Albendazole

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ALBENZEE

Composition:

Active substance: albendazole;

5 ml of suspension contain albendazole 200 mg;

Excipients: sucrose; sodium methylparahydroxybenzoate (E 219); sodium propylparahydroxybenzoate (E 217); sodium carmellose; polysorbate 80; citric acid monohydrate; sodium citrate; colloidal anhydrous silicon dioxide; banana flavoring; purified water.

Pharmaceutical form. Oral suspension.

Main physicochemical properties: white or almost white suspension with a pleasant odor, free from foreign particles.

Pharmacotherapeutic group. Anthelmintic agents. Agents used in nematodosis. Benzimidazole derivatives. ATC code P02CA03.

Pharmacological properties.

Pharmacodynamics.

Albenzi is a broad-spectrum antiprotozoal and anthelmintic agent belonging to the carbamate benzimidazole group. Albendazole acts against both intestinal and tissue parasites in the form of eggs, larvae, and adult helminths. The anthelmintic effect of albendazole is due to inhibition of tubulin polymerization, leading to disruption of metabolism and subsequent death of helminths.

Albendazole is active against the following intestinal parasites: nematodes – Ascaris lumbricoides, Trichuris trichiura, Enterobius vermicularis, Ancylostoma duodenale, Necator americanus, Strongyloides stercoralis, Cutaneus Larva Migrans; cestodes – Hymenolepsis nana, Taenia solium, Taenia saginata; trematodes – Opisthorchis viverrini, Clonorchis sinensis; protozoa – Giardia lamblia (intestinalis or duodenalis).

Pharmacokinetics.

After oral administration, the drug is poorly absorbed (up to 5%) from the gastrointestinal tract. Concomitant intake of fatty food increases drug absorption approximately fivefold.

Albendazole is rapidly metabolized in the liver during first-pass metabolism. The main metabolite, albendazole sulfoxide, retains about half of the pharmacological activity of the parent compound.

The elimination half-life of albendazole sulfoxide from blood plasma is approximately 8.5 hours. Albendazole sulfoxide and other metabolites are excreted predominantly in bile, with only a small fraction eliminated in urine. After prolonged administration of high doses, elimination of the drug from cysts continues for several weeks.

Clinical characteristics.

Indications.

Intestinal forms of helminthiases: enterobiasis, ancylostomiasis, necatoriasis, hymenolepiasis, taeniasis, strongyloidiasis, ascariasis, trichocephalosis, clonorchiasis, opisthorchiasis, giardiasis in children.

Contraindications.

Hypersensitivity to albendazole, other benzimidazole derivatives, or to any other component of the drug. Diseases of the retina. Pregnancy and lactation. Planned pregnancy. Women of childbearing age should use effective non-hormonal contraceptive methods during treatment and for 1 month after discontinuation of the drug.

Interaction with other medicinal products and other types of interactions.

Albendazole induces enzymes of the cytochrome P450 system.

Concomitant use with cimetidine, praziquantel, and dexamethasone may increase plasma levels of albendazole metabolites responsible for systemic activity, which in turn may lead to drug overdose.

Medicinal products that may slightly reduce the efficacy of albendazole: anticonvulsants (e.g., phenytoin, fosphenytoin, carbamazepine, phenobarbital, primidone), levamisole, ritonavir.

Therapeutic response should be monitored in patients; alternative dosing regimens or therapies may be required.

Grapefruit juice also increases plasma levels of albendazole sulfoxide.

Due to the potential effect on cytochrome P450 activity, there is a theoretical risk of interaction with the following drugs: oral contraceptives, anticoagulants, oral hypoglycemic agents, theophylline.

When albendazole is used concomitantly with theophylline, plasma theophylline levels should be monitored.

Concomitant intake of the drug with fatty food increases absorption of albendazole from the gastrointestinal tract (see section "Pharmacokinetics").

Special precautions for use.

Short-term treatment of intestinal infections.

To prevent administration of albendazole during early pregnancy, women of childbearing potential should be treated only during the first week after menstruation or after a negative pregnancy test. Reliable contraception is required during therapy.

Albendazole treatment may unmask pre-existing neurocysticercosis, particularly in areas with high prevalence of Tenia solium strains. Patients may develop neurological symptoms such as seizures, increased intracranial pressure, and focal neurological signs due to inflammatory reactions caused by the death of parasites in the brain. Symptoms may appear rapidly after treatment initiation; therefore, prompt initiation of appropriate therapy with corticosteroids and anticonvulsants is necessary.

When administering to women of childbearing potential, the following should be observed:

• Treatment should begin only after a negative pregnancy test;
• Patients must be informed about the necessity of using effective contraceptive methods during treatment and for one month after discontinuation of the drug.

