HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the infor-
mation needed to use GLYDO (lidocaine HCl
jelly) 2% safely and effectively. See full pre-
scribing information for GLYDO (lidocaine
HCI jelly) 2%.

GLYDO (lidocaine hydrochloride) 2% jelly
Initial U.S. Approval: 1953

pieleieioiatel INDICATIONS AND USAGE ——-

GLYDO (lidocaine HCl jelly) 2% contains
lidocaine, an amide local anesthetic, and is
indicated in adult patients:

forpreventionandcontrolofpainin procedures
involving the male and female urethra (1}

for topical treatment of painful urethritis (1)

as an anesthetic lubricant for oral
and nasal endotracheal intubation (1)

cesses DOSAGE AND ADMINISTRATION —–

The toxic effects of local anesthetics are
additive. When using this product
concomitantly with other lidocaine-
containing products, consider the total
dose of lidocaine and monitor patients for
cardiovascular and respiratory vital signs. (2.1)

For surface anesthesia of male adult urethra:
15 mL (300 mg lidocaine HCl) followed by
additional 15 mL if needed (2.2)

For surface anesthesia of female adult
urethra: 3 mL to 5 mL (60 mg to 100 mg
lidocaine HCl) (2.3)

For lubrication for endotracheal intubation:
sufficient amount to coat the external
surface of endotracheal tube (2.4)
Forpediatricpatients: Not morethan4.5mg/kg
body weight of lidocaine HCI (2.5)

coos DOSAGE FORMS AND STRENGTHS —-
120 mg per 6 mL Prefilled Syringe (3)
220 mg per Tl mL Prefilled Syringe (3)

eoneeene- CONTRAINDICATIONS ———

Known hypersensitivity to any local
anesthetic agent of the amide-type or to
other components of GLYDO 2% Jelly (4.1)

Infected and/or Severely Traumatized
Mucosa (4.2)

Severe shock or heart block (4.3)

leleieiel WARNINGS AND PRECAUTIONS —–

Dose-Related Toxicity: follow dosing
instructions carefully. (5.1)
Methemoglobinemia: Cases have been
reported in association with local anesthetics
use. See full prescribing information for more
details on managing these risks. (5.2)

Familial Malignant Hyperthermia: Monitoring
of patients is recommended (5.3)

Endotracheal_ Tube Occlusion: Avoid
introduction of jelly into the lumen of the
endotracheal tube (5.4)

Risk of Aspiration and Biting Trauma with
Oral Use: Food and chewing gum should not
be taken while the mouth or throat area is
anesthetized (5.7)

ceeceeee- ADVERSE REACTIONS ———
Most common adverse reactions are as follows:

Central Nervous System: Lightheadedness,
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. (6)

Cardiovascular _ System: Bradycardia,
hypotension, and cardiovascular collapse. (6)
Allergic: Cutaneous lesions, urticaria, edema
or anaphylactoid reactions. (6)

Neurologic: Positional
hypotension and backache. (6)

Hematologic: Methemoglobinemia. (6)

To report SUSPECTED ADVERSE REACTIONS,
contact Sagent Pharmaceuticals
at 1-866-625-1618 or FDA at 1-800-FDA-1088

or www.fda.gov/medwatch.

chia DRUG INTERACTIONS ———

Local Anesthetics: The toxic effects of local
anestheticsareadditive.Monitorforneurologic
and cardiovascular effects when additional
local anesthetics are administered (7.1).

Drugs Associated with Methemoglobinemia:
Patients are at increased risk of developing
methemoglobinemia when concurrently
exposed to nitrates, nitrites, local anesthetics,
antineoplastic agents, antibiotics,
antimalarials, anticonvulsants, and other
drugs (7.2).

