Pyridostigmine bromide
Pyridostigmine bromide: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Pyridostigmine bromide
ATX code: N07AA02
Active ingredient: pyridostigmine bromide (Pyridostigmine bromide)
Producer: Federal State Unitary Enterprise Research and Production Center "Pharmzashchita" FMBA of Russia (Russia)
Description and photo update: 2019-21-11
Prices in pharmacies: from 311 rubles.
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Pyridostigmine bromide - cholinesterase inhibitor; slows down the activity of the enzyme acetylcholinesterase, thereby increasing the level of the neurotransmitter acetylcholine in the body.
Release form and composition
The dosage form of the drug is tablets: round, biconvex, almost white, on one of the sides there is a dividing risk (10 pcs. In packs of cell contour made of polyvinyl chloride film, in a cardboard box 5 or 10 packs and instructions for the use of Pyridostigmine bromide)
Composition for 1 tablet:
- active ingredient: pyridostigmine bromide - 60 mg;
- auxiliary components: MCC (microcrystalline cellulose) - 431 mg; pregelatinized starch - 100 mg; povidone - 50 mg; glutamic acid hydrochloride - 2 mg; colloidal silicon dioxide - 3.5 mg; magnesium stearate - 3.5 mg.
Pharmacological properties
Pharmacodynamics
Pyridostigmine bromide is an acetylcholinesterase inhibitor (ACh inhibitor), an indirect cholinomimetic. The accumulation of acetylcholine occurs at receptors in cholinergic synapses, which leads to a more pronounced prolonged effect of acetylcholine. The drug primarily affects the peripheral nervous system. Its active substance does not penetrate the blood-brain barrier, since it has poor lipid solubility, therefore, therapy does not affect the functioning of the central nervous system (central nervous system).
Pyridostigmine bromide improves the transmission of neuromuscular contractions, enhances the peristalsis and tone of the gastrointestinal tract, increases the tone of the bladder and bronchial smooth muscles, the secretion of exocrine glands, and can cause bradycardia.
Pharmacokinetics
After oral administration of pyridostigmine bromide, the maximum plasma concentrations of the substance in the blood are reached after 1 hour 40 minutes - 3 hours 10 minutes. Taking the drug in a dose of 60 mg ensures its plasma content at a level of 40 to 60 ng / ml.
In the process of studying the use of the drug for the treatment of patients with myasthenia gravis, it was found that the maximum concentration of pyridostigmine bromide in the blood is reached after 3 hours. The initial manifestations of neurophysiological and clinical action were noted after 30 minutes and reached a maximum after 2 hours - 2 hours 30 minutes. No clear relationship was found between the dose received and the level of the substance in the blood plasma and / or changes in myasthenic symptoms. However, it was found that after reaching a plasma concentration of more than 100 ng / ml, a further increase in the dose does not increase the clinical efficacy of the drug.
The volume of distribution of the substance in tissues and organs is from 0.5 to 1.7 l / kg of body weight.
Pyridostigmine bromide is metabolized in the liver to form the main metabolite, 3-hydroxy-N-methylpyridine. It is excreted mainly by the kidneys. After parenteral administration, T 1/2 (half-life) from plasma is approximately 1 hour 30 minutes. Oral administration of the drug increases T 1/2 to 3 hours - 3 hours 30 minutes.
Bioavailability due to oral administration of the drug varies from 8 to 20%, and in patients with myasthenia gravis, it can decrease to 4% or less.
Indications for use
Pyridostigmine bromide 60 mg tablets are recommended for the symptomatic treatment of patients with myasthenia gravis.
Contraindications
Absolute:
- bronchial asthma, COB (chronic obstructive bronchitis);
- mechanical intestinal obstruction of various etiologies, intestinal obstruction;
- spastic conditions (spasms of smooth muscles) of the organs of the gastrointestinal tract;
- obstruction or blockage of the biliary tract;
- obstructive uropathy;
- inflammation of the iris of the eye (iritis);
- myotonia of various origins;
- postoperative shock;
- previous administration of depolarizing muscle relaxants (for example, decamethonium bromide, suxamethonium);
- period of pregnancy and lactation;
- children and adolescents up to 18 years old;
- hypersensitivity to pyridostigmine bromide and / or other ingredients of the drug.
Relative contraindications for which the use of Pyridostigmine bromide is recommended with caution are heart failure in the stage of decompensation, acute myocardial infarction, arterial hypotension, impaired renal / hepatic function, gastric ulcer, diabetes mellitus, bradycardia, parkinsonism, cholelithiasis / urolithiasis in the absence of, conditions after intraperitoneal operations on the organs of the gastrointestinal tract, hyperthyroidism.
Patients who have been diagnosed with at least one of the listed diseases or conditions should consult a doctor before taking the drug.
