Haloperidol side effects after taking. Haloperidol. Scary story with a happy ending

Haloperidol is an antipsychotic drug that works by changing the activity of chemicals in the brain. It is used to treat schizophrenia and motor and speech tics in people with Tourette's syndrome. Haloperidol may also be used for other purposes.

Before taking the drug

This medicine should not be used in Parkinson's disease or certain conditions that affect the central nervous system. In addition, it is contraindicated in case of allergies or in the following cases:

• Parkinson's disease;
• certain conditions that affect the central nervous system (for example, severe drowsiness or slow thinking caused by other drugs or alcohol).

Haloperidol is not approved for use in psychotic conditions associated with dementia. It may increase the risk of death in older people with conditions associated with dementia.

To make sure haloperidol is safe, tell your doctor about your:

• thyroid disease;
• liver diseases;
• kidney disease;
• heart disease, angina pectoris (chest pain);
• epilepsy or other convulsive disorders;
• you or a family member has a history of long QT interval syndrome;
• electrolyte imbalance (for example, low levels of potassium and magnesium in the blood);
• if you are taking blood-thinning drugs (warfarin, coumadin).

The FDA (U.S. Food and Drug Administration) has assigned the drug Category C for pregnancy. It is not known whether haloperidol will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medicine.

Taking antipsychotic medications in the last 3 months of pregnancy can cause problems in the newborn, such as withdrawal symptoms, breathing problems, feeding problems, restlessness, tremors, and lethargy or muscle stiffness. However, if you stop taking medication during pregnancy, you may experience withdrawal symptoms or other problems. If you become pregnant while taking haloperidol, do not stop taking it without talking to your doctor.

Haloperidol can pass into breast milk and may harm a nursing baby. You should not breast-feed while using this medicine.

Follow all directions in the instructions. Your doctor may occasionally change your dose to make sure you get the best results. Do not take this medicine in larger or smaller amounts, or for longer than recommended.

Haloperidol can be taken with or without food.

Measure liquid medication with a dosing syringe, measuring spoon, or cup.

Taking large amounts of haloperidol can lead to serious heart rhythm disturbances or sudden death. Do not take more than the dose prescribed by your doctor.

It may take several weeks for symptoms to improve. Take the drug as directed and tell your doctor if symptoms do not improve.

Do not suddenly stop taking haloperidol or you may experience unpleasant withdrawal symptoms. Ask your doctor how to safely stop using haloperidol.

Store at room temperature away from moisture, heat and light. Do not allow liquid medicine to freeze.

If you miss a dose, take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take additional medicines to make up for a missed dose.

In case of overdose, seek emergency medical attention. An overdose of haloperidol can be fatal.

Haloperidol may impair thinking or reactions. Be careful if you drive a car or do anything that requires attention.

Do not get up too quickly from a sitting or lying position, or you may feel dizzy. Get up slowly and keep your balance so as not to fall.

Drinking alcohol may increase some of the side effects of haloperidol.

Avoid overheating or dehydration during physical activity and in hot weather. While taking haloperidol, the likelihood of heat stroke may increase.

Video about haloperidol

Dosage

Usual Adult Dose for Initiation of Intensive Care and Resuscitation:

Haloperidol lactate:

Intermittent intravenous administration: 0.03-0.15 mg/kg IV (2-10 mg) every 30 minutes to 6 hours.

Intravenous infusion: A dosage of 3-25 mg/hour by continuous intravenous infusion has been used in mechanically ventilated patients with agitation and delirium.

Usual Adult Dose for Dementia:

For non-psychotic behavioral problems associated with dementia:

Initial dose: 0.5 mg orally 2-3 times a day.

Maintenance dose: 0.5-2 mg orally 3 times a day.

Usual Adult Dose for Mania:

Orally:

Initial dose: 0.5-5 mg orally 2-3 times a day

Maintenance dose: 1-30 mg/day in 2-3 divided doses. Infrequently, haloperidol has been used at doses above 100 mg in unresponsive patients. However, limited clinical use has not demonstrated the safety of long-term use of such doses.

Parenterally:

Haloperidol lactate:

Usual Adult Dose for Nausea/Vomiting:

Orally:

1-5 mg orally every 4-6 hours as needed.

Parenterally:

Haloperidol lactate:

5 mg intramuscularly or intravenously every 4 to 6 hours as needed.

Usual Adult Dose for Psychosis:

Orally:

Initial dose: 0.5-5 mg orally 2-3 times a day.

Maintenance dose: 1-30 mg/day in 2-3 divided doses. Daily doses up to 100 mg have been used. Infrequently, haloperidol has been used at doses above 100 mg in unresponsive patients. However, limited clinical use has not demonstrated the safety of long-term use of such doses.

Parenterally:

Haloperidol lactate:

2-5 mg intramuscularly or intravenously for operational control. May be repeated every 4-8 hours. Doses of 8-10 mg can be administered intramuscularly. Highly agitated patients may require hourly injections.

Haloperidol Decanoate:

Initial dose: 10-15 times the previous oral daily dose intramuscularly every 3-4 weeks. The initial dose should not exceed 100 mg, and the remainder should be administered within 3-7 days. There is limited experience with doses greater than 450 mg/month. Do not administer intravenously.

Usual Adult Dose for Tourette's Syndrome:

Initial dose: 0.5-2 mg orally 2-3 times a day.

Maintenance dose: may be increased every 5-7 days to 3-5 mg 2-3 times daily in more severe or resistant cases.

Usual Geriatric Dose for Psychosis:

Orally:

Initial dose: 0.5-2 mg orally 2-3 times a day.

Maintenance dose: 1-30 mg/day in 2-3 divided doses. Daily doses up to 100 mg have been used. Infrequently, haloperidol has been used at doses above 100 mg in unresponsive patients. However, limited clinical use has not demonstrated the safety of long-term use of such doses. The lowest possible effective dose should be used, as elderly patients are more susceptible to the adverse effects of haloperidol (eg, tardive dyskinesia).

Parenterally:

Haloperidol lactate:

2-5 mg intramuscularly or intravenously for operational control. May be repeated every 4-8 hours. Doses of 8-10 mg can be administered intramuscularly. Highly agitated patients may require hourly injections.

Usual Dose for Psychosis in Children:

Orally:

2 years and younger or weight less than 15 kg: Not recommended.

3-12 years old and weighing 15-40 kg:

Maintenance dose: the daily dose can be increased every 5-7 days by 0.25-0.5 mg. The usual range is 0.05-0.15 mg/kg/day in 2-3 divided doses. There is little evidence that behavioral improvement is further enhanced at doses greater than 6 mg/day.

13-18 years old and weight over 40 kg:

Initial dose: 0.5-5 mg orally 2-3 times a day.

Maintenance dose: 1 to 30 mg/day in 2 to 3 divided doses. Daily doses up to 100 mg have been used. Infrequently, haloperidol has been used at doses above 100 mg in unresponsive patients. However, limited clinical use has not demonstrated the safety of long-term use of such doses.

Parenterally:

Haloperidol lactate:

6–12 years: 1–3 mg IM every 4–8 hours as needed (max. 0.15 mg/kg/day). Patients should be switched to oral therapy as soon as possible.

Haloperidol Decanoate:

17 years or younger: Safety and efficacy not established.

Usual Dose for Tourette Syndrome in Children:

2 years and under or weighing less than 15 kg: Not recommended for use.

3-12 years old and weighing 15-40 kg:

Initial dose: 0.5 mg/day orally in 2-3 divided doses.

Maintenance dose: the daily dose can be increased every 5-7 days in increments of 0.25-0.5 mg. The usual range is 0.05-0.15 mg/kg/day in 2-3 divided doses. There is little evidence that behavioral improvement is further enhanced at doses greater than 6 mg/day.

