Nemozol, 100 mg/5 ml suspension 20 ml

Nemozolol is an anthelmintic drug. Main mechanism of action is connected with inhibiting effect on polymerization of beta-tubulin, which leads to destruction of cytoplasmic micro-channels of cells of intestinal tract of helminthes; it changes course of biochemical processes (inhibits utilization of glucose), blocks movement of secretory granules and other organelles in muscle cells of roundworms, causing their death. It is most active against larval forms of cestodes – Echinococcus granulosus and Taenia solium, against nematodes – Strongyloides stercolatis.

Pharmacokinetics

Intake and distribution

After oral administration it is poorly absorbed from the gastrointestinal tract, unchanged is not determined in plasma. Bioavailability when ingested is low, about 30%. Simultaneous use with fatty food increases absorption and Cmax value in blood plasma by 5 times.

Metabolism and excretion

Albendazole is rapidly biotransformed in the liver into the primary metabolite – albendazole sulfoxide, which also has anthelminthic activity. Cmax of albendazole sulfoxide in blood plasma is reached within 2 to 5 hours, the binding with plasma proteins is 70%. Albendazole sulfoxide is almost completely distributed throughout the body; it is found in the urine, bile, liver, cyst wall and cystic fluid, cerebrospinal fluid.

Albendazole sulfoxide is converted in the liver to albendazole sulfone (secondary metabolite) and other oxidized products. T1/2 of albendazole sulfoxide is 8-12 hours. It is excreted as different metabolites in the urine.

Pharmacokinetics in special clinical cases

The excretion of albendazole and its main metabolite does not change with impaired renal function.

In patients with impaired liver function the bioavailability is increased, Cmax of albendazole sulfoxide in plasma is increased by 2 times, T1/2 is prolonged. Albendazole is an inducer of microsomal enzymes of cytochrome P450 system; it accelerates metabolism of many drugs.

Indications

nematodes:
ascariasis, causative agent – round helminth Ascaris lumbricoidesl;
trichocephalosis (whipworm), caused by the round helminth Trichocephalus trichiurus;
enterobiasis (pinworms), the causative agent is the round helminth – Enterobius vermicularis;
hookworm (hookworm), pathogens americanus – Ancylostoma duodenale and Necator
trichinosis, pathogens – Trichinella spiralis;
toxocariasis, causative agent – Toxocara canis;
giardiasis, causative agent – Giardia intestinalis;
strictyloidosis (intestinal eel), causative agent – round helminth Strongiloides strcoralis, as well as mixed infestations

– tissue cestodoses:

Neurocysticercosis, causative agent – Cysticercus cellulosus (larval stage of pork tapeworm);
hydatid echinococcosis of the liver, lungs, peritoneum, causative agent – Echinococcus granulosus (larval stage of the canine tapeworm);

as an adjuvant in the surgical treatment of alveolar echinococcosis, the causative agent is Echinococcus multilocularis.

Pharmacological effect

Pharmacotherapeutic group: anthelmintic and antiprotozoal agent.

ATX code: P02CA03

Pharmacological properties

Pharmacodynamics

Nemozol is an anthelmintic drug, the pharmacological properties of which are determined by the action of the active substance albendazole. Albendazole belongs to the group of carbamate benzimidazoles. The mechanism of action of albendazole is its ability to disrupt the activity of the microtubular system of the cells of the intestinal canal of helminths, causing damage to the tubulin protein.

The consequence of this is biochemical disturbances in the cell and inhibition of the transport of glucose and fumarate reductose, which underlies the suppression of cell division at the metaphase stage and with which the inhibition of oviposition and the development of helminth larvae is associated. Albendazole blocks the movement of secretory granules and other organelles in the muscle cells of roundworms, causing their death. Albendazole is effective against most intestinal nematodes, as well as larval (larval stages) cestodes, as well as Giardia. Albendazole as an antiparasitic drug has a fairly wide spectrum of action.

Pharmacokinetics

Suction. After oral administration, the drug is poorly absorbed from the gastrointestinal tract and is not detected in unchanged form in the blood plasma. Bioavailability when taken orally is low. Eating fatty foods increases absorption and maximum concentration by 5 times. Metabolism. Albendazole is rapidly converted in the liver into the primary metabolite albendazole sulfoxide, which also has anthelmintic activity. Distribution. The maximum plasma concentration of albendazole sulfoxide is achieved 2-5 hours after administration. 70% of the metabolite is bound to plasma proteins and is completely distributed throughout the body: found in urine, bile, liver, in the wall and fluid of helminth cysts, and cerebrospinal fluid. Excretion. Albendazole sulfoxide is converted in the liver to albendazole sulfone (a secondary metabolite) and other oxidized products. The half-life of albendazole sulfoxide is 8-12 hours.

