Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/2929
| Predicate | Object |
|---|---|
| rdf:type | |
| rdfs:label |
Lidocaine Hydrochloride (Injection, Solution)
|
| dailymed-instance:dosage |
Adults: Single Direct Intravenous Injection (bolus): ONLY
THE 5 mL, 50 MG or 100 MG DOSAGE SIZES should be used for direct intravenous
injection. The usual dose is 50 to 100 mg of lidocaine hydrochloride (0.70
to 1.4 mg/kg; 0.32 to 0.63 mg/lb) administered intravenously under ECG monitoring.
This dose may be administered at the rate of approximately 25 to 50 mg/min
(0.35 to 0.70 mg/kg/min; 0.16 to 0.32 mg/lb/min). Sufficient time should be
allowed to enable a slow circulation to carry the drug to the site of action.
If the initial injection of 50 to 100 mg does not produce a desired response,
a second dose may be injected after five minutes. NO MORE THAN 200 TO 300
MG OF LIDOCAINE HYDROCHLORIDE SHOULD BE ADMINISTERED DURING A ONE HOUR PERIOD. Continuous Intravenous Infusion: Following bolus
administration, intravenous infusions of lidocaine hydrochloride may be initiated
at the rate of 1 to 4 mg/min of lidocaine hydrochloride (0.014 to 0.057 mg/kg/min;
0.006 to 0.026 mg/lb/min). The rate of intravenous infusions should be reassessed
as soon as the patient's basic cardiac rhythm appears to be stable
or at the earliest signs of toxicity. It should rarely be necessary to continue
intravenous infusions of lidocaine for prolonged periods. Solutions for intravenous infusion may be prepared by the addition of
one gram (or two grams) of lidocaine hydrochloride to one liter of 5% dextrose
in water using aseptic technique. Approximately a 0.1% (or 0.2%) solution
will result from this procedure; that is, each milliliter will contain approximately
1 mg (or 2 mg) of lidocaine hydrochloride. In those cases in which fluid restriction
is medically appropriate, a more concentrated solution may be prepared. Lidocaine Hydrochloride Injection, USP has been found to be chemically
stable for 24 hours after dilution in 5% dextrose in water. However, as with
all intravenous admixtures, dilution of the solution should be made just prior
to its administration. When administering lidocaine
hydrochloride (or any potent medication) by continuous intravenous infusion,
it is advisable to use a precision volume control I.V. set. Pediatric: Controlled clinical studies in the pediatric
population to establish dosing schedules have not been conducted. The American
Heart Association's Standards and Guidelines recommends a bolus dose of 1 mg/kg, and an infusion rate of between
20-50��g/kg/min for prolonged therapy. When drug clearance is reduced,
as in patients with shock, congestive heart failure or cardiac arrest, the
infusion rate should not exceed 20��g/kg/min. NOTE: Regarding Prolonged Infusions: There are
data that indicate the half-life may be 3 hours or longer following infusions
of greater than 24 hours in duration. Do not use if solution is discolored
or cloudy. Parenteral drug products should be
inspected visually for particulate matter and discoloration prior to administration
whenever solution and container permit. To prevent
needle-stick injuries, needles should not be recapped, purposely bent or broken
by hand.
