Kalimin 60 N, tablets 60 mg 100 pcs.

Pharmacotherapeutic group: cholinesterase inhibitor

ATX code: N07AA02

Pharmacological properties

Pharmacodynamics

Pyridostigmine bromide has a cholinomimetic effect through reversible inhibition of cholinesterase and enhancement of acetylcholine action. It improves neuromuscular transmission, increases gastrointestinal motility, increases bladder and bronchial tone, secretion of exocrine glands, causes bradycardia, mild miosis, spasm of accommodation. It has no central action.

Pharmacokinetics

Bioavailability 8-20%, in myasthenia gravis may decrease to 4%. Time to reach maximum concentration (C_max) in blood plasma is 1.5-3 h, concomitant meal does not reduce bioavailability, but may delay time to maximum concentration. The elimination half-life (T_1/2) is 2.5 h. Does not penetrate the blood-brain barrier. Practically does not bind with plasma proteins. Partially metabolized in the liver to form inactive metabolites. It is excreted unchanged by the kidneys and as metabolites. Average plasma clearance in healthy people is 0.36-0.65 l/kg/h.

Indications

Active ingredient

Composition

How to take, the dosage

Ingestion with plenty of water.

In the initial symptoms of the disease, the recommended dose is ½-1 tablet (30 – 60 mg) 1-2 times a day.

In the progression of the disease, 1-3 tablets (60 – 180 mg) 2-4 times a day.

The maximum daily dose is 12 tablets (720 mg).

The dosing of pyridostigmine bromide in gravis myasthenia gravis is strictly individualized, depending on the severity of the disease and patients’ response to treatment. Therefore, the dose regimens recommended for this indication should be considered indicative.

Patients with impaired renal function

Patients with renal disease are treated with Calimin® 60 N is prescribed in lower doses as pyridostigmine bromide in unchanged form is mainly excreted by kidneys. Therefore, the required dose of the drug is chosen individually for each patient depending on the action of the drug.

Interaction

Special Instructions

Patients are strictly prohibited from drinking alcohol during treatment.

If a patient forgets to take the next dose of medication on time, do not double-dose the medication at the time of the next dose.

The demand for pyridostigmine bromide usually decreases significantly after thymectomy or additional therapy (steroids, immunosuppressants), and therefore the dose of the medication needs to be adjusted.

Influence on the ability to drive vehicles, mechanisms

Pyridostigmine bromide reduces visual acuity, so avoid driving vehicles or other mechanisms during treatment with the drug.

Synopsis

Contraindications

With caution

Arterial hypotension, decompensated heart failure, renal failure, acute myocardial infarction, peptic ulcer, bradycardia, diabetes, parkinsonism, cholelithiasis in absence of obstruction, urolithiasis in absence of obstruction, conditions after gastrointestinal surgery, liver failure, hyperthyroidism.

Side effects

According to the WHO, adverse reactions are classified according to their frequency of occurrence as follows: very common (>1/10), frequent(>1/100 to < 1/10), infrequently (>1/1000 to <1/100), seldom(>1/10,000 to < 1/1000), very rarely (< 1/10,000); frequency unknown (cannot be determined from available data).

immune system disorders

Infrequency unknown – hypersensitivity.

Visual disorders

Prevalence unknown – miosis; lacrimation; accommodation disorders.

Cardiac disorders

Prevalence unknown – arrhythmia (including bradycardia, tachycardia, atrioventricular block).

vascular disorders

Prevalence unknown – decreased blood pressure; syncope.

Disorders of the respiratory system, thorax and mediastinum

Prevalence unknown – increased bronchial gland secretion combined with bronchospasm.

Gastrointestinal tract disorders

Prevalence unknown – nausea; vomiting; diarrhea; spasmodic abdominal pain; gastrointestinal hyperkinesia; increased salivation.

Skin and subcutaneous tissue disorders

Rarely, skin rash (usually disappears soon after stopping treatment).

Prevalence unknown – intense sweating.

Musculoskeletal and connective tissue disorders

Prevalence unknown – increased muscle weakness; tremor and myofibrillation or muscle hypotension.

Recreational and urinary tract disorders

Prevalence unknown – urge to urinate.

The above side effects may be signs of overdose or cholinergic crisis. Therefore, the cause of the symptoms should always be investigated and, if necessary, atropine sulfate should be used to reverse the cholinomimetic effects.

Cholinergic crisis, among other symptoms, may cause an abrupt or gradual increase in myasthenia gravis symptoms to paralysis. There is a danger of developing life-threatening respiratory paralysis. Other concomitant effects accompanied by a decrease in blood pressure may lead to vascular failure, bradycardia and cause cardiac arrest or paradoxical reflex tachycardia. In such case, 1-2 mg of atropine sulfate should be administered after immediate discontinuation of the drug Kalimin® 60 N.

Overdose

Symptoms:. increased secretion of lacrimal, salivary and sweat glands, skin hyperemia, severe weakness, visual disturbance, miosis, dizziness, nausea, vomiting, involuntary defecation and urination, colic, bronchospasm, pulmonary edema, marked or increasing muscle weakness, respiratory muscle paralysis, lower blood pressure, collapse, bradycardia, paradoxical tachycardia or cardiac arrest.

Treatment: The specific antidote is atropine sulfate, which is administered intravenously (slowly) in a dose of 1-2 mg. Depending on pulse rate, if necessary, the initial dose is given again after 2-4 hours. Activated charcoal, other enterosorbents and gastric lavage should also be used. Control of water-electrolyte balance of the body, monitoring of respiration and cardiac activity is necessary. In case of pulmonary failure or cardiac arrest, appropriate resuscitation measures should be performed.

Pregnancy use