Lidocaine injection

Lidocaine is an antiarrhythmic agent (affects heart rhythm) as well as a local anesthetic (amide type).

The initial dose for anesthesia in adults depends on the procedure, necessary depth of anesthesia, blood flow to the region, desired duration of anesthesia, and condition of the patient. For anesthesia, the maximum dose is 4.5 mg/kg and should not exceed 300 mg per dose. For control of arrhythmias (abnormal heart rhythm), an initial intravenous or intraosseous (injected into bone) dose is 1 to 1.5 mg/kg. If providing dose by endotrachial tube the initial dose is 2 to 3.75 mg/kg. Lidocaine is rapidly metabolized. Any conditions that later liver functions may alter the half live of lidocaine.

Injection Solution with or without preservatives: 0.4%, 0.5%, 0.8%, 1%, 1.5%, 2%, 4%, 5% in 2, 5, 10, 20, 30, 50, 250, 500 mL.

Lidocaine should be stored at room temperature, between 15 C to 30 C (59 F to 86 F).

Lidocaine is similar to bupivacaine and procaine. Lidocaine, like other local anesthetics causes a loss of sensation by reducing the flow of sodium in and out nerves to decrease the initiation and transfer of nerve signals. Compared to procaine, lidocaine has a more rapid onset, longer duration of action, and more potent activity. Lidocaine works as an antiarrhythmic by also decreasing conduction of electrical signals in damaged (ischemic) heart tissue.

Lidocaine was approved by the FDA in November 1948.

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Get emergency medical help if you have signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Tell your caregiver right away if you have:

• twitching, tremors, seizure (convulsions);

• a light-headed feeling, like you might pass out;

• slow heart rate, weak pulse, weak or shallow breathing;

• sudden feeling of warmth with muscle stiffness and pain;

• dark urine;

• blue appearance of the skin; or

• severe anxiety, unusual fear or uneasy feeling.

Common side effects may include:

• drowsiness, dizziness;

• vomiting;

• feeling hot or cold;

• confusion, ringing in your ears, blurred vision, double vision; or

• numbness in places where the medicine is accidentally applied.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

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.

Hemodynamics: Excessive blood levels may cause changes in cardiac output, total peripheral resistance, and mean arterial pressure. With central neural blockade these changes may be attributable to block of autonomic fibers, a direct depressant effect of the local anesthetic agent on various components of the cardiovascular system, and/or the beta-adrenergic receptor stimulating action of epinephrine when present. The net effect is normally a modest hypotension when the recommended dosages are not exceeded.

Pharmacokinetics and Metabolism: 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. Except for intravascular administration, the highest blood levels are obtained following intercostal nerve block and the lowest after subcutaneous administration.

The plasma binding of lidocaine is dependent on drug concentration, and the fraction bound decreases with increasing concentration. At concentrations of 1 mcg to 4 mcg of free base per mL, 60 to 80 percent of lidocaine is protein bound. Binding is also dependent on the plasma concentration of the alpha-1-acid glycoprotein.

Lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion.

Lidocaine is metabolized rapidly by the liver, and metabolites and unchanged drug are excreted by the kidneys. Biotransformation includes oxidative N-dealkylation, ring hydroxylation, cleavage of the amide linkage, and conjugation. N-dealkylation, a major pathway of biotransformation, yields the metabolites monoethylglycinexylidide and glycinexylidide. The pharmacological/toxicological actions of these metabolites are similar to, but less potent than, those of lidocaine. Approximately 90% of lidocaine administered is excreted in the form of various metabolites, and less than 10% is excreted unchanged. The primary metabolite in urine is a conjugate of 4-hydroxy-2,6- dimethylaniline.

The elimination half-life of lidocaine following an intravenous bolus injection is typically 1.5 to 2 hours. Because of the rapid rate at which lidocaine is metabolized, any condition that affects liver function may alter lidocaine kinetics. The half-life may be prolonged two-fold or more in patients with liver dysfunction. Renal dysfunction does not affect lidocaine kinetics but may increase the accumulation of metabolites.

Factors such as acidosis and the use of CNS stimulants and depressants affect the CNS levels of lidocaine required to produce overt systemic effects. Objective adverse manifestations become increasingly apparent with increasing venous plasma levels above 6 mcg free base per mL. In the rhesus monkey arterial blood levels of 18 mcg/mL to 21 mcg/mL have been shown to be threshold for convulsive activity.

Lidocaine HCl injection is indicated for production of local or regional anesthesia by infiltration techniques such as percutaneous injection and by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks, when the accepted procedures for these techniques as described in standard textbooks are observed.

LIDOCAINE HYDROCHLORIDE INJECTION, FOR INFILTRATION AND NERVE BLOCK, SHOULD BE EMPLOYED ONLY BY CLINICIANS WHO ARE WELL VERSED IN DIAGNOSIS AND MANAGEMENT OF DOSE-RELATED TOXICITY AND OTHER ACUTE EMERGENCIES THAT MIGHT ARISE FROM THE BLOCK TO BE EMPLOYED AND THEN ONLY AFTER ENSURING THE IMMEDIATE AVAILABILITY OF OXYGEN, OTHER RESUSCITATIVE DRUGS, CARDIOPULMONARY EQUIPMENT AND THE PERSONNEL NEEDED FOR PROPER MANAGEMENT OF TOXIC REACTIONS AND RELATED EMERGENCIES. (See also ADVERSE REACTIONS and PRECAUTIONS.) DELAY IN PROPER MANAGEMENT OF DOSE-RELATED TOXICITY, UNDERVENTILATION FROM ANY CAUSE AND/OR ALTERED SENSITIVITY MAY LEAD TO THE DEVELOPMENT OF ACIDOSIS, CARDIAC ARREST AND, POSSIBLY, DEATH.

Intra-articular infusions of local anesthetics following arthroscopic and other surgical procedures is an unapproved use, and there have been post-marketing reports of chondrolysis in patients receiving such infusions. The majority of reported cases of chondrolysis have involved the shoulder joint; cases of gleno-humeral chondrolysis have been described in pediatric and adult patients following intra-articular infusions of local anesthetics with and without epinephrine for periods of 48 to 72 hours. There is insufficient information to determine whether shorter infusion periods are not associated with these findings. The time of onset of symptoms, such as joint pain, stiffness and loss of motion can be variable, but may begin as early as the 2nd month after surgery. Currently, there is no effective treatment for chondrolysis; patients who experienced chondrolysis have required additional diagnostic and therapeutic procedures and some required arthroplasty or shoulder replacement.

To avoid intravascular injection, aspiration should be performed before the local anesthetic solution is injected. The needle must be repositioned until no return of blood can be elicited by aspiration. Note, however, that the absence of blood in the syringe does not guarantee that intravascular injection has been avoided.

Lidocaine Hydrochloride Injection, USP, 2%

Discard unused portion after initial use.

Store at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.]

Revised: 5/2015

EN-3677
Hospira, Inc., Lake Forest, IL 60045 USA     

Consult your pharmacist.

How to use Lidocaine Hcl Vial

Consult your pharmacist.