Clear colorless sterile solution for injection.
Each mL contains Lidocaine hydrochloride 20 mg.
Pharmacology: Pharmacodynamics: Lidocaine Hydrochloride is a local anaesthetic of the amide type. It has a rapid onset and a medium duration of action. Onset and the duration of the local anaesthetic effect of lidocaine depend on the dose and the site of ministration. Lidocaine, like other local anaesthetics, causes a reversible blockade of impulse propagation along nerve fibres by preventing the inward movement of sodium ions through the cell membrane of the nerve fibres. The ion channels of the nerve membrane are considered a receptor for local anaesthetic molecules.
Pharmacokinetics: Absorption: The plasma concentration of lidocaine depends upon the dose, the route of administration and the vascularity of the injection site.
Distribution: The pKa of Lidocaine Hydrochloride is 7.86 and is 60-80% protein-bound (mainly to alpha-1-acid glycoprotein) in plasma, total plasma clearance of 0.95 L/min, Vd is 1.1-2.1 LK; alterable by many patient factors, decrease in CHF and liver disease and crosses blood-brain barrier. Lidocaine readily crosses the placenta. Lidocaine is excreted in breast milk, but in such small quantities that there is no risk of affecting the child with therapeutic doses.
Metabolism: Lidocaine is almost entirely due to liver metabolism 90%. The main metabolites formed from lidocaine are monoethylglycinexylidide (MEGX) and glycinexylidide (GX) can accumulate and may cause CNS toxicity.
Excretion: Lidocaine is metabolism occurs and metabolites are excreted in the urine with less than 10% of unchanged lidocaine. Lidocaine shows biphasic half-life elimination and prolonged with CHF, liver disease, shock, severe renal disease.
Initial: 7-30 minutes; Terminal: Infants, premature 3.2 hours; Adults 1.5-2 hours.
Local Anaesthesia by the following techniques: Infiltration; Peripheral or Sympathetic nerve block; Epidural (including caudal) block.
Administration: Percutaneous injection and intravenous regional nerve block. Dosage of Lidocaine hydrochloride in children and adults varies, depending on the site of injection, procedures used, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, physical condition of patient and individual patient response.
Maximum: 4.5 mg/kg/Dose (or 300 mg) do not repeat within 2 hours.
(* For paracervical and continuous epidural should not be repeated more frequently than every 90 minutes). (See Table 1.)
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Systemic toxic effects of local anesthetics are related to blood concentrations as absorption varies considerably according to the site of action. Furthermore, most cases of severe toxicity did not result from over dosage but from inadvertent intravascular injection or too rapid injection. The most serious effects of lidocaine intoxication are on the CNS and cardiovascular system and overdose can result in severe hypotension, bradycardia, arrhythmia and cardiac arrest, seizures. In severe cases apnea may occur.
Treatment of acute toxicity: If signs of acute systemic toxicity appear, injection of the local anaesthetic should be stopped immediately and CNS symptoms (convulsion, CNS depression) must promptly be treated with appropriate airway/respiratory support and the administration of anticonvulsant drugs such as benzodiazepines (diazepam). If circulatory arrest should occur, immediate cardiopulmonary resuscitation should be instituted. Optimal oxygenation and ventilation and the circulation should be maintained with infusion of intravenous fluids. Vasopressors should not be given to patients receiving oxytocic drug.
Hypersensitivity to another local anaesthetics of the amide type or to any of the excipients.
In general lidocaine should not be given to patients with hypovolaemia, heart block or other condition disturbances, and should be used in with caution in patients with congestive heart failure, bradycardia, or respiratory depression. Lidocaine is metabolised in the liver and must be given with caution to patients with hepatic impairment or pseudocholinesterase deficiency. Metabolites of lidocaine may accumulate in patients with renal impairment. May have increased risk of lidocaine toxicity.
The intramuscular injection of lidocaine may increase creatine phosphokinase concentrations that can interfere with the diagnosis of acute myocardial infarction.
Pregnancy: No specific disturbances to the reproductive process have so far been reported, eg, no increased incidence of malformations. Adverse effects in fetal due to local anaesthetics, seem to be most apparent in paracervical block anaesthesia. Large dose can cause fetal bradycardia and can cause neonatal respiratory depression hypotonia. Such effects may be due to high concentrations of anaesthetic reaching the fetus from used locally to provide analgesia prior to episiotomy and during repair of obstetric lacerations. Administration by the perineal route may effects results in greater absorption than administration by the epidural route however when used in appropriate doses the risk of the fetus is low.
Lactation: Lidocaine may enter the mother's milk, but in such small amounts that there is generally no risk of this affecting the neonate.
See Table 2.
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Should avoid concomitant use of Lidocaine with Conivaptan and Saquinavir.
Increased effect/Toxicity: Lidocaine may increase the levels/effect of Prilocaine.
The levels/effect of Lidocaine may be increased by Abiraterone acetate, Amiodarone, Beta-blockers, Conivaptan, CYP1A2 inhibitors (Moderate), CYP1A2 inhibitors (Strong), CYP3A4 inhibitors (Moderate), CYP3A inhibitors (Strong), Darunavir, Dasatinib, Deferasirox, Disopyramide, Hyaluronidase, Ivacaftor, Mifepristone, Saquinavir, Telaprevir.
Decreased effect: The levels/effect of Lidocaine may be decreased by CYP1A2 inducers (Strong), CYP3A4 inducers (Strong), Cyproterone, Deferasirox, Etravirine, Herb (CYP3A4 inducers), Tocilizumab.
Interactions with Ethanol/Nutrition/Herb: Herb and Nutraceutical may decrease lidocaine levels/effect should avoid concurrent use.
N01BB02 - lidocaine ; Belongs to the class of amides. Used as local anesthetics.
Chalocard 2% Non-Preservative soln for inj 20 mg/mL
((10 mL)) 1's; ((5 mL)) 1's; ((50 mL)) 1's
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