|
| dailymed-instance:descripti... |
Lidocaine Hydrochloride Injection, USP is a sterile, nonpyrogenic
solution of an antiarrhythmic agent administered intravenously by either direct
injection or continuous infusion. It is available in various concentrations
with the following characteristics: *1000 mg and 2000 mg concentrations FOR DILUTION ONLY. Must not be administered without proper dilution prior to
injection. May contain sodium hydroxide
and/or hydrochloric acid for pH adjustment. Injections containing 10 mg/mL
(1%) contain sodium chloride 7 mg and injections containing 20 mg/mL (2%)
lidocaine hydrochloride contain sodium chloride 6 mg to adjust tonicity. Single-dose
solutions contain no preservative and unused portions must be discarded after
use. Lidocaine Hydrochloride, USP is chemically designated
2-(Diethylamino)-2',6'-acetoxylidide monohydrochloride monohydrate,
a white powder freely soluble in water. The molecular formula is CHNO���HCl���HO. The molecular weight is 288.82. It has
the following structural formula: The semi-rigid vial used for the plastic vials is fabricated from a specially
formulated polyolefin. It is a copolymer of ethylene and propylene. The safety
of the plastic has been confirmed by tests in animals according to USP biological
standards for plastic containers. The container requires no vapor barrierto maintain the proper drug concentration. The
plastic syringe is molded from a specially formulated polypropylene. Water
permeates from inside the container at an extremely slow rate which will have
an insignificant effect on solution concentration over the expected shelf
life. Solutions in contact with the plastic container may leach out certain
chemical components from the plastic in very small amounts; however, biological
testing was supportiveof the safety of the syringe material.
|
| dailymed-instance:clinicalP... |
Mechanism of Action and Electrophysiology: Studies of the effects of therapeutic concentrations
of lidocaine on the electrophysiological properties of mammalian Purkinje
fibers have shown that lidocaine attenuates phase 4 diastolic depolarization,
decreases automaticity and causes a decrease or no change in excitability
and membrane responsiveness. Action potential duration and effective refractory
period of Purkinje fibers are decreased while the ratio of effective refractory
period to action potential duration is increased. Action potential duration
and effective refractory period of ventricular muscle are also decreased.
Effective refractory period of the AV node may increase, decrease or remain
unchanged and atrial effective refractory period is unchanged. Lidocaine raises
the ventricular fibrillation threshold. No significant interactions between
lidocaine and the autonomic nervous system have been described and consequently
lidocaine has little or no effect on autonomic tone. Clinical electrophysiological studies with lidocaine have demonstrated
no change in sinus node recovery time or sinoatrial conduction time. AV nodal
conduction time is unchanged or shortened and His-Purkinje conduction time
is unchanged. Hemodynamics: At therapeutic doses, lidocaine has minimal
hemodynamic effects in normal subjects and in patients with heart disease.
Lidocaine has been shown to cause no, or minimal decrease in ventricular contractility,
cardiac output, arterial pressure or heart rate. Pharmacokinetics and Metabolism: Lidocaine
is rapidly metabolized by the liver and less than 10% of a dose is excreted
unchanged in the urine. Oxidative N-dealkylation, a major pathway of metabolism,
results in the metabolites monoethylglycinexylidide and glycinexylidide. The
pharmacological/toxicological activities of these metabolites are similar
to but less potent than lidocaine. 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. There are data that indicate that the half-life may be 3 hours
or longer following infusions of greater than 24 hours. Because of the rapid rate at which lidocaine is metabolized, any condition
that alters liver function, including changes in liver blood flow, which could
result from severe congestive heart failure or shock may alter lidocaine kinetics.
The half-life may be two-fold or more greater in patients with liver dysfunction.
Renal dysfunction does not affect lidocaine kinetics, but may increase the
accumulation of metabolites. Therapeutic effects
of lidocaine are generally associated with plasma levels of 6 to 25��mole/L
(1.5 to 6��g free base per mL). The blood to plasma distribution ratio
is approximately 0.84. Objective adverse manifestations become increasingly
apparent with increasing plasma levels above 6��g free base per mL. The plasma protein binding of lidocaine is dependent on drug concentration
and the fraction bound decreases with increasing concentration. At concentrations
of 1 to 4��g free base per mL, 60 to 80 percent of lidocaine is protein
bound. In addition to lidocaine concentration, the binding is dependent on
the plasma concentration of the��-1-acid glycoprotein. Lidocaine readily crosses the placental and blood-brain barriers. Dialysis
has negligible effects on the kinetics of lidocaine.
|
| dailymed-instance:activeIng... | |
| dailymed-instance:contraind... |
Lidocaine hydrochloride is contraindicated in patients with
a known history of hypersensitivity to local anesthetics of the amide type.
