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Lidocaine information from DrugsUpdate  

See Available Brands of Lidocaine in India

P - Caution when used during pregnancy
FI - Food *
LI - Lab *

Lidocaine or lignocaine is a common local anesthetic and antiarrhythmic drug. Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic or as a local anesthetic for minor surgery.

Pharmacodynamics

Anesthesia
Lidocaine alters signal conduction in neurons by blocking the fast voltage gated sodium (Na+) channels in the neuronal cell membrane, which are responsible for signal propogation. With sufficient blockade, the membrane of the postsynaptic neuron will not depolarize and so fail to transmit an action potential, leading to its anaesthetic effects. Careful titration allows for a high degree of selectivity in the blockage of sensory neurons, whereas higher concentrations will also affect other modalities of neuron signaling.

Pharmacokinetics

Lidocaine is an amide type local anaesthetic. It stabilises the neuronal membrane and inhibits sodium ion movements, which are necessary for conduction of impulses. In the heart, lidocaine reduces phase 4 depolarisation and automaticity. Duration of action potential and effective refractory period are also reduced.


Onset
45-90 seconds

Duration
10-20 minutes

Absorption

Readily absorbed from the GI tract, mucous membranes, damaged skin, inj sites, including muscle; poor through intact skin.

Distribution
Crosses the placenta, blood-brain barrier and enters breast milk. Protein-binding: 66% (α1-acid glycoprotein).

Metabolism
90% hepatic; converted to monoethylglycinexylidide and glycinexylidide. First-pass metabolism is extensive, bioavailability after oral dose is approx 35%.

Excretion
Via urine (<10% unchanged). Elimination half-life: biphasic; initial: 7-30 min; terminal: 1.5-2 hours (adults), 3.2 hours (infants, premature infants).

Lidocaine Indications / Lidocaine Uses

Information Not Available

Lidocaine Adverse Reactions / Lidocaine Side Effects

Dizziness, paraesthesia, drowsiness, confusion, respiratory depression and convulsions.

Potentially Fatal: Hypotension and bradycardia leading to cardiac arrest; anaphylaxis.

Precautions

The safety and effectiveness of Lidocaine depend on proper dosage, correct technique, adequate precautions, and readiness for emergencies. Resuscitative equipment, oxygen and other resuscitative drugs should be available for immediate use. The lowest dosage that results in effective anesthesia should be used to avoid high plasma levels and serious adverse effects. Repeated doses of Lidocaine may cause significant increases in blood levels with each repeated dose, because of slow accumulation of the drug or its metabolites. Tolerance to elevated blood levels varies with the status of the patient. Debilitated, elderly patients, acutely ill patients, and children should be given reduced doses commensurate with their age and physical status. Lidocaine should also be used with caution in patients with severe shock or heart block.


Overdosage
Severe hypotension, asystole, bradycardia, apnoea, seizures, coma, cardiac arrest, respiratory arrest, and death.

Special Precautions

Hepatic or renal impairment; CHF and following cardiac surgery; bradycardia; respiratory depression; porphyria; elderly or debilitated patients; pregnancy.

Other Drug Interactions

Additive cardiac effects with IV phenytoin. Effects antagonized by hypokalaemia caused by acetazolamide, loop diuretics and thiazides. Dose requirements may be increased with long-term use of phenytoin and other enzyme-inducers.

Potentially Fatal: Cimetidine and propranolol increase plasma concentration and toxicity. Increased risk of myocardial depression with beta blockers and other antiarrhythmics.

Other Interactions

Food Interaction
Decreased levels with St John's wort.

Dosage

Intravenous
Pulseless ventricular fibrillation or ventricular tachycardia
Adult: As hydrochloride: 1-1.5 mg/kg repeated as necessary. Max total: 3 mg/kg. For ventricular arrhythmias in more stable patients: Usual loading dose: 50-100 mg as an IV injection at 25-50 mg/minute, may repeat once or twice up to a max of 200-300 mg in 1 hour, followed by 1-4 mg/minute via continuous IV infusion. May need to reduce dose if the infusion is longer than 24 hours.

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Intravenous
Intravenous regional anaesthesia
Adult: 50-300 mg (10-60 ml) of a 0.5% solution without adrenaline; max dose: 4 mg/kg.

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Intramuscular
Emergency treatment of ventricular arrhythmias
Adult: As hydrochloride: 300 mg injected into the deltoid muscle, repeat after 60-90 minutes if necessary.

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Parenteral
Sympathetic nerve block
Adult: As hydrochloride: 50 mg (5 ml) of a 1% solution for cervical block or 50-100 mg (5-10 ml) of a 1% solution for lumbar block.

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Parenteral
Percutaneous infiltration anaesthesia
Adult: As hydrochloride: 5-300 mg (1-60 ml of a 0.5% solution or 0.5-30 ml of a 1% solution).

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Parenteral
Peripheral nerve block
Adult: As hydrochloride: For brachial plexus block: 225-300 mg (15-20 ml) of a 1.5% solution; for intercostal nerve block: 30 mg (3 ml) of a 1% solution; for paracervical block: 100 mg (10 ml) of a 1% solution on each side, repeated not more frequently than every 90 minutes; for paravertebral block: 30-50 mg (3-5 ml) of a 1% solution; for pudendal block: 100 mg (10 ml) as a 1% solution on each side; for retrobulbar block: 120-200 mg (3-5 ml) of a 4% solution.

