Proserin solution for injection 0.05%, 1ml # 10
Expiration Date: 05/2027
Russian Pharmacy name:
Прозерин раствор для инъекций 0.05%, 1мл №10
Myasthenia gravis (in children only myasthenia gravis);
movement disorders after brain injury; paralysis; recovery period after meningitis; poliomyelitis; encephalitis; neuritis;
prevention and treatment of postoperative intestinal atony and urinary retention;
stimulation of labor;
to stop the action of non-depolarizing muscle relaxants.
Route of administration : subcutaneously, intramuscularly, intravenously.
The drug should be administered very slowly. A solution of atropine should always be available to eliminate severe cholinergic reactions that occur.
For the treatment of movement disorders after cerebral paralysis during the recovery period after meningitis, poliomyelitis encephalitis : adults are usually prescribed subcutaneously 05-1-2 mg (05 mg - 1 ml of 005% solution) 1-2 times a day, the maximum single dose is 2 mg daily - 6 mg.
The course of treatment (except for myasthenia gravis) is 25-30 days, if necessary, the course of treatment is repeated after a 3-4 week break. Most of the total daily dose is given during the daytime when the patient is most tired.
When myasthenia gravis is administered subcutaneously, 05 mg per day; the course of treatment is long with a change in the route of administration. With the development of myasthenic crisis in adults, 025-05 mg (05-1 ml of solution) is injected intravenously (with 09% sodium chloride solution) Proserin then subcutaneously in usual doses at short intervals.
To enhance the action of Proserin, ephedrine is sometimes injected under the skin in addition 1 ml of a 5% solution 2 times a day.
To stimulate labor, you can inject 05 mg (1 ml of solution) of Proserin under the skin - 1-2 times at intervals of 1 hour, simultaneously with the first injection, 1 mg (1 ml of 01% solution) of atropine is injected once under the skin.
With postoperative intestinal atony of the bladder: for prophylaxis, incl. postoperative urinary retention - subcutaneously or intramuscularly at 025 mg (05 ml solution) of Proserin as early as possible after surgery and again - every 4-6 hours for 3-4 days; treatment of urinary retention - subcutaneously or intramuscularly 05 mg (1 ml of solution) Proserin; if within 1 hour the urine does not leave, catheterization is performed and after emptying the bladder, a total of 5 injections are injected every 3 hours.
When using the drug to stop the action of non-depolarizing muscle relaxants, atropine is preliminarily injected intravenously at a dose of 05-07 mg (05-07 ml of a 01% solution), an increase in pulse is expected, and after 15-2 minutes, 15 mg (3 ml of solution) of Proserin is injected intravenously. If the effect of this dose was insufficient, the same dose is re-administered (when bradycardia appears, an additional injection of atropine is made). In total, you can enter 5-6 mg (10-12 ml of solution) of Proserin within 20-30 minutes. Ensure adequate ventilation during the procedure.
Children with myasthenia gravis (only in hospital!) Subcutaneously at 005 mg (01 ml of 005% solution) for 1 year of life per day but not more than 375 mg (075 ml of 005% solution) per injection. Usually, the drug is prescribed for children once a day, however, if necessary, the daily dose can be divided into two or three doses.
Active ingredient: neostigmine methyl sulfate (proserin) in terms of 100% substance - 0.5 mg
Excipient: water for injection - up to 1 ml.
Hypersensitivity to the drug
epilepsy
hyperkinesis
vagotomy
coronary heart disease
bradycardia
arrhythmias
angina
bronchial asthma
severe atherosclerosis
thyrotoxicosis
peptic ulcer of the stomach and duodenum
peritonitis
mechanical obstruction of the gastrointestinal tract and urinary tract
period of acute infectious disease
hyperplasia of the prostate
intoxication in severely weakened children
pregnancy
period of breastfeeding.
Carefully:
It is prescribed with caution against the background of anticholinergics in children (with myasthenia gravis) against the background of neomycin streptomycin kanamycin and other antibiotics with a non-depolarizing effect of local anesthetics and antiarrhythmic agents for general anesthesia and a number of other drugs that violate cholinergic transmission.
Trade name of the drug
Proserin
International non-proprietary name
Neostigmine methyl sulfate
Dosage form
injection
Composition
Active ingredient: neostigmine methyl sulfate (proserin) in terms of 100% substance - 0.5 mg
Excipient: water for injection - up to 1 ml.
Description
Transparent, colorless liquid.
