Anesthesia, Topical

Author: Mary L Windle, PharmD,

Adjunct Assistant Professor,
University of Nebraska Medical
Center College of Pharmacy,
Pharmacy Editor, eMedicine.com,
Inc
Contributor Information and
Disclosures
Updated: Jun 4, 2008

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References
Overview
Many options to deliver anesthesia
have developed over the last several
decades. Administration of topical
anesthetics to control pain associated
with procedures such as laceration
repair may avoid the need for

infiltrative local anesthesia injections

and associated pain from the
injections. Topical anesthesia also
avoids the risk of wound margin
distortion that exists with infiltrative
injection administration. Many
dosage forms exist (eg, gels, sprays,
creams, ointments, patches) and
provide the clinician with precise
options for application under various
circumstances.
Mechanism of action
Topical anesthetics reversibly block
nerve conduction near their site of
administration, thereby producing
temporary loss of sensation in a
limited area. Nerve impulse
conduction is blocked by decreasing
nerve cell membrane permeability to
sodium ions, possibly by competing

with calcium-binding sites that control

sodium permeability. This change in
permeability results in decreased
depolarization and an increased
excitability threshold that, ultimately,
prevents the nerve action potential
from forming.1,2,3
Absorption
Skin absorption is highly variable.
Most anesthetic agents exist as
solids and are only superficially
absorbed through intact skin. Eutectic
mixtures result in liquids that melt at
lower temperatures than their single
components. This permits higher
concentrations of anesthetics, which
results in superior dermal anesthesia
for intact skin. Other methods of
increasing skin penetration include
liposomal preparations,
iontophoresis, and transdermal

patches.1,3
Indications
Topical anesthetics are used for
various skin and mucous membrane
conditions, including (but not limited
to) pruritus and pain due to minor
burns, skin eruptions (eg, varicella,
sunburn, poison ivy, insect bites), and
local analgesia on intact skin. With
the exception of lidocaine-prilocaine
as a eutectic mixture (EMLA), topical
anesthetics are poorly absorbed
through intact skin. Because of
variation in systemic absorption and
toxicity, the ideal choice of topical
anesthetic and particular
concentration depends on the
intended use. EMLA has also been
applied to children to minimize
discomfort prior to injections or to

starting an intravenous line.2,3

Dosage guidelines and
administrative techniques

Apply the cream, ointment, or

solution to the chosen area in
incremental amounts.
The total dose for a topical
anesthetic is smaller than that
used for subcutaneous infiltration.
EMLA cream does not require an
occlusive dressing (eg,
DuoDERM, Tegaderm, Saran
Wrap); however, when an
occlusive dressing is applied,
absorption is improved and time of
onset is decreased.2,3
Viscous lidocaine may be used
alone or in a compounded mixture
as a mouthwash (ie, swish and
expectorate).3

Iontophoresis has been used to

improve the effects of topical
anesthesia; however, the
equipment is expensive and bulky,
and some patients experience
discomfort from the mild electrical
sensation.1,3
Sequential layered application of
topical lidocaine with epinephrine
(TLE) has been described for
small facial or scalp wounds. Onehundred patients were enrolled in
a randomized controlled trial, with
50 in each group. The study group
received TLE using a unique
method of "sequential layered
application." The control group
received 2% lidocaine infiltration
anesthesia. Patients rated the pain
from the application of anesthesia
and from suturing, using a zero-toten visual analog pain scale.

Follow-up interviews were

conducted to assess for
complications and to rate patients'
wound repair experience. Patients
in the study group reported
significantly less pain from TLE
application, with 66% reporting no
pain vs 0% reporting no pain from
the infiltration in the control group
(P <0.001). No difference in pain
during wound repair was noted
between the 2 groups (P ~0.59).
On follow-up, 95% of patients
contacted in the TLE group rated
their experience in regard to pain
as "excellent," compared to 5% of
patients in the control group (P
<0.001).4
Deciphering drug concentration

Concentrations: Drug
concentration is expressed as a

percentage (eg, dibucaine 1%,

benzocaine 0.5%).
Percentage is measured in
grams per 100 mL (ie, 1% is 1
g/100 mL [1000 mg/100 mL] or
10 mg/mL)
Calculate the mg/mL
concentration quickly from the
percentage by moving the
decimal point 1 place to the
right, as follows:
Tetracaine 0.5% = 5 mg/mL
Viscous lidocaine 2% = 20
mg/mL
Benzocaine 20% = 200
mg/mL

o
o

Adverse effects
Adverse effects are usually caused
by high plasma concentrations of
topical anesthetics that typically
result from excessive exposure