Pyridostigmine bromide, instructions for use: method and dosage
Pyridostigmine bromide tablets are taken orally with water.
The dose of the drug and the duration of therapy, depending on the clinical picture of the disease and the patient's response to the drug, is determined by the attending physician, taking into account the results of a thorough medical examination.
With myasthenia gravis, careful individual selection of the dosage regimen is required.
For the purpose of symptomatic therapy of myasthenia gravis, adult patients can be prescribed from 1 to 3 tablets of Pyridostigmine bromide 3-4 times a day. The daily dose ranges from 180 to 720 mg.
The doses indicated above are recommended, however, the maximum daily dose of 720 mg should not be exceeded.
Side effects
According to the approved information by the WHO (World Health Organization), unwanted adverse reactions are classified according to the frequency of development in this way: very often - at least 10%; often - 1-10%; infrequently - 0.1–1%; rarely - 0.01-0.1%; very rarely - less than 0.01%; with unknown frequency - it is not possible to determine the frequency of occurrence from the available data.
Possible negative side effects from systems and organs due to the use of Pyridostigmine bromide:
- cardiovascular system: with an unknown frequency - arrhythmias (including bradycardia, tachycardia, atrioventricular block), as well as hypotension;
- organ of vision: with an unknown frequency - lacrimation, miosis, violation of the accommodation of the eye;
- respiratory system, chest and mediastinal organs: with an unknown frequency - a combination of bronchospasm with increased secretion of bronchial glands;
- gastrointestinal tract: with an unknown frequency - nausea / vomiting, diarrhea, abdominal pain of a spasmodic nature, gastrointestinal hyperkinesia, hypersalivation (increased salivation);
- skin and subcutaneous fat: with an unknown frequency - a skin rash that goes away on its own soon after the end of therapy; hyperhidrosis (increased sweating);
- musculoskeletal and connective tissue: with an unknown frequency - tremor, myofibrillation, increased muscle weakness, muscle hypotension;
- urinary system: with an unknown frequency - frequent urge to urinate.
These side effects can be both signs of an overdose and relate to the symptoms of a cholinergic crisis, and therefore it is necessary to determine the true cause of the symptoms. In order to eliminate cholinomimetic reactions, if necessary, atropine sulfate is used in a dose of 1-2 mg, subcutaneously, intramuscularly, or slowly intravenously.
In case of aggravation of any side effects indicated in the instructions, or the manifestation of negative reactions not described above, you should consult a doctor.
Overdose
In case of an unintentional overdose of pyridostigmine bromide, you should immediately seek professional medical attention.
Overdose symptoms are increased salivation and / or lacrimation, skin redness, hyperhidrosis, weakness, fatigue, miosis (pupillary constriction), blurred vision, dizziness, nausea / vomiting, uncontrolled urination and defecation, colic, muscle paralysis (as a result of neuromuscular blockade), pulmonary edema, bronchospasm, lowering blood pressure, bradycardia and reflex tachycardia.
In addition, due to intoxication, the development of a cholinergic crisis is possible, the symptoms of which are characterized by pronounced or increasing muscle weakness, up to the patient's life-threatening paralysis of the respiratory center; a strong decrease in blood pressure, up to vascular collapse; a decrease in heart rate, up to a complete cardiac arrest, or a paradoxical increase in heart rate (so-called reflex tachycardia).
In order to treat an overdose with oral administration of pyridostigmine bromide, it is necessary to immediately stop taking the drug, then flush the patient's stomach, give enterosorbents, for example, activated carbon.
When a cholinergic crisis is diagnosed, the drug is immediately canceled and atropine sulfate is slowly injected intravenously at a dose of 1–2 mg. Provides heart rate control. Depending on its value, the injection may be repeated after 2–4 hours. At the same time, they maintain the patency of the airways, do artificial respiration if necessary. In case of cardiac arrest, a set of measures is used to maintain blood circulation (heart massage). Measures are taken to restore the patient's water-salt balance.
special instructions
Pyridostigmine bromide in special cases can be prescribed only after a thorough assessment of the risk of negative side effects and the expected beneficial clinical effect and should be taken with extreme caution in patients with stomach ulcers, bronchial asthma, decompensated heart failure, thyrotoxicosis, epilepsy, as well as in patients who have had myocardial infarction …
It is recommended to use the drug with caution in patients with arrhythmias, bradycardia (decreased heart rate), diabetes mellitus, impaired renal function (if necessary, the dosage regimen is adjusted), parkinsonism, past liver diseases, as well as after intraperitoneal surgery on the organs of the gastrointestinal tract …
After thymectomy (surgical removal of the thymus gland) or additional therapy, such as steroids or immunosuppressants, the need for pyridostigmine bromide is usually significantly reduced.
