Albendazole - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Anthelmintic agents

Included in the formulation

Gelmodol-BM

pills inwards

World Medical Co., Ltd. Egypt

Nemozol®

pills inwards

Ipka Laboratories Ltd. India

Nemozol®

suspension inwards

Ipka Laboratories Ltd. India

Sanoxual

pills inwards

Oxford Laboratories Pvt. Ltd. India

АТХ:

P.02.C.A.03 Albendazole

P.02.C.A Benzimidazole derivatives

Pharmacodynamics:Albendazole belongs to the benzimidazole group, having a similar structure with such drugs as omeprazole, dibasol. It is active against nematodes (larvae, eggs, adult forms) and some species of cestodes (only larvae). Is a prodrug, since the main effect is its metabolite - albendazole sulfoxide. It suppresses the assembly of microtubules from β-tubulin in the epithelium of the intestinal canal of helminths. This leads to the destruction of cytoplasmic tubules and disrupts intracellular transport and movement of organelles. Also, albendazole inhibits the utilization of glucose and disrupts the synthesis of adenosine triphosphate. Lack of energy substrate leads to impaired mobility and death of helminths. The maximum effect is manifested in larval forms of flatworms - Echinococcus granulosus and Taenia solium, nematodes Strongyloides stercolalis.

Pharmacokinetics:In the intestines it is absorbed badly. In the plasma, only its metabolite, albendazole sulfoxide, is determined. Simultaneous reception with fatty foods increases absorption and maximum metabolite concentration by 5 times. Time to reach C_max - 2-5 hours.The connection with the plasma proteins of albendazole sulfoxide is 70%. The half-life of the metabolite is 8-15 hours, with hepatic insufficiency up to 35 hours. The half-life of albendazole sulfoxide from the blood plasma is about 8.5 hours. Eliminated mainly by the kidneys, a small amount of albendazole and metabolites is excreted with feces.

Indications:Nematodes: ascariasis, enterobiasis, ankylostomidosis, trichocephalosis, strongyloidiasis, trichinosis (adult forms, first-line drug), gnathostomiasis, capillarial disease (first-line drug), toxocarosis, trichostrongilease.

Microsporidiosis.

Cestodoza (effect on larvae): echinococcosis (first-line preparation), alveococcosis (first-line preparation).

Parasitosis caused by protozoa: giardiasis, trichomoniasis.

ICD-10

I.A00-A09.A07.1 Giardiosis (giardiasis)

I.B50-B64.B60.8 Other specified protozoal infections

I.A00-A09.A07.8 Other specified protozoal intestinal diseases

I.B65-B83.B66.0 Opisthorchiasis

I.B65-B83.B67 Echinococcosis

I.B65-B83.B69.0 Cysticercosis of the central nervous system

I.B65-B83.B75 Trichinosis

I.B65-B83.B76 Ankylostomiasis

I.B65-B83.B77 Ascaridosis

I.B65-B83.B78 Strontyloidosis

I.B65-B83.B79 Trichurosis

I.B65-B83.B80 Enterobiosis

I.B65-B83.B81.4 Intestinal helminthiases of mixed etiology

Contraindications:Hypersensitivity to the drug; pregnancy and the period of breastfeeding; children under 6 years of age (safety and efficacy not studied).

Carefully:With caution in the suppression of bone marrow hematopoiesis; hepatic insufficiency and liver cirrhosis; neurocysticercosis with the involvement of a reticular membrane. Before the beginning of treatment it is necessary to study the retina (there is a risk of aggravation of its pathology).

Pregnancy and lactation:Do not use during pregnancy! The action category for the fetus by the FDA is C. There have not been well-controlled studies on humans. In animal experiments, the drug caused teratogenic and embryotoxic effects.

Lactation: Do not use the drug in lactation or stop breastfeeding for the period of treatment. There is no data on the penetration of the drug into breast milk.

Dosing and Administration:The maximum single dose is 400 mg. The maximum daily dose is 800 mg.

Neurocysticercosis caused by the larval form of the pork chain is 400 mg twice a day for 8-30 days.

