Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/482
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Lidocaine Hydrochloride and Dextrose (Injection, Solution)
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Spinal anesthesia with 5% Lidocaine Hydrochloride and 7.5%
Dextrose Injection, USP may be induced in the right or left lateral recumbent
or the sitting position. Since this is a hyperbaric solution, the anesthetic
will tend to move in the direction in which the table is tilted. After the
desired level of anesthesia is obtained and the anesthetic has become fixed,
usually in 5 to 10 minutes with lidocaine, the patient may be positioned according
to the requirement of the surgeon or obstetrician. In
clinical trials, the safety of hyperbaric lidocaine for single injection spinal
anesthesia was demonstrated using 22 or 25 gauge spinal needles. In these
studies, free flow of CSF was visible before injection of lidocaine. Neurologic
deficits have been reported with the use of small bore needles and microcatheters
for spinal anesthesia. It has been postulated, based on in
vitro models, that these deficits were caused by pooling and non-uniform
distribution of concentrated local anesthetic within the subarachnoid space.Animal
studies suggest mixing of 5% lidocaine hydrochloride with an equal volume
of CSF or preservative-free 0.9% saline solution may reduce the risk of nerve
injury due to pooling of concentrated local anesthetic.(See PRECAUTIONS). Intrathecal
distribution of anesthetic may be facilitated by using a spinal needle of
sufficient gauge to insure adequate withdrawal of CSF through the needle prior
to and after anesthetic administration. If the technique is properly placed
in the subarachnoid space, a separate injection is seldom necessary. An
incomplete or patchy block not responsive to patient repositioning may indicate
misplacement or inadequate distribution of drug. To avoid excessive drug pooling,
additional doses of lidocaine should not be administered with the same needle
placement. INJECTIONS SHOULD BE MADE SLOWLY. Consult
standard textbooks for specific techniques for spinal anesthetic procedures. Recommended dosages Normal
healthy adults: The following recommended dosages are for normal healthy adults
and serve only as a guide to the amount of anesthetic required for most routine
procedures. In all cases, the smallest dose that will produce the desired
result should be given. If the technique is properly
performed, and the needle is properly placed in the subarachnoid space, it
should not be necessary to administer more than one ampul (100 mg). Obstetrical low spinal or���saddle block���anesthesia: The dosage recommended for normal
vaginal delivery is approximately 1 mL (50 mg). For Caesarean section and
those deliveries requiring intrauterine manipulations, 1.5 mL (75 mg) is usually
adequate. Surgical
anesthesia: The dosage recommended for abdominal
anesthesia is 1.5 to 2 mL (75 to 100 mg). Pediatric Patients: The
dosage recommendations in healthy adolescents, 16 years of age and older,
is the same as for normal healthy adults. There is insufficient data in pediatric
patients below the age of 16 years to make dosage recommendations (see PRECAUTIONS). 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. Unused portions of solutions should be
discarded following initial use. 5% Lidocaine Hydrochloride
and 7.5% Dextrose Injection, USP may be autoclaved once at 15 pounds pressure,
121��C (250��F) for 15 minutes. Since this preparation contains dextrose,
carmelization may occur under prolonged heating and, in some instances, prolonged
storage. Therefore this preparation should not be autoclaved more than once,
according to the above instructions, and should not be permitted to remain
in the autoclave any longer than necessary. Do not administer any solution
which is discolored or contains particulate matter.
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| dailymed-instance:descripti... |
5% Lidocaine Hydrochloride and 7.5% Dextrose Injection, USP
is a sterile, nonpyrogenic, hyperbaric solution for use in spinal anesthesia. 5%
Lidocaine Hydrochloride and 7.5% Dextrose Injection, USP contains lidocaine
HCl, which is chemically designated as 2-(diethylamino)-N-(2,6-dimethylphenyl)-acetamide
monohydrochloride, monohydrate and Dextrose (D-Glucose monohydrate) which
have the following structural formulas: Lidocaine Hydrochloride
(monohydrate) Dextrose (hydrous) 5% Lidocaine Hydrochloride and 7.5% Dextrose Injection, USP contains 50
mg/mL of lidocaine hydrochloride, anhydrous with 75 mg/mL of dextrose, hydrous
in water for injection. May contain sodium hydroxide and/or hydrochloric acid
for pH adjustment. pH 6.5 (6.0 to 7.0). The osmolar concentration is 0.75
mOsmol/mL (calc.). The specific gravity is 1.030 to 1.035.
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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. The duration of perineal
anesthesia provided by 1 mL (50 mg) 5% Lidocaine Hydrochloride and 7.5% Dextrose
Injection, USP averages 100 minutes, with analgesia continuing for an additional
40 minutes. The duration of surgical anesthesia provided by 1.5 to 2 mL (75
to 100 mg) of this agent is approximately two hours. 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, or 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 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, thehighest 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/toxicologial 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 6.0
mcg free base per mL. In the rhesus monkey arterial blood levels of 18 to
21 mcg/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. The
following conditions preclude the use of spinal anesthesia:
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5% Lidocaine Hydrochloride and 7.5% Dextrose Injection, USP
is supplied in a single-dose 2 mL ampul (List No. 4712). Store
at 20 to 25��C (68 to 77��F). [See USP Controlled Room Temperature.] HOSPIRA, INC., LAKE FOREST,
IL 60045 USA
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General:: The safety and effectiveness of lidocaine depend on proper
dosage, correct technique, adequate precautions, and readiness for emergencies.
