M-cholinoblockers (atropine, homatropine hydrobromide, platyphylline, etc.), ganglioblockers (pachycardine hydroiodide), quinidine, novokainamide, and local anesthetics are pharmacological antagonists of neostigmine methyl sulfate.
Proserine : instructions for use
Drugs for the treatment of diseases of the nervous system others. Anticholinesterase drugs. Neostigmine.
Bioavailability of Proserine when given parenterally is high – 0.5 mg of Proserine given parenterally corresponds to 15 mg taken orally. Bioavailability increases with increasing dosage of the drug. Time to reach maximal concentration in blood in intramuscular injection is 30 min. Binding with plasma proteins (albumin) is 15-25%. The drug penetrates poorly through the blood-brain barrier and has no central action. Metabolized in two ways due to hydrolysis at the junction with cholinesterase and microsomal enzymes in the liver. Inactive metabolites are formed in the liver 80% of the administered dose is excreted by the kidneys within 24 hours (of which 50% – unchanged and 30% – as metabolites). Half-life (T1/2) when administered intramuscularly is 51-90 min, when administered intravenously – 53 min.
Proserine-Darnica is a synthetic cholinesterase blocker of reversible action. It has a high affinity to acetylcholinesterase, which is due to its structural similarity to acetylcholine. Proserine (like acetylcholine) first interacts with the catalytic center of cholinesterase, but later, unlike acetylcholine, it forms a stable compound with cholinesterase enzyme due to its carbamine group. Cholinesterase temporarily (several minutes to several hours) loses its specific activity. During this period, the proserine-cholinesterase complex undergoes hydrolysis, as a result of which cholinesterase activity is restored. This action leads to accumulation and enhancement of acetylcholine action in cholinergic synapses. Proserine has pronounced M-cholinomimetic and H-cholinomimetic effects, and has a direct excitatory effect on skeletal muscles.
It causes decrease in heart rate, increases secretion of excretory glands (salivary, bronchial, sweat and digestive tract) and promotes hyper salivation, bronchorrhea, increase in acidity of gastric juice, narrows the pupil, causes accommodation spasm, decreases intraocular pressure, increases tone of intestinal smooth muscle (increases peristalsis and relaxes sphincters) and bladder, causes bronchial spasm, tones skeletal muscle.
The drug is administered subcutaneously in a dose of 0.5-2 mg (1-4 ml) 1-2 times a day. Maximum single dose for adults is 2 mg, daily – 6 mg. Treatment duration (except for myasthenia gravis, myasthenic crisis, postoperative atony of bowel and bladder, myorelaxant overdose) is 25-30 days. If necessary, prescribe a second course in 3-4 weeks. Most of the total daily dose is prescribed in the daytime, when the patient is most tired.
Myasthenia gravis: the drug is administered subcutaneously or intramuscularly in a dose of 0.5 mg (1 ml) per day. The course of treatment is long, with a change of routes of administration.
Myasthenic crisis (with difficulty in breathing and swallowing): the drug is administered intravenously in a dose of 0.25-0.5 mg (0.5-1 ml), then subcutaneously, at short intervals.
Postoperative atony of bowel and bladder, prevention of atony, incl. postoperative urinary retention: the drug is administered subcutaneously or intramuscularly, in a dose of 0.25 mg (0.5 ml), as soon as possible after surgery, and repeatedly every 4-6 hours for 3-4 days.
As an antidote in myorelaxant overdose (after previous injection of atropine sulfate in a dose of 0.6-1.2 mg intravenously, until pulse rate increases to 80 bpm): the drug is administered intravenously slowly in a dose of 0.5-2 mg in 0.5-2 minutes. If necessary, the injections are repeated (including atropine in case of bradycardia) in a total dose of no more than 5-6 mg (10-12 ml) for 20-30 minutes. Artificial lung ventilation is provided during the procedure.
In children (in hospital only), 0.05 mg (0.1 ml of 0.05% solution) per 1 year of life per day, but not more than 3.75 mg (0.75 ml of 0.05% solution) per 1 injection.
The drug is administered subcutaneously in a dose of 0.5-2 mg (1-4 ml) 1-2 times a day. Maximum single dose for adults is 2 mg, daily dose is 6 mg. Treatment duration (except for myasthenia gravis, myasthenic crisis, postoperative atony of bowel and bladder, myorelaxant overdose) is 25-30 days. If necessary, prescribe a second course in 3-4 weeks. Most of the total daily dose is prescribed in the daytime, when the patient is most tired.
Myasthenia gravis: the drug is administered subcutaneously or intramuscularly in a dose of 0.5 mg (1 ml) per day. The course of treatment is long, with a change of routes of administration.
Myasthenic crisis (with difficulty in breathing and swallowing): the drug is administered intravenously in a dose of 0.25-0.5 mg (0.5-1 ml), then subcutaneously, at short intervals.
Postoperative bowel and bladder atony, prevention of atony, including postoperative urinary retention: the drug is administered subcutaneously or intramuscularly, in a dose of 0.25 mg (0.5 ml), as soon as possible after surgery, and repeatedly – every 4-6 hours for 3-4 days.
