Universal reference book for medicines
Product name: SENORM (SENORM)

Active substance: haloperidol decanoate

Type: Antipsychotic drug (antipsychotic)

Manufacturer: Sun Pharmaceutical Industries (India)
Composition, form of production and packaging
Solution for the / m introduction of oily
transparent, viscous, from colorless to light yellow color.

1 ml

haloperidol decanoate 50 mg

[PRING] benzyl alcohol, sesame oil.

1 ml - ampoules of dark glass (5) - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

Haloperidol decanoate is antipsychotic.
drug prolonged action. After the / m introduction of the ester of haloperidol decanoate by hydrolysis, a gradual release of the active ingredient, the neuroleptic haloperidol, occurs. The drug for chemical structure refers to derivatives of butyrofenone, has a central antidopaminergic effect and is a highly effective neuroleptic. It blocks postsynaptic dopamine receptors in the mesolimbic and mesocortical structures of the brain. It inhibits the release of mediators, reducing the permeability of presynaggic membranes, violates the reverse neuronal capture and deposition. High antipsychotic activity is combined with a moderate sedative effect (in small doses has an activating effect) and pronounced antiemetic effect. Causes extrapyramidal disorders, virtually no cholinoblocking effect.
Sedative action is not expressed, due to blockade of β-adrenoreceptors of the reticular formation of the brainstem;
antiemetic effect - blockade of dopamine D2 receptors in the trigger zone of the vomiting center; hypothermic action and galactorrhea - blockade of dopamine receptors of the hypothalamus. Prolonged reception is accompanied by a change in the endocrine status, in the anterior pituitary gland prolactin production increases and decreases - gonadotropic hormones.
Effective in patients resistant to other neuroleptic drugs.
Has some activating effect. In hyperactive children, eliminates excessive motor activity, behavioral disorders (impulsivity, difficulty concentrating, aggressiveness). The therapeutic effect can last up to 6 weeks.
PHARMACOKINETICS

Haloperidol 92% binds to blood plasma proteins.
After the / m administration, the absorption is slow and constant (due to release from the depot), the C max of active haloperidol is reached in the serum by 3-9 days (in elderly patients - 1 day) and then decreases. T 1/2 is 3 weeks. Equilibrium plasma concentration is achieved after 2-4 injections (monthly administration) and is 4-20 mg / ml (10.6-53.2 μmol / L). Easily passes through the histohematological barriers, including the BBB. Penetrates into breast milk. The pharmacokinetics of haloperidol decanoate after IM is dose dependent. Between the administration of the drug in a dose of less than 450 mg and achieved at this concentration of haloperidol in the blood plasma revealed a linear relationship. Isolation from the body occurs in the form of metabolites, 60% with feces, 40% with urine.
INDICATIONS

- supportive therapy of chronic forms of schizophrenia in cases when short-acting haloperidol used earlier had a good therapeutic effect;
especially if there is a need for the use of a potent neuroleptic with a mild sedative effect.
DOSING MODE

Only in / m injections are allowed;
in / in not to enter! A single monthly dose of the drug is recommended to be injected deep into the gluteal muscles. The transition to the use of long-acting drugs is appropriate in cases where the patient constantly takes an oral antipsychotic drug (usually haloperidol). Calculation of the dose of a long-acting drug is carried out using the oral dose of haloperidol or another neuroleptic.
Initially, every 10 to 10 times a single dose of the oral preparation should be administered every 4 weeks, which is usually 25-75 mg (0.5-1.5 ml) of haloperidol decanoate.
The initial dose should not exceed 100 mg of haloperidol decanoate.
Further, depending on the therapeutic response, the dose of the drug can be increased gradually by 50 mg, until the optimal effect is achieved.

The usual maintenance dose, administered every 4 weeks, is 20 times the one-day oral dose of haloperidol.

