DailyMed Label: Lidocaine

DailyMed Label: Lidocaine

2022

DailyMed Prescription

Lidocaine

LIDOCAINE HYDROCHLORIDE

Fresenius Kabi USA, LLC

NDC: 63323-201

NDC: 63323-202

NDC: 63323-201

NDC: 63323-201

NDC: 63323-202

NDC: 63323-202

Lidocaine Hydrochloride Injection, USP is a local anesthetic which is a sterile, nonpyrogenic solution intended for parenteral injection.  See INDICATIONS AND USAGE   for specific uses. Lidocaine hydrochloride is chemically designated as 2-(Diethylamino)-2’, 6’-acetoxylidide monohydrochloride and has the following structural formula: C 14 H 22 N 2 O • HCl                              M.W. 288.82 Each mL contains: Lidocaine hydrochloride 10 or 20 mg; methylparaben 0.1%; sodium chloride (7 mg and 6 mg of sodium chloride for 1% and 2% respectively) to render it isotonic; Water for Injection q.s.  Hydrochloric acid and/or sodium hydroxide may have been added for pH adjustment (5.0 to 7.0). structure

Lidocaine Hydrochloride Injection, USP is indicated for the production of local anesthesia, by infiltration techniques, such as percutaneous injection, and by peripheral nerve block techniques, such as brachial plexus and inter-costal, when the accepted procedures for these techniques as described in standard textbooks are observed.

Table 1 (Recommended Dosages) summarizes the recommended volumes and concentrations of lidocaine hydrochloride injection for various types of anesthetic procedures.  The dosages suggested in this table are for normal healthy adults and refer to the use of epinephrine-free solutions.  When larger volumes are required, only solutions containing epinephrine should be used, except in those cases where vasopressor drugs may be contraindicated. There have been adverse event reports of chondrolysis in patients receiving intra-articular infusions of local anesthetics following arthroscopic and other surgical procedures.  Lidocaine is not approved for this use (see WARNINGS   and DOSAGE AND ADMINISTRATION ). These recommended doses serve only as a guide to the amount of anesthetic required for most routine procedures.  The actual volumes and concentrations to be used depend on a number of factors such as type and extent of surgical procedure, depth of anesthesia and degree of muscular relaxation required, duration of anesthesia required and the physical condition of the patient.  In all cases the lowest concentration and smallest dose that will produce the desired result should be given.  Dosages should be reduced for children and for elderly and debilitated patients and patients with cardiac and/or liver disease. The onset of anesthesia, the duration of anesthesia and the degree of muscular relaxation are proportional to the volume and concentration (i.e. total dose) of local anesthetic used.  Thus, an increase in volume and concentration of lidocaine hydrochloride injection will decrease the onset of anesthesia, prolong the duration of anesthesia, provide a greater degree of muscular relaxation and increase the segmental spread of anesthesia.  However, increasing the volume and concentration of lidocaine hydrochloride injection may result in a more profound fall in blood pressure when used in epidural anesthesia.  Although the incidence of side effects with lidocaine is quite low, caution should be exercised when employing large volumes and concentrations, since the incidence of side effects is directly proportional to the total dose of local anesthetic agent injected.

Lidocaine HCl is contraindicated in patients with a known history of hypersensitivity to local anesthetics of the amide type.

