Bloxiverz (neostigmine methylsulfate)

Bloxiverz (neostigmine methylsulfate) Medicine

Overdose

Solution for injection, Dragees, Solution for intravenous and subcutaneous administration, Substance-powderPills

Symptoms associated with overexcitation of cholinergic receptors (cholinergic crisis): bradycardia, hypersalivation, miosis, bronchospasm, nausea, increased peristalsis, diarrhea, increased urination, twitching of the tongue and skeletal muscles, gradual development of general weakness, decreased blood pressure.

Treatment: reduce the dose of proserin or stop treatment, if necessary, enter atropine (1 ml of 0.1% solution), metacin and other holinoblokiruyuschie drugs.

Symptoms associated with overexcitation of cholinergic receptors (cholinergic crisis): bradycardia, hypersalivation, miosis, bronchospasm, nausea, increased peristalsis, diarrhea, increased urination, twitching of the tongue and skeletal muscles, gradual development of general weakness, decreased blood pressure.

Treatment: reduce the dose of Bloxiverz (Neostigmine Methylsulfate)a or stop treatment, if necessary, enter atropine (1 ml of 0.1% solution), metacin and other holinoblokiruyuschie drugs.

Contraindications

hypersensitivity,

epilepsy,

hyperkinesis,

vagotomy,

coronary heart disease,

bradycardia,

arrhythmias,

angina pectoris,

bronchial asthma,

severe atherosclerosis,

thyrotoxicosis,

peptic ulcer of the stomach and duodenum,

peritonitis,

mechanical obstruction of the gastrointestinal tract and urinary tract,

prostate adenoma,

period of acute illness,

intoxication in severely weakened children,

pregnancy,

lactation period.

With caution. On the background of anticholinergic drugs, in children (with myasthenia gravis) on the background of neomycin, streptomycin, kanamycin and other antibiotics that have an antidepolarizing effect, local and some general anesthetics, antiarrhythmic and a number of other drugs that violate cholinergic transmission.

Incompatibilities

Solution for injection, Dragees, Solution for intravenous and subcutaneous administration, Substance-powderPills

When myasthenia gravis is prescribed in combination with aldosterone antagonists, corticosteroids and anabolic hormones.

Atropine, metacin and other m-holinoblockers weaken the m-holinomimetic effects of proserin (including pupil constriction, bradycardia, increased gastrointestinal motility, hypersalivation).

When myasthenia gravis is prescribed in combination with aldosterone antagonists, corticosteroids and anabolic hormones.

Atropine, metacin and other m-cholinoblockers weaken the m-cholinomimetic effects of Bloxiverz (Neostigmine Methylsulfate)a (including pupil constriction, bradycardia, increased gastrointestinal motility, hypersalivation).

Undesirable effects

From the gastrointestinal tract: hypersalivation, spastic contraction and increased intestinal motility, nausea, vomiting, flatulence, diarrhea.

From the nervous system and sensory organs: headache, dizziness, weakness, loss of consciousness, drowsiness, miosis, visual impairment, tremor, spasms and twitching of skeletal muscles, including fasciculations of the muscles of the tongue, convulsions, dysarthria.

From the CCC side: arrhythmia, brady-or tachycardia, AV block, block, nodal rhythm, non-specific changes on the ECG, cardiac arrest.

From the respiratory system: shortness of breath, respiratory depression, up to a stop, bronchospasm.

Allergic reactions: flushing of the face, rash, itching, anaphylaxis.

Other: increased urination, arthalgia, profuse sweating.

Therapeutic indications

Solution for injection, Dragees, Solution for intravenous and subcutaneous administration, Substance-powderPills

myasthenia gravis,

motor disorders after brain injury,

paralysis,

the recovery period after suffering meningitis, poliomyelitis, encephalitis,

weakness of labor activity (rarely),

open-angle glaucoma,

neuritis, atrophy of the optic nerve,

atonia of the gastrointestinal tract,

atony of the bladder,

elimination of residual disorders of neuromuscular transmission by non-depolarizing muscle relaxants.

In children's practice: myasthenia gravis, motor disorders after brain injury, paralysis, recovery period after meningitis, polio, encephalitis, neuritis, atrophy of the optic nerve, atony of the gastrointestinal tract, atony of the bladder, elimination of residual disorders of neuromuscular transmission with non-depolarizing muscle relaxants.

myasthenia gravis,

motor disorders after brain injury,

paralysis,

the recovery period after suffering meningitis, poliomyelitis, encephalitis,

weakness of labor activity (rarely),

open-angle glaucoma,

neuritis, atrophy of the optic nerve,

atonia of the gastrointestinal tract,

atony of the bladder,

elimination of residual disorders of neuromuscular transmission by non-depolarizing muscle relaxants.