Hepatic Impairment: Consider reduced
dosing and increased monitoring for local
anesthetic systemic toxicity in patients
with hepatic impairment (8.6)

headaches,

cases USE IN SPECIFIC POPULATIONS —–

Pediatric Use: Dose should be reduced
commensurate with age, body weight and
physical condition (8.4)

See 17 for PATIENT COUNSELING

INFORMATION and FDA-approved patient

labeling.
apeling Revised: 05/2025

FULL PRESCRIBING INFORMATION: CONTENTS*
1 INDICATIONS AND USAGE
2 DOSAGE AND ADMINISTRATION

21 For Surface Anesthesia of the Male

Adult Urethra

2.2 For Surface Anesthesia of the Fema-
le Adult Urethra

2.3. Lubrication for Endotracheal Intuba-
tion

24 Dosing for Pediatric Patients
25 Administration Instructions
3 DOSAGE FORMS AND STRENGTHS
4 ~~ CONTRAINDICATIONS
41 — Hypersensitivity
42 Use on Infected and/or Severely
Traumatized Mucosa
4.3 Use in Severe Shock or Heart Block
5 WARNINGS AND PRECAUTIONS
51 Dose Related Toxicity
5.2. Methemoglobinemia
53 Familial Malignant Hyperthermia
54 Endotracheal Tube Occlusion
55 Anaphylactic Reactions
56 Risk of Toxicity in Patients with He-
patic Impairment
5.7 _ Risk of Aspiration and Biting Trauma
with Oral Use
6 ADVERSE REACTIONS

7 DRUG INTERACTIONS
71 ~~ Local Anesthetics
72 Drugs Associated with Methemoglobi-
nemia
8 USE IN SPECIFIC POPULATIONS
81 Pregnancy
8.2 Lactation
84 Pediatric Use
85 Geriatric Use
86 Hepatic Impairment
10 OVERDOSAGE
1 DESCRIPTION

CLINICAL PHARMACOLOGY
121 Mechanism of Action

Pharmacodynamics

Pharmacokinetics
T3 NONCLINICAL TOXICOLOGY
13.1 Carcinogenesis, Mutagenesis, Im-
pairment of Fertility
16 HOW SUPPLIED/STORAGE AND
HANDLING
17 PATIENT COUNSELING INFORMATION
171 Allergic Type Reactions
172 Methemoglobinemia
173 Aspiration
174 Risk of Biting Trauma

Sections or subsections omitted from the full
prescribing information are not listed.

FULL PRESCRIBING INFORMATION

1 INDICATIONS AND USAGE

GLYDO (lidocaine HCl jelly) 2% is an amide local
anesthetic indicated:

for prevention and control of pain
in procedures involving the male and
female urethra

for topical treatment of painful urethritis

as an anesthetic lubricant for oral and
nasal endotracheal intubation

2 DOSAGE AND ADMINISTRATION

2.1 Important Dosage and
Administration Information
Administration Precautions

The toxic effects of local anesthetics are
additive. Monitor for neurologic and
cardio-vascular effects related to local
anesthetic systemic toxicity when additional
local anesthetics are administered with
GLYDO (lidocaine HCI jelly) 2% [see Warnings
and Precautions (5.1), Adverse Reactions (6),
Overdosage (i0}].

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
GLYDO (lidocaine HCl jelly) 2% is quite low,
caution should be exercised, particularly when
employing large amounts, since the incidence
of adverse effects is directly proportional
to the total dose of local anesthetic agent
administered.

No more than 600 mg of lidocaine HCI should
be given in any 12 hour period.

2.2 For Surface Anesthesia of the Male
Adult Urethra

Slowly instill approximately 15 mL (300 mg of

lidocaine HCl) into the urethra. Apply a penile

clamp for several minutes at the corona. An

additional dose of not more than 15 mL (300 mg}

can be instilled if needed.

Prior to sounding or cystoscopy, a penile clamp
should be applied for S to 10 minutes to obtain
adequate anesthesia. A total dose of 30 mL
(600 mg) is usually required to fill and dilate the
male urethra.

Prior to catheterization, 5 mL to 10 mL (100 mg
to 200 mg) are recommended for lubrication.

23 For Surface Anesthesia of the Female
Adult Urethra

Slowly instill approximately 3 mL to 5 mL
(60 mg to 100 mg of lidocaine HCl) into the
urethra. In order to obtain adequate anesthesia,
wait for several minutes prior to performing
urological procedures. If desired, some jelly may
be deposited on a cotton swab and introduced
into the urethra.

24 Lubrication for Endotracheal Intubation
Apply a sufficient amount of jelly to coat the
external surface of the endotracheal tube
shortly before use. Care should be taken to
avoid introducing the product into the lumen
of the tube.

Do not use the jelly to lubricate endotracheal
stylettes. (see WARNINGS and ADVERSE
REACTIONS concerning rare reports of inner
lumen occlusion). It is also recommended
that use of endotracheal tubes with dried jelly
on the external surface be avoided for lack of
lubricating effect.

