Drug Information

 


    











Pharmacokinetics

 


Metoclopramide is
rapidly and almost completely absorbed from the gastrointestinal tract
following a dose by mouth, although conditions such as vomiting or
impaired gastric motility may reduce absorption. Peak plasma
concentrations of metoclopramide occur about 1 to 2 hours after an oral
dose. However, it undergoes hepatic first-pass metabolism, which varies
considerably between subjects, and hence the absolute bioavailability
and the plasma concentrations are subject to wide interindividual
variation. On average, the bioavailability of oral metoclopramide is
about 75%, but it appears to vary between about 30 and 100%.

Attempts to overcome the problems of oral administration by rectal or
intranasal administration have demonstrated that bioavailability is
equally variable by these routes, although it may be somewhat better if
given intramuscularly.

Metoclopramide is widely distributed in the body, with an apparent
volume of distribution of about 3.5 litres per kg. It readily crosses
the blood-brain barrier into the CNS. It also freely crosses the
placenta, and has been reported to attain concentrations in fetal plasma
about 60 to 70% of those in maternal plasma. Concentrations higher than
those in maternal plasma may be reached in the breast milk of lactating
mothers, particularly in the early puerperium, although concentrations
decrease somewhat in the late puerperium.

Elimination of metoclopramide is biphasic, with a terminal elimination
half-life of about 4 to 6 hours, although this may be prolonged in renal
impairment, with consequent elevation of plasma concentrations. It is
excreted in the urine, about 85% of a dose being eliminated in 72 hours,
20 to 30% as unchanged metoclopramide and the remainder as sulphate or
glucuronide conjugates, or as metabolites. About 5% of a dose is
excreted in faeces viat

he bile.




                                                                                          
TOP

 

Indication
& Dosage



 


Oral; IM/IV

NAUSEA, VOMITING DUE TO VARIOUS CAUSES EXCEPT IN MOTION SICKNESS;
DELAYED GASTRIC EMPTYING; DIABETIC GASTROPARESIS:
Adult: 10mg 2-4
times/day. Young Adults 15-20 yrs: 5-10mg 2-4 times/day. 5-8 yrs: 2.5mg
2-4 times/day. 3-4 yrs: 2mg 2-4 times/day. 1-2 yr: 1mg 2-4 times/day.
under 1yr: img b.i.d. Maximum daily oral dose: 0.5mg/kg.


OESOPHAGEAL REFLUX: 10-15mg q.i.d. 30 min befor each meal and at
bedtime. 

CANCER CHEMOTHERAPY (NAUSEA, VOMITING):
2-4mg/kg as IV drip over
15-30min. Maintenace dose: 3-5mg/kg given over 8 hrs. Max: 10mg/kg/day.

NOTE: Renal impairment: Creatinine clearance under 40ml/min, the
starting dose is reduced by 50%

TOP.

   

Action

 

Metoclopramide blocks central and peripheral dopamine receptors. The
latter activity results in stimulation of plain muscle in the stomach
and upper GI tract. This results in rapid gastric emptying and faster
intestinal trasnsit. Lower oesophageal sphincter pressure is increased
and this prevents oesophageal reflux. Central dopamine inhibition
abolishes nauses and vomiting. Prolactin levels are increased and
extrapyramidal side effects may be seen.

 TOP


Interactions

 


Caution should be observed when using metoclopramide in patients taking
other drugs that can also cause extrapyramidal reactions, such as the
phenothiazines. Increased toxicity may occur if metoclopramide is used
in patients receiving lithium, and caution is advisable with other
centrally active drugs including antidepressants, antiepileptics, and
sympathomimetics. Antimuscarinics and opioid analgesics antagonise the
gastrointestinal effects of metoclopramide.

The absorption of other drugs may be affected by metoclopramide; it may
either diminish absorption from the stomach (as with digoxin) or enhance
absorption from the small intestine (for example, with aspirin or
paracetamol). It inhibits serum cholinesterase and may prolong
suxamethonium-induced neuromuscular blockade.

Metoclopramide may also increase prolactin blood-concentrations and
therefore interfere with drugs which have a hypoprolactinaemic effect
such as bromocriptine. It has been suggested that it should not be given
to patients receiving monoamine oxidase inhibitors (MAOIs).

