DESCRIPTION
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.
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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
AND USAGE
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).
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CONTRAINDICATIONS
BILTRICIDE®
should not be given to patients who previously have shown hypersensitivity
to the drug. Since parasite destruction within the eye may cause
irreparable lesions, ocular cysticercosis should not be treated
with this compound.
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: 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.
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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.
ADVERSE
EFFECTS
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.
OVERDOSAGE
In
rats and mice the acute LD 50 was about 2,500 mg/kg. No data are
available in humans. In the event of overdose a fast-acting laxative
should be given.
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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' 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.
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