Description:
Round, flat-cylindrical tablets from white to light yellow in color with a chamfer and a score.
Pharmacotherapeutic group:
anthelmintic agent.
ATX code:
P02CA01
Pharmacological properties
Pharmacodynamics:
Broad-spectrum anthelmintic drug; most effective against Enterobius
vermicularis , Trichuris trichura , Ascaris lumbricoides , Ancylostoma duodenale , Necator americanus , Strongyloides stercoralis , Taenia solium , Echinococcus granulosus , Echinococcus multilocularis , Trichinella spiralis , Trichinella nativa , Trichinella nelsoni
. Causing an irreversible disruption of glucose utilization, it depletes glycogen reserves in the tissues of helminths, prevents the synthesis of cellular tubulin, and also inhibits the synthesis of adenosine triphosphate (ATP).
Pharmacokinetics:
Practically not absorbed in the intestines. After taking the drug at a dose of 100 mg twice a day for three consecutive days, the plasma concentration of mebendazole and its metabolite (2-amino derivative) does not exceed 0.03 mcg/ml and 0.09 mcg/ml, respectively. Communication with plasma proteins – 90%. It is unevenly distributed throughout the organs, accumulates in adipose tissue, liver, and helminth larvae. In the liver it is metabolized to a 2-amino derivative, which does not have anthelmintic activity. The half-life is 2.5-5.5 hours. More than 90% of the dose is eliminated unchanged through the intestines. The absorbed part (5-10%) is excreted by the kidneys.
Analogs
Level 4 ATC code matches: Medamin
Vermakar
Nemozol
Vermox
Aldazole
Zentel
Wormil
Vormin
Sanoxal
Analogs include drugs containing the active substance mebendazole: Vermox , Agelmin .
Directions for use and doses
Inside with a small amount of water.
Adults and children over 3 years old.
For enterobiasis - once 100 mg/day (1 tablet); course of treatment is 1 day. Since reinfection with enterobiasis occurs quite often, treatment should be repeated after 2 and 4 weeks.
It is recommended to treat all family members simultaneously.
For ascariasis, trichuriasis, hookworm and mixed helminthiasis: 200 mg/day (1 tablet in the morning, 1 tablet in the evening); course of treatment is 3 days.
For taeniasis, strongyloidiasis. Adults: 400 mg/day (2 tablets in the morning, 2 tablets in the evening); course of treatment is 3 days. Children over 3 years old: 200 mg/day (1 tablet in the morning, 1 tablet in the evening); course of treatment is 3 days.
For echinococcosis. Adults and children over 14 years of age: in the first three days, 500 mg 2 times a day, in the next 3 days the dose is increased to 500 mg 3 times a day; subsequently the dose is increased to 1000-1500 mg 3 times a day. The average duration of treatment for echinococcosis caused by Echinococcus granulosis is 4-6 weeks, and up to two years for those caused by Echinococcus multilocularis.
For trichinosis, on the 1st day 3 times a day, 200-300 mg, on the 2nd day, 4 times a day, 200-300 mg, and from days 3 to 14 – 3 times a day, 500 mg.
Side effect
Allergic reactions: skin rash, urticaria, angioedema, Steven-Johnson syndrome, toxic epidermal necrolysis, exanthema, anaphylactic and anaphylactoid reactions.
From the hematopoietic organs: neutropenia.
From the digestive system: nausea, vomiting, abdominal pain, diarrhea, increased activity of liver transaminases, alkaline phosphatase, hepatitis (when used in high doses for a long time).
From the nervous system: dizziness, headache, drowsiness, convulsions.
From the urinary system: hypercreatininemia, glomerulonephritis (when used in high doses for a long time).
Other: hair loss (when used in high doses for a long time).
special instructions
The drug contains lactose, therefore this drug is contraindicated in patients with rare hereditary lactose intolerance, lactase deficiency or impaired glucose/galactose absorption.
In patients with diabetes mellitus, it is necessary to monitor the concentration of glucose in the blood plasma.
With long-term use, it is necessary to monitor the peripheral blood picture, liver and kidney function.
