Biltritsid

General characteristics. Structure:

Active agent of 600 mg of a prazikvantel.
Excipients: starch corn, cellulose microcrystallic, povidone, sodium lauryl sulfate, magnesium stearate, gipromelloz, macrogoal 4000, titanium dioxide.
Description: oblong, biconvex tablets, film coated, white or almost white color with a subtle orange shade. On the tablet face - an engraving of "BAYER", on reverse - "LG". On both parties of a tablet the 3rd dividing risks are caused.

Pharmacological properties:

Pharmacodynamics. The praziquantel increases permeability of membranes of cells of helminths for calcium ions that causes generalized reduction of muscles of parasites. Also causes damage of a tegument (an outside cover of flat worms). Slows down glucose capture by cells of helminths, at the same time the maintenance of a glycogen decreases and release of compounds of lactic acid is stimulated. Death of parasites results.
The praziquantel is specifically active concerning trematodes and cestodes, is not active concerning nematodes (including filarias).
The data on safety based on researches of system toxicity, genotoxicity, carcinogenicity, reproductive toxicity did not reveal danger of use of a prazikvantel to people.

Pharmacokinetics. Absorption. After intake the praziquantel is quickly and completely soaked up. The maximum concentration in plasma is reached within 1-2 hours. An elimination half-life of a prazikvantel in not changed look 1-2,5 hours, together with metabolites - 4 hours.
It is necessary for achievement of therapeutic effect during 4-6 (as much as possible to 10) hours to maintain concentration of drug in plasma, equal 0.19 mg/l. Distribution. Gets through a blood-brain barrier; concentration in liquor makes 10-20% of its concentration in a blood plasma. Gets into breast milk in the concentration making 20-25% of concentration in blood serum.
Metabolism. Is exposed to metabolism of "the first passing" through a liver. The main metabolites - hydroxylated products of a prazikvantel.
Removal. It is carried out preferential through kidneys. More than 80% of a dose are removed within 4 days, and 90% of this quantity - within 24 hours.
Renal failure. As at a prazikvantel preferential renal way of excretion (80% of a prazikvantel and its metabolites are excreted by kidneys), at a renal failure there can be a delay of its removal.
Liver failure. At a dekompensirovanny liver failure metabolism of drug in a liver is reduced that is followed by lengthening of an elimination half-life and increase in concentration of a prazikvantel in blood.

Indications to use:

■ Treatment  of the infections caused by different types shistosy (S. haematobium, S. mansoni, S.intercalatum, S.japonicum, S.mekongi)
■ Treatment of the infections caused by hepatic flukes (Clonorchis sinensis, Opistorchis viverrini) and pulmonary flukes (Paragonimus westermani, other types)

Route of administration and doses:

The pill should be taken inside, without chewing, with a small amount of liquid in time or after meal. If the single dose of drug in days is recommended, then the pill should be taken in the evening. At repeated use of drug the interval between receptions is within a day recommended not less than 4 and no more than 6 hours. At division of a tablet into 4 parts each fragment contains 150 mg of active ingredient that allows to select easily a dosage taking into account the body weight of the patient. Adults and children are more senior than 4 years
Biltritsid's doses are selected strictly individually and depend on a type of the activator. Schistosoma haematobium: 40 mg/kg of body weight once. Treatment duration - 1 day. Schistosoma mansoni and Schistosoma intercalatum: 40 mg/kg of 1 times a day or 20 mg/kg 2 times a day. Treatment duration-1 day.
Schistosoma japonicum, Schistosoma mekongi: 60 mg/kg of 1 times a day or 30 mg/kg 2 times a day. Treatment duration-1 day.
Clonorchis sinensis, Opisthorchis viverrini: 25 mg/kg 3 times a day within 1-3 days. Paragonimus westermani and other species of pulmonary flukes: 25 mg/kg 3 times a day within 2-3 days. Children up to 4 years
Safety of drug at children is younger than 4 years is not established.

Features of use:

At a dekompensirovanny liver failure and a hepatolienal schistosomiasis the drug Biltritsid® should be used with care because of risk of its longer presence at the increased concentration in a vascular bed, including collateral vessels. Such patients for performing treatment can be hospitalized. In cases of disturbance of a heart rhythm and at a concomitant use with foxglove drugs treatment by the drug Biltritsid® has to be carried out under observation of the doctor. The patients living or living in areas, endemic on cysticercosis and a trematodoz, are recommended to carry out treatment in stationary conditions.
As Biltritsid® can cause the exacerbations of diseases of the central nervous system caused by shistosomoza, paragonimiases or the cysticercosis caused by Taenia solium, as a rule, this drug it is not necessary to appoint to persons in whose anamnesis there are instructions on epilepsy and/or other symptoms of possible damage of the central nervous system, for example, the hypodermic small knots allowing to assume cysticercosis.
Influence on ability to manage the car / moving mechanisms
At use of the drug Biltritsid® it is necessary to refrain from control of the car / moving mechanisms in day/days of administration of drug and during the next 24 hours.

