Haloperidol-Richter - instructions for use, dose, side effects, contraindications

Excipients: starch potato 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.

Description:White or almost white, flat disk-like tablets, without labeling, practically odorless.

Pharmacotherapeutic group:Antipsychotic (antipsychotic) remedy.

ATX: & nbsp

N.05.A.D.01 Haloperidol

Pharmacodynamics:

Haloperidol is a pronounced antagonist of central dopamine receptors and refers to strong antipsychotics. Does not have antihistaminergic or anticholinergic activity. Haloperidol is highly effective in the treatment of hallucinations and delusions, thanks to direct blockade of central dopamine receptors

(acts, probably on the mesocortical and limbic structures), affects the basal ganglia (nigrostrial bundle). Has a pronounced soothing effect in psychomotor agitation, is effective in mania and other agitations.

The limbic activity of haloperidol is manifested in a sedative effect, is effective as an additional agent in the treatment of chronic pain.Exposure to the basal ganglia causes extrapyramidal reactions (dystonia, akathisia, parkinsonism). Pronounced peripheral

antidopaminergic activity forms the basis of antiemetic action (stimulation of the chemoreceptors in the trigger zone), relaxation of gastrointestinal sphincters and increased release of prolactin (blocks the prolactin-inhibiting factor at the level of the adenohypophysis).

Pharmacokinetics:Absorbed by passive diffusion, in a non-ionized form, mainly from the small intestine. Bioavailability: 60-70%. When administered orally, the maximum concentration in the blood is reached after 2-6 hours, with intramuscular - in 20 minutes. The therapeutic effect occurs at a plasma concentration of 4-20-25 mg / l. The volume of distribution is large, 7.9 +/- 2.5 l / kg, communication with blood proteins - 92%. Easily penetrates through gistogematicheskie barriers, including blood-brain,

Metabolized in the liver, has the effect of "first pass" through the liver. The isozymes CYP3A3, CYP3A5, CYP3A7 take part in the metabolism of the drug. It is an inhibitor of CYP2D6. There are no active metabolites. The half-life from plasma (T1 / 2) after oral administration is 24 h (12-37 h). It is excreted in the form of metabolites with fecal masses - 60% (incl.with bile - 15%), with urine - 40%, (including 1% - unchanged). Penetrates into breast milk.

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 persistent therapy of vomiting, including those associated with antitumor therapy, hiccups.

Contraindications:

hypersensitivity to the components of the drug;

- severe oppression of the central nervous system, against xenobiotic intoxication, coma of various genesis;

- diseases of the central nervous system, accompanied by pyramidal or extrapyramidal symptoms (including Parkinson's disease);

- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

- pregnancy, lactation period;

- Children weighing up to 60 kg.

Carefully:

Decompensated cardiovascular diseases (including angina pectoris), intracardiac conduction disorders,prolongation of the QT interval on an electrocardiogram (ECG) or a predisposition to it - hypokalemia, simultaneous use of other drugs that may cause prolongation of the QT interval, epilepsy, angle-closure glaucoma, hepatic and / or renal failure, hyperthyroidism (with thyrotoxicosis phenomena), pulmonary-cardiac and respiratory failure (including COPD and acute infectious diseases), prostatic hyperplasia with a delay in urine, alcoholism.

Pregnancy and lactation: Haloperidol-Richter contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside during or after a meal, with a full (240 ml) glass of water or milk.

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 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.

Adults:

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 to 5 mg), until the required therapeutic effect is reached (on average - up to 10-15 mg / day, for chronic forms of schizophrenia 20-40 mg / day, in If necessary, the dose can be increased to 50-60 mg / day.) The maximum daily dose: 100 mg. Duration of treatment - 2-3 months. Reduce the dose slowly, maintenance doses (outside the exacerbation): from 0.5-0.75 mg to 5 mg / day.

Acute and chronic psychosis

In acute psychoses, a single dose of 1.5-5 mg (up to 10 mg), in tablets, usually every 4 to 8 hours. At oral intake not more than 100 mg per day. Supportive therapy: from 0.5 mg to 20 mg per day orally. A minimum dose is used that can support remission.

Nonpsychotic behavior disorders, Gilles de la Tourette's syndrome -

0,05 mg / kg / day in 2-3 divided doses, then the dose is gradually increased 1 time 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.

Tiki, Goettington's chorea - Inside, 0.025-0.05 mg / kg / day.

If there is no effect within one month, treatment should not be continued.

Long-lasting and resistant to therapy vomiting

With "indomitable" vomiting - 1,5-2 mg 2 times a day.