13-18 years: 2-5 mg intramuscularly every 4-8 hours as needed.

Side effects of haloperidol

Get emergency medical help if you have any of these signs of an allergic reaction: hives, trouble breathing, swelling of your face, lips, tongue, or throat.

High doses or long-term use of this medication may cause serious movement disorders that may be irreversible. Symptoms include uncontrolled muscle movements of the lips, tongue, eyes, face, arms, or legs. The longer you take haloperidol, the more likely you are to develop a serious movement disorder. The risk of this side effect is higher in women and the elderly.

Call your doctor right away if you have:

• sudden mood changes, agitation, hallucinations, unusual thoughts or behavior;
• twitching or uncontrolled movements of the eyes, lips, tongue, face, arms, or legs;
• hardening of the muscles in the neck, tightness in the throat, difficulty breathing or swallowing;
• sudden weakness or soreness, fever, chills, swollen gums, sore throat, painful mouth sores, skin sores, cold or flu symptoms, pain when swallowing, cough, easy bruising or bleeding;
• stitching pain in the chest, cough with yellow or green mucus, shortness of breath;
• headache with chest pain and severe dizziness, fainting, fast or pounding heartbeat;
• severe reaction of the nervous system - very stiff muscles, high fever, sweating, confusion, fast or uneven pulse, tremor, pre-syncope.

Possible common side effects:

• headache, dizziness, feeling dizzy, drowsiness;
• tremor, restlessness, uncontrolled muscle movements;
• stiffness in the muscles of the neck or back, problems with speech;
• feelings of restlessness or anxiety;
• sleep problems (insomnia);
• breast enlargement, irregular menstrual periods, loss of interest in sex;
• overactive reflexes.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about unwanted effects.

Information for the consumer

Refers to haloperidol in the form of oral solution, oral tablets

Other dosage forms: intramuscular oil, intramuscular solution, intramuscular suspension.

In addition to the desired effects of haloperidol, adverse events that require medical attention are possible.

If you experience any of the following side effects while taking haloperidol, talk to your doctor right away:

More common

• difficulty speaking or swallowing
• inability to move eyes
• loss of balance control
• mask-like face
• restlessness or need to keep moving (severe)
• muscle spasms, especially in the neck and back
• shuffling gait
• stiffness of the arms and legs
• trembling of fingers and hands
• twisting body movements
• weakness of the arms and legs.

Less common

• reduced thirst
• difficulty urinating
• dizziness, lightheadedness, or fainting
• hallucinations (being able to see or hear things that are not there)
• smacking or pursing of the lips
• cheek puffing
• uncontrolled movements of the arms and legs
• fast or wormlike tongue movements
• skin rash
• uncontrolled chewing movements.

Rare

• confusion
• convulsions
• difficult or rapid breathing
• fast heartbeat or irregular pulse
• heat
• high or low blood pressure
• hot, dry skin or lack of sweating
• increased blinking or spasms of the eyelids
• excessive sweating
• loss of bladder control
• muscle stiffness (severe)
• muscle weakness
• sore throat and fever
• uncontrolled twisting movements of the neck, torso, arms, or legs
• unusual bleeding or bruising
• unusual tiredness or weakness
• unusual facial expressions or body positions
• unusually pale skin
• yellow eyes or skin.

Frequency not known

• ongoing nausea or vomiting
• increased frequency of seizures
• loss of appetite
• swelling of the face
• fatigue and weakness.

If you experience any of the following overdose symptoms while taking haloperidol, seek emergency care right away:

• overdose symptoms
• difficulty breathing (heavy)
• dizziness (severe)
• drowsiness (severe)
• muscle tremors, twitching, stiffness, or uncontrollable movements (severe)
• unusual tiredness or weakness (severe).

Some of the side effects that can occur while taking haloperidol may not require medical attention. As the body gets used to the drug during treatment, these side effects may go away. The specialist will explain to you how to reduce or prevent some of the negative effects. If any of the following side effects persist, are bothersome, or if you have questions about them, talk to your healthcare professional:

More common

• blurred vision
• changes in menstruation
• constipation
• dry mouth
• breast swelling or pain (in women)
• unusual secretion of milk
• weight gain.

Less common

• decreased sexual ability
• drowsiness
• increased skin sensitivity to the sun (skin rash, itching, redness or other changes in skin color or severe sunburn)
• nausea or vomiting.

Information for healthcare professionals

Refers to haloperidol: powder for mixing, solution for injection, intramuscular solution, oral concentrate, oral tablets.

Local

Local side effects have included the formation of non-infectious, edematous, itchy, painful masses following intramuscular injection of haloperidol decanoate. They slowly pass over several months.

Drowsiness associated with haloperidol therapy may resolve after a few doses.

Tardive dyskinesia includes involuntary, dyskinetic, repetitive movements and may be more common in older women receiving haloperidol. Tardive dyskinesia may be irreversible and is related to the duration of therapy and the total amount of drug consumed. Frequent discontinuation and resumption of therapy may predispose patients to the development of tardive dyskinesia.

Dystonia often includes tongue protrusion, muscle stiffness, torticollis, and opisthotonos. This condition usually resolves upon discontinuation of antipsychotics, but may require antihistamine and antiparkinsonian therapy if symptoms are severe or if breathing is disturbed. Treatment of dystonic reactions and extrapyramidal effects, in addition to general supportive measures, may include the judicious use of one or more drugs such as benztropine, trihexyphenidyl, biperiden, or diphenhydramine.

Signs of pseudo-Parkinsonism: flat face, pill-rolling tremor, shuffling gait, and cogwheel-like rigidity. Symptoms of pseudo-parkinsonism may respond to the judicious use of one or more drugs such as benztropine, trihexyphenidyl, biperiden, or diphenhydramine.

Seizures associated with haloperidol have been reported, but many reports include patients with a history of seizures or underlying organic brain disease.

Low (poor) baseline scores predicted greater cognitive improvement. Changes in cognitive performance were weakly associated with changes in symptom severity.

Nervous side effects are common and include sedation, drowsiness, and rarely seizures. There have also been reports of events such as tardive dyskinesia, dystonia, pseudo-parkinsonism, neuromuscular hyperexcitability, and neuroleptic malignant syndrome (NMS). Low doses of haloperidol have been associated with improved cognition on a test in patients in the early stages of schizophrenia.

Other

There have been reports of other side effects including dry mouth, anticholinergic effects, constipation, urinary retention, and blurred vision.

There have been reports of hepatic side effects, including transient increases in liver function tests.

The cardiovascular system

Rarely, cardiovascular side effects have been reported, including hypotension, hypertension, tachycardia, and cardiac arrest associated with haloperidol therapy (although many of these patients had serious underlying conditions). A number of cases of prolongation of the QT interval and ventricular flutter-fibrillation have been noted in patients receiving parenteral haloperidol. Sudden death and unexpected death have also been associated with haloperidol administration.

Most cases of QT interval prolongation and bidirectional tachycardia included patients treated for critical care delusions. Cardiac monitoring is recommended for ICU patients who must receive haloperidol due to delirium.

There are reports of endocrine side effects including hyperprolactinemia and galactorrhea. In some male patients, haloperidol-induced hyperprolactinemia has been associated with sexual dysfunction.

One test-tube study suggested that haloperidol may increase sperm motility.

In one report of patients on long-term haloperidol use (mean dose 15.7 mg/day; mean duration of illness 15.5 years), mean prolactin levels and the prevalence of chronic hyperprolactinemia were significantly higher in women than in men (74 ng /ml vs. 24 ng/ml and 93% vs. 47%, respectively).

