Lignocaine

Overview

Lignocaine is a sodium channel blocking agent, used as a local anesthetic and antiarrhythmic agent. It stabilizes nerve cell membranes to prevent impulse conduction. Used topically or by injection for local anaesthesia in minor operations.Intravenous injection or infusion used to treat abnormal heart rhythms. Excessive doses also block motor impulses and normal cardiac conduction. It has a low incidence of toxicity and a high degree of effeciveness in arrhythmias. Lignocaine is one of the least cardiotoxic drug of the currently used sodium channel blocker.

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Primary Characterstics

Lignocaine is also known as Lidocaine. Lidocaine (HCl), Lidocaine (HCl) are the derivatives of LignocaineLignocaine is also known as Lidocaine. Lidocaine (HCl), Lidocaine (HCl) are the derivatives of Lignocaine It is of Synthetic origin and belongs to Amide. It belongs to Na-Channel Local Anesthetic antagonist pharmacological group on the basis of mechanism of action and also classified in Analgesic pharmacological group.The Molecular Weight of Lignocaine is 234.30.

It is weakly acidic drug, 4.00% solution of the drug is isotonic and Its pKa is 7.86.

Indications

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Pharmacokinetics

Oral absorption of Lignocaine is found to be 17.5% ±17.5. Volume of distribution is found to be 1.3 l/kg and plasma protien binding is 64%. Presystemic metabolism is noted to be 67.5% ±2.5 and metabolism is reported Hepatic. Renal Excretion accounts for <10% and plasma half life is 1-2hr.

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Contraindications

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Drug Interactions

Lignocaine is known to interact with other drugs, the details of drug interactions is as follows:

Severity N/A

Alcuronium (Cl)

Interaction of Alcuronium (Cl) with Lignocaine

Amphotericin B

Interaction of Amphotericin B with Lignocaine

Atracurium (Besylate)

Interaction of Atracurium (Besylate) with Lignocaine

Edrophonium (Cl)

Interaction of Edrophonium (Cl) with Lignocaine

Enflurane

Interaction of Enflurane with Lignocaine

Halothane

Interaction of Halothane with Lignocaine

Suxamethonium (Cl)

Interaction of Suxamethonium (Cl) with Lignocaine

Nadolol

Interaction of Nadolol with Lignocaine

Oxprenolol (HCl)

Interaction of Oxprenolol (HCl) with Lignocaine

Propafenone (HCl)

Interaction of Propafenone (HCl) with Lignocaine

Suxamethonium (Cl)

Interaction of Suxamethonium (Cl) with Lignocaine

Timolol (Maleate)

Interaction of Timolol (Maleate) with Lignocaine

Tocainide (HCl)

Interaction of Tocainide (HCl) with Lignocaine

Rocuronium (Br)

Interaction of Rocuronium (Br) with Lignocaine

Fosphenytoin

Interaction of Fosphenytoin with Lignocaine

Pentazocine

Interaction of Pentazocine with Lignocaine

Propranolol (HCl)

Interaction of Propranolol (HCl) with Lignocaine

Details: Propranolol reduces clearance of lignocaine.
Cimetidine (HCl)

Interaction of Cimetidine (HCl) with Lignocaine

Details: Cimitidine increases lignocaine toxicity.

Major

Amprenavir

Interaction of Amprenavir with Lignocaine

Details: Amprenavir possibly increases plasma concentration of Lignocaine; increased risk of ventricular arrhythmias. ADVICE: Avoid concomitant use.

These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

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Side Effects

The severe or irreversible adverse effects of Lignocaine, which give rise to further complications include Allergy, Bronchospasm, Tissue necrosis, Sinus bradycardia, Blurred vision, Hypotension, Coma, Angina, Respiratory depression, Tremors, Neonatal depression, Seizures, Hypertension, Malignant hyperthermia, Cardiovascular depression.

Lignocaine produces potentially life-threatening effects which include Respiratory depression, Bradycardia, Convulsions, Hypersensitivity, CNS toxicity, Cardiac Arrest, Tonic & clonic convulsion, Medullary depression. which are responsible for the discontinuation of Lignocaine therapy.

The signs and symptoms that are produced after the acute overdosage of Lignocaine include Bradycardia, Hypotension, Apnea, Death, Seizures, Respiratory arrest, Decrease cardiac output, Cardiovascular collapse.

The symptomatic adverse reactions produced by Lignocaine are more or less tolerable and if they become severe, they can be treated symptomatically, these include Dizziness, Headache, Drowsiness, Nausea, Vomiting, Anxiety, Restlessness, Palpitation, Nervousness, Tinnitus, Abdominal pain, Confusion, Tremor, Nystagmus, Abdominal discomfort, Twitching, nervousness.

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Dosage

Flurazepam (HCl)'s dosage details are as follows:
Dose Single Dose Frequency Route Instructions

Adult Dosage

50 to 300 mg180 (175)As recommended.IV InfMax of 4mg/kg
50 to 100 mg75 (75)As recommended.IV InjFor ventricular arrythmias.
4.5 mg/ kg /dose4.5 (4.5)As recommended.SCDose vary with procedure. do not repeat within two hours.
1 to 2 %1.5 (1.5)3 hourlyTopicalAs Required
5 %5 (5)As recommended.TopicalFor spinal Anestheria as hyperbaric.

Paedriatic Dosage (20kg)

20 to 50 ug/kg.min35 (35)As recommended.IV InfusionMaintenance, As Required
0.5 to 1 mg/kg0.75 (0.75)As recommended.Slow IVInitially, As Required
2 %2 (2)3 hourlyTopicalAs Required

Neonatal Dosage (3kg)

20 to 50 ug/kg.min35 (35)As recommended.IV InfusionMaintenance, As Required
0.5 to 1 mg/kg0.75 (0.75)As recommended.Slow IVInitially, As Required
2 %2 (2)3 hourlyTopicalAs Required

High Risk Groups

Drug should not be given to Cardiac / Hypertensive Patients, patients suffering from Liver Malfunction, and Neonates.

If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.

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Warning / Precautions

Lignocaine should be used with caution in patients receiving anti-coagulant therapy, with genetic predisposition of malignant hyperthermia, hypovolemia, shock and all types of heart block, congestive heart failure, bradycardia, respiratory depression or impaired liver or renal function. The injection of lignocaine should not be administered in areas of inflammation or infection. It should be avoided if plasma cholinesterase concentration is low.

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Storage Conditions

Inj, Soln, Gel

Store Between 15°C-30°C. Do not Freeze. Protect from Sunlight.

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Interference in Pathology

No data regarding the pathological interferences produced by Lignocaine is available.

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Brands / Trade Names of Flurazepam (HCl)

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