In children's practice: myasthenia gravis, motor disorders after brain injury, paralysis, recovery period after meningitis, polio, encephalitis, neuritis, atrophy of the optic nerve, atony of the gastrointestinal tract, atony of the bladder, elimination of residual disorders of neuromuscular transmission with non-depolarizing muscle relaxants.

Pharmacotherapeutic group

  • Cholinesterase inhibitor [m -, n-Cholinomimetics, including anticholinesterase agents]

Pharmacodynamic properties

Solution for injection, Dragees, Solution for intravenous and subcutaneous administration, Substance-powderPills

Synthetic anticholinesterase agent. Reversibly blocks cholinesterase, which leads to the accumulation and strengthening of the action of acetylcholine on organs and tissues and the restoration of neuromuscular conduction.

It causes a decrease in heart rate, increases the secretion of glands (salivary, bronchial, sweat and gastrointestinal glands), which contributes to the development of hypersalivation, bronchorrhea, increased acidity of gastric juice, narrows the pupil, causes spasm of accommodation, reduces intraocular pressure, increases the tone of the smooth muscles of the intestine (increases peristalsis and relaxes the sphincters) and the bladder, causes bronchial spasm, tones skeletal muscles.

Neostigmine is an antagonist antidepolyarizuyuschih curariform drugs. At the same time, in large doses, proserin can itself cause a violation of neuromuscular conduction as a result of the accumulation of acetylcholine and persistent depolarization in the synaptic region. Gives a direct n-cholinomimetic effect. The effect of the drug coincides with the characteristic effects of the excitation of cholinergic nerves. Unlike physostigmine, it stimulates the muscles of the intestines, bladder and uterus to a greater extent, has little effect on the heart and does not cause central effects. When administered in therapeutic doses, greatly excited the n-cholinergic receptors of skeletal muscles, increases neuromuscular transmission

Synthetic anticholinesterase agent. Reversibly blocks cholinesterase, which leads to the accumulation and strengthening of the action of acetylcholine on organs and tissues and the restoration of neuromuscular conduction.

It causes a decrease in heart rate, increases the secretion of glands (salivary, bronchial, sweat and gastrointestinal glands), which contributes to the development of hypersalivation, bronchorrhea, increased acidity of gastric juice, narrows the pupil, causes spasm of accommodation, reduces intraocular pressure, increases the tone of the smooth muscles of the intestine (increases peristalsis and relaxes the sphincters) and the bladder, causes bronchial spasm, tones skeletal muscles.

Bloxiverz (Neostigmine Methylsulfate) is an antagonist of antidepolarizing curare-like drugs. At the same time, in high doses, Bloxiverz (Neostigmine Methylsulfate) can itself cause a violation of neuromuscular conduction as a result of the accumulation of acetylcholine and persistent depolarization in the synaptic region. Gives a direct n-cholinomimetic effect. The effect of the drug coincides with the characteristic effects of the excitation of cholinergic nerves. Unlike physostigmine, it stimulates the muscles of the intestines, bladder and uterus to a greater extent, has little effect on the heart and does not cause central effects. When administered in therapeutic doses, greatly excited the n-cholinergic receptors of skeletal muscles, increases neuromuscular transmission

Pharmacokinetic properties

Being a quaternary ammonium base, it penetrates poorly through the BBB and does not have a central effect. Bioavailability of 1-2%. Binding to plasma proteins — 15-25%. T1/2 with oral administration-52 min. Metabolism-in the liver with the formation of inactive metabolites. 80% of the administered dose is excreted by the kidneys within 24 hours (of which 50% is unchanged and 30% is in the form of metabolites).

Name of the medicinal product

Bloxiverz (Neostigmine Methylsulfate)

Qualitative and quantitative composition

Neostigmine Methylsulfate

Dosage (Posology) and method of administration

Inside, 30 minutes before the meal.

Adults - 10-15 mg 2-3 times a day, the maximum single dose is 15 mg, the maximum daily dose is 50 mg.

For children up to 10 years — 1 mg per 1 year of life per day, older than 10 years-up to 10 mg/day (no more).

Course of treatment (except for myasthenia gravis) - 25-30 days, if necessary — again, after 3-4 weeks. A large part of the total daily dose administered in the daytime, when the patient is in the highest degree of fatigue.

In case of weakness of labor activity-inside 3 mg 4-6 times a day with an interval of 40 minutes.