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Lidocaine (INN) (pronounced /ˈlaɪdoʊkeɪn/) or lignocaine (former BAN) (/ˈlɪgnoʊkeɪn/) 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, and in minor surgery. The most commonly encountered lidocaine preparations are marketed by Abraxis Pharmaceutical Products under the brand names Xylocaine and Xylocard, and as 'Lanacane' topical ointment in the UK, though lidocaine is also found in many other proprietary preparations.
Lidocaine, the first amino amide-type local anesthetic, was first synthesised under the name xylocaine by Nils Löfgren in 1943. His colleague Bengt Lundqvist made the first injection anesthesia experiments on himself.It was first marketed in 1948.
Lidocaine has a more rapid onset of action and longer duration of action than amino ester-type local anesthetics such as procaine. It is approximately 90% metabolized in the liver by CYP1A2 (and to a minor extent CYP3A4) to the pharmacologically-active metabolites monoethylglycinexylidide and glycinexylidide.
The elimination half-life of lidocaine is approximately 1.5–2 hours in most patients. This may be prolonged in patients with hepatic impairment (average 343 minutes) or congestive heart failure (average 136 minutes). (Thomson et al., 1973)
Lidocaine alters depolarization in neurons, by blocking the fast voltage gated sodium (Na+) channels in the cell membrane. With sufficient blockade, the membrane of the presynaptic neuron will not depolarize and so fail to transmit an action potential, leading to its anesthetic 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 signalling.
Indications for the use of lidocaine include:
Contraindications for the use of lidocaine include:
Adverse drug reactions
Adverse drug reactions (ADRs) are rare when lidocaine is used as a local anesthetic and is administered correctly. Most ADRs associated with lidocaine for anesthesia relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, but allergic reactions can rarely occur..
Systemic exposure to excessive quantities of lidocaine mainly result in central nervous system (CNS) and cardiovascular effects – CNS effects usually occur at lower blood plasma concentrations and additional cardiovascular effects present at higher concentrations, though cardiovascular collapse may also occur with low concentrations. CNS effects may include CNS excitation (nervousness, tingling around the mouth, tinnitus, tremor, dizziness, blurred vision, seizures) followed by depression (drowsiness, loss of consciousness, respiratory depression and apnea). Cardiovascular effects include hypotension, bradycardia, arrhythmias, and/or cardiac arrest – some of which may be due to hypoxemia secondary to respiratory depression. (Rossi, 2006)
ADRs associated with the use of intravenous lidocaine are similar to toxic effects from systemic exposure above. These are dose-related and more frequent at high infusion rates (≥3 mg/minute). Common ADRs include: headache, dizziness, drowsiness, confusion, visual disturbances, tinnitus, tremor, and/or paraesthesia. Infrequent ADRs associated with the use of lidocaine include: hypotension, bradycardia, arrhythmias, cardiac arrest, muscle twitching, seizures, coma, and/or respiratory depression. (Rossi, 2006)
Lidocaine, usually in the form of lidocaine hydrochloride, is available in various forms including:
Additive in cocaine
Lidocaine is often added to cocaine as a diluent. Cocaine numbs the gums when applied, and since lidocaine causes stronger gingival numbness, customers get the impression of high-quality cocaine when in actuality, the user is receiving a diluted product.
|This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Lidocaine". A list of authors is available in Wikipedia.|