Instructions Prozerin-Darnitsa solution for injection 0.5 mg/ml ampoule 1 ml No. 10
Composition
active ingredient: neostigmine methylsulphate;
1 ml of solution contains 0.5 mg of proserin;
excipient: water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: clear colorless liquid.
Pharmacotherapeutic group
Anticholinesterase agents. ATX code N07A A01.
Pharmacological properties
Pharmacodynamics.
Proserin-Darnitsa is a synthetic cholinesterase blocker of reversible action. It has a high affinity for acetylcholinesterase, due to its structural identity with acetylcholine. Like acetylcholine, proserin initially interacts with the catalytic center of cholinesterase, but later, unlike acetylcholine, it forms, due to its carbamine group, a stable compound with the enzyme. The enzyme temporarily (from several minutes to several hours) loses its specific activity. After this time, due to the slow hydrolysis of proserin, cholinesterase is released from the blocker and restores its activity. This action leads to the accumulation and enhancement of the action of acetylcholine in cholinergic synapses. Proserin has a pronounced muscarinic and nicotinic action, and has a direct excitatory effect on skeletal muscles.
Causes a decrease in heart rate, increases secretion of excretory glands (salivary, bronchial, sweat, and digestive tract) and contributes to the development of hypersalivation, bronchorrhea, increased acidity of gastric juice, constricts the pupil, causes accommodation spasm, reduces intraocular pressure, increases the tone of smooth muscles of the intestine (increases peristalsis and relaxes sphincters) and bladder, causes bronchial spasm, tones skeletal muscles.
Pharmacokinetics.
The bioavailability of proserin when administered parenterally is high - 0.5 mg of proserin administered parenterally corresponds to 15 mg taken orally. With an increase in the dose of the drug, bioavailability increases. The time to reach maximum concentration in the blood when administered intramuscularly is 30 minutes. The connection with proteins (albumin) of blood plasma is 15-25%. The drug penetrates poorly through the blood-brain barrier and has no central action. It is metabolized in two ways: by hydrolysis at the site of connection with cholinesterase and microsomal liver enzymes. Inactive metabolites are formed in the liver. 80% of the administered dose is excreted by the kidneys within 24 hours (of which 50% - in an unchanged state and 30% - in the form of metabolites). The half-life (T1/2) for intramuscular administration is 51-90 minutes, for intravenous administration – 53 minutes.
Indication
Myasthenia, acute myasthenic crisis; motor disorders after brain injury; paralysis; recovery period after meningitis, poliomyelitis, encephalitis; neuritis, optic nerve atrophy; intestinal atony, bladder atony; elimination of residual phenomena after blockade of neuromuscular transmission with non-depolarizing muscle relaxants.
Contraindication
Hypersensitivity to the active substance or to other components of the drug; epilepsy; hyperkinesia; vagotomy; ischemic heart disease; angina pectoris; arrhythmias; bradycardia; bronchial asthma; severe atherosclerosis; thyrotoxicosis; gastric and duodenal ulcers; peritonitis; mechanical obstruction of the gastrointestinal tract and urinary tract; prostatic hypertrophy accompanied by dysuria; acute period of infectious disease; intoxication in severely weakened children, simultaneous use with depolarizing muscle relaxants.
Interaction with other medicinal products and other types of interactions
When using the drug simultaneously with other drugs, it is possible:
with drugs for local anesthesia and some general anesthetics, antiarrhythmic drugs, organic nitrates, tricyclic antidepressants, antiepileptic drugs, antiparkinsonian drugs, guanethidine - reduced effectiveness of Prozerin;
with m-cholinoblockers – weakening of the m-cholinomitemic effects of proserin;
with depolarizing muscle relaxants – prolongation and enhancement of the latter's action;
with antidepolarizing muscle relaxants – weakening of the action of the latter. Prozerin should be used as an antidote in case of overdose with antidepolarizing muscle relaxants;
with other anticholinesterase drugs - increased toxicity;
with m-cholinomimetics – digestive tract dysfunction, toxic effect on the nervous system;
with β-blockers – increased bradycardia;
with ephedrine – potentiation of the action of proserin.
Use with caution when administered simultaneously with neomycin, streptomycin, kanamycin.
For myasthenia gravis, prescribe in combination with aldosterone antagonists, glucocorticosteroids, and anabolic hormones.
Application features
If a myasthenic (at insufficient therapeutic dose) or cholinergic (due to overdose) crisis occurs during treatment, further use of the drug requires careful differential diagnosis due to the similarity of symptoms.
Before medical or dental treatment, or surgery, you must inform your doctor about taking Prozerin.
The drug should be prescribed with special caution to patients after intestinal and bladder surgeries, and to patients with Parkinson's disease.
Use during pregnancy or breastfeeding
Strictly controlled studies on the use of the drug in pregnant women have not been conducted. Use is possible only if the benefit to the mother outweighs the possible risk to the fetus. If necessary, the use of Prozerin should stop breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
During treatment with the drug, it is contraindicated to drive vehicles and engage in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
Method of administration and doses
Adults.