Lidocaine hydrochloride should not be used in patients with Stokes-Adams syndrome,
Wolff-Parkinson-White syndrome or with severe degrees of sinoatrial, atrioventricular
or intraventricular block in the absence of an artificial pacemaker.
|
| dailymed-instance:supply |
Lidocaine Hydrochloride Injection, USP is supplied as follows: For preparing solutions for intravenous infusion: **Abboject Unit of Use Syringe with Male
Luer Lock Adapter and protected needle. Store at controlled
room temperature 15��to 30��C (59��to 86��F) [See USP.] ��Hospira 2004
EN-0118 Printed in USA HOSPIRA,
INC., LAKE FOREST, IL 60045 USA Abboject is
a trademark of the Abbott group of companies.
|
| dailymed-instance:activeMoi... | |
| dailymed-instance:inactiveI... | |
| dailymed-instance:precautio... |
1. General:: Caution should be employed in the use of lidocaine hydrochloride
in patients with severe liver or kidney disease because accumulation of the
drug or metabolites may occur. Lidocaine Hydrochloride
Injection, USP should be used with caution in the treatment of patients with
hypovolemia, severe congestive heart failure, shock and all forms of heart
block. In patients with sinus bradycardia or incomplete heart block, the administration
of lidocaine hydrochloride intravenously for the elimination of ventricular
ectopic beats without prior acceleration in heart rate (e.g., by atropine,
isoproterenol or electric pacing) may promote more frequent and serious ventricular
arrhythmias or complete heart block. (See CONTRAINDICATIONS). Dosage should be reduced for pediatric patients and for debilitated
and/or elderly patients, commensurate with their age and physical status. The safety of amide local anesthetic agents in patients with genetic
predisposition of malignant hyperthermia has not been fully assessed; therefore,
lidocaine should be used with caution in such patients. In hospital environments where drugs known to be triggering agents for
malignant hyperthermia (fulminant hypermetabolism) are administered, it is
suggested that a standard protocol for management should be available. It is not known whether lidocaine may trigger this reaction; however,
large doses resulting in significant plasma concentrations, as may be achievedby intravenous infusion, pose potential risk to these individuals. Recognition
of 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 triggering agent
and institution of treatment including oxygen therapy, supportive measures
and dantrolene (for details see dantrolene package insert).<br/>2. Patient Information:: The patient should be advised of the possible occurrence
of the experiences listed under ADVERSE REACTIONS.<br/>3. Laboratory Tests:: None known.<br/>4. Drug Interactions:: Lidocaine Hydrochloride Injection, USP should be used with
caution in patients with digitalis toxicity accompanied by atrioventricular
block. Concomitant use of beta-blocking agents or cimetidine may reduce hepatic
blood flow and thereby reduce lidocaine clearance. The concomitant use of
these two agents may cause an increased incidence of adverse reactions, including
central nervous system adverse reactions such as seizure. Lidocaine and tocainide are pharmacodynamically similar.<br/>5. Carcinogenesis, Mutagenesis, Impairment of Fertility:: Long term studies in animals to evaluate the carcinogenic
and mutagenic potential or the effect on fertility of lidocaine HCl have not
been conducted.<br/>6. Pregnancy::<br/>Teratogenic Effects::<br/>7. Labor and Delivery:: The effects of lidocaine HCl on the mother and the fetus,
when used in the management of cardiac arrhythmias during labor and delivery
are not known. Lidocaine readily crosses the placental barrier.<br/>8. Nursing Mothers:: 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 is administered to a nursing woman.<br/>9. Pediatric Use:: Controlled clinical studies have not been conducted in the
pediatric population to establish safety and efficacy in this population (see
DOSAGE AND ADMINISTRATION).
|
| dailymed-instance:overdosag... |
Overdosage of lidocaine HCl usually results in signs of central
nervous system or cardiovascular toxicity. See ADVERSE REACTIONS. Should convulsions or signs of respiratory depression and arrest develop,
the patency of the airway and adequacy of ventilation must be assured immediately.
