Haloperidol-Richter

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Latin name: Haloperidol-Richter

ATX code: N05AD01

Active ingredient: haloperidol (Haloperidol)

Producer: Gedeon Richter OJSC (Gedeon Richter, Plc.) (Hungary); Gedeon Richter-Rus JSC (Russia)

Description and photo update: 2020-04-07

Haloperidol-Richter is an antipsychotic drug (neuroleptic).

Release form and composition

Dosage forms of Haloperidol-Richter:

solution for intravenous (i / v) and intramuscular (i / m) administration: transparent, colorless or pale yellow, without mechanical impurities (1 ml each in a colorless glass ampoule with a break point; in a contour plastic package 5 ampoules; in a cardboard box 1 package);
tablets: round, flat, almost white or white, beveled, practically odorless; at a dose of 1.5 mg - engraved "|||" on one side (25 pcs. in a blister, 2 blisters in a cardboard box).

Each pack also contains instructions for the use of Haloperidol-Richter.

1 ml of solution contains:

active substance: haloperidol - 5 mg;
additional components: water for injection (d / i), lactic acid.

1 tablet contains:

active substance: haloperidol - 1.5 or 5 mg;
additional components: colloidal silicon dioxide, potato starch, gelatin, corn starch, talc, magnesium stearate, lactose monohydrate.

Pharmacological properties

Pharmacodynamics

Haloperidol is a neuroleptic (antipsychotic) derivative of butyrophenone. It has a pronounced antipsychotic effect, blocks postsynaptic dopamine receptors in the structures of the mesolimbic and mesocortical tracts of the brain. Does not show antihistaminergic or anticholinergic activity. A significant antipsychotic effect is combined with a moderate sedative effect (demonstrates an activating effect in small doses) and a pronounced antiemetic activity.

Due to the direct blockade of central dopamine receptors, Haloperidol-Richter shows high efficiency in the treatment of hallucinations and delusions. Leads to extrapyramidal disorders, does not have an m-anticholinergic effect. The pronounced sedative effect of the drug is observed against the background of psychomotor agitation, it is also used with good results in mania and other agitations.

Sedative activity of the substance is associated with inhibition of α-adrenergic receptors of the reticular formation of the brain stem, and antiemetic activity - with suppression of dopamine D ₂ receptors of the trigger zone, which affects the vomiting center. The hypothermic action and the development of galactorrhea are due to the blockade of dopamine receptors in the hypothalamus by haloperidol.

Prolonged use of Haloperidol-Richter leads to a change in the endocrine status, in the anterior lobe of the pituitary gland, the production of prolactin increases and the synthesis of gonadotropins decreases.

Pharmacokinetics

After oral administration, the drug is absorbed in non-ionized form by passive diffusion, predominantly from the small intestine. The maximum concentrations (C _max) of the active substance in the blood after oral administration are noted after 2-6 hours, the bioavailability is 60-70%. The therapeutic effect is recorded at a plasma level of haloperidol from 4 to 20-25 μg / L. The agent binds to plasma proteins by 92%, in an equilibrium state the volume of distribution is 7.9 ± 2.5 l / kg.

After intramuscular administration, Cmax in the blood is noted after 20 minutes, the connection of haloperidol with plasma proteins is 90%, the rest (10%) is a free fraction. In the tissues, the level of the active substance is higher than in the blood. Haloperidol-Richter is prone to accumulation in tissues, the ratio of its content in erythrocytes to plasma content is 1 ÷ 12.

Metabolic transformation occurs in the liver, the agent has the effect of first passing through the liver. The isoenzymes CYP3A3, CYP3A5, CYP2D6, CYP3A7 are responsible for the course of its metabolism. Haloperidol is a CYP2D6 inhibitor, there are no active metabolites.

The half-life from plasma (T _1/2) with intravenous administration is 14 hours (10–19 hours), with intramuscular administration - 21 hours (17–25 hours), with oral administration - 24 hours (12–37 hours). Haloperidol is excreted in the form of metabolites: 60% - with feces (including 15% - with bile), 40% - with urine (including 1% - unchanged). Passes through the blood-brain barrier and the placenta, is detected in breast milk.

