Sulpiridum

General characteristics. Structure:

Active ingredient: 50 mg or 200 mg of Sulpiridum.

Excipients: lactose (sugar milk); potato starch; MKTs; gelatin; talc; magnesium stearate (magnesium stearate).

The antipsychotic drug possessing the stimulating and antidepressive action.

Pharmacological properties:

Pharmacodynamics. Antipsychotic means (neuroleptic) from group of the replaced benzamides. Renders moderate antipsychotic, and also antidepressive action in combination with the activating action. The mechanism of antipsychotic action is connected with selective blockade central dopamine D2 receptors. Sedative action is expressed poorly, alpha and adrenoceptor blocking activity low, practically does not cause antimuskarinovy effects. Seldom causes extrapyramidal frustration therefore treats "atypical" neuroleptics. Promotes healing of cankers of a stomach and duodenum.

Pharmacokinetics. After introduction of Sulpiridum in oil in a dose of 100 mg of Cmax in plasma it is reached in 30 min., after intake in a dose of 200 mg - in 4.5 h. Bioavailability at intake makes 25-35% and is characterized by considerable individual variability.

Concentration of Sulpiridum in plasma is proportional to a dose. Linkng with proteins of plasma makes no more than 40%. Sulpiridum quickly gets into all body tissues, quicker - into a liver and kidneys, more slowly - into brain tissues (at the same time the main quantity collects in a hypophysis). With breast milk 0.1% of a daily dose of Sulpiridum are allocated.

It is removed by kidneys in not changed look by glomerular filtering (92%). The general clearance (as a rule, equal to renal) makes 126 ml/min. of T1/2 - about 7 h.

Indications to use:

The neurotic states which are followed by block; psychosomatic disturbances, including at a peptic ulcer of a stomach and duodenum, NYaK; acute and chronic psychoses with dominance of block, an agrammatism, abulia; the acute and chronic psychoses which are followed by nonsense or confusion of consciousness including at schizophrenia.

Route of administration and doses:

Inside adult - 100-300 mg/days in 2-3 receptions. If necessary enter in oil 100-800 mg/days in a dose. At children apply 5 mg/kg in a daily dose.

The maximum daily dose at intake for adults makes 1.6 g.

Features of use:

With care apply at patients with parkinsonism, elderly people. At a heavy renal failure the dose decline or carrying out a discontinuous course of treatment is recommended.

At patients with epilepsy before therapy it is necessary to conduct preliminary clinical and electrophysiologic survey since Sulpiridum lowers a threshold of convulsive readiness.

In case of a hyperthermia which is one of the ZNS elements Sulpiridum should be cancelled immediately.

During treatment not to allow alcohol intake.

With care apply at children.

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

During treatment it is necessary to abstain from occupations potentially dangerous types of activity requiring special attention and bystry psychomotor reactions.

Side effects:

From TsNS: excitement, dizziness, frustration of a dream, oral automatism, aphasia.

From the alimentary system: dryness in a mouth, heartburn, vomiting, a lock.

From cardiovascular system: increase in the ABP.

From endocrine system: disturbances of a menstrual cycle, decrease in sexual activity. At long reception in high doses - a galactorrhoea, a gynecomastia.

Allergic reactions: skin rash, itch.

Interaction with other medicines:

At simultaneous use of medicines, the oppressing TsNS (opioid analgetics, hypnotic drugs, tranquilizers, a clonidine, antibechics of the central action), the oppressing influence on TsNS amplifies.

At simultaneous use with anti-hypertensive means anti-hypertensive action amplifies and the risk of development of orthostatic hypotension increases.

At simultaneous use with a levodopa efficiency of Sulpiridum decreases.

Cases of development of heavy extrapyramidal reactions at simultaneous use of Sulpiridum from lithium are described by a carbonate.

At simultaneous use with fluoxetine development of extrapyramidal symptoms and dystonia is possible.

Contraindications:

Pheochromocytoma, arterial hypertension, psychomotor excitement, hypersensitivity to Sulpiridum.

Overdose:

Symptoms: dyskinesia (spasm of chewing muscles, spastic wryneck), extrapyramidal disturbances. In some cases — the expressed parkinsonism, a coma.

At use of tablets the sight nablyudatsya:pomutneniye, arterial hypertension, sedation, nausea, dryness in a mouth, vomiting, the increased sweating and a gynecomastia, development of ZNS can.

Treatment: symptomatic. Purpose of holinoblokator of the central action.

Storage conditions:

To store in dry, protected from light and the place, unavailable to children, at a temperature not above 30 °C.

Issue conditions:

According to the recipe

Packaging:

10 pieces - planimetric strip packagings (3) - packs cardboard.
30 pieces - banks of dark glass (1) - a pack cardboard.