TOP


 

Adverse
Effect & Precaution


 

Drowsiness, facial spasm, trismus, oculogyric crisis seen commonly in
children and young adults. Tardive dyskinesia in elderly on prolonged
use, gynaecomastia, galactorrhoea, diarrhoea and restlessness.



Precaution: IV injection ot be administered slowly to avoid restlessness
and anxiety.

Pregnancy: Safety not established.

Breast Feeding: Use with Caution.

Man: May be givenin reduced dose.

TOP


  

Brand
available in market


 













































EMENIL

Astra-IDL
TAB 10mg 10 5.13
TAB 10mg 1000 191.23
VIAL 5mg/ml 10ml 12.75
MAXERON

Wallace
TAB 10mg 10 7.00
INJ 5mg/ml 2ml 3.60
INJ 5mg/ml 10ml 9.50
LIQUID 5mg/5ml 30ml 11.00
MAXINORM

Pharmasynth
TABS 10mg 10 4.75
METOCONTIN

Modi Mundi Pharma
TAB 15mg 10 13.00
PERINORM

IPCA
TAB 10mg 10 8.00
TAB 10mg 250 105.50
INJ 5mg/5ml 2ml 4.25
VIAL 5mg/5ml 10ml 10.00
LIQUID 5mg/5ml 30ml 9.90
PERINORM-CD

IPCA
TAB 15mg 10 15.00
REGGI

Shalaks
TAB 10mg 100 31.50
SYRUP 5mg/5ml 30ml 9.10
SYRUP 5mg/ml 450ml 48.50
TAB 5mg/ml 10 4.00
REGLAN

CFL
TAB 10mg 10 7.00
SYRUP 5mg/5ml 30ml 11.00
INJ 5mg/ml 2ml 3.60
VIAL 5mg/ml 10ml 9.50
SIGMET

Sigma
TAB 10mg 10 5.20
INJ 5mg/ml 10x2ml 27.00
VIAL 5mg/ml 10ml 7.55
TOMID

Gufic
TAB 10mg 10 4.00
SYRUP 5mg/5ml 30ml 5.35
UGINORM.INJ

Helios
INJ 5mg/ml 2ml 5.00



TOP


 

 






 

 

 

 
Drug Information
 

    

Pharmacokinetics
 

Metoclopramide is rapidly and almost completely absorbed from the gastrointestinal tract following a dose by mouth, although conditions such as vomiting or impaired gastric motility may reduce absorption. Peak plasma concentrations of metoclopramide occur about 1 to 2 hours after an oral dose. However, it undergoes hepatic first-pass metabolism, which varies considerably between subjects, and hence the absolute bioavailability and the plasma concentrations are subject to wide interindividual variation. On average, the bioavailability of oral metoclopramide is about 75%, but it appears to vary between about 30 and 100%.
Attempts to overcome the problems of oral administration by rectal or intranasal administration have demonstrated that bioavailability is equally variable by these routes, although it may be somewhat better if given intramuscularly.
Metoclopramide is widely distributed in the body, with an apparent volume of distribution of about 3.5 litres per kg. It readily crosses the blood-brain barrier into the CNS. It also freely crosses the placenta, and has been reported to attain concentrations in fetal plasma about 60 to 70% of those in maternal plasma. Concentrations higher than those in maternal plasma may be reached in the breast milk of lactating mothers, particularly in the early puerperium, although concentrations decrease somewhat in the late puerperium.
Elimination of metoclopramide is biphasic, with a terminal elimination half-life of about 4 to 6 hours, although this may be prolonged in renal impairment, with consequent elevation of plasma concentrations. It is excreted in the urine, about 85% of a dose being eliminated in 72 hours, 20 to 30% as unchanged metoclopramide and the remainder as sulphate or glucuronide conjugates, or as metabolites. About 5% of a dose is excreted in faeces viat
he bile.

