Dibazolum

General characteristics. Structure:

Active ingredient: 10 mg of Bendazolum in 1 ml of solution.

Excipients: Acidum hydrochloricum, water for injections.

Dibazolum has a hypotensive, spasmolytic and immunopromoting effect.

Pharmacological properties:

Pharmacodynamics. The mechanism of action is connected with ability of Dibazolum to block activity of phosphodiesterase IV like (FDE IV). Blockade of enzyme leads to the termination of hydrolysis of tsAMF, increase in their concentration in smooth muscle cells of vessels, internals. tsAMF limits receipt of calcium ions in a muscle cell and inactivates a kinase of light chains of a myosin – sokratitelny protein which provides reduction of a muscle.

Dibazolum reduces a tone and weakens unstriated muscles of internals (a GIT, respiratory tracts, urinogenital system) and vessels. Dibazolum expands preferential arterial vessels and promotes increase in a blood-groove, including cerebral. Hypotensive effect of Dibazolum short (2 - 3 h) and moderate. At prolonged use (especially) causes decrease in cordial emission and deterioration in indicators of electric activity of a myocardium (ECG) in elderly persons.

Dibazolum exerts the stimulating impact on functions of a spinal cord, facilitating synoptic cholinergic transfer. The similar effect is observed from peripheral nervous trunks (cranial nerves, neuroplexes of extremities).

The immunopromoting effect of Dibazolum is connected with blockade of FDE IV in immune cells that leads to ratio shift tsAMF/tsGMF in cells towards dominance of tsGMF. tsGMF stimulates proliferation of mature sensibilized T - and V-lymphocytes, secretion by them of monokin and other factors of mutual regulation, activation of final effector function of immune cells.

Pharmacokinetics. Dibazolum pharmacokinetics is in detail not described. After intramuscular introduction it is quickly and fully absorbed. At repeated use of medicine its pharmacokinetics does not change. Cumulation of Dibazolum does not happen.

Indications to use:

- stopping of hypertensive crises (as a part of a combination therapy);

- treatment of atherosclerosis of arteries of the lower extremities, vasospasms of a brain and extremities (as a part of complex therapy);

- the prevention and stopping of spasms of unstriated muscles of internals at a peptic ulcer, cholecystitis, a spastic colitis, a pylorospasm;

- stopping of bilious and renal colic;

- residual phenomena of poliomyelitis, flaccid paralysis of a facial nerve.

Route of administration and doses:

For stopping of hypertensive crisis and gripes enter 30 - 40 mg (6 - 8 ml 5 mg/ml of solution) intramusculary or intravenously slowly.

At treatment of diseases of a nervous system apply 5 mg of 1 times a day or every other day intramusculary within 5 - 10 days. The course is repeated in 3 - 4 weeks. Further courses are conducted each 1 - 2 month.

To children at treatment of diseases of a nervous system appoint till 1 year - in a dose of 1 mg, at the age of 1 - 3 years - 2 mg, 4 - 8 years - 3 mg, 8 - 12 years - 4 mg, 12 years - 5 mg are more senior.

Features of use:

Pregnancy and lactation. At pregnancy and in the period of a lactation safety and efficiency of use of Dibazolum are not established.

Use in pediatrics. Dibazolum can be applied to treatment of neurologic disturbances (an effect of birth trauma) at newborn children.

Use in gerontology. It is necessary to be careful and use short courses of Dibazolum at treatment of persons 70 years, in connection with a possibility of decrease at them are more senior than cordial emission and deterioration in indicators of an ECG.

Influence on ability to driving of motor transport and control of mechanisms. Dibazolum does not exert undesirable impact on ability of control of the vehicle or other operator activity.

Side effects:

- allergic reactions.

- deterioration in indicators of an ECG at prolonged use in connection with reduction of cordial emission.

- at use in high doses – feeling of heat, the increased sweating, dizziness, nausea, a headache.

Interaction with other medicines:

At simultaneous use with a papaverine mutual strengthening of spasmolytic effect of medicines is observed.

At simultaneous use with phentolamine, a clonidine, Reserpinum and diuretics strengthening of their hypotensive action is observed. Prevents the increase in peripheric resistance of vessels mediated by β-adrenoblockers.

At combined use with ascorbic acid strengthening of the immunostimulating effect of Dibazolum is observed.

Contraindications:

- hypersensitivity to Dibazolum;

- a convulsive syndrome or epileptic seizures in the anamnesis.

With care. Advanced age (decrease in cordial emission).

Overdose:

Symptoms of intoxication are shown at introduction of high doses. Emergence of a diaforez (perspiration), feeling of inflows of heat, dizziness, nausea, headache is characteristic.

Treatment: the specific antidote does not exist. Measures of the help include the medicine cancellation, a gastric lavage with absorbent carbon supporting and the symptomatic therapy directed to elimination of the arisen disturbances and increase in the ABP.

Storage conditions:

At a temperature from +5 to +25 °C. To store in the place, unavailable to children. A period of validity - 3 years. Not to use medicine after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in ampoules in packaging No. 10, No. 10 x 1.