Composition, form of production and packaging
Tablets from white to white with a slightly yellowish hue of color, flat-cylindrical shape, with a bevel.
1 tab.
haloperidol 1.5 mg
Auxiliary substances: potato starch, lactose (sugar milk), gelatin medical, talc, magnesium stearate.
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (4) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
100 pieces. - polymer cans (1) - packs of cardboard.
Tablets from white to white with a slightly yellowish hue of color, flat-cylindrical shape, with a facet and a risk.
1 tab.
haloperidol 5 mg
Auxiliary substances: potato starch, lactose (sugar milk), gelatin medical, talc, magnesium stearate.
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (4) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
100 pieces. - polymer cans (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
Haloperidol is a neuroleptic belonging to butyrofenone derivatives. Has a pronounced antipsychotic and antiemetic effect. Expressed antipsychotic activity is combined with a mild sedative effect (in small doses it has an activating effect).
The antipsychotic effect of haloperidol is associated with blockade of central dopamine (D 2) and a-adrenergic receptors in the mesocortical and limbic structures of the brain. Blockade of O2-receptors of the hypothalamus leads to a decrease in body temperature, galactorrhea (increased production of prolactin). Interaction with dopaminergic structures of the extrapyramidal system can lead to extrapyramidal disorders. The inhibition of dopamine receptors in the trigger zone of the vomiting center underlies the antiemetic effect.
Haloperidol enhances the effect of hypnotics, opioid analgesics, general anesthetics, analgesics and other drugs that depress the function of the central nervous system.
PHARMACOKINETICS
Haloperidol is absorbed, mainly in the small intestine, by passive diffusion. Bioavailability of 60-70%. When administered orally, the maximum concentration in the blood is reached after 3-6 hours. Haloperidol binds to plasma proteins by 90%.
The ratio of concentration in erythrocytes to plasma concentration is 1:12.
The concentration of haloperidol in the tissues is higher than in the blood.
Haloperidol is metabolized in the liver, the metabolite is not pharmacologically active.
Haloperidol is excreted by the kidneys (40%) and with feces (60%), it penetrates into breast milk.
T 1/2 from the plasma after oral administration is an average of 24 h (12-37 h).
INDICATIONS
The drug is used strictly according to the doctor's prescription.
- 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 resistant to therapy hiccups and vomiting, incl. associated with antitumor therapy;
- Premedication before surgery.
DOSING MODE
Assign inside, half an hour before meals (you can with milk to reduce the irritating effect on the mucous membrane of the stomach).
The initial daily dose is 0.5-5 mg divided into 2-3 doses. Then the dose is gradually increased by 0.5-2 mg (in resistant cases by 2-4 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, in resistant cases to 50-60 mg / day. The duration of treatment, on average, 2-3 months. Supporting doses (outside the exacerbation) from 0.5 to 5 mg / day (the dose is reduced gradually).
Children 3-12 years old (with a body weight of 15-40 kg) - 0.025-0.05 mg / kg body weight / day in 2-3 divided doses, increasing the dose no more often than every 5-7 days, to a daily dose of 0.15 mg / kg .
The elderly patients and the weakened patients are prescribed 1 / 3-1 / 2 of the usual dose for adults, with its increase not more often than every 2-3 days.
As an antiemetic, 1.5 mg is prescribed.
For more accurate dosing, another dosage form of the drug, for example, drops for oral administration, may be required.
SIDE EFFECT
From the side of the nervous system: extrapyramidal disorders of varying severity, parkinsonism, transient akineto-rigid syndrome, oculogic crises, headache, dizziness, insomnia or drowsiness (varying degrees of severity), anxiety, anxiety, psychomotor agitation, fear, akathisia, euphoria, depression, epileptic seizures, in rare cases, exacerbation of psychosis, incl. hallucinations; 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, tachycardia, changes in the ECG (prolongation of the QT interval, signs of flutter and fibrillation of the ventricles).
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.
From the hematopoiesis: rarely - temporary leukopenia or leukocytosis, agranulocytosis, erythropenia and a tendency to monocytosis.
On the part of the genitourinary system: urinary retention (with prostatic hyperplasia), peripheral edema, pain in the mammary glands, gynecomastia, hyperprolactinaemia, menstrual cycle disorder, decreased potency, increased libido, priapism.
From the sense organs: cataract, retinopathy, blurred vision.
Allergic reactions: maculopapular and acne-like skin changes, photosensitivity, rarely - bronchospasm, laryngospasm.
From the skin: hyperfunction of the sebaceous glands.
Laboratory indicators: hyponatremia, hyper- or hypoglycemia, increased activity of hepatic transaminases.
Other: alopecia, weight gain.
