Vinpotsetin-Darnitsa

General characteristics. Structure:

Active ingredient: vinpocetine; 

1 ml of a concentrate contains a Vinpocetine in terms of 100% dry matter of 5 mg;

excipients: a benzetoniya chloride, propylene glycol, glycine, sodium sulfite anhydrous (Е 221), dinatrium эдетат, divorced Acidum hydrochloricum, water for injections.

Pharmacological properties:

Pharmacodynamics. The Vinpocetine has vasodilating, anti-hypoxemic effect (thanks to strengthening of transport of glucose and oxygen through a blood-brain barrier, to increase in a share of aerobic metabolism of glucose), improves cerebral circulation, selectively expands the struck vessels in the ischemic center of a brain, without having significant effect on peripheral blood supply and cardiac performance, does not cause a phenomenon of "burglarizing", strengthens intake of blood first of all in the struck ischemic sites with low perfusion.

Drug activates metabolism of a brain due to increase in utilization of glucose and oxygen, increase in the tsAMF, ATP level and a ratio of ATF/AMF, and also level of noradrenaline and serotonin in a brain.

Neurotyre-tread action of a vinpotsenin is connected with reduction of expressiveness of the cytotoxic reactions caused by the stimulating amino acids, reduction of activity of cellular transmembrane sodium and calcic tubules and receptors of NMDA and AMPA, increase in neurotyre-tread action of adenosine.

Together with it the Vinpocetine has anti-aggregation effect, improves rheological properties of blood and microcirculation in brain fabric, and also possesses antioxidant action. Drug blocks aggregation of thrombocytes, reduces patholologically the increased viscosity of blood, increases ability of erythrocytes to deformation, promotes interstitial transport of oxygen by reduction of affinity of erythrocytes to it.

Pharmacokinetics. At intravascular introduction for 66% contacts proteins of a blood plasma. The therapeutic effect is shown at concentration in blood within 10-20 mg/ml, transformed in a liver with formation of inactive metabolites: apovinkaminovy acid, hydroxide of a Vinpocetine, gidroksiapovinkaminovy acid, dihydro-Vinpocetine-glitsinata. Diseases of a liver and kidneys do not influence metabolism of a Vinpocetine. The elimination half-life (T1/2) makes 4-5 hours. The insignificant quantity in an invariable look is removed with urine in the form of metabolites.

Pharmaceutical characteristics.

Main physical and chemical properties: transparent colourless or slightly greenish liquid.

Incompatibility.

Vinpotsetin-Darnitsa pharmaceutical is incompatible with heparin therefore they cannot be entered in one syringe.

Solution of a Vinpocetine is chemically incompatible with the infusion solutions containing amino acids therefore they cannot be applied to cultivation of a concentrate Vinpotsetin-Darnitsa.

Indications to use:

Neurology. Disturbance of cerebral circulation (an ischemic stroke, a state after a stroke vertebro-basilar and cerebrovascular insufficiency, atherosclerosis of vessels of a brain, vascular dementia, hypertensive and posttraumatic encephalopathy); tranzitorny ischemic attack, brain vasospasm, partial occlusion of arteries of a brain; neurologic and mental symptoms of disturbance of cerebral circulation; motive frustration, including apraxia; aphasia.

Otology. Toxic (including medicamentous), vascular changes of hearing, and also change of hearing of other genesis (idiopathic, caused by a noise overload); Menyer's disease, kokhleovestibulyarny neuritis, a ring in ears.

Ophthalmology. Chronic vascular diseases of a choroid and a retina of an eye (including – a vasomotor spasm and thrombosis of the central artery or vein of a retina).

Route of administration and doses:

Solution Vinpotsetin-Darnitsa is applied only intravenously in the form of slow drop infusion (speed of infusion should not exceed 80 drops 1 minute). It is forbidden to administer the drug subcutaneously, intramusculary and in the concentrated look intravenously.

Usually initial daily dose makes 20 mg of a Vinpocetine (2 ampoules) divorced in 500-1000 ml of solution for infusions (0,9% of solution of sodium of chloride, 5% of solution of glucose, Ringer's solution). If necessary and good tolerance appoint repeated (2-3 times a day) slow drop infusions, gradually raising a dose within 3-4 days to maximum – 1 mg/kg of body weight a day.

