PROZERIN AMPOULES 0.05% 1ML

Mechanism of action

Synthetic anticholinesterase agent. Reversibly blocks cholinesterase, which leads to the accumulation and enhancement of the action of acetylcholine on organs and tissues, and the restoration of neuromuscular conduction. It causes a decrease in heart rate, increases the secretion of glands (salivary, bronchial, sweat and gastrointestinal ) and the bladder causes bronchospasm, tones the skeletal muscles.

Being a quaternary ammonium base, poorly penetrates through the BBB and has no central action. Bioavailability - 1-2%. With v / m the introduction of TCmax - 30 minutes. Communication with plasma proteins - 15-25%. T1 / 2 by oral administration - 52 min, i / m - 51-90 min, i / v - 53 min. Metabolism - in the liver with the formation of inactive metabolites. 80% of the administered dose is excreted by the kidneys within 24 hours (of which 50% in unchanged form and 30% in the form of metabolites).

Indications and usage

Myasthenia gravis, motor impairment after brain injury, paralysis, recovery period after suffering meningitis, polio, encephalitis, weakness of labor activity (rarely), open-angle glaucoma,atrophy of the optic nerve, neuritis; atony of the digestive tract, atony of the bladder. Elimination of residual disorders of the neuromuscular transmission of non-depolarizing muscle relaxants.

Prozerin take inside, 30 minutes before meals, adults - 10-15 mg 2-3 times a day, the maximum single dose - 15 mg, daily - 50 mg; children - preferably in the form of granules (dissolved before use in warm boiled water to the “100 ml” mark, obtaining a solution of 0.02% concentration with a content of 5 ml of solution - 1 mg), up to 10 years - 1 mg for 1 year of life per day, older than 10 years - up to 10 mg / day (not more).

PC: adults - 0.5-1-2 mg (0.5 mg - 1 ml of 0.05% solution) 1-2 times a day, the maximum single dose - 2 mg, daily - 6 mg; children (only in the hospital) - 0.05 mg (0.1 ml of 0.05% solution) for 1 year of life per day, but not more than 3.75 mg (0.75 ml of 0.05% solution) per injection. The course of treatment (except for myasthenia) - 25-30 days, if necessary - again, after 3-4 weeks. Most of the total daily dose is given in the daytime, when the patient is most fatigued. With myasthenia, 15 mg is prescribed by mouth and sc; or 0.5 mg / m daily; The course of treatment is long, with a change in the route of administration. When myasthenic crisis (with difficulty breathing and swallowing) - 0.5-1 ml of 0.05% solution in / in an adult, then s / c, with short intervals. For postoperative intestinal atony, bladder: for prophylaxis, incl. postoperative urinary retention - s / c or v / m, 0.25 mg, as early as possible after surgery, and again - every 4-6 hours for 3-4 days; treatment of urinary retention - s / c or i / m 0.5 mg; if within 1 hour the urine does not move,catheterization is performed and, after emptying the bladder, it is administered every 3 hours, for a total of 5 injections. To reduce intraocular pressure, instilled into the conjunctival sac in 1-2 cap 0.5% solution 1-4 times a day. With the weakness of labor activity - inside 3 mg 4-6 times a day with an interval of 40 min or n / a - 1 ml of 0.05% solution 1-2 times with an interval of 1 hour (in combination with 1 ml of 0.1% solution of atropine sulfate, p (once, on the background of the first injection). As an antidote to muscle relaxants (after pre-administration of atropine sulfate at a dose of 0.6-1.2 mg IV, until the pulse rises to 80 beats / min), 0.5-2 mg IV is administered after 1 / 2-2 min slowly. If necessary, repeat injections (including atropine in the case of bradycardia) in a total dose of not more than 5-6 mg (10-12 ml) for 20-30 minutes; during the procedure, provide good ventilation of the lungs.

Contraindications

Hypersensitivity, epilepsy, hyperkinesia, vagotomy, ischemic heart disease, bradycardia, arrhythmia, angina pectoris, bronchial asthma, marked atherosclerosis, hyperthyroidism, gastric ulcer and duodenal ulcer, peritonitis, mechanical obstruction of the gastrointestinal tract and stomach, duodenal ulcer, peritonitis, mechanical obstruction of the gastrointestinal sharply weakened children, pregnancy, lactation.

Adverse reactions

Hypersalivation, spastic contraction and increased intestinal motility, nausea, vomiting, flatulence, diarrhea; headache, dizziness, weakness, loss of consciousness, drowsiness; miosis, visual impairment,arrhythmias, brady- or tachycardia, AV blockade, nodal rhythm, nonspecific ECG changes, cardiac arrest, decreased blood pressure (mainly when administered parenterally), shortness of breath, respiratory depression until stopping, bronchospasm, tremor, spasms and twitching of skeletal muscles, including fasciculations muscles of the tongue, convulsions, dysarthria, arthralgia; increased urination; excessive sweating; allergic reactions (facial flushing, rash, itching, anaphylaxis). Overdose. Symptoms: associated with overexcitation of cholinergic receptors (cholinergic crisis): bradycardia, hypersalivation, miosis, bronchospasm, nausea, increased peristalsis, diarrhea, frequent urination, twitching of the muscles of the tongue and skeletal muscles, the gradual development of general weakness, decreased blood pressure. Treatment: reduce the dose or stop treatment, if necessary, inject atropine (1 ml of 0.1% solution), metacin and other anticholinergic drugs.

With parenteral administration of large doses, it is necessary (preliminary or simultaneous) the appointment of atropine. When a myasthenic (with insufficient therapeutic dose) or cholinergic (due to overdose) crisis occurs during treatment, a thorough differential diagnosis is required due to the similarity of symptoms.

Drug Interactions

When myasthenia is prescribed in combination with antagonists of aldosterone, corticosteroids and anabolic hormones. Atropine, metacin and others.M-cholinoblockers weaken M-cholinomimetic effects (pupil constriction, bradycardia, increased gastrointestinal motility, hypersalivation, etc.). Lengthens and strengthens (with parenteral administration) the effect of depolarizing muscle relaxants (dithiline, etc.); weakens or eliminates - anti-depolarizing. With caution prescribed against the background of anticholinergics, in children (with myasthenia) on the background of neomycin, streptomycin, kanamycin and other antibiotics with anti-depolarizing effect, local and some general anesthetics, antiarrhythmic and some other drugs that violate cholinergic transmission.

Storage conditions

A. List: In a dry, dark place at a temperature of 15-25 ° C. Shelf life 2 years.

Prozerin