Belupo's Sulpiridum

General characteristics. Structure:

Active agent: Sulpiridum of 50 mg

Excipients: lactoses monohydrate, starch corn, starch corn prezhelatinizirovanny, magnesium stearate 
 
Structure of capsules: titanium dioxide, gelatin.

Active agent: Sulpiridum of 200 mg

Excipients: lactoses monohydrate, starch corn, magnesium stearate  

Structure of capsules: a lid — titanium dioxide, gelatin; the case — FD&C Blue 2 indigo carmine, titanium dioxide, gelatin.

Pharmacological properties:

Sulpiridum - an atypical neuroleptic from group of the replaced benzamides.
Sulpiridum has moderate antipsychotic activity in a combination to the stimulating and timoanaleptichesky (antidepressive) action.
The antipsychotic effect is connected with anti-dopaminergic action. In TsNS Sulpiridum blocks preferential dopaminergic receptors of limbic system, and influences neostriatny system slightly, it possesses antipsychotic action and causes insignificant number of by-effects.
Peripheral action of Sulpiridum is based on oppression of presynaptic receptors. With increase in quantity of a dopamine in TsNS connect improvement of mood, with reduction - development of symptoms of a depression.
Antipsychotic action of Sulpiridum is shown in doses more than 600 mg/days, in doses to 600 mg/days the stimulating and antidepressive action prevails.
Sulpiridum does not make considerable impact on adrenergic, cholinergic, serotoninovy, histamine and receptors of piperidic acid (GABA receptors).
In small doses Sulpiridum can be applied as supportive application at treatment of psychosomatic diseases, in particular, it is effective in stopping of negative mental symptoms of a peptic ulcer of a stomach and duodenum. At an irritable colon Sulpiridum reduces intensity of abdominal pains and leads to improvement of a clinical condition of the patient.
Low doses of Sulpiridum (50-300 mg/days) are effective at dizzinesses, irrespective of an etiology. Sulpiridum stimulates secretion of prolactin and has the central antiemetichesky effect (oppression of the emetic center).

Pharmacokinetics. After oral administration of Cmax in plasma are reached in 1.5-3 h. Bioavailability of Sulpiridum - 27%. Linkng of Sulpiridum with proteins of plasma makes less than 40%. Concentration of Sulpiridum in TsNS makes 2-5% of concentration in plasma. Sulpiridum is allocated with breast milk. Sulpiridum in a human body is not exposed to metabolism and is removed practically in not changed look through kidneys. T1/2 makes 6-8 p. T1/2 considerably increases at patients with a moderate and heavy renal failure to 20-26 h later in/in introductions. Such patients should lower a dose of Sulpiridum and/or to increase an interval between administration of drug.

Indications to use:

As monotherapy or in combination with other psychotropic drugs.
— acute and chronic schizophrenia;
— acute delirious states;
— depressions of various etiology;
— neurotic frustration;
— dizziness of various etiology (vertebro-basilar insufficiency, vestibular neuritis, Menyer's disease, a state after a craniocereberal injury, average otitis);
— auxiliary therapy at a peptic ulcer of a stomach and duodenum and an irritable colon.

Route of administration and doses:

Inside.
It is not recommended to accept drug in the second half of day (after 16 h) in connection with increase in level of wakefulness.

The maximum recommended daily dose makes 1600 mg of Sulpiridum.
Acute and chronic schizophrenia, acute delirious psychosis: initial doses of Sulpiridum depend on a clinical picture of a disease and make 600–1200 mg/days divided into several receptions, maintenance doses — 300–800 mg/days.

Depression: from 150-200 to 600 mg/days divided into several receptions.

Dizziness: 150–200 mg/days, in serious conditions it is possible to increase a dose to 300–400 mg/days. Treatment duration — not less than 14 days.
Auxiliary therapy at a peptic ulcer of a stomach and duodenum, an irritable colon: 100–300 mg/days in one or two receptions.

Doses at patients with a renal failure:
Because Sulpiridum is brought out of an organism preferential through kidneys, it is recommended to reduce a dose of Sulpiridum and/or to increase an interval between introduction of separate doses of drug depending on indicators of clearance of creatinine:

Cl of creatinine, ml/min.	Sulpiridum dose in comparison with standard, %	Increase in an interval between receptions of Sulpiridum, time
30–60	70	1,5
10–30	50	2
less than 10	30	3

Doses for elderly people: for elderly people the initial dose of Sulpiridum has to make 1/4–1/2 doses for adults.

Doses for children: the standard dose of Sulpiridum for children is more senior than 14 years makes 3–5 mg/kg.

Features of use:

At emergence of a hyperthermia during treatment by the drug Belupo's Sulpiridum it is necessary to cancel. The hyperemia can be a sign of development of the malignant antipsychotic syndrome (which is shown a hyperthermia, dyskinesia, vegetative frustration), described at treatment by neuroleptics. Though data on development of a syndrome against the background of treatment by the drug Belupo's Sulpiridum are absent, care is necessary, in particular at purpose of high doses of drug.

At purpose of the drug Belupo's Sulpiridum patients with epilepsy before an initiation of treatment need to conduct preliminary clinical and electrophysiologic survey since drug reduces a threshold of convulsive activity.

Influence on ability to driving of motor transport and to control of mechanisms

During treatment the control of vehicles and the work with mechanisms requiring special attention and also alcohol intake is forbidden.

Side effects:

The undesirable phenomena developing as a result of reception of Sulpiridum are similar to the undesirable phenomena caused by other psychotropic drugs, but the frequency of their development, generally is less.

From endocrine system: development of a reversible giperprolaktinemiya most of which frequent manifestations are a galactorrhoea, disturbance of a menstrual cycle is possible, is more rare - a gynecomastia, impotence and frigidity.