The average daily dose of drug makes 50 mg at the body weight of 70 kg (contents of 5 ampoules divorced in 500 ml of infusion solution).

The average duration of treatment by drug – 10-14 days.

Upon termination of a course of intravenous therapy it is recommended to continue treatment by Vinpocetine drugs in the form of tablets.

Patients with diseases of a liver and kidneys can appoint drug in the same doses.

Features of use:

It is necessary to be careful at purpose of solution Vinpotsetin-Darnitsa to patients with dekompensirovanny chronic heart failure in combination with bradycardia at whom on an ECG lengthening of an interval of QT is observed. It is recommended to carry out control of an ECG in cases of existence of a syndrome of the extended QT or at simultaneous use of drugs which can extend QT interval. At hemorrhagic strokes Vinpotsetin-Darnitsa it is possible to appoint only in 5-7 days after an acute phase of a disease. It is not recommended to appoint the patient with labile arterial pressure. With care appoint the patient accepting anti-hypertensive means.

Hypodermic, intramuscular or intravenous jet administration is not allowed. Drug is incompatible with alcohol.

In view of absence Vinpotsetin-Darnits gepato-and nephrotoxic action has no need for change of a dose at patients with diseases of kidneys or a liver.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

Because Vinpotsetin-Darnitsa slows down reaction, during use of drug it is necessary to be careful at management of transport and work with difficult mechanisms.

Side effects:

From the central and peripheral nervous system: dizziness, a headache, irritability a sleep disorder (sleeplessness, drowsiness), block, weakness, the increased sweating, feeling of heat.

From digestive tract: dryness in a mouth, nausea, heartburn, dyspepsia.

From cardiovascular system: delay of intra ventricular conductivity, ST segment depression, lengthening of an interval of QT, change of arterial pressure, tachycardia, premature ventricular contraction, rushes of blood to the person, thrombophlebitis in an injection site.

From system of blood: development of an agranulocytosis is in rare instances possible.

Dermatological reactions: dermahemia.

Allergic reactions: skin hypersensitivity reactions.

Interaction with other medicines:

Simultaneous use of a Vinpocetine with β-blockers ((((((((((hloranololy, Pindololum), Clopamidum, glibenclamide, digoxin, atsenokumaroly or Hydrochlorthiazidum in clinical trials was not followed by any interaction between them.

Heparin – at simultaneous parenteral appointment with a Vinpocetine increase in risk of development of bleedings is possible.

Hypotensive medicines (α-Methyldopum)))))))))) – at simultaneous parenteral appointment with a Vinpocetine strengthening of hypotensive effect therefore at such treatment regular control of arterial pressure is necessary is possible.

Despite the lack of these clinical trials which would confirm a possibility of interaction, recommend to apply with care a Vinpocetine together with drugs which influence the central nervous system, antiarrhythmic drugs, anticoagulating and fibrinolitic means.

Contraindications:

Severe forms of thrombophlebitis, coronary heart disease and heavy arrhythmias. Hypersensitivity to a Vinpocetine, the first days after a cerebral hemorrhagic stroke, the increased intraocular and intracranial pressure, pregnancy, the feeding period a breast, children's age.

Use during pregnancy or feeding by a breast.

The Vinpocetine can get through a placenta and be allocated in breast milk therefore Vinpotsetin-Darnits's use is not recommended during pregnancy and feeding by a breast.

Children.

Vinpotsetin-Darnits's appointment is not recommended to children in view of insufficient clinical experience.

Overdose:

Overdose cases Vinpotsetin-Darnitsa were not noted by drug.

At overdose are possible: arterial hypotension, block, nausea, vomiting.

Symptomatic treatment.

Storage conditions:

Period of validity 2 years. To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 2 ml of a concentrate in an ampoule.
 
On 5 ampoules in a blister strip packaging; on the 2nd blister strip packagings in a pack.
 
On 10 ampoules in a blister strip packaging; on 1 blister strip packaging in a pack.