Biltricide^® (Tablets) Instructions for Use

Marketing Authorization Holder

Bayer, AG (Germany)

Manufactured By

Bayer, AG (Germany)

Labeled By

BAYER, AG (Germany)

Or

PROCTER & GAMBLE HEALTH AUSTRIA, GmbH and Co. OG (Austria)

Quality Control Release

BAYER, AG (Germany)

ATC Code

P02BA01 (Praziquantel)

Active Substance

Praziquantel (Rec.INN registered by WHO)

Dosage Form

Biltricide®

Film-coated tablets, 600 mg: 6 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white with a slight orange tint, oblong, biconvex, with the engraving “BAYER” on one side and “LG” on the other; both sides of the tablet have 3 division lines.

Excipients : corn starch (maize starch), microcrystalline cellulose, povidone, sodium lauryl sulfate, magnesium stearate, hypromellose 15 cp (hydroxypropyl methylcellulose 2910), macrogol 4000 (polyethylene glycol 4000), titanium dioxide.

6 pcs. – dark glass bottles (1) – cardboard packs.
6 pcs. – dark glass bottles (1) – cardboard packs with first opening control (sticker).

Clinical-Pharmacological Group

Anthelmintic drug

Pharmacotherapeutic Group

Anthelmintic agent

Pharmacological Action

Anthelmintic agent, a derivative of pyrazinoisoquinoline. It has a broad spectrum of action, which includes many trematodes and cestodes. Thus, Praziquantel is highly active against all human pathogenic agents of schistosomiasis, clonorchiasis, paragonimiasis, opisthorchiasis, as well as against Fasciolopsis buski, Heterophyes heterophyes and Metagonimus yokogawai (intestinal flukes). Among trematodes, Fasciola hepatica is resistant to praziquantel; the mechanism of resistance is not clear.

Praziquantel is highly effective against agents of intestinal cestodiasis: hymenolepiasis (Hymenolepis nana), diphyllobothriasis (Diphyllobothrium latum), taeniarhynchosis (Taeniarhynchus saginatus), taeniasis (Taenia solium), and also acts on cysticerci.

Praziquantel is characterized by two main effects on sensitive helminths. In low doses, it causes an increase in muscle activity, followed by contraction of the musculature and spastic paralysis. In slightly higher doses, it causes damage to the tegument (the outer covering of flatworms). The mechanism of action is not fully understood. It is believed that the effect of praziquantel is due to its ability to increase membrane permeability to calcium ions (and some other mono- and divalent cations).

Pharmacokinetics

Rapidly and completely absorbed from the gastrointestinal tract. C_max is reached in 1-3 hours. Plasma protein binding is 80%. Metabolized in the liver to form inactive mono- and polyhydroxylated metabolites. T_1/2 is 0.8-1.5 hours for praziquantel and 4-6 hours for its metabolites.

It is mainly excreted by the kidneys (80% within 4 days), predominantly in the form of metabolites: 90% is excreted within 24 hours. A small amount is excreted in the feces. It passes into breast milk in small amounts. In case of renal impairment, excretion is slowed down; in case of liver damage, the intensity of metabolism is reduced, which is accompanied by a longer presence of unchanged praziquantel in the body with the creation of high concentrations.

Indications

Schistosomiasis, including intestinal schistosomiasis and genitourinary schistosomiasis; opisthorchiasis, clonorchiasis, paragonimiasis, metagonimiasis, fasciolopsiasis and other trematodoses caused by sensitive helminths. Intestinal cestodiasis: hymenolepiasis, diphyllobothriasis, taeniarhynchosis, taeniasis. Neurocysticercosis.

ICD codes

Dosage Regimen

Administer the dosage based on the specific parasitic infection and the patient’s body weight.

For schistosomiasis caused by Schistosoma haematobium, S. mansoni, or S. intercalatum, administer a total dose of 40 mg/kg as a single oral dose or as two divided doses of 20 mg/kg on the same day.

For schistosomiasis caused by Schistosoma japonicum or S. mekongi, administer a total dose of 60 mg/kg as two divided doses of 30 mg/kg on the same day or as three divided doses of 20 mg/kg in one day.

For clonorchiasis, opisthorchiasis, and intestinal fluke infections, administer 25 mg/kg three times daily for one or two consecutive days.

For paragonimiasis, administer 25 mg/kg three times daily for two consecutive days.

For intestinal cestodiasis (taeniasis, diphyllobothriasis), administer a single dose of 10-25 mg/kg.

For hymenolepiasis, administer a single dose of 25 mg/kg; repeat the dose after 7-10 days.

For neurocysticercosis, administer 50 mg/kg/day in three divided doses for 14 days; corticosteroid co-administration is recommended to manage inflammatory reactions.

Swallow tablets whole with fluid during a meal; do not chew the tablets due to their bitter taste.

Space doses by 4-6 hours for multi-dose regimens; a shorter interval is acceptable if well tolerated.

Adjust the total daily dose for patients with severe hepatic impairment; avoid use in hepatic cysticercosis.

Adverse Reactions

From the central and peripheral nervous system headache, dizziness, drowsiness, myalgia; when treating neurocysticercosis, meningism, thinking disorders, increased intracranial pressure, hyperthermia are possible.

From the digestive system abdominal pain, nausea, vomiting; rarely – transient increase in liver transaminase levels.

Allergic reactions rarely – fever, skin rashes.

Contraindications

Hypersensitivity to praziquantel, ocular cysticercosis, first trimester of pregnancy, lactation, children under 4 years of age, hepatic insufficiency, hepatic cysticercosis.

Use in Pregnancy and Lactation

Praziquantel is contraindicated for use in the first trimester of pregnancy and during lactation (breastfeeding).

In the second and third trimesters of pregnancy, Praziquantel is used only for strict indications.

If use during lactation is necessary, it is recommended to interrupt breastfeeding on the day of praziquantel intake and for the next 72 hours.

Use in Hepatic Impairment

Contraindicated in hepatic insufficiency, hepatic cysticercosis.

Pediatric Use

Contraindicated in children under 4 years of age.

Special Precautions

Praziquantel is not used for ocular cysticercosis due to the danger of developing eye tissue damage during the death of cysticerci.

Effect on ability to drive vehicles and mechanisms

During the intake of praziquantel and for the following 24 hours, it is necessary to refrain from driving vehicles and other potentially hazardous activities.

Drug Interactions

Dexamethasone reduces the plasma concentration of praziquantel.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.