During the day after administration, it is prohibited to consume ethanol, fatty foods, or take laxatives.
Periodic examination of smears of the anal area and feces after completion of treatment is mandatory: therapy is considered effective if there are no helminths or their eggs within the next 7 days.
The results of a study on the development of Steven-Johnson syndrome and toxic epidermal necrolysis indicate a possible connection between their occurrence and the simultaneous use of mebendazole and metronidazole. There are no other data documenting cases of such drug interactions. That is why the simultaneous use of mebendazole and metronidazole should be avoided.
Mebendazole Grindeks tablets 100 mg No. 6x1
Name
Mebendazole Grindeks tablet 100 mg in blister pack No. 6x1
Description
6 tablets in a blister made of aluminum foil and polyvinyl chloride film. 1 blister along with instructions for medical use of the drug in a cardboard pack. text
Main active ingredient
Mebendazole
Release form
Pills.
Dosage
100 mg in blister pack No. 6x1
Pharmacodynamics
Mebendazole is an anthelmintic agent of the benzimidazole group with a broad spectrum of action. It is most active against intestinal nematodes; it is also effective against other helminths, their larvae and eggs. The greatest anthelmintic activity of mebendazole is observed in cases of infestation of the following helminths: Ascaris lumbricoides (98%), Ancylostoma duodenale (96%), Necator americanus (96%), Enterobius vermicularis (95%), Trichuris trichiura (68%). Mebendazole is also effective against Mansonella, Trichinella and the primary animal parasites Angiostrongylus cantonensis and Grathostoma spinigerum. Mebendazole is ineffective in cases of Echinococcus infestation. The ability of mebendazole to inhibit the activity of helminths depends on many factors, including the duration of treatment, the degree of helminth infestation, etc. The mechanism of the antihelminthic action of mebendazole is based on its ability to influence the energy processes of helminths, reducing the glucose reserve, depleting glycogen reserves in the tissues of helminths, preventing the synthesis of cellular tubulin, as well as inhibiting ATP synthesis.
Pharmacokinetics
Absorption After oral administration, about 20% of the administered dose reaches the systemic circulation due to incomplete absorption and extensive first-pass metabolism (the “first pass” effect). Maximum plasma concentrations are usually observed 2-4 hours after taking mebendazole. The simultaneous use of mebendazole with food containing fats leads to a slight increase in its bioavailability. Distribution Plasma protein binding is 90-95%. The volume of distribution is 1-2 l/kg, which indicates the distribution of mebendazole outside the blood vessels. This is supported by data obtained from patients who used mebendazole long-term (eg, 40 mg/kg/day for 3-21 months) and in whom tissue levels of mebendazole were determined. Metabolism After oral administration, mebendazole is metabolized primarily in the liver. Plasma concentrations of its main metabolites (in the form of amines and hydroxylated amino derivatives of mebendazole) are significantly higher than those of mebendazole. Impaired liver function, metabolic disorders or impaired biliary excretion may lead to increased concentrations of mebendazole in the blood plasma. Excretion Mebendazole, its conjugated forms and metabolites are partially subject to enterohepatic recirculation and are excreted in urine and bile. The half-life after oral administration in most patients is 3-6 hours. Impaired renal function does not have a significant effect on the excretion of mebendazole from the body. Pharmacokinetics at steady state With long-term use (for example, 40 mg/kg/day for 3-21 months), the plasma concentration of mebendazole and its main metabolites increases, which leads to an approximately 3-fold increase in the total systemic effect compared with a single dose. Pharmacokinetics in children under 2 years of age has not been studied; in children over 2 years of age, they are similar to pharmacokinetics in adults. Pharmacokinetics in elderly patients does not have any peculiarities.
Indications for use
Mebendazole-Grindeks tablets are used for the treatment of single or mixed gastrointestinal infestation of cestodes and nematodes, such as Enterobius vermicularis (pinworms), Trichuris trichiura (whipworm), Ascaris lumbricoides (roundworms), Ancylostoma duodenale and Necator americanus (nematodes).
