Ingredient
LIDOCAINE HYDROCHLORIDE 20 MG / ML
Caution
THIS MEDICINE MAY REDUCE your ability to swallow. Do not eat for at least 1 hour after using this medicine. THIS MEDICINE MAY CAUSE NUMBNESS of the tongue or mouth lining. Do not eat or chew gum while your mouth feels numb. Also be careful not to bite your tongue or the inside of your mouth after using this medicine.
Xylocaine is also available in "Over the Counter"
by clicking here. Xylocaine
Counter
Where can I order Xylocaine from? Can I buy Xylocaine
at Canadian Prices?
Yes, if you are from the U.S. then you can
buy Xylocaine at Canadian prices. Currently we will only accept
an order for Xylocaine from U.S. and Canadian residents. Both
U.S. and Canadian residents require a prescription to purchase
Xylocaine and when you order Xylocaine it will be delivered with
express shipping.
Xylocaine
Action
And Clinical Pharmacology: Mechanism of
Action: Xylocaine stabilizes the neuronal membrane by inhibiting
the ionic fluxes required for the initiation and conduction
of impulses thereby, effecting local anesthetic action. Local
anesthetics of the amide type are thought to act within the
sodium channels of the nerve membrane.
Onset of Action: After application of Xylocaine Viscous, local
anesthesia is achieved within 5 minutes. Duration of anesthesia
is approximately 20 to 30 minutes. Xylocaine Viscous is ineffective
when applied to intact skin.
Hemodynamics: Xylocaine, like other local anesthetics, may
also have effects on excitable membranes in the brain and
myocardium. If excessive amounts of drug reach the systemic
circulation rapidly, symptoms and signs of toxicity will appear,
emanating from the central nervous and cardiovascular systems.
CNS toxicity (see Overdose: Symptoms and Treatment) usually
precedes the cardiovascular effects since it occurs at lower
plasma concentrations. Direct effects of local anesthetics
on the heart include slow conduction, negative inotropism
and eventually cardiac arrest.
Pharmacokinetics: The rate and extent of absorption depends
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 to wound surfaces and mucous membranes
is high, and occurs most rapidly after intratracheal and bronchial
administration. Xylocaine is also well absorbed from the gastrointestinal
tract, although little intact drug may appear in the circulation
because of biotransformation in the liver.
Xylocaine readily crosses the placenta, and equilibrium in
regard to free, unbound drug will be reached. Because the
degree of plasma protein binding in the fetus is less than
in the mother, the total plasma concentration will be greater
in the mother, but the free concentrations will be the same.
The plasma binding of Xylocaine is dependent on drug concentration,
and the fraction bound decreases with increasing concentration.
At concentrations of 1 to 4 µg of free base per mL,
60 to 80% of Xylocaine is protein bound. Binding is also dependent
on the plasma concentration of the alpha-1-acid glycoprotein.
Xylocaine has a total plasma clearance of 0.95 L/min, a volume
of distribution at steady state of 91 L, an elimination half-life
of 1.6 hours and an estimated hepatic extraction ratio of
0.65. The clearance of Xylocaine is almost entirely due to
liver metabolism, and depends both on liver blood flow and
the activity of metabolizing enzymes.
Xylocaine 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. Only 2% of Xylocaine
is excreted unchanged. Most of it is metabolized first to
monoethylglycinexylidide (MEGX) and then to glycinexylidide
(GX) and 2,6-xylidine. Up to 70% appears in the urine as 4-hydroxy-2,6-xylidine.
The elimination half-life of Xylocaine following an i.v. bolus
injection is typically 1.5 to 2.0 hours. The elimination half-life
in neonates (3.2 hours) is approximately twice that of adults.
The half-life may be prolonged 2-fold or more in patients
with liver dysfunction. Renal dysfunction does not affect
Xylocaine kinetics but may increase the accumulation of metabolites.
Acidosis increases the systemic toxicity of Xylocaine while
the use of CNS depressants may increase the levels of Xylocaine
required to produce overt CNS effects. Objective adverse manifestations
become increasingly apparent with increasing venous plasma
levels above 6.0 µg free base per mL.
