Pyridostigmine bromide (Pyridostigmine bromide)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substancePyridostigmine bromidePyridostigmine bromide
Dosage form: & nbspTabletki.
Composition:For one tablet:

active substance: pyridostigmine bromide - 60 mg;

Excipients: cellulose microcrystalline - 431 mg, pregelatinized starch - 100 mg, povidone - 50 mg, glutamic acid hydrochloride - 2 mg, silicon dioxide colloid - 3,5 mg, magnesium stearate - 3,5 mg.

Description:

The tablets are almost white in color, round in shape, biconvex, with a risk on one side.

Pharmacotherapeutic group:cholinesterase inhibitor
ATX: & nbsp

N.07.A.A.02   Pyridostigmine bromide

Pharmacodynamics:

Pyridostigmine bromide inhibits cholinesterase. Refers to holinomimetikam not direct action. Inhibition of the enzyme promotes the accumulation of acetylcholine on the receptors in the cholinergic synapses, leading to a more pronounced and long-term effect of acetylcholine. The drug mainly acts on the peripheral nervous system. It does not affect the functions of the central nervous system, because it does not penetrate the blood-brain barrier because of low lipid solubility.

Pharmacokinetics:

Maximum plasma concentrations are achieved 1.7-3.2 hours after taking pyridostigmine bromide. After taking 60 mg of pyridostigmine bromide, the plasma level is 40-60 ng / ml. In studies in patients with myasthenia gravis, maximum blood levels are reached after 3 hours, and manifestations of clinical and neurophysiological effects were observed after 30 minutes and reached a maximum after 120-150 minutes. There is no clear relationship between dose and plasma concentration / plasma level or changes in myasthenic symptoms. However, at levels above 100 ng / ml the effectiveness of the drug does not increase.

The volume of distribution of pyridostigmine bromide is approximately 0.5-1.7 l / kg body weight.

Pyridostigmine bromide is metabolized in the liver. The main metabolite is 3-hydroxy-Nmethylpyridine. It is excreted mainly by the kidneys, after the introduction the half-life period from the plasma is about 1.5 hours. After oral administration, the elimination half-life increases to 3-3.5 hours. Bioavailability of pyridostigmine bromide after oral administration ranged from 8% to 20%. In patients with myasthenia gravis, bioavailability can decrease below 4%.

Indications:

Myasthenia gravis (gravis).

Contraindications:

- Hypersensitivity to pyridostigmine bromide and other components of the drug;

- previous administration of depolarizing muscle relaxants (suxamethonium, decamethonium bromide);

- irit;

- chronic obstructive bronchitis, bronchial asthma;

- Obturation (mechanical) intestinal obstruction;

- obstruction of the bile-excreting and urinary tract;

- spastic conditions of the gastrointestinal tract;

- myotonia;

- shock in the postoperative period;

- pregnancy;

- lactation period;

- age to 18 years.

Carefully:

- Arterial hypotension;

- Decompensated heart failure;

- kidney failure;

- acute myocardial infarction;

- stomach ulcer;

- bradycardia;

- diabetes;

- Parkinsonism;

- cholelithiasis in the absence of obstruction;

- urolithiasis in the absence of obstruction;

- state after operations on the gastrointestinal tract;

- liver failure;

- hyperthyroidism.

If you have one of the listed diseases (conditions), before taking the drug always consult a doctor.

Pregnancy and lactation:

The safety of the use of pyridostigmine bromide during pregnancy and during breastfeeding has not been studied. The use of the drug in animal studies did not reveal a teratogenic effect when administered orally. The drug does not have teratogenic effects, but it has fetotoxicity. It is known that the administration of anticholinesterase during pregnancy can cause premature birth. The risk of premature birth is higher when taking the drug in the III trimester of pregnancy. Therefore, the drug should be used only after a thorough assessment of the risk ratio and the expected beneficial effect.

Pyridostigmine bromide penetrates into breast milk, so pyridostigmine bromide should not be used during lactation. In cases where the use of the drug is necessary, breastfeeding should be discontinued.

Dosing and Administration:

Inside, washing down with water.

The dose and duration of treatment is determined by the doctor depending on the course of the disease and the patient's response to treatment.

Myasthenia gravis

For symptomatic treatment of myasthenia gravis in adults, it is recommended to use 1-3 tablets of the drug Pyridostigmine bromide 3-4 times a day (180-720 mg per day).

Patients with myasthenia gravis require careful individual selection of the dose depending on the course of the disease and the patient's response to treatment. The above doses are only recommendations, but do not exceed the maximum daily dose of 720 mg.

Treatment of patients with kidney disease

Patients with kidney disease should be prescribed at low doses, because pyridostigmine bromide in unchanged form is excreted from the body mainly by the kidneys (75%). At a creatinine level of 2 mg / dl, a half maintenance dose should be used, or the interval between doses should be doubled accordingly. Therefore, the necessary dose should be selected individually for each patient, depending on the response to therapy with the drug. A thorough medical examination is recommended.

Side effects:

According to WHO, undesirable side effects are classified according to their developmental frequency as follows: very often (≥1/10), often (from ≥1 / 100 to <1/10), infrequently (from ≥1 / 1000 to < 1/100), rarely (from ≥1 / 10,000 to <1/1000), very rarely (<1/10 000); frequency is not known - according to available data, it is not possible to establish the frequency of occurrence.