Directions for use and doses
For oral use with a small amount of water. The tablet can be swallowed whole, chewed or crushed and added to food. During treatment with mebendazole there is no need to follow a diet or use laxatives. For adults and children over 2 years of age, the doses are the same. For pinworm infestation, 100 mg (1 tablet) is prescribed once. Due to the short life cycle of pinworms and the high risk of re-infection, especially in closed groups, the course of treatment should be repeated after 2 weeks. For infection with other helminths and mixed helminth infections - 100 mg in the morning and evening for 3 DAYS in a row. Treatment is repeated if, after 3 weeks, signs of helminthiasis are again detected. The drug should not be prescribed to children under 2 years of age, since its safety for young children has not been confirmed by clinical data. If you forget to take the next dose of medicine on time, wait and do it at the usual time. Do not use a double dose to replace a forgotten dose. If you have any questions about using this medicine, ask your doctor or pharmacist.
Use during pregnancy and lactation
In animal experiments, mebendazole revealed embryotoxic and teratogenic effects. The potential risk to humans is unknown and use during pregnancy is not recommended. Use during breastfeeding is not recommended as it is not known whether mebendazole is excreted into mother's milk.
Precautionary measures
To avoid repeated invasions and relapses of the disease, patients should strictly observe the rules of personal hygiene. With long-term use, it is necessary to monitor the peripheral blood picture, liver and kidney function. Within 24 hours after administration, the consumption of ethanol, fatty foods, and laxatives is prohibited. Periodic examination of smears of the anal area and feces after completion of treatment is mandatory: therapy is considered effective if there are no helminths or their eggs within the next 7 days. In rare cases, mebendazole may cause seizures in children under 2 years of age, so the use of mebendazole in children in this age group is not recommended. The use of mebendazole in very young children is only possible if pinworm infection has an obvious impact on the nutritional status and physical development of the child. The results of clinical studies indicate a possible association between the simultaneous use of mebendazole and metronidazole and the development of Stevens-Johnson syndrome/toxic epidermal necrolysis. Therefore, the simultaneous use of mebendazole and metronidazole should be avoided. The tablets contain lactose, so the use of the drug is contraindicated in patients with rare congenital galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. Sunset yellow dye (E110) contained in the tablets may cause allergic reactions.
Interaction with other drugs
In therapeutic doses without exceeding the duration of treatment, mebendazole practically does not interact with other drugs. With long-term simultaneous use with cimetidine, the inactivation of mebendazole in the liver may be slowed down, as a result of which mebendazole accumulates in the body. In this case, it is recommended to determine the concentration of mebendazole in the blood plasma in order to correctly adjust the dose. The simultaneous use of mebendazole and metronidazole should be avoided (see section "Precautions").
Contraindications
Hypersensitivity to mebendazole and/or to any excipient of the drug.
Compound
One tablet contains: active substance - mebendazole 100 mg; excipients: lactose monohydrate, corn starch, povidone, sodium starch glycolate (type A), magnesium stearate, sunset yellow (E 110).
Overdose
Symptoms: in case of acute overdose, disorders of the gastrointestinal tract were observed - abdominal pain, nausea, vomiting, diarrhea, accompanied by a feeling of dizziness and headaches. When using doses significantly higher than recommended or long-term use, the following side effects have been reported in rare cases: alopecia, reversible liver dysfunction, hepatitis, agranulocytosis, neutropenia and glomerulonephritis. Treatment is symptomatic; there is no specific antidote. It is necessary to remove the drug from the stomach by inducing vomiting or performing gastric lavage, as well as taking activated charcoal.
Side effect
Due to the fact that at recommended doses mebendazole acts mainly locally on the gastrointestinal tract, side effects are rare and are usually associated with disturbances in the functioning of the gastrointestinal tract. The side effects mentioned below are in accordance with the MedDRA classification of organ systems and the frequency of occurrence: very often: (? 1/10), often: (? 1/100 to
Storage conditions
Store at a temperature not exceeding 25 °C. Keep out of the reach of children! Do not use after the expiration date stated on the package. Shelf life - 5 years.