25 Dosing for Pediatric Patients
Amaximum dose of GLYDO (lidocaine HCl jelly)
2% for children varies based on age and weight.
The maximum dose should not exceed 4.5 mg/
kg of body weight. For children over 3 years of
age, the maximum dose is determined by the
child’s age and weight. For example, in a child
of 5 years weighing approximately 23 kg, the
dose of lidocaine hydrochloride should not
exceed approximately 75 mg to 100 mg (3.3 mg/
kg to 4.4 mg/kg).

adverse effects, including seizures, coma,
arrhythmias, and death. Discontinue GLYDO 2%
Jelly and any other oxidizing agents. Depending
on the severity of the signs and symptoms,
patients may respond to supportive care, i.e.,
oxygen therapy, hydration. A more severe
clinical presentation may require treatment
with methylene blue, exchange transfusion, or
hyperbaric oxygen.

5.3 Familial Malignant Hyperthermia
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).

54 Endotracheal Tube Occlusion

When used for endotracheal tube lubrication,
care should be taken to avoid introducing the
product into the lumen of the tube. Do not use
the jelly to lubricate the endotracheal stylettes.
If allowed into the inner lumen, the jelly may
dry on the inner surface leaving a residue which
tends to clump with flexion, narrowing the
lumen. There have been rare reports in which
this residue has caused the lumen to occlude
[see Adverse Reactions (6) and Dosage and
Administration (2)].

55 Anaphylactic Reactions
Anaphylactic reactions may occur following
administration of lidocaine hydrochloride [see
Adverse Reactions (6)]. Patients allergic to
para-aminobenzoic acid derivatives (procaine,
tetracaine, benzocaine, etc.) have not shown
cross sensitivity to lidocaine.

56 Risk of Toxicity in Patients with
Hepatic Impairment
Because amide local anesthetics such as
lidocaine are metabolized by the liver, consider
reduced dosing and increased monitoring
for lidocaine systemic toxicity in patients with
moderate to severe hepatic impairment who
are treated with GLYDO 2% Jelly, especially with
repeat doses [see Use in Specific Populations

(8.6)].

57 Risk of Aspiration and Biting Trauma
with Oral Use

When used orally (i.e. endotracheal tube
lubrication), topical anesthesia may occur to
oropharyngeal structures. This 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 gum should
not be taken while the mouth or throat area is
anesthetized.

6 ADVERSE REACTIONS

The following adverse reactions associated
with the use of GLYDO 2% Jelly were identified
in clinical studies or postmarketing reports.
Because some of these reactions were reported
voluntarily from a population of uncertain size,
it is not always possible to reliably estimate their
frequency or establish a causal relationship to
drug exposure.

Adverse experiences following the
administration of lidocaine are similar in nature
to those observed with other amide local
anesthetic agents. A major cause of adverse
reactions to this group of drugs is excessive

The lowest effective dose should be used.

3 DOSAGE FORMS AND STRENGTHS
GLYDO (lidocaine HCl jelly, USP) 2% in:

120 mg per 6 mL Prefilled Syringe
220 mg per Tl mL Prefilled Syringe

4 CONTRAINDICATIONS

41 Hypersensitivity

GLYDO 2% Jelly is contraindicated in patients
with a known history of hypersensitivity to
lidocaine or to any local anesthetics of the
amide type or to other components of GLYDO
2% Jelly.

4.2 Use on Infected and/or Severely
Traumatized Mucosa

GLYDO 2% Jelly should not be used on infected

and/or severely traumatized mucosa in the area

of application.

43 Use in Severe Shock or Heart Block
GLYDO 2% Jelly should not be used in patients
with severe shock or heart block.

5 WARNINGS AND PRECAUTIONS

51 Dose-Related Toxicity

The safety and effectiveness of GLYDO 2% Jelly
depends on proper dosage, correct technique,
adequate precautions, and readiness for
emergencies [see Adverse Reactions (6)]. Careful
and constant monitoring of cardiovascular and
respiratory (adequacy of ventilation) vital signs
and the patient’s state of consciousness should
be performed after application of GLYDO 2%
Jelly. Possible early warning signs of central
nervous system (CNS) toxicity are restlessness,
anxiety, incoherent speech, lightheadedness,
numbness and tingling of the mouth and
lips, metallic taste, tinnitus, dizziness, blurred
vision, tremors, twitching, CNS depression, or
drowsiness. 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.