Indications And Clinical Uses:
To provide relief of pain and discomfort in connection with:
irritated or inflamed mucous membranes of the mouth and pharynx,
e.g., lesions following tonsillectomy; introduction of instruments
and catheters into the respiratory and digestive tracts, e.g.,
bronchoscopy, esophagoscopy; painful diseases of the upper
gastrointestinal tract e.g., esophagitis.
Contra-Indications: In patients with a known history
of hypersensitivity to local anesthetics of the amide type
or to other components of the solution, e.g., methylparaben,
propylparaben. tag_WarningWarnings
Manufacturers' Warnings In Clinical States: Excessive
dosage, or short intervals between doses, can result in high
plasma levels of Xylocaine or its metabolites and serious
adverse effects. Following too high or repeated doses of viscous
Xylocaine in children under the age of 3, serious side effects
have been reported. Absorption from the mucous membranes is
variable but is especially high from the bronchial tree. Such
applications may therefore result in rapidly rising or excessive
plasma concentrations, with an increased risk for toxic symptoms,
such as convulsions. Patients should be instructed to strictly
adhere to the recommended dosage. This is especially important
in children where doses vary with weight. The management of
serious adverse reactions may require the use of resuscitative
equipment, oxygen and other resuscitative drugs (see Overdose:
Symptoms and Treatment).
Xylocaine should be used with caution in patients with sepsis
and/or traumatized mucosa at the area of application, since
under such conditions there is the potential for rapid systemic
absorption.
Xylocaine Viscous is for topical use only and must not be
used for injection.
Precautions:
The lowest dosage that results in effective anesthesia should
be used to avoid high plasma levels and serious adverse effects.
Absorption from mucous membranes is variable but especially
high from the bronchial tree. 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. Xylocaine should also be used with caution in patients
with epilepsy, impaired cardiac conduction, bradycardia, impaired
hepatic or renal function, and in severe shock.
Because amide-type local anesthetics such as Xylocaine are
metabolized by the liver, these drugs, especially repeated
doses, should be used cautiously in patients with hepatic
disease. Patients with severe hepatic disease, because of
their inability to metabolize local anesthetics normally,
are at greater risk of developing toxic plasma concentrations.
Xylocaine 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 AV conduction produced by these drugs.
Many drugs used during the conduct of anesthesia are considered
potential triggering agents for familial malignant hyperthermia.
It has been shown that the use of amide local anesthetics
in malignant hyperthermia patients is safe. However there
is no guarantee that neural blockade will prevent the development
of malignant hyperthermia during surgery. It is also difficult
to predict the need for supplemental general anesthesia. Therefore
a standard protocol for the management of malignant hyperthermia
should be available.
Xylocaine 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 Xylocaine.
Drug Interactions: Xylocaine should be used with caution
in patients receiving other local anesthetics or agents structurally
related to amide-type local anesthetics, since the toxic effects
are additive.
Information for Patients: See also Blue Section - Information
for the Patient "Xylocaine Viscous 2%". 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. Numbness of the tongue
or buccal mucosa may enhance the danger of unintentional biting
trauma. Food or chewing gum should not be taken while the
mouth or throat area is anesthetized.
Pregnancy : It is reasonable to assume that a large number
of pregnant women and women of childbearing age have been
given Xylocaine. No specific disturbances to the reproductive
process have so far been reported, e.g., no increased incidence
of malformations. However, care should be given during early
pregnancy when maximum organogenesis takes place.
There are no adequate and well-controlled studies in pregnant
women on the effect of Xylocaine on the developing fetus.
Labor and Delivery: Xylocaine is not contraindicated in labor
and delivery. Should Xylocaine Viscous 2% be used concomitantly
with other products containing Xylocaine, the total dose contributed
by all formulations must be kept in mind.
Lactation: Xylocaine is excreted in the breast milk, but in
such small quantities that there is generally no risk of affecting
the infant at therapeutic dose levels.
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