Indications for use

Haloperidol-Richter solution is used in the following cases:

therapy and relief of psychotic disorders of various origins;
premedication before surgery;
long-term and treatment-resistant vomiting, including those caused by anticancer therapy.

Haloperidol-Richter tablets are prescribed for the treatment of such conditions / diseases:

behavioral disorders, personality changes (schizoid, paranoid and others), Gilles de la Tourette's syndrome in children and adults;
psychosomatic disorders, manic states, chronic and acute psychosis, proceeding with agitation, delusional and hallucinatory disorders;
chorea of Huntington, tics;
vomiting that persists for a long time and is resistant to the action of other agents, including those caused by anticancer treatment, as well as hiccups.

Contraindications

Absolute:

severe toxic suppression of the central nervous system (CNS) function (against the background of intoxication with xenobiotics - for tablets) and coma of various origins;
diseases of the central nervous system, accompanied by pyramidal and extrapyramidal disorders (including Parkinson's disease);
psychotic disorders caused by dementia in elderly patients (solution);
glucose-galactose malabsorption, lactose intolerance, lactase deficiency (tablets);
age up to 3 years - for solution, body weight in children up to 60 kg - for tablets;
pregnancy and lactation;
hypersensitivity to any component of the agent and to any derivatives of butyrophenone.

Relative (use both Haloperidol-Richter dosage forms with extreme caution):

decompensated diseases of the cardiovascular system (CVS), including intracardiac conduction disorders, angina pectoris, prolongation of the QT interval on the electrocardiogram (ECG), or the presence of risk factors for these pathologies (for example, hypokalemia);
combined use with other drugs that can lead to a prolongation of the QT interval (especially when using a solution);
pulmonary heart and respiratory failure, including arising against the background of acute infectious lesions and chronic obstructive pulmonary disease (COPD);
hepatic and / or renal failure;
epilepsy;
hyperthyroidism (with symptoms of thyrotoxicosis);
alcoholism;
hyperplasia of the prostate with urinary retention;
angle-closure glaucoma;
children and old age (for solution).

Haloperidol-Richter, instructions for use: method and dosage

Solution for i / v and i / m administration

Haloperidol-Richter solution is intended for parenteral use, it is injected into muscle tissue or into a vein.

Recommended dosage regimen:

psychotic disorders of various origins (for therapy and relief): in the first days of the course 2-3 times / day at a dose of 2-5 mg IM or IV (the contents of the ampoule should be diluted in 10-15 ml of water d / i), the maximum daily dose should not be higher than 60 mg; when fixing a stable sedative effect, the patient is transferred to a tablet form; elderly patients are administered 0.5–1.5 mg (0.1–0.3 ml of solution), the maximum daily dose is 5 mg (1 ml); children over 3 years of age receive the drug at a dose of 0.025–0.05 mg per day, divided into 2 injections, the daily dose should not be higher than 0.15 mg / kg;
acute psychosis (in case of impossibility of ingestion): at a dose of 5-10 mg intravenously or intramuscularly, the dose can be re-administered 1–2 times with an interval of 30–40 minutes until the necessary control of symptoms is achieved; the maximum dose per day is 100 mg;
acute alcoholic psychosis: 5–10 mg IV, if the response to therapy is insufficient, an additional infusion of 10–20 mg is prescribed at an infusion rate of no more than 10 mg / min;
premedication before surgery: intravenously or intramuscularly 30–40 minutes before surgery at a dose of 2–5 mg;
resistant to treatment and long-term vomiting, including those caused by anticancer therapy: with indomitable vomiting 2 times / day, 1.5-2 mg.

Parenteral administration of Haloperidol-Richter should be carried out under close medical supervision, especially in children and the elderly. When fixing the therapeutic effect, you should switch to taking the oral form of the drug.

Pills

Haloperidol-Richter tablets are intended for oral administration. They are taken with or after meals with 240 ml (1 full glass) of water or milk.

