Composition, form of production and packaging
Tablets are white or almost white in color, flat, disk-like, with a facet, practically odorless, with an engraved "I | I" on one side.
1 tab.
haloperidol 1.5 mg
Auxiliary substances: potato starch - 1 mg, silicon dioxide colloid - 1.25 mg, gelatin - 2 mg, magnesium stearate - 2.5 mg, talc - 5.75 mg, corn starch - 79 mg, lactose monohydrate - 157 mg.
25 pcs. - blisters (2) - packs of cardboard.
Tablets are white or almost white, round, flat-cylindrical, practically odorless.
1 tab.
haloperidol 5 mg
Auxiliary substances: potato starch - 1 mg, silicon dioxide colloid - 1.25 mg, gelatin - 2 mg, magnesium stearate - 2.5 mg, talc - 5.75 mg, corn starch - 79 mg, lactose monohydrate - 153.5 mg.
25 pcs. - blisters (2) - packs of cardboard.
The solution for intravenous and / or injection is colorless or slightly yellowish, transparent, without mechanical impurities.
1 amp.
haloperidol 5 mg
Excipients: lactic acid - 5 mg, water d / and - up to 1 ml.
1 ml - ampoules of colorless glass (5) - cardboard boxes.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
Antipsychotic agent (neuroleptic), a derivative of butyrophenone. Has a pronounced antipsychotic effect, blocks postsynaptic dopamine receptors in the mesolimbic and mesocortical structures of the brain. High antipsychotic activity is combined with a moderate sedative effect (in small doses has an activating effect) and pronounced antiemetic effect. Does not have antihistaminergic or anticholinergic activity.
Sedative action is due to blockade of ОІ-adrenoreceptors of the reticular formation of the brainstem; antiemetic effect - blockade of dopamine D 2 receptors in the trigger zone of the vomiting center; hypothermic action and galactorrhea - blockade of dopamine receptors of the hypothalamus.
As a result of exposure to the basal ganglion causes extrapyramidal disorders (dystonia, akathisia, parkinsonism).
Long-term use is accompanied by a change in the endocrine status, in the anterior part of the pituitary gland prolactin production increases and the production of gonadotropic hormones decreases.
Haloperidol is highly effective in the treatment of hallucinations and delusions. Has a pronounced soothing effect in psychomotor agitation, is effective in mania and other agitation, and as an additional tool in the treatment of chronic pain.
PHARMACOKINETICS
Suction
When ingested, absorbed by passive diffusion, in a non-ionized form, mainly from the small intestine. Bioavailability is 60-70%. When administered orally, Cmax in the blood is reached after 2-6 hours, with IM in 20 minutes. The therapeutic effect occurs at a plasma concentration of 20-25 mg / l.
Distribution
Haloperidol binds to plasma proteins 90%, 10% is a free fraction. V d in the equilibrium state is 7.9 В± 2.5 l / kg. The ratio of concentration in erythrocytes to plasma concentration is 1:12. The concentration of haloperidol in tissues is higher than in blood, the drug tends to accumulate in tissues. Easily passes through the histohematological barriers, including placental and GEB. Penetrates into breast milk.
Metabolism
Exposed to the effect of "first passage" through the liver. Metabolised in the liver by oxidative N-dealkylation and glucuronation. The isozymes CYP2D6, CYP3A3, CYP3A5, CYP3A7 take part in the metabolism of the drug. It is an inhibitor of CYP2D6. There are no active metabolites.
Excretion
T 1/2 from the blood plasma for ingestion - 24 h (12-37 h), after the / m introduction - 21 h (17-25 h), after iv - 14 h (10-19 h). It is excreted in the form of metabolites with feces - 60% (including bile 15%), with urine - 40% (including 1% - unchanged).
INDICATIONS
- acute and chronic psychoses accompanied by excitement, hallucinatory and delusional disorders, manic conditions, psychosomatic disorders;
- Behavioral disorders, personality changes (paranoid, schizoid and others), Gilles de la Tourette's syndrome, both in childhood and in adults;
- ticks, Goettington's chorea;
- long-lasting and unchanged vomiting, incl. associated with antitumor therapy, and hiccups;
- Premedication before surgery.
DOSING MODE
Solution for intravenous and / m administration
To stop and treat psychotic disorders of various etiologies in the early days, haloperidol is administered intravenously 2.5-5 mg 2-3 times / day, or IV in the same dose (the ampoule should be diluted in 10-15 ml of water for injection), the maximum daily dose is 60 mg. After achieving a stable sedative effect, they switch to taking the drug inside.