Pharmacotherapeutic group
Cholinesterase inhibitor
ATX code
S01EB
Pharmacodynamics:
Synthetic cholinesterase inhibitor. 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. Causes a decrease in heart rate increases the secretion of glands (salivary bronchial sweat and gastrointestinal tract) and promotes the development of hypersalivation of bronchorhea, an increase in gastric acidity, constricts the pupil, causes spasm of accommodation, reduces intraocular pressure, enhances the tone of intestinal smooth muscles (strengthens peristalsis and relaxes the urinary sphincter) causes a spasm of the bronchi, tones up the skeletal muscles.
Pharmacokinetics:
Being a quaternary ammonium base, it poorly penetrates the blood-brain barrier and does not have a central effect. The connection with plasma proteins is 15-25%. After intravenous administration, the maximum effect is observed after 5-15 minutes, the duration of the effect is 25-4 hours.
The half-life for intravenous administration is 53 minutes for intramuscular administration Ч 51-90 minutes.
It is metabolized in the liver by microsomal enzymes with the formation of inactive metabolites.
Excretion: 80% of the administered dose is excreted by the kidneys within 24 hours (of which 50% is unchanged and 30% is in the form of metabolites).
Indications:
Myasthenia gravis (in children only myasthenia gravis);
movement disorders after brain injury; paralysis; recovery period after meningitis; poliomyelitis; encephalitis; neuritis;
prevention and treatment of postoperative intestinal atony and urinary retention;
stimulation of labor;
to stop the action of non-depolarizing muscle relaxants.
Contraindications:
Hypersensitivity to the drug
epilepsy
hyperkinesis
vagotomy
coronary heart disease
bradycardia
arrhythmias
angina
bronchial asthma
severe atherosclerosis
thyrotoxicosis
peptic ulcer of the stomach and duodenum
peritonitis
mechanical obstruction of the gastrointestinal tract and urinary tract
period of acute infectious disease
hyperplasia of the prostate
intoxication in severely weakened children
pregnancy
period of breastfeeding.
Carefully:
It is prescribed with caution against the background of anticholinergics in children (with myasthenia gravis) against the background of neomycin streptomycin kanamycin and other antibiotics with a non-depolarizing effect of local anesthetics and antiarrhythmic agents for general anesthesia and a number of other drugs that violate cholinergic transmission.
Pregnancy and lactation:
Use during pregnancy and breastfeeding is contraindicated.
Method of administration and dosage:
Route of administration : subcutaneously, intramuscularly, intravenously.
The drug should be administered very slowly. A solution of atropine should always be available to eliminate severe cholinergic reactions that occur.
For the treatment of movement disorders after cerebral paralysis during the recovery period after meningitis, poliomyelitis encephalitis : adults are usually prescribed subcutaneously 05-1-2 mg (05 mg - 1 ml of 005% solution) 1-2 times a day, the maximum single dose is 2 mg daily - 6 mg.
The course of treatment (except for myasthenia gravis) is 25-30 days, if necessary, the course of treatment is repeated after a 3-4 week break. Most of the total daily dose is given during the daytime when the patient is most tired.
When myasthenia gravis is administered subcutaneously, 05 mg per day; the course of treatment is long with a change in the route of administration. With the development of myasthenic crisis in adults, 025-05 mg (05-1 ml of solution) is injected intravenously (with 09% sodium chloride solution) Proserin then subcutaneously in usual doses at short intervals.
To enhance the action of Proserin, ephedrine is sometimes injected under the skin in addition 1 ml of a 5% solution 2 times a day.
To stimulate labor, you can inject 05 mg (1 ml of solution) of Proserin under the skin - 1-2 times at intervals of 1 hour, simultaneously with the first injection, 1 mg (1 ml of 01% solution) of atropine is injected once under the skin.
With postoperative intestinal atony of the bladder: for prophylaxis, incl. postoperative urinary retention - subcutaneously or intramuscularly at 025 mg (05 ml solution) of Proserin as early as possible after surgery and again - every 4-6 hours for 3-4 days; treatment of urinary retention - subcutaneously or intramuscularly 05 mg (1 ml of solution) Proserin; if within 1 hour the urine does not leave, catheterization is performed and after emptying the bladder, a total of 5 injections are injected every 3 hours.
When using the drug to stop the action of non-depolarizing muscle relaxants, atropine is preliminarily injected intravenously at a dose of 05-07 mg (05-07 ml of a 01% solution), an increase in pulse is expected, and after 15-2 minutes, 15 mg (3 ml of solution) of Proserin is injected intravenously. If the effect of this dose was insufficient, the same dose is re-administered (when bradycardia appears, an additional injection of atropine is made). In total, you can enter 5-6 mg (10-12 ml of solution) of Proserin within 20-30 minutes. Ensure adequate ventilation during the procedure.