Use the lowest dosage that results in effective
anesthesia 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.

Patients and healthcare providers should
be instructed to strictly adhere to the
recommended dosage and administration
guidelines as set forth in this package insert.
The management of serious adverse reactions
may require the use of resuscitative equipment,
oxygen, and other resuscitative drugs.

52 Methemoglobinemia

Cases of methemoglobinemia have been
reported in association with local anesthetic
use. Although all patients are at risk for
methemoglobinemia, patients with glucose-
6-phosphate dehydrogenase _ deficiency,
congenital or idiopathic methemoglobinemia,
cardiac or pulmonary compromise, infants
under 6 months of age, and concurrent
exposure to oxidizing agents or their
metabolites are more susceptible to
developing clinical manifestations of the
condition [see Drug Interactions (7.2)]. If local
anesthetics must be used in these patients,
close monitoring for symptoms and signs of
methemoglobinemia is recommended.

Signs of methemoglobinemia may occur
immediately or may be delayed some hours
after exposure, and are characterized by a
cyanotic skin discoloration and/or abnormal
coloration of the blood. Methemoglobin levels
may continue to rise; therefore, immediate
treatment is required to avert more serious
central nervous system and cardiovascular

plasma levels, which may be due to overdosage
or slow metabolic degradation.

The most commonly encountered acute
adverse reactions that demand immediate
counter measures were related to the CNS
and the cardiovascular system. These adverse
experiences are, in general, dose-related and
may result from high plasma levels caused by
excessive dosage or rapid absorption, 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.

There have been rare reports of endotracheal
tube occlusion associated with the presence of
dried jelly residue in the inner lumen of the tube.

Nervous System Disorders
Adverse reactions were characterized by

excitation and/or depression of the central
nervous system and included lightheadedness,
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.

Cardiac Disorders

High doses have led to high plasma levels
and related depression of the myocardium,
decreased cardiac output, heartblock,
hypotension, bradycardia, and cardiovascular
collapse, which may lead to cardiac arrest.

Immune System Disorders

Allergic reactions are characterized by
cutaneous lesions, urticaria, edema, or
anaphylactoid reactions. Allergic reactions may
occur as a result of sensitivity either to the local
anesthetic agent or to other components in the
formulation.

7 DRUG INTERACTIONS

71 Local Anesthetics

The toxic effects of local anesthetics are
additive. If coadministration of other local
anesthetics with GLYDO 2% Jelly cannot be
avoided, monitor patients for neurologic
and cardiovascular effects related to local
anesthetic systemic toxicity [see Warnings and
Precautions (5.1)].

7.2 Drugs Associated with
Methemoglobinemia
Patients who are administered local

anesthetics are at increased risk of developing
methemoglobinemia when concurrently
exposed to the following drugs, which
could include other local anesthetics:

Examples of Drugs Associated with
Methemoglobinemia:

Class Examples
Nitrates/Nitrites | nitric oxide, nitroglycerin,
nitroprusside, nitrous oxide
Local articaine, benzocaine,
anesthetics bupivacaine, lidocaine,

mepivacaine, prilocaine,
procaine, ropivacaine,
tetracaine

cyclophosphamide,

Antineoplastics

Agents flutamide, hydroxyurea,
ifosfamide, rasburicase
Antibiotics dapsone, nitrofurantoin,

para-aminosalicylic acid,
sulfonamides
Antimalarials chloroquine, primaquine
Anticonvulsants | Phenobarbital, phenytoin,
sodium valproate
acetaminophen,

metoclopramide, quinine,
sulfasalazine

Other drugs

8 USE IN SPECIFIC POPULATIONS

8.1 Pregnancy

Risk Summary

Available published data and decades of clinical
use with GLYDO 2% Jelly in pregnant women
have not identified any drug-associated risk
for major birth defects, miscarriage, or other
adverse maternal or fetal outcomes. Local
anesthetics may cause varying degrees of
toxicity to the mother and fetus and adverse
reactions include alterations of the central
nervous system, peripheral vascular tone and
cardiac function {see Clinical Considerations].

There was no evidence of teratogenicity when
lidocaine was administered to pregnant rats and
rabbits subcutaneously at 0.8 and 0.16 times,
respectively, the maximum recommended
human dose (MRHD) of 600 mg during the
period of organogenesis. In a published animal
reproduction study, pregnant rats administered
lidocaine by continuous subcutaneous infusion
at 8 times the MRHD during the period of
organogenesis resulted in lower fetal body
weights [see Data].

