Drug Information

    


  











Pharmacokinetics

  


Lignocaine is readily absorbed
from the gastrointestinal tract, from mucous membranes, and through
damaged skin. Absorption through intact skin is poor. It is rapidly
absorbed from injection sites including muscle.

After an intravenous dose lignocaine is rapidly and widely distributed
into highly perfused tissues followed by redistribution into skeletal
muscle and adipose tissue. Lignocaine is bound to plasma proteins,
including alpha(1)-acid glycoprotein (AAG). The extent of binding is
variable but is approximately 66%. Plasma protein binding of lignocaine
depends in part on the concentrations of both lignocaine and AAG. Any
alteration in the concentration of AAG can greatly affect plasma
concentrations of lignocaine

Plasma
concentrations decline rapidly after an intravenous dose with an initial
half-life of less than 30 minutes; the elimination half-life is 1 to 2
hours but may be prolonged if infusions are given for longer than 24
hours or if hepatic blood flow is reduced.

Lignocaine is largely metabolised in the liver and any alteration in
liver function or hepatic blood flow can have a significant effect on
its pharmacokinetics and dosage requirements. First-pass metabolism is
extensive and bioavailability is about 35% after oral administration.
Metabolism in the liver is rapid and approximately 90% of a given dose
is dealkylated to form monoethylglycinexylidide (MEGX) and
glycinexylidide (GX). Both of these metabolites may contribute to the
therapeutic and toxic effects of lignocaine and since their half-lives
are longer than that of lignocaine, accumulation, particularly of
glycinexylidide, may occur during prolonged infusions. Further
metabolism occurs and metabolites are excreted in the urine with less
than 10% of unchanged lignocaine. Reduced clearance of lignocaine has
been found in patients with heart failure, alcoholic liver disease, or
chronic or viral hepatitis. Concomitant therapy with drugs that alter
hepatic blood flow or induce drug-metabolising microsomal enzymes can
also affect the clearance of lignocaine. Renal impairment does not
affect the clearance of lignocaine but accumulation of its active
metabolites can occur and may lead to toxicity. Lignocaine
crosses the placenta and blood-brain barrier; it is distributed into
breast milk.

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Indication
& Dosage


 


INFILTRATION
ANAESTHESIA, SURFACE ANAESTHESIA, NERVE BLOCK, EPIDURAL ANAESTHESIA, IV
TOPICALLY TO FACTILITATE ENDOTRACHEAL INTUBATION, OTOLOGICALM RECTAL AND
VAGINAL EXAMINATION, URETHRAL EXAMINATION, URETHRAL PROCEDURES,
CATHETERISTATION, CYSTOSCOPY, BRONCHOSCOPY, PAINFUL CYSTITIS, PAIN AND
ITCHING DUE TO MINOR BURNS, INSECT BITES, HAEMORRHOIDS AND ANAL FISSURES:

(1-5% strength prepns.) Dosage depends on several factors such route, type
and extent of surgical procedures, duration of anaeshtesia and patients’
condition and age. During infiltration use, max lognocaine dose should not
exceed 200mg. see lit.

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Action

It is a local anaesthetic which stabillises the
neuronal membrane and inhibits the ion movements which are necessary for
conduction of impulses. In the heart lignocaine reduces phase 4
depolarisation, decreases automaticity. Duration of action potential and
effective recactory period is reduced.

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Interactions

Propranolol: Increased lidocaine levels
resulting in toxicity.

Cimetidine: Decreased lidocaine clearance with possible toxicity.

Procainamide: Additive cardidepressant action may occur with
potential for conduction abnormalities.

Tocainide: Increased incidence of adverse reactions.

Adrenaline: Reduces the absorption of lidocaine.

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Adverse
Effect & Precautions


 

Convulsion,
tremor, dizziness, blurred vision, nervousness, nausea and
respiratory arrest. Cardiovascular collapse and cardiac arrest.
Symptoms may occur quickly, without warning.



Precaution: Resuscitation facilities should be avilable when local
anaesthesia is being given. Bradycardia. Hepatic and renal
dysfunction.