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).
For children older than 3 years, the dose is 0.025-0.05 mg / day, divided into 2 injections. The maximum daily dose is 0.15 mg / kg.
In acute psychoses , 5-10 mg IV or IM. This dose can be repeated 1-2 times with an interval of 30-40 minutes until the desired effect is obtained. The maximum daily dose is 100 mg.
With acute alcoholic psychosis - IV 5-10 mg; if ineffectiveness, an additional infusion in a dose of 10-20 mg with a speed of no more than 10 mg / min is performed.
As a premedication before an operative intervention - for 30-40 minutes before an operative intervention in / in or / m 2-5 mg.
With long-lasting and resistant to therapy, vomiting, incl. associated with antitumor therapy - 1.5-2 mg 2 times / day.
The parenteral route of administration of haloperidol should be carried out under close medical supervision, especially in elderly patients and children. After achieving a therapeutic effect, you should switch to taking the drug inside.
Pills
Is taken orally, during or after a meal, with a full (240 ml) glass of water or milk.
The dose 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 dose reduction in order to ensure the lowest effective dose. High doses are used only in cases of ineffectiveness of smaller doses. The following are the average doses.
The initial daily intake for adults is 1.5-5 mg, divided into 2-3 doses. If necessary, the dose is gradually increased by 1.5-3 mg (in resistant cases to 5 mg) until the necessary therapeutic effect is achieved. The maximum daily dose is 100 mg. On average, the therapeutic dose is 10-15 mg / day, with chronic forms of schizophrenia - 20-40 mg / day, if necessary, the dose can be increased to 50-60 mg / day. The maximum dose is 100 mg / day. On average, the duration of treatment is 2-3 months.Supporting doses (outside the exacerbation) range from 0.5-0.75 mg to 5 mg / day (the dose is reduced gradually).
In acute psychoses , a single dose of 1.5-5 mg (up to 10 mg) in tablets, usually every 4-8 hours. The daily dose for oral administration of the drug is not more than 100 mg. Supportive therapy: in the interior - from 0.5 mg to 20 mg / day. A minimum dose is used that can support remission.
For nonpsychotic behavioral disorders, Gilles de la Tourette's syndrome - inside, at first 0.05 mg / kg / day in 2-3 doses, then gradually increase the dose 1 every 5-7 days to a total dose of 0.075 mg / kg / day.
With children's autism - inside 0.025-0.05 mg / kg / day.
When ticks, chorea Huntington - inside 0.025-0.05 mg / kg / day.
If there is no effect for 1 month, treatment should not be continued.
With long-lasting and resistant to therapy, vomiting - 1.5-2 mg 2 times / day.
Older or weakened patients are prescribed 1 / 3-1 / 2 of the usual dose for adults, the dose is increased no more often than every 2-3 days.
Children with a body weight of 60 kg and more with psychotic disorders - inside 0.05 mg / kg / day in 2-3 divided doses; if necessary taking into account the tolerability dose is gradually increased 1 time every 5-7 days to a total dose of 0.15 mg / kg / day.
SIDE EFFECT
From the side of the nervous system: headache, dizziness, insomnia or drowsiness (varying degrees of severity), anxiety, akathisia, euphoria, depression, convulsive disorders, extrapyramidal disorders; long-term dyskinesia (lip smacking and puckering, cheek swelling, rapid and wormlike movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the hands and feet), late dystonia (rapid blinking or spasms of the eyelids, unusual facial expression or body position, uncontrollable curving movements of the neck, trunk, arms and legs) and malignant neuroleptic syndrome (hyperthermia, muscle rigidity, difficulty or rapid breathing, tachycardia, arrhythmia, increased or decreased blood pressure, elevated sweating, urinary incontinence, convulsive disorders, depression of consciousness).
From the cardiovascular system: when used in high doses - reduced blood pressure, orthostatic hypotension, arrhythmias (ventricular arrhythmias such as pirouettes), changes in ECG (prolongation of the QT interval, signs of flutter and fibrillation of the ventricles), cases of sudden death.
On the part of the digestive system: when used in high doses - decreased appetite, dry mouth, hypo-salivation, nausea, vomiting, diarrhea or constipation, impaired liver function, until the development of jaundice.