The safety and effectiveness of lidocaine HCl depend on proper dosage, correct technique, adequate precautions, and readiness for emergencies.  Standard textbooks should be consulted for specific techniques and precautions for various regional anesthetic procedures. Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use (see WARNINGS   and ADVERSE REACTIONS ).  The lowest dosage that results in effective anesthesia should be used to avoid high plasma levels and serious adverse effects.  Syringe aspirations should also be performed before and during each supplemental injection when using indwelling catheter techniques.  An intravascular injection is still possible even if aspirations for blood are negative.  Repeated doses of lidocaine HCl may cause significant increases in blood levels with each repeated dose, because of slow accumulation of the drug or its metabolites.  Tolerance to elevated blood levels varies with the status of the patient.  Debilitated, elderly patients, acutely ill patients, and children should be given reduced doses commensurate with their age and physical condition.  Lidocaine HCl should also be used with caution in patients with severe shock or heart block. Careful and constant monitoring of cardiovascular and respiratory (adequacy of ventilation) vital signs and the patient’s state of consciousness should be accomplished after each local anesthetic injection.  It should be kept in mind at such times that restlessness, anxiety, tinnitus, dizziness, blurred vision, tremors, depression or drowsiness may be early warning signs of central nervous system toxicity. Since amide-type local anesthetics are metabolized by the liver, lidocaine HCl should be used with caution in patients with hepatic disease.  Patients with severe hepatic disease, because of their inability to metabolize local anesthetic normally, are at greater risk of developing toxic plasma concentrations.  Lidocaine HCl should also be used with caution in patients with impaired cardiovascular function since they may be less able to compensate for functional changes associated with the prolongation of A-V conduction produced by these drugs. Many drugs used during the conduct of anesthesia are considered potential triggering agents for familial malignant hyperthermia.  Since it is not known whether amide-type local anesthetics may trigger this reaction and since the need for supplemental general anesthesia cannot be predicted in advance, it is suggested that a standard protocol for the management of malignant hyperthermia should be available.  Early unexplained signs of tachycardia, tachypnea, labile blood pressure and metabolic acidosis may precede temperature elevation.  Successful outcome is dependent on early diagnosis, prompt discontinuance of the suspect triggering agent(s) and institution of treatment, including oxygen therapy, indicated supportive measures and dantrolene (consult dantrolene sodium intravenous package insert before using). Lidocaine HCl should be used with caution in persons with known drug sensitivities.  Patients allergic to para-aminobenzoic acid derivatives (procaine, tetracaine, benzocaine, etc.) have not shown cross-sensitivity to lidocaine HCl. Small doses of local anesthetics injected into the head and neck area, including retrobulbar, dental and stellate ganglion blocks, may produce adverse reactions similar to systemic toxicity seen with unintentional intravascular injections of larger doses.  Confusion, convulsions, respiratory depression and/or respiratory arrest, and cardiovascular stimulation or depression have been reported.  These reactions may be due to intra-arterial injection of the local anesthetic with retrograde flow to the cerebral circulation.  Patients receiving these blocks should have their circulation and respiration monitored and be constantly observed.  Resuscitative equipment and personnel for treating adverse reactions should be immediately available.  Dosage recommendations should not be exceeded (see DOSAGE AND ADMINISTRATION ). Concurrent administration of vasopressor drugs (for the treatment of hypotension related to obstetric blocks) and ergot-type oxytocic drugs may cause severe, persistent hypertension or cerebrovascular accidents. The intramuscular injection of lidocaine HCl may result in an increase in creatine phosphokinase levels.  Thus, the use of this enzyme determination, without isoenzyme separation, as a diagnostic test for the presence of acute myocardial infarction may be compromised by the intramuscular injection of lidocaine HCl. Studies of lidocaine HCl in animals to evaluate the carcinogenic and mutagenic potential or the effect on fertility have not been conducted. Teratogenic Effects: Pregnancy Category B Reproduction studies have been performed in rats at doses up to 6.6 times the human dose and have revealed no evidence of harm to the fetus caused by lidocaine HCl.  There are, however, no adequate and well-controlled studies in pregnant women.  Animal reproduction studies are not always predictive of human response.  General consideration should be given to this fact before administering lidocaine HCl to women of childbearing potential, especially during early pregnancy when maximum organogenesis takes place. Local anesthetics rapidly cross the placenta and when used for epidural, paracervical, pudenal, or caudal block anesthesia, can cause varying degrees of maternal, fetal and neonatal toxicity (see CLINICAL PHARMACOLOGY-Pharmacokinetics and Metabolism ).  The potential for toxicity depends upon the procedure performed, the type and amount of drug used, and the technique of drug administration.  Adverse reactions in the parturient, fetus and neonate involve alterations of the central nervous system, peripheral vascular tone and cardiac function. Local anesthetics produce vasodilation by blocking sympathetic nerves. Elevating the patient’s legs and positioning her on her left side will help prevent decreases in blood pressure.  The fetal heart rate also should be monitored continuously, and electronic fetal monitoring is highly advisable. Paracervical or pudendal anesthesia may alter the forces of parturition through changes in uterine contractility or maternal expulsive efforts.  In one study paracervical block anesthesia was associated with a decrease in the mean duration of first stage labor and facilitation of cervical dilation.  The use of obstetrical anesthesia may increase the need for forceps assistance. The use of some local anesthetic drug products during labor and delivery may be followed by diminished muscle strength and tone for the first day or two of life.  The long-term significance of these observations is unknown.  Fetal bradycardia may occur in 20 to 30% of patients receiving paracervical nerve block anesthesia with the amide-type local anesthetics and may be associated with fetal acidosis.  Fetal heart rate should always be monitored during paracervical anesthesia.  The physician should weigh the possible advantages against risks when considering a paracervical block in prematurity, toxemia of pregnancy, and fetal distress.  Careful adherence to recommended dosage is of the utmost importance in obstetrical paracervical block.  Failure to achieve adequate analgesia with recommended doses should arouse suspicion of intravascular or fetal intracranial injection.  Cases compatible with unintended fetal intracranial injection of local anesthetic solution have been reported following intended paracervical or pudendal block or both.  Babies so affected present with unexplained neonatal depression at birth, which correlates with high local anesthetic serum levels, and often manifest seizures within six hours.  Prompt use of supportive measures combined with forced urinary excretion of the local anesthetic has been used successfully to manage this complication. Case reports of maternal convulsions and cardiovascular collapse following use of some local anesthetics for paracervical block in early pregnancy (as anesthesia for elective abortion) suggest that systemic absorption under these circumstances may be rapid.  The recommended maximum dose of each drug should not be exceeded.  Injection should be made slowly and with frequent aspiration.  Allow a 5-minute interval between sides. It is not known whether this drug is excreted in human milk.  Because many drugs are excreted in human milk, caution should be exercised when lidocaine HCl is administered to a nursing woman. Dosages in children should be reduced, commensurate with age, body weight and physical condition (see DOSAGE AND ADMINISTRATION ).

