Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/2108
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Lidocaine Hydrochloride (Injection, Solution)
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dailymed-instance:dosage |
When 4% Lidocaine Hydrochloride Injection, USP is
used concomitantly with other products containing lidocaine, the total
dose contributed by all formulations must be kept in mind. The dosage varies and depends upon the area to be anesthetized,
vascularity of the tissues, individual tolerance and the technique
of anesthesia. The lowest dosage needed to provide effective anesthesia
should be administered. Dosages should be reduced for children and
for elderly and debilitated patients. Although
the incidence of adverse effects with 4% Lidocaine Hydrochloride Injection,
USP is quite low, caution should be exercised, particularly when employing
large volumes and concentrations of lidocaine since the incidence
of adverse effects is directly proportional to the total dose of local
anesthetic agent administered. For specific techniques and procedures
refer to standard textbooks. The dosages below
are for normal, healthy adults. RETROBULBAR
INJECTION: The suggested dose for a 70 kg person is 3���5 mL
(120���200 mg of lidocaine HCl), i.e., 1.7���3 mg/kg or
0.9���1.5 mg/lb body weight. A portion of this is injected retrobulbarly
and the rest may be used to block the facial nerve. TRANSTRACHEAL INJECTION: For local anesthesia by the transtracheal
route 2���3 mL should be injected through a large enough needle
so that the injection can be made rapidly. By injecting during inspiration
some of the drug will be carried into the bronchi and the resulting
cough will distribute the rest of the drug over the vocal cords and
the epiglottis. Occasionally it may be necessary
to spray the pharynx by oropharyngeal spray to achieve complete analgesia.
For the combination of the injection and spray, it should rarely be
necessary to utilize more than 5 mL (200 mg of lidocaine HCl), i.e.,
3 mg/kg or 1.5 mg/lb body weight. TOPICAL APPLICATION:
For laryngoscopy, bronchoscopy and endotracheal intubation, the pharynx
may be sprayed with 1���5 mL (40���200 mg of lidocaine HCl),
i.e., 0.6���3 mg/kg or 0.3-1.5 mg/lb body weight. Maximum Recommended Dosages Normal Healthy Adults: The maximum recommended
dose of 4% Lidocaine Hydrochloride Injection, USP should be such that
the dose of lidocaine HCl is kept below 300 mg and in any case should
not exceed 4.5 mg/kg (2 mg/lb) body weight. Children: It is difficult to
recommend a maximum dose of any drug for children since this varies
as a function of age and weight. For children of less than ten years
who have a normal lean body mass and normal body development, the
maximum dose may be determined by the application of one of the standard
pediatric drug formulas (e.g., Clark's rule). For example,
in a child of five years weighing 50 lbs, the dose of lidocaine hydrochloride
should not exceed 75���100 mg when calculated according to Clark's
rule. In any case, the maximum dose of lidocaine hydrochloride and
epinephrine injection should not exceed 7 mg/kg (3.2 mg/lb) of body
weight. When used without epinephrine, the amount of lidocaine administered
should be such that the dose is kept below 300mg and in any
case should not exceed 4.5 mg/kg (2 mg/lb) of body weight. NOTE: Parenteral drug products should be inspected visually
for particulate matter and discoloration prior to administration whenever
the solution and container permit. Solutions that are discolored and/or
contain particulate matter should not be used. Do not use unless solution
is clear and container undamaged.
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dailymed-instance:descripti... |
4% Lidocaine Hydrochloride Injection, USP is a sterile,
nonpyrogenic solution containing lidocaine hydrochloride, anhydrous
40 mg/mL in water for injection. May contain sodium hydroxide and/or
hydrochloric acid for pH adjustment. pH 6.5 (5.0 to 7.0). Lidocaine has cardiac antiarrhythmic properties and is
a local anesthetic of the amide type. Lidocaine
Hydrochloride, USP is chemically designated 2-(diethylamino)-2���,6���-acetoxylidide
monohydrochloride monohydrate, a white powder freely soluble in water.
It has the following structural formula:
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dailymed-instance:clinicalP... |
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. Onset and duration of anesthesia: The onset
of action is rapid. For retrobulbar injection, 4 mL of 4% Lidocaine
Hydrochloride Injection, USP provides an average duration of action
of 1 to 1��hours. This duration may be extended for ophthalmic
surgery by the addition of epinephrine, the usual recommended dilution
being 1:50,000 to 1:100,000. Hemodynamics: Excessive blood levels may
cause changes in cardiac output, total peripheral resistance, and
mean arterial pressure. These changes may be attributable to 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. Pharmacokinetics and metabolism: Information derived from other formulations, concentrations and
usages reveals that lidocaine is completely absorbed following parenteral
administration, its rate of absorption depending, for example, upon
such factors such as the site of administration and the presence or
absence of a vasoconstrictor agent. Lidocaine may be absorbed following
topical administration to mucous membranes, its rate and extent of
absorption depending upon concentration and total dose administered,
the specific site of application and duration of exposure. In general,
the rate of absorption of local anesthetic agents following topical
application occurs most rapidly after intratracheal administration.