Children with myasthenia gravis (only in hospital!) Subcutaneously at 005 mg (01 ml of 005% solution) for 1 year of life per day but not more than 375 mg (075 ml of 005% solution) per injection. Usually, the drug is prescribed for children once a day, however, if necessary, the daily dose can be divided into two or three doses.
Side effects:
Adverse reactions are grouped according to the damage to organs and organ systems according to the MedDRA dictionary.
Immune system disorders: allergic reactions (facial redness, rash, itching, anaphylaxis).
Disturbances from the nervous system: headache dizziness weakness loss of consciousness drowsiness miosis visual disturbances tremor spasms and twitching of skeletal muscles including twitching of the tongue muscles convulsions dysarthria arthralgia.
Heart disorders: arrhythmias (brady - or tachycardia, atrioventricular block, extrasystole, junctional rhythm), nonspecific changes in the electrocardiogram, sudden cardiac arrest.
Vascular disorders: lowering blood pressure.
Disturbances from the respiratory system of the chest and mediastinal organs: shortness of breath, bronchospasm, respiratory depression up to a stop, increased bronchial tone, increased secretion of bronchial glands.
Disturbances from the gastrointestinal tract: hypersalivation, spastic contraction and increased intestinal motility, nausea, vomiting, flatulence, diarrhea.
Kidney and urinary tract disorders: increased urination.
General disorders and disorders at the injection site: profuse sweating arthralgia.
Overdose:
Symptoms : associated with overexcitation of cholinergic receptors (cholinergic crisis): bradycardia hypersalivation miosis bronchospasm nausea increased intestinal motility diarrhea increased frequency of urination twitching of the muscles of the tongue and skeletal muscles gradual development of muscle weakness decrease in blood pressure.
Treatment : reduce the dose or stop treatment, if necessary, inject atropine (1 ml of 01% solution) methocinium iodide and other anticholinergics. Further treatment is symptomatic.
Interaction:
Neurin and depolarizing muscle relaxants (suxamethonium iodide, etc.) are pharmacologically incompatible, since the direct interaction enhances the effect of suxamethonium iodide. However, in the case of the use of depolarizing muscle relaxants in large doses, after the depolarizing effect, an anti-depolarizing effect ('double block') develops; therefore, it is advisable to prescribe Proserin.
With myasthenia gravis, it is prescribed in combination with glucocorticosteroids and anabolic hormones.
Neosycin weakens or eliminates the effect of non-depolarizing muscle-clasants (atracuria besylate rocuronium bromide, etc.)
M-anticholinergics (atropine methocinium iodide homatropine hydrobromide platifillin and others) ganglion blockers (pachicarpine hydroiodide) quinidine procainamide local anesthetics are pharmacological antagonists of Proserin.
ћежду трициклическими антидепрессантами противоэпилептическими и противопаркинсоническими средствами существует относительный антагонизм.
?ианокобаламин в больших дозах ослабл¤ет действие ѕрозерина.
—нижает активность пиридоксина.
»нгибиторы холинэстеразы в сочетании со стрихнином значительно повышают тонус блуждающего нерва; со слабительными - усиливают их действие; с противоаритмическими препаратами (?-адреноблокаторами) ¤вл¤ютс¤ синергистами (усугубление брадикардии).
Ёфедрин усиливает действие ѕрозерина поэтому при миастенических кризах их ввод¤т вместе.
Ќесовместимость
Ћегко разрушаетс¤ щелочами и окислител¤ми.
ќсобые указани¤:
ѕри парентеральном введении больших доз необходимо (предварительное или одновременное) назначение атропина.
ѕри возникновении во врем¤ лечени¤ миастенического (при недостаточности терапевтической дозы) или холинергического (вследствие передозировки) криза требуетс¤ тщательна¤ дифференциальна¤ диагностика из-за схожести симптоматики.
¬ли¤ние на способность управл¤ть трансп. ср. и мех.:
¬ период лечени¤ необходимо воздерживатьс¤ от управлени¤ транспортными средствами и зан¤тий другими потенциально опасными видами де¤тельности требующими повышенной концентрации внимани¤ и быстроты психомоторных реакций.
‘орма выпуска/дозировка:
–аствор дл¤ инъекций 05 мг/мл.
”паковка:
ѕо 1 мл в ампулы нейтрального стекла с точками надлома или кольцами.
ѕо 10 ампул вместе с инструкцией по применению помещают в коробку из картона.
ѕо 5 ампул в контурную ¤чейковую упаковку из пленки поливинилхлоридной.
2 blister packs, together with instructions for use, are placed in a cardboard box.
Storage conditions:
In a dark place at a temperature not exceeding 25 ? C.
Keep out of the reach of children.
Shelf life:
4 years.
Do not use after the expiration date.
Vacation conditions
On prescription.