It should be noted that the formulation contains sucrose; therefore, if intolerance to certain sugars has been diagnosed, medical advice should be sought before taking this medicinal product.

The presence of sodium methylhydroxybenzoate (E219) and sodium propylhydroxybenzoate (E217) in the formulation may cause allergic reactions (possibly delayed).

Use during pregnancy or breastfeeding. The drug is contraindicated during pregnancy and lactation, and in women planning to become pregnant. Breastfeeding must be discontinued during treatment with this drug.

Ability to influence reaction speed when driving or operating machinery.

Given the possibility of dizziness as an adverse reaction, it is recommended to refrain from driving vehicles and operating machinery during albendazole treatment.

Method of administration and dosage.

The dose is determined individually by a physician.

Children aged 1 to 2 years with enterobiasis, ancylostomiasis, necatoriasis, ascariasis, trichocephalosis: administer the drug as a single dose of 5 ml of suspension (200 mg) once daily.

Adults and children aged 2 years and older with enterobiasis, ancylostomiasis, necatoriasis, ascariasis, trichocephalosis: administer 10 ml of suspension (400 mg) orally once daily as a single dose.

For confirmed diagnosis of strongyloidiasis, taeniasis, and hymenolepiasis: administer 10 ml of suspension (400 mg) once daily for 3 consecutive days to adults and children aged 2 years and older. For hymenolepiasis, a repeat course of treatment is recommended from day 10 to day 21 after completion of the previous course.

For opisthorchiasis and clonorchiasis: administer 10 ml of suspension (400 mg) twice daily for 3 days to adults and children aged 2 years and older. This regimen is also effective in mixed infestations with Opisthorchis viverrini and Clonorchis sinensis.

For giardiasis: administer 10 ml of suspension (400 mg) once daily for 5 days to children aged 2 to 12 years.

Elderly patients

Experience with the use of the drug in elderly patients is limited. Dose adjustment is not required; however, albendazole should be used with caution in elderly patients with impaired liver function.

Renal impairment

Since albendazole is excreted in negligible amounts by the kidneys, dose adjustment is not necessary in this patient group. However, patients with signs of renal impairment should be closely monitored.

Hepatic impairment

Since albendazole is extensively metabolized in the liver to a pharmacologically active metabolite, impaired liver function may significantly affect its pharmacokinetics. Therefore, patients with abnormal liver function tests (elevated transaminase levels) should be carefully evaluated before initiating albendazole therapy. If significant increases in transaminase levels or clinically relevant decreases in blood parameters occur, treatment should be discontinued.

Children. The drug is contraindicated for use in children under 1 year of age.

Administer to children according to the information specified in the section "Method of administration and dosage."

Overdose.

Symptoms: nausea, vomiting, diarrhea, tachycardia, drowsiness, visual disturbances, visual hallucinations, speech disturbances, dizziness, loss of consciousness, hepatomegaly, elevated transaminase levels, jaundice; respiratory distress, brown-red or orange discoloration of the skin, urine, sweat, saliva, tears, and feces proportional to the administered dose of the drug.

Treatment: perform gastric lavage and administer symptomatic and supportive therapy.

Adverse reactions.

Gastrointestinal tract and liver: stomatitis, dry mouth, heartburn, nausea, vomiting, abdominal pain, flatulence, diarrhea, constipation, transient increase in liver enzyme activity, jaundice, hepatitis, hepatocellular disorders.

Cardiovascular system: increased blood pressure, tachycardia.
CNS and peripheral nervous system: insomnia or somnolence, headache, dizziness, confusion, disorientation, hallucinations, seizures, decreased visual acuity.

Blood and lymphatic system: leukopenia; neutropenia; thrombocytopenia; anemia, including aplastic anemia; agranulocytosis, pancytopenia. Patients with liver disease, including hepatic echinococcosis, are more susceptible to bone marrow suppression.

Skin and subcutaneous tissue: skin rashes, hyperemia, erythema multiforme, Stevens–Johnson syndrome, reversible alopecia, dermatitis, edema.

Renal and urinary system: renal function impairment, acute renal failure, proteinuria.

Allergic reactions: hypersensitivity reactions, including rash; itching; urticaria; bullous eruption; dermatitis; fever.

General disorders: bone and throat pain; chills; weakness.

Patients with liver diseases, including hepatic echinococcosis, are more susceptible to bone marrow suppression.

Shelf life. 3 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Shake well before use.

Packaging. 1 vial per cardboard box.

Prescription category. Prescription only.

Manufacturer. Indochem Remedies Limited.

Manufacturer's address and place of business.
L-14, Verna Industrial Estate, Verna, Goa IN-403 722, India.