Lidocaine Hydrochloride Injection is preserved with 0.1% methylparaben and is available in the following concentrations: Product Code Unit of Sale Strength Each 920102 NDC 63323-201-02 Unit of 25 1% 20 mg per 2 mL (10 mg per mL) NDC 63323-201-01 2 mL Vial 20110 NDC 63323-201-10 Unit of 25 1% 100 mg per 10 mL (10 mg per mL) NDC 63323-201-03 10 mL Multiple Dose Vial 20202 NDC 63323-202-02 Unit of 25 2% 40 mg per 2 mL (20 mg per mL) NDC 63323-202-01 2 mL Vial Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from light.

Lidocaine HCl stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action. 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.  The net effect is normally a modest hypotension when the recommended dosages are not exceeded. Information derived from diverse formulations, concentrations and usages reveals that lidocaine HCl 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 HCl is dependent on drug concentration, and the fraction bound decreases with increasing concentration.  At concentrations of 1 to 4 mcg of free base/mL, 60 to 80% of lidocaine HCl is protein bound.  Binding is also dependent on the plasma concentration of the alpha-1-acid glycoprotein. Lidocaine HCl crosses the blood-brain and placental barriers, presumably by passive diffusion. Lidocaine HCl 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 HCl.  Approximately 90% of lidocaine HCl 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 HCl following an intravenous bolus injection is typically 1.5 to 2 hours.  Because of the rapid rate at which lidocaine HCl 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 HCl 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 HCl required to produce overt systemic effects.  Objective adverse manifestations become increasingly apparent with increasing venous plasma levels above 6 mcg free base/mL.  In the rhesus monkey arterial blood levels of 18 to 21 mcg/mL have been shown to be threshold for convulsive activity.

PACKAGE LABEL - PRINCIPAL DISPLAY – Lidocaine 10 mL Multiple Dose Vial Label NDC 63323-201-03         20110 LIDOCAINE HCl INJECTION, USP 1% 100 mg per 10 mL (10 mg per mL) FOR INFILTRATION AND NERVE BLOCK. NOT FOR EPIDURAL OR CAUDAL USE. 10 mL Multiple Dose Vial          Rx only PACKAGE LABEL - PRINCIPAL DISPLAY – Lidocaine 10 mL Multiple Dose Vial Label