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Synthetic anticholinesterase agent. Reversibly blocks cholinesterase, which leads to the accumulation and enhancement of the action of acetylcholine on organs and tissues and the restoration of neuromuscular conduction.
Causes a decrease in heart rate, increases the secretion of glands (salivary, bronchial, sweat and gastrointestinal tract (GIT)) and contributes to the development of hypersalivation, bronchorea, increase the acidity of gastric juice, narrows the pupil, causes a spasm of accommodation, reduces intraocular pressure, increases the tone of the smooth the muscles of the intestine (increases peristalsis and relaxes the sphincters) and the bladder, causes bronchospasm, tones the skeletal muscles.
Prozerin is an antagonist of anti-depolarizing curare-like drugs. At the same time, in high doses, prozerin itself can cause a neuromuscular conduction disorder as a result of acetylcholine accumulation and persistent depolarization in the synapse region. Gives a direct H-cholinomimetic effect.
The action of the drug coincides with the characteristic effects of excitation of cholinergic nerves. Unlike physostigmine, it more stimulates the muscles of the intestines, bladder and uterus, has little effect on the heart and does not cause central effects. When administered in therapeutic doses, skeletal muscle N-cholinergic receptors are largely excited, and neuromuscular transmission is enhanced.
Being a quaternary ammonium base, it does not penetrate through the blood-brain barrier and has no central action. Bioavailability - 1-2%. Communication with plasma proteins - 15-25%. The oral half-life is 52 minutes. 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 in an unchanged form and 30% is in the form of metabolites).
Myasthenia gravis, motor impairment after brain injury, paralysis, recovery period after suffering meningitis, polio, encephalitis, weakness of labor activity (rarely), open-angle glaucoma, optic atrophy, neuritis; atony of the digestive tract, atony of the bladder.
Elimination of residual disorders of the neuromuscular transmission of non-depolarizing muscle relaxants.
In pediatric practice: myasthenia gravis, motor disorders after brain injury, paralysis, recovery period after suffering meningitis, polio, encephalitis, optic nerve atrophy, neuritis; atony of the digestive tract, atony of the bladder. Elimination of residual disorders of the neuromuscular transmission of non-depolarizing muscle relaxants.
1 ml of solution contains:
Active substance:neostigmine methyl sulfate - 500 mcg
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Dosage and Administration
The drug is taken orally, regardless of the meal, at any time of the day.
- Adults: 2 mg once a day.
- Older people (over 65): Start with 1 mg once a day, if necessary, increase the dose to 2 mg once a day.
- Children and teenagers: Resolor is not recommended for use in children and adolescents younger than 18 years.
Patients with impaired renal function with severe renal impairment (glomerular filtration rate less than 30 ml / min / 1.73 m), the dose is 1 mg once a day. For patients with mild and moderate renal impairment dose adjustment is not required.
Patients with impaired liver function: in severe hepatic impairment (class C on Child-Pugh) dose is 1 mg 1 time per day. For patients with mild and moderate hepatic impairment dose adjustment is not required.
Due to the specific mechanism of action of prucaloprid (stimulation of intestinal motility), an increase in the daily dose of more than 2 mg is unlikely to increase the effect. If taking prukaloprid 1 time per day for 4 weeks does not give effect, you should re-examine the patient and determine the feasibility of continuing treatment.
The most frequent adverse reactions in the use of the drug Resolor were headache and adverse reactions from the gastrointestinal tract (abdominal pain, nausea, diarrhea), each of which was observed in about 20% of patients. Adverse reactions developed predominantly at the beginning of treatment and usually disappeared after a few days, without requiring cancellation of treatment. Other undesirable reactions were observed sporadically. Most adverse reactions were mild or moderate.
At the recommended dose of prucaloprid 2 mg, the following adverse reactions were recorded in clinical studies, the frequency of which is indicated as:
- very often (> 1/10);
- often (> 1/100, <1/10);
- infrequently (> 1/1000, <1/100);
- rarely (> 1/10000, <1/1000);
- very rarely (<1/10000), including isolated cases.