The attending physician sets the dosage regimen depending on the clinical response. As a rule, in the acute phase of the disease, the dose is slowly increased, and during maintenance treatment, it is gradually reduced to the lowest effective dose.

For adults, the drug is recommended in an initial daily dose of 1.5–5 mg, divided into 2-3 doses. If the therapeutic effect is insufficient, the dose can be gradually increased by 1.5-3 mg (in some cases up to 5 mg) until the desired effect is achieved (approximately - up to 10-15 mg / day, with chronic schizophrenia - 20-40 mg / day, in resistant cases - up to 50-60 mg / day). The course can vary from 2 to 3 months, the maximum daily dose should not exceed 100 mg / day. The dose should be reduced slowly, without exacerbation, maintenance doses can range from 0.5-0.75 to 5 mg / day.

Recommended doses and frequency of administration of Haloperidol-Richter, depending on the indications:

chronic and acute psychoses: 1.5-5 mg (up to 10 mg) every 4-8 hours; when carrying out maintenance therapy, daily doses can vary from 0.5 to 20 mg; the minimum dose should be used that is able to maintain remission;
Gilles de la Tourette's syndrome, non-psychotic behavioral disorders: the initial daily dose is 0.05 mg / kg, divided into 2-3 doses, then it is gradually increased with an interval of 5-7 days to a total maintenance dose of 0.075 mg / kg / day;
Huntington's chorea, tics: a daily dose of 0.025–0.05 mg / kg, if the desired result cannot be achieved after 30 days of therapy, it is not advisable to continue taking the drug;
treatment-resistant and long-term vomiting: 1.5–2 mg 2 times / day.
In the treatment of childhood autism, 0.025–0.05 mg / kg / day is prescribed. Children with a body weight of 60 kg or more with psychotic disorders use Haloperidol-Richter in 2-3 doses at a daily dose of 0.05 mg / kg. If necessary, given the tolerability of therapy, the dose is gradually increased at intervals of 5-7 days to a total dose of 0.15 mg / kg / day.

Weakened or elderly patients are advised to take ⅓ – ½ of the recommended dose of Haloperidol-Richter for adults, and it is allowed to increase it no more often than every 2-3 days.

Side effects

CNS: dizziness, headache, insomnia / drowsiness (of varying severity), akathisia, anxiety, euphoria / depression, extrapyramidal / convulsive disorders; with long-term therapy - tardive dyskinesia (worm-like and rapid movements of the tongue, puffing out of the cheeks / smacking, puckering of the lips, uncontrolled movements of the arms and legs, uncontrolled chewing movements), tardive dystonia (spasms of the eyelids or rapid blinking, uncontrolled bending movements of the trunk, neck, arms and legs; unusual facial expression or body position), neuroleptic malignant syndrome (NMS) [muscle stiffness, hyperthermia, increased sweating, tachycardia, shortness of breath / rapid breathing, arrhythmia, increased / decreased blood pressure (BP), seizures, urinary incontinence, depression consciousness]; change in mental state (for solution),accompanied by increased activity of creatine phosphokinase, catatonic manifestations, acute renal failure, myoglobinuria (rhabdomyolysis);
hematopoietic organs: agranulocytosis, leukocytosis or temporary leukopenia, erythropenia and a predisposition to monocytosis;
heart and blood vessels: with the introduction of high doses - lowering blood pressure, orthostatic hypotension, tachycardia, arrhythmias (including ventricular arrhythmias, such as "pirouette"), ECG changes (signs of flutter and fibrillation of the ventricles, lengthening of the QT interval); for solution - cases of sudden death;
digestive system: when used in large doses - loss of appetite, hyposalivation, dry mouth, diarrhea / constipation, nausea, vomiting, impaired liver function, up to the appearance of jaundice;
genitourinary system: peripheral edema, urinary retention (in the presence of prostatic hyperplasia), gynecomastia, pain in the mammary glands, decreased potency, menstrual irregularities, hyperprolactinemia, priapism, increased libido;
allergic reactions: photosensitivity, acne-like and maculopapular skin rashes, laryngospasm, bronchospasm;
organ of vision: blurred vision, retinopathy, cataract;
others: weight gain, alopecia; for mortar - heat stroke;
laboratory parameters: hyper- or hypoglycemia, hyponatremia.

