Helmindazole tablets 100 mg

Instructions for use Helmindazole tablets 100 mg

Trade name: Helmindazole

International nonproprietary name: Mebendazole

Dosage form: tablets

Composition:

Active substance: Mebendazole (calculated as 100% substance) – 100.0 mg;

Excipients: corn starch – 72.0 mg, colloidal silicon dioxide – 3.0 mg, talc – 3.0 mg, magnesium stearate – 3.0 mg,  crospovidone – 3.0 mg, sodium lauryl sulfate – 0.5 mg, lactose monohydrate – up to a tablet weight of 300.0 mg.

Description:

Round, flat-cylindrical tablets from white to light yellow in color, with a bevel and a score line.

Pharmacotherapeutic group: Anthelmintic agent.

ATC code: P02CA01

Pharmacological properties

Pharmacodynamics:

A broad-spectrum anthelmintic agent; most effective against Enterobius vermicularis, Trichuris trichiura, Ascaris lumbricoides, Ancylostoma duodenale, Necator americanus, Strongyloides stercoralis, Taenia solium, Echinococcus granulosus, Echinococcus multilocularis, Trichinella spiralis, Trichinella nativa, Trichinella nelsoni. By causing irreversible impairment of glucose utilization, it depletes glycogen stores in helminth tissues, inhibits the synthesis of cellular tubulin, and also slows the synthesis of adenosine triphosphate (ATP).

Pharmacokinetics:

Practically not absorbed in the intestine. After taking the drug at a dose of 100 mg twice daily for three consecutive days, the plasma concentration of mebendazole and its metabolite (2-amine derivative) does not exceed 0.03 µg/ml and 0.09 µg/ml, respectively. Plasma protein binding is 90%. It is distributed unevenly throughout the organs, accumulating in adipose tissue, liver, and helminth larvae. In the liver, it is metabolized to a 2-amine derivative, which lacks anthelmintic activity. Half-life is 2.5-5.5 hours. More than 90% of the dose is eliminated through the intestine unchanged. The absorbed portion (5-10%) is excreted by the kidneys.

Indications for use

Enterobiasis, ascariasis, hookworm infection, strongyloidiasis, trichuriasis, trichinellosis,  taeniasis, both in mono-infections and in mixed helminthiases; echinococcosis (when surgical treatment is not possible).

Contraindications

• Hypersensitivity to mebendazole, other components of the drug,
• Ulcerative colitis,
• Crohn's disease,
• Hepatic insufficiency,
• Children under 3 years of age,
• Pregnancy,
• Lactation period,
• Lactose intolerance,
• Lactase deficiency,
• Glucose-galactose malabsorption,
• Concurrent use with metronidazole, phenytoin, carbamazepine, ritonavir.

Use during pregnancy and breastfeeding

Pregnancy.

Use of the drug during pregnancy is contraindicated.

Breastfeeding period.

There are no data on whether mebendazole passes into breast milk. If use of the drug is necessary during lactation, breastfeeding is recommended to be discontinued.

Dosage and administration

Orally, with a small amount of water.

For adults and children over 3 years old.

For enterobiasis: 100 mg/day (1 tablet) as a single dose; treatment course is 1 day. Since reinfection with enterobiasis is quite common, treatment should be repeated after 2 and 4 weeks.

Simultaneous treatment of all family members is recommended.

For ascariasis, trichuriasis, hookworm infection, and mixed helminthic infections: 200 mg/day (1 tablet in the morning, 1 tablet in the evening); treatment course is 3 days.

For taeniasis, strongyloidiasis: Adults: 400 mg/day (2 tablets in the morning, 2 tablets in the evening); treatment course is 3 days. Children over 3 years: 200 mg/day (1 tablet in the morning, 1 tablet in the evening); treatment course is 3 days.

For echinococcosis: Adults and children over 14 years: For the first three days, 500 mg twice daily; for the next 3 days, the dose is increased to 500 mg three times daily; subsequently, the dose is increased to 1000-1500 mg three times daily. The average duration of treatment for echinococcosis caused by Echinococcus granulosus is 4-6 weeks, and for that caused by Echinococcus multilocularis – up to two years.

For trichinellosis: On day 1: 200-300 mg three times daily; on day 2: 200-300 mg four times daily; and from day 3 to day 14: 500 mg three times daily.

Adverse reactions

Allergic reactions: skin rash, urticaria, angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis, exanthema, anaphylactic and anaphylactoid reactions.

Blood and lymphatic system disorders: neutropenia.

Gastrointestinal disorders: nausea, vomiting, abdominal pain, diarrhea, increased activity of "liver" transaminases, alkaline phosphatase, hepatitis (with long-term use in high doses).

Nervous system disorders: dizziness, headache, drowsiness, convulsions.

Renal and urinary disorders: hypercreatininemia, glomerulonephritis (with long-term use in high doses).

Other: hair loss (with long-term use in high doses).

Overdose

Symptoms: abdominal pain, nausea, vomiting, diarrhea. With long-term use in high doses: reversible liver function disorders, hepatitis, neutropenia.

Treatment: remove the drug from the stomach by inducing vomiting or gastric lavage, administer activated charcoal, provide symptomatic therapy.

Drug interactions

Reduces the need for insulin in patients with diabetes mellitus.

Should not be used concurrently with lipophilic substances.

Cimetidine may increase its blood concentration; carbamazepine and other metabolism inducers may decrease it; therefore, the concentration of the medicinal product in the blood serum should be monitored.

Concurrent use of mebendazole and metronidazole should be avoided.

Special warnings and precautions

The drug contains lactose, therefore it is contraindicated in patients with rare hereditary lactose intolerance, lactase deficiency, or glucose/galactose malabsorption.

In patients with diabetes mellitus, plasma glucose concentration should be monitored.

With long-term use, peripheral blood count, liver and kidney function should be monitored.

For 24 hours after administration, consumption of ethanol, fatty foods, and intake of laxatives is prohibited.

Periodic examination of anal swabs and stool after treatment is mandatory; therapy is considered effective if no helminths or their eggs are detected for the following 7 days.

Results from studies on the development of Stevens-Johnson syndrome and toxic epidermal necrolysis indicate a possible association between their occurrence and the concurrent use of mebendazole and metronidazole. There are no other data documenting cases of such drug interaction. Therefore, concurrent use of mebendazole and metronidazole should be avoided.

Effects on ability to drive and use machines

Patients should exercise caution when driving vehicles or operating machinery, as dizziness and drowsiness may occur during treatment.

Dosage form

Tablets 100 mg.

6 or 10 tablets in a blister strip made of polyvinyl chloride film and printed lacquered aluminum foil.

1, 2, 3  or 4 blister packs of 6 tablets or 1 blister pack of 10 tablets, together with the instructions for use, are placed in a cardboard carton.

Storage conditions

In a dry place, protected from light and moisture  at a temperature not exceeding 25 ^oC. Keep out of reach of children.

Prescription status

By prescription.

Shelf life

2 years. Do not use after the expiration date printed on the packaging.

Name and address of the legal entity in whose name the registration certificate is issued / Organization accepting claims:

JSC "AVVA RUS", Russia, 121614,

 Moscow, Krylatskie Kholmy st., 30, building 9.

Tel.: +7 (495) 956-75-54

Production site address:

JSC "AVVA RUS", Russia, 610044, Kirov region,  Kirov, Luganskaya st., 53a.

Tel.:  +7 (8332) 25-12-29

avva.com.ru