Composition, form of production and packaging
The solution for intravenous and / or injection is clear, colorless.
1 ml
haloperidol 5 mg
Auxiliary substances: lactic acid 90% for injection forms, water d / u.
1 ml - dark glass ampoules (10) - packings, cellular outline (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2012.
PHARMACHOLOGIC EFFECT
Haloperidol is a neuroleptic belonging to butyrofenone derivatives. Has a pronounced antipsychotic and antiemetic effect.
The effect of haloperidol is associated with blockade of central dopamine (D2) and alpha-adrenergic receptors in the mesocortical and limbic structures of the brain.Blockade of D2-receptors of the hypothalamus leads to a decrease in body temperature, galactorrhea (increased production of prolactin). The 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. Expressed antipsychotic activity is combined with a mild sedative effect (in small doses it has an activating effect). Strengthens the action of hypnotics, narcotic analgesics, means for general anesthesia, 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 90% binds to plasma proteins. The ratio of concentration in erythrocytes to the concentration in the plasma 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. The plasma half-life after oral administration is, on average, 24 hours (12-37 hours).
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 resistant to therapy hiccups and vomiting, including those associated with antitumor therapy;
- Premedication before surgery.
The drug is used strictly according to the doctor's prescription!
DOSING MODE
To stop psychomotor excitement Haloperidol in the early days are prescribed intramuscularly 2-5 mg 2-3 times a day, or intravenously in the same dosage (the ampoule should be diluted in 10-15 ml of water for injection), the maximum daily dose of 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 per day, divided by 2 doses. The maximum daily dose is 0.15 mg / kg.
The parenteral route of administration of Haloperidol should be performed under the close supervision of the physician, especially in elderly patients and children , when the therapeutic effect is achieved, the preparation should be taken orally.
SIDE EFFECT
From the side of the central nervous system: extrapyramidal disorders of varying severity, parkinsonism. Most patients have transient akineto-rigid syndrome, oculogic crises, akathisia, dystonic phenomena.
Perhaps the development of neuroleptic malignant syndrome, one of the first signs of which is an increase in body temperature, drowsiness. With long-term administration of haloperidol, it is possible to develop late dyskinesias, especially in elderly patients and patients with organic deficiency of the central nervous system, so doses for this category of patients should be reduced.
At the beginning of therapy, there may be lethargy, drowsiness or insomnia, headaches that occur after the appointment of correctors.
From the cardiovascular system: arrhythmias, tachycardia, orthostatic hypotension, lability of blood pressure, changes in the ECG.
On the part of the hematopoiesis system: transient leukopenia or leukocytosis, erythropenia, lymphomonocytosis, rarely - agranulocytosis.
From the liver: increased activity of "liver" transaminases, jaundice.
Dermatological reactions: allergic reactions, rash, toxicodermia, dry skin, photosensitivity, hyperfunction of the sebaceous glands.
On the part of the digestive system: anorexia, dyspepsia, dry mouth, sometimes giller salivation, nausea, vomiting, constipation, diarrhea.
On the part of the endocrine system: dysmenorrhea, frigidity, gynecomastia, galactorrhea, impotence, priapism, weight gain.
Other: urinary retention, blurred vision, increased fatigue, decreased thirst, heat stroke, alopecia, hyponatremia, hyper- or hypoglycemia.
CONTRAINDICATIONS
- severe toxic oppression of the central nervous system caused by xenobiotics, coma of different genesis;
- extrapyramidal disorders (Parkinson's disease, etc.);
- hypersensitivity to butyrofenone derivatives;
- pregnancy, the period of breastfeeding;
- Children's age up to 3 years.
With caution: decompensated cardiovascular diseases (including angina pectoris), impaired conduction of the heart muscle; severe diseases of the kidneys, liver, pulmonary heart disease (including bronchial asthma and acute infections), epilepsy, zakratougolnaya glaucoma, hyperthyroidism (thyrotoxicosis), prostatic hyperplasia (urinary retention), active alcoholism.
PREGNANCY AND LACTATION
Contraindicated in pregnancy, during breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution: severe kidney disease.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution: severe liver disease.
APPLICATION FOR CHILDREN
Contraindicated in childhood up to 3 years.
The parenteral route of administration of haloperidol in children should be carried out under the careful supervision of a physician, when the therapeutic effect is achieved, it is necessary to switch to taking the drug inside.
APPLICATION IN ELDERLY PATIENTS
The parenteral route of administration of haloperidol in elderly patients should be carried out under the careful supervision of a physician, when the therapeutic effect is achieved, the preparation should be taken orally.
SPECIAL INSTRUCTIONS
During treatment, patients should regularly monitor ECG, blood formulas, hepatic samples.
For relief of extrapyramidal disorders, antiparkinsonic agents (cyclodol., Etc.), nootropics, vitamins are prescribed.
The severity of extrapyramidal disorders is associated with a dose, often with a decrease in dose, they may decrease or disappear.
In some cases, signs of neurological disorders are observed when the drug is withdrawn after a long course of treatment, so haloperidol should be canceled gradually by lowering the dose.
With the development of tardive dyskinesia should not abruptly cancel the drug; a gradual dose reduction is recommended.
Protect open areas of the skin from excessive sunlight due to the increased risk of photosensitivity.
The antiemetic effect of haloperidol can mask the signs of drug toxicity and make it difficult to diagnose conditions, the first symptom of which is nausea.
Impact on the ability to drive vehicles and manage mechanisms
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 taking alcohol
OVERDOSE
In case of 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: discontinuation of therapy with neuroleptics, appointment of correctors (intravenous diazepam, glucose solution, nootropics, B and C vitamins, symptomatic therapy).
DRUG INTERACTION
Haloperidol increases the severity of oppressive effects on the CNS of opioid analgesics, hypnotics, tricyclic antidepressants, agents for general anesthesia, alcohol.
When used simultaneously 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 arterial pressure and tachycardia when combined.
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).
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. In particular, with the simultaneous use of tea or coffee, the effect of haloperidol may 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 psychostimulatory effect of amphetamines are reduced, due to the blockade of haloperidol-adrenergic receptors. Haloperidol may reduce the effect of bromocriptine
Anticholinergic, antihistamine (anxiety), antidiskinetic drugs can enhance anticholinergic side effects and reduce the antipsychotic effect of haloperidol.
TERMS OF RELEASE FROM PHARMACY
According to doctor's prescription.
TERMS AND CONDITIONS OF STORAGE
Store in a dark place at a temperature of no higher than 25 В° C. List B.
Shelf life - 5 years.
