Vermakar susp. 100mg/5ml in vial. 30ml per pack. No. 1 (mebendazole)

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.

Mebendazole

Stylab / Catalog / Antihelmintics / Mebendazole

STYLAB offers mebendazole standards for analysis in food raw materials and products by chromatographic methods in accordance with GOST 32834-2014.

Mebendazole is a broad-spectrum anthelmintic of the benzimidazole class. It is effective against nematodes and cestodes and is used in both medicine and veterinary medicine. This substance is included in the WHO Model List of Essential Medicines. Mebendazole is prescribed for the treatment of enterobiasis, ascariasis, trichinosis and other parasitic infestations caused by helminths that live primarily in the intestines. In addition, mebendazole is effective for the treatment of echinococcosis, including liver damage by echinococcosis. It is also used to treat gnathostomosis, a disease in which nematodes attack internal organs, eyes, the central nervous system, or live under the skin. In veterinary medicine, mebendazole preparations are used for the same purposes. In the Russian Federation, as of 2021, the only drug containing mebendazole is registered for veterinary use - “Quantum”. It is intended for deworming dogs.

The mechanism of action of mebendazole on helminths is based on the ability of this substance to bind to the colchicine site of beta-tubulin and inhibit the synthesis of cytoplasmic microtubules involved in the transport of substances within the cell. This leads to a selective, irreversible impairment of glucose utilization, depletion of glycogen stores, and decreased ATP synthesis. As a result, the helminth's body becomes exhausted, it loses its ability to reproduce and dies.

Mebendazole is poorly absorbed in the intestines of mammals. It is known that in humans, when taking this anthelmintic twice a day in an amount of 100 mg, the concentration of mebendazole and its main metabolite in the blood is no more than 0.03 and 0.09 mcg/ml, respectively. Taking mebendazole with fatty foods or alcohol increases its absorption. Absorbed mebendazole is metabolized in the liver and then excreted by the kidneys. Basically, this substance acts in the intestines and is excreted in feces. It is known that mebendazole accumulates in the adipose tissue and liver of animals, as well as in helminth larvae, which makes it possible to use it for the treatment of parasitic infestations outside the intestine.

Among the acute side effects of mebendazole for humans are allergic reactions, including angioedema and anaphylactic shock, changes in blood composition, nausea, vomiting, abdominal pain, headache, dizziness, as well as kidney disorders, including hematuria ( appearance of blood in the urine). In rare cases and in case of overdose, seizures may occur. Mebendazole irritates the skin and mucous membranes upon contact with them.

For mammals, mebendazole is of low toxicity. Its LD50 upon oral administration is 714 mg/kg body weight for rats, 620 mg/kg body weight for mice, 1280 mg/kg body weight for dogs, and more than 640 mg/kg body weight for rabbits. In acute oral poisoning in animals, signs such as vomiting and diarrhea were predominantly observed. In addition, increased activity of liver enzymes, neutropenia, skin itching, fever and hair loss were recorded.

The chronic effects of mebendazole in humans have been well studied. With its long-term use in high doses, anemia, drug-induced hepatitis and liver failure, as well as glomerulonephritis, are possible. In studies on rats with long-term exposure to mebendazole, the same signs of poisoning were noted, as well as a decrease in the relative weight of the gonads, impaired spermatogenesis, and liver and kidney damage. Similar results were obtained in dogs. This anthelmintic does not exhibit mutagenic or carcinogenic properties.

Mebendazole has demonstrated embryotoxic and teratogenic properties in studies in rats. At a dosage of 10 mg/kg body weight, both the weight of the embryo and their number in the litter decreased. Many rat pups had skeletal developmental disorders, including the absence of a sternum, a shortened or absent tail, scoliosis, deformation of the ribs and bones of the limbs, and a herniated brain. At a dosage of 40 mg/kg body weight, all embryos died. In this regard, mebendazole is not recommended for use during pregnancy and for the treatment of children under 3 years of age.

Mebendazole can interact with other drugs. For example, it reduces the need for insulin in diabetes mellitus. This drug should not be given while you are taking metronidazole. In animal studies, mebendazole showed antitumor effects. It significantly inhibited the growth of adrenocortical carcinoma and induced apoptosis in cultured lung cancer cells. More research into these properties of mebendazole is currently required.

Mebendazole can enter the environment with wastewater. This anthelmintic is resistant to hydrolysis, but its similarity to albendazole indicates that it should be rapidly destroyed by exposure to sunlight. The lipid solubility of mebendazole determines the ability of this substance to bioconcentrate in aquatic organisms. In addition, mebendazole causes reproductive problems in birds and is toxic to invertebrates, including earthworms. These properties necessitate the classification of mebendazole as an ecotoxicant .

In the Russian Federation and the countries of the EAEU, maximum permissible levels (MAL) of mebendazole in food products of animal origin are not established by law. In the European Union, the MRLs for mebendazole are specified in regulation 2377/90. For lamb, goat meat and horse meat they are 60 mcg/kg, calculated as the sum of mebendazole and its metabolites. The same restriction applies to fat and kidneys from sheep, goats and horses. The liver of these animals may contain no more than 400 mcg/kg of mebendazole. In addition, in the European Union it is prohibited to use this anthelmintic for animals whose milk is intended for human food.

The method for analyzing mebendazole and other anthelmintics in food raw materials and the requirements for materials, including standards, are described in GOST 32834-2014 “Food products, food raw materials. Method for determining the residual content of anthelmintics using high-performance liquid chromatography with a mass spectrometric detector.” STYLAB offers pure substances, isotopically labeled forms, standard solutions of mebendazole and its mixtures with other anthelmintics. Certified Standard Manufacturers are accredited to ISO 17034:2016. Certified standards are accompanied by certificates.

Literature

1. Mebendazole. Register of medicines in Russia.
2. Mebendazole. Pubchem
3. EMEA/MRL/781/01-FINAL Committee for Veterinary Medicinal Products. Mebendazole. Summary Report (2). March 2001
4. Martarelli D, Pompei P, Baldi C, Mazzoni G. Mebendazole inhibits growth of human adrenocortical carcinoma cell lines implanted in nude mice. Cancer Chemother. Pharmacol. April 2008. 61 (5): 809–17.
5. Sasaki J, Ramesh R, Chada S, Gomyo Y, Roth JA, Mukhopadhyay T. The anthelmintic drug mebendazole induces mitotic arrest and apoptosis by depolymerizing tubulin in non-small cell lung cancer cells. Mol. Cancer Ther. November 2002. 1 (13): 1201–9.
6. Pantziarka, P; Bouche, G; Meheus, L; Sukhatme, V; Sukhatme, V.P. Repurposing Drugs in Oncology (ReDO)-mebendazole as an anti-cancer agent. Ecancermedicalscience. 2014. 8: 443.
7. C. N. L. Macpherson, S. Bidaisee. Role of society and culture in the epidemiology and control of foodborne parasites. Foodborne Parasites in the Food Supply Web, 2015

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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.

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 .

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.