Pharmacological properties of the drug Albendazole
An anthelmintic agent that is also active against pathogenic protozoa. Acts on intestinal and tissue forms of parasites; active against eggs, larvae and adult helminths. The antihelminthic effect of albendazole is due to inhibition of tubulin polymerization, leading to metabolic disturbances and death of helminths. Albendazole is active against intestinal parasites, including nematodes - Ascaris lumbricoides, Trichuris trichiura, Enterobius vermicularis, Ancylostoma duodenale, Necator americanus, Strongyloides stercoralis, Cutaneous Larva Migrans ; cestodes - Hymenolepsis nana (dwarf tapeworm), Taenia solium (pork tapeworm), Taenia saginata (bovine tapeworm); trematodes - Opisthorchis viverrini , Clonorchis sinensis ; protozoa - Giardia lamblia . Albendazole is active against tissue parasites, including cystic echinococcosis and alveolar echinococcosis, caused by invasion of Echinococcus granulosus and Echinococcus multilocularis , respectively. Effective in the treatment of neurocysticercosis caused by infestation of the larvae of the pork tapeworm T. solium , capillariasis caused by Capillaria philippinensis , and gnathostomiasis caused by infestation of Gnathostoma spinigerum . Albendazole destroys cysts or significantly reduces their size in patients with granular echinococcosis. After treatment with albendazole, the number of nonviable cysts increases to 90% compared to 10% in patients who did not receive treatment. After using albendazole for cysts caused by Echinococcus multilocularis , complete cure was observed in a minority of patients, and improvement or stabilization of the disease was observed in the majority. When administered orally, albendazole is poorly absorbed (less than 5%). Simultaneous intake of fatty foods increases the absorption of the drug by approximately 5 times. Rapidly metabolized in the liver during the first pass. The main metabolite, albendazole sulfate, retains half the pharmacological activity of the original substance. The half-life of albendazole is 8.5 hours. Albendazole sulfate and its metabolites are mainly excreted in the bile, and only a small part is excreted in the urine. It has been established that after prolonged administration of the drug in high doses, its elimination from cysts continues for several weeks.
Albendazole
Stylab / Catalog / Antihelmintics / Albendazole
STYLAB offers standards for albendazole and its metabolites for their analysis in food raw materials and products by chromatographic methods in accordance with GOST 32834-2014.
| Standards and standard solutions | Anthelmintic standards for analysis in accordance with GOST 32834-2014 |
Albendazole, or albendazole, belongs to the group of benzimidazoles - aromatic nitrogen-containing substances, many of which exhibit biological activity. Albendazole is a broad-spectrum anthelmintic It is effective for the treatment of ascariasis, strongyloidiasis, trichurosis and some other helminthiases caused by nematodes or helminths of several species. It is also prescribed for giardiasis - intestinal damage by protozoa. Albendazole is used to treat echinococcosis. It is most effective against parasite larvae.
Albendazole has been used in human and veterinary medicine since 1975. It is on the WHO Model List of Essential Medicines. Both medical (Nemazol, Sanoxal) and veterinary preparations of albendazole are registered in the Russian Federation. The latter include Ritril, Tenalben, Zalben, Febtal®-combo, Benalben, Alvet and others. They are used to treat helminth infections in horses, cattle, sheep, goats, pigs, poultry, dogs, cats and reptiles.
Albendazole is practically insoluble in water and is poorly absorbed (less than 5% of the dose) in the gastrointestinal tract. Thus, this anthelmintic mainly acts locally, on parasites located in the intestines. However, the presence of fat, for example from food, increases the bioavailability of albendazole by 5 times. The difference in the LD50 of albendazole for rats with oral and intravenous administration is also indicative. They differ almost 10 times and are 2400 mg/kg body weight and 265 mg/kg body weight, respectively.
In the body, albendazole is rapidly metabolized in the liver. Its primary metabolite is albendazole sulfoxide, which is also toxic to helminths. Albendazole sulfoxide is then metabolized to albendazole sulfone and other substances, which are excreted in urine and milk.
