Biltricide, 600 mg 6 pcs.

BILTRICIDE is an anthelmintic drug. It increases permeability of helminth cell membranes for calcium ions, which causes generalized contraction of parasite muscles, and also inhibits glucose capture by helminth cells, thus glycogen level decreases and release of lactic acid compounds is stimulated. As a result, death of parasites occurs. Praziquantel is specifically active against trematodes and cestodes.

Pharmacokinetics

Intake

After oral administration praziquantel is quickly and completely absorbed. The maximum plasma concentration is reached within 1-2 hours. Period of half-life of the drug in unchanged form is 1-2.5 hours, together with metabolites – 4 hours.

To achieve therapeutic effect the plasma concentration of the drug must be maintained for 4-6 (maximum up to 10) hours to 0.19 mg/l.

Distribution

The drug penetrates through the barrier. Concentration in cerebrospinal fluid is 10-20% of its concentration in blood plasma. It penetrates into breast milk at a concentration of 20-25% of its concentration in blood serum.

Metabolism

It is subjected to metabolism during “first passage” through the liver. The main metabolites are hydroxylated degradation products of praziquantel.

Elimination

Extracted mainly by the kidneys. More than 80% of the dose is excreted within 4 days, with 90% of this amount excreted within 24 hours.

Pharmacokinetics in special clinical cases

Because the drug has a predominantly renal route of excretion, there may be delayed excretion in renal insufficiency.

In decompensated hepatic insufficiency the drug metabolism in the liver is decreased, which is accompanied by prolongation of T1/2 and increased concentration of praziquantel in blood.

Indications

– Treatment of infections caused by various types of schistosomes (S. haematobium, S. mansoni, S. intercalatum, S. japonicum, S. mekongi)
– Treatment of infections caused by liver flukes (Clonorchis sinensis, Opistorchis viverrini) and lung flukes (Paragonimus westermani, other species)

Pharmacological effect

BILTRICIDE is an anthelmintic drug. It increases the permeability of helminth cell membranes to calcium ions, which causes a generalized contraction of parasite muscles, and also inhibits the uptake of glucose by helminth cells, while the level of glycogen decreases and the release of lactic acid compounds is stimulated. As a result, the parasites die. Praziquantel is specifically active against trematodes and cestodes.

Pharmacokinetics

Suction

After oral administration, praziquantel is rapidly and completely absorbed. Maximum plasma concentration is achieved within 1-2 hours. The half-life of the drug in unchanged form is 1-2.5 hours, together with metabolites – 4 hours.

To achieve a therapeutic effect, it is necessary to maintain a plasma drug concentration of 0.19 mg/l for 4-6 (maximum up to 10) hours.

Distribution

Penetrates through the BBB. The concentration in the cerebrospinal fluid is 10-20% of its concentration in the blood plasma. Penetrates into breast milk in a concentration of 20-25% of the concentration in the blood serum.

Metabolism

It is metabolized during the first pass through the liver. The main metabolites are hydroxylated degradation products of praziquantel.

Removal

It is excreted primarily by the kidneys. More than 80% of the dose is eliminated within 4 days, with 90% of this amount within 24 hours.

Pharmacokinetics in special clinical situations

Since the drug has a predominantly renal route of excretion, in case of renal failure there may be a slowdown in its elimination.

In case of decompensated liver failure, the metabolism of the drug in the liver is reduced, which is accompanied by a prolongation of T1/2 and an increase in the concentration of praziquantel in the blood.

Special instructions

Simultaneous administration of laxatives is not required.

When treating patients with uncomplicated liver failure or hepatosplenic schistosomiasis with Biltricid, higher concentrations are observed and T1/2 is prolonged (metabolic slowdown), and treatment should be carried out in a hospital setting.

Active ingredient

Praziquantel

Composition

1 tablet contains:

Active substances:

praziquantel 600 mg.

Excipients:

corn starch,

microcrystalline cellulose,

polyvinylpyrrolidone,

sodium lauryl sulfate,

magnesium stearate,

hypromellose,

polyethylene glycol MG 4000,

titanium dioxide

Contraindications

– Hypersensitivity to any component of the drug Biltricid;
– Cysticercosis of the eye;
– Combined use with rifampicin.
– Children under 4 years of age (safety and effectiveness have not been established)
With caution: Decompensated liver failure, hepatolienal schistosomiasis, heart rhythm disturbances.

Side Effects

From the digestive system: abdominal pain, nausea, vomiting; lack of appetite; diarrhea mixed with blood.

From the side of the central nervous system: headache, dizziness; dizziness, drowsiness; convulsions.

From the body as a whole: asthenia, fever.

From the musculoskeletal system: myalgia.

From the cardiovascular system: arrhythmia.

Allergic reactions: urticaria; generalized allergic reactions, including polyserositis.

Interaction

When used simultaneously with drugs that induce liver enzymes of the cytochrome P450 system, for example, with anticonvulsants, dexamethasone, the concentration of praziquantel in the blood plasma may decrease, and when combined with drugs that inhibit these enzymes, for example, with cimetidine, it may increase.

Chloroquine reduces the plasma concentration of praziquantel.

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

5 years

Manufacturer

Bayer AG, Germany