Lidocaine Other names: Lignocaine

Chemical formula: C₁₄H₂₂N₂O  Molecular mass: 234.337 g/mol  PubChem compound: 3676

Interactions

Lidocaine interacts in the following cases:

Impaired hepatic function

If the dose or site of administration is likely to result in high blood levels, lidocaine, in common with other local anaesthetics, should be used with caution in patients with impaired hepatic function, who will require special attention to prevent potentially dangerous side effects.

Severe renal dysfunction

If the dose or site of administration is likely to result in high blood levels, lidocaine, in common with other local anaesthetics, should be used with caution in patients with severe renal dysfunction, who will require special attention to prevent potentially dangerous side effects.

Antiarrhythmic drugs class III

Patients treated with antiarrhythmic drugs class III (e.g. amiodarone) should be under close surveillance and ECG monitoring considered, since cardiac effects may be additive.

Diuretics

Diuretics antagonize the action of lidocaine due to hypokalaemia.

Beta-blockers

Drugs that reduce the clearance of lidocaine (e.g. beta-blockers) may cause potentially toxic plasma concentrations when lidocaine is given in repeated high doses over a long time period. Such interactions should therefore be of no clinical importance following short-term treatment with lidocaine at recommended doses.

CYP1A2 substrates

Lidocaine as a potent inhibitor of CYP1A2 reduces the metabolism of CYP1A2 substrates.

Epilepsy

If the dose or site of administration is likely to result in high blood levels, lidocaine, in common with other local anaesthetics, should be used with caution in patients with epilepsy, who will require special attention to prevent potentially dangerous side effects.

Atazanavir

Co-administration of lidocaine with atazanavir increases the risk of cardiotoxicity and arrhythmias.

Cimetidine

Drugs that reduce the clearance of lidocaine (e.g. cimetidine) may cause potentially toxic plasma concentrations when lidocaine is given in repeated high doses over a long time period. Such interactions should therefore be of no clinical importance following short-term treatment with lidocaine at recommended doses.

Darunavir

Darunavir may increase lidocaine levels in blood serum.

Quinupristine

Co-administration of lidocaine with quinupristine increases the risk of toxicity.

Tamoxifen

Lidocaine may reduce the therapeutic effect of tamoxifen by reducing the production of its active metabolites.

Telithromycin

Telithromycin may reduce the clearance of lidocaine.

Terbinafine

Terbinafine may reduce the metabolism and clearance of lidocaine.

Voriconazole

Voriconazole may increase lidocaine levels in blood serum by reducing its metabolism.

Atrioventricular block

If the dose or site of administration is likely to result in high blood levels, lidocaine, in common with other local anaesthetics, should be used with caution in patients with atrioventricular block, who will require special attention to prevent potentially dangerous side effects.

Endotracheal tube

Lidocaine should not be used on cuffs of endotracheal tubes (ETT) made of plastic. Lidocaine base in contact with both PVC and non-PVC cuffs of endotracheal tubes may cause damage of the cuff. This damage is described as pinholes, which may cause leakage that could lead to pressure loss in the cuff.

Porphyria

Lidocaine is probably porphyrinogenic and should only be prescribed to patients with acute porphyria on strong or urgent indications. Appropriate precautions should be taken for all porphyric patients.

Cardiovascular disease, heart failure

If the dose or site of administration is likely to result in high blood levels, lidocaine, in common with other local anaesthetics, should be used with caution in patients with cardiovascular disease and heart failure, who will require special attention to prevent potentially dangerous side effects.

Pregnancy

There is no, or inadequate evidence of safety of the drug in human pregnancy but it has been in wide use for many years without apparent ill consequence, and animal studies have shown no hazard. If drug therapy is needed in pregnancy, this drug can be used if there is no safer alternative.

Nursing mothers

Lidocaine enters the mother’s milk, but in such small quantities that there is generally no risk of the child being affected at therapeutic dose levels.

Effects on ability to drive and use machines

Lidocaine has minor influence on the ability to drive and use machines. Depending on the dose, local anaesthetics may have a very mild effect on mental function and may temporarily impair locomotion and co-ordination.

Adverse reactions


In extremely rare cases amide-type local anaesthetic preparations have been associated with allergic reactions (in the most severe instances anaphylactic shock).

Local irritation at the application site has been described. Following application to laryngeal mucosa before endotracheal intubation, reversible symptoms such as “sore throat”, “hoarseness” and “loss of voice” have been reported. The use of Xylocaine pump spray provides surface anaesthesia during an endotracheal procedure but does not prevent post-intubation soreness.

Systemic adverse reactions are rare and may result from high plasma levels due to excessive dosage or rapid absorption (e.g. following application to areas below the vocal chords) or from hypersensitivity, idiosyncrasy or reduced tolerance on the part of the patient. Such reactions involve the central nervous system and/or the cardiovascular system.

CNS reactions are excitatory and/or depressant and may be characterised by nervousness, dizziness, convulsions, unconsciousness and possibly respiratory arrest. The excitatory reactions may be very brief or may not occur at all, in which case the first manifestations of toxicity may be drowsiness, merging into unconsciousness and respiratory arrest.

Cardiovascular reactions are depressant and may be characterised by hypotension, myocardial depression, bradycardia and possibly cardiac arrest.

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