The mechanism of action of albendazole on parasites is due to the ability of this substance to prevent the elongation of special cellular structures - microtubules. This leads to disruption of the transport of substances within the cell. Albendazole also reduces glucose uptake and ATP synthesis. As a result, the cells of the intestines and integument of the worm die, which, in turn, leads to paralysis and death of the helminths themselves.
Side effects of albendazole in humans include various skin reactions, nausea, vomiting, abdominal pain, headache, dizziness, fever, alopecia (hair loss), and drug-induced hepatitis. This substance has nephro- and hepatotoxicity and can cause acute renal failure and liver cirrhosis. The use of albendazole leads to changes in blood composition. In some cases, aplastic anemia or decreased hematopoietic function of the bone marrow may occur. In animals poisoned with albendazole, drowsiness, nausea, diarrhea, decreased food intake, abdominal pain, and weakness were observed.
In animal experiments, albendazole did not exhibit carcinogenic properties. However, it has embryotoxicity and teratogenic effects. In rats and rabbits, the death of pregnant females was observed under the influence of this substance. The embryos showed disturbances in the development of the skull and bones of the limbs, as well as a decrease in the size of the lungs and kidneys relative to the control. Some of the embryos died. In addition, with long-term use of albendazole, testicular pathologies were observed in male mice, rats and dogs.
In bacterial studies, albendazole did not demonstrate genotoxicity. However, in vivo experiments on mice showed that this substance causes mutations in somatic cells, including bone marrow cells. It is currently unknown whether albendazole can cause inherited mutations.
Albendazole is highly mobile in soil and easily migrates into water. In the environment, this substance quickly decomposes when exposed to sunlight. Its half-life during photolysis is, depending on the pH and temperature of the water, 6-80 minutes. The bioconcentration potential of albendazole is considered low despite its lipid solubility. Albendazole can enter the human body through contact with the substance, as well as with products of animal origin, including milk and meat. This usually occurs when the waiting period after using the drug is not observed. It must also be taken into account that albendazole is not destroyed when the product is heated. This means that it can also be present in prepared foods.
In the Russian Federation, 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.” It describes in detail the methodology for analyzing anthelmintic drugs, including albendazole, in food raw materials and contains requirements for materials, including standards. STYLAB offers pure substances, isotopically labeled forms, standard solutions and mixtures of albendazole and its derivatives. Certified Standard Manufacturers are accredited to ISO 17034:2016. Certified standards are accompanied by certificates.
Literature
- Albendazole. Register of medicines in Russia.
- Albendazole. PubChem.
- Neonatal Formulary: Drug Use in Pregnancy and the First Year of Life. John Wiley & Sons. 2014. p. 64.
- Cooper KM, Whelan M, Danaher M, Kennedy DG. Stability during cooking of anthelmintic veterinary drug residues in beef. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2011 Feb;28(2):155-65.
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Indications for use of the drug Albendazole
Enterobiasis, hookworm and necatoriasis, hymenolepiasis, taeniasis, strongyloidiasis, ascariasis, trichinosis, clonorchiasis, cutaneous larvae migrans, giardiasis in children. Long-term treatment with albendazole in high doses is indicated for the following systemic helminthic infestations:
- cystic echinococcosis (caused by Echinococcus granulosus ): if surgical intervention is not possible;
- before surgery;
- after surgery, if preoperative treatment was too short, if there is a prevalence of helminths or if live forms were found during surgery;
- after percutaneous drainage of cysts for diagnostic or therapeutic purposes;
- in case of inoperable disease, in particular during palliative surgical treatment;
- single or multiple cysts or granulomatous brain lesions;
Albendazole is also used for capillarosis, gnathostomiasis, trichinosis (caused by Trichinella spiralis and T. pseudospiralis ), toxocariasis (caused by Tohosaga canis and other related species).