Lidocaine is also well absorbed from the gastrointestinal tract, but
intact drug appears in the circulation because of biotransformation
by the liver. 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. Studies have shown that peak blood levels of lidocaine
may occur as early as 5 and as late as 30 minutes after endotracheal
administration of a 4% lidocaine HCl injection. The plasma binding of lidocaine is dependent on drug concentration,
and the fraction bound decreases with increasing concentration. At
concentrations of 1 to 4��g 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. Studies of lidocaine metabolism
following intravenous bolus injections have shown that the elimination
half-life of this agent 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��g free base per mL.
In the rhesus monkey arterial blood levels of 18���21��g/mL
have been shown to be threshold for convulsive activity.
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Lidocaine is contraindicated in patients with a known
history of hypersensitivity to local anesthetics of the amide type.
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dailymed-instance:supply |
4% Lidocaine Hydrochloride Injection, USP (40 mg/mL)
is supplied as a single-dose 5 mL ampul (NDC No. 0409-4283-01) in
packages of 25. Store at 20 to 25��C (68
to 77��F). [See USP Controlled Room Temperature.] Revised: May, 2007
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dailymed-instance:precautio... |
General:: The safety and effectiveness of lidocaine depend
on proper dosage, correct technique, adequate precautions, and readiness
for emergencies. 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.
Repeated doses of lidocaine 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 status. Lidocaine should also be used
with caution in patients with severe shock or heart block. Local anesthetic solutions containing a vasoconstrictor
should be used cautiously and in carefully circumscribed quantities
in areas of the body supplied by end arteries or having otherwise
compromised blood supply. Patients with peripheral vascular disease
and those with hypertensive vascular disease may exhibit exaggerated
vasoconstrictor response. Ischemic injury or necrosis may result.
Preparations containing a vasoconstrictor should be used with caution
in patients during or following the administration of potent general
anesthetic agents, since cardiac arrhythmias may occur under such
conditions. 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 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 a greater risk of
developing toxic plasma concentrations. Lidocaine 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. Use in Ophthalmic Surgery: When local anesthetic solutions are employed for retrobulbar block,
lack of corneal sensation should not be relied upon to determine whether
or not the patient is ready for surgery since corneal sensation usually
precedes clinically acceptable external ocular muscle akinesia. 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 management 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 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. Use in the Head and Neck Area: 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.)<br/>Information for Patients:: When topical anesthetics are used in the mouth, the
patient should be aware that the production of topical anesthesia
may impair swallowing and thus enhance the danger of aspiration. For
this reason, food should not be ingested for 60 minutes following
use of local anesthetic preparations in the mouth or throat area.
This is particularly important in children because of their frequency
of eating. Numbness of the tongue or buccal
mucosa may enhance the danger of unintentional biting trauma. Food
and chewing gums should not be taken while the mouth or throat area
is anesthetized.<br/>Clinically significant drug
interactions:: The administration of local anesthetic solutions
containing epinephrine or nor-epinephrine to patients receiving monoamine
oxidase inhibitors, tricyclic antidepressants or phenothiazines may
produce severe, prolonged hypotension or hypertension. Concurrent
use of these agents should generally be avoided. In situations when
concurrent therapy is necessary, careful patient monitoring is essential.<br/>Drug/Laboratory test interactions:: The intramuscular injection of lidocaine 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 myocardiac infarction may be compromised
by the intramuscular injection of lidocaine.<br/>Carcinogenesis, mutagenesis,
impairment of fertility:: Studies of lidocaine in animals to evaluate the carcinogenic
and mutagenic potential or the effect on fertility have not been conducted.<br/>Use in Pregnancy:: 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. 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 to women of childbearing potential,
especially during early pregnancy when maximum organogenesis takes
place.<br/>Labor and delivery:: Lidocaine is not contraindicated in labor and delivery.
Should 4% Lidocaine Hydrochloride Injection, USP be used concomitantly
with other products containing lidocaine, the total dose contributed
by all formulations must be kept in mind.<br/>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/>Pediatric use:: Dosages in children should be reduced, commensurate
with age and body weight. (See DOSAGE AND ADMINISTRATION.)
