Pharma action:
Kalimin 60 N has a cholinomimetic effect due to reversible inhibition of cholinesterase and increased action of acetylcholine. It improves neuromuscular transmission, enhances gastrointestinal motility, increases the tone of the bladder, bronchi, secretion of exocrine glands, causes bradycardia, mild miosis, spasm of accommodation.
Does not have a central effect.
Indications:
myasthenia gravis.
Contraindications:
– previous administration of depolarizing muscle relaxants (suxamethonium, decamethonium);
– iritis;
– chronic obstructive bronchitis;
– bronchial asthma;
– mechanical intestinal obstruction;
– obstruction of the biliary and urinary tract;
– spastic conditions of the digestive tract;
– myotonia;
— shock in the postoperative period;
– pregnancy;
– lactation period;
– age up to 18 years;
– hypersensitivity to the components of the drug Kalimin 60 N.
Carefully:
Arterial hypotension, decompensated heart failure, renal failure, acute myocardial infarction, gastric ulcer, bradycardia, diabetes mellitus, parkinsonism, cholelithiasis in the absence of obstruction, urolithiasis in the absence of obstruction, condition after gastrointestinal surgery, liver failure, hyperthyroidism.
Dosing:
Inside, drinking water.
With the initial symptoms of the disease – 1/2-1 tablet (30-60 mg) 1-2 times / day.
With the progression of the disease – 1-3 tablets (60-180 mg) 2-4 times / day.
The maximum daily dose is 12 tablets (720 mg).
Dosing of pyridostigmine bromide in myasthenia gravis is carried out strictly individually, depending on the severity of the disease and the patient’s response to treatment. Therefore, the dosage regimens recommended for this indication should be considered indicative.
For patients with kidney disease, the drug is prescribed in lower doses, because. Pyridostigmine bromide is excreted unchanged from the body mainly by the kidneys. Therefore, the necessary dose of the drug is selected individually for each patient, depending on the effect of the drug.
Side effect:
Allergic reactions, increased sweating, increased salivation and lacrimation, increased secretion of bronchial glands, nausea, vomiting, diarrhea, cramping abdominal pain due to increased intestinal motility, frequent urination, muscle tremors, skeletal muscle spasms, muscle weakness and accommodation disorders.
When using the drug Kalimin 60 N in higher doses, bradycardia and a decrease in blood pressure may develop. In very rare cases, skin rashes appear.Pharmacokinetics:
Bioavailability 8-20%, with myasthenia gravis can be reduced to 4%. The time to reach Cmax is 1.5-3 hours; simultaneous food intake does not reduce bioavailability, but may delay the time to reach Cmax. T1 / 2 – 2.5 hours
Does not penetrate the blood-brain barrier. Practically does not bind to plasma proteins. Partially metabolized in the liver to inactive metabolites. Excreted by the kidneys unchanged and as metabolites. The average plasma clearance in healthy people is 0.36-0.65 l / kg / h.
Overdose:
Symptoms: increased secretion of the lacrimal, salivary and sweat glands, skin flushing, severe weakness, blurred vision, miosis, dizziness, nausea, vomiting, involuntary defecation and urination, intestinal colic, bronchospasm, pulmonary edema, severe or increasing muscle weakness, paralysis of the respiratory muscles , decreased blood pressure, collapse, bradycardia, paradoxical tachycardia or cardiac arrest.
Treatment: the specific antidote is atropine, which is administered intravenously (slowly) at a dose of 1-2 mg. Depending on the pulse rate, if necessary, the initial dose is administered again after 2-4 hours. Activated charcoal, other enterosorbents and gastric lavage should also be used. It is necessary to control the water and electrolyte balance of the body, monitor respiration and cardiac activity. In case of pulmonary insufficiency or cardiac arrest, appropriate resuscitation measures must be carried out.
Interaction:
Atropine weakens the m-cholinomimetic effect of pyridostigmine bromide (bradycardia and hypersecretion), but not its effect on skeletal muscles.
Pyridostigmine bromide enhances the action of depolarizing muscle relaxants, morphine and its derivatives, barbiturates.
Incompatible with ethanol.
M-anticholinergics, ganglioblockers, quinidine, procainamide, local anesthetics, tricyclic antidepressants, antiepileptic and antiparkinsonian drugs reduce the severity of the action of pyridostigmine bromide.
Special instructions:
During treatment, patients are strictly forbidden to drink alcohol.
If the patient forgot to take the next dose of the drug in a timely manner, do not take a double dose of the drug during the next dose.
Influence on the ability to drive vehicles and control mechanisms
During the period of treatment, care should be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Category of action on the fetus:
Pyridostigmine bromide is not teratogenic, but has fetotoxicity. The drug can cause premature birth, especially when used in the last weeks of pregnancy.
Pyridostigmine bromide passes into breast milk. When prescribing Kalimin 60 N, breastfeeding should be interrupted.
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