Respiratory system

There have been rare reports of respiratory side effects, including bronchospasm and pneumonitis.

Hematological

There are reports of hematological side effects, including reversible leukopenia and leukocytosis.

Musculoskeletal system

Musculoskeletal side effects have been reported, including two cases of rhabdomyolysis (no evidence of overt NMS). There was also a case of laryngeal dystonia due to haloperidol.

genitourinary system

There are reports of urogenital side effects, including priapism.

Renal dose adjustment

Hepatic dose adjustment

Dose adjustment

Haloperidol has been associated with dose-dependent prolongation of the QT interval.

Precautionary measures

Haloperidol is contraindicated in severe toxic central nervous system depression or coma from any cause and in people with Parkinson's disease.

There have been reports of sudden death in psychiatric patients treated with haloperidol. In addition, QT interval prolongation and bidirectional tachycardia have been observed in patients treated with haloperidol. The risk of QT interval prolongation and bidirectional tachycardia appears to increase with higher than recommended doses and intravenous administration. Patients with conditions that prolong the QT interval (eg, cardiac abnormalities, hypothyroidism, long QT syndromes, hypokalemia, hypomagnesemia, electrolyte imbalances, drugs that prolong the QT interval, etc.) should be treated cautiously. Haloperidol decanoate should never be administered intravenously. Haloperidol lactate is not approved for intravenous administration. However, when administered intravenously, the QT interval and arrhythmias should be monitored by ECG.

Dialysis

An additional dose for dialysis is not required.

Other comments

When a satisfactory therapeutic response is achieved, the dosage should be gradually reduced to a low maintenance level.

Interaction

A total of 1045 (5900 brand and generic) drugs interact with haloperidol:

• 177 drugs - strong interaction
• 833 drugs - moderate interaction
• 34 drugs - easy interaction.

• abilify (aripiprazole)
• Aricept (donepezil)
• ativan (lorazepam)
• cogentin (benztropine)
• depakote (divalproex sodium)
• fish oil (omega-3 polyunsaturated fatty acids)
• lasix (furosemide)
• lexapro (escitalopram)
• milk of magnesia (magnesium hydroxide)
• miralax (polyethylene glycol 3350)
• namenda (memantine)
• paracetamol (acetaminophen)
• Plavix (clopidogrel)
• prilosec (omeprazole)
• seroquel (quetiapine)
• synthroid (levothyroxine)
• Tylenol (paracetamol)
• vitamin D3 (cholecalciferol)
• zoloft (sertraline)
• zyprexa (olanzapine).

Before using haloperidol, tell your doctor if you regularly take other medicines that cause drowsiness (cold or allergy medicines, narcotic pain relievers, sleeping pills, muscle relaxants, and medicines for depression or anxiety). They may increase the drowsiness caused by haloperidol.

Tell your doctor about all the medicines you are taking and those you plan to start using during your treatment with haloperidol, especially the following:

• cancer drugs – arsenic trioxide, nilotinib, toremifene, vandetanib, vemurafenib;
• antidepressant - citalopram;
• antimalarial drugs - lumefantrine;
• drugs to normalize the heart rhythm - amiodarone, disopyramide, dofetilide, procainamide, quinidine, sotalol;
• medicines for the treatment of mental disorders - iloperidone, pimozide, thioridazine, ziprasidone, others.

This list is not complete. Other drugs may interact with haloperidol, including over-the-counter and prescription medicines, vitamins, and herbal products. Not all possible interactions are listed here.

There is one interaction of haloperidol with food/alcohol.

The use of haloperidol along with ethanol may increase nervous system side effects such as dizziness, drowsiness, and difficulty concentrating. Some people may also experience deterioration in thinking and judgment. Alcohol consumption should be avoided or limited during treatment with haloperidol. Do not use more than the recommended dose of haloperidol, and avoid activities that require mental alertness, such as driving or operating dangerous machines, until you know how the medicine affects you. It is important to tell your doctor about all other medications you are taking, including vitamin and herbal remedies. Do not stop using any medication without consulting your doctor.

11 diseases interact with haloperidol:

• hyperthyroidism
• parkinsonism
• acute alcohol intoxication
• cardiovascular disease
• CNS depression
• tardive dyskinesia
• kidney/liver disease
• mammary cancer
• convulsive disorders.

Description of haloperidol

Haloperidol is the first drug in the butyrophenone family of essential antipsychotic drugs. The chemical formula is 4-(p-chlorophenyl)-4-hydroxypiperidine] 4"-fluorobutyrophenone.

Haloperidol is available in sterile parenteral forms for intramuscular administration. The injection provides 5 mg of haloperidol (as lactate) and lactic acid to adjust the pH between 3.0 and 3.6.

Action

The exact mechanism of action has not been clearly established.

Indications

Haloperidol is indicated for use in the treatment of schizophrenia.

Haloperidol is indicated for the control of tics and vocal utterances in Tourette's disorder.

Contraindications

Haloperidol is contraindicated in severe CNS toxic depression or comatose states of any cause and in people with hypersensitivity to this drug or Parkinson's disease.

Warnings

Increased mortality in elderly patients with dementia-related psychosis.

Elderly patients with dementia-related psychosis treated with antipsychotics are at increased risk of death. Haloperidol injection is not approved for the treatment of patients with dementia-related psychosis.

Tardive dyskinesia

A syndrome consisting of potentially irreversible, involuntary dyskinetic movements may develop in patients taking antipsychotic medications. Although the prevalence of the syndrome appears to be highest among the elderly, especially older women, prevalence estimates cannot be relied upon to predict at the start of antipsychotic therapy which patients are likely to develop the syndrome. Whether antipsychotic drugs differ in their ability to cause tardive dyskinesia is unknown.

Both the risk of developing tardive dyskinesia and the likelihood that it will become irreversible increases with the duration of treatment and the increase in the patient's total cumulative dose of antipsychotics. However, the syndrome may develop, although much less frequently, after relatively short periods at low doses.

There is no known cure for established cases of tardive dyskinesia, although the syndrome may improve, partially or completely, if antipsychotic treatment is withdrawn. However, the antipsychotic treatment itself may suppress (or partially suppress) the symptoms and signs of the syndrome, and thus may possibly obscure the underlying process. The effect that symptomatic suppression has on the long-term course of the syndrome is unknown.

With these considerations in mind, antipsychotics should be administered in a way that is more likely to minimize the occurrence of tardive dyskinesia. Chronic antipsychotic treatment should generally be reserved for patients who suffer from chronic conditions known to respond to antipsychotics and for whom alternative, equally effective but potentially less harmful therapies are not available or appropriate. In patients who require chronic treatment, the minimum dose and the shortest duration of treatment, a satisfactory clinical response should be expected. The need for continued therapy should be reassessed periodically.

If a patient on antipsychotics develops symptoms and signs of tardive dyskinesia, drug discontinuation should be considered. However, some patients may require treatment despite the presence of the syndrome.

Malignant neuroleptic syndrome (NMS)

A potentially fatal complex symptom, sometimes referred to as neuroleptic malignant syndrome (NMS), has already been reported in association with antipsychotics. Clinical manifestations of NMS are hyperpyrexia, muscle rigidity, mental status changes (including catatonic signs), and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, sweating, and cardiac arrhythmia). Additional signs may include an increase in creatine phosphokinase, myoglobinuria (rhabdomyolysis) and acute renal failure.

Diagnostic evaluation of patients with this syndrome is difficult. When making a diagnosis, it is important to identify cases where clinical manifestations include serious illness (eg, pneumonia, systemic infection, etc.) and untreated or inadequately treated extrapyramidal symptoms and signs (EPS). Other important considerations in the differential diagnosis include central anticholinergic toxicity, heat stroke, drug-induced fever, and primary central nervous system (CNS) pathology.