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Rectal
Haemorrhoids
Adult: Apply topically to clean, dry area or using applicator, insert rectally, up to 6 times/day.
Child: ≥12 years: Apply topically to clean, dry area or using applicator, insert rectally, up to 6 times/day.

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Rectal
Perianal pain and itching
Adult: Apply topically to clean, dry area or using applicator, insert rectally, up to 6 times/day.
Child: ≥12 years: Apply topically to clean, dry area or using applicator, insert rectally, up to 6 times/day.

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Ophthalmic
Surface anaesthesia
Adult: As hydrochloride 4 % with fluorescein: 1 or more drops as required.
Child: As hydrochloride 4 % with fluorescein : As directed by physician.

Topical/Cutaneous
Surface anaesthesia
Adult: As eutectic mixture containing lidocaine base 2.5% and prilocaine base 2.5%: Apply cream to skin under an occlusive dressing before procedure. Use without an occlusive dressing for genital warts.

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Mouth/Throat
Surface anaesthesia
Adult: For pain: 300 mg (15 ml) of 2% solution rinsed and ejected for mouth and throat pain; or gargled and swallowed if necessary for pharyngeal pain. Not to be used more frequently than every 3 hours. Max (topical oral solution): 2.4 g/day. Before bronchoscopy, bronchography, laryngoscopy, oesophagoscopy, endotracheal intubation, and biopsy in the mouth and throat: 40-300 mg (1-7.5 ml) of 4% solution. For dentistry and otorhinolaryngology procedures: 10-50 mg of 10% solution sprayed to mucous membrane. For laryngotracheal anaesthesia: 160 mg of 4% solution sprayed or instilled as a single dose into the lumen of the larynx and trachea.

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Urethral
Surface anaesthesia
Adult: As 2% gel: Female: 60-100 mg inserted into the urethra several minutes before examination. Male: 100-200 mg before catheterisation and 600 mg before sounding or cystoscopy.

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Epidural

Epidural anaesthesia
Adult: As hydrochloride: 2-3 ml solution administered for each dermatome to be anaesthesized. Recommended doses are: lumbar epidural 250-300 mg (25-30 ml of a 1% solution) for analgesia and 225-300 mg (15-20 ml of a 1.5% solution) or 200-300 mg (10-15 ml of a 2% solution) for anaesthesia; for thoracic epidural: 200-300 mg of a 1% solution. For obstetric caudal analgesia, up to 300 mg (30 ml of a 0.5% or 1% solution); for surgical caudal analgesia: 225-300 mg (15-20 ml of a 1.5% solution). For continuous epidural anaesthesia, not to repeat max doses more frequently than 1.5 hourly.

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Intraspinal
Spinal anaesthesia
Adult: As hyperbaric solution of 1.5% or 5% lidocaine in 7.5% glucose solution. Normal vaginal delivery: 50 mg (1 ml) of a 5% solution or 9-15 mg (0.6-1 ml) of a 1.5% solution. Caesarian operation: Up to 75 mg (1.5 ml) of a 5% solution. Other surgical procedures: 75-100 mg (1.5-2 ml).

Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis.

Injection
Pupil dilatation during phacoemulsification cataract surgery
Adult: As a 1% ophthalmic preservative-free solution (often used in combination with phenylephrine and cyclopentolate). To be injected into the anterior chamber of the eye at the beginning of the procedure.

Reconstitution
Standard diluent: 2 g/250 ml dextrose 5%.
Incompatibility: Y-site incompatibility: Amphotericin B cholesteryl sulfate complex, thiopental. Syringe incompatibility: Cefazolin. Admixture incompatibility: Phenytoin, amphotericin B, dacarbazine, methohexital.

Food(before/after)

Information Not Available

List of Contraindications

Lidocaine and Pregnancy

Caution when used during pregnancy

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

As LA & cardiac drug.

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Lidocaine and Lactation

Information Not Available

Lidocaine and Children

Dosages in children should be reduced, commensurate with age and body weight.

Lidocaine and Geriatic

Information Not Available

Lidocaine and Other Contraindications

Hypovolaemia; heart block or other conduction disturbances

Storage

Epidural
Stable at room temperature.

Intramuscular
Stable at room temperature. Intraspinal: Stable at room temperature.


Intravenous
Stable at room temperature.

Mouth/Throat
Stable at room temperature.

Ophthalmic
Store at 15-25°C. Protect from light. Discard after use.

Parenteral

Stable at room temperature.

Rectal

Stable at room temperature.

Topical/Cutaneous
Stable at room temperature.

Urethral
Stable at room temperature.

Lab interference

Epidural
Stable at room temperature.

Intramuscular
Stable at room temperature. Intraspinal: Stable at room temperature.


Intravenous
Stable at room temperature.

Mouth/Throat
Stable at room temperature.

Ophthalmic
Store at 15-25°C. Protect from light. Discard after use.

Parenteral

Stable at room temperature.

Rectal

Stable at room temperature.

Topical/Cutaneous
Stable at room temperature.

Urethral
Stable at room temperature.

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