caused by application to abraded or

torn skin.2,5 Possible adverse effects
include the following:
Burning or stinging may occur
local to the administration site.
Oral viscous lidocaine may cause
systemic toxicity, particularly with
repeated use in infants or children.
CNS: High plasma concentration
initially produces CNS stimulation
(including seizures), followed by
CNS depression (including
respiratory arrest). The CNS
stimulatory effect may be absent
in some patients, particularly when
amides (eg, tetracaine) are
administered. Solutions that
contain epinephrine may add to
the CNS stimulatory effect.
Cardiovascular: High plasma
levels typically depress the heart
and may result in bradycardia,

arrhythmias, hypotension,
cardiovascular collapse, and
cardiac arrest. Local anesthetics
that contain epinephrine may
cause hypertension, tachycardia,
and angina.
Gag-reflex suppression may occur
with oral administration.
Other body systems can also
experience adverse effects.
Transient burning sensation
Skin discoloration
Swelling
Neuritis (Click here to complete
a Medscape CME activity on
the diagnosis and treatment of
optic neuritis.)
Tissue necrosis and sloughing
Methemoglobinemia (with
prilocaine)
o
o
o
o

o
o

The United States Food and Drug

Administration (FDA) has issued an

advisory regarding risk of serious

adverse effects with use of topical
anesthetics for cosmetic procedures.
For more information, see the FDA
Medwatch Public Health Advisory.
Warnings regarding cocaine as a
topical anesthetic
Various anesthetic mixtures that
contain cocaine have been used to
anesthetize minor skin lacerations,
especially on the face or scalp. One
such combination that is
extemporaneously prepared by
hospital pharmacies includes
tetracaine 0.5%, epinephrine
(Adrenaline) 1:2000, and cocaine
11.8%. This combination is commonly
referred to as TAC solution. Its use
results in decreased pain on
application and may provide better

patient tolerance of suturing,

particularly in those who are unable
to tolerate injections or who have
difficulty following instructions or
sitting still (eg, children, individuals
with mental disabilities). However,
serious toxic effects (eg, seizures,
cardiac death) have been described
following topical cocaine application,
particularly in infants and children.2,5
Because of increased toxicity,
expense, and federal regulatory
issues, cocaine is no longer
recommended for topical anesthesia.
Compounded mixtures such as
lidocaine, epinephrine, tetracaine
(LET) solutions, have replaced
cocaine with lidocaine 4% because of
their superior safety when applied to
nonintact skin. Still, these solutions
should not be applied to wounds with

end-arteriolar blood supply.

Allergic reaction to local
anesthetics
Actual hypersensitivity is rare and
accounts for less than 1% of all
reactions to local anesthetics. Allergic
reactions may be attributed to other
factors such as acute toxicity,
concurrent drug therapy (eg,
tachycardia caused by epinephrine),
or preservatives, such as paraben or
sulfites, that the product may
contain.2,5
Local anesthetics with a para -amino
benzoic acid (PABA) ester-type
structure seem to cause most
anesthesia-related allergic reactions.
Consequently, use esters (eg,
tetracaine, benzocaine) with caution

or use a topical anesthetic from the

amide class (eg, dibucaine,
lidocaine). Documented crosssensitivity has been exhibited within
the ester-based local anesthetics and
structurally related compounds (eg,
paraben preservatives).
Hypersensitivity to the amide local
anesthetics is rare.1,3 To quickly
determine whether an anesthetic
agent is an ester or an amide, note
whether the generic name contains
the letter i once or twice. Esters
contain the letter i once in their
generic names, whereas the generic
names for amides contain the letter i
twice.
Physiochemical variables
Onset of action, anesthesia depth,
and duration of action are determined
by the pKa level, pH level, lipid

solubility, protein binding, and

vasodilatory effects of the specific
local anesthetic. These factors also
depend on the area of the skin to
which the anesthetic is applied, the
vascularity of tissues, the surface
area, and anesthesia technique.
Duration of application is important to
improve topical anesthetic
properties.3
Table 2. Topical Anesthesia6,1,2,3,5
Open table in new window

An Com Availa Do Ma Ma Ma Pe Du
est mon ble/R sa xim xi xi ak rat
het Topi ecom ge um m m Eff ion
ic cal mend For Ad u u ect ,
m( ult m m , Mi
Cla Ane ed
ss sthet Conc s) Top Ad Pe Mi nu
ics entrat
ical ult dia nu

Gen ion(s)
eric , %*
Nam
e
(Tra
de
Nam
e)

Dibu
A cain
mi e
1
de (Nup
s ercai
nal)
Lido 2-5
cain
e

Do Mu tri testes
se, co c
mg sal Mu
Do co
se, sal
m Do
g se,
m
g/k
g
Cre
am,
30oint 25 -- -- <5
60
me
nt
Vis Vari 25 3-42-5 15cou abl 0Lip 45
s e 30
os

