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Rx
VOMICARE
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Composition:
Each film coated tablet contains:
Ondansetron Hydrochloride USP
eqv. to
Ondansetron 2mg/4mg
DESCRIPTION:
It is the prototype of a new
class of antiemetic drugs developed to control cancer chemotherapy/radiotherapy
induced vomiting and later found to be highly effective in postoperative nausea
and vomiting as well.
Pharmacodynamics
VOMICARE blocks the action of 5-HT through 5-HT3
receptors on vagal afferents in the g.i.t. as well as in NTS and CTZ. Cytotoxic
drugs/radiation produces Nausea and vomiting by causing cellular damage. This
releases mediators including 5-HT from intestinal mucosa which then causes
activation of vagal afferents in the gut. This sends the emetogenic impulses to
the NTS and CTZ causing Vomiting centre to induce vomit.
VOMICARE inhibits emetogenic impulses both at their peripheral origin
and their central relay. It does not block dopamine receptors and apomorphine
or motion sickness induced vomiting.
PHARMACOKINETICS:
VOMICARE is well absorbed from the gastrointestinal tract and
undergoes some first-pass metabolism. The absolute bioavailability is about
60%. It is extensively distributed in the body; results in vitro suggest that
about 70 to 75% of the drug in plasma is protein bound. Bioavailability is
slightly enhanced by the presence of food but is unaffected by antacids. It is cleared
from the systemic circulation by hepatic metabolism, and about 5% of the
unchanged drug excreted from the urine. The terminal elimination half life is
about 3 hours in younger subjects; prolonged to 5 hours in elderly. These
differences are not considered sufficient to warrant dosage adjustments.
However, in patients with severe hepatic impairment, to whom bioavailability
may reach 100% and clearance is markedly slowed, with elimination half life of
15-32 hours, dosage reduction is advisable.
Indication
VOMICARE is a highly selective 5-HT-receptor antagonist with potent
antiemetic activity. It is use in the management of nausea and vomiting induced
by cytotoxic chemotherapy and radiotherapy, particularly when there is severe
or unresponsive to other therapy .
Dose and Adminstration
Ø Prevention of Nausea and vomiting
associated with highly emetogenic cancer therapy:
The recommended adult oral dose
of VOMICRE is single 24mg (three 8mg
tablets) administered 30 minutes before the start of single day highly
emetogenic chemotherapy, including ciplastin.
Geriartic Use: The recommended dosage is same as for the general
population.
Ø Prevention of Nausea and vomiting
associated with moderate emetogenic cancer therapy:
The recommended adult oral dose
is 8mg VOMICARE Tablet given twice a
day. The first dose should be administered 30 minutes before the start of
emetogenic chemotherapy therapy, with the subsequent dose 8 hours after the
first dose. One 8mg of VOMICARE
should be administered twice a day (every 12 hours) for 1-2 days after the
completion of chemotherapy.
Pediartic use: For pediatric patients 12 years of age and older,
the dosage is the same as for adults. For pediatric patients 4 to 11 years of
age, the dosage is on 4mg
VOMICARE Tablet given 3 times a day. The first dose should be
administered 30 minutes before the start of emetogenic chemotherapy therapy,
with the subsequent dose 4 and 8 hours after the first dose. One 4mg VOMICARE tablets should be administered
3 times a day (every 8 hours) for 1-2 days after the completion of
chemotherapy.
Ø Prevention of Nausea and vomiting
associated with Radio therapy:
The recommended adult oral dose
is 8mg VOMICARE Tablet given three
times a day to be given 1-2 hours before the therapy.
Ø Postoperative Nausea and vomiting:
The recommended dose is 16mg
given as two 8mg VOMICARE Tablet or
four VOMICARE Tablet 1 hour before
administration of anesthesia.
Ø Dosage adjustment for Patients with
impaired renal function: The dosage recommendation is same as for the general
population.
Ø Dosage adjustment for Patients with
impaired hepatic function: In patients with severe hepatic impairment
clearance is reduced and apparent volume of distribution is increased with a
resultant increase in plasma half life. In such patients, a total daily dose of
8mg should not be exceeded.
ADVERSE REACTIONS:
Flusing, rare case of
hypersensitivity, angioedema, bronchospasm, shortness of breath, hypotension,
urticaria are some of the side effect observed
CONTRAINDICATIONS:
VOMICARE is contraindicated for patients known to have
hypersensitivity to Ondansetron Hydrochloride.
VOMICARE: SAFETY PROFILE
·
No dosage adjustment is required for VOMICARE taking phenytoin,
carbamazepine, Rifamipicin as these drugs hastens the metabolism of other drugs.
- Carcinogenesis, mutagenesis and
impairment of fertility:
Carcinogenic
effects were not seen in 2-years studies in rats and mice with dose up to 10
and 30 mg/kg/day, respectively. Ondansetron was not mutagenic in standard tests
for mutagenicity. Oral administration of ondansetron up to 15 mg/kg/day did not
affect he fertility or general reproductive performance of male and female
rats.
- Pregnancy: Teratogenicity:
Studies have
been performed in pregnant rats and rabbits at daily oral dose up to 15 and 30
mg/kg/day, respectively and have revealed no evidence of impaired fertility or
harm to the fetus. There are however, no adequate and well control tests
carried out in pregnant women, the drug, should therefore be used in pregnancy
only if clearly indicated.
- Nursing Mothers:
Ondansetron is
excreted in the breast milk of rats. It is not known whether ondansetron is
excreted in human milk, caution should be exercised when ondansetron is
administered to a nursing woman.
- Pediartic Use:
Little
information is available about dosage in pediatric patients 4 years of age or
younger.
- Geriartic Use:
Of the total
number of subjects enrolled in the cancer chemotherapy induced and post
operative nausea and vomiting clinical trials, no overall differences in the
safety and effectiveness were observed in young and geriartic (over 65years)
subjects. Dose adjustment in not needed in patients over the age of 65 years.