Depending on the therapeutic response of the patient to haloperidol decanoate, with the repeated increase in the symptoms of the disease, additional use of haloperidol is possible orally.
Doses are set individually depending on the patient's condition. It may be necessary to temporarily interrupt treatment or more frequent than once in 4 weeks, the introduction of the drug. It is undesirable to inject more than 3 ml of the drug in one injection because of the risk of discomfort in the patient.
In elderly and debilitated patients, lower initial doses should be used - 12.5-25 mg once every 4 weeks.
In the future, depending on the patient's condition, the dose of the drug can be increased (the interval between doses and dosage is adjusted with a periodicity of at least 1 month).
SIDE EFFECT

Adverse events after the administration of haloperidol decanoate are the same, which can occur with the use of other dosage forms of haloperidol.

Extrapyramidal symptoms: with prolonged use may occur tremor, rigidity of muscles, bradykinesia, - akathisia, acute muscular dystopia, oculogic crisis, laryngeal dystonia (spastic dysphonia).
Correction: antiparkinsonian preparations of m-cholinoblocking action should be prescribed. However, it must be borne in mind that their constant use reduces the effectiveness of haloperidol.
Late dyskinesia: as with other antipsychotics, may occur with prolonged use or withdrawal of the drug.
It is manifested by rhythmic movements of muscles of the face, lips, tongue or jaw area that can not be controlled by volitional control. This disorder in some patients may have the nature of residual events. Disorders cease with the resumption of haloperidol, with increasing doses or when switching to treatment with another drug. When signs of late dyskinesia, it is advisable to continue treatment with another drug.
Malignant neuroleptic syndrome (CNS): the use of haloperidol can cause CNS.
A rare reaction that arises as a type of idiosyncrasy is characterized by hyperthermia, generalized rigidity of the muscles, vegetative lability, difficulty breathing or rapid breathing, arrhythmias, increased or decreased blood pressure, increased sweating, urinary incontinence, epileptic seizures, and impaired consciousness. The early sign of the NSA is often hyperthermia. When symptoms of NSA appear in all cases, it is necessary to interrupt treatment with antipsychotic. drugs and, in conditions of careful observation, to start supporting, including detoxification, therapy.
Other side effects on the part of the CNC: depression, inhibition (up to a state similar to lethargy) or psychomotor, agitation, insomnia or drowsiness (especially at the beginning of treatment), headache, transient mexico-intellectual disorders, dizziness, motor anxiety, anxiety , fear, or euphoria, - epileptic seizures like "grand mal" and the resumption of psychotic symptoms (the development of a paradoxical reaction).

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 endocrine system: due to the antidopamin effect, hyperprolactinaemia, galactorrhea, gynecomastia, oligo- and amenorrhea, hyper- or hypoglycemia, and a decrease in the secretion of antidiuretic hormone can be observed.

From the side of the cardiovascular system: when used in high doses, a decrease in blood pressure, orthostatic

hypotension, arrhythmias, tachycardia, changes in the ECG (prolongation of the QT interval).

On the part of the hematopoiesis: transient leukopenia or leukocytosis, agranulocytosis, erythropenia and a tendency to monocytosis.

Allergic reactions: urticaria, anaphylaxis, photosensitization, maculopapular and acneiform changes in the skin, bronchospasm, laryngospasm, hyperpyrexia.

On the part of the genitourinary system: urinary retention (with prostatic hyperplasia), peripheral edema, decreased potency, increased libido, priapism.

Laboratory indicators: hyponatremia.

Other: alopecia, heat stroke, weight gain, local reactions, cataract, retinopathy, blurred vision.
Elderly patients may experience seizures of angle-closure glaucoma.
CONTRAINDICATIONS

- oppression of the CNS activity of toxic (alcoholic or medicamentous) genesis in severe form;

- coma of different genesis;

- CNS diseases, accompanied by pyramidal or extrapyramidal symptoms (including Parkinson's disease);

- Depression;

- hysteria;

- Pregnancy;

- lactation period;

- childhood;

- pathological process with localization in the basal nucleus region;

- previously noted increased sensitivity to the components of the drug.