From the side of the organ of vision: frequency is not known: miosis, lacrimation, violation of accommodation;

From the heart: frequency is not known: arrhythmia (including bradycardia, tachycardia, AV blockade), as well as hypotension;

On the part of the respiratory system, the organs of the thorax and the mediastinum: frequency is not known: increased secretion of bronchial glands in combination with bronchospasm;

From the gastrointestinal tract: frequency not known: nausea, vomiting, diarrhea, abdominal cramping, gastrointestinal hyperkinesia, increased salivation;

From the skin and subcutaneous tissues: frequency is not known: skin rash (usually disappears soon after cessation of treatment), intense sweating;

From the side of the musculoskeletal and connective tissue: frequency is not known: increased muscle weakness, tremor and myofibrillation, or muscle hypotension;

From the side of the kidneys and urinary tract: frequency is not known: urge to urinate.

These undesirable reactions may be signs of an overdose or cholinergic crisis. Therefore, it is necessary to find out the cause of the symptoms and, if necessary, apply 1-2 mg of atropine sulfate by subcutaneous, intramuscular or slow administration to eliminate cholinomimetic effects.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, inform the doctor about it.

Overdose:

In case of an accidental overdose of Pyridostigmine with bromide, it is necessary to immediately seek help from a doctor.

Symptoms of intoxication. Salivation, lacrimation, redness of the skin, increased sweating, fatigue, weakness, narrowing of the pupils, impaired vision, dizziness, nausea, vomiting, involuntary urination and defecation, colic and muscle paralysis (as a consequence of neuromuscular blockade), bronchospasm, pulmonary edema, decrease AD, bradycardia, reflex tachycardia is possible.

Overdose can cause the development of a cholinergic crisis, which is characterized by a pronounced or increasing muscle weakness, including paralysis of the respiratory system, which threatens the patient's life. Other concomitant phenomena may be a decrease in blood pressure to vascular collapse, as well as a reduction in the heart rate to complete cardiac arrest, or a paradoxical increase in the heart rate (reflex tachycardia).

Treatment of overdose. The drug should be immediately canceled. It is necessary to wash the stomach and take activated charcoal. In cases of a cholinergic crisis, the drug should be immediately withdrawn and intravenously injected slowly atropine sulfate in an amount of 1-2 mg. Depending on the pulse rate, the introduction of atropine sulfate after 2-4 hours can be repeated. It is necessary to maintain airway patency and, if necessary, provide artificial respiration.

In case of cardiac arrest, cardiac massage should be performed. Restore the water and electrolyte balance. After oral administration of pyridostigmine bromide - gastric lavage and the use of enterosorbents.

Interaction:

The combination with other cholinesterase inhibitors or cholinomimetics can enhance the action of pyridostigmine bromide.

The drug is able to enhance the cholinomimetic effects of morphine and its derivatives.

Increases the effect of depolarizing muscle relaxants (eg, succinylcholine).

Atropine weakens the side effects of pyridostigmine bromide on the salivary glands, eyes, heart, bronchial muscles and intestines. In this case, nicotinergic effects on skeletal muscles remain unchanged.

Methylcellulose completely inhibits the absorption of pyridostigmine bromide, and Activated carbon almost completely adsorbs it.

Aminoglycosides (for example, streptomycin, neomycin, kanamycin, gentamicin), polypeptide antibiotics (polymyxin, colistin), some other antibiotics, for example, oxytetracycline, clindamycin and lincomycin, numerous antiarrhythmics (quinidine, procainamide, propranolol), penicillamine, lithium, benzodiazepine type tranquilizers and phenothiazines (for example, chlorpromazine) can weaken the effect of pyridostigmine bromide and, as a result, cause myasthenic symptoms.

High doses of corticosteroids can also weaken the effect of pyridostigmine bromide.

In the event that you take other medicines, before taking the drug always consult a doctor.

Special instructions:

Only after a thorough risk assessment and the expected favorable effect pyridostigmine bromide can be prescribed to patients with bronchial asthma, gastric ulcer, thyrotoxicosis, with decompensated heart failure, epilepsy, a patient with myocardial infarction.

With great care pyridostigmine bromide is prescribed for patients with arrhythmia, a reduced heart rate (bradycardia), a diabetic patient, with kidney disease (if necessary, the dose should be adjusted), a patient with Parkinsonism, with liver diseases transferred, and also after operations on the organs of the gastrointestinal tract.

The need for pyridostigmine usually considerably reduced after thymectomy or additional therapy (steroids, immunosuppressants).

If the drug was not taken on time, you do not need to increase the dose, but you should continue treatment according to the described dosing regimen.

Do not stop taking the drug Pyridostigmine bromide without first consulting a doctor, as the symptoms of the disease may again increase.

In patients with liver diseases, it is necessary to regularly monitor its function.

In the process of treatment, patients are strictly forbidden to drink alcohol.

Effect on the ability to drive transp. cf. and fur:

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

Form release / dosage:Tablets, 60 mg.
Packaging:

For 10 tablets in a contour mesh box made of polyvinyl chloride film and aluminum foil.

For 5 or 10 contour mesh packages together with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

The drug should not be used after the expiry date indicated on the package.

Terms of leave from pharmacies:On prescription
Registration number:LP-003633
Date of registration:16.05.2016
Expiration Date:16.05.2021
The owner of the registration certificate:FARMZASCHITA NPC, FSUE FARMZASCHITA NPC, FSUE Russia
Manufacturer: & nbsp
Information update date: & nbsp12.07.2016
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