Treatment of NMS should include immediate discontinuation of antipsychotics and other medications not needed for concomitant therapy; intensive symptomatic treatment and medical supervision; treatment of any associated serious health problems for which specific treatments have been developed. There is no general agreement on specific pharmacological treatment regimens for uncomplicated cases of NMS.

If a patient requires antipsychotic treatment after recovery from NMS, potential reintroduction of drug therapy should be carefully considered. The patient should be closely monitored as recurrent cases of NMS have been reported.

When taking haloperidol, hyperpyrexia and heat stroke, not associated with the complex of symptoms described above, have also been reported.

Combined use of haloperidol and lithium

Encephalopathic syndrome (with characteristic weakness, lethargy, fever, trembling and confusion, extrapyramidal symptoms, leukocytosis, elevated serum enzymes, BUN, and fasting blood sugar) and then irreversible brain damage occurred in several patients on lithium and haloperidol therapy. A causal relationship between these events and concomitant administration of lithium and haloperidol has not been established. However, in patients receiving such combination therapy, the first signs of neurological toxicity should be closely monitored and treatment should be stopped as soon as such signs appear.

General

A number of cases of bronchopneumonia, some fatal, have been followed by the use of antipsychotic drugs, including haloperidol. It has been suggested that lethargy and decreased sensation of thirst due to central inhibition may lead to dehydration, blood clots, and reduced pulmonary ventilation. Therefore, if the signs and symptoms described above appear, especially in the elderly, the physician should promptly initiate corrective therapy.

Although there are no reports for haloperidol, reduced serum cholesterol and/or skin and ocular changes have been reported in patients receiving chemically related drugs.

Precautionary measures

Leukopenia, neutropenia, agranulocytosis

Leukopenia/neutropenia temporally associated with antipsychotics, including haloperidol, have been reported in a clinical study and/or post-marketing experience. Agranulocytosis has also been mentioned.

Possible risk factors for leukopenia/neutropenia include pre-existing low white blood cell levels and a history of drug-induced leukopenia/neutropenia. Patients with a history of clinically significant low white blood cell count or drug-induced leukopenia/neutropenia should have frequent complete blood counts during the first few months of therapy, and discontinuation of haloperidol should be considered at the first sign of a clinically significant decrease in white blood cell count in the absence of other causative factors.

Patients with clinically significant neutropenia should be closely monitored for fever or symptoms and signs of infection and promptly treated. In patients with severe neutropenia (absolute neutrophil count<1000/мм3) следует прекратить введение галоперидола и следить за уровнем белых кровяных телец до восстановления.

Other

Haloperidol should be administered cautiously to patients:

• with severe cardiovascular disorders, due to the possibility of transient hypotension and / or precipitation of angina pectoris. occurs If hypotension occurs and a vasopressor is required, epinephrine should not be used, as haloperidol may block its vasopressor activity and a paradoxical further decrease in blood pressure may occur. Instead, metaraminol, phenylephrine, or norepinephrine should be used.
• taking anticonvulsants, with a history of seizures, or with EEG abnormalities because haloperidol may lower the seizure threshold. If indicated, adequate anticonvulsant therapy should be concomitantly maintained.
• with a known allergy or a history of allergic reactions to medications.
• receiving anticoagulants, as there was a single case of intervention with the consequences of one anticoagulant (phenindione).

When haloperidol is used to manage mania in cyclic disorders, there may be a rapid mood swing to depression.

Severe neurotoxicity (rigidity, inability to walk or talk) may occur in patients with thyrotoxicosis who are also receiving antipsychotic medications, including haloperidol.

drug interaction

Drug interactions can be pharmacodynamic (combined pharmacological effects) or pharmacokinetic (changes in plasma concentration). The risks of using haloperidol in combination with other drugs have been assessed as described below.

Pharmacodynamic interaction

Since prolongation of the QT interval is observed during treatment with haloperidol, caution should be exercised when prescribing it to a patient with conditions of prolongation of the QT interval (long QT interval syndrome, hypokalemia, electrolyte imbalance) or to patients receiving drugs that prolong the QT interval or cause electrolyte imbalance.

If concurrent antiparkinsonian treatment is required, it may need to be continued after stopping haloperidol due to differences in excretion. If both therapies are stopped at the same time, extrapyramidal symptoms may develop. The physician should be aware of the possible increase in intraocular pressure if anticholinergic drugs, including antiparkinsonian agents, are administered simultaneously with haloperidol.

As with other antipsychotics, it should be noted that haloperidol may potentiate CNS depressants such as anesthetics, opiates, and alcohol.

Ketoconazole is a potent inhibitor of CYP3A4. Prolongation of the QT interval has been observed when haloperidol is administered in combination with the metabolic inhibitors ketoconazole (400 mg/day) and paroxetine (20 mg/day). It may be necessary to reduce the dosage of haloperidol.

Pharmacokinetic interaction

Effect of other drugs on haloperidol

Haloperidol is metabolized in several ways, including glucuronidation and the cytochrome P450 enzyme system. Inhibition of these metabolic pathways by another drug may lead to an increase in haloperidol concentrations and potentially increase the risk of some side effects, including prolongation of the QT interval.

Drugs characterized as substrates, inhibitors or inducers of CYP3A4, CYP2D6 or glucuronidation

Mild to moderate elevations in haloperidol concentrations have been reported in pharmacokinetic studies when administered concomitantly with drugs characterized as substrates or inhibitors of CYP3A4 or CYP2D6 isoenzymes, such as itraconazole, nefazodone, buspirone, venlafaxine, alprazolam, fluvoxamine, quinidine, fluoxetine, sertraline, chlorpromazine and promethazine.

If long-term treatment (1-2 weeks) with enzyme-stimulating drugs such as rifampin or carbamazepine is added to haloperidol therapy, this leads to a significant decrease in its plasma levels.

Rifampin

In a study of 12 patients with schizophrenia who received concomitant oral haloperidol and rifampin, plasma levels of haloperidol decreased by an average of 70%. In 5 other schizophrenic patients treated with haloperidol and rifampin, discontinuation of rifampin produced a mean 3.3-fold increase in haloperidol concentrations.

Carbamazepine

In a study of 11 patients with schizophrenia, when haloperidol was co-administered with an increase in the dose of carbamazepine, plasma concentrations of haloperidol decreased linearly with increasing carbamazepine concentration.

Thus, close clinical monitoring is warranted when enzyme-stimulating drugs such as rifampin or carbamazepine are administered or discontinued in patients on haloperidol treatment. In combination therapy, the dose of haloperidol must be adjusted when necessary. After stopping these drugs, it may be necessary to reduce the dosage of haloperidol.

Valproate

Sodium valproate, a drug that inhibits glucuronidation, does not affect plasma concentrations of haloperidol.

Information for patients

Haloperidol may impair the mental and/or physical abilities required to perform hazardous tasks such as operating machinery or driving a car. The outpatient should be warned accordingly.

Drinking alcohol with this drug should be avoided due to possible addictive effects and hypotension.

Carcinogenesis, Mutagenesis and Impairment of Fertility

The mutagenic potential of haloperidol was not detected in the Salmonella Amesw microsomal activation assay. Negative or inconsistent positive results have been reported in in vitro and in vivo studies of the effects of haloperidol on chromosome structure and number. The available cytogenetic evidence is considered too conflicting to be conclusive at present.