Elderly and weakened patients prescribe 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 doses; if necessary, taking into account the tolerability dose is gradually increased 1 time every 5-7 days to a total dose of 0.015 mg / kg / day.

Side effects:

From the nervous system: ego 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 puffing, 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 curved movements of the neck, trunk, arms and legs) and malignant neuroleptic syndrome (hyperthermia, muscle rigidity, difficulty or rapid breathing, tachycardia, arrhythmia, increased or decreased arterial tension (AD), increased 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).

From 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 organs of blood and blood: temporary leukopenia or leukocytosis, agranulocytosis, erythropenia and a tendency to monocytosis.

From the genitourinary system: retention of urine (with hyperplasia of the prostate gland), peripheral edema, pain in the mammary glands, gynecomastia, hyperprolactinaemia, violation of the menstrual cycle, decreased potency, increased libido, priapism.

From the sense organs: cataract, retinopathy, blurred vision.

Allergic reactions: maculopapular and acne-like skin changes, photosensitivity, bronchospasm, laryngospasm.

Laboratory indicators: hyponatremia, hyper- or hypoglycemia.

Other: alopecia, weight gain.

Overdose:

In case of an overdose of the drug, the appearance of acute neuroleptic reactions, listed above, is possible.

Symptoms:

muscle rigidity, tremor, drowsiness, decrease, sometimes an increase in blood pressure, in severe cases - coma, respiratory depression, shock, QT interval prolongation on the ECG, artium.

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:

when ingested - gastric lavage, Activated carbon.

If breathing is depressed, artificial ventilation may be required. With hypotension and collapse - intravenously, to maintain circulation, plasma or concentrated albumin, dopamine, or norepinephrine as an invoker. Epinephrine in these cases it is strictly forbidden to apply, as it can provoke a pronounced hypotension! For relief of extrapyramidal symptoms, central m-holinoblokatory and antiparkinsonian drugs. Intravenously injected diazepam, a solution of destroses, nootropics, vitamins of group B and C. Dialysis is ineffective. There is no specific antidote.

Interaction:

Increases the severity of the inhibitory effect on the central nervous system (CNS) of ethanol, tricyclic antidepressants, narcotic analgesics, barbiturates and hypnotic drugs, funds for general anesthesia.

Strengthens the action of peripheral m-holinoblokatorov and most hypotensive sidstv (reduces the effect of guanetidine due to its displacement from alpha-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 alpha-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, deceleration and and difficulty -

processes of thinking). Amphetamines reduce antipsychotic effect of haloperidol, which, in turn, reduces their inducing effect (haloperidol blockade of alpha-adrenoceptors).

M-holinoblokatory, blockers of H1-histamine receptors of the first 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

microsomal liver enzymes reduces the concentration of haloperidol in plasma.

In combination with lithium preparations (especially in high doses), it is possible to develop encephalopathies (may cause irreversible neurointoxication) and enhance 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.

Special instructions:

Because the haloperidol may cause prolongation of the QT interval, caution should be exercised if there is a risk of prolongation of QT (QT syndrome, hypokalemia, drugs causing prolongation of the RT interval), especially with parenteral administration.

In connection with the metabolism of haloperidol in the liver, it is important to exercise caution when prescribing it to patients with impaired hepatic function.

During treatment, patients should regularly monitor ECG, blood formulas, "liver" samples.

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 used with extreme caution.

For relief of extrapyramidal disorders, antiparkinsonian agents are prescribed (cyclodol, etc.), nootropics; vitamins; Their application is continued after haloperidol withdrawal, if they

are excreted faster than haloperidol to avoid extrapyramidal symptoms. 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 doing heavy physical work, taking a hot bath (possibly developing a heat stroke due to the suppression of central and peripheral thermoregulation in the hypothalamus).

During treatment, do not take anti-cold non-prescription drugs (possibly increasing the m-cholinergic effects of 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.

During drug treatment, alcohol consumption is not recommended.

Effect on the ability to drive transp. cf. and fur:During the reception of the drug is prohibited to drive vehicles and engage in other activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, 5 mg.

Packaging:For 25 tablets in a blister of Al / PVC, 2 blisters with instructions for use in a cardboard box.

Storage conditions:At a temperature of 15 to 30 ° C

Keep out of the reach of children!

Shelf life:5 years. Do not use the product after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011975 / 01

Date of registration:09.08.2011

The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary

Manufacturer: & nbsp

Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary

Information update date: & nbsp09.08.2011

Illustrated instructions

Instructions

Haloperidol-Richter (Haloperidol-Richter)