Biltricid

Biltricid contains praziquantel, which has effective anthelmintic properties.

The principle of drug activity is based on the potentiation of the permeability of helminth cell walls under the action of Ca ions. An increase in Ca above normal levels inside the body of the helminth leads to muscular 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.

There is also a powerful effect of the drug on nematodes with cystodes.

[1], [2]

Indications Biltricid

Used for such disorders:

• helminth infections caused by various types of schistosomes;
• infections caused by pulmonary or hepatic fluke activity (Chinese fluke, but also Paragonimus westermani, squirrel fluke, etc.).

[3], [4]

Release form

The release of the drug component is implemented in tablets - 6 pieces inside a glass bottle. In pack 1 such a bottle.

[5]

Pharmacokinetics

After the introduction of praziquantel, it is fully absorbed at high speed, reaching plasma values of Cmax after 1-2 hours. After taking 5-50 mg / kg of a substance, the values of drugs inside the peripheral blood are 0.05-5 μg / ml. Compared to the level inside the peripheral blood, the rate inside the mesenteric artery is three times / four times higher.

Praziquantel in unchanged condition overcomes the BBB; indicators inside the cerebrospinal fluid are 10-20% of plasma values (data taken from preclinical testing). Taking into account the small amount of information, it can be assumed that the level of praziquantel inside the human cerebrospinal fluid also equals approximately 10-20% of its serum values.

20% of the substance of its serum indicators excreted in human milk. After 24 hours from the moment of 1-time use of a portion of 50 mg / kg or after 32 hours from the 1-day treatment cycle (20 mg / kg of the drug 3 times per day), the drug values inside the mother's milk are reduced to the minimum detectable mark (4 µg / l).

Praziquantel undergoes rapid metabolic processes during the 1st intrahepatic passage (influence of first-pass metabolism). The term half-life of an unchanged form of a substance is 1-2.5 hours. The term half-life of systemic radioactivity (praziquantel together with metabolic elements) is 4 hours. Excretion of praziquantel through the kidneys occurs only in a metabolized state. Over 80% of the applied portion is excreted through the kidneys for 4 days (80-90% of this volume - for the first 24 hours).

The main metabolic components are hydroxylated products arising in the process of praziquantel degradation (they are 4-hydroxycyclohexylcarbonyl analogues). Approximately 60-80% of these hydroxylated products are excreted through the kidneys; another 15-37% is from the bile, and the remaining 6% is excreted through the intestinal lumen.

In order to provide the desired effect, the parasites must be influenced by a suitable concentration of the active element over the required time period. There are no accurate data regarding humans, but based on preclinical testing and information obtained in human pharmacokinetics studies, it can be assumed that for the development of a therapeutic effect, plasma drug indicators should be maintained at 0.6 μm / l (corresponding to 0.1875 μg / ml) for at least 4-6 hours (but not more than 10).

[6], [7], [8]

Dosing and administration

The drug is taken orally; chew pill prohibited. It is necessary to use drugs before eating or with it. It is recommended to apply the medicine in the evening (with a 1-fold dose per day). If the medicine needs to be consumed several times a day, the interval between applications should last 5 hours. Portion sizes are determined by the type of pathogenic pathogen. Dosages are selected as follows:

• blood schistosome - 40 mg / kg, 1 time per day (the cycle lasts 1 day);
• Munson Schistosome or Intercalatum Schistosome - 20 (2-fold) or 40 (1 one-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 per day (the cycle lasts 1-3 days);
• pulmonary flukes (also Paragonimus westermani) - 25 mg / kg 3-fold per day (2-3-day cycle).

[16]

Use Biltricid during pregnancy

In the 1st trimester, the drug is not prescribed. In the future, it can only be used after evaluating all the pros and cons of this option. The decision must be taken by the treating gynecologist together with the parasitologist.

[9], [10], [11],

Contraindications

The main contraindications:

• eye cysticercosis;
• use together with rifampicin;
• personal intolerance to praziquantel and other auxiliary elements of drugs.

Caution is required for such violations:

• failure of the activity of the hepatic function, which has a decompensated nature;
• myocardial rhythm disorders;
• hepatolenal schistosomiasis.

[12], [13],

Side effects Biltricid

Among the adverse events after taking the medication:

• polyserotic;
• bloody diarrhea, nausea, anorexia, or vomiting;
• urticaria, anaphylaxis, fever, or Quincke's edema;
• convulsions, arrhythmia, dizziness, asthenic conditions or drowsiness;
• myalgia.

[14], [15]

Interactions with other drugs

Substances that induce the action of intrahepatic enzymes reduce the plasma indices of praziquantel (with drugs that slow down the activity of these enzymes, praziquantel values, on the contrary, increase).

A decrease in the intraplasma level of praziquantel is detected when Biltricid is combined with chloroquine.

[17]

Storage conditions

Biltricid must be kept in a dry, closed from the penetration of children, a dark place. Temperature indicators - not above the mark of 30 ° C.

[18],

Shelf life

Biltricid can be used for a 5-year term since the release of the therapeutic agent.

[19]

Application for children

It is forbidden to assign in the case of helminthiasis to children under 4 years of age.

[20],

Analogs

Analogues of the medication are the substances Tsesol and Azinoks with Praziquantel.

[21], [22], [23]

Reviews

Biltricid gets pretty good reviews - with the right dosage selection, the drug acts very effectively, quickly eliminating worms. Among the shortcomings, a large number of adverse symptoms, which often develop with the use of drugs, are noted, as well as a rather high cost.

[24], [25], [26]