Use of the drug Albendazole
For enterobiasis, hookworm, necatoriasis, ascariasis, trichinosis, the usual dose for adults and children over 2 years of age is 400 mg. Children aged 1–2 years are usually prescribed a single dose of 200 mg. In cases of diagnosed or suspected strongyloidiasis, taeniasis and hymenolepiasis, adults and children over 2 years of age are usually prescribed 400 mg once a day for 3 days in a row. For confirmed hymenolepiasis, it is recommended to repeat the course of treatment after 10–21 days. For opisthorchiasis and clonorchiasis, adults and children over 2 years of age are prescribed 400 mg 2 times a day for 3 days. This regimen also provides effective treatment for mixed infestations of Opisthorchis viverrini and Chlonorchis sinensis . For cutaneous larva migrans ( Cutaneous larva migrans ), adults and children over 2 years of age are usually prescribed 400 mg daily for 1–3 days. For giardiasis, children aged 2–12 years are prescribed 400 mg/day daily for 5 days. For systemic helminthic infestations, the dose of albendazole depends on the type of parasite, the patient’s body weight and the severity of the disease. For cystic echinococcosis, patients weighing more than 60 kg are prescribed a daily dose of 800 mg in 2 doses of 400 mg for 28 days, patients weighing less than 60 kg are prescribed a daily dose of 15 mg/kg in two equal parts (maximum dose 800 mg/day), as indicated above. The course of treatment can be repeated at intervals of 14 days; If necessary, 3 such courses can be conducted. For alveolar echinococcosis, patients weighing more than 60 kg are prescribed a daily dose of 800 mg in 2 doses of 400 mg for 28 days with a 14-day break between cycles. Patients weighing less than 60 kg are prescribed a daily dose of 15 mg/kg in two equal parts (maximum dose 800 mg/day), as indicated above. If necessary, treatment is extended for months and years. For neurocysticercosis, patients weighing more than 60 kg are prescribed a daily dose of 800 mg in 2 divided doses of 400 mg for 7–30 days, depending on the result. Patients weighing less than 60 kg are prescribed a daily dose of 15 mg/kg in two equal parts (maximum dose 800 mg/day), as indicated above. A second course of treatment can be carried out after 1–2 weeks. For capillariasis, children and adults are prescribed 400 mg daily for 10 days. For gnathostomosis, children and adults are prescribed 400 mg daily for 10–20 days.
POWDER.
Albendazole 10% powder (Albendazolum 10% pulvis). In appearance, the drug is a white to light gray powder. 1.0 g of the drug contains 0.1 g of albendazole and up to 1.0 g of filler. The drug is produced in bags made of metallized foil or containers made of polymer material or in paper bags with a nominal weight of 50.0 g; 100.0 g; 200.0 g; 400.0 g; 500.0 g; 1000.0 g, 5.0 kg; 10.0 kg; 20.0 kg; 25.0 kg.
The drug is stored according to list B in a dry place, protected from light, at a temperature from plus 5 ºС to plus 25 ºС. The shelf life of the drug is 2 years from the date of manufacture, subject to the rules of storage and transportation.
PHARMACOLOGICAL PROPERTIES
Albendazole, which is part of the drug, belongs to the group of benzimidazoles and has a wide spectrum of antiparasitic effects. Effective against nematodes, cestodes and trematodes, having an ovicidal effect, reduces the infestation of pastures with helminth eggs.
The mechanism of action of the drug is to disrupt metabolism, inhibit the activity of fumarate reductase and ATP synthesis of the parasite, which leads to the death of helminths.
When administered orally, albendazole is partially absorbed from the gastrointestinal tract and penetrates into organs and tissues. It is excreted from the body mainly in feces, urine and bile unchanged, as well as in the form of metabolites.
APPLICATION OF THE DRUG
The drug is used orally in pigs for ascariasis, metastrongylosis, esophagostomosis, trichuriasis, strongyloidiasis, ollulanosis; large and small cattle with fascioliasis, moniesiosis, strongyloidiasis, as well as strongylatosis of the gastrointestinal tract and respiratory organs; horses with parascariasis, oxyurosis, strongylatosis and strongyloidiasis; fish with ligulosis, caviosis and bothriocephalosis.