With care: diseases of the cardiovascular system in the stage of decompensation, epilepsy, zakratougolnaya glaucoma, hepatic and / or renal failure, thyrotoxicosis (with the phenomena of thyrotoxicosis), pulmonary-cardiac and respiratory failure (including chronic obstructive pulmonary disease and acute infectious diseases), prostatic hyperplasia with a delay in urine, alcoholism.

PREGNANCY AND LACTATION

Observation results.
for a large number of patients showed that haloperidol does not reliably increase the number of congenital pathologies. In some cases, congenital anomalies are described against the background of haloperidol during pregnancy, usually in combination with other drugs. Thus, the use of haloperidol decanoate during pregnancy is contraindicated.
Haloperidol penetrates into the mother's milk.
In some cases, extrapyramidal disorders have been noted in newborns whose mother has taken haloperidol. Therefore, breastfeeding should stop breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER

Carefully.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Carefully.

APPLICATION FOR CHILDREN

Contraindicated.

APPLICATION IN ELDERLY PATIENTS

In elderly patients , lower initial doses should be used - 12.5-25 mg once every 4 weeks.
In the future, depending on the patient's condition, the dose of the drug can be increased (the interval between doses and dosage is adjusted with a periodicity of at least 1 month).
SPECIAL INSTRUCTIONS

There are cases of observation of sudden death of patients taking antipsychotic drugs, in particular haloperidol.
Since in the treatment of haloperidol in a number of patients there was an increase in the QT interval on the ECG, the drug should be used with caution in patients who are at risk of prolonging the QT interval (hypokalemia, concomitant use of other drugs that may cause prolongation of the QT interval). If it is necessary to use haloperidol decanoate, first haloperidol should be administered orally, to determine the possible unexpected increased sensitivity.
Due to the fact that haloperidol is metabolized in the liver, caution is needed in the use of haloperidol in severe hepatic pathology.
With prolonged use, periodic monitoring of the blood picture and liver function is necessary.
In some cases, the development of the phenomena of convulsive syndrome is described against the background of the use of haloperidol.
Therefore, patients with epilepsy, as well as those patients who have increased convulsive readiness (chronic intoxication, both alcoholic and other genesis, traumatic brain injury, etc.), haloperidol decanoate should be administered with caution.
Thyroxine increases the toxicity of haloperidol, therefore haloperidol in patients with hyperthyroidism is only applicable under the cover of adequate thyreostatic therapy.

Patients who have a history of depressive syndrome in the picture of psychopathological disorders, haloperidol should be administered in combination with antidepressants.
If there is a need for simultaneous administration of antiparkinsonian therapy to a patient, then after administration of the last dose of haloperidol decanoate, the treatment with these drugs should be continued for some time, since. removal from the body of an antiparkinsonian drug occurs faster than haloperidol decanoate - a drug of prolonged action.
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 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.

Treatment is stopped gradually to avoid the occurrence of 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.

Before the appointment of a prolonged form, you should first transfer the patient from any other neuroleptic to haloperidol (prevention of unexpected hypersensitivity to haloperidol).

Impact on the ability to drive vehicles and manage mechanisms

In the initial period of treatment, you can not drive a car or work in conditions of increased risk of injury.
Subsequently, the degree of restrictions is determined on an individual basis. During the use of the drug, you should not drink alcohol.
OVERDOSE

Symptoms of an overdose of haloperidol decanoate are similar to those observed with other haloperidol dosage forms.

If suspicion of an overdose of haloperidol decanoate should take into account the prolonged nature of the drug.

The most important signs of an overdose: severe extrapyramidal disorders (muscle stiffness, muscle hypertonicity, general or localized tremor is possible), arterial hypo-, sometimes hypertension, a state of severe inhibition.

