PRAZIQUANTEL
DESCRIPTION:
DISTOCIDE (praziquantel) is a trematodicide provided in tablet form for the
oral treatment of schistosome infections and infections due to liver fluke.
DISTOCIDE (praziquantel) is 2-(cyclohexylcarbonyl)-1,2,3,6,7, 11b-hexahydro-
4H-pyrazino (2, 1-a) isoquinolin-4-one with the molecular formula; C19H24N2O2.
Praziquantel is a white to nearly white crystalline powder of bitter taste. The
compound is stable under normal conditions and melts at 136-140 deg 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.
DISTOCIDE 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.
ACTIONS/CLINICAL PHARMACOLOGY:
DISTOCIDE 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 DISTOCIDE 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:
DISTOCIDE 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, and cysticercosis(approval of this indication was based on studies in which the two species were not differentiated).
CONTRAINDICATIONS:
DISTOCIDE 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 DISTOCIDE 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 DISTOCIDE
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 DISTOCIDE. 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: DISTOCIDE 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 DISTOCIDE treatment and during the subsequent 72 hours.
Pediatric use: Safety in children under 4 years of age has not been established.
DRUG INTERACTIONS:
No data are available regarding interaction of DISTOCIDE with other drugs.
ADVERSE REACTIONS:
ADVERSE EFFECTS
In general DISTOCIDE 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 DISTOCIDE have occurred which would necessitate restriction in
use.
OVERDOSAGE:
In rats and mice the acute LD50 was about 2,500 mg/kg. No data are available in
humans. In the event of overdose a fast-acting laxative should be given.
DOSAGE AND ADMINISTRATION:
The dosage recommended for the treatment of schistosomiasis is: 3 X 20 mg/kg
bodyweight as a one day treatment. The recommended dose for clonorchiasis and
opisthorchiasis is: 3 X 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.
Neurocysticercosis :- 50 mg / kg of body wt. Daily in 3 devided doses for 15 days or as required.
T.solium,t.saginatum,d.pacificum :- 10 mg/kg of body wt. As a single dose.
H.nana :- 15mg/kg of body wt. As a single dose.
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