Biltricide® (Biltricide®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substancePraziquantelPraziquantel
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  • Biltricide®
    pills inwards 
    Bayer Schering Pharma AG     Germany
    • Dosage form: & nbspfilm-coated tablets
    Composition:

    1 tablet, coated, contains:

    active substance: praziquantel 600 mg;

    Excipients: corn starch, microcrystalline cellulose, polyvinylpyrrolidone, sodium lauryl sulfate, magnesium stearate, hypromellose, polyethylene glycol MG 4000, titanium dioxide.

    Description:

    Oblong, biconvex tablets, covered with a film membrane white or almost white with a light orange tint. On the front side of the tablet - engraving "BAYER", on the reverse -"LG"There are 3 dividing risks on both sides of the tablet.

    The view of the fracture is a homogeneous mass of white or almost white color.

    Pharmacotherapeutic group:Anthelminthic remedy
    ATX: & nbsp

    P.02.B.A.01   Praziquantel

    Pharmacodynamics:

    Praziquantel increases the permeability of helminth cell membranes to calcium ions, which causes a generalized contraction of the parasite's musculature. Also causes damage to the tegument (the outer cover of flat worms).

    It inhibits the capture of glucose by helminth cells, while the content of glycogen decreases and the release of lactic acid compounds is stimulated. As a result, parasites die.

    Praziquantel is specifically active against trematodes and cestodes, is not active against nematodes (including filarias).

    Safety data based on studies of systemic toxicity, genotoxicity, carcinogenicity, reproductive toxicity, did not reveal the hazard of using praziquantel for of people.

    Pharmacokinetics:

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

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

    Distribution. Penetrates through the blood-brain barrier; 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. Exposed to the metabolism of the "first pass’’ through the liver. Basic metabolites of hydroxylated products praziquantel.

    Excretion. It is carried out mainly through the kidneys.More than 80% of the dose is withdrawn within 4 days, and 90% of this amount - within 24 hours.

    Renal insufficiency. Since praziquantel has a predominantly renal excretion pathway (80% of praziquantel and its metabolites are excreted by the kidneys), renal failure may be slowed by excretion.

    Liver failure. Decompensated hepatic insufficiency reduces the metabolism of the drug in the liver, which is accompanied by an elongation of the half-life and an increase in the concentration of praziquantel in the 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 hepatic ligament (Clonorchis sinensis, Opistorchis viverrini) and pulmonary flukes (Paragonimus westermani, etc.).

    Contraindications:

    - Hypersensitivity to any component of the drug;

    - cysticercosis of the eye;

    - combined use with strong cytochrome P450 inducers, such as rifampicin;

    - children under 4 years of age (safety and efficacy not established).

    Carefully:

    Decompensated hepatic insufficiency, hepatolienal schistosomiasis, cardiac arrhythmias.

    Pregnancy and lactation:

    Application in pregnancy

    In the safety studies, there was no evidence of potential adverse effects on the maternal organism or fetus. According to WHO publications, the analysis of the benefit-risk ratio has shown that in regions with endemic schistosomiasis or soil-tolerant helminthiases, the benefits of treating pregnant women and women of reproductive age far outweigh the health risks of women and their children. The benefits of treating pregnant women include reducing the incidence of anemia among mothers, increasing the body weight of children and improving their survival.

    According to available data, women living in endemic regions (schistosomiasis and helminthiases transmitted through soil) can receive treatment with praziquantel in I, II and III trimesters of pregnancy.

    In non-endemic regions it is not recommended to prescribe praziquantel in the first trimester of pregnancy.

    Application during lactation

    The concentration of praziquantel in human milk is 20-25% of the concentration in the plasma. It is not known with what probability this substance can cause pharmacological effects in infants. When using the drug in the lactation period, the diagnosis should be established accurately.

    For short-term therapy with praziquantel during lactation, breastfeeding should be avoided during the course of therapy (1 to 3 days) and the next 24 hours (ie for a maximum of 4 days). When deciding whether to suspend breastfeeding, the physician should assess the benefit / risk ratio, taking into account the availability of nutrition equivalent to breast milk and the possible loss of milk production from the mother. Benefit from the continuation of breastfeeding on the background of treatment prazikvantelom certainly exceeds the risk of starving the child and loss of milk production from the mother.

    Dosing and Administration:

    The tablet should be taken orally, without chewing, with a small amount of liquid during or after a meal. If a single dose is recommended per day, then the pill should be taken in the evening. With repeated use of the drug during the day, it is recommended that the interval between doses is not less than 4 and not more than 6 hours.

    When dividing the tablets into 4 parts, each fragment contains 150 mg of the active ingredient, which makes it easy to choose the dosage taking into account the patient's body weight.

    Adults and children over 4 years of age

    Doses of Biltricida® are selected strictly individually and depend on the type of pathogen.

    Schistosoma haematobium: 40 mg / kg body weight once. Duration of treatment - 1 day.

    Schistosoma mansoni and Schistosoma intercalatum: 40 mg / kg 1 once a day or 20 mg / kg 2 times a day. Duration of treatment - 1 day.

