Drug Information

    

         












Pharmacokinetics

Following oral administration,
ondansetron is rapidly absorbed with peak plasma concentration of around
0.03 to 0.04 micrograms per mL being reported about 1.5 to 2 hours after
an oral dose of 8 mg. The absolute bioavailability is about 60%, due
mainly to hepatic first-pass metabolism. It is extensively distributed
in the body; results in vitro suggest that about 70 to 75% of the drug
in plasma is protein bound. It is cleared from the systemic circulation
predominantly by hepatic metabolism, with less than 5% of a dose being
excreted in urine unchanged: clearances of around 6 mL per minute per kg
have been reported in young, healthy subjects. In elderly subjects,
bioavailability may be somewhat higher (65%) and clearance lower (4 to 5
mL per minute per kg), presumably due to reduced hepatic metabolism. The
terminal elimination half-life is about 3 hours in younger subjects,
prolonged to 5 hours in the elderly. These differences are not
considered sufficient to warrant dosage adjustment; however, in patients
with severe hepatic impairment, in whom bioavailability may approach
100% and clearance is markedly slowed, with elimination half-lives of 15
to 32 hours, dosage restriction is advisable.



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Indication
& Dosage




IV

MANAGEMENT OF NAUSEA, VOMITING ASSOCIATED WITH CANCER CHEMOTHERAPY OR
RADIOTHERAPY:
Highly emetrogenic regimens: 8mg by slow IV injection
mimmediately before chemotherapy. Followed by 2 further IV doses of 8 mg
ecach 2 or 4 hrs apart or a constant infusion of of 1 mg/hr for upto 24
hrs. OR A single dose of 32mg in 50-100ml of normal saline infused over
15 min just before chemotherpy. A single IV doses of dexamethassone
sodium phosphate 20mg before chemotherapy increases the effect of
ondansetron. To prevent delayed emesis, continue ondansetronorally 8 mg
12 hrly for upto 5 days. IV: Children: A single IV DOSE OF 5mg/m2 just
before chemotherapy followed by 4mg orally b.i.d. if necessary 


POSTOPERATIVE NAUSEA, VOMITING:
Adult: A single dose of 4mg slow IV
injection at induction.


Oral

POSTOPERATIVE NAUSEA, VOMITING:
8mg i hr before induction & 2
further doses of 8mg at 8hr intervals.

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Action




Antagonises 5HT3 receptor present peripherally on vagal nerve
terminals and centrally in the chemoreceptor trigger zone. Ondansetron
probably acts at both sites to prevent vomiting due to cancer
chemotherapy and radiotherapy.

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Interaction

Induces or
inhibitors of hepatic Cytochrome P450 drug metabolising enzymes : May
chage the clearance and hence half-life of ondansteron but on the basis
of available data there is no  need to adjust the dose of
ondasteron.

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Adverse Effect & Precautions



Well tolerated drug,
headache, constipation, dizziness, allergic reactions.



Precaution: Hepatic impairment.

Pregnancy: Safety not established.

Pregnancy: Use with caution.

Man: May be given.

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Brands
available in market


























































EMESET

Cipla
TAB 4mg 10 96.70
TAB 8mg 10 163.00
INJ 2mg/ml 2ml 28.00
INJ 2mg/ml 4ml 40.00
EMITRON

Criticare
TAB 4mg 6 44.28
TAB 8mg 6 75.48
INJ 2mg/ml 2ml 24.15
INJ 2mg/ml 4ml 45.29
EMSETRON

T.D.P.L
TAB 4mg 6 41.40
TAB 8mg 6 75.00
INJ 2mg/ml 2ml 19.90
INJ 2mg/ml 4ml 31.90
ONCODEN

Torrent
TAB 4mg 10 61.90
TAB 8mg 10 119.90
INJ 2mg/ml 2ml 20.90
INJ 2mg/ml 4ml 37.90
ONDEM

Alkem
TAB 4mg 10 76.00
TAB 8mg 10 130.95
INJ 2mg/ml 2ml 25.75
INJ 2mg/ml 4ml 40.90
OSETRON

DR.Reddy’s
TAB 4mg 10 74.80
TAB 8mg 10 130.95
INJ 2mg/ml 2ml 23.40
INJ 2mg/ml 4ml 37.53
VOMIS

Indon
TAB 4mg 6 40.41
TAB 8mg 6 80.92
INJ 2mg/ml 2ml Amp 32.21
INJ 2mg/ml 4ml Amp 46.80
VOMISET 4

Indipharma
F-C-TABS 4mg 10 82.50
F-C-TABS 8mg 10 153.00
VOMISET INJ

Indipharma
INJ 2mg/ml 2ml 27.00
INJ 2mg/ml 4ml 38.00
VOMIZ

Alidac
TAB 4mg 6 40.41
TAB 8mg 6 80.92
INJ 2mg/ml 2ml 32.21
INJ 2mg/ml 4ml 46.80
ZOFER

Natco
TAB 4mg 10 76.69
TAB 8mg 10 105.62
INJ 2mg/ml 2ml 23.96
INJ 2mg/ml 4ml 38.34