The background risk of major birth defects
and miscarriage for the indicated population is
unknown. All pregnancies have a background
risk of birth defect, loss, or other adverse
outcomes. In the U.S. general population, the
estimated background risks of major birth
defects and miscarriage in clinically recognized
pregnancies is 2 to 4% and 15 to 20%, respectively.

Clinical Considerations

Maternal adverse reactions

During treatment of systemic toxicity, which
may appear as maternal hypotension or
fetal bradycardia, the parturient should be
maintained in the left lateral decubitus position
if possible or manual displacement of the
uterus off the great vessels be accomplished.
Elevating the patient’s legs will also help prevent
decreases in blood pressure. The fetal heart rate
also should be monitored continuously, and
electronic fetal monitoring is highly advisable.

Labor or delivery

Local anesthetics rapidly cross the placenta and
can cause varying degrees of maternal, fetal and
neonatal toxicity {see Clinical Pharmacology
(12.3)]. The incidence and degree of toxicity
depend upon the procedure performed,
the type and amount of drug used, and the
technique of drug administration. Adverse
reactions in the parturient, fetus and neonate
involve alterations of the central nervoussystem,
peripheral vascular tone, and cardiac function.
However, dosage recommendations for local
anesthesia are much lower than dosage
recommendations for other major blocks.

Data

Animal Data

Reproduction studies for lidocaine have been
performed in both rats and rabbits. There was
no evidence of harm to the fetus when pregnant
rats were given subcutaneous doses of up to
50 mg/kg lidocaine (approximately 0.8 times
the MRHD of 600 mg based on body surface
area (BSA) comparison) during the period
of organogenesis. In addition, there was no
evidence of harm to the fetus when pregnant
rabbits were given a subcutaneous dose of
5 mg/kg (approximately 0.16 times the MRHD
based on BSA comparison) during the period of
organogenesis. Treatment of pregnant rabbits
with 25 mg/kg (approximately 0.8 times the
MRHD based on BSA comparison) produced
evidence of maternal toxicity and evidence of
delayed fetal development, including a non-
significant decrease in fetal weight (7%) and an
increase in minor skeletal anomalies (skull and
sternebral defect, reduced ossification of the
phalanges).

The effect of lidocaine on _ post-natal
development was examined in rats by treating
pregnant female rats daily subcutaneously at
doses of 2, 10, and 50 mg/kg (approximately
0.03, 0.16, and 0.8 times, respectively, the MRHD
based on BSA comparison) from Day 15 of
pregnancy and up to 20 days postpartum. No
signs of adverse effects were seen either in
dams or in the pups up to and including the
dose of 10 mg/kg; however, the number of

vital signs and the patient’s state of
consciousness after each local anesthetic
administration. 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, 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 patient airway or if prolonged
ventilatory support (assisted or controlled) is
indicated.

Dialysis is of negligible value in the treatment of
acute overdosage with lidocaine.

1 DESCRIPTION

GLYDO (lidocaine HCl jelly, USP) 2% is a
sterile aqueous product that contains a local
anesthetic agent and is administered topically
(see INDICATIONS AND USAGE for specific
uses).

GLYDO (lidocaine HCI jelly, USP) 2%
contains lidocaine HCl which is chemically
designated as acetamide, 2-(diethylamino)-
N-(2,6-dimethylphenyl)-, | monohydrochloride,
the molecular weight is 270.8. The molecular
formula is C,,H2CIN,O, and has the following
structural formula:

CH, CoH
NH-CO-CH.-N @ ul
\
CoH
CH als

GLYDO (lidocaine HCl jelly, USP) 2% also
contains hypromellose, and the resulting
mixture maximizes contact with mucosa and
provides lubrication for instrumentation. The
unused portion should be discarded after initial
use,

Composition of GLYDO (lidocaine HCl jelly, USP)
2% 6 mL or Tl mL syringes: Each mL contains
20 mg of lidocaine HCI. The formulation also
contains hypromellose, and sodium hydroxide
to adjust pH to 6.0 to 7.0.

12 CLINICAL PHARMACOLOGY

12.1 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.

