Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Anthelmintic means of a wide spectrum of action; benzimidazole carbamate derivative. Anthelmintic and antiprotozoal . Selectively suppresses the polymerization of beta-tubulin, which leads to the destruction of cytoplasmic microtubules of intestinal tract cells of helminths; causes an irreversible violation of glucose utilization in the helminth organism and inhibits the synthesis of ATP; blocks the movement of secretory granules and other organelles in the muscle cells of roundworms, causing their death. The most effective for larval forms of cestodes is Echinococcus granulosus and Taenia solium; nematodes - Strongyloides stercolatis.
PHARMACOKINETICS
When administered orally, albendazole is poorly absorbed from the gastrointestinal tract, unchanged is not detected in the plasma, bioavailability is low. The intake of fatty foods increases the absorption and C max by 5 times. The time to reach C max of albendazole sulfoxide is 2-5 hours. Binding to plasma proteins - 70%, penetrates in significant amounts into bile, liver, cerebrospinal fluid, urine, wall and liquids of helminth cysts. Metabolised in the liver with the formation of a primary metabolite (albendazole sulfoxide), which has anthelmintic activity. Albendazole sulfoxide is metabolized to albendazole sulfone (secondary metabolite) and other oxidized products.
T 1/2 albendazole sulfoxide is 8-12 hours. It is excreted with bile through the intestine as an active metabolite of albendazole sulfoxide, only a small amount is excreted in the urine. With liver damage, bioavailability is increased, while C max albendazole sulfoxide increases by a factor of 2, and T 1/2 is lengthened. It is the inducer of CYP1A isoenzymes in human liver cells.
INDICATIONS
Echinococcosis, neurocysticercosis, nematodes (ascaridosis, trichocephalosis, ankylostomiasis, enterobiasis, strongyloidiasis), trematodes (opisthorchiasis), giardiasis, microsporidiosis, mixed helminthiases. As an aid in the surgical treatment of echinococcus cysts.
DOSING MODE
When administered orally, a single dose is 400 mg. Frequency and duration of use depend on the indications and treatment regimen.
SIDE EFFECT
On the part of the digestive system: abdominal pain, nausea, vomiting, increased activity of hepatic transaminases.
From the side of the central nervous system: headache, dizziness, meningeal symptoms.
On the part of the hematopoiesis system: leukopenia, granulocytopenia, agranulocytosis, thrombocytopenia, pancytopenia.
Allergic reactions: skin rash, itching.
From the side of the urinary system: a violation of kidney function, acute renal failure.
Other: hyperthermia, increased blood pressure, alopecia.
CONTRAINDICATIONS
Pregnancy, lactation (breastfeeding), children under 3 years old, hypersensitivity to albendazole.
PREGNANCY AND LACTATION
Albendazole is contraindicated in pregnancy and lactation (breastfeeding).
Women of childbearing age during the period of treatment are recommended to use non-hormonal methods of contraception. It is not known whether albendazole and its active metabolite are excreted in breast milk.
In experimental studies on animals, the teratogenicity of albendazole is shown.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution appoint albendazole to patients with hepatic insufficiency, cirrhosis of the liver.
SPECIAL INSTRUCTIONS
With caution apply albendazole in patients with oppression of bone marrow hematopoiesis, liver failure, liver cirrhosis, retinal pathology.
It is necessary to stop therapy with the development of leukopenia. With neurocysticercosis with eye damage before the beginning of treatment, retinal examination is necessary (the risk of aggravation of retinal pathology increases). Patients receiving high doses should be carefully monitored, with constant monitoring of blood and liver function.
DRUG INTERACTION
With simultaneous use with dexamethasone, praziquantel, an increase in the concentration of albendazole sulfoxide in the blood plasma is possible.
An increase in the concentration of albendazole sulfoxide in the bile and in the contents of the echinococcal cyst with an simultaneous use of albendazole and cimetidine has been found, which can increase the effectiveness of echinococcosis treatment.