There is no need to increase the next dose if the previous dose was missed. Treatment should be continued according to the prescribed dosing regimen. Also, you can not stop therapy without first consulting a doctor, since the symptoms of myasthenia gravis may worsen again.
Patients with previous liver diseases need to ensure regular monitoring of its function.
During the entire course of therapy, patients are strictly prohibited from drinking alcohol.
Influence on the ability to drive vehicles and complex mechanisms
Due to the fact that pyridostigmine bromide reduces visual acuity, while taking the drug, one should refrain from driving and working with other complex mechanisms.
Application during pregnancy and lactation
The safety of using pyridostigmine bromide for the treatment of pregnant and breastfeeding women has not been studied.
According to the results of studies carried out on animals, the teratogenic effect of the drug when taken orally was not revealed. The fetotoxic effect of pyridostigmine bromide has been established. It is also known that the administration of anticholinesterase during pregnancy can provoke premature birth. The likelihood of premature delivery is higher in pregnant women taking an ACh inhibitor in the third trimester. In connection with the above, the appointment of the drug during pregnancy is permissible only after a comprehensive assessment of the ratio of the expected beneficial effect for the mother and the potential risk for the development of the fetus.
Since pyridostigmine bromide is secreted into breast milk, the drug should not be used during lactation. If therapy is essential, breastfeeding should be discontinued.
Pediatric use
Pyridostigmine bromide is contraindicated in pediatrics for the treatment of children and adolescents under 18 years of age.
With impaired renal function
With extreme caution, the drug is used to treat patients with previous kidney disease.
Up to 75% of pyridostigmine bromide is excreted unchanged from the body by the kidneys. Therefore, in case of renal failure, the drug is prescribed in lower doses. For patients with a creatinine level of 2 mg / dL, it is recommended to use 1/2 of the maintenance dose, or to double the interval between doses.
For violations of liver function
With extreme caution, the drug is used to treat patients with previous liver diseases.
Drug interactions
Possible pharmacological interaction of Pyridostigmine bromide with other drugs / substances used simultaneously:
- depolarizing muscle relaxants (for example, succinylcholine): their effect is aggravated;
- other cholinesterase inhibitors or cholinomimetics: can enhance the effectiveness of the drug;
- morphine and its derivatives: an increase in their cholinomimetic action is possible;
- atropine: reduces the side effects of pyridostigmine bromide on the myocardium, salivary glands, bronchial muscles, eyes, intestines; does not alter the nicotinergic effect on skeletal muscle;
- methylcellulose: completely inhibits the absorption of the drug;
- activated carbon: almost completely adsorbs pyridostigmine bromide;
- aminoglycosides (kanamycin, streptomycin, neomycin, gentamicin, etc.), polypeptide antibiotics (colistin, polymyxin), some other antibiotics (clindamycin, oxytetracycline, lincomycin), lithium preparations, antiarrhythmic drugs (procainamide, quinidine, propranicilolamine), transenicylamide benzodiazepine series and phenothiazines (chlorpromazine): can weaken the effect of pyridostigmine bromide, which may result in the development of myasthenic symptoms;
- high-dose corticosteroids: may reduce the effect of the drug.
You should definitely inform your doctor about taking other medicines during pyridostigmine bromide therapy.
Analogs
Analogs of Pyridostigmine bromide are Axamon, Ipigrix, Kalimin 60 N, Nivalin, Neuromidin, Proserin-Darnitsa, Proserin, etc.
Terms and conditions of storage
Store at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Pyridostigmine bromide
Currently, myasthenia gravis is considered a fairly common disease with an annual increase in the number of patients in all age groups. It disrupts the ability to work, reduces the quality of life, leads to disability of patients, and in the absence of therapy can cause death. Therefore, pyridostigmine bromide is included in the list of vital and essential drugs (vital and essential drugs).
Previously, drugs produced in other countries were used to treat the disease, which was often the reason for their lack of sale. The Federal State Unitary Enterprise of the Federal Medical and Biological Agency of Russia opened the production of a similar drug in 2017. Due to the recent launch of production, there are few patient reviews of Pyridostigmine bromide, but they are all positive.
Price for Pyridostigmine bromide in pharmacies
The approximate price for Pyridostigmine bromide 60 mg for 50 tablets in a package is 325 rubles; 100 pieces. in the package - 593 rubles.
Pyridostigmine bromide: prices in online pharmacies
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Drug name Price Pharmacy |
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Pyridostigmine bromide 60 mg tablets 50 pcs. RUB 311 Buy |
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Pyridostigmine bromide 60mg tablets 50 pcs. 349 r Buy |
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Pyridostigmine bromide tablets 60mg 100 pcs. RUB 619 Buy |
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Pyridostigmine bromide 60 mg tablets 100 pcs. RUB 619 Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