From the side of the central nervous system: very often - headache; often - dizziness; infrequently - tremor.
Since the cardiovascular system: infrequently - heartbeat.
From the gastrointestinal tract: very often - nausea, diarrhea, abdominal pain; often - vomiting, dyspepsia, rectal bleeding, flatulence, abnormal intestinal noise; infrequently - anorexia.
From the genitourinary system: often - pollakiuria.
Are common: often - weakness; infrequently - fever, feeling unwell.
Carefully: The use of the drug in patients with severe and clinically unstable concomitant diseases (diseases of the liver, lungs, cardiovascular, neurological, endocrine diseases, mental disorders, oncological diseases, AIDS) has not been studied. Caution should be exercised in the appointment of the drug Resolor® patients with such diseases. In particular, the drug should be used with caution in patients with cardiac arrhythmias or ischemic heart disease in history.
In vitro data indicate a weak ability of prucaloprid to interact, and at therapeutic concentrations it is unlikely to affect the metabolism of simultaneously used drugs by cytochrome system enzymes. Although prucalopride may poorly bind to P-glycoprotein (P-HP), in clinically significant concentrations it does not inhibit activity (P-HP).
A potent inhibitor of CYP3A4 and P-glycoprotein ketoconazole at a dose of 200 mg twice a day increased the AUC (area under the concentration-time curve) of prucalopride by about 40%. This effect is too small to be clinically significant, and is most likely associated with the suppression of the active P-glycoprotein in the kidneys by P-glycoprotein. The same interaction as with ketoconazole can be observed with other active inhibitors of P-glycoprotein, for example, verapamil, cyclosporin A and quinidine. Prucalopride is also likely transported by kidney and other vectors. Theoretically, the suppression of the activity of all vectors involved in the active secretion of prucaloprid in the kidney (including P-glycoprotein) can increase the level of its systemic effect by 75%.
Studies with healthy volunteers showed no clinically significant effect of prucalopride on the pharmacokinetics of warfarin, digoxin, ethyl alcohol, and paroxetine. With the simultaneous use of prucaloprid and erythromycin, the concentration of the latter in the blood plasma increases by 30%. The mechanism of this interaction is not completely clear, but the available data indicate that it is most likely not the result of the direct action of prucalopride, but the result of the high variability of the pharmacokinetics of erythromycin itself.
Probenecid, cimetidine, erythromycin and paroxetine in therapeutic doses did not affect the pharmacokinetics of prukaloprid.
Resolor should be used with caution along with drugs that can lengthen the QTc interval.
Atropin-like substances may weaken the effects of prucalopride mediated through NT receptors.4.
No interaction with food detected.
Pregnancy and Lactation
Experience with prucalopride during pregnancy is limited. In clinical studies, cases of miscarriage have been reported, although, given the presence of other risk factors, the association of these phenomena with the use of prucalopride remains unproven. Animal studies have not revealed a direct or indirect adverse effect on the course of pregnancy, embryo / fetus development, childbirth, and postnatal development of the offspring. The drug Resolor is not recommended for use during pregnancy. During the period of treatment with prucalopride, women capable of childbirth should use adequate methods of contraception.
Prukaloprid is excreted in breast milk, but when used in therapeutic doses, the drug is unlikely to affect newborns / infants. Due to the lack of data on the use of nursing mothers, the drug is not recommended for use during breastfeeding.
Ability to conceive
Animal studies have not revealed any effect of the drug on the fertility of the male and female individuals.
The main route of elimination of prucaloprid is through the kidneys. For patients with severely impaired renal function, the recommended dose is 1 mg.
In severe diarrhea, the effectiveness of oral contraceptives may decrease, and it is recommended to use additional methods of contraception to prevent a decrease in the effectiveness of oral contraceptives. Impaired liver function is unlikely to have a clinically significant effect on metabolism and the level of systemic exposure to prucalopride in humans. There is no data on the use of the drug in patients with mild, moderate or severe liver dysfunction, therefore, a lower dose is recommended for patients with severe liver dysfunction.