Antipsychotic drugs raise prolactin levels; growth is maintained with chronic administration. Tissue culture experiments show that approximately one-third of human breast cancers are dependent on in vitro prolactin, a factor of potential importance if prescribing such a drug to a patient with previously diagnosed breast cancer is being considered. Although disorders such as galactorrhea, amenorrhea, gynecomastia and impotence have already been mentioned, the clinical significance of elevated serum prolactin levels for most patients is unknown. An increase in neoplasms in the mammary glands has been found in rodents after chronic administration of antipsychotic drugs. However, clinical studies and epidemiological studies conducted to date have not shown an association between chronic administration of these drugs and breast tumors. The available evidence is considered too limited to be conclusive at present.

Use during pregnancy

There are no well-controlled studies of haloperidol in pregnant women. However, there are reports of cases of limb malformations observed due to maternal use of haloperidol along with other drugs with suspected teratogenic potential during the first trimester of pregnancy. A causal relationship has not been established in these cases. Since such experience does not exclude the possibility of fetal harm due to haloperidol, this drug should be used during pregnancy or in women of childbearing potential only if the benefit clearly justifies the potential risk to the fetus. Infants should not be breast-fed while being treated with this medicine.

Non-teratogenic effects

Haloperidol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

endocrine disorders

Breastfeeding, breast engorgement, mastalgia, menstrual irregularities, gynecomastia, impotence, increased libido, hyperglycemia, hypoglycemia, and hyponatremia.

Gastrointestinal effects

Anorexia, constipation, diarrhea, hypersalivation, dyspepsia, nausea and vomiting.

Vegetative reactions

Dry mouth, blurred vision, urinary retention, diaphoresis and priapism.

Respiratory effects

Laryngospasm, bronchospasm and increased depth of breathing.

Cataract, retinopathy and visual impairment.

Post-marketing events

Hyperammonemia was mentioned in a report on the treatment of a 5.5-year-old child with citrullinaemia, an inherited disorder of urinary ammonia excretion, after treatment with haloperidol.

Overdose

Manifestations

In general, overdose symptoms will be an exaggeration of known pharmacological effects and adverse reactions, the most notable of which are severe extrapyramidal reactions; hypotension or sedation. The patient enters a comatose state with respiratory depression and hypotension, which may be severe enough to produce a shock-like state. Extrapyramidal reactions will be manifested by muscle weakness or rigidity and generalized or localized tremor, as demonstrated by the akinetic or tremor types, respectively. A 2-year-old child with an accidental overdose developed hypertension rather than hypotension. The risk of ECG changes associated with bidirectional tachycardia should be considered.

Treatment

Because there is no specific antidote, treatment is primarily supportive. It is necessary to secure an open airway using an oropharyngeal airway or endotracheal tube, or, in cases of prolonged coma, tracheostomy. Respiratory failure can be neutralized by artificial respiration and mechanical respirators. Hypotension and heart failure can be counteracted with intravenous infusion, plasma or concentrated albumin, and vasopressor agents such as metaraminol, phenylephrine, and norepinephrine. Adrenaline cannot be used. In case of severe extrapyramidal reactions, an antiparkinsonian drug should be administered. The ECG and vital signs should be monitored specifically for signs of QT prolongation or arrhythmias, and monitoring should be continued until the ECG is normal. Severe arrhythmias should be treated with appropriate antiarrhythmic measures.

Dosage and administration of haloperidol

All patients need a different amount of medication for treatment. As with all medications used to treat schizophrenia, dosage should be individualized based on the needs and response of each patient. Dosage adjustments up or down should be made as quickly as possible to achieve optimal therapeutic control.

The patient's age, disease severity, previous reaction to other antipsychotics, and any concomitant medications or illnesses should be considered in determining the starting dose. Debilitated or elderly patients, as well as patients with a history of adverse reactions to antipsychotic drugs, may require less haloperidol. Optimal response in these patients usually occurs with gradual dose adjustments and at lower doses.

A parenteral drug administered intramuscularly in doses of 2-5 mg is used for the rapid control of acutely excitable patients with schizophrenia, with moderately severe and very severe symptoms. Depending on the response of the patient, subsequent doses may be given every hour, although intervals of 4-8 hours may be satisfactory. The maximum dose is 20 mg/day.

Controlled trials to establish the safety and efficacy of intramuscular injection in children have not been conducted.

Parenteral preparations should be inspected visually for particulate matter and discoloration prior to administration, if solutions and container permit.

Switch order

The oral form should replace the injectable as soon as possible. In the absence of bioavailability studies establishing bioequivalence between these two dosage forms, the following dosage guidelines are suggested. For an initial approximation of the total required daily dose, the parenteral dose in the previous 24 hours can be used. Since this dose is only an initial estimate, close monitoring for clinical signs and symptoms, including clinical efficacy, side effects, and sedation, is recommended periodically during the first few days after initiation of the transition. Thus, it is possible to quickly adjust the dose up or down. Depending on the clinical condition of the patient, the first oral dose should be administered within 12-24 hours after the last parenteral dose.

The active substance is haloperidol .

The tablets contain 1.5 or 5 mg of this substance. Additional elements are: talc, potato starch, gelatin, magnesium stearate, lactose monohydrate.

1 ml of solution contains 5 mg of the active substance. Additional substances are: injection water, lactic acid, methylparaben, propylparaben.

Drops from the company Ratiopharm contain 2 mg of active substance per 1 ml. Additional substances are: methyl parahydroxybenzoate, purified water, propyl parahydroxybenzoate, lactic acid.

Release form

Tablets and solution for injections. Haloperidol drops are also produced by Ratiopharm.

pharmachologic effect

What is Haloperidol? What is this drug? Haloperidol is neuroleptic, antipsychotic, antiemetic drug .

Pharmacodynamics and pharmacokinetics

The active ingredient is a derivative of butyrophenone. Blocks dopamine, postsynaptic receptors in the mesocortical, mesolimbic structures of the brain, has a pronounced antipsychotic effect. Despite the high antipsychotic activity , the drug combines a moderately pronounced sedative and antiemetic effects. It does not have an anticholinergic effect, but causes extrapyramidal disorders. The sedative effect is due to blockade in the reticular pharmacy of alpha-adrenergic receptors.

Antiemetic effect achieved by blockade of the vomiting center in the trigger zone. With the blockade of dopamine receptors in the hypothalamas, galactorrhea and hypothermic effects are manifested. With long-term therapy, a change in the endocrine status occurs, the production of gonadotropic hormones decreases and prolactin synthesis due to the influence on the anterior lobe. The drug allows you to eliminate persistent personality changes, mania, hallucinations, delirium, increases the patient's interest in the outside world.

Haloperidol is prescribed to patients who have developed resistance to other antipsychotic drugs. The drug has an activating effect on patients.

In hyperactive children, Haloperidol is able to eliminate behavioral disorders, excessive motor activity.

Haloperidol decanoate has a longer duration of action than haloperidol.

The therapeutic effect of prolonged forms of the drug lasts up to 6 weeks.

The maximum concentration after applying the solution is observed after 10-20 minutes, when using tablets - after 3-6 hours. The solution and tablets are excreted in the urine and feces in a ratio of 2:3. Drops are excreted in bile (15%) and urine (40%).

Indications for the use of Haloperidol

Indications for use are as follows. The drug is prescribed for hallucinations , delirium, acute psychosis, psychomotor agitation, "steroid" psychosis, alcoholic and drug psychosis, with agitated depression, mental retardation, Tourette's disease , psychoses of various genesis, with chorea of ​​Huntington , with psychosomatic disorders, with stuttering, children's , hyperactivity in children.

