Prozerin-Darnitsa, solution for and 0.05% on 1 ml No. 10

General characteristics. Structure:

international and chemical names: Neostigmine methylsulphate; (N-(meta-dimetilkarbamoil-oxyphenyl) - trimetilammony methyl sulfate);
main physical and chemical properties: transparent colourless liquid;
structure: 1 ml of solution contains a neostigmin of methyl sulfate - 0,0005 g;
excipients: water for injections - to 1 ml.

Pharmacological properties:

Prozerin-Darnitsa is the synthetic antikholinesterazny substance having quarternary ammonium group in the molecule and treats reversible inhibitors of cholinesterase. Blockade of the last leads to accumulation of acetylcholine in the field of synapses of cholinergic nerves, to strengthening of action of the last on bodies and fabrics and to recovery of neuromuscular conductivity. As the quarternary ammonium basis Prozerin-Darnitsa badly gets through a blood-brain barrier, than its preferential peripheral influence speaks. On peripheral effects Prozerin-Darnitsa is close to physostigmine and Galantaminum: it causes an urezheniye of serdtsebiyeniye, increase in salivation, narrowing of a pupil, strengthens a tone of muscles of intestines, bladder, causes a spasm of bronchial tubes, etc.
Prozerin-Darnitsa is the antagonist of the anti-depolarizing kurarepodobny drugs, but in high doses itself can cause disturbance of neuromuscular conductivity as a result of accumulation of acetylcholine and permanent depolarization in the field of synapses.

Pharmacokinetics. After parenteral administration of a neostigmin bromide is exposed to hydrolysis, and also is metabolized in a liver. Linkng with proteins of plasma makes 15-25%. It is removed with urine in the form of not changed substance and metabolites. Badly gets through a blood-brain barrier.

Indications to use:

Prozerin-Darnitsa apply at a myasthenia, motive disturbances after brain injuries, paralyzes, in the recovery period after the postponed meningitis, poliomyelitis, encephalitis and other neuroinfections, at neuritis, to the prevention and treatment of an atony of intestines and a bladder, sometimes - at weakness of patrimonial activity. In eye practice Prozerin-Darnitsa appoint at an atrophy of an optic nerve, is more rare - for narrowing of a pupil and decrease in intraocular pressure at an open-angle form of glaucoma.
As an antidote of muscle relaxants drug is appointed at muscular weakness and respiratory depression on the termination of anesthesia using the anti-depolarizing kurarepodobny drugs, and also at use of the depolarizing muscle relaxants (Dithylinum) if the last begin to act as anti-depolarizing (\"the double block \").

Route of administration and doses:

