Universal reference book for medicines
Product name: MAZEPTIL ® (MAJEPTIL)

Active substance: thioproperazine

Type: Antipsychotic drug (antipsychotic)

Manufacturer: Laboratoires AVENTIS (France) manufactured by FAMAR LYON (France)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

PHARMACHOLOGIC EFFECT
Antipsychotic agent (neuroleptic), piperazine derivative of phenothiazine.
Antipsychotic effect, apparently, is due to the blockade of postsynaptic dopamine receptors in the mesolimbic structures of the brain. Has a weak antiemetic effect, the central mechanism of which is associated with oppression or blockade of dopamine D 2receptors in the chemoreceptor trigger zone of the cerebellum, and peripheral with the blockade of the vagus nerve in the digestive tract. Has a weak alpha-adrenoblocking activity. Anticholinergic activity, sedative and hypotensive action are also weakly expressed. Has extrapyramidal effect.
PHARMACOKINETICS
Clinical data on the pharmacokinetics of thioproperazine are limited.

Phenothiazines have a high binding to plasma proteins.
They are mainly excreted by the kidneys and partly by bile.
INDICATIONS
Schizophrenia (especially gebefrenic and continuously flowing catatonic forms), chronic hallucinatory psychoses, manic syndrome, bouts of polymorphic delirium.

DOSING MODE
Install individually.
When administered orally, the initial dose is 5 mg / day, then the dose is gradually increased by 5 mg every 2-3 days. If necessary, the daily dose can reach 30-40 mg, in severe cases - up to 90 mg / day. With the / m introduction dose is 50% of the dose for oral administration.
SIDE EFFECT
From the side of the central nervous system: akinesia or hyperkinesia in combination with increased or normal muscle tone, apathy, anxious reactions, mood swings, dizziness;
with prolonged treatment, tardive dyskinesia is possible.
On the part of the digestive system: nausea, vomiting, diarrhea;
rarely - cholestatic jaundice.
On the part of the endocrine system: galactorrhea, gynecomastia, hyperprolactinaemia, impotence, frigidity, amenorrhea.

From the urinary system: rarely - oliguria.

From the cardiovascular system: rarely - violations of the heart rate.

On the part of the hematopoiesis system: in isolated cases - agranulocytosis.

On the part of metabolism: weight gain (possibly significant), increased sweating.

Dermatological reactions: pallor of the skin, photosensitivity.

Effects caused by anticholinergic action: dry mouth, constipation, accommodation disorders, urinary retention.

CONTRAINDICATIONS
Severe cardiovascular diseases, severe CNS depression, a history of toxic agranulocytosis, closed-angle glaucoma, prostate disease, parkinsonism, hypersensitivity to thioproperazine.

PREGNANCY AND LACTATION
Adequate and strictly controlled studies of the use of thioproperazine during pregnancy in humans have not been conducted.

There is no data on the release of thioproperazine with breast milk.
It should be borne in mind that phenothiazines penetrate into breast milk and can cause drowsiness in the child and increase the risk of developing dystonia and tardive dyskinesia. Considering this, if it is necessary to use thioproperazine during lactation, breastfeeding should be discontinued.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With special care apply phenothiazines for violations of liver function.

APPLICATION FOR CHILDREN
In children, especially with acute diseases, the use of phenothiazines is more likely to develop extrapyramidal reactions.
With special care apply phenothiazines for chronic respiratory diseases in children.
APPLICATION IN ELDERLY PATIENTS
Use with caution in elderly patients (due to increased risk of excessive sedation and hypotensive effect).

SPECIAL INSTRUCTIONS
They are used with caution in cases of hypersensitivity to other phenothiazine drugs, in elderly patients (due to an increased risk of excessive sedative and hypotensive action), in exhausted and weakened patients.

With special care apply phenothiazines with pathological changes in the blood picture, liver function disorders, alcohol intoxication, Reye's syndrome, as well as in breast cancer, cardiovascular diseases, predisposition to the development of glaucoma, Parkinson's disease, peptic ulcer and duodenal ulcer, urinary retention , chronic diseases of the respiratory system, epileptic seizures, vomiting.

During the treatment period, patients with epilepsy should be closely monitored, EEG should be performed, since thioproperazine lowers the threshold of convulsive readiness.
In the case of hyperthermia, which is one of the elements of the NSA, thioproperazine should be immediately discontinued.
During the treatment period, do not drink alcohol.

In children, especially with acute diseases, the use of phenothiazines is more likely to develop extrapyramidal reactions.
With special care apply phenothiazines for chronic respiratory diseases in children.
Impact on the ability to drive vehicles and manage mechanisms

If it is necessary to use in patients whose activity requires a high concentration of attention and speed of psychomotor reactions, it should be borne in mind that thioproperazine can cause drowsiness, especially at the beginning of treatment.

DRUG INTERACTION
When used simultaneously with drugs that exert a depressing effect on the central nervous system, with ethanol, ethanol-containing drugs, an increase in the oppressive effect on the central nervous system is possible.

With the simultaneous use of tricyclic antidepressants, maprotiline, MAO inhibitors, the risk of developing ZNS increases.

With simultaneous use with anticonvulsants, the threshold of convulsive readiness may be reduced;
with drugs for the treatment of hyperthyroidism - increases the risk of agranulocytosis; with agents that cause extrapyramidal reactions - it is possible to increase the frequency and severity of extrapyramidal disorders.
With simultaneous use with drugs that cause arterial hypotension, pronounced orthostatic hypotension is possible;
with anticholinergics - it is possible to increase their anticholinergic effects, while the antipsychotic effect of the antipsychotic may decrease.
With simultaneous use, it is possible to suppress the action of amphetamines, levodopa, clonidine, guanethidine, epinephrine.

With the simultaneous use of antacids, antiparkinsonian agents, lithium preparations disrupt the absorption of phenothiazines.

With simultaneous application, it is possible to weaken the vasoconstrictive effect of ephedrine.

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