Contraindications

The drug is not used for severe CNS depression, with intolerance to the active substance, with CNS pathology, which is accompanied by extrapyramidal and pyramidal symptoms, with breastfeeding , hysteria, depression, during pregnancy, children under three years of age. In violation of intracardiac conduction, with angina pectoris, prolongation of the QT interval, with angle-closure glaucoma, with hypokalemia, decompensated heart disease, with epilepsy, pathology of the kidneys and liver, with respiratory and pulmonary heart failure, with, prostatic hyperplasia with urinary retention, with acute infectious diseases, with COPD Haloperidol is used with caution.

Side effects of Haloperidol

Nervous system:, agitation, anxiety, akathisia , fears, anxiety, exacerbation, psychosis, lethargy, depression, or seizures of epilepsy, tardive dyskinesia, with prolonged therapy, extrapyramidal disorders, tardive dystonia (eyelid spasms, rapid blinking, uncontrolled movements of the arms, legs, torso, neck) are noted, neuroleptic malignant syndrome (loss of consciousness, urinary incontinence, rapid or difficult breathing, increased sweating, blood pressure instability, arrhythmia, tachycardia , hyperthermia, epileptic seizures, muscle rigidity).

The cardiovascular system: signs of flicker and flutter of the ventricles on the ECG, tachycardia, arrhythmia, orthostatic hypotension , drop in blood pressure.

Digestive system:, dry mouth, loss of appetite, hyposalivation, diarrhea, nausea, vomiting, abnormalities in the liver.

Hematopoietic organs: tendency to monocytosis, erythropenia, agranulocytosis, leukocytosis, leukopenia are temporary.

Urogenital system: priapism, increased libido or decreased potency, menstrual irregularities in females, gynecomastia , pain in the mammary glands, peripheral edema, with prostatic hyperplasia, urinary retention is noted.

The following side effects are also possible: photosensitivity , laryngospasm, bronchospasm, maculopapular changes in the skin, blurred vision, retinopathy, cataracts, hyponatremia, hypoglycemia, weight gain, alopecia.

Application instruction of Haloperidol (Way and dosage)

Haloperidol tablets, instructions for use

It is taken orally, washed down with a full glass of milk, water. The initial dosage is 0.5-5 mg three times a day. Not more than 100 mg per day. The duration of therapy is 2-3 months. The drug is canceled gradually, the dosage is reduced slowly, they switch to maintenance doses - 5-10 mg per day.

Tourette's disease, non-psychotic behavioral disorders: 0.05 mg/kg/day 2-3 times a day, with a gradual increase in the dose by 0.5 mg 1 time per week to a maximum of 0.075 mg/kg/day.

Solution use

The average single dose for intramuscular administration of Haloperidol is 2-5 mg, the interval between injections is 48 hours. Acute alcoholic psychosis: intravenously 5-10 mg.

Instructions for drops Haloperidol Ratiopharm

Usually consumed up to three times a day with food.

Adults are usually prescribed 0.5-1.5 mg 3 times a day. Further, the dose of the drug can be increased to an average of 10-15 mg per day. For acute symptoms, 15 mg per day or more is allowed. The maximum dose is 100 mg per day.

The initial dose for children from three years old is 0.025-0.05 mg per kg of body weight, which is taken 3 times. The maximum can be increased to 0.2 mg per kg of body weight.

Overdose

appears, muscle stiffness , falling . In severe cases, shock, respiratory depression, coma are recorded. Requires gastric lavage, the appointment of enterosorbents. Norepinephrine and albumin are used to improve circulation. Application is not allowed . Antiparkinsonian drugs and central anticholinergics can reduce the severity of extrapyramidal symptoms. Dialysis has not been proven to be effective.

Interaction

Haloperidol enhances the severity of the inhibitory effect of sleeping pills, barbiturates, opioid analgesics , tricyclic antidepressants, ethanol, agents for general anesthesia on the central nervous system. The drug enhances the effect of antihypertensive drugs, m-anticholinergics, inhibits the process of MAO inhibitors, tricyclic antidepressants, at the same time, their toxicity and sedative effect mutually increase. Buprorion in combination with haloperidol increases the likelihood of grand mal seizures and lowers the epileptic threshold. The drug weakens the vasoconstrictor effect of norepinephrine, , epinephrine. The drug reduces the effectiveness anticonvulsants , antiparkinsonian drugs, changes the effect of anticoagulants. The risk of developing mental disorders increases when administered with the drug. Amphetamines can reduce the antipsychotic effect of haloperidol. With the use of strong coffee, tea, a decrease in the effectiveness of haloperidol is noted. Antiparkinsonian, antihistamine, anticholinergic agents increase the m-anticholinergic effect of the neuroleptic, reduce the severity of its antipsychotic effect. With prolonged use of microsomal oxidation inducers, barbiturates, the concentration of neuroleptic in the blood decreases. In combination with lithium preparations, the formation of encephalopathy, an increase in the severity of extrapyramidal disorders is possible. can enhance the severity of extrapyramidal symptoms, side effects from the nervous system. The appointment of drugs that cause extrapyramidal reactions leads to an increase in the severity and frequency extrapyramidal disorders .

Terms of sale

Need a prescription.

Storage conditions

In a dark place inaccessible to children at a temperature not exceeding 25 degrees Celsius.

Best before date

Not more than 3 years.

special instructions

Regular monitoring of the level of "liver" tests, monitoring of ECG dynamics, blood counts is required. Parenteral administration of the drug is carried out only under the supervision of the attending physician. After achieving a therapeutic effect, they switch to taking tablet forms of the drug. In case of late registration dyskinesia against the background of treatment, a gradual decrease in dosage is required up to a complete cessation. When taking a hot bath, heat stroke is possible due to the suppression of peripheral, central thermoregulation located in. Care must be taken when performing a heavy type of physical work. It is not recommended to use over-the-counter "cold" drugs during the entire period of treatment due to the risk of heat stroke, increased anticholinergic effects. Due to the risk of photosensitivity, patients need to protect exposed skin from sunlight. Haloperidol is canceled gradually in view of the risk of developing the "withdrawal" syndrome. Often the antiemetic effect of the drug masks the symptoms drug toxicity , and also makes it difficult to diagnose conditions that are accompanied by nausea. Haloperidol may precipitate when its solution is mixed with tea, coffee. Before the appointment of prolonged forms of the drug, the patient is transferred to Haloperidol from other antipsychotics to prevent a sharp hypersensitivity to the drug. The drug affects the management of vehicles.

The drug is described in Wikipedia.

INN: haloperidol.

OKPD: 24.42.13.693

Haloperidol and alcohol

The drug is incompatible with alcohol, due to an increase in their effect on the central nervous system when used together.

Analogues

Coincidence in the ATX code of the 4th level:

Analogues are drugs halomond , Halopril , Senorm .

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

Haloperidol- a neuroleptic 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, 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).

Enhances the effect of hypnotics, narcotic analgesics, general anesthesia, analgesics and other drugs that depress the function of the central nervous system.

Pharmacokinetics

It is absorbed by passive diffusion, in a non-ionized form, mainly from the small intestine. Bioavailability - 60-70%. Haloperidol is metabolized in the liver, the metabolite is pharmacologically inactive. Haloperidol also undergoes oxidative N-dealkylation and glucuronidation. It is excreted as metabolites through the intestines - 60% (including with bile - 15%), by the kidneys - 40%, (including 1% - unchanged). Easily penetrates through 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 unresponsive to therapy hiccups;
• vomiting that is not amenable to treatment with classical antiemetics, including those associated with anticancer therapy;
• premedication before surgery.

Release forms

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

Solution for intramuscular injection (oily) Haloperidol Decanoate (forte or prolong formula).

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

There are no other forms, whether 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 decrease in the dose to ensure the lowest effective dose. High doses are used only in cases of ineffectiveness of smaller doses. The average doses are suggested below.

