Properties
What is it?
ALBENDAZOLE ALBENDAZOLE ALBENDAZOLE USP Qualitative and quantitative composition: Each chewable tablet contains Albendazole USP 400mg. Pharmaceutical form: Albendazole tablet is a white, round, flat chewable tablet with a score line on one side and free from specks. Pharmacological properties: Pharmacodynamics Pharmacological group: Anthelmintic. Albendazole is a broad-spectrum anthelmintic agent. The mechanism of action of albendazole is primarily related to the inhibition of tubulin polymerization, which leads to the loss of cytoplasmic microtubules. Albendazole causes degenerative changes in the helminth cuticle and intestinal cells due to binding to the colchicine-sensitive site of tubulin, thus inhibiting its polymerization or assembly into microtubules. By reducing cytoplasmic microtubules, glucose uptake by larval and adult parasites is impaired and their glycogen stores are depleted. Degenerative changes in the endoplasmic reticulum, mitochondria of the germinal layer, and release of lysosomes reduce the formation of adenosine triphosphate (ATP), which is the energy required for helminth survival. Due to the reduction in energy production, the parasite ceases to move and dies. Pharmacokinetics Absorption and metabolism Albendazole is poorly absorbed from the gastrointestinal tract due to its low solubility in water. Plasma concentrations of albendazole are negligible or undetectable as it is rapidly converted to its sulfoxide metabolite before reaching systemic circulation. Systemic anthelmintic activity is primarily associated with the major metabolite, albendazole sulfoxide. Bioavailability appears to be enhanced when albendazole is taken with a fatty meal (estimated fat content 40g), as evidenced by significantly higher plasma concentrations of albendazole sulfoxide (mean 5-fold higher) compared to administration in the fasting state. Peak plasma concentrations of albendazole sulfoxide are usually achieved between 2 to 5 hours after dosing and average 1.31 mcg/mL (range 0.46 to 1.58 mcg/mL) in six patients with echinococcosis after oral administration of albendazole (400 mg) with a fatty meal. Plasma concentrations of albendazole sulfoxide increase dose-proportionally after a fatty meal (fat content 43.1g) at therapeutic doses. The mean apparent terminal elimination half-life of albendazole sulfoxide typically ranges from 8 to 12 hours, based on data from 25 normal subjects, 14 patients with echinococcosis, and 8 patients with neurocysticercosis. After 4 weeks of treatment with albendazole (200 mg three times daily), 12 patients showed approximately 20% lower plasma concentrations of albendazole sulfoxide than after the first half of the treatment period, suggesting that albendazole may induce its own metabolism. Distribution: Albendazole sulfoxide is 70% protein-bound in plasma and distributes widely throughout the body; it has been detected in urine, bile, liver, cyst fluid, and cerebrospinal fluid (CSF). Plasma concentrations were 3- to 10-fold and 2- to 4-fold higher than simultaneously determined levels in cyst fluid and CSF, respectively. Limited in vitro and clinical data suggest that elimination of albendazole sulfoxide from cysts may occur at a much slower rate than from plasma. Metabolism and excretion: Albendazole is rapidly converted in the liver to its primary metabolite, albendazole sulfoxide, which is further metabolized to albendazole sulfone and other primary oxidative metabolites detected in human urine. Albendazole has not been detected in human urine after oral administration. Urinary excretion of albendazole sulfoxide is minimal, accounting for less than 1%. Biliary elimination is approximately the same as confirmed by concentrations of albendazole sulfoxide. Indications for use Albendazole is indicated for single and mixed infections such as: 1. Nematodes (Ancylostoma, Necator) 2. Roundworm (Ascaris) 3. Pinworm (Enterobius) 4. Whipworm 5. Strongyloides 6. Tapeworm 7. Opisthorchiasis 8. Echinococcosis 9. Neurocysticercosis 10. Systemic nematodes 11. Giardiasis 12. Microsporidiosis Dosage and administration In adults or children over 2 years of age: Take 400mg (1 Albendazole