12.2 Pharmacodynamics
The onset of action is 3 to 5 minutes. It is
ineffective when applied to intact skin.

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.

weeks prior to mating, and reproductive effects
were assessed. Rats dosed up to 250 mg/kg/
day (approximately 4 times the MRHD based
on BSA comparison) showed no effects on
copulatory rate, pregnancy rate, numbers of
corpora lutea, or implantations.

16 HOW SUPPLIED/STORAGE
AND HANDLING

GLYDO? (lidocaine HCl jelly, USP) 2% is supplied
as follows:

surviving pups was reduced at 50 mg/kg, both
at birth and the duration of lactation period, the
effect most likely being secondary to maternal
toxicity. No other effects on litter size, litter
weight, abnormalities in the pups and physical
developments of the pups were seen in this
study.

A second study examined the effects of
lidocaine on post-natal development in the rat
that included assessment of the pups from
weaning to sexual maturity. Rats were treated
for 8 months with 10 or 30 mg/kg, s.c. lidocaine
(approximately 0.8 and 1.6 times, respectively,
the MRHD based on BSA comparison). This
time period encompassed 3 mating periods.
There was no evidence of altered post-natal
development in any offspring; however, both
doses of lidocaine significantly reduced the
average number of pups per litter surviving
until weaning of offspring from the first
2 mating periods.

In a published study, lidocaine administered
to pregnant rats by continuous subcutaneous
infusion during the period of organogenesis at
100, 250, and 500 mg/kg/day, did not produce
any structural abnormalities, but did result
in lower fetal weights at 500 mg/kg/day dose
(approximately 8 times the MRHD based on
BSA comparison) in the absence of maternal
toxicity.

8.2 Lactation

Risk Summary

Published data report the presence of lidocaine
and its metabolites in human milk in low
amounts, along with poor oral bioavailability.
There are no data on the effect of lidocaine
on the breastfed infant or the effect on milk
production.

The developmental and health benefits of
breastfeeding should be considered along
with the mother’s clinical need for GLYDO 2%
Jelly and any potential adverse effects on the
breastfed child from GLYDO 2% Jelly or from
the underlying maternal condition.