To stop 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. Upon reaching a stable sedative effect, they switch to taking the drug orally.

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

The parenteral route of administration of haloperidol should be carried out under the close supervision of a physician, especially in elderly patients and children. After achieving a therapeutic effect, you should switch to taking the drug inside.

Tablets

Assign inside, 30 minutes before meals (possible with milk to reduce the irritating effect on 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 desired therapeutic effect is achieved. The maximum daily dose is 100 mg. On average, the therapeutic dose is 10-15 mg per day, in 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 the course of treatment is 2-3 months. Maintenance doses (without exacerbation) - from 0.5-0.75 mg to 5 mg per day (the dose is reduced gradually).

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

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

Oil solution (Decanoate)

The drug is intended exclusively for adults, exclusively for the / m administration!

Do not administer intravenously!

Adults: Patients on long-term treatment with oral antipsychotics (mainly haloperidol) may be advised to switch to depot injections.

The dose should be selected on an individual basis in view of the 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 neuroleptics prescribed during previous treatment.

At the beginning of treatment, every 4 weeks it is recommended to prescribe doses 10-15 times 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 in steps, 50 mg each, until the optimal effect is obtained. Typically, the maintenance dose corresponds to 20 times the daily dose of oral haloperidol. With the resumption of symptoms of the underlying disease during the period of dose selection, treatment with Haloperidol Decanoate can be supplemented with oral haloperidol.

Usually injections are administered every 4 weeks, however, due to large individual differences in effectiveness, more frequent use of the drug may be required.

Side effect

• headache;
• insomnia or drowsiness (especially at the beginning of treatment);
• anxiety;
• anxiety;
• excitation;
• fears;
• euphoria or depression;
• lethargy;
• epileptic seizures;
• development of a paradoxical reaction - exacerbation of psychosis and hallucinations;
• tardive dyskinesia (smacking and wrinkling of the lips, pouting of the cheeks, fast and worm-like movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the arms and legs);
• tardive dystonia (increased blinking or spasms of the eyelids, unusual facial expression or body position, uncontrolled twisting movements of the neck, torso, arms and legs);
• neuroleptic malignant syndrome (difficulty or rapid breathing, tachycardia, arrhythmia, hyperthermia, increase or decrease in blood pressure, increased sweating, urinary incontinence, muscle rigidity, epileptic seizures, loss of consciousness);
• decrease in blood pressure;
• orthostatic hypotension;
• arrhythmias;
• tachycardia;
• ECG changes (prolongation of the QT interval, signs of flutter and ventricular fibrillation);
• loss of 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;
• violation of the menstrual cycle;
• decrease in potency;
• increased libido;
• priapism;
• cataract;
• retinopathy;
• blurred vision;
• photosensitivity;
• bronchospasm;
• laryngospasm;
• the development of local reactions associated with the injection;
• alopecia;
• weight gain.

Contraindications

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

Use during pregnancy and lactation

Haloperidol does not cause a significant increase in the incidence of congenital malformations. Isolated cases of birth defects have been reported when taking haloperidol concomitantly with other drugs during pregnancy. Taking haloperidol during pregnancy is acceptable only in cases where the intended benefit to the mother outweighs the risk to the fetus. Haloperidol is excreted in breast milk. In cases where haloperidol is unavoidable, the benefits of breastfeeding in relation to the potential hazard must be justified. In some cases, estrapyramidal symptoms were 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 older than 3 years, the dose is 0.025-0.05 mg per day, divided into 2 injections. The maximum daily dose is 0.15 mg/kg.

The parenteral route of administration of haloperidol should be carried out under the close supervision of a physician, especially in children. After achieving a therapeutic effect, you should switch to taking the drug inside.

Tablets

Children aged 3-12 years (weighing 15-40 kg): 0.025-0.05 mg / kg body weight per day 2-3 times a day, increasing the dose no more than 1 time in 5-7 days, up to the 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 1 time in 5-7 days to 3 mg per day. With 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 and pediatric patients. Upon reaching a therapeutic effect, you should switch to an oral form of treatment.

Since haloperidol can cause QT interval prolongation, caution should be exercised if there is a risk of QT prolongation (QT syndrome, hypokalemia, drugs that cause QT interval prolongation), especially when administered parenterally. Due to the metabolism of haloperidol in the liver, it is important to exercise caution when prescribing it to patients with impaired hepatic function.

Cases of development of the spasms caused by a haloperidol are known. Patients with epilepsy and patients in conditions predisposing to the development of a convulsive syndrome (alcoholism, brain injury), the drug should be used with extreme caution.

In case of lactose intolerance, it should be borne in mind that a 1.5 mg tablet contains 157 mg of lactose, a 5 mg tablet contains 153.5 mg.

With heavy physical exertion, taking a hot bath, caution is required due to the possible development of heat stroke as a result of ineffective central and peripheral thermoregulation of the hypothalamus due to the drug.

The patient should be warned about the need to avoid taking medicines for colds, acquired without a prescription, because. it is possible to increase the anticholinergic effects of haloperidol and the development of heat stroke. During treatment, patients should regularly monitor the ECG, blood counts, liver tests.

For the relief of extrapyramidal disorders, antiparkinsonian drugs (cyclodol), nootropics, vitamins are prescribed; their use is continued after the withdrawal of haloperidol, if they are excreted from the body faster than haloperidol in order to avoid exacerbation of extrapyramidal symptoms.

The severity of extrapyramidal disorders is related to the dose, often, with a decrease in dose, they can decrease or disappear.

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

With the development of tardive dyskinesia, the drug should not be abruptly discontinued; gradual dose reduction is recommended.

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

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

Influence on the ability to drive vehicles and control mechanisms

While taking haloperidol, it is forbidden to drive vehicles, maintain mechanisms and perform other types of work that require increased concentration of attention, as well as drinking alcohol.

drug interaction

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

With simultaneous use with antiparkinsonian drugs (levodopa and others), the therapeutic effect of these drugs may decrease due to the antagonistic effect on dopaminergic structures.

When used with methyldopa, the development of disorientation, difficulty and slowing down of thinking processes is possible.

Haloperidol can weaken the action of adrenaline (epinephrine) and other sympathomimetics, cause a "paradoxical" decrease in blood pressure and tachycardia when they are used together.

Enhances the effect of peripheral M-anticholinergics 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 seizure threshold; in addition, serum concentrations of haloperidol may also decrease. In particular, with the simultaneous use of tea or coffee, the effect of haloperidol may weaken.

Haloperidol can reduce the effectiveness of indirect anticoagulants, therefore, when taken together, the dose of the latter should be adjusted.

Haloperidol slows down the metabolism of tricyclic antidepressants and MAO inhibitors, as a result of which their plasma levels increase and toxicity increases.

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

With the simultaneous administration of haloperidol 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, as well as increase extrapyramidal symptoms.

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

Haloperidol may reduce 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 hyperthyroidism, haloperidol can be prescribed only with the simultaneous conduct of appropriate thyreostatic therapy.

With simultaneous use with anticholinergic drugs, an increase in intraocular pressure is possible.

Analogues of the drug Haloperidol

Structural analogues for the active substance:

• Apo Haloperidol;
• Galloper;
• Haloperidol decanoate;
• Haloperidol Akri;
• Haloperidol ratiopharm;
• Haloperidol Richter;
• Haloperidol Ferein;
• Senorm.

In the absence of analogues of the drug for the active substance, you can follow the links below to the diseases that the corresponding drug helps with and see the available analogues for the therapeutic effect.