As an antidote in myorelaxant overdose (after previous injection of atropine sulfate in a dose of 0.6-1.2 mg intravenously, until pulse rate increases to 80 bpm): the drug is administered intravenously slowly in a dose of 0.5-2 mg in 0.5-2 minutes. If necessary, the injections are repeated (including atropine in case of bradycardia) in a total dose of no more than 5-6 mg (10-12 ml) for 20-30 minutes. Artificial lung ventilation is provided during the procedure.
For children (in hospital only) – 0.05 mg (0.1 ml of 0.05% solution) per 1 year of life per day, but not more than 3.75 mg (0.75 ml of 0.05% solution) per 1 injection.
Side effects
– hyper salivation, nausea, vomiting, diarrhea spastic stomach contraction, increased intestinal peristalsis, flatulence, involuntary emptying
-arrhythmia, brady- or tachycardia, atrioventricular block, nodal rhythm, nonspecific changes on ECG, cardiac arrest, decreased blood pressure
– Headache, dizziness, loss of consciousness, weakness, drowsiness, tremors, seizures, spasms and twitching of skeletal muscles, including muscles of tongue and throat, numbness of legs, dysarthria
– Rashes, itching, hyperemia, urticaria, allergic reactions, including anaphylactic shock
Contraindications
- Hypersensitivity to the drug components
- epilepsy
- hyperkinesias
- vagotomy
- coronary artery disease
- angina pectoris, arrhythmias, bradycardia
- bronchial asthma
- significant atherosclerosis
- thyrotoxicosis
- gastric and duodenal ulcer
- peritonitis
- mechanical obstruction of the gastrointestinal tract and urinary tract
- Prostate hypertrophy accompanied by difficulty urinating
- Acute period of infectious disease
- Intoxication in severely weakened children
- Pregnancy and lactation
In myasthenia gravis is prescribed in combination with aldosterone antagonists, glucocorticosteroids and anabolic hormones. Atropine, methacin and other m-cholinoblockers weaken the m-cholinomimetic effects. Prolongs and enhances the effects of depolarizing myorelaxants, weakens or eliminates the effects of antidepolarizing ones. Caution is used simultaneously with neomycin, streptomycin, kanamycin, which have antidepolarizing effects. Concomitant use with local and some general anesthetics, antiarrhythmic drugs that disrupt cholinergic transmission may lead to weakening of the effects of Proserine. Organic nitrates reduce the effectiveness of Proserine.
Simultaneous use of Proserine with beta-adrenoblockers may increase bradycardia.
Cautions
Caution should be exercised when adjusting the dose of Proserine taking into account possible high individual sensitivity to it.
Use with caution in arterial hypotension, heart rhythm disorders, especially in bradycardia, with predominant tone n.vagus, hyperthyroidism, Addison's disease, gastric and duodenal ulcers, anticholinergic agents, children with myasthenia gravis who use antibacterial drugs with antidepolarizing effect (neomycin, streptomycin, kanamycin, etc.), local and general anesthetics, antiarrhythmic drugs that disrupt cholinergic transmission.
If large doses of Proserine are used, atropine sulfate should be administered before or at the same time.
Because of the coincidence of clinical symptoms of myasthenic crisis (in case of insufficient therapeutic dose of the drug) and cholinergic crisis (as a consequence of Proserine overdose) a careful differential diagnosis is necessary.
During treatment it is prohibited to drive vehicles and engage in other potentially dangerous activities that require high concentration and psychomotor reaction rate.
Children are used subcutaneously (only in hospital conditions) in doses specified in section "Dosage and administration".
Side effects
Adverse reactions are classified according to the classification of lesions of organs and organ systems according to the MedDRA Dictionary.
Immune system disorders: Allergic reactions (facial redness, rash, itching, anaphylaxis).
Nervous system disorders: Headache, dizziness, weakness, loss of consciousness, drowsiness, miosis, visual disturbances, tremor, spasms and twitching of skeletal muscles, including twitching of the tongue muscles, seizures, dysarthria, arthralgia.
Cardiac disorders: bradycardia, tachycardia, atrioventricular block, extrasystole, nodal rhythm, nonspecific electrocardiogram changes, sudden cardiac arrest.
Vascular disorders: decreased blood pressure.
Respiratory system, thorax and mediastinum disorders Dyspnea, bronchospasm, respiratory depression up to and including respiratory arrest, increased bronchial tone, increased secretion of bronchial glands.
Gastrointestinal tract disorders: Hyper salivation, spastic contraction and increased intestinal peristalsis, nausea, vomiting, flatulence, diarrhea.
Renal and urinary tract disorders: Increased frequency of urination.
General disorders and disorders at the injection site: profuse sweating, arthralgia.
Overdose .
Symptoms: Hyper salivation, profuse sweat, abdominal pain, diarrhea, difficulty breathing, bradycardia, cyanosis, miosis, skeletal muscle twitching, muscle weakness.