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Drug Information
    

         

Pharmacokinetics

Following oral administration, ondansetron is rapidly absorbed with peak plasma concentration of around 0.03 to 0.04 micrograms per mL being reported about 1.5 to 2 hours after an oral dose of 8 mg. The absolute bioavailability is about 60%, due mainly to hepatic first-pass metabolism. It is extensively distributed in the body; results in vitro suggest that about 70 to 75% of the drug in plasma is protein bound. It is cleared from the systemic circulation predominantly by hepatic metabolism, with less than 5% of a dose being excreted in urine unchanged: clearances of around 6 mL per minute per kg have been reported in young, healthy subjects. In elderly subjects, bioavailability may be somewhat higher (65%) and clearance lower (4 to 5 mL per minute per kg), presumably due to reduced hepatic metabolism. The terminal elimination half-life is about 3 hours in younger subjects, prolonged to 5 hours in the elderly. These differences are not considered sufficient to warrant dosage adjustment; however, in patients with severe hepatic impairment, in whom bioavailability may approach 100% and clearance is markedly slowed, with elimination half-lives of 15 to 32 hours, dosage restriction is advisable.

TOP
   

Indication & Dosage

IV
MANAGEMENT OF NAUSEA, VOMITING ASSOCIATED WITH CANCER CHEMOTHERAPY OR RADIOTHERAPY:
Highly emetrogenic regimens: 8mg by slow IV injection mimmediately before chemotherapy. Followed by 2 further IV doses of 8 mg ecach 2 or 4 hrs apart or a constant infusion of of 1 mg/hr for upto 24 hrs. OR A single dose of 32mg in 50-100ml of normal saline infused over 15 min just before chemotherpy. A single IV doses of dexamethassone sodium phosphate 20mg before chemotherapy increases the effect of ondansetron. To prevent delayed emesis, continue ondansetronorally 8 mg 12 hrly for upto 5 days. IV: Children: A single IV DOSE OF 5mg/m2 just before chemotherapy followed by 4mg orally b.i.d. if necessary 
POSTOPERATIVE NAUSEA, VOMITING: Adult: A single dose of 4mg slow IV injection at induction.
Oral
POSTOPERATIVE NAUSEA, VOMITING:
8mg i hr before induction & 2 further doses of 8mg at 8hr intervals.

TOP
   

Action

Antagonises 5HT3 receptor present peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone. Ondansetron probably acts at both sites to prevent vomiting due to cancer chemotherapy and radiotherapy.

TOP
   

Interaction

Induces or inhibitors of hepatic Cytochrome P450 drug metabolising enzymes : May chage the clearance and hence half-life of ondansteron but on the basis of available data there is no  need to adjust the dose of ondasteron.

TOP
   

Adverse Effect & Precautions

Well tolerated drug, headache, constipation, dizziness, allergic reactions.

Precaution: Hepatic impairment.
Pregnancy: Safety not established.
Pregnancy: Use with caution.
Man: May be given.

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EMESET

Cipla

TAB

4mg

10

96.70

TAB

8mg

10

163.00

INJ

2mg/ml

2ml

28.00

INJ

2mg/ml

4ml

40.00

EMITRON

Criticare

TAB

4mg

6

44.28

TAB

8mg

6

75.48

INJ

2mg/ml

2ml

24.15

INJ

2mg/ml

4ml

45.29

EMSETRON

T.D.P.L

TAB

4mg

6

41.40

TAB

8mg

6

75.00

INJ

2mg/ml

2ml

19.90

INJ

2mg/ml

4ml

31.90

ONCODEN

Torrent

TAB

4mg

10

61.90

TAB

8mg

10

119.90

INJ

2mg/ml

2ml

20.90

INJ

2mg/ml

4ml

37.90

ONDEM

Alkem

TAB

4mg

10

76.00

TAB

8mg

10

130.95

INJ

2mg/ml

2ml

25.75

INJ

2mg/ml

4ml

40.90

OSETRON

DR.Reddy’s

TAB

4mg

10

74.80

TAB

8mg

10

130.95

INJ

2mg/ml

2ml

23.40

INJ

2mg/ml

4ml

37.53

VOMIS

Indon

TAB

4mg

6

40.41

TAB

8mg

6

80.92

INJ

2mg/ml

2ml Amp

32.21

INJ

2mg/ml

4ml Amp

46.80

VOMISET 4

Indipharma

F-C-TABS

4mg

10

82.50

F-C-TABS

8mg

10

153.00

VOMISET INJ

Indipharma

INJ

2mg/ml

2ml

27.00

INJ

2mg/ml

4ml

38.00

VOMIZ

Alidac

TAB

4mg

6

40.41

TAB

8mg

6

80.92

INJ

2mg/ml

2ml

32.21

INJ

2mg/ml

4ml

46.80

ZOFER

Natco

TAB

4mg

10

76.69

TAB

8mg

10

105.62

INJ

2mg/ml

2ml

23.96

INJ

2mg/ml

4ml

38.34

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By |2022-07-20T16:42:53+00:00July 20, 2022|Uncategorized|Comments Off on Ondansetron

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