Drug Information 

 


    











Pharmacokinetics

   


Haloperidol is readily
absorbed from the gastrointestinal tract. It is metabolised in the liver
and is excreted in the urine and, via the bile, in the faeces; there is
evidence of enterohepatic recycling. Owing to the first-pass effect of
metabolism in the liver, plasma concentrations following oral
administration are lower than those following intramuscular
administration. Moreover, there is wide intersubject variation in plasma
concentrations of haloperidol, but in practice, no strong correlation
has been found between plasma concentrations of haloperidol and its
therapeutic effect. Paths of metabolism of haloperidol include oxidative
N-dealkylation and reduction of the ketone group to form an alcohol
known as reduced haloperidol. Haloperidol has been reported to have a
plasma elimination half-life ranging from about 12 to 38 hours after
oral administration. Haloperidol is about 92% bound to plasma proteins.
It is widely distributed in the body and crosses the blood-brain
barrier. Haloperidol is distributed into breast milk.

The decanoate ester of haloperidol is very slowly absorbed from the site
of injection and is therefore suitable for depot injection. It is
gradually released into the bloodstream where it is rapidly hydrolysed
to haloperidol.

Top

    

Indication
& Dosage




Oral

ACUTE SCHIZOPHRENIA AND RELATED CONDITIONS-CHRONIC SCHIZOPHERENIA,
BIPOLAR AFFECTIVE DISORDERS, ACUTE MANIA AND HYPOMANIA:
0.5-5mg 2 or 3
times a day. In severe cases upto 100mg/day. Use lowest maintenance
doses.


PSYCHOTIC DISOREDERS, NON-PSYCHOTIC BEHAVIOUR PROBLEMS AND TOOURETTER’S
DISORDER IN CHILDREN:
Start at 25-50 mcg/kg/day in 2 divided doses.
Increases carefully upto 150mcg/kg/day.

ANXIETY STATE(NONPSYCHOTIC): 0.25mg t.i.d. or 0.5mg b.i.d. 

SEVERE AGITATION IN ELDERLY: 2-6mg/day.



IM

PSYCHOTIC STATES: Adult: Initially 2-5mg repeated every 4-8 hrs. In
serverely disturbed patients upto 30mg may be needed. Children: IM 
use not recommended.

IM depot prep: Haloperidol decanoate 50mg/ml 25-5mg every 15-30 days.

Top

    

Action

Potent antagonist at central and
perihpheral dopamine receptors and selective for the D2-receptors.
Produces calmness, sedation without sleep. Aggressive behaviour is
controlled. Hallucinations and delusions disappear. Patients become more
responsive. Haloperidol increases prolactin secretion. Causes hypothemia
in a dose-dependent manner. Seizure threshold is reduced.

Top

    

Interaction

Central
nervous system (CNS) depressants,Tricyclic antidepressants: Taking these
drugs with haloperidol may result in increased CNS and other depressant
effects, and in an increased chance of hypotension. Epinephrine : Severe
hypotension or cardiac arrhythmias may occur. Levodopa : Haloperidol may
reduce the potency of this drug.

Top

    

Adverse
Effect & Precaution




Dystonia, halucinations,
restlessness, nausea, epigastric discomfort, anaemia, blurred vision,
hypersensitivity reaction, blood dyscrasia, jaundice. Galactorrhoea,
gynecomastia and amenorrhoea.

Precaution has to be taken in patients with epilepsy,
allergy, glaucoma and in thyrotoxicosis.

Pregnancy: Safety not established.

Breast Feeding: Contraindicated

Man: May be used in reduced dose.

Top

    

Brands
available in market





























































 


CIZOREN


Stamed


TAB


1.5mg


10


7.80


TAB


5mg


10


9.50


TAB


10mg


10


16.00


DEPIDOL


Torrent


TAB


0.25mg


10


4.90


TAB


1.5mg


10


7.90


TAB


5mg


10


16.90


INJ-LA


50mg


1ml


110.00


DROPS


2mg/ml


30ml


17.20


HALIDOL


Biddle Sawyer


TAB


0.25mg


10


1.96


HALOPIDOL


Ethnor


TAB


0.25mg


10


5.41


TAB


2mg


10


14.50


TAB


5mg


10


29.50


TAB


10mg


10


41.00


TAB


20mg


10


55.00


LIQUID


2mg/ml


30ml


31.09


DROPS


10mg/ml


15ml


42.15


HALORID


Pace(SOL)


TAB


1.5mg


10


9.80


TAB


5mg


10


22.15


TAB


10mg


10


31.00


LARENASE


LA Pharma


TAB


1.5mg


10


6.60


TAB


5mg


10


13.00


TAB


10mg


10


22.50


SENORM


Sun Pharma


TAB


1.5mg


10


8.80


TAB


5mg


10


18.69


TAB


10mg


10


26.56


INJ


5mg


10ml


4.40


SENORM-LA


Sun Pharma


INJ


50mg/ml


1ml


105.00


SERADOL


Sigma


TAB


5mg


10


11.95


TAB


10mg


10


23.10


INJ


5mg/ml


10x1ml


44.00


SERENACE


RPG


TAB


0.25mg


10


5.54


TAB


1.5mg


10


11.06


TAB


5mg


10


24.65


TAB


10mg


10


34.58


TAB


20mg


10


41.32


LIQUID


2mg/ml


30ml


32.65


INJ


5mg/ml


5amp


21.02


TRANCODOL


Intas


TAB


1.5mg


10


4.25


TAB


5mg


10


9.00


TAB


10mg


10


15.00


TAB


20mg


10


34.25


INJ


5mg


1ml


4.75


Top

   