tablet) as a single dose for Enterobius vermicularis, trichuris trichiura, Ascaris lumbricoides, Ancylostoma duodenale, and Necator. For strongyloidiasis or taeniasis, take 400 mg (1 Albendazole tablet) as a single dose for 3 consecutive days. If the patient is not cured after three weeks, a second course of treatment is recommended. Albendazole tablets should be chewed. Contraindications: Albendazole is contraindicated in patients who are hypersensitive to benzimidazoles or any component of albendazole. Special warnings and precautions for use Albendazole has caused bone marrow suppression, aplastic anemia, and agranulocytosis in patients with and without impaired liver function. Patients with liver disease, including hepatic echinococcosis, are at higher risk of bone marrow suppression, leading to pancytopenia, aplastic anemia, agranulocytosis, and leukopenia, and blood monitoring is essential. All patients should discontinue albendazole if a clinically significant decrease in blood cell counts occurs. Interactions with other medicinal products and other forms of interaction Dexamethasone: Plasma concentrations of albendazole sulfoxide increase by 56% when albendazole is administered with dexamethasone at a dose of 8 mg daily, at a dose of 15 mg/kg/day in 8 patients with neurocysticercosis. Praziquantel: When taken on a full stomach, praziquantel (40mg/kg) increases the maximum plasma concentration and area under the curve of albendazole by 50% in healthy subjects (n=10) compared to groups (n=6) taking albendazole alone. Maximum plasma concentration and elimination half-life of albendazole sulfoxide remain unchanged. The pharmacokinetic parameters of praziquantel remain unchanged when taken with albendazole (400mg). Cimetidine: At a dose of (10 mg/kg/day) (n=7), concentrations of albendazole sulfoxide in bile and cyst fluid are doubled compared to albendazole alone (20 mg/kg/day) (n=12). Plasma concentrations of albendazole sulfoxide remained unchanged for 4 hours. Theophylline: The pharmacokinetics of theophylline (aminophylline 5.8 mg/kg infused over 20 minutes) were unchanged by the oral administration of albendazole (400 mg) in 6 healthy subjects. Side effects Several cases of gastrointestinal discomfort and headache have been reported, but a specific relationship to the drug has not been established. Overdose and treatment Toxicity and fatality have been observed in male and female mice at an overdose of 5,000 mg/kg; in rats at doses of 1,300 and 2,400 mg/kg; in hamsters at an overdose of 10,000 mg/kg; and in rabbits at doses of 500 and 1,250 mg/kg. Symptoms observed in animals include diarrhea, vomiting, tachycardia, and respiratory distress. One case of overdose was reported when a patient ingested 16 grams of albendazole over 12 hours. No adverse effects were observed. In case of overdose, symptomatic treatment and general supportive measures are recommended. Use during pregnancy and lactation Pregnancy: There are no adequate and well-controlled studies in pregnant women taking albendazole. Albendazole should be taken during pregnancy only if the potential benefit justifies the potential risk to the fetus. Lactation: Albendazole is excreted in animal milk. It is not known whether it is excreted in human milk. Since most drugs are excreted in human milk, caution should be exercised when a nursing mother takes albendazole. Effect on ability to drive and use machinery No adverse effects on the ability to drive or operate machinery have been reported. List of excipients: Microcrystalline cellulose, Povidone - K-30, Mannitol powder, Sucrose, Aspartame, Saccharin sodium, Purified talc, Magnesium stearate, Sodium starch glycolate, Dry strawberry flavor, Dry orange flavor, Peppermint oil, Purified water. Instructions for use: Keep out of reach of children. Storage instructions: Store at a temperature not exceeding 30°C, in a dark, dry place, out of reach of children. Do not use after the expiry date. Shelf life: 36 months. Dosage form and packaging: Tablet. 1 tablet per blister and 1 blister with instructions for use are placed in a cardboard box. Dispensing category: Pharmaceutical product group II, dispensed by prescription form №3
