days, up to daily dose 0.15 mg/kg.

For behavioral disorders, Tourette's syndrome: 0.05 mg/kg per day, divided into 2-3 doses and increasing the dose no more than once every 5-7 days to 3 mg per day. For autism - 0.025-0.05 mg/kg per day.

Special instructions

Parenteral administration should be carried out under the strict supervision of a physician, especially in the case of elderly patients and children. Once the therapeutic effect is achieved, you should switch to the oral form of treatment.

Because haloperidol may cause QT prolongation, caution should be used if there is a risk of QT prolongation (QT syndrome, hypokalemia, drugs known to prolong the QT interval), especially parenteral administration. Due to the metabolism of haloperidol in the liver, it is important to exercise caution when prescribing it to patients with impaired hepatic function.

There are known cases of seizures caused by haloperidol. Patients with epilepsy and patients in conditions predisposing to the development of convulsive syndrome (alcoholism, brain injury) should use the drug with extreme caution.

If you are lactose intolerant, please note that a 1.5 mg tablet contains 157 mg of lactose, a 5 mg tablet contains 153.5 mg.

For severe physical activity, taking a hot bath requires caution due to possible development heat stroke as a result of ineffective central and peripheral thermoregulation of the hypothalamus due to taking the drug.

The patient should be warned about the need to avoid taking medications against colds purchased without a prescription, because it is possible to enhance the anticholinergic effects of haloperidol and develop heat stroke. During treatment, patients should regularly monitor ECG, blood counts, and liver tests.

To relieve extrapyramidal disorders, antiparkinsonian drugs (cyclodol), nootropics, and vitamins are prescribed; their use is continued after haloperidol is discontinued if they are eliminated from the body faster than haloperidol in order to avoid increased extrapyramidal symptoms.

The severity of extrapyramidal disorders is dose-related; often, when the dose is reduced, they may decrease or disappear.

In some cases, signs neurological disorders observed when discontinuing the drug, after a long course of treatment, so haloperidol should be discontinued, gradually reducing the dose.

If tardive dyskinesia develops, the drug should not be abruptly discontinued; A gradual dose reduction is recommended.

Exposed skin should be protected from excess sunlight due to the increased risk of photosensitization in such cases.

The antiemetic effect of haloperidol may mask signs of drug toxicity and make it difficult to diagnose conditions in which nausea is the first symptom.

Impact on the ability to drive vehicles and operate machinery

While taking haloperidol, driving vehicles, servicing machinery and performing other types of work that require increased concentration, as well as drinking alcohol, is prohibited.

Drug interactions

Haloperidol enhances the inhibitory effect of opioid analgesics, hypnotics, tricyclic antidepressants, general anesthesia, and alcohol on the central nervous system.

When used simultaneously with antiparkinsonian drugs (levodopa and others), the therapeutic effect of these drugs may be reduced due to the antagonistic effect on dopaminergic structures.

When used with methyldopa, disorientation, difficulty and slowdown in thinking processes may develop.

Haloperidol can weaken the effect of adrenaline (epinephrine) and other sympathomimetics, causing a “paradoxical” decrease in blood pressure and tachycardia when used together.

Enhances the effect of peripheral M-anticholinergic drugs and most antihypertensive drugs (reduces the effect of guanethidine due to its displacement from alpha-adrenergic neurons and suppression of its uptake by these neurons).

When combined with anticonvulsants (including barbiturates and other inducers of microsomal oxidation), the doses of the latter should be increased, because haloperidol lowers the threshold for seizure activity; in addition, serum concentrations of haloperidol may also decrease. In particular, when simultaneous use tea or coffee, the effect of haloperidol may be weakened.

Haloperidol may reduce the effectiveness of indirect anticoagulants, so if joint reception the dose of the latter should be adjusted.

Haloperidol slows down the metabolism of tricyclic antidepressants and MAO inhibitors, resulting in an increase in their plasma levels and increased toxicity.

When used simultaneously with bupropion, it reduces the epileptic threshold and increases the risk of epileptic seizures.

When haloperidol is taken concomitantly with fluoxetine, the risk of side effects on the central nervous system, especially extrapyramidal reactions, increases.

When administered simultaneously with lithium, especially in high doses, it can cause irreversible neurointoxication and also increase extrapyramidal symptoms.

When taken simultaneously with amphetamines, the antipsychotic effect of haloperidol and the psychostimulating effect of amphetamines are reduced due to the blockade of alpha-adrenergic receptors by haloperidol.