Overdose

In case of an overdose of haloperidol, it is possible to develop acute neuroleptic reactions, such as drowsiness, tremors, muscle rigidity, a decrease or sometimes an increase in blood pressure, convulsive disorders; in serious cases - arrhythmia, prolongation of the QT interval on the ECG, shock, respiratory depression, coma. With severe intoxication, convulsive seizures, various forms of impairment of consciousness, up to coma, are possible. Particular attention should be paid to a possible increase in body temperature, since this may be one of the signs of NNS.

If an overdose occurs after oral administration of Haloperidol-Richter, gastric lavage is performed, and activated charcoal is prescribed. With a significant decrease in blood pressure and collapse, in order to maintain blood circulation, concentrated albumin or plasma, dopamine or norepinephrine are administered intravenously. In such cases, the use of epinephrine is prohibited, since its administration can lead to severe hypotension. With respiratory depression, artificial ventilation is prescribed, for the removal of extrapyramidal symptoms - antiparkinsonian drugs and central m-anticholinergics. They also introduce intravenous dextrose solution, diazepam, nootropics, vitamins C and group B.

The specific antidote is unknown, dialysis is ineffective.

special instructions

In the course of therapy with Haloperidol-Richter, patients need to carry out regular monitoring of liver function tests, blood counts, and ECG.

Cases of seizures associated with haloperidol have been reported, therefore, in the presence of epilepsy and conditions predisposing to the onset of convulsive syndrome (including a history of brain injury, alcoholism), the drug should be used with extreme caution.

In order to relieve extrapyramidal disorders, nootropics, antiparkinsonian drugs (cyclodol), vitamins are used. Treatment with these agents, provided that they are eliminated from the body faster than haloperidol, should be continued after the latter is discontinued to prevent an increase in the severity of extrapyramidal symptoms.

Against the background of the development of tardive dyskinesia, a gradual decrease in the dose of Haloperidol-Richter is recommended, up to its complete cancellation.

In view of the aggravation of the risk of heatstroke and the possible potentiation of m-anticholinergic effects, anti-cold OTC drugs should be avoided during the treatment period.

In the case of performing intense physical work or while taking a hot bath during therapy, care must be taken, since as a result of oppression in the hypothalamus of peripheral and central thermoregulation, the likelihood of heat stroke increases.

To prevent the development of withdrawal syndrome, the course use of Haloperidol-Richter must be completed gradually.

Due to the increased risk of photosensitization, exposed skin areas must be protected from excessive sun exposure during treatment.

The antiemetic effect demonstrated by the drug can mask the signs of drug toxicity and can interfere with the diagnosis of conditions, the first symptoms of which include nausea.

During therapy, the use of ethanol-containing drinks and drugs is not recommended.

Influence on the ability to drive vehicles and complex mechanisms

During the period of using Haloperidol-Richter, it is prohibited to drive vehicles or work with other complex and potentially dangerous machinery.

Application during pregnancy and lactation

Haloperidol-Richter therapy is contraindicated for pregnant and lactating women.

Pediatric use

The use of the solution in children under 3 years of age and tablets in children with a body weight of less than 60 kg is contraindicated. The solution should be used with caution in children over 3 years of age.

With impaired renal function

Patients with renal insufficiency should use Haloperidol-Richter with caution.

For violations of liver function

Caution is required during treatment in the presence of impaired hepatic function, since the metabolism of haloperidol occurs in the liver.

Use in the elderly

Haloperidol-Richter in the form of a solution for intravenous and intramuscular administration is not intended for the treatment of elderly patients with psychosis due to dementia. The use of antipsychotics (including haloperidol) for the treatment of psychotic disorders caused by dementia in elderly patients increases the risk of death. Over a 10-week placebo-controlled clinical trial in the antipsychotic group, the death rate was approximately 4.5%, compared with an average of 2.6% in the placebo group. Most deaths were caused by cardiovascular (heart failure) or infectious (pneumonia) lesions. Observational studies have shown that, as with atypical antipsychotics,treatment with traditional antipsychotics is associated with increased mortality in elderly patients.

