Biltricide

Biltricid contains the substance praziquantel, which has effective anthelmintic properties.

The principle of medicinal activity is based on the potentiation of the permeability of helminth cell walls under the action of Ca ions. An increase in Ca values above the normal level inside the helminth body leads to muscle contraction in combination with a disorder of carbohydrate metabolism, a decrease in glycogen values and the formation of toxic indicators of lactic acid derivatives. These changes contribute to the destruction of parasites.

The drug also has a powerful effect on nematodes and cystodes.

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Indications Biltricide

It is used for the following disorders:

• helminthic lesions caused by the action of various types of schistosomes;
• infections caused by the activity of lung or liver flukes (Chinese fluke, as well as Paragonimus westermani, squirrel fluke, etc.).

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Release form

The medicinal component is released in tablets - 6 pieces inside a glass bottle. There is 1 such bottle in a pack.

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Pharmacokinetics

After administration, praziquantel is fully and rapidly absorbed, reaching plasma Cmax values after 1-2 hours. After taking 5-50 mg/kg of the substance, the values of the drug in the peripheral blood are 0.05-5 μg/ml. Compared with the level in the peripheral blood, the indicator in the mesenteric artery is three to four times higher.

Unchanged praziquantel crosses the blood-brain barrier; levels in the CSF are 10-20% of plasma values (data taken from preclinical testing). Given the paucity of information, it can be assumed that the level of praziquantel in human CSF is also approximately 10-20% of its serum values.

20% of the substance from its serum values is excreted with breast milk. After 24 hours from the moment of a single use of a dose of 50 mg / kg or after 32 hours from a 1-day treatment cycle (20 mg / kg of the drug 3 times a day), the values of the drug in breast milk decrease to the minimum detectable mark (4 mcg / l).

Praziquantel undergoes rapid first-pass intrahepatic metabolism (presystemic metabolism). The half-life of the unchanged substance is 1-2.5 hours. The half-life of systemic radioactivity (praziquantel with metabolic elements) is 4 hours. Praziquantel is excreted through the kidneys only in the metabolized state. Over 80% of the administered dose is excreted through the kidneys within 4 days (80-90% of this volume - within the first 24 hours).

The main metabolic components are hydroxylated products that arise during the degradation of praziquantel (they are 4-hydroxycyclohexylcarbonyl analogues). Approximately 60-80% of these hydroxylated products are excreted via the kidneys; another 15-37% - with bile, and the remaining 6% are excreted through the intestinal lumen.

To ensure the required effect, parasites must be exposed to the appropriate concentration of the active ingredient for the required period of time. There is no precise data on humans, but based on preclinical testing and data obtained from pharmacokinetic studies in humans, it can be assumed that plasma levels of the drug must be maintained at 0.6 μm/l (equivalent to 0.1875 μg/ml) for at least 4-6 hours (but not more than 10) to achieve a therapeutic effect.

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Dosing and administration

The medicine is taken orally; chewing the tablet is prohibited. The medicine should be taken before or with food. It is recommended to take the medicine in the evening (with 1 dose per day). If the medicine needs to be taken several times a day, the interval between doses should be 5 hours. Portion sizes are determined by the type of pathogen. Dosages are selected as follows:

• blood schistosome – 40 mg/kg, 1 time per day (the cycle lasts 1 day);
• Schistosoma Mansonii or Schistosoma intercalatum – 20 (2 times) or 40 (1 time) mg/kg per day (1-day course);
• Japanese schistosome or Schistosoma mekongi – 30 (2 times) or 60 (1 time) mg/kg per day (the course lasts 1 day);
• Chinese or squirrel fluke – 25 mg/kg 3 times a day (the cycle lasts 1-3 days);
• lung flukes (also Paragonimus westermani) – 25 mg/kg 3 times a day (2-3-day cycle).

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Use Biltricide during pregnancy

The drug is not prescribed in the first trimester. In the future, it can be used only after assessing all the pros and cons of this option. The decision should be made by the attending gynecologist together with the parasitologist.

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Contraindications

Main contraindications:

• ocular cysticercosis;
• use together with rifampicin;
• personal intolerance to praziquantel and other auxiliary elements of the drug.

Caution is required in the following cases:

• insufficiency of liver function activity, which has a decompensated nature;
• myocardial rhythm disorders;
• hepatosplenic schistosomiasis.

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Side effects Biltricide

Side effects after taking the medicine include:

• polyserositis;
• bloody diarrhea, nausea, anorexia, or vomiting;
• urticaria, anaphylaxis, fever or angioedema;
• convulsions, arrhythmia, dizziness, asthenic conditions or drowsiness;
• myalgia.

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Interactions with other drugs

Substances that induce the action of intrahepatic enzymes reduce plasma levels of praziquantel (while drugs that slow the activity of these enzymes, on the contrary, increase praziquantel levels).

A decrease in the intraplasma level of praziquantel is recorded when Biltricide is combined with chloroquine.

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Storage conditions

Biltricid should be stored in a dry, dark place, out of the reach of children. Temperature indicators should not exceed 30°C.

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Shelf life

Biltricide can be used for a period of 5 years from the date of release of the therapeutic agent.

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Application for children

It is prohibited to prescribe in case of helminthiasis to children under 4 years of age.

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Analogues

Analogues of the drug are the substances Cesol and Azinox with Praziquantel.

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Reviews

Biltricid gets pretty good reviews - with the right dosage, the drug is very effective, quickly getting rid of helminths. Among the disadvantages, they note a large number of side effects that often develop when using the drug, as well as a fairly high cost.

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