The drug is administered subcutaneously at a dose of 0.5-2 mg (1-4 ml) 1-2 times a day. The maximum single dose for adults is 2 mg, daily dose is 6 mg. The duration of the course of treatment (except for myasthenia gravis, myasthenic crisis, postoperative atony of the intestine and bladder, overdose with muscle relaxants) is 25-30 days. If necessary, a repeated course is prescribed after 3-4 weeks. Most of the total daily dose is prescribed during the daytime, when the patient is most tired.
Myasthenia gravis: the drug is administered subcutaneously or intramuscularly at a dose of 0.5 mg (1 ml) per day. The course of treatment is long, with a change in the route of administration.
Myasthenic crisis (with difficulty breathing and swallowing): the drug is administered intravenously at a dose of 0.25-0.5 mg (0.5-1 ml), then subcutaneously, at short intervals.
Postoperative intestinal and bladder atony, prevention, including postoperative urinary retention: the drug should be administered subcutaneously or intramuscularly, at a dose of 0.25 mg (0.5 ml), as early as possible after surgery, and repeatedly every 4-6 hours for 3-4 days.
As an antidote for muscle relaxant overdose (after prior administration of atropine sulfate at a dose of 0.6-1.2 mg intravenously, until the pulse rate increases to 80 beats/min): administer the drug intravenously slowly at a dose of 0.5-2 mg after 0.5-2 minutes. If necessary, repeat the injection (including atropine in case of bradycardia) with a total dose of no more than 5-6 mg (10-12 ml) for 20-30 minutes. During the procedure, artificial ventilation of the lungs should be provided.
Children (only in a hospital setting).
Myasthenia gravis:
Newborns: at the initial stage, the drug is prescribed in a dose of 0.1 mg as an intramuscular injection. After that, the dose is selected individually, usually 0.05-0.25 mg or 0.03 mg/kg of body weight of the drug intramuscularly every 2-4 hours. Due to the special nature of the disease in newborns, the daily dose of the drug can be reduced even to complete cancellation.
Children under 12 years of age: 0.2-0.5 mg by injection as needed. The dosage of the drug should be adjusted according to the patient's response.
As an antidote for muscle relaxant overdose (after prior administration of atropine sulfate at a dose of 0.02-0.03 mg/kg body weight intravenously, until the pulse rate increases to 80 beats/min): the drug should be administered intravenously slowly at a dose of 0.05-0.07 mg/kg body weight over 1 minute. The maximum recommended dose in children is 2.5 mg.
Other indications: The drug is prescribed in a dose of 0.125-1 mg by injection. The doses can be adjusted according to the individual needs of the patient.
Children.
The medicine can be used in children only in a hospital setting.
Overdose
Symptoms: associated with overexcitation of cholinergic receptors (cholinergic crisis): tachycardia, bradycardia, hypersalivation, difficulty swallowing, miosis, bronchospasm, difficulty breathing, nausea, vomiting, increased peristalsis, diarrhea, increased urination, coordination disorders, twitching of the tongue and skeletal muscles, cold sweat, gradual development of general weakness, paralysis, decreased blood pressure, anxiety, panic. Very high doses can cause agitation, impatience. Fatal outcome can occur due to cardiac arrest or respiratory paralysis, pulmonary edema. In patients with myasthenia gravis, in whom overdose is more likely, muscle twitching and parasympathomimetic effects may be absent or weakly expressed, which complicates the differential diagnosis of overdose with myasthenic crisis.
Treatment: reduce the dose or discontinue the drug. If necessary, administer atropine (1 ml of 0.1% solution), metacin. Further treatment is symptomatic.
Side effects
On the part of the organs of vision: miosis, visual impairment.
On the part of the gastrointestinal tract: hypersalivation, spastic contraction and increased intestinal peristalsis, nausea, vomiting, flatulence, diarrhea, involuntary defecation.
Renal and urinary disorders: increased urination, involuntary urination.
From the nervous system: headache, dizziness, fainting, weakness, drowsiness, tremor, convulsions, spasms and twitching of skeletal muscles, including the muscles of the tongue and larynx, numbness of the legs, dysarthria.
From the cardiovascular system: arrhythmia, bradycardia or tachycardia, atrioventricular block, atrioventricular nodal rhythm, nonspecific ECG changes, cardiac arrest, decreased blood pressure (mainly with parenteral administration).
On the part of the immune system: rash, itching, hyperemia, urticaria, allergic reactions, including anaphylactic shock.
General disorders and administration site conditions: increased sweating, feeling hot, lacrimation, arthralgia, injection site disorders including hyperemia, itching, skin edema.
Expiration date
4 years.
Do not use the medicine after the expiry date stated on the packaging.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 ° C. Do not freeze.
Keep out of reach of children.
Incompatibility
Prozerin should not be mixed in the same syringe with alkaline solutions and oxidizing agents, as this leads to its destruction.
Packaging
1 ml in an ampoule; 5 ampoules in a contour blister pack; 2 contour blister packs in a pack.
Vacation category
According to the recipe.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Address
Ukraine, 02093, Kyiv, Boryspilska St., 13.