Prozerin-Darnitsa enter subcutaneously and intravenously. At development of myasthenic crisis Prozerin-Darnitsa enter subcutaneously in usual doses with small intervals. At especially acute cases of crisis at adults the drug is administered intravenously in a dose of 0,5-1 ml of 0,05% of solution on isotonic solution of sodium of chloride, then in usual doses subcutaneously with small intervals. For potentiation of action of Prozerin-Darnits sometimes subcutaneously in addition enter 1 ml of 5% of solution of ephedrine of a hydrochloride. If necessary treatment of a myasthenia of Prozerinom-Darnits is carried out in combination with antagonists of Aldosteronum (Spironolactonum), anabolic hormones and corticosteroids. At use of drug in insufficient doses the state can worsen, and at reception in the overestimated doses there can be cholinergic crisis, permanent disturbance of neuromuscular conductivity and disorder of breath. Myasthenias carry out Prozerinom-Darnits's treatment is long. At other diseases duration of use of drug makes 25-30 days. If necessary the course of treatment is repeated after a 3-4 weeks break.
For stimulation of childbirth it is possible to administer the drug subcutaneously on 0,5 mg (1 ml of 0,05% of solution) 1-2 times with intervals at 1 o'clock. Along with the first injection of Prozerin-Darnits once subcutaneously enter 1 mg (1 ml of 0,01% of solution) of Atropini sulfas. For stopping of action of muscle relaxants before Prozerinom-Darnitsa intravenously enter Atropini sulfas in a dose of 0,5-0,7 mg (0,5-0,7 ml of 0,1% of solution). In 1,5-2 minutes after increase of pulse intravenously enter 1,5 mg (3 ml of 0,05% of solution) of Prozerin-Darnits. If the effect at this dose is insufficient, Prozerin-Darnitsa repeatedly enter in the same dose (at emergence of bradycardia in addition enter Atropini sulfas). Total quantity of Prozerin-Darnits which can be entered within 20-30 minutes makes 5-6 mg (10-12 ml of 0,05% of solution).
In eye practice for the purpose of decrease in intraocular pressure at an open angle glaucoma 1-4 times a day enter 0,05% of solution of Prozerin-Darnits into a conjunctival sac on 1-2 drops.
The highest doses for adults subcutaneously: one-time 0,002 g (2 mg), daily 0,006 g (6 mg). To children after 1 year Prozerin-Darnitsa appoint subcutaneously on 0,00005 g (0,05 mg = 0,1 ml of 0,05% of solution) to 1 year of life, but it is no more than 0,75 ml of 0,05% of solution for 1 injection. As a rule, to children Prozerin-Darnitsa appoint 1 time a day, but if necessary the daily dose of drug can be divided into 2-3 receptions. Prozerin-Darnitsa in all dosage forms at children apply only in the conditions of a hospital!

Features of use:

With care apply at bradycardia, arrhythmias, arterial hypotension, a vagotonia, Addison's disease, a hyper thyroidism, a peptic ulcer of a stomach and a 12-perstny gut.
During treatment it is necessary to abstain from driving of motor transport and other potentially dangerous types of activity at which concentration of attention and high speed of psychomotor reactions is necessary.
Prozerin-Darnitsa gets through a placenta, in very small quantities is allocated with breast milk. At pregnancy and in the period of a lactation apply only according to vital indications. 

Side effects:

Hypersalivation, cold sweat, weakness, delay of a cordial rhythm, lowering of arterial pressure, miosis, bronchospasm, strengthening of bronchial secretion, strengthening of a vermicular movement of intestines, diarrhea, the accelerated urination, nausea, vomiting, spontaneous twitching of muscles of language and skeletal muscles, the general weakness.

Interaction with other medicines:

Prozerin-Darnitsa shows antagonism concerning M-holinoblokatorov (atropine, homatropine, Platyphyllinum, etc.), ganglioblokator, quinidine, a novokainamid, reduces activity of a pyridoxine of a hydrochloride (B6 vitamin); cyanocobalamine in high doses weakens Prozerin-Darnits's action.

Contraindications:

Use Prozerin-Darnitsa is contraindicated at epilepsy, hyperkinesias, bronchial asthma, stenocardia, the expressed atherosclerosis; do not appoint to the weakened children during the acute period of a disease, at intoxication; at mechanical impassability of intestines and uric ways; in late durations of gestation.

Overdose:

At Prozerin-Darnits's overdose or hypersensitivity (bad portability) to him the side effects caused by overexcitation of holinoretseptor (cholinergic crisis) can be observed: bradycardia, hypotension, the strengthened salivations, narrowing of pupils, a bronchospasm, nausea, vomiting, strengthening of a vermicular movement of intestines, diarrhea, a frequent urination, twitching of muscles of language and skeletal muscles, development of the general weakness. For elimination of by-effects the dose of drug is reduced or stop use it. If necessary enter Atropini sulfas (1 ml of 0,1% of solution), Methacinum and other cholinolytic means.

Storage conditions:

Store in the place protected from light at a temperature from +8 to +25 ° C.

Period of validity - 4 years.

Issue conditions:

According to the recipe

Packaging:

On 1 ml in ampoules No. 10.