The drug is administered to animals once individually or in a group in a mixture with food without prior dietary preparation; fish - twice.
For the treatment and prevention of moniesiosis, pulmonary and gastrointestinal nematodes, the drug is administered to cattle individually at a dose of 0.075 g/kg of animal weight, for chronic fascioliasis - at a dose of 0.1 g/kg of animal weight.
It is used individually or in groups for small cattle. For moniesiosis, pulmonary and intestinal nematodes, the drug is used at a dose of 0.05 g/kg of animal weight. For chronic fascioliasis, the drug is used at a dose of 0.075 g/kg, for chronic dicroceliosis - at a dose of 0.15 g/kg of animal weight. For the group method of administration, the drug is weighed per group of no more than 150 animals, thoroughly mixed with feed (at the rate of 50 - 100 g of feed per animal). The mixture is placed in feeders, providing free access to them for animals.
Pigs are given the drug in the morning feeding in a group manner with concentrated feed. The drug is weighed at the rate of 0.1 g/kg of animal weight for a group of no more than 50 animals, mixed with half the amount of feed and laid out in feeders, providing the animals with free access to them.
Horses are given the drug individually with feed at a dose of 0.075 g/kg animal weight.
For fish, the drug is given in a mixture with feed at the rate of 3 kg/1 ton of feed. Medicinal feed with the drug is used at the rate of 5% of the medicinal feed by weight of the fish by group feeding once a day for two days in a row.
If necessary, the drug can be used repeatedly in animals.
Before mass treatments, each batch of the drug is first tested on small groups of animals (5-15 heads) of varying fatness and age. If the animals do not show signs of toxicosis within two days after treatment, they begin to treat the entire livestock.
SIDE EFFECTS
When using the drug in recommended doses in accordance with the instructions, no adverse reactions or complications are observed. If allergic and other side effects occur, the drug is discontinued and antihistamines, calcium supplements and symptomatic medications are prescribed.
CONTRAINDICATIONS
The use of the drug is contraindicated for acute fascioliasis, animals in the breeding period, females in the first third of pregnancy, weakened, exhausted animals and animals suffering from infectious diseases.
SPECIAL INSTRUCTIONS
Slaughter of animals for meat is permitted no earlier than 14 days after the last use of the drug. Marketable fish is sold 14 days after the last course of use of the drug. In the event of forced slaughter of animals, or catching fish before the due date, meat and fish can be used to feed carnivores. Milk from dairy animals can be used for food purposes after 4 days after deworming; before the required period, they can be used to feed animals after heat treatment.
The purchase of veterinary drugs at our enterprise is carried out in wholesale quantities. Since we are direct manufacturers of medicines, the purchasing cost is much lower than market prices.
As manufacturers of veterinary drugs, we strictly monitor the quality of our products, conduct laboratory tests on modern high-precision equipment, use proven methods and store them in specialized warehouses.
If you need to purchase medicines for animals, you want to get acquainted with the prices and consider the price list for veterinary drugs, contact our employees by phone!
Special instructions for the use of Albendazole
To avoid accidental use in early pregnancy, women of reproductive age should begin treatment with albendazole in the 1st week of menstruation or if a pregnancy test is negative. Patients should be warned about the need to use effective methods of contraception during treatment with albendazole and for 1 month after its discontinuation. During treatment, liver enzyme activity should be monitored before the start of each treatment cycle and (preferably) every 2 weeks during treatment. If the value is more than 2 times the upper limit of normal, treatment with albendazole should be interrupted until it is completely normalized. The white blood cell count should be monitored at baseline and every 2 weeks during each 28-day treatment cycle. The use of albendazole for leukopenia can be continued if the degree of reduction is insignificant and the leukopenia does not progress.