Haloperidol may decrease the effect of bromocriptine.

Anticholinergic, antihistamine (1st generation), antiparkinsonian drugs may increase anticholinergic side effects and reduce the antipsychotic effect of haloperidol.

Thyroxine may increase the toxicity of haloperidol. In case of hyperthyroidism, haloperidol can be prescribed only with simultaneous administration of appropriate thyreostatic therapy.

When used simultaneously with anticholinergic drugs, intraocular pressure may increase.

Analogues of the drug Haloperidol

Structural analogues of the active substance:

Apo Haloperidol;
Galoper;
Haloperidol decanoate;
Haloperidol Acri;
Haloperidol ratiopharm;
Haloperidol Richter;
Haloperidol Ferein;
Senorm.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.

Psychiatry is a special field of medicine that requires certain medications to help a patient with an established diagnosis cope with emerging problems. One of the remedies used in practice is Haloperidol (drops). Instructions for use of this drug, telling why and how it is prescribed, will be discussed in the article.

How is the drug produced?

Haloperidol was developed pharmaceutical company Janssen Pharmaceutica in 1957. Those companies that produce medicines produce the medicine of the same name only in tablets or as long-acting injections. A solution of "Haloperidol" in drops is produced by one company, Ratiopharm GmbH, which was acquired by the transnational corporation Teva Pharmaceutical Industries Ltd in 2010. (Teva). The drops represent clear liquid, packaged in 30 mg bottles. 1 ml drops contain 2 mg active substance haloperidol. As auxiliary components the drops contain:

methyl parahydroxybenzoate, used in food, pharmaceutical and cosmetic industry, as a preservative with some antibacterial properties;
lactic acid, which plays a significant role in metabolic tissue processes, in the functioning of the nervous system and brain,
propyl parahydroxybenzoate is another preservative;
purified water, used in the amount required for a certain concentration of the solution.

Which pharmaceutical group does the medicine belong to?

The drug "Haloperidol" (drops), photos of which can be seen on medical websites, belongs to the antipsychotic (neuroleptic) group of drugs as defined by the State Register of the Ministry of Health of the Russian Federation.

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 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 has an effect on 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.

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.

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;
and exogenous etiology in the chronic stage;
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.

Possible contraindications

Information about contraindications is contained in the instructions for use of Haloperidol (drops). Reviews that have a negative connotation are based precisely on this aspect of the medicine’s functionality. "Haloperidol" should not be prescribed for such conditions and diseases as:

coma of various origins;
diseases of the central nervous system accompanied by motor-muscular symptoms;
intoxication with xenobiotics followed by severe depression of central nervous system function;
individual sensitivity to the components of the drug or butiferon derivatives.

Haloperidol should not be taken by children under 3 years of age. The same restriction applies to pregnant and breastfeeding women, since this substance passes through and into breast milk.

Medicinal drops "Haloperidol" can be prescribed with extreme caution and only for absolute medical reasons in the following cases:

alcohol intoxication;
arrhythmias;
bradycardia;
vegetative-vascular dystonia;
prostatic hyperplasia;
hyperthyroidism;
hypokalemia;
severe arterial hypotension;
depression of endogenous origin;
orthostatic dysregulation;
diseases of the hematopoietic system;
angle-closure glaucoma;
(in history);
changes in the electrocardiogram with prolongation of the QT interval;
clinical cardiac disorders;
tumors dependent on the hormone prolactin (for example, mammary glands);
organic brain lesions;
poisoning with opioid analgesics, sleeping pills and psychotropic substances;
renal and/or liver failure;
thyrotoxicosis;
epilepsy.

If the use of "Haloperidol" is the only possible option treatment of certain conditions, it is prescribed with extreme caution to patients with neurological symptoms of damage to the subcortical structures of the brain and a reduced seizure threshold. In this case, a grand mal seizure (grandmal seizure) may occur. For such patients, the use of this drug is indicated only while continuing to take it. anticonvulsants.

If the patient is diagnosed with depression and requires treatment of the concomitant disease with Haloperidol, then antidepressants are taken in combination.

If the patient has a disease endocrine system and thyroxine therapy is carried out, then the use of Haloperidol is contraindicated. If the use of this drug is necessary, antithyroid therapy should be administered in case the number of unwanted effects increases.

