Dosage form

Chewable tablets.
400 mg, No. 3
Main physicochemical properties: round biconvex tablets, white, nearly white, or white with a grayish hue, with a score line and a specific odor. The tablets may exhibit marbling on the surface.

Pharmacological group

Anthelmintic agents. Used for nematode infections. Benzimidazole derivatives. Albendazole. ATC code P02CA03.

Pharmacological properties

Pharmacodynamics:
Albendazole is an antiprotozoal and anthelmintic drug from the benzimidazole carbamate group. The drug acts on both intestinal and tissue parasites in the form of eggs, larvae, and adult helminths. Albendazole’s anthelmintic action is due to the inhibition of tubulin polymerization, leading to disruption of metabolism and death of the helminths. Albendazole exhibits activity against such intestinal parasites as: nematodes – Ascaris lumbricoides, Trichuris trichiura, Enterobius vermicularis, Ancylostoma duodenale, Necator americanus, Strongyloides stercoralis, Cutaneous Larva Migrans; cestodes – Hymenolepis nana, Taenia solium, Taenia saginata; trematodes – Opisthorchis viverrini, Clonorchis sinensis; protozoa – Giardia lamblia (intestinalis or duodenalis). Albendazole also demonstrates activity against tissue parasites, including cystic and alveolar echinococcosis caused by Echinococcus granulosus and Echinococcus multilocularis, respectively. Albendazole is effective in treating neurocysticercosis caused by larval invasion of Taenia solium, capillariasis caused by Capillaria philippinensis, and gnathostomiasis caused by Gnathostoma spinigerum. Albendazole destroys cysts or significantly reduces their size (up to 80%) in patients with granular echinococcosis. After albendazole treatment, the number of non-viable cysts increases to 90% compared to 10% in patients who did not undergo treatment. Following albendazole administration for cysts caused by Echinococcus multilocularis, complete recovery was observed in a minority of patients, while improvement or stabilization of the condition was seen in the majority.

Pharmacokinetics:
Poorly absorbed from the gastrointestinal tract (up to 5%), albendazole is not detected unchanged in blood plasma as it rapidly converts in the liver to its primary metabolite, albendazole sulfoxide, which also possesses anthelmintic properties. The bioavailability is low when administered orally (approximately 30%). Concurrent administration with fatty food enhances absorption and increases the maximum concentration (C max ) by 5 times. C max of albendazole sulfoxide is achieved within 2-5 hours. Plasma protein binding is 70%. Albendazole sulfoxide is extensively distributed throughout the body, penetrating in significant amounts into bile, liver, cerebrospinal fluid, urine, and the cyst wall fluids of helminths. In the liver, albendazole sulfoxide is further metabolized to albendazole sulfone (a secondary metabolite) and other oxidized products. The half-life (T 1/2 ) of albendazole sulfoxide is 8-12 hours. It is excreted in the form of various metabolites in urine. Renal function impairment does not affect the clearance of albendazole and its primary metabolites. In the presence of liver impairment, the drug’s bioavailability increases, C max of albendazole sulfoxide doubles, and T 1/2 prolongs. Albendazole is an inducer of microsomal enzyme system cytochrome P450.

Indications

Intestinal forms of helminthiasis and Cutaneous Larva Migrans syndrome (short-term treatment with low doses): enterobiasis, hookworm disease (ancylostomiasis) and necatoriasis, hymenolepiasis, taeniasis, strongyloidiasis, ascariasis, trichocephaliasis, clonorchiasis, opisthorchiasis, giardiasis in children.

Systemic helminthic infections (long-term treatment with high doses):

Cystic echinococcosis (caused by Echinococcus granulosus):

when surgical intervention is not possible;
before surgical intervention;
after surgery, if preoperative treatment was short, if there is spread of parasites, or if live forms were found during surgery;
after percutaneous cyst drainage for diagnostic or therapeutic purposes.
Alveolar echinococcosis (caused by Echinococcus multilocularis):

inoperable disease, especially in cases of local or distant metastases;
after palliative surgical intervention;
after radical surgical intervention or liver transplantation.
Neurocysticercosis (caused by larvae of Taenia solium):

in the presence of single or multiple cysts or granulomatous brain lesions;
in arachnoidal or intraventricular cysts;
in racemose cysts.
Capillariasis (caused by Capillaria philippinensis), gnathostomiasis (caused by Gnathostoma spinigerum and related species), trichinellosis (caused by Trichinella spiralis and T. pseudospiralis), toxocariasis (caused by Toxocara canis and related species).

SIDE EFFECTS