CONTRAINDICATIONS
- severe toxic oppression of the central nervous system caused by xenobiotics, coma of various origins;
- CNS diseases, accompanied by pyramidal and extrapyramidal disorders (Parkinson's disease, etc.);
- pregnancy, the period of breastfeeding;
- Children's age up to 3 years.
- Hypersensitivity to derivatives of butyrophenone.
Due to the presence of lactose (milk sugar) in the formulation, its administration is contraindicated in cases of congenital lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
With caution: should take haloperidol in decompensated cardiovascular diseases (including angina pectoris, intracardiac conduction disorders, prolongation of the QT interval or predisposition to it - hypokalemia, simultaneous use of other drugs that can cause prolongation of the QT interval); with severe diseases of the kidneys, liver, pulmonary heart disease (including bronchial asthma and acute infections), epilepsy, zakratougolnoy glaucoma, hyperthyroidism (thyrotoxicosis), prostatic hyperplasia (urinary retention), active alcoholism.
SPECIAL INSTRUCTIONS
During therapy, patients should regularly monitor the ECG, the blood formula, "liver" tests.
The severity of extrapyramidal disorders is associated with a dose, often with a decrease in dose, they may decrease or disappear.
With the development of tardive dyskinesia, it is recommended that the dose be gradually reduced (until the drug is completely discontinued).
Care must be taken when performing heavy physical work, taking a hot bath (it is possible to develop a heat stroke due to the suppression of central and peripheral thermoregulation in the hypothalamus).
During treatment, do not take "cold" non-prescription drugs (possibly increasing the anticholinergic effects and the risk of heat stroke).
Protect open areas of the skin from excessive sunlight due to the increased risk of photosensitivity.
Treatment is stopped gradually to avoid the occurrence of the "withdrawal" syndrome.
An antiemetic effect can mask the signs of drug toxicity and make it difficult to diagnose conditions, the first symptom of which is nausea.
It was noted that doses for children 6 mg / day cause additional improvement in behavioral disorders and tics.
During the reception of haloperidol it is forbidden to drive vehicles, service mechanisms and other types of work that require increased concentration of attention, as well as alcohol intake.
OVERDOSE
Symptoms: with an overdose of the drug, the appearance of acute neuroleptic reactions, listed above, is possible. 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: gastric lavage, activated charcoal. With respiratory depression - artificial ventilation. To improve blood circulation in / in injected plasma or albumin solution, norepinephrine. In these cases, epinephrine is strictly forbidden! Reduction of extrapyramidal symptoms of central holinoblokatory and antiparkinsonian drugs. Dialysis is ineffective.
DRUG INTERACTION
Haloperidol increases the severity of oppressive effects on the CNS of opioid analgesics, hypnotics, tricyclic antidepressants, agents for general anesthesia, alcohol.
With the simultaneous use with antiparkinsonian drugs (levodopa, etc.), the therapeutic effect of these drugs may decrease because of the antagonistic effect on the dopaminergic structures.
When used with methyldopa, development of disorientation, difficulty and slowing down of thinking processes is possible.
Haloperidol can reduce the intensity of action of epinephrine (epinephrine) and other sympathomimetics, cause a paradoxical reduction in blood pressure and tachycardia when they are used together.
Strengthens the action of peripheral m-holinoblokatorov and most antihypertensives (reduces the effect of guanetidine due to its displacement from a-adrenergic neurons and suppression of its capture by these neurons).
When combined with anticonvulsants (including barbiturates and other inducers of microsomal oxidation), the doses of the latter should be increased, haloperidol reduces the threshold of convulsive activity; serum concentrations of haloperidol may also decrease.
Haloperidol can reduce the effect of indirect anticoagulants, so when combined, the dose of the latter should be adjusted.
Haloperidol slows the metabolism of tricyclic antidepressants and MAO inhibitors, which increases their plasma levels and increases toxicity.
With simultaneous use with bupropion 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 increases, especially extrapyramidal reactions.
With the simultaneous administration of haloperidol with lithium, especially in high doses, it can cause irreversible neurointoxication, as well as intensify extrapyramidal symptoms.
With simultaneous reception with amphetamines, the antipsychotic effect of haloperidol and the psychostimulant effect of amphetamines are reduced, due to the blockade of haloperidol a-adrenergic receptors.
Haloperidol can reduce the effect of bromocriptine.
Anticholinergic, antihistamine (1st generation) and antiparkinsonian drugs can enhance the m-cholinoblock effect of haloperidol and reduce its antipsychotic effect (dose adjustment may be required).
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
List B. Keep out of reach of children, dry, protected from light at a temperature of no higher than 25 В° C. Shelf life - 3 years.