In severe cases, a comatose state may occur, with respiratory depression on the background of severe arterial hypotension.
It is necessary to take into account the possibility of developing ventricular arrhythmias with an extension of the QT interval.
Treatment: there is no specific antidote.
Symptomatic therapy: when comatose, support for the function of the respiratory system is necessary, if necessary, connect to the apparatus of artificial ventilation. It is necessary to monitor the ECG and other vital functions of the body. To treat severe arterial hypotension or circulatory insufficiency, an adequate volume of fluid, blood plasma or a concentrated albumin solution, as well as the appointment of vasopressor drugs (norepinephrine or dopamine) should be administered. In these cases, epinephrine is strictly forbidden! In combination with haloperidol, it can cause severe arterial hypotension). In case of severe extrapyramidal symptoms, it is necessary to use parenterally anti-Parkinsonics and central holinoblokatory. Hemodialysis is ineffective.
DRUG INTERACTION

The drug is able to enhance the effect of drugs that depress the central nervous system - alcohol, sedatives and hypnotics, as well as narcotic analgesics.
The simultaneous administration of haloperidol with these drugs can lead to respiratory depression. In combination with methyldopa enhances the effect of the latter on the central nervous system, increases the risk of developing mental disorders (including disorientation in space, slowing down and obstructing thinking processes).
Reduces the antiparkinsonian effect of levodopa and other anticonvulsants (reduction of convulsive threshold with haloperidol).

Haloperidol inhibits the metabolism of tricyclic antideprasal sites and monoamine oxidase inhibitors, so their concentration may increase.
in blood plasma, with increasing m-holinoblokiruyuschey action, as well as toxicity, including. in relation to the cardiovascular system.
Pharmacokinetic studies revealed an increase in moderate or moderate severity, the level of haloperidol in the blood serum, when combined with haloperidol, the following drugs;
quinidine, buspirone, fluoxetine. If they need to be combined, a dose reduction of haloperidol may be required.
With prolonged use of drugs that have the properties of inducers of microsomal liver enzymes (carbamazepine, rifampicin, phenobarbital, etc.), the concentration of haloperidol in the blood decreases.
Therefore, if necessary, their combined use may require an increase in the dose of haloperidol. In the case of subsequent withdrawal of therapy with these drugs should be borne in mind the advisability of reducing the dose of haloperidol.
In rare cases, with the combined use of haloperidol and lithium salts, the following disorders were observed: the phenomena of encephalopathy, extrapyramidal symptoms, tardive dyskinesia, malignant neuroleptic syndrome, brain stem symptomatology, coma.
In most cases, these disorders are reversible. The reason for their manifestation in this situation is unclear. When the manifestation of these disorders should immediately cease the use of haloperidol.
Haloperidol change (may increase or decrease) the effect of anticoagulants.
Haloperidol reduces the effectiveness of the group of antihypertensives blockers.
, Decreases the vasoconstrictor action of dopamine, phenylephrine, norepinephrine, epinephrine and ephedrine (alpha-adrenergic blockade by haloperidol, can lead to distortion of the action of epinephrine and a paradoxical decrease in blood pressure).
It enhances the action of m-peripheral anticholinergics and most antihypertensives (guanethidine reduces the effect due to the displacement of its alpha-adrenergic neuron and suppression of its capture these neurons).
Lets diazoxide inhibition of insulin release. In an application with bupropion reduces the seizure threshold, and increases the risk of large seizures.
Decreases antiparkinsonian effect (antagonistic effect on CNS dopaminergic structure).
It reduces the effect of bromocriptine (may require dose correction).
Amphetamines reduce antipsychotic effect of haloperidol, which, in turn, reduces their inducing effect (haloperidol blockade of alpha-adrenoceptors).
M-anticholinergic, antihistaminic (I generation) and means antidiskineticheskie agents: m-may enhance anticholinergic effect of haloperidol and reduce its antipsychotic effects (may require dose correction).
While the use of drugs that cause extrapyramidal reactions, increases the incidence and severity estrapiramidnyh 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

Store in a dry place, protected from light, out of reach of children, at a temperature not exceeding 25 ° C.
Shelf life - 2 years.
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