If something went wrong

For many patients, the use of a drug such as Haloperidol drops is indicated. Reviews about it often mention the development of side effects. In this regard, the medicine is often perceived negatively by patients. During studies of the drug, as well as observations of patients taking it, it was noted that a therapeutic dose of 1-2 mg per day does not have long-term, pronounced side effects. Even if they arise, they are of a quickly passing (transient) nature. TO adverse reactions from taking "Haloperidol" include:

From the nervous system: akathisia, anxiety, insomnia, agitation, hallucinations, headache, dizziness, depression, lethargy, psychosis, anxiety, drowsiness, fear, euphoria, epilepsy. With a long course, the appearance of extrapyramidal disorders, tardive dystonia, and neuroleptic malignant syndrome may occur. They are expressed in smacking, puckering of lips, puffing out of cheeks, rapid and worm-like movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the neck, torso, arms and legs, rapid blinking, unusual expression of the face or body, difficulty or rapid breathing, hyperthermia, increased or decreased Blood pressure, increased sweating, urinary incontinence, muscle rigidity, epileptic seizures, loss of consciousness.
On the part of the cardiovascular system, an inadequate response to taking the drug, especially in large dosages, is manifested by arrhythmia, decreased blood pressure, orthostatic hypotension, tachycardia, ECG changes expressed in prolongation of the QT interval, flutter and ventricular fibrillation.
The respiratory system may respond to the drug with pathological changes in breathing rhythm, shortness of breath, inflammatory diseases lungs.
The digestive system may be characterized by hyposalivation (decreased salivation), dry oral mucosa, decreased appetite, nausea, vomiting, diarrhea, constipation, liver dysfunction, and the development of jaundice.
The hematopoietic organs may exhibit a negative reaction in the form of agranulocytosis, monocytosis, transient leukopenia or leukocytosis, erythropenia.
The genitourinary system may respond with pain in the mammary glands, gynecomastia, hyperprolactinemia, urinary retention (especially with prostatic hyperplasia), menstrual irregularities, the appearance of peripheral edema, decreased potency, increased libido, priapism (painful erection without sexual arousal).

As a side effect of the drug, the patient may experience alopecia, cataracts, retinopathy, skin irritation, weight gain, and photosensitivity.

The appearance of any abnormal sensations and health conditions requires either adjustment of the dose of the drug or its discontinuation. Only a doctor can decide whether to change the treatment regimen.

Medication regimen and dosage

For those patients who are prescribed antipsychotics, it is important to know how to take Haloperidol drops. The answer to this question should be given by a doctor when prescribing a drug for medical reasons. The dosage regimen is slightly different for different age groups and takes into account concomitant diseases or the patient's condition. For the drug "Haloperidol" (in drops), the instructions for use remind that 10 drops of the solution contain 1 mg of the active substance. The amount of the substance prescribed by the doctor should be divided into 1, 2 or 3 times. If the dose required for treatment and determined by a specialist is greater than that indicated in the standard instructions, then it can be divided into 4-5 doses. It should be remembered that this antipsychotic is taken with food, measuring required quantity drops using a pipette. The product can be diluted in drinks or added to food. Those patients who do not suffer from diabetes or high blood sugar levels can use lump sugar to take the drug.

For pediatric patients (from 3 to 18 years), the treatment uses a progressive change in the dosage of the drug, taking into account the amount active component per 1 kg of child’s body weight. Start with 0.025 mg. Then the dosage is adjusted, if necessary, to 0.05 mg (per 1 kilogram of the patient’s body weight). In case of acute need, the doctor may increase this dose to 0.2 mg/kg for adequate treatment.

For the treatment of adult patients, progressive dosage changes are also used. Start with a daily amount of medication of 0.5-1.5 mg 2-3 times a day, then the dosage is increased to 2-4 mg for each of 2-3 doses of medication per day. If treatment is carried out in a specialized medical institution under the supervision of specialists and prescribed for relief acute symptoms, then the dose can be increased to 15 mg of the active substance. It should be remembered that the maximum allowable amount of haloperidol that can be taken per day should not exceed 100 mg. Clinicians have found that for therapeutic purposes the medicine is used at a dose of 10-15 mg per day. If the patient suffers from chronic schizophrenia, the dose is increased to 40 mg. With frequently recurring exacerbations, with resistance to traditional treatment the amount of halopperidol is increased to 60 mg per day.

In maintenance therapy during outpatient treatment, it is most often recommended daily dosage at 0.5-5 mg, taking into account the medical history, the patient’s condition, the course of the disease, and concomitant diseases. The doctor monitors the patient's condition systematically.

A single dose of the drug "Haloperidol" (in drops) for elderly people, as well as physically weakened patients should not be higher than 1.5 mg. In this case, the maximum daily amount of the active substance should not be more than 5 mg.