Should convulsions persist despite ventilatory therapy with oxygen, small
increments of anticonvulsive agents may be given intravenously. Examples of
such agents include a benzodiazepine (e.g., diazepam), an ultrashort-acting
barbiturate (e.g., thiopental or thiamylal) or a short-acting barbiturate
(e.g., pentobarbital or secobarbital). If the patient is under general anesthesia,
a short-acting muscle relaxant (e.g., succinylcholine) may be administered. Should circulatory depression occur, vasopressors may be used. Should
cardiac arrest occur, standard CPR procedures should be instituted. Dialysis is of negligible value in the treatment of acute overdosage from
lidocaine HCl.
|
| dailymed-instance:genericMe... |
Lidocaine Hydrochloride
|
| dailymed-instance:fullName |
Lidocaine Hydrochloride (Injection, Solution)
|
| dailymed-instance:adverseRe... |
Adverse experiences following the administration of lidocaine
are similar in nature to those observed with other amide local anesthetic
agents. Adverse experiences may result from high plasma levels caused by excessive
dosage or may result from a hypersensitivity, idiosyncrasy or diminished tolerance
on the part of the patient. Serious adverse experiences are generally systemic
in nature. The following types are those most commonly reported. The adverse
experiences under Central Nervous System and Cardiovascular System are listed,
in general, in a progression from mild to severe.
|
| dailymed-instance:warning |
IN ORDER TO MANAGE POSSIBLE ADVERSE REACTIONS, RESUSCITATIVE
EQUIPMENT, OXYGEN AND OTHER RESUSCITATIVE DRUGS SHOULD BE IMMEDIATELY AVAILABLE
WHEN LIDOCAINE HYDROCHLORIDE INJECTION IS USED. THE 10% AND 20% CONCENTRATED SOLUTIONS MUST NOT BE INJECTED UNDILUTED.
See DOSAGE AND ADMINISTRATION. Systemic toxicity
may result in manifestations of central nervous system depression (sedation)
or irritability (twitching), which may progress to frank convulsions accompanied
by respiratory depression and/or arrest. Early recognition of premonitory
signs, assurance of adequate oxygenation and, where necessary, establishment
of artificial airwaywith ventilatory support are essential to management
of this problem. Should convulsions persist despite ventilatory therapy with
oxygen, small increments of anticonvulsant
drugs may be used intravenously. Examples of such agents include benzodiazepines
(e.g., diazepam), ultrashort-acting barbiturates (e.g., thiopental or thiamylal)
or a short-acting barbiturate (e.g., pentobarbital or secobarbital). If the
patient is under anesthesia, a short-acting muscle relaxant (e.g., succinylcholine)
may be used. Longer acting drugs should be used only when recurrent convulsions
are evidenced. Should circulatory depression
occur, vasopressors may be used. Constant electrocardiographic
monitoring is essential to the proper administration of lidocaine hydrochloride.
Signs of excessive depression of cardiac electrical activity such as sinus
node dysfunction, prolongation of the P-R interval and QRS complex or the
appearance or aggravation of arrhythmias, should befollowed by flow adjustment
and, if necessary, prompt cessation of the intravenous infusion of this agent.
Occasionally, acceleration of ventricular rate may occur when lidocaine hydrochloride
is administered to patients with atrial flutter or fibrillation.
|
| dailymed-instance:indicatio... |
Lidocaine hydrochloride injection administered intravenously
or intramuscularly, is specifically indicated in the acute management of ventricular
arrhythmias such as those occurring in relation to acute myocardial infarction,
or during cardiac manipulation, such as cardiac surgery.
|
| dailymed-instance:represent... | |
| dailymed-instance:routeOfAd... | |
| dailymed-instance:name |
Lidocaine Hydrochloride
|