Serdolekt

• Structure
• Release form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications to use
• Contraindications
• Side effects
• Serdolekt, application instruction (Way and dosage)
• Overdose
• Interaction
• Terms of sale
• Storage conditions
• Period of validity
• Analogs
• Responses

Structure

In 1 tablet of a sertindol of 4, 12, 16 or 20 mg. Starch corn, MKTs, lactoses monohydrate, magnesium stearate, hypro rod, sodium of a kroskarmelloz, as auxiliary components.

Release form

Tablets in a cover of 4, 12, 16 and 20 mg.

Pharmacological action

Antipsychotic.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Is the atypical neuroleptic selektivno influencing limbic structures. Antipsychotic action is caused by blockade to the same extent central dopamine D2 receptors and serotoninovy 5HT2-receptors. Suppresses productive symptomatology (hallucinations, nonsense, disturbances of thinking, psychotic excitement, aggression, frustration of behavior).

Moderate adrenolytic action causes hypotensive reactions. Does not influence histamine and muskarinovy receptors as is absent anticholinergic and sedative effects. Does not exert also impact on prolactin level. So, its level remained with patients who accepted drug a long time (1 year and more) normal.

Pharmacokinetics

At intake it is well absorbed, Cmax in blood is defined in 10 hours. Meal does not influence absorption. For 99% contacts blood proteins. Gets through GEB, it is metabolized in a liver by isoenzymes of CYP2D6 and CYP3A. Antipsychotic activity at metabolites is not revealed. T1/2 about 3 days. The most part with a stake and with urine insignificant part is removed.

Indications to use

Schizophrenia. It is impossible to apply in case of emergency to stopping of frustration.

Contraindications

• hypopotassemia and hypomagnesiemia;
• heavy cardiovascular pathology;
• heart failure;
• arrhythmias;
• myocardium hypertrophy;
• bradycardia;
• syndrome of lengthening of QT (inborn and acquired);
• liver failure;
• age till 18 flyings;
• pregnancy;
• hypersensitivity;
• concomitant use of drugs which extend QT (antiaritmik, thioridazine, erythromycin, gatifloksatsin, terfenadin and astemizol, lithium drugs);
• concomitant use with verapamil, diltiazem, Cimetidinum.

With care it is appointed to patients at whom in the anamnesis convulsive attacks are noted.

Side effects

• rhinitis, short wind, hypostasis mucous nose;
• paresthesias, dizziness;
• spasms, late dyskinesia (seldom);
• postural hypotension;
• hypostases of the lower extremities;
• lengthening of QT;
• ventricular tachycardia;
• leukocyturia and hamaturia;
• dryness in a mouth, a weight increase;
• hyperglycemia (seldom).

Serdolekt, application instruction (Way and dosage)

How to accept Serdolekt? Accept in 1 times a day. An initial dose — 4 mg, then increase it each 5 days by 4 mg. Usually optimum effective dose from 12 mg to 20 mg a day. Selection of a dose is carried out by the doctor in the conditions of a hospital. In exceptional cases appoint the maximum dose of 24 mg.

To elderly people increase of a dose is carried out slowly, a titration method. Considering risk of cardiotoxicity, it is obligatory to carry out ECG researches. At a renal failure the mode of dosing is not adjusted.

Overdose

It is shown by drowsiness, tachycardia, decrease in the ABP, indistinctness of the speech, lengthening of an interval of QT, Bouveret's ventricular disease sometimes develops. Treatment consists in drug withdrawal, carrying out a gastric lavage, reception of sorbents and laxatives. The specific antidote does not exist. Symptomatic therapy and observation over the patient in the conditions of a hospital to a total disappearance of symptoms of overdose is made.

Interaction

Not to apply along with the drugs extending QT interval. The medicines inhibiting CYP2D6 (paroksetin, fluoxetine, quinidine), increase concentration of active agent in blood therefore it is necessary to carry out ECG inspection often. Simultaneous use of erythromycin, diltiazem and verapamil leads to increase in concentration of active ingredient in blood. Extent of increase in concentration is higher at patients with reduced activity of CYP2D6. At reception with carbamazepine, phenobarbital, Phenytoinum and rifampicin strengthening of a metabolism of active agent is possible that reduces concentration of a neuroleptic therefore for achievement of effect increase of a dose can be required.

Terms of sale

According to the recipe.

Storage conditions

Temperature is up to 25 °C.

Period of validity

5 years.

Serdolekt's analogs

Zeldoks, Zipsila, Sertindol, Sulpiridum, Risperidon, Rileptid.

About Serdolekta

Significant milestone in treatment of schizophrenia is emergence of neuroleptics. However, classical neuroleptics cause extrapyramidal frustration in patients. Use of atypical neuroleptics — a risperidon, an amisulprid, a serdolekt, clozapine, olanzapine, not defiant or causing extremely seldom extrapyramidal frustration, is more acceptable at this disease in spite of the fact that cost is much higher than them and they have no the injection and prolonged dosage forms.

Drug of Serdolekt was accepted by the patients suffering from panic attacks and schizophrenia. In all cases treatment was continuous and long. Almost all patients note existence of side reactions. From negative influences of this drug most often note a weight increase, obtusion of emotions, decrease in a libido in responses. If by-effects were expressed with the doctor the issue of transfer into reception of other neuroleptic was resolved.

• "… Two years I accept this drug, from side effects: a congestion of a nose and the increased appetite, recovered on 10 kg. Despite it, quality of life is much better, than at reception of typical neuroleptics. Got a job, became more self-assured".
• "… Touched many neuroleptics. Serdolekt's reception returned 4 mg to life. Normally I work, I react to jokes of colleagues, the sense in life appeared, the intelligence returned. Became contact, communication with people pleases".
• "… I accept drug the ninth month: symptoms of an illness disappeared, thoughts are not confused, drowsiness has not enough. From shortcomings I can note that emotions were gone, there is no wish to communicate with anybody and gained excess weight".
• "… I accept Serdolekt of 12 mg a day. Assured that there will be no side effects, but it appeared not so. There is a wish to sleep, the congestion of a nose and constant feeling of hunger appeared. Sometimes the head hurts".
• "… On Serdolekta I had a negative symptomatology there was more sluggish, there are differences of mood depending on weather".

The positive moment of this drug is that it does not oppress cognitive functions, and even stimulate them.

What cannot be told about typical neuroleptics which prolonged use leads to a bigger destruction of the personality (disturbance of memory, thinking, depression and an adynamia, a social otgorozhennost).