 






 

   

   
Drug Information 
 

    

Pharmacokinetics
   

Haloperidol is readily absorbed from the gastrointestinal tract. It is metabolised in the liver and is excreted in the urine and, via the bile, in the faeces; there is evidence of enterohepatic recycling. Owing to the first-pass effect of metabolism in the liver, plasma concentrations following oral administration are lower than those following intramuscular administration. Moreover, there is wide intersubject variation in plasma concentrations of haloperidol, but in practice, no strong correlation has been found between plasma concentrations of haloperidol and its therapeutic effect. Paths of metabolism of haloperidol include oxidative N-dealkylation and reduction of the ketone group to form an alcohol known as reduced haloperidol. Haloperidol has been reported to have a plasma elimination half-life ranging from about 12 to 38 hours after oral administration. Haloperidol is about 92% bound to plasma proteins. It is widely distributed in the body and crosses the blood-brain barrier. Haloperidol is distributed into breast milk.
The decanoate ester of haloperidol is very slowly absorbed from the site of injection and is therefore suitable for depot injection. It is gradually released into the bloodstream where it is rapidly hydrolysed to haloperidol.

Top
    

Indication & Dosage

Oral
ACUTE SCHIZOPHRENIA AND RELATED CONDITIONS-CHRONIC SCHIZOPHERENIA, BIPOLAR AFFECTIVE DISORDERS, ACUTE MANIA AND HYPOMANIA:
0.5-5mg 2 or 3 times a day. In severe cases upto 100mg/day. Use lowest maintenance doses.
PSYCHOTIC DISOREDERS, NON-PSYCHOTIC BEHAVIOUR PROBLEMS AND TOOURETTER’S DISORDER IN CHILDREN: Start at 25-50 mcg/kg/day in 2 divided doses. Increases carefully upto 150mcg/kg/day.
ANXIETY STATE(NONPSYCHOTIC): 0.25mg t.i.d. or 0.5mg b.i.d. 
SEVERE AGITATION IN ELDERLY: 2-6mg/day.

IM
PSYCHOTIC STATES: Adult: Initially 2-5mg repeated every 4-8 hrs. In serverely disturbed patients upto 30mg may be needed. Children: IM  use not recommended.
IM depot prep: Haloperidol decanoate 50mg/ml 25-5mg every 15-30 days.

Top
    

Action

Potent antagonist at central and perihpheral dopamine receptors and selective for the D2-receptors. Produces calmness, sedation without sleep. Aggressive behaviour is controlled. Hallucinations and delusions disappear. Patients become more responsive. Haloperidol increases prolactin secretion. Causes hypothemia in a dose-dependent manner. Seizure threshold is reduced.

Top
    

Interaction

Central nervous system (CNS) depressants,Tricyclic antidepressants: Taking these drugs with haloperidol may result in increased CNS and other depressant effects, and in an increased chance of hypotension. Epinephrine : Severe hypotension or cardiac arrhythmias may occur. Levodopa : Haloperidol may reduce the potency of this drug.

Top
    

Adverse Effect & Precaution

Dystonia, halucinations, restlessness, nausea, epigastric discomfort, anaemia, blurred vision, hypersensitivity reaction, blood dyscrasia, jaundice. Galactorrhoea, gynecomastia and amenorrhoea.

Precaution has to be taken in patients with epilepsy, allergy, glaucoma and in thyrotoxicosis.
Pregnancy: Safety not established.
Breast Feeding: Contraindicated
Man: May be used in reduced dose.

Top
    

 

CIZOREN

Stamed

TAB

1.5mg

10

7.80

TAB

5mg

10

9.50

TAB

10mg

10

16.00

DEPIDOL

Torrent

TAB

0.25mg

10

4.90

TAB

1.5mg

10

7.90

TAB

5mg

10

16.90

INJ-LA

50mg

1ml

110.00

DROPS

2mg/ml

30ml

17.20

HALIDOL

Biddle Sawyer

TAB

0.25mg

10

1.96

HALOPIDOL

Ethnor

TAB

0.25mg

10

5.41

TAB

2mg

10

14.50

TAB

5mg

10

29.50

TAB

10mg

10

41.00

TAB

20mg

10

55.00

LIQUID

2mg/ml

30ml

31.09

DROPS

10mg/ml

15ml

42.15

HALORID

Pace(SOL)

TAB

1.5mg

10

9.80

TAB

5mg

10

22.15

TAB

10mg

10

31.00

LARENASE

LA Pharma

TAB

1.5mg

10

6.60

TAB

5mg

10

13.00

TAB

10mg

10

22.50

SENORM

Sun Pharma

TAB

1.5mg

10

8.80

TAB

5mg

10

18.69

TAB

10mg

10

26.56

INJ

5mg

10ml

4.40

SENORM-LA

Sun Pharma

INJ

50mg/ml

1ml

105.00

SERADOL

Sigma

TAB

5mg

10

11.95

TAB

10mg

10

23.10

INJ

5mg/ml

10x1ml

44.00

SERENACE

RPG

TAB

0.25mg

10

5.54

TAB

1.5mg

10

11.06

TAB

5mg

10

24.65

TAB

10mg

10

34.58

TAB

20mg

10

41.32

LIQUID

2mg/ml

30ml

32.65

INJ

5mg/ml

5amp

21.02

TRANCODOL

Intas

TAB

1.5mg

10

4.25

TAB

5mg

10

9.00

TAB

10mg

10

15.00

TAB

20mg

10

34.25

INJ

5mg

1ml

4.75

Top
   

 

 

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

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