On the part of the hematopoiesis system: transient leukopenia or leukocytosis, agranulocytosis, erythropenia and a tendency to monocytosis.
From the urinary system: urinary retention (for example, with prostatic hyperplasia), peripheral edema.
On the part of the reproductive system and the breast: pain in the mammary glands, gynecomastia, hyperprolactinaemia, menstrual cycle disorder, decreased potency, increased libido, priapism.
From the side of the organ of vision: cataract, retinopathy, blurred vision.
From the side of metabolism: hyponatremia, hyper- or hypoglycemia.
Dermatological reactions: maculopapular and acne-like skin changes, photosensitivity.
Allergic reactions: bronchospasm, laryngospasm.
Other: alopecia, weight gain, heat stroke.
CONTRAINDICATIONS
- severe toxic oppression of the central nervous system caused by xenobiotics, coma of different genesis;
- CNS diseases, accompanied by pyramidal and extrapyramidal disorders (Parkinson's disease);
- psychotic disorders associated with dementia in elderly patients (solution for IM and IV injections);
- Pregnancy;
- lactation period;
- Children's age up to 3 years (solution for / m and / in the introduction);
- Children weighing up to 60 kg (tablets);
- lactase deficiency, lactose intolerance, glucose-galactose malabsorption (tablets);
- hypersensitivity to butyrofenone derivatives;
- Hypersensitivity to the components of the drug.
Caution should be given to the drug in decompensated diseases of the cardiovascular system (including angina pectoris, intracardiac conduction disorders, prolongation of the QT interval on the ECG or predisposition to it - hypokalemia, simultaneous use of other drugs that can cause prolongation of the QT interval) epilepsy, angle-closure glaucoma, hepatic and / or renal insufficiency, hyperthyroidism (with thyrotoxicosis), pulmonary-cardiac and respiratory failure (including COPD and ost infectious diseases), prostatic hyperplasia with a delay in urine, alcoholism; solution for in / m and / in the introduction - in childhood and the elderly.
PREGNANCY AND LACTATION
Haloperidol-Richter is contraindicated in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be exercised in case of kidney failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Care should be taken with liver failure.
APPLICATION FOR CHILDREN
The drug in the form of a solution for IM and / or in administration is contraindicated in childhood to 3 years; in the form of tablets - for children weighing up to 60 kg.
The parenteral route of administration of haloperidol should be performed under the close supervision of the physician, especially in children.
APPLICATION IN ELDERLY PATIENTS
The parenteral route of administration of haloperidol should be carried out under close medical supervision, especially in elderly patients.
SPECIAL INSTRUCTIONS
Parenteral administration should be carried out under the strict supervision of a physician, especially in elderly and children. When the therapeutic effect is achieved, the oral form of treatment should be switched.
The drug Haloperidol-Richter, a solution for intravenous and / or injection, is not intended for the treatment of elderly patients with psychosis associated with dementia. The appointment of antipsychotics (including haloperidol) for the treatment of psychotic disorders associated with dementia in elderly patients, causes a risk of death. During the 10-week placebo-controlled clinical trial, mortality in the group of patients receiving antipsychotics was about 4.5%, compared to about 2.6% in the placebo group. Most of the deaths have been cardiovascular (eg, heart failure, sudden death) and / or infectious (eg, pneumonia) causes. Observational clinical studies have shown that therapy with traditional antipsychotics can increase mortality.
During treatment, ECG monitoring, blood formulas, and liver samples should be monitored regularly.
Since haloperidol can induce prolongation of the QT interval, caution should be exercised if there is a risk of prolonging the QT interval (QT prolonged interval syndrome, hypokalemia, use of QT prolongation drugs), especially with parenteral administration.
Due to the fact that haloperidol is metabolized in the liver, it is important to be cautious when administering the drug to patients with impaired liver function.
There are cases of development of seizures caused by haloperidol. Patients with epilepsy and patients, in conditions predisposing to the development of convulsive syndrome (alcoholism, a history of brain trauma), the drug should be administered with extreme caution.
For relief of extrapyramidal disorders, antiparkinsonian agents (cyclodol), nootropics, vitamins are prescribed; their use continues after haloperidol withdrawal, if they are excreted from the body more quickly than haloperidol, in order to avoid the increase of extrapyramidal symptoms.
With the development of tardive dyskinesia should not abruptly cancel the drug; a gradual dose reduction is recommended.