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dailymed-instance:overdosag... |
Acute emergencies from local anesthetics are generally
related to high plasma levels encountered during therapeutic use of
local anesthetics or to unintended subarachnoid injection of local
anesthetic solution (see ADVERSE REACTIONS, WARNINGS and PRECAUTIONS). Management of local anesthetic
emergencies: The first consideration is prevention, best
accomplished by careful and constant monitoring of cardiovascular
and respiratory vital signs and the patient's state of consciousness
after each local anesthetic injection. At the first sign of change,
oxygen should be administered. The first step
in the management of convulsions consists of immediate attention to
the maintenance of a patent airway and assisted or controlled ventilation
with oxygen and a delivery system capable of permitting immediate
positive airway pressure by mask. Immediately after the institution
of these ventilatory measures, the adequacy of the circulation should
be evaluated, keeping in mind that drugs used to treat convulsions
sometimes depress the circulation when administered intravenously.
Should convulsions persist despite adequate respiratory support, and
if the status of the circulation permits, small increments of an ultra-short
acting barbiturate (such as thiopental or thiamylal) or a benzodiazepine
(such as diazepam) may be administered intravenously. The clinician
should be familiar, prior to use of local anesthetics, with these
anticonvulsant drugs. Supportive treatment of circulatory depression
may require administration of intravenous fluids and, when appropriate,a vasopressor as directed by the clinical situation (e.g., ephedrine). If not treated immediately, both convulsions and cardiovascular
depression can result in hypoxia, acidosis, bradycardia, arrhythmias
and cardiac arrest. If cardiac arrest should occur, standard cardiopulmonary
resuscitative measures should be instituted. Endotracheal intubation, employing drugs and techniques familiar
to the clinician, may be indicated, after initial administration of
oxygen by mask, if difficulty is encountered in the maintenance of
a patent airway or if prolonged ventilatory support (assisted or controlled)
is indicated. Dialysis is of negligible value
in the treatment of acute overdosage with lidocaine. The intravenous LDof Lidocaine HCl in female mice is
26 (21���31) mg/kg and the subcutaneous LDis 264
(203���304) mg/kg.
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Lidocaine Hydrochloride
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dailymed-instance:fullName |
Lidocaine Hydrochloride (Injection, Solution)
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dailymed-instance:adverseRe... |
Adverse experiences following the administration
of lidocaine are similar in nature to those observed with other amide
local anesthetic agents. These adverse experiences are, in general,
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. Serious adverse experiences are generally
systemic in nature. The following types are those most commonly reported: Central nervous system: CNS manifestations are excitatory and/or depressant and may be characterized
by light-headedness, nervousness, apprehension, euphoria, confusion,
dizziness, drowsiness, tinnitus, blurred or double vision, vomiting,
sensations of heat, cold or numbness, twitching, tremors, convulsions,
unconsciousness, respiratory depression and arrest. The excitatory
manifestations may be very brief or may not occur at all, in which
case the first manifestation of toxicity may be drowsiness merging
into unconsciousness and respiratory arrest. Drowsiness following the administration of lidocaine is usually an
early sign of a high blood level of the drug and may occur as a consequence
of rapid absorption. Cardiovascular system: Cardiovascular manifestations are
usually depressant and are characterized by bradycardia, hypotension,
and cardiovascular collapse, which may lead to cardiac arrest. Allergic: Allergic
reactions are characterized by cutaneous lesions, urticaria, edema
or anaphylactoid reactions. Allergic reactions as a result of sensitivity
to lidocaine are extremely rare and, if they occur, should be managed
by conventional means. The detection of sensitivity by skin testing
is of doubtful value. Neurologic: The incidences of adverse reactions associated
with the use of local anesthetics may be related to the total dose
of local anesthetic administered and are also dependent upon the particular
drug used, the route of administration and the physical status of
the patient.
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dailymed-instance:warning |
4% LIDOCAINE HYDROCHLORIDE INJECTION, USP 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 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. 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. 4% Lidocaine Hydrochloride Injection, USP should be used with extreme
caution if there is sepsis or severely traumatized mucosa in the area
of application, since under such conditions there is the potential
for rapid systemic absorption.
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dailymed-instance:indicatio... |
4% Lidocaine Hydrochloride Injection, USP is indicated
for the production of topical anesthesia of the mucous membranes of
the respiratory tract or the genito-urinary tract. It may be injected
trans-tracheally to anesthetize the larynx and trachea, and it may
be administered by retrobulbar injection to provide anesthesia for
ophthalmic surgery.
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dailymed-instance:name |
Lidocaine Hydrochloride
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