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| CATEGORIES ABOUT LIDOCAINE | |
| antiarrhythmic agents | |
| local anesthetics | |
Lidocaine ( and Antiarrhythmic drug. The most commonly encountered lidocaine preparations are marketed by AstraZeneca under the brand names '''Xylocaine''' and '''Xylocard''', though lidocaine is also found in many other proprietary preparations. HISTORY Lidocaine, the first Amino Amide -type local anesthetic, was developed by Nils Löfgren and Bengt Lundqvist in 1943 and first marketed in 1948 . PHARMACOKINETICS 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) PHARMACOLOGY Anesthesia Lidocaine alters depolarization in Neuron s, by blocking the fast sodium (Na+) channels in the cell membrane. With sufficient blockade, the membrane will not depolarise and so not transmit an action potential, leading to its anesthetic effects. Antiarrhythmia Lidocaine is classified as a Class Ib Antiarrhythmic Agent , blocking the Sodium channel of the Cardiac Action Potential , which decreases automaticity by reducing the slope of phase 0 of Depolarization with little effect on the PR Interval , QRS Complex or QT Interval . CLINICAL USE Indications Indications for the use of lidocaine include:
Contraindications Contraindications for the use of lidocaine include:
Adverse drug reactions Adverse Drug Reaction s (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, however 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 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, Seizure s) followed by depression (drowsiness, loss of consciousness, Respiratory Depression and Apnea ). Cardiovascular effects include Hypotension , Bradycardia , Arrhythmia s, 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, , Bradycardia , Arrhythmia s, Cardiac Arrest , muscle twitching, Seizure s, Coma , and/or respiratory depression. (Rossi, 2006) Dosage forms Lidocaine, usually in the form of lidocaine hydrochloride, is available in various forms including:
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