Treatment is stopped gradually to avoid the occurrence of withdrawal syndrome.
Care must be taken when performing heavy physical work, taking a hot bath (possibly developing a heat stroke due to suppression of central and peripheral thermoregulation in the hypothalamus).
During treatment, it is not necessary to take "anti-cold" non-prescription drugs (possibly increasing m-cholinoblocking effects and the risk of heat stroke).
Protect open areas of the skin from excessive sunlight due to the increased risk of photosensitivity.
An antiemetic effect can mask the signs of drug toxicity and make it difficult to diagnose conditions, the first symptom of which is nausea.
During drug treatment, alcohol consumption is not recommended.
Impact on the ability to drive vehicles and manage mechanisms
During the use of the drug is prohibited to drive vehicles and engage in other activities that require increased concentration and speed of psychomotor reactions.
OVERDOSE
When an overdose of the drug, the appearance of acute neuroleptic reactions.
Symptoms: muscle stiffness, tremor, drowsiness, decrease, sometimes an increase in blood pressure, in severe cases - coma, respiratory depression, shock, prolongation of QT interval on ECG, arrhythmia. Particularly should alarm the increase in body temperature, which may be one of the symptoms of malignant neuroleptic syndrome. In severe cases of overdose, various forms of impaired consciousness can be observed, including coma, convulsive reactions.
Treatment: ingestion - gastric lavage, activated charcoal. When respiratory depression, ventilation may be required. With a decrease in blood pressure and collapse, plasma or concentrated albumin, dopamine or norepinephrine is administered to maintain blood circulation. In these cases, epinephrine is strictly forbidden; its introduction can provoke a pronounced hypotension. For relief of extrapyramidal symptoms - central m-holinoblokatory and antiparkinsonian drugs. In / in is administered diazepam, a solution of dextrose, nootropics, vitamins B and C. Dialysis is ineffective. There is no specific antidote.
DRUG INTERACTION
Increases the severity of the inhibitory effect on the CNS ethanol, tricyclic antidepressants, narcotic analgesics, barbiturates and hypnotics, funds for general anesthesia.
Strengthens the action of peripheral m-holinoblokatorov and most antihypertensives (reduces the effect of guanetidine due to its displacement from? -adrenergic neurons and suppression of its capture by these neurons).
It inhibits the metabolism of tricyclic antidepressants and MAO inhibitors, while their (mutually) sedative effect and toxicity increase.
With simultaneous use with bupropion reduces the threshold of convulsive readiness and increases the risk of major epileptic seizures.
Reduces the effect of anticonvulsants (reducing the convulsive threshold with haloperidol).
Weaken the vasoconstrictive effect of dopamine, phenylephrine, norepinephrine, ephedrine and epinephrine (blockade of ОІ-adrenoreceptors by haloperidol, which can lead to a distortion of the action of epinephrine and a paradoxical decrease in blood pressure).
Reduces the effect of antiparkinsonian drugs (blockade of dopamine receptors in the central nervous system).
Changes (may increase or decrease) the effect of anticoagulants.
Reduces the effect of bromocriptine (dose adjustment may be required).
When used with methyldopa increases the risk of developing mental disorders (including disorientation in space, slowing and hindering thinking processes).
Amphetamines reduce the antipsychotic effect of haloperidol, which in turn reduces their psycho-stimulating effect (haloperidol-ОІ-adrenoreceptor blockade).
M-holinoblokatory, blockers of histamine H 1 -receptors of the 1st generation and antiparkinsonian agents can enhance the m-cholinoblocking effect of haloperidol and reduce its antipsychotic effect (dose adjustment may be required).
Long-term use of carbamazepine, barbiturates and other inducers of microsomal liver enzymes reduces the concentration of haloperidol in plasma.
In combination with lithium preparations (especially in high doses), the development of encephalopathy (can cause irreversible neurointoxication) and an increase in extrapyramidal symptoms.
With simultaneous use with fluoxetine, the risk of side effects from the central nervous system increases, especially extrapyramidal reactions.
With simultaneous use with drugs that cause extrapyramidal reactions, increases the frequency and severity of estropyramide disorders.
The use of strong tea or coffee (especially in large quantities) reduces the effect of haloperidol.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
Tablets should be stored out of reach of children at a temperature of 15-30 В° C.
Solution for iv and / m introduction should be stored in a place protected from light, inaccessible to children at a temperature of 15-30 В° C.
Shelf life - 5 years.