Treatment: The drug administration should be stopped and atropine (1 ml of 0.1% solution under the skin) or other cholinoblockers should be administered immediately. In cases of severe poisoning with Proserine, atropine sulfate shall be administered at 10 minute intervals up to 3 times (until dry mouth). If seizures occur, intravenous administration of sodium thiopental under medical supervision.
Proserine shots for what cats are prescribed
To stimulate bladder function, proserine was prescribed in a dosage of 1 ml. (0.5 preparations + 0.5 saline) subcutaneously 1 p.d. Today I put it in. The cat almost died. Started with heavy salivation, then vomiting, uncontrollable urination, cramps, vomiting again, though no more. After two hours, the cat recovered a little. The cat is 12 years old, weighs 3 kg, neuter. Who knows, please tell me if it is an individual intolerance or overdose?
Yes, it could be. P. the drug is heavy, side effects of this kind can be, alas. Any doctor will tell you that in case of such a reaction the drug should be discontinued. Consult your doctor, there is also Neuromidin, which has a similar effect, maybe you should try it.
And, if it is not a secret, what is the reason for the stimulation of the urinary tract? Trauma?
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You should prescribe Proserine in small doses, gradually increasing (if necessary) and then gradually decreasing.
0.5 ml is a lot, in my opinion, for 3 kg of weight.
If you can't do without the medication, you should start with at least 0.2 ml.
About bladder stimulation:
When the cat was sick, he peed rarely, sparingly and with blood. He ate and drank almost nothing. Urinalysis showed severe inflammation, the clinic explained it was a kind of cystitis. Antibiotic injections and pills were administered. After six days of treatment, the cat was almost cured: his urine was normal, he began to eat and drink water well, but he urinated once every other day. At the last appointment at the clinic he was prescribed 10 injections of Proserine 1 ml subcutaneously 1 p.d., the first injection was given and it was explained that the cat's bladder contracted badly, and Proserine would stimulate its work. After the first shot, there was abundant salivation for an hour and that was it. But after the second one. It has been 13 hours and the cat is still not himself.
Hold on! Or I am an idiot, or why Prozerin… This is the first time I have seen Prozerin prescribed for IBC or cystitis(?). olenka12, give me the tests and the scheme of treatment, it seems to me that the appointments are incorrect.
Terms of sale
You can buy Proserine by prescription, the doctor writes a prescription in Latin.
When administered parenterally in large doses, Atropine should be given at the same time or in advance.
If myasthenic crisis (due to insufficient dose) or cholinergic crisis (due to overdose) develops during treatment, a careful differential diagnosis should be made due to the similarity of signs.
It is recommended to refrain from driving motor transport and other hazardous activities that require maximum concentration.
Proserine analogues
The analogue of this drug is the remedy Neostigmine methyl sulfate.. Analogue drugs by the mechanism of action are Armin, Amiridin, Deoxypeganine hydrochloride, Ubretide, Oxazyl.
For the treatment of children, Prozerin is recommended in the form of pellets that are dissolved in water beforehand. Children under 10 years of age are indicated to take 1 mg of the drug per day for each year of life. Electrophoresis with Proserine is also practiced in children under the supervision of a doctor.
When is Proserine used?
It is recommended to inject Proserine in the following situations:
- Muscle weakening. Nervous disorders can cause the animal to become significantly weaker and may lose not only weight but also activity. The cat often does not have enough strength even to get up. An injection of Proserine stimulates the muscles.
- The solution is prescribed to eliminate the effects of brain injuries. Street cats often suffer serious head injuries, and it is also a frequent cause of mutilation in careless kittens. The doctor prescribes the drug to restore motor function and to treat after a stroke.
- Veterinarians recommend buying Proserine to correct vision problems. The optic nerve can become inflamed, which is fraught with complete loss of function. The drug helps to minimize the risks and get hope for a full recovery.
- The main use of Proserine for veterinary purposes is to stimulate the tone of the bowel and bladder muscles. The dosage of Proserine for cats with atony is minimal, but it is enough to guarantee a stable and safe rehabilitation.
One option is to buy the drug for treatment "after treatment". Some potent medications have a negative effect on the body, leading to toxicity. Proserine mitigates the effects and protects against contraindications.
What you need to know about contraindications
Proserine is not recommended as a permanent medication. It is fraught with complications, which may include the following contraindications:
- Prozerin contains an active ingredient in its composition. Not every cat can withstand such a load. This is especially true for mature individuals, whose immunity is weakened.
- The drug is prohibited for use in epilepsy and other diseases that lead to increased and spontaneous activity of the skeletal muscles.
- Cats with cardiovascular problems should also not come into contact with the medicine. Excessive stimulation is dangerous.
Even a small amount of mL once a year is dangerous if the cat's body is prone to severe intoxication. Consultation with a veterinarian and a full examination of the chemical composition will help prevent the risks.
Instructions for the use of Proserine for cats involves the purchase of the drug in ampoules. The solution is sold in the form of 10 ampoules of 1 ml. It is administered subcutaneously and intravenously.
The best way is to ask the veterinarian. The drug can be administered routinely at the clinic or at home: special veterinary services are available for this purpose.