Drug interactions

most antihypertensive drugs, peripheral m-anticholinergics: the effect of these drugs is potentiated;
guanethidine: the effect of this substance is weakened as a result of its displacement from α-adrenergic neurons and blocking the capture by these neurons;
narcotic analgesics, tricyclic antidepressants, hypnotics, barbiturates, ethanol, general anesthetics: the severity of the inhibitory effect of these drugs on the central nervous system is aggravated;
bupropion: the threshold of convulsive readiness decreases and the threat of large epileptic seizures increases;
lithium preparations (especially in large doses): the risk of increased extrapyramidal symptoms and the appearance of encephalopathy increases (irreversible neurointoxication may occur);
phenylephrine, norepinephrine, ephedrine, dopamine, epinephrine: the vasoconstrictor activity of these substances decreases as a result of the blockade of α-adrenergic receptors with haloperidol; this combination can provoke a perversion of the action of epinephrine and lead to a paradoxical decrease in blood pressure;
monoamine oxidase (MAO) inhibitors, tricyclic antidepressants: their metabolism slows down, and sedation and toxicity mutually increase;
anticonvulsants: their effect is weakened, since the convulsive threshold is reduced;
anticoagulants: there may be an increase / decrease in their action;
antiparkinsonian drugs: the effectiveness of these drugs decreases, which is caused by blockade of dopamine receptors in the central nervous system;
bromocriptine: its effect is weakened, because of which a dose change may be necessary;
drugs leading to the appearance of extrapyramidal reactions: the frequency and severity of extrapyramidal disorders increases;
amphetamines: the antipsychotic effect of Haloperidol-Richter decreases, at the same time it leads to a weakening of the psychostimulating effect of these drugs, which is due to the blockade of α-adrenergic receptors;
inducers of microsomal liver enzymes, including barbiturates and carbamazepine (with a long course): the plasma content of haloperidol decreases;
methyldopa: the risk of mental disorders, such as inhibition and difficulty in thinking processes, disorientation in space, is aggravated;
blockers of H ₁ -histamine receptors of the 1st generation, antiparkinsonian drugs, m-anticholinergics: it is possible to increase the m-anticholinergic effect of Haloperidol-Richter and weaken its antipsychotic effect (a dose change may be required);
fluoxetine: the threat of the appearance of undesirable phenomena from the central nervous system, mainly extrapyramidal reactions, increases;
caffeine (in high doses): decreases the effectiveness of Haloperidol-Richter.

Analogs

Haloperidol-Richter analogs are Haloperidol, Haloperidol Velpharm, Haloperidol-ALSI, Haloperidol-Acri, Haloperidol-ratiopharm, Haloperidol-Ferein, Senorm, etc.

Terms and conditions of storage

Store at a temperature of 15-30 ° C, in a place protected from light and out of reach of children.

The shelf life is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Haloperidol-Richter

Patients leave mixed reviews about Haloperidol-Richter. Many people note that the drug, having a pronounced antipsychotic effect, gives a tangible and rapid effect in the treatment and relief of psychotic disorders of various origins, reduces mental agitation and lowers psychomotor activity. But it is recommended to use this tool only for the intended purpose and under the supervision of a doctor.

However, other patients complain of the development of very severe adverse events during therapy, due to which they had to stop using the drug, despite its high effectiveness. Some believe that, in general, this antipsychotic is outdated and it is better to use more expensive modern drugs with fewer side effects.

Price for Haloperidol-Richter in pharmacies

The price of Haloperidol-Richter, in the form of a solution for intravenous and intramuscular administration (5 mg / ml), can be 90–110 rubles. per package containing 5 ampoules of 1 ml.

The price of the tablets is unknown, since the drug in this dosage form is currently not available in pharmacies.

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!