    Schistosoma iaponicum. Schistosoma mekongi: 60 mg / kg once a day or 30 mg / kg 2 times a day. Duration of treatment - 1 day.

    Clonorchis sinensis. Opisthorchis viverrini: 25 mg / kg 3 once a day for 1-3 days.

    Paragonimus westermani and other types of pulmonary flukes: 25 mg / kg 3 times a day for 2-3 days:

    Children under 4 years

    Safety of the drug in children younger than 4 years is not established.

    Side effects:

    Side effects vary depending on the dose and duration of treatment praziquantel. In addition, they depend on the types of helminths, the degree of infection, the duration of infection and the localization of helminths in the body.

    The following undesirable phenomena noted with the use of Biltricid® are distributed according to the frequency of occurrence according to the following gradation: very often (≥10% of patients), often (from ≥ 1% to <10% of patients), infrequently ≥0.1% to <1% of patients), rarely (from ≥0.01% to 0.1% of patients), very rarely (<0.01% of patients).

    Disturbances from the nervous system

    Very often: headache, dizziness.

    Often: vertigo, doubt.

    Very rarely: convulsions.

    Disorders from the cardiovascular system

    Very rarely: unspecified rhythm disturbances.

    Disorders from the digestive system

    Very often: gastrointestinal pain and abdominal pain, nausea, vomiting.

    Often: anorexia, diarrhea (very rare with an admixture of blood).

    Disturbances from the skin and subcutaneous tissues

    Very often: urticaria.

    Often: rash.

    Very rarely: itching.

    Disorders from the musculoskeletal system

    Often: myalgia.

    Systemic disorders and conditions

    Very common: fatigue

    Immune system disorders

    Very rarely: allergic reactions (including generalized allergic reactions), eosinophilia.

    Often: malaise, fever.

    Adverse reactions can be caused both by prazikvantelom (I, a direct relationship with the administration of the drug), and arise as a result of an endogenous reaction to the death of parasites (II, an indirect relationship with the drug), as well as symptoms of infection (III, there is no relationship with the drug). It is very difficult conduct a differential diagnosis between I, II and III variants and establish the exact cause of the development of adverse reactions.

    Overdose:

    There are no data on toxicity for humans.

    In case of an overdose, osmotic laxatives should be prescribed.

    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 blood plasma may decrease, and when combined with preparations inhibiting these enzymes, for example, with cimetidine, increase.

    Simultaneous application of the drug with potent inhibitors of cytochrome P450, for example, rifampicin, should be avoided, as it may prevent the achievement of therapeutic concentrations of praziquantel in blood plasma.

    Special instructions:

    In decompensated hepatic insufficiency and hepatolienne schistosomiasis, Biltricid® should be used with caution because of reduced metabolism in the liver and the risk of a longer presence in the increased drug concentration in vascular bed, including collateral vessels. For the treatment, these patients can be hospitalized.

    Published data in vitro showed a possible lack of efficacy of praziquantel in the migration of schistosomes. Data from two observational cohort studies in patients showed that treatment with praziquantel in the acute phase of infection can not prevent the transition of the disease into a chronic form.

    In addition, the use of praziquantel in patients with schistosomiasis can cause clinical disorders (paradoxical reactions, reactions like serum sickness, the Yarisch-Gerxheimer reaction: an acute inflammatory immune reaction that is associated with release of schistosomal antigens). In general, these reactions occur in patients treated in the acute phase of schistosomiasis. They can lead to possible life-threatening phenomena, for example, respiratory failure, encephalopathy and / or cerebral vasculitis.

    Since 80% of praziquantel and its metabolites are excreted by the kidneys, in patients with impaired renal function excretion may be delayed. The nephrotoxic effect of praziquantel is unknown.

    In cases of cardiac arrhythmias and with simultaneous administration with digitalis preparations, treatment with Biltricid® should be performed under the supervision of a physician.Patients who live or live in cysticercosis and trematodosis endemic areas are recommended to undergo treatment in a hospital setting.

    Since Biltricid® can cause exacerbations of central nervous system diseases due to schistosomiasis, paragonimoses, or cysticercosis caused by Taenia solium, as a rule, this drug should not be prescribed to persons with a history of epilepsy and / or other symptoms of possible damage to the central nervous system, for example, subcutaneous nodules that suggest cysticercosis.

    Effect on the ability to drive transp. cf. and fur:

    When using Biltricid®, you should refrain from driving or moving machinery on the day (s) of taking the drug and for the next 24 hours.

    Form release / dosage:Tablets, film-coated, 600 mg.
    Packaging:

    For 6 tablets in a bottle of amber glass, equipped with a plastic stopper; 1 bottle together with instructions for use in a cardboard box.

    Storage conditions:

    At a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013666 / 01
    Date of registration:17.04.2008 / 11.09.2012
    Expiration Date:Unlimited
    The owner of the registration certificate: Bayer Schering Pharma AG Bayer Schering Pharma AG Germany
    Manufacturer: & nbsp
    Representation: & nbspBayer HellsCare AG Bayer HellsCare AG Germany
    Information update date: & nbsp11.02.2017
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