It should be remembered that for the drug "Haloperidol" (drops), the instructions for use in terms of dosage are advisory in nature. The correct and adequate dosage and regimen of medication is prescribed by the doctor treating the patient.

Overdose and drug poisoning

The question of how long you can take Haloperidol drops is also decided by your attending physician. Long-term inadequate use of this drug can cause overdose and poisoning, they manifest themselves as follows:

aspiration
excitation;
hyperthermia;
hypothermia;
glossopharyngeal syndrome;
delirium;
dyskinetic disorders;
dystonic disorders;
urinary retention;
coma;
respiratory failure;
intestinal paresis;
pneumonia;
cardiovascular failure
decrease or increase in blood pressure;
confusion;
drowsiness;
epileptic seizures.

In case of overdose, symptomatic therapy is used, which should take into account the following aspects:

vomiting may be impossible due to the antiemetic effect of this drug;
gastric lavage will help relieve detoxification of the body only in case of early diagnosis of poisoning or overdose due to the fact that the drug has a high degree of absorption;
Dialysis and forced diuresis are ineffective;
during symptomatic treatment of poisoning or overdose with haloperidol, analeptic drugs should not be used, as there is a high risk of epileptic seizures;
to relieve extrapyramidal symptoms, it is necessary to use antiparkinsonian drugs such as biperiden, administered intravenously, such therapy can be carried out for quite a long time;
if the patient is in a coma, then intubation is indicated, which is performed using short-acting muscle relaxants to relieve spasm of the pharyngeal muscles.

Cases of haloperidol overdose or poisoning with this drug should be subject to clinical symptomatic treatment with constant monitoring of blood pressure and cardiac activity. It should be noted that developed respiratory depression may require artificial ventilation.

"Haloperidol" and other drugs, analogues

Just like itself medicine"Haloperidol" (drops), analogues this drug should be prescribed for use taking into account the medications taken by the patient for the treatment of concomitant diseases. These include the following drugs: “Galoper”, “Senorm”. In addition, medicines produced by other manufacturers in the form of tablets and injection solutions are considered analogues: “Haloperidol-Acri”, “Haloperidol-PAR”, “Haloperidol-ratiopharm”, etc.

Antihypertensive drugs, as well as m-anticholinergic drugs, enhance their effect when taken together with Haloperidol. But the effect of anticonvulsants: bromocriptine, dopamine, norepinephrine, phenylephrine, epinephrine, ephedrine, when used together, is, on the contrary, reduced. The antipsychotic becomes more toxic if taken together with tricyclic antidepressants and MAO inhibitors due to decreased metabolism of these drugs.

"Haloperidol" should never be taken together with alcohol-containing substances, including medications, opioid analgesics, barbiturates, tricyclic antidepressants, and other sleeping pills due to a sharp decrease in blood pressure and depression of the central nervous system.

Where and how to buy medicine?

The drug "Haloperidol" (in drops) has mostly positive reviews; they have been left by more than one generation of patients and practicing doctors. It should be remembered that this drug can be used in treatment strictly for medical reasons and according to a doctor’s prescription. In the pharmacy chain it is sold exclusively on a special prescription form; free dispensing of this medicine is prohibited. This feature treatment with the drug "Haloperidol" (drops) is confirmed by the instructions for use. The cost of the medicine is low - about 50 rubles for 1 bottle of 30 ml. After opening the package, the medicine must be used within six months, then it must be disposed of.

Some features

As in the case of other antipsychotics, instructions for use describe the features of treatment with Haloperidol (drops). With increasing dosing of the medicine for pediatric patients or old age, as well as for weakened patients, adjustments to its intake should be carried out no more than once every 3-5 days.

Any self-medication with other drugs during the course of taking this medication is strictly prohibited. Consultation with a doctor regarding all substances taken is essential.

The period of treatment with Haloperidol should be supervised by a doctor; the patient's condition needs to be monitored.

Before stopping taking the drug, it is necessary to gradually reduce the dose of the active substance, both daily and simultaneously. This must be done in order to avoid the so-called “withdrawal syndrome”.

During treatment with this drug, extreme caution must be exercised when driving vehicles and engaging in other activities that require psychomotor speed and increased concentration.

The use of "Haloperidol" in drops is a sought-after therapeutic measure in the treatment of many diseases in psychiatric practice, despite numerous contraindications and a high probability of side effects. The medicine should be prescribed only by the attending physician.