Accucaine

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 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 2.0 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 6.0 mcg free base per mL. In the rhesus monkey arterial blood levels of 18-21 mcg/mL have been shown to be threshold for convulsive activity.

Lidocaine Hydrochloride Injection, USP is indicated 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, 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.

Local anesthetic solutions containing antimicrobial preservatives (e.g., methylparaben) should not be used for epidural or spinal anesthesia because the safety of these agents has not been established with regard to intrathecal injection, either intentional or accidental.

RL-4823

5mL NDC 0409-4713-12

Preservative-Free

Rx only

1%

LIDOCAINE HCl

Injection, USP

50 mg/5mL

(10 mg/mL)

Hospira, Inc.

Lake Forest, IL 60045 USA

Hospira

NDC: 76420-715-01 Rx Only

Accucaine™

Kit Contains

1 Lidocaine HCl Injection, USP 1% (5mL)

1 Ultrasound Transmission Gel (20g)

1 Gebauer's Pain Ease® (30mL)

1 BD Integra Syringe with Retracting BD PrecisionGlide™ Needle (3mL 23G x 1”)

1 BD Integra Syringe with Retracting BD PrecisionGlide™ Needle (3mL 25G x 1”)

1 Pair Nitrile Powder Free Sterile Gloves (M)

1 Drape

1 Adhesive Bandage

1 Isopropyl Alcohol 70% Prep Pad

5 Non-sterile 4x4 gauze

1 Face mask

1 Dose

Single Use Only

Distributed by Enovachem™ 


PHARMACEUTICALS

Torrance, CA 90501

Applies to lidocaine: compounding powder, injectable solution, intravenous solution

General

Adverse reactions following administration of this drug are similar in nature to those observed with other amide local anesthetic agents. The most serious adverse reactions tend to be systemic in nature. In general, these adverse reactions are dose-related and may result from high plasma levels caused by excessive dosage, rapid absorption, or inadvertent intravascular injection, or may result from a hypersensitivity, idiosyncrasy, or diminished tolerance on the part of the patient.[Ref]

Cardiovascular

Frequency not reported: Bradycardia, hypotension, cardiovascular collapse, cardiac arrest, circulatory collapse, hypertension, arrhythmia, maternal hypotension, shock, tachycardia, ventricular fibrillation, heart block, myocardial depression, peripheral vasodilation[Ref]

Nervous system

Frequency not reported: Lightheadedness, headache, dizziness, drowsiness, cold/numbness, tremor, convulsions, unconsciousness, positional headache, peripheral nerve symptoms, spinal cord deficit, paresthesia, speech slurred, arachnoiditis, peripheral nerve injury, coma, paralysis of the lower extremities, cauda equina syndrome, Horner's syndrome, hemiparesis, circumoral paresthesia, nystagmus[Ref]

Gastrointestinal

Frequency not reported: Vomiting, nausea, bowel control loss, swallowing difficult, numbness of tongue[Ref]

Psychiatric

Frequency not reported: Nervousness, apprehension, euphoria, confusion, agitation, disorientation, psychosis, restlessness, excitement[Ref]

Hematologic

Frequency not reported: Methemoglobinemia[Ref]

Dermatologic

Frequency not reported: Urticaria, cutaneous lesion, dermatitis, rash, angioedema, face edema[Ref]

Genitourinary

Frequency not reported: Bladder control loss, sexual function loss, perineal sensation loss, urinary retention[Ref]

Immunologic

Frequency not reported: Allergic reaction, anaphylaxis/anaphylactoid reaction[Ref]

Local

Frequency not reported: Persistent anesthesia[Ref]

Metabolic

Frequency not reported: Hypoglycemia[Ref]

Musculoskeletal

Frequency not reported: Twitching, backache, leg pain, buttock pain[Ref]

Ocular

Frequency not reported: Blurred/doubled vision, diplopia, transient amaurosis, bilateral amaurosis[Ref]

Other

Frequency not reported: Tinnitus, feeling hot, edema, shiver, total spinal block, hyperacusis, weakness, sphincter control loss[Ref]

Respiratory

Frequency not reported: Respiratory depression, respiratory arrest, dyspnea, bronchospasm, hypoventilation, apnea, respiratory inadequacy, respiratory failure, yawning[Ref]

Some side effects of lidocaine may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

Initial dose: 50 to 100 mg IV bolus once over 2 to 3 minutes; may repeat after 5 minutes if necessary not to exceed up to 300 mg in a 1-hour period
Following bolus administration: 1 to 4 mg/min continuous IV infusion

Comments:
-Patients should be under constant ECG monitoring during administration of this drug.
-Sufficient time should be allowed to enable a slow circulation to carry this drug to the site of action.
-The rate of the IV infusion should be reassessed as soon as the patient's basic cardiac rhythm appears stable or at the earliest signs of toxicity.

Uses: For the acute management of ventricular arrhythmias occurring during cardiac manipulations, such as cardiac surgery; and for life-threatening arrhythmias which are ventricular in origin, such as those that occur during acute myocardial infarction

The American Heart Association (AHA) recommends:
IV:
-Initial dose: 1 to 1.5 mg/kg IV bolus once; may repeat if necessary at a dose of 0.5 to 0.75 mg/kg IV every 5 to 10 minutes up to a maximum cumulative dose of 3 mg/kg
-Following bolus administration: 1 to 4 mg/min continuous IV infusion (30 to 50 mcg/kg/min)

Endotracheal: May be administered endotracheally (bolus dose only) if IV access unavailable at a dose of 2 to 2.5 times the IV dose diluted in 5 to 10 mL NS or distilled water

Uses: For the treatment of ventricular fibrillation (VF) or pulseless ventricular tachycardia (pVT) unresponsive to CPR, defibrillation, and vasopressor therapy as an alternative to amiodarone

3 years or older with normal lean body mass and normal body development: Maximum dose based on patient's age and weight

Comments:
-The manufacturer product information should be consulted.
-Dose varies with procedure, depth of anesthesia and degree of muscle relaxation needed, duration of anesthesia required, and physical condition of patient.
-In all cases the lowest effective dose that will produce the desired result should be used.

Use: For the production of local or regional anesthesia by infiltration techniques such as percutaneous injection and IV 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, when the accepted procedures for these techniques as described in standard textbooks are observed

Use with caution; renal dysfunction may increase the accumulation of metabolites, leading to toxicity.

• Higher dosages or volumes of lidocaine will result in a shorter time to the onset of anesthesia, a longer duration of effect, a greater degree of muscle relaxation, and an increase in the spread of the anesthesia.
• The duration of action of lidocaine may be prolonged in people with liver disease.

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