Haloperidol: instructions for use and reviews

Latin name: Haloperidol

ATX code: N05AD01

Active substance: haloperidol (haloperidol)

Manufacturer: Gedeon Richter (Hungary), Moskhimfarmpreparaty im. N.A.Semashko (Russia)

Description and photo update: 12.07.2018

Gross formula

Pharmacological group of the substance Haloperidol

Nosological classification (ICD-10)

CAS code

Characteristics of the substance Haloperidol

Antipsychotic, butyrophenone derivative.

Amorphous or microcrystalline powder from white to light yellow. Practically insoluble in water, sparingly soluble in alcohol, methylene chloride, ether. A saturated solution is neutral to slightly acidic.

Pharmacology

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. It inhibits the release of mediators, reducing the permeability of presynaptic membranes, disrupts the reverse neuronal uptake and deposition.

Eliminates persistent personality changes, delirium, hallucinations, mania, enhances interest in the environment. Influences autonomic functions (reduces the tone of hollow organs, motility and secretion of the gastrointestinal tract, eliminates vasospasm) in diseases accompanied by excitement, anxiety, fear of death. Long-term use is accompanied by a change in the endocrine status, in the anterior pituitary gland, the production of prolactin increases and the production of gonadotropic hormones decreases.

When taken orally, 60% is absorbed. Plasma protein binding - 92%. T max when administered orally - 3-6 hours, with intramuscular injection - 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 the tissue, because. easily passes histohematic barriers, including the BBB. V ss is 18 l/kg. Metabolized in the liver, exposed to the effect of the first pass through the liver. A strict relationship between plasma concentration and effects has not been established. T 1/2 when administered orally - 24 hours (12-37 hours), with intramuscular injection - 21 hours (17-25 hours), with intravenous administration - 14 hours (10-19 hours), for haloperidol decanoate - 3 weeks (single or multiple doses). It is excreted by the kidneys and with bile.

Effective in patients resistant to other antipsychotics. It has some activating effect. In hyperactive children, it eliminates excessive motor activity, behavioral disorders (impulsivity, difficulty concentrating, aggressiveness).

Application of the substance Haloperidol

Psychomotor agitation of various origins (manic state, oligophrenia, psychopathy, schizophrenia, chronic alcoholism), delusions and hallucinations (paranoid states, acute psychosis), Gilles de la Tourette syndrome, Huntington's chorea, psychosomatic disorders, behavioral disorders in the elderly and childhood, stuttering , long-lasting and therapy-resistant vomiting and hiccups. For haloperidol decanoate: schizophrenia (maintenance therapy).

Contraindications

Hypersensitivity, severe toxic CNS depression or coma caused by taking drugs; diseases of the central nervous system, accompanied by pyramidal and extrapyramidal symptoms (including Parkinson's disease), epilepsy (convulsive threshold may decrease), severe depressive disorders (possible aggravation of symptoms), cardiovascular diseases with decompensation phenomena, pregnancy, breastfeeding, age up to 3 years.

Application restrictions

Glaucoma or predisposition to it, pulmonary insufficiency, hyperthyroidism or thyrotoxicosis, impaired liver and / or kidney function, urinary retention.

Use during pregnancy and lactation

Contraindicated in pregnancy.

At the time of treatment should stop breastfeeding (penetrates into breast milk).

Side effects of Haloperidol

From the nervous system and sensory organs: akathisia, dystonic extrapyramidal disorders (including spasm of the muscles of the face, neck and back, tic-like movements or twitches, weakness in the arms and legs), parkinsonian extrapyramidal disorders (including difficulty in speaking and swallowing, mask-like face, shuffling gait, tremor of the hands and fingers), headache, insomnia, drowsiness, anxiety, anxiety, agitation, agitation, euphoria or depression, lethargy, epileptic seizures, confusion, exacerbation of psychosis and hallucinations, tardive dyskinesia (see "Precautions"); visual impairment (including visual acuity), cataract, retinopathy.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): tachycardia, hypotension/hypertension, interval prolongation QT, ventricular arrhythmia, ECG changes; there are reports of sudden death, prolongation of the interval QT and violation of the heart rhythm type "pirouette" (see "Precautions"); transient leukopenia and leukocytosis, erythropenia, anemia, agranulocytosis.

From the respiratory system: laryngospasm, bronchospasm.

From the digestive tract: anorexia, constipation / diarrhea, hypersalivation, nausea, vomiting, dry mouth, abnormal liver function, obstructive jaundice.

From the genitourinary system: breast engorgement, unusual milk secretion, mastalgia, gynecomastia, menstrual irregularities, urinary retention, impotence, increased libido, priapism.

From the side of the skin: maculopapular and acne-like skin changes, photosensitivity, alopecia.

Others: neuroleptic malignant syndrome, accompanied by hyperthermia, muscle rigidity, loss of consciousness; hyperprolactinemia, sweating, hyperglycemia/hypoglycemia, hyponatremia.

Interaction

Enhances the effect of antihypertensive drugs, opioid analgesics, antidepressants, barbiturates, alcohol, weakens - indirect anticoagulants. It inhibits the metabolism of tricyclic antidepressants (their plasma level increases) and increases toxicity. With long-term administration of carbamazepine, the plasma level of haloperidol falls (it is necessary to increase the dose). In combination with lithium, it can cause an encephalopathy-like syndrome.

Overdose

Symptoms: pronounced extrapyramidal disorders, arterial hypotension, drowsiness, lethargy, in severe cases - coma, respiratory depression, shock.

Treatment: there is no specific antidote. Perhaps gastric lavage, the subsequent appointment of activated charcoal (if the overdose is associated with ingestion). With 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 anticholinergics and antiparkinsonian drugs.

Routes of administration

In / in, in / m and inside.

Precautions Substance Haloperidol

Increased mortality in older patients with dementia-associated psychosis. According to Food and Drug Administration (FDA) 1 , antipsychotic drugs increase mortality in elderly patients in the treatment of psychosis on the background of 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 who received placebo. In typical 10-week controlled trials, the drug-associated mortality rate was about 4.5%, while in the placebo group it was 2.6%. Although the causes of death varied, the majority were related to cardiovascular problems (such as heart failure, sudden death) or pneumonia. Observational studies suggest that, like atypical antipsychotics, treatment with conventional antipsychotics may also be associated with increased mortality.

Tardive dyskinesia. As with other antipsychotics, haloperidol has been associated with the development of tardive dyskinesia, a syndrome characterized by involuntary movements (may appear in some patients during long-term treatment or occur after drug therapy has been discontinued). The risk of developing tardive dyskinesia is higher in elderly patients with high doses, especially in women. Symptoms are persistent and, in some patients, irreversible: rhythmic involuntary movements of the tongue, face, mouth, and jaw (eg, protrusion of the tongue, pouting of the cheeks, wrinkling of the lips, uncontrolled chewing movements), sometimes they may be accompanied by involuntary movements of the limbs and trunk. With the development of tardive dyskinesia, drug withdrawal is recommended.

Dystonic extrapyramidal disorders are most common in children and young people, and also at the beginning of treatment; may subside within 24-48 hours after discontinuation of haloperidol. Parkinsonian extrapyramidal effects are more likely to develop in the elderly and are detected in the first few days of treatment or during long-term therapy.

Cardiovascular effects. Cases of sudden death, interval prolongation QT and torsades de pointes have been reported in patients treated with haloperidol. Caution should be exercised in the treatment of patients with predisposition factors for interval prolongation. QT, incl. electrolyte imbalance (especially hypokalemia and hypomagnesemia), concomitant use of drugs that prolong the interval QT. When treating with haloperidol, it is necessary to regularly monitor the ECG, blood counts, and evaluate the level of liver enzymes. During therapy, patients should refrain from engaging in potentially hazardous activities that require increased attention, rapid mental and motor reactions.