Pregnancy: May be used.

Breast Feeding: Use with caution.

Man: May be used.

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Brands available in market :








































GESICAIN


SPPL


INJ


2%


30ML


9.70


GESICAIN 2 % VISCOUS


SPPL


VISC


2%


100ML


20.00


GESICAIN HEAVY 5%


SPPL


INJ


(Lignocaine Hcl 53.33mg, dextrose 75mg, sod. hydroxide to adjust pH
between 6.3-6.7


25x2ml


74.97


GESICAIN OINT


SPPL


OINT


5%


10g


19.99


GESICAIN TOPICAL


SPPL


SOLN


4%


30ml


19.99


LOX HEAVY


Neon Labs


INJ


(Lignocaine 53.3mg, dextrsoe 75mg/ml)


100ml


36.90


LOX TOPICAL


Neon Labs


LOTION


4%


30ml


13.50


LOX VISCOUS


Neon Labs


INJ


(Methyl paraben 0.61mg , propyl paraben

21.30mg/ml


100ml


13.14


LOX-2%


Neon Labs


INJ


21.3mg/ml


30ml


12.60


XYLOCAINE


Astra-IDL


INJ


1%


30ml


13.50


INJ


2%


30ml


12.40


XYLOCAINE HEAVY


Astra-IDL


INJ


(lIGNOCAINE hCL 53.3MG, DEXTROSE 75MG/ML)


25x2ml


105.00


XYLOCAINE JELLY


Astra-IDL


JELLY


2%


30g


21.75


XYLOCAINE OINTMENT


Astra-IDL


TUBE


5%


20g


18.60


XYLOCAINE PUMP SPRAY


Astra-IDL


SPRAY


100MG/ML


80ml


155.00


XYLOCAINE TOPICAL


Astra-IDL


SOLN


4%


30ml


13.25


XYLOCAINE VISCOUS 2%


Astra-IDL


BOTTLE


2%


100ml


13.60






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Drug Information
    

  

Pharmacokinetics
  

Lignocaine is readily absorbed from the gastrointestinal tract, from mucous membranes, and through damaged skin. Absorption through intact skin is poor. It is rapidly absorbed from injection sites including muscle.
After an intravenous dose lignocaine is rapidly and widely distributed into highly perfused tissues followed by redistribution into skeletal muscle and adipose tissue. Lignocaine is bound to plasma proteins, including alpha(1)-acid glycoprotein (AAG). The extent of binding is variable but is approximately 66%. Plasma protein binding of lignocaine depends in part on the concentrations of both lignocaine and AAG. Any alteration in the concentration of AAG can greatly affect plasma concentrations of lignocaine
Plasma concentrations decline rapidly after an intravenous dose with an initial half-life of less than 30 minutes; the elimination half-life is 1 to 2 hours but may be prolonged if infusions are given for longer than 24 hours or if hepatic blood flow is reduced.
Lignocaine is largely metabolised in the liver and any alteration in liver function or hepatic blood flow can have a significant effect on its pharmacokinetics and dosage requirements. First-pass metabolism is extensive and bioavailability is about 35% after oral administration. Metabolism in the liver is rapid and approximately 90% of a given dose is dealkylated to form monoethylglycinexylidide (MEGX) and glycinexylidide (GX). Both of these metabolites may contribute to the therapeutic and toxic effects of lignocaine and since their half-lives are longer than that of lignocaine, accumulation, particularly of glycinexylidide, may occur during prolonged infusions. Further metabolism occurs and metabolites are excreted in the urine with less than 10% of unchanged lignocaine. Reduced clearance of lignocaine has been found in patients with heart failure, alcoholic liver disease, or chronic or viral hepatitis. Concomitant therapy with drugs that alter hepatic blood flow or induce drug-metabolising microsomal enzymes can also affect the clearance of lignocaine. Renal impairment does not affect the clearance of lignocaine but accumulation of its active metabolites can occur and may lead to toxicity. Lignocaine crosses the placenta and blood-brain barrier; it is distributed into breast milk.