Standard textbooks should be consulted for specific techniques and precautions
for spinal anesthetic procedures. Resuscitative equipment, oxygen and other
resuscitative drugs should be available for immediate use. (See WARNINGS and
ADVERSE REACTIONS.) The lowest dosage thatresults 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 physical condition of the
patient. Debilitated, elderly patients, acutely ill patients and children
should be given reduced doses commensurate with their age and physical status.
Lidocaine shouldalso be used with caution in patients with severe shock or
heart block. Neurologic deficits have been reported
with the use of small bore needles and microcatheters for spinal anesthesia.
It has been postulated, based on in vitro models,
that these deficits were due to pooling and non-uniform distribution of concentrated
local anesthesia within the subarachnoid space.Animal studies
suggest mixing of 5% lidocaine hydrochloride with an equal volume of CSF or
preservative-free 0.9% saline solution may reduce the risk of nerve injury
due to pooling of concentrated local anesthetic.(See DOSAGE AND
ADMINISTRATION.). The following conditions may preclude
the use of spinal anesthesia, depending upon the physician's ability
to deal with the complications or complaints that may occur: a.
Pre-existing diseases of the central nervous system such as those attributable
to poliomyelitis, pernicious anemia, paralysis from nerve injuries, and syphilis. b.
Disturbance in blood morphology and/or anticoagulant therapy. In these conditions,
trauma to a blood vessel during needle puncture may result in uncontrollable
hemorrhage into the epidural or subarachnoid space. Also profuse hemorrhage
into the soft tissue may occur. c. Extremes of age. d.
Chronic backache and preoperative headache. e. Hypotension
and hypertension. f. Arthritis or spinal deformity. g.
Technical problems (persistent paresthesias, persistent bloody tap). h.
Psychotic or uncooperative patients. CONSULT STANDARD
TEXTBOOKS FOR SPECIFIC TECHNIQUES AND PRECAUTIONS FOR SPINAL ANESTHETIC PROCEDURES. 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 a greater risk of developing
toxic plasma concentrations. Lidocaine should also be used with caution inpatients 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 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.<br/>Information for Patients:: When appropriate, patients should be informed in advance
that they may experience temporary loss of sensation and motor activity, usually
in the lower half of the body, following proper administration of spinal anesthesia.<br/>Clinically significant drug interactions:: The administration of local anesthetic solutions containing
epinephrine or norepinephrine 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. Concurrent administration
of vasopressor drugs (for the treatment of hypotension related to spinal blocks)
and ergot-type oxytocic drugs may cause severe, persistent hypertension or
cerebrovascular accidents.<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:: Maternal hypotension has resulted from regional anesthesia.
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 highlyadvisable. Spinal
anesthesia may alter the forces of parturition through changes in uterine
contractility or maternal expulsive efforts. However, spinal anesthesia has
also been reported to prolong the second stage of labor by removing the parturient's
reflex urge to bear down or by interfering with motor function. The use of
obstetrical anesthesia may increase the need for forceps assistance.<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:: Safety and effectiveness in pediatric patients below the
age of 16 years have not been established.
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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, as well as underventilation or
apnea due to excessive cephalad spread of the spinal block, 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 theclinical situation (e.g., ephedrine). If
not treated immediately, both convulsions and cardiovascular depression can
result in hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest.
Underventilation or apnea due to excessive cephalad spread of the spinal block
may produce these same signs and also lead to cardiac arrest if ventilatory
support is not instituted. 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 to 31)
mg/kg and subcutaneous LDis 264 (203 to 304) mg/kg.
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Lidocaine Hydrochloride and Dextrose
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Lidocaine Hydrochloride and Dextrose (Injection, Solution)
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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 lightheadedness, nervousness, apprehension, euphoria,
confusion, dizziness, lethargy, slurred speech, 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. In a prospective review of 10,440
patients who received lidocaine for spinal anesthesia, the incidences of adversereactions were reported to be about 3 percent each for positional headaches,
hypotension and backache; 2 percent for shivering; and less than 1 percent
each for peripheral nerve symptoms, nausea, respiratory inadequacy and double
vision. Many of these observations may be related to local anesthetic techniques,
with or without a contribution from the local anesthetic. Neurologic
effects following spinal anesthesia may include loss of perineal sensation
and sexual function; persistent anesthesia, paresthesia, weakness and paralysis
of the lower extremities, and loss of sphincter control all of which may have
slow, incomplete, or no recovery; hypotension; high or total spinal block;
urinary retention; headache; backache; septic meningitis; meningismus, arachnoiditis;
slowing of labor; increased incidence of forceps delivery; shivering; cranial
nerve palsies due to traction on nerves from loss of cerebrospinal fluid;
and fecal and urinary incontinence.
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5% LIDOCAINE HYDROCHLORIDE AND 7.5% DEXTROSE INJECTION, USP
FOR SPINAL ANESTHESIA 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 SPINAL ANESTHESIA 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. Spinal
anesthetics should not be injected during uterine contractions since spinal
fluid current may carry the drug farther cephalad than desired.
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| dailymed-instance:indicatio... |
5% Lidocaine Hydrochloride and 7.5% Dextrose Injection, USP
is indicated for the production of spinal anesthesia when the accepted procedures
for this technique as described in standard textbooks are observed.
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Lidocaine Hydrochloride and Dextrose
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