Praziquantel

BILTRICIDE® (praziquantel) is a trematodicide provided in tablet form for the oral treatment of schistosome infections and infections due to liver fluke.

BILTRICIDE® (praziquantel) is 2-(cyclohexylcarbonyl)-1,2,3,6,7, 11b-hexahydro-4H-pyrazino [2, 1-a] isoquinolin-4-one with the molecular formula; C ₁₉ H ₂₄ N ₂ O ₂ .

Praziquantel is a white to nearly white crystalline powder of bitter taste. The compound is stable under normal conditions and melts at 136-140°C with decomposition. The active substance is hygroscopic. Praziquantel is easily soluble in chloroform and dimethylsulfoxide, soluble in ethanol and very slightly soluble in water.

BILTRICIDE® tablets contain 600 mg of praziquantel. Inactive ingredients: corn starch, magnesium stearate, microcrystalline cellulose, povidone, sodium lauryl sulfate, polyethylene glycol, titanium dioxide and HPM cellulose.

CLINICAL PHARMACOLOGY

BILTRICIDE® induces a rapid contraction of schistosomes by a specific effect on the permeability of the cell membrane. The drug further causes vacuolization and disintegration of the schistosome tegument.

After oral administration BILTRICIDE® is rapidly absorbed (80%), subjected to a first pass effect, metabolized and eliminated by the kidneys. Maximal serum concentration is achieved 1-3 hours after dosing. The half-life of praziquantel in serum is 0.8-1.5 hours.

INDICATIONS

BILTRICIDE® is indicated for the treatment of infections due to: all species of schistosoma (e.g. Schistosoma mekongi, Schistosoma japonicum, Schistosoma mansoni and Schistosoma hematobium), and infections due to the liver flukes, Clonorchis sinensis/Opisthorchis viverrini (approval of this indication was based on studies in which the two species were not differentiated).

DOSAGE AND ADMINISTRATION

The dosage recommended for the treatment of schistosomiasis is: 3 × 20 mg/kg bodyweight as a one day treatment. The recommended dose for clonorchiasis and opisthorchiasis is: 3 × 25 mg/kg as a one day treatment. The tablets should be washed down unchewed with some liquid during meals. Keeping the tablets or segments thereof in the mouth can reveal a bitter taste which can promote gagging or vomiting. The interval between the individual doses should not be less than 4 and not more than 6 hours.

HOW SUPPLIED

BILTRICIDE® is supplied as a 600 mg white to orange tinged, filmcoated, oblong tablets with three scores. The tablet is coded with "BAYER" on one side and "LG" on the reverse side. When broken each of the four segments contain 150 mg of active ingredient so that the dosage can be easily adjusted to the patient's bodyweight.

Segments are broken off by pressing the score (notch) with thumbnails. If ¹ / ₄ of a tablet is required, this is best achieved by breaking the segment from the outer end.

BILTRICIDE® is available in bottles of 6 tablets.

Store below 86°F (30°C).

Bayer Corporation
Pharmaceutical Division
400 Morgan Lane
West Haven, CT 06516 USA
Made in Germany

Caution: Federal (USA) law prohibits dispensing without a prescription.

In general BILTRICIDE® is very well tolerated. Side effects are usually mild and transient and do not require treatment. The following side effects were observed generally in order of severity: malaise, headache, dizziness, abdominal discomfort with or without nausea, rise in temperature and, rarely, urticaria. Such symptoms can, however, also result from the infection itself. Such side effects may be more frequent and/or serious in patients with a heavy worm burden. In patients with liver impairment caused by the infection, no adverse effects of BILTRICIDE® have occurred which would necessitate restriction in use.

DRUG INTERACTIONS

No data are available regarding interaction of BILTRICIDE® with other drugs.

WARNINGS

No Information Provided.

PRECAUTIONS

Information for the patient: Patients should be warned not to drive a car and not to operate machinery on the day of BILTRICIDE® treatment and the following day.

Minimal increases in liver enzymes have been reported in some patients.

When schistosomiasis or fluke infection is found to be associated with cerebral cysticercosis it is advised to hospitalize the patient for the duration of treatment.

Drug Interactions:  No data are available regarding interaction of BILTRICIDE® with other drugs.

Mutagenesis, Carcinogenesis:  Mutagenic effects in Salmonella tests found by one laboratory have not been confirmed in the same tested strain by other laboratories. Long term carcinogenicity studies in rats and golden hamsters did not reveal any carcinogenic effect.

Pregnancy Category B:  Reproduction studies have been performed in rats and rabbits at doses up to 40 times the human dose and have revealed no evidence of impaired fertility or harm to the fetus due to BILTRICIDE® . There are, however, no adequate and well-controlled studies in pregnant women. An increase of the abortion rate was found in rats at three times the single human therapeutic dose. While animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Nursing mothers:  BILTRICIDE® appeared in the milk of nursing women at a concentration of about 1 / 4 that of maternal serum. Women should not nurse on the day of BILTRICIDE® treatment and during the subsequent 72 hours.

Pediatric use:  Safety in children under 4 years of age has not been established.