(Xylo
cain
e,
ELAMax,
Lido
derm
)

jelly
,
dep
pat
end
ch,
ing
oint
on
me
0
dos
nt,
age
lipo
for
so
m
me
s

Est Benz 0.5-20 Aer -ers ocai

oso
ne
l,
(Ame
cre
ricai
am,
ne,
gel
Ceta
s,
cain
loti
e,
on,

om
e:
30

-- -- <5 1545

Der
mopl
ast,
Solar
cain
e)

oint
me
nt,
sol
utio
n

Coca
4-10
ine

Sol
1
30utio 200 mg 1 1-5
60
n
/kg

Tetra
cain
e
0.5-2
(Pon
tocai
ne)

Sol
utio
n,
0.7
3050 20
3-8
gel,
5
60
cre
am

Mi Dycl 0.5-1 Aer -sc onin

oso
ell

50 -- <1 <6
0 0

e
an (Cep
eo acol,
us Sucr
ets)

Pram
oxin
e
(Proc
toFo
am, 1
Cala
dryl
Crea
m for
Kids)

l,
loz
eng
e
Aer
oso
l
foa
m,
ple
dge 200 -- -- 3-5-ts,
cre
am,
oint
me
nt

Lido 2.5/2. Cre 1

-- -- 60: 30-

3
cm
de 60
pth aft
12 er
0: re
5 mo
cm val
de
pth

cain
e/Pril
ocai
5
ne
(EML
A)

am,
tra
g/1
nsd
0
er
cm2
mal
pat
ch

Lido -cain
e 70
mg
and
tetra
cain
e 70
mg
(Syn

Tra Adu -- -- 10 -0
nsd lts
er or
mal chil
pat dre
ch n:
App
ly 1
pat
ch

era
Patc
h)

2030
min
bef
ore
sup
erfi
cial
der
mat
olo
gica
l
pro
ced
ure

An Com Availa Do Ma Ma Ma Pe Du
est mon ble/R sa xim xi xi ak rat
het Topi ecom ge um m m Eff ion

ic cal mend For Ad u u ect ,

Cla Ane ed
m( ult m m , Mi
ss sthet Conc s) Top Ad Pe Mi nu
ics entrat
ical ult dia nu tes
Gen ion(s)
Do Mu tri tes
eric , %*
se, co c
Nam
mg sal Mu
e
Do co
(Tra
se, sal
de
m Do
Nam
g se,
e)
m
g/k
g

Dibu
A cain
mi e
1
de (Nup
s ercai
nal)
Lido 2-5
cain
e
(Xylo
cain
e,
ELAMax,
Lido
derm
)

Cre
am,
30oint 25 -- -- <5
60
me
nt
Vis Vari 25 3-42-5 15cou abl 0Lip 45
s e 30
os
jelly dep 0
om
, end
e:
pat ing
30
ch, on
oint dos
me age
nt, for
lipo m
so
me

s
Benz
Aer
ocai
oso
ne
l,
(Ame
cre
ricai
am,
ne,
gel
Ceta
s,
Est cain 0.5-20 loti -ers e,
on,
Der
oint
mopl
me
ast,
nt,
Solar
sol
cain
utio
e)
n
Coca 4-10
ine

15-- -- <5
45

Sol 200 1 1 1-530utio

mg
60

Mi
sc
ell
an
eo
us

/kg

Tetra
cain
e
0.5-2
(Pon
tocai
ne)

Sol
utio
n,
0.7
3050 20
3-8
gel,
5
60
cre
am

Dycl
onin
e
(Cep 0.5-1
acol,
Sucr
ets)

Aer
oso
l,
-loz
eng
e

Pram 1
oxin
e

Aer 200 -- -- 3-5-oso

l

<1 <6
50 -0 0

(Proc
toFo
am,
Cala
dryl
Crea
m for
Kids)

Lido 2.5/2.
cain 5
e/Pril
ocai
ne
(EML
A)

foa
m,
ple
dge
ts,
cre
am,
oint
me
nt
Cre 1 -- -- 60: 30am, g/1
3 60
tra 0
cm aft
nsd cm2
de er
er
pth re
mal
12 mo
pat
0: val
ch
5
cm
de

pth
Lido -cain
e 70
mg
and
tetra
cain
e 70
mg
(Syn
era
Patc
h)

Tra Adu -- -- 10 -0
nsd lts
er or
mal chil
pat dre
ch n:
App
ly 1
pat
ch
2030
min
bef
ore
sup
erfi
cial
der

mat
olo
gica
l
pro
ced
ure

*Use lower concentrations for

children or patients who are elderly or
debilitated.
Cocaine is generally not
recommended for topical or mucosal
application (see warnings above).
This dose also applies to the
pediatric population (maximum
application time in children aged <3
mo = 1 h; >3 mo = 4 h).
Keywords

topical anesthesia, anesthetics, local

anesthetic, drug concentration, drug
dilution, epinephrine, onset of action,
duration of action, local absorption,
topical absorption, lidocaine, viscous
lidocaine, plasma concentration, TAC
solution, LET solution, TAC, LET

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