Brands, Medical Use, Clinical Data
Drug Category
- Antiarrhythmic Agents
- Anesthetics
Dosage Forms
- Cream
- Gel
- Implant
- Jelly
- Kit
- Liquid
- Ointment
- Solution
- Spray
Brands / Synonyms
After Burn Double Strength Gel; After Burn Double Strength Spray; After Burn Gel; After Burn Spray; Alphacaine; Anestacon; Anestacon Jelly; Axsain; Cappicaine; Dalcaine; DermaFlex; Dilocaine; Duncaine; Emla; Esracaine; Gravocain; Isicaina; L-Caine; Lanabiotic; Leostesin; Lidocaine; Lidocaine and Dextrose; Lidocaine and Epinephrine; Lidocaine and Prilocaine; Lidoderm; Lidoject-1; Lidoject-2; Lidopen; Lidosite; Lignocaine; Maricaine; Norwood Sunburn Spray; Octocaine; Octocaine-100; Octocaine-50; Oraqix; Pliaglis; Rocephin Kit; Synera; Xylocaine; Xylocaine 5% Spinal; Xylocaine Dental Ointment; Xylocaine Endotracheal; Xylocaine Test Dose; Xylocaine Viscous; Xylocaine-MPF; Xylocaine-MPF with Glucose; Xylocard; Zilactin-L
; Zingo
Indications
For production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks.
Pharmacology
Lidocaine is an anesthetic agent indicated for production of local or regional anesthesia and in the treatment of ventricular tachycardia occurring during cardiac manipulation, such as surgery or catheterization, or which may occur during acute myocardial infarction, digitalis toxicity, or other cardiac diseases. The mode of action of the antiarrhythmic effect of Lidocaine appears to be similar to that of procaine, procainamide and quinidine. Ventricular excitability is depressed and the stimulation threshold of the ventricle is increased during diastole. The sinoatrial node is, however, unaffected. In contrast to the latter 3 drugs, Lidocaine in therapeutic doses does not produce a significant decrease in arterial pressure or in cardiac contractile force. In larger doses, lidocaine may produce circulatory depression, but the magnitude of the change is less than that found with comparable doses of procainamide.
Mechanism of Action
Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action.
Absorption
Information derived from diverse formulations, concentrations and usages reveals that lidocaine is completely absorbed following parenteral administration, its rate of absorption depending, for example, upon various factors such as the site of administration and the presence or absence of a vasoconstrictor agent.
Toxicity
The oral LD 50 of lidocaine HCl in non-fasted female rats is 459 (346-773) mg/kg (as the salt) and 214 (159-324) mg/kg (as the salt) in fasted female rats. Symptoms of overdose include convulsions, hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest.
Biotrnasformation / Drug Metabolism
Primarily hepatic.
Contraindications
Lidocaine is contraindicated in patients with a known history of hypersensitivity to local anesthetics of the amide type.
Drug Interactions
The administration of local anesthetic solutions containing epinephrine or norepinephrine to patients receiving monoamine oxidase inhibitors or tricyclic antidepressants may produce severe, prolonged hypertension.
Phenothiazines and butyrophenones may reduce or reverse the pressor effect of epinephrine.
Concurrent use of these agents should generally be avoided. In situations when concurrent therapy is necessary, careful patient monitoring is essential.
Concurrent administration of vasopressor drugs (for the treatment of hypotension related to obstetric blocks) and ergot-type oxytocic drugs may cause severe, persistent hypertension or cerebrovascular accidents.
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