It is excreted through the kidneys in the form of various metabolites. Renal excretion of albendazole and albendazole sulfoxide is negligible. In patients with impaired renal function, clearance does not change. In patients with liver damage, bioavailability increases, the maximum concentration of albendazole sulfoxide in blood plasma increases by 2 times, and the half-life is extended. Albendazole induces cytochrome CYPIA2 in human liver cells and accelerates the metabolism of many drugs.

Special instructions

It is recommended to treat all family members simultaneously. Monitoring of blood cellular composition is recommended; If leukopenia occurs, discontinue drug therapy. In case of neurocysticercosis with eye damage, before starting treatment, it is necessary to examine the retina due to the risk of worsening its pathology. In women of childbearing age, a pregnancy test is performed before starting treatment. During therapy and for 1 month after its completion, reliable contraception is necessary.

It should be remembered that before using albendazole, like any other anthelmintic drug, you should thoroughly clean the room, wash children’s toys, carry out hygiene procedures daily (morning and evening), and change underwear. During treatment and several days after taking the drug, it is advisable to change bed linen more frequently or iron it with a hot iron. Concomitant use of albendazole and theophylline may lead to an increased risk of theophylline toxicity (nausea, vomiting, rapid heartbeat, seizures). Although single doses of albendazole do not inhibit theophylline metabolism, albendazole does induce cytochrome P4501A in hepatocytes. In this regard, it is recommended to monitor plasma concentrations of theophylline during treatment with albendazole. Patients should avoid consuming grapefruit products while taking albendazole as plasma concentrations of albendazole may increase, increasing the risk of adverse reactions.

Impact on the ability to drive vehicles and machinery

It is necessary to avoid driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions, as the drug can cause dizziness and other side effects that can affect these abilities.

Active ingredient

Albendazole

Composition

Every 5 ml of suspension contains:

Active substance: albendazole 100.00 mg

Excipients: microcrystalline cellulose and sodium carmellose (microcrystalline cellulose 84%, sodium carmellose 11%, water 5%) – 25.00 mg, sodium carmellose 45.00 mg, glycerol 750.00 mg, benzoic acid 10.00 mg, potassium hydroxide 10.50 mg, sorbic acid 10.00 mg, polysorbate 80 5.00 mg, sorbitol 2750.00 mg, fruit flavor 0.01 ml, ice cream flavor 0.0025 ml, purified water up to 5 ml.

Pregnancy

Albendazole is contraindicated during pregnancy and breastfeeding.

Contraindications

– Hypersensitivity to albendazole, other components of the drug and other benzimidazole derivatives;
– fructose intolerance;
– pathology of the retina;
– children under 1 year of age;
– pregnancy and breastfeeding

With caution

Albendazole is used with caution in cases of liver dysfunction (it is necessary to regularly monitor liver function before and during treatment), inhibition of bone marrow hematopoiesis, and liver cirrhosis.

Side Effects

From the digestive system: impaired liver function with changes in functional liver tests (weak or moderate increase in the activity of “liver” transaminases), hepatitis, acute liver failure, epigastric pain, anorexia, constipation, diarrhea and dry mouth, nausea, vomiting.

From the hematopoietic system: inhibition of bone marrow hematopoiesis (leukopenia, granulocytopenia, agranulocytosis, thrombocytopenia, pancytopenia, aplastic anemia, suppression of bone marrow activity, neutropenia).

From the cardiovascular system: increased blood pressure.

From the central nervous system: headache and dizziness, meningeal symptoms, increased intracranial pressure.

From the urinary system: changes in kidney function indicators (acute renal failure).

From the skin: itching, skin rash, erythema multimorpha, Stevens-Johnson syndrome. Allergic reactions: angioedema, immediate hypersensitivity reactions.

Other: hyperthermia, alopecia. If any of the side effects indicated in the instructions get worse, or any other side effects not listed in the instructions appear, you must inform your doctor.

Interaction

Concomitant use of albendazole with praziquantel, dexamethasone and cimetidine may increase the concentration of albendazole sulfoxide in the blood.

Concomitant use with carbamazepine, phenytoin, phenobarbital and panax ginseng may lead to a decrease in the concentration of albendazole in the intestine.

Overdose

Symptoms: increased dose-dependent side effects.

Treatment: gastric lavage, use of activated carbon, symptomatic therapy.

Storage conditions

Store in a dry place, protected from light, at a temperature below 25° C.

Keep out of the reach of children.

Shelf life

3 years

Manufacturer

Ipka Laboratories Limited, India