84 Pediatric Use

Although the safety and effectiveness of GLYDO
2% Jelly in pediatric patients have not been
established, a study of 19 premature neonates
(gestational age <33 weeks) found nocorrelation between the plasma concentration of lidocaine or monoethylglycinexylidide and infant body weight when moderate amounts of lidocaine (ie. 0.3 mL/kg of lidocaine gel 20 mg/mL) were used for lubricating both intranasal and endotracheal tubes. No neonate had plasma levels of lidocaine above 750 mcg/L. Dosages in children should be reduced, commensurate with age, body weight, and physical condition [see Dosage and Administration (2)]. 85 Geriatric Use Elderly patients should be given reduced doses commensurate with their age and physical condition. 8.6 Hepatic Impairment Amide-type local anesthetics such as lidocaine are metabolized by the liver. Patients with severe hepatic impairment, because of their inability to metabolize local anesthetics normally, are at greater risk of developing toxic plasma concentrations and potentially local anesthetic systemic toxicity. Therefore, consider reduced dosing and increased monitoring for local anesthetic systemic toxicity in patients with hepatic impairment treated with GLYDO 2% Jelly especially with repeat doses [see Warnings and Precautions (5.6)]. 10 OVERDOSAGE Acute emergencies from local anesthetics are generally related to high plasma levels encountered during therapeutic use of local anesthetics [see Warnings and Precautions (5) and Adverse Reactions (6)]. Tne use of this product concomitantly with other lidocaine products should be done with caution and appropriate patient monitoring. Management of Local Anesthetic Emergencies The first consideration is prevention, best accomplished by careful and constant monitoring of cardiovascular and respiratory Factors such as acidosis and the use of CNS stimulants and depressants affect the CNS levels of lidocaine hydrochloride required to produce overt systemic effects. Objective adverse manifestations become increasingly apparent with increasing venous plasma levels above 6 mcg free base per mL. In the rhesus monkey arterial blood levels of 18 to 21 meg/mL have been shown to be threshold for convulsive activity. 12.3 Pharmacokinetics Absorption 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 little intact drug may appear in the circulation because of biotransformation in the liver. Distribution The plasma binding of lidocaine is dependent on drug concentration, and the fraction bound decreases with increasing concentration. At concentrations of 1to 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-l-acid glycoprotein. Lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion. Elimination Lidocaine is metabolized rapidly by the liver, and metabolites and unchanged drug are excreted by the kidneys. Biotransformation includes oxidative N-dealkylation, ring hydroxylation,cleavageoftheamidelinkage,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 of lidocaine metabolism following intravenous bolus injections have shown that the elimination half-life of this agent is typically 15 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 twofold or more in patients with liver dysfunction. Renal dysfunction does not affect lidocaine kinetics but may increase the accumulation of metabolites. 13 NONCLINICAL TOXICOLOGY 13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis Long-term studies in animals have not been performed to evaluate the carcinogenic potential of lidocaine. Mutagenesis The mutagenic potential of lidocaine has been tested in the Ames Salmonella reverse mutation assay, an in vitro chromosome aberrations assay in human lymphocytes and in an in vivo mouse micronucleus assay. There was no indication of any mutagenic effect in these studies. Impairment of Fertility The effect of lidocaine on fertility was examined in the rat model. Administration of 30 mg/kg, s.c. (approximately 0.5 times the MRHD based on BSA comparison) to the mating pair did not produce alterations in fertility or general reproductive performance of rats. There are no studies that examine the effect of lidocaine on sperm parameters. There was no evidence of altered fertility. In a published study, female Sprague-Dawley rats were treated subcutaneously with lidocaine via osmotic pumps starting two INSTRUCTIONS FOR USE Please note: The blister package contains a sterile syringe. Do not open the blister until ready to use. When ready to use, open the blister and drop the syringe onto a sterile field. Before removing the tip cap, press in the plunger to remove any resistance that may be present. This helps ensure that the syringe will empty easily and uniformly. Storage Conditions Store at 20° to 25°C (68° to 77°F} [See USP Controlled Room Temperature]. Discard unused portion. Sterile, Preservative-free, PVC-free. The container and container closure are not made with natural rubber latex. 17 PATIENT COUNSELING INFORMATION 71 Allergic-Type Reactions Assess if the patient has had allergic-type reactions to amide-type local anesthetics or to other formulation ingredients fsee Contraindications (4), Warnings and Precautions (5.6), Adverse Reactions (6)]. 17.2 Methemoglobinemia Inform patients that use of local anesthetics may cause methemoglobinemia, a serious condition that must be treated promptly. Advise patients or caregivers to stop use and seek immediate medical attention if they or someone in their care experience the following signs or symptoms: pale, gray, or blue colored skin (cyanosis); headache; rapid heart rate; shortness of breath; lightheadedness; or fatigue [see Warnings and Precautions (5.2)]. 17.3 Risk of Aspiration 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. 17.4 Risk of Biting Trauma Numbness of the tongue or buccal mucosa may enhance the danger of unintentional biting trauma. Food and chewing gum should not be taken while the mouth or throat area is anesthetized. Brands listed are the trademarks of their respective owners. sagent Mfd. for SAGENT Pharmaceuticals Schaumburg, IL 60173 (USA) Mfd. by Klosterfrau Berlin GmbH Made in Germany ©2025 Sagent Pharmaceuticals Revised: May 2025 NDC GLYDO® Package “Tip Cap lidocaine HCI | Factor / Jelly, USP) 2% (20 mg per mL) 25021-673-76 | 120 mg per 10 syringes per 6mLSingle- | carton Dose Prefilled Syringe 25021-673-77 | 220 mg per 10 syringes per 3. Remove the tip cap from the syringe. The TimL Single- | carton syringe is now ready for use. Dose Prefilled Syringe GLYDO (lidocaine HCl jelly, USP) 2% should be instilled slowly and evenly into the urethra. See the DOSAGE AND ADMINISTRATION section for additional details. MALE N Urethra 5, Wait for a few minutes after instillation of GLYDO (lidocaine HCl jelly, USP) 2% for the anesthetic to take full effect. Full anesthetic effect will occur in 5 to 10 minutes after complete instillation. Any gel not used ina single application must be discarded. sagent Mfd. for SAGENT Pharmaceuticals Schaumburg, IL 60173 (USA) Mfd. by Klosterfrau Berlin GmbH Made in Germany ©2025 Sagent Pharmaceuticals 05P0525 220005091 Revised: May 2025 This “Instructions for Use” has been approved by the U.S. Food and Drug Administration. [/scroller]