From the alimentary system: dryness in a mouth, heartburn, nausea, vomiting, a lock, increase in activity of transaminases and an alkaline phosphatase in blood serum.

From TsNS: sedation, drowsiness, dizziness, a headache, a tremor, it is rare - an extrapyramidal syndrome, early and late dyskinesia, an akathisia, oral automatism, aphasia. At use in small doses psychomotor excitement, uneasiness, irritability, frustration of a dream, visual acuity disturbance are possible. At development of a hyperthermia drug should be cancelled since fervescence can indicate development of the antipsychotic malignant syndrome (AMS).

From cardiovascular system: tachycardia, increase or a lowering of arterial pressure is possible, development of orthostatic hypotension, lengthening of a QT interval, seldom, arrhythmia like "pirouette" is in rare instances possible.

Allergic reactions: skin rash, an itch, eczema are possible.

During treatment the increased perspiration, increase in body weight can be noted by Sulpiridum.

Interaction with other medicines:

The concomitant use of Sulpiridum and drugs, the oppressing TsNS (narcotic analgetics, antihistaminic drugs, barbiturates, benzodiazepines and other anxiolytics), can lead to strengthening of sedation of these drugs.

Sulpiridum combination with alcohol can also strengthen sedative effect of alcohol.

It is necessary to avoid co-administration with a levodopa because of mutual antagonism of a levodopa and Sulpiridum.

There is an increased risk of development of orthostatic hypotension at a concomitant use of Sulpiridum and anti-hypertensive means.

Sukralfat, the antacids containing Mg2+ and/or Al3+ reduce bioavailability by 20-40%.

Antagonism with agonists of dofaminergichesky receptors (амантадин, Apomorphinum, Bromocriptinum, каберголин, энтакапон, лизурид, перголид, piribedit, прамипексол, кинаголид, ропинирол) and neuroleptics. At the extrapyramidal syndrome induced by neuroleptics do not apply agonists of dofaminergichesky receptors, and use anticholinergic medicines. In need of treatment of patients with Parkinson's disease against the background of use of agonists of dofaminergichesky receptors the dose of the last should be lowered gradually to full cancellation (sharp cancellation can lead to development of a malignant antipsychotic syndrome).

Risk of development of ventricular arrhythmias like "torsade de pointes" at simultaneous use with: antiarrhythmic medicines 1 of a class A (quinidine, hydroquinidine, Disopyramidum) and the III class (Amiodaronum, соталол, dofetit, ибутилид), some neuroleptics (thioridazine, Chlorpromazinum, levomepromazinum, трифлуоперазин, циамемазин, амисульприд, тиаприд, a haloperidol, Droperidolum, Pimozidum), medicinal means, causing bradycardia (diltiazem, verapamil, beta-blockers, a clonidine, гуанфацин, foxglove drugs, donepezil, ривастигмин, такрин, an ambenoniya chloride, Galantaminum, pyridostigmine, неостигмин), the medicines causing a hypopotassemia (kaliyvyvodyashchy diuretics, some laxatives, Amphotericinum In in/in, GKS, тетракозактид) and others (including bepridit, цизаприд, difemanit, erythromycin intravenously, мизоластин, Vincaminum in/in, галофантрин, pentamidine, спарфлоксацин, moxifloxacin).

Contraindications:

— acute alcoholic poisoning, hypnagogues, analgetics;
— hypersensitivity to Sulpiridum; pheochromocytoma;
— epilepsy;
— prolaktinzavisimy tumors (including breast cancer);
— giperprolaktinemiya;
— patients in the heat of passion and aggression which have a danger of provocation of symptoms;
— breastfeeding period;
— children up to 14 years;
— Parkinson's disease;
— galactosemia;
— sprue of a glucose/galactose or deficit of lactase.

With care: it is necessary to observe precautionary measures at purpose of Sulpiridum to patients with a renal failure as to 95% of Sulpiridum it is removed through kidneys. These patients are recommended to reduce Sulpiridum dose; it is also necessary to observe precautionary measures at purpose of Sulpiridum to patients with heart diseases, blood vessels, stenocardia, arterial hypertension, a liver failure, a malignant antipsychotic syndrome in the anamnesis, epilepsy, glaucoma, a prostate hyperplasia, an ischuria, to young women with an irregular menstrual cycle, to patients of advanced age.

Use of the drug BELUPO'S SULPIRIDUM at pregnancy and feeding by a breast
Purpose of Sulpiridum is not recommended to pregnant women, except for cases when the doctor, having estimated a ratio of advantage and risk for the pregnant woman and a fruit, makes the decision that use of drug is necessary. During treatment by drug it is necessary to stop breastfeeding.

Use at abnormal liver functions
With care to appoint to patients with a liver failure.

Use at renal failures
It is necessary to observe precautionary measures at purpose of Sulpiridum to patients with a renal failure as to 95% of Sulpiridum it is removed through kidneys. These patients are recommended to reduce Sulpiridum dose

Use for elderly patients
For elderly people the initial dose of Sulpiridum has to make 1/4 – 1/2 doses for adults.

Use for children
The standard dose of Sulpiridum for children is more senior than 14 years makes 3-5 mg/kg of body weight. Drug is contraindicated to children up to 14 years.

Overdose:

At overdose of Sulpiridum there are no specific symptoms. At overdose of Sulpiridum can be observed: sight opacification, arterial hypertension, sedation, nausea, extrapyramidal symptoms, dryness in a mouth, vomiting, the increased sweating and a gynecomastia, development of ZNS. Due to the lack of a specific antidote it is necessary to apply a symptomatic and maintenance therapy.

Storage conditions:

At a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Капс. 200 mg: 12 pieces.

Капс. 50 mg: 30 pieces.