Echinococcosis of the liver, lungs, peritoneum caused by the larval form of the canine tapeworm - 400 mg once a day for 3 days; repeated course not earlier than 3 weeks.

With nematodes - 400 mg once a day for 3 days; repeated course not earlier than 3 weeks.

Uncomplicated strongyloidiasis, giardiasis - 400 mg once a day for 3 days; repeated course not earlier than 3 weeks.

A special diet for taking the drug is not required. Take after eating, without chewing the tablets, wash down with water.

Dosage in children

Neurocysticercosis

Inside. Children under 2 years - 15 mg / kg per day for 8 days; if necessary, repeat; 2-18 years - 0.4 g 2 times a day for 8-30 days.

Ankylostomiasis, enterobiasis, ascariasis

Inside. Children under 2 years - 0.2 g once, if necessary, repeat after 3 weeks; 2-18 years - 0,4 g once, if necessary, repeat after 3 weeks.

Strontyloidosis, cestodoza

Inside. Children under 2 years - 0.2 g per day for 3 days, if necessary, repeat after 3 weeks; 2-18 years - 0.4 g once a day for 3 days, if necessary, repeat after 3 weeks.

In children 6-13 years of age, there was no difference in the pharmacokinetics of albendazole compared with adult patients (2013). There is insufficient clinical data on the use of albendazole in children under 6 years of age. The administration of albendazole to patients in this age group is not recommended.

Application in elderly patients

Clinical use of albendazole in 26 patients older than 79 years with echinococcosis suggests the absence of clinically significant differences in pharmacokinetics in elderly patients and young patients.

Side effects:

Allergic reactions: skin rash, itching, fever.

On the part of the hematopoiesis system: leukopenia, granulocytopenia, agranulocytosis, thrombocytopenia, pancytopenia.

From the skin: polymorphic erythema, Stevens-Johnson syndrome.

From the side of the central nervous system: dizziness, headache, meningeal symptoms.

From the digestive tract: diarrhea, nausea, vomiting, abdominal pain. Laboratory increase of serum transaminases.

Urinary system: impaired renal function, acute renal failure.

The profile of side effects of albendazole may differ in case of its use for neurocysticercosis and echinococcosis. Thus, a violation of liver function in patients with neurocysticercosis almost does not occur, and in patients with echinococcosis in the treatment of albendazole, liver failure develops in 15% of cases.

Overdose:Stop breathing, tachyarrhythmias, convulsions.

Treatment: symptomatic.You may need a blood transfusion, the introduction of anticonvulsants.

Interaction:

Corticosteroids, praziquantel, cimetidine increase the serum concentration of albendazole.

Theophylline - it is possible to increase the serum concentration of the latter.

An increase in the concentration of albendazole sulfoxide in bile and the content of the echinococcal cyst by the action of cimetidine has been found, that is, the latter can increase the effectiveness of the drug in the treatment of echinococcosis.

Special instructions:Combination therapy with anthelmintic drugs improves the effect of treatment of helminthiases resistant to monotherapy.

Required monitoring with albendazole:

- examination of the perianal area;

- analysis of feces for eggs and parts of helminths;

- monitoring the parameters of myelogenous hematopoiesis - a general blood test - to detect myelosuppression;

- Functional liver samples (transaminases, alkaline phosphatase, lactate dehydrogenase);

- control of the side effects of theophylline.

Possible debut of neurocysticercosis in patients receiving albendazole for other indications. Patients can complain about neurologic disorders (cerebral palsy, focal symptomatology).The main reason for this is the death of cysticercles present in the brain and intoxication. This clinical picture may appear soon after the end of the course of albendazole. In such a case, glucocorticosteroids and anticonvulsants should be immediately prescribed to the patient.

Patients with liver diseases, including those with hepatic form of echinococcosis, against the background of taking albendazole have a higher risk of suppression of bone marrow hematopoiesis. They need more frequent clinical blood analysis, dynamic control of the hematopoietic function of the red bone marrow.

Instructions

Albendazole (Albendazolum)