TOP
   

Indication & Dosage
 

INFILTRATION ANAESTHESIA, SURFACE ANAESTHESIA, NERVE BLOCK, EPIDURAL ANAESTHESIA, IV TOPICALLY TO FACTILITATE ENDOTRACHEAL INTUBATION, OTOLOGICALM RECTAL AND VAGINAL EXAMINATION, URETHRAL EXAMINATION, URETHRAL PROCEDURES, CATHETERISTATION, CYSTOSCOPY, BRONCHOSCOPY, PAINFUL CYSTITIS, PAIN AND ITCHING DUE TO MINOR BURNS, INSECT BITES, HAEMORRHOIDS AND ANAL FISSURES: (1-5% strength prepns.) Dosage depends on several factors such route, type and extent of surgical procedures, duration of anaeshtesia and patients’ condition and age. During infiltration use, max lognocaine dose should not exceed 200mg. see lit.

TOP
   

Action

It is a local anaesthetic which stabillises the neuronal membrane and inhibits the ion movements which are necessary for conduction of impulses. In the heart lignocaine reduces phase 4 depolarisation, decreases automaticity. Duration of action potential and effective recactory period is reduced.

TOP
   

Interactions

Propranolol: Increased lidocaine levels resulting in toxicity.
Cimetidine: Decreased lidocaine clearance with possible toxicity.
Procainamide: Additive cardidepressant action may occur with potential for conduction abnormalities.
Tocainide: Increased incidence of adverse reactions.
Adrenaline: Reduces the absorption of lidocaine.

TOP
   

Adverse Effect & Precautions
 
Convulsion, tremor, dizziness, blurred vision, nervousness, nausea and respiratory arrest. Cardiovascular collapse and cardiac arrest. Symptoms may occur quickly, without warning.

Precaution: Resuscitation facilities should be avilable when local anaesthesia is being given. Bradycardia. Hepatic and renal dysfunction.
Pregnancy: May be used.
Breast Feeding: Use with caution.
Man: May be used.

TOP
   

Brands available in market :

GESICAIN

SPPL

INJ

2%

30ML

9.70

GESICAIN 2 % VISCOUS

SPPL

VISC

2%

100ML

20.00

GESICAIN HEAVY 5%

SPPL

INJ

(Lignocaine Hcl 53.33mg, dextrose 75mg, sod. hydroxide to adjust pH between 6.3-6.7

25x2ml

74.97

GESICAIN OINT

SPPL

OINT

5%

10g

19.99

GESICAIN TOPICAL

SPPL

SOLN

4%

30ml

19.99

LOX HEAVY

Neon Labs

INJ

(Lignocaine 53.3mg, dextrsoe 75mg/ml)

100ml

36.90

LOX TOPICAL

Neon Labs

LOTION

4%

30ml

13.50

LOX VISCOUS

Neon Labs

INJ

(Methyl paraben 0.61mg , propyl paraben
21.30mg/ml

100ml

13.14

LOX-2%

Neon Labs

INJ

21.3mg/ml

30ml

12.60

XYLOCAINE

Astra-IDL

INJ

1%

30ml

13.50

INJ

2%

30ml

12.40

XYLOCAINE HEAVY

Astra-IDL

INJ

(lIGNOCAINE hCL 53.3MG, DEXTROSE 75MG/ML)

25x2ml

105.00

XYLOCAINE JELLY

Astra-IDL

JELLY

2%

30g

21.75

XYLOCAINE OINTMENT

Astra-IDL

TUBE

5%

20g

18.60

XYLOCAINE PUMP SPRAY

Astra-IDL

SPRAY

100MG/ML

80ml

155.00

XYLOCAINE TOPICAL

Astra-IDL

SOLN

4%

30ml

13.25

XYLOCAINE VISCOUS 2%

Astra-IDL

BOTTLE

2%

100ml

13.60


TOP
   

                    

 

By |2022-07-20T16:42:55+00:00July 20, 2022|Uncategorized|Comments Off on Lignocaine

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