Side effects:

Side effects vary depending on a dose and duration of treatment prazikvantely. Besides, they depend on types of helminths, degree of infection, duration of an infection and localization of helminths in an organism.
The listed below undesirable phenomena noted at drug Biltritsid® use are distributed on emergence frequency according to the following gradation: very often (> 10% of patients), it is frequent (from> 1% to <10% of patients), infrequently (from> 0,1% to <1% of patients), is rare (from> 0,01% to 0,1% of patients), is very rare (<0,01% of patients), - and on systems of bodies.
From immune system: very seldom - allergic reactions (including
generalized allergic reactions), polyserositis, eosinophilia.
 From the central nervous system:  very often - a headache,
dizziness; often - вертиго, drowsiness; very seldom - spasms.
From cardiovascular system: very seldom - arrhythmia.
From the alimentary system: very often - gastrointestinal pains and pains
in a stomach, nausea, vomiting; often - anorexia, diarrhea (it is very rare with blood impurity).
From skin and skin appendages: very often - a small tortoiseshell; very seldom - an itch.
From a musculoskeletal system: often - a mialgiya.
System disturbances and states: often - an indisposition, fever.

Side reactions can be caused as a prazikvantel (I, direct interrelation with administration of drug), and to result from endogenous reaction to death of parasites (II, indirect interrelation with administration of drug), and also to be infection symptoms (III, do not have interrelation with administration of drug).
It is very difficult to carry out the differential diagnosis between I, II and III options and to establish the exact reason of development of side reactions.

Interaction with other medicines:

At simultaneous use with the drugs inducing enzymes of a liver of system of P450 cytochrome, for example, with anticonvulsants, dexamethasone concentration of a prazikvantel in a blood plasma can decrease, and at a combination to the drugs inhibiting these enzymes, for example, with Cimetidinum - to raise. Chloroquine reduces concentration of a prazikvantel in a blood plasma.
It is necessary to avoid simultaneous use of drug with powerful inhibitors of P450 cytochrome, for example, rifampicin as it can interfere with achievement of therapeutic concentration of a prazikvantel in a blood plasma.

Contraindications:

■ Hypersensitivity to any component of drug;
■ Cysticercosis of eyes;
■ the Combined use with rifampicin.
■ Children's age up to 4 years (safety and efficiency are not established)

With care - a dekompensirovanny liver failure, a hepatolienal schistosomiasis, disturbances of a cordial rhythm.

Use at pregnancy and in the period of a lactation
Use at pregnancy
In researches of safety data on potential harmful effects on a maternal organism or a fruit were not obtained. According to publications of WHO the analysis of a ratio of advantage and risk showed that in regions with an endemic schistosomiasis or helminthoses of advantage of treatment of pregnant women and women of reproductive age postponed with the soil considerably surpass risk for health of women and their children.
The advantage of treatment of pregnant women includes decrease in incidence of anemia among mothers, increase in body weight of children and increase in their survival. According to the available data of the woman, living in endemic regions (the schistosomiasis and helminthoses which are transmitted through the soil) can receive treatment prazikvantely in I, II and III trimesters of pregnancy. In ecdemic regions it is not recommended to appoint a praziquantel in the I trimester of pregnancy.
Use in the period of a lactation
Concentration of a prazikvantel in women's milk makes 20-25% of concentration in plasma. It is unknown with what probability this substance can cause pharmacological effects in babies. At use of drug in the period of a lactation the diagnosis has to be established precisely.
For short-term therapy prazikvantely in the period of a lactation it is necessary to refrain from breastfeeding throughout a therapy course (from 1 to 3 days) and the next 24 hours (i.e. within at most 4 days). At making decision on breastfeeding suspension the doctor has to estimate an advantage/risk ratio, in view of availability of the food equivalent to breast milk, and possible loss of volume of production of milk at mother. The advantage of continuation of breastfeeding against the background of treatment prazikvantely certainly exceeds risk of starvation of the child and loss of production of milk at mother.

Overdose:

Data on toxicity for people are absent. In case of overdose it is necessary to appoint osmotic purgatives.

Storage conditions:

Period of validity: 5 years. Not to use after expiry date. At a temperature not above 30 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets film coated 600 mg.
On 6 tablets in the bottle of amber glass supplied with a plastic stopper. 1 bottle together with the application instruction is packed into a cardboard pack.