The drug contains lactose monohydrate, so the drug should not be taken in patients with congenital lactase deficiency, lactose intolerance, or with glucose-galactose malabsorption.
For prucalopride, neither the rebound phenomenon nor the development of dependence was identified. Studying the effect of prucalopride on the QT interval in therapeutic (2 mg) and supra-therapeutic (10 mg) dosages did not show significant differences compared with placebo in relation to the values of the QT interval.
The incidence of adverse events associated with the QT interval and ventricular arrhythmias was low and comparable with placebo.
Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention
Studies of the effect of prucalopride on the ability to drive and moving machinery was not conducted. In some cases, the use of the drug Resolor® was associated with the development of dizziness and weakness, especially in the first days of treatment, which may affect the ability to drive a car and moving machinery.
A study with healthy volunteers showed that prukaloprid was well tolerated when the dose was increased to 20 mg 1 time per day (10 times the recommended therapeutic dose).
Overdose can lead to symptoms due to increased known side effects of the drug, including headache, nausea and diarrhea.
There is no specific antidote for Resolor. In case of overdose, symptomatic and supportive therapy should be carried out if necessary. Large fluid loss due to diarrhea or vomiting may require correction of electrolyte imbalance.
- Brand name: Gemaza
- Active ingredient: Prourokinase
- Dosage form: Lyophilisate for preparation of solution for injections.
- Manufacturer: Technogen
- Country of Origin: Russia
- Annulate lamellae-soleplate nuclei associations in skeletal muscle fibers of rats during chronic high-dose exposure to neostigmine
- ChemInform Abstract: Synthesis of Some New Neostigmine Methyl Sulfates and Related Compounds
- Effects of a low-doses treatment with cuprum on neostigmine digestive action in female mice
- Inhibitions by 6-hydroxydopamine and neostigmine singly or together of gastric carcinogenesis induced by N-methyl-N′-nitro-n-nitrosoguanidine in wistar rats
- Effect of neostigmine on the tissue concentration of antibiotic in streptomycin treated rats
- Influence of physostigmine and neostigmine on the responses of goldfish intestine to acetylcholine
- Synthesis and Preliminary Pharmacology of an Internal Standard for Assay of Neostigmine
- Alkali halide-assisted penetration of neostigmine across excised human skin: A combination of structured water disruption and a donnan-like effect
- A note on the acute toxicity of neostigmine methyl bromide in the rat
- Intracerebral injection of neostigmine and eserine in conscious mice
- Prednisone-neostigmine interactions at cholinergic junctions
- Effect of lumbar epidural administration of neostigmine on lower urinary tract function
- Synergism of the toxicity of physostigmine and neostigmine by lithium or by a reserpine-like agent (Ro4-1284)
- Use of low-dose neostigmine intravenously in the treatment of supraventricular tachycardia: An immediate bradycardic effect
- Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine
- Flow injection determination of neostigmine and galanthamine by immobilised acetylcholinesterase inhibition
- Effect of neostigmine on concentration and extraction fraction of acetylcholine using quantitative microdialysis
- Neostigmine for the Treatment of Neurotoxicity Following Envenomation by the Asiatic Cobra
- Reversed-phase, ion-pair liquid chromatography of quaternary ammonium compounds : Determination of pyridostigmine, neostigmine and edrophonium in biological fluids
- Determination of neostigmine in human plasma and cerebrospinal fluid by high-performance liquid chromatography with ultraviolet detection
- Sepsis attenuates the intensity of the neuromuscular blocking effect of d-tubocurarine and the antagonistic actions of neostigmine and edrophonium accompanying depression of muscle contractility of the diaphragm
- Efficacy of intrathecal neostigmine for the relief of postinguinal herniorrhaphy pain