                                                                                           TOP
 

Indication & Dosage
 
Oral; IM/IV
NAUSEA, VOMITING DUE TO VARIOUS CAUSES EXCEPT IN MOTION SICKNESS; DELAYED GASTRIC EMPTYING; DIABETIC GASTROPARESIS:
Adult: 10mg 2-4 times/day. Young Adults 15-20 yrs: 5-10mg 2-4 times/day. 5-8 yrs: 2.5mg 2-4 times/day. 3-4 yrs: 2mg 2-4 times/day. 1-2 yr: 1mg 2-4 times/day. under 1yr: img b.i.d. Maximum daily oral dose: 0.5mg/kg.
OESOPHAGEAL REFLUX: 10-15mg q.i.d. 30 min befor each meal and at bedtime. 
CANCER CHEMOTHERAPY (NAUSEA, VOMITING):
2-4mg/kg as IV drip over 15-30min. Maintenace dose: 3-5mg/kg given over 8 hrs. Max: 10mg/kg/day.
NOTE: Renal impairment: Creatinine clearance under 40ml/min, the starting dose is reduced by 50%

TOP.
   

Action
 
Metoclopramide blocks central and peripheral dopamine receptors. The latter activity results in stimulation of plain muscle in the stomach and upper GI tract. This results in rapid gastric emptying and faster intestinal trasnsit. Lower oesophageal sphincter pressure is increased and this prevents oesophageal reflux. Central dopamine inhibition abolishes nauses and vomiting. Prolactin levels are increased and extrapyramidal side effects may be seen.

 TOP

Interactions
 

Caution should be observed when using metoclopramide in patients taking other drugs that can also cause extrapyramidal reactions, such as the phenothiazines. Increased toxicity may occur if metoclopramide is used in patients receiving lithium, and caution is advisable with other centrally active drugs including antidepressants, antiepileptics, and sympathomimetics. Antimuscarinics and opioid analgesics antagonise the gastrointestinal effects of metoclopramide.
The absorption of other drugs may be affected by metoclopramide; it may either diminish absorption from the stomach (as with digoxin) or enhance absorption from the small intestine (for example, with aspirin or paracetamol). It inhibits serum cholinesterase and may prolong suxamethonium-induced neuromuscular blockade.
Metoclopramide may also increase prolactin blood-concentrations and therefore interfere with drugs which have a hypoprolactinaemic effect such as bromocriptine. It has been suggested that it should not be given to patients receiving monoamine oxidase inhibitors (MAOIs).

TOP
 

Adverse Effect & Precaution
 
Drowsiness, facial spasm, trismus, oculogyric crisis seen commonly in children and young adults. Tardive dyskinesia in elderly on prolonged use, gynaecomastia, galactorrhoea, diarrhoea and restlessness.

Precaution: IV injection ot be administered slowly to avoid restlessness and anxiety.
Pregnancy: Safety not established.
Breast Feeding: Use with Caution.
Man: May be givenin reduced dose.

TOP
  

EMENIL

Astra-IDL

TAB

10mg

10

5.13

TAB

10mg

1000

191.23

VIAL

5mg/ml

10ml

12.75

MAXERON

Wallace

TAB

10mg

10

7.00

INJ

5mg/ml

2ml

3.60

INJ

5mg/ml

10ml

9.50

LIQUID

5mg/5ml

30ml

11.00

MAXINORM

Pharmasynth

TABS

10mg

10

4.75

METOCONTIN

Modi Mundi Pharma

TAB

15mg

10

13.00

PERINORM

IPCA

TAB

10mg

10

8.00

TAB

10mg

250

105.50

INJ

5mg/5ml

2ml

4.25

VIAL

5mg/5ml

10ml

10.00

LIQUID

5mg/5ml

30ml

9.90

PERINORM-CD

IPCA

TAB

15mg

10

15.00

REGGI

Shalaks

TAB

10mg

100

31.50

SYRUP

5mg/5ml

30ml

9.10

SYRUP

5mg/ml

450ml

48.50

TAB

5mg/ml

10

4.00

REGLAN

CFL

TAB

10mg

10

7.00

SYRUP

5mg/5ml

30ml

11.00

INJ

5mg/ml

2ml

3.60

VIAL

5mg/ml

10ml

9.50

SIGMET

Sigma

TAB

10mg

10

5.20

INJ

5mg/ml

10x2ml

27.00

VIAL

5mg/ml

10ml

7.55

TOMID

Gufic

TAB

10mg

10

4.00

SYRUP

5mg/5ml

30ml

5.35

UGINORM.INJ

Helios

INJ

5mg/ml

2ml

5.00

TOP
 
 

 

By |2022-07-20T16:44:59+00:00July 20, 2022|Uncategorized|Comments Off on Metoclopramide

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