lidocaine topical (Lidoderm, Xylocaine Jelly, Xylocaine Topical Solution, AneCream, AneCream5, Derma Numb, Epic, Hawaiian Tropic Gel, Lidocoll, LidoRx, LidoStat, LMX4, Premjact, Promescent, Regenecare HA, Solarcaine Aloe Extra Burn Relief, Topicaine, Xolido, Lidocare Patch)
Dosing and uses of Lioderm, Xylocaine Jelly (lidocaine topical)
Adult dosage forms and strengths
transdermal patch
- 5% (Lidoderm; Rx)
- 4% (Lidocare Patch; OTC)
topical jelly
- 2% (Xylocaine Jelly)
topical geL
- 0.5% (Solarcaine Aloe Extra Burn Relief)
- 0.8% (Hawaiian Tropic Gel)
- 3% (LidoRx)
- 4% (Topicaine)
topical cream
- 2% (Xolido) 4%
- (AneCream, LidoStat, LMX4, Xolido)
- 5% (AneCream5)
topical ointment
- 5%
topical lotion
- 3%
topical spray
- 2% (Regenecare HA)
- 4% (Derma Numb, Lidocoll)
- 10mg/spray (Epic, Premjact, Promescent)
topical solution, mouth/throat
- 2%
- 4% (Xylocaine Solution)
Postherpetic Neuralgia Pain
Transdermal patch: Apply to intact skin to cover the most painful area
Apply up to 3 patches, only once for up to 12 hr within a 24-hr period
Patches may be cut into smaller sizes with scissors prior to removal of the release liner
Clothing may be worn over the area of application
Smaller areas of treatment are recommended in a debilitated patient, or a patient with impaired elimination
Patches may not stick if wet; avoid contact with water such as bathing, swimming, or showering
Anesthetic Lubricant for Intubation
Indicated as an anesthetic lubricant for oral or nasal endotracheal intubation
Jelly (2%): Apply moderate amount to external surface of endotracheal tube shortly before use
Ointment: Apply to tube prior to intubation
Not to exceed 600 mg/12 hr
Urethral Surface Anesthesia
When using Xylocaine 2% Jelly 30 mL tubes for urologic procedures, sterilize the plastic cone for 5 minutes in boiling water, cool, and attach to the tube
Females
- Instill 2-5 mL jelly (60-100 mg) into urethra
- Some jelly may also be deposited on a cotton swab and introduced into urethra
- Allow several minutes following instillation prior to performing urological procedure
Males
- Slowly instill 15 mL (300 mg lidocaine) into urethra or until patient experiences tension
- Apply a penile clamp for several minutes at the corona
- An additional dose of not more than 15 mL (300 mg) can be instilled for adequate anesthesia
- Prior to sounding or cystoscopy, a penile clamp should be applied for 5-10 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, smaller volumes of 5-10 mL (100-200 mg) are usually adequate for lubrication
Premature Ejaculation
Temporarily reduces sensitivity of the penis, which helps to delay ejaculation
Epic, Premject, Promescent: Apply 3 or more sprays (10 mg/spray), not to exceed 10 sprays, to the head and shaft of the penis before intercourse
Wash product off after intercourse
Correct quantity and time of application will be determined by individual requirements; use the minimum effective quantity
Do not exceed 24 sprays/24 hr
Skin Irritation
Indicated for temporary relief of pain and itching caused by minor skin irritations (eg, sunburn, minor burns, minor cuts, scrapes, insect bites, minor skin irritations)
Apply topically to affected area TID/QId
Pediatric dosage forms and strengths
topical jelly
- 2% (Xylocaine Jelly)
topical geL
- 0.5% (Solarcaine Aloe Extra Burn Relief)
- 0.8% (Hawaiian Tropic Gel)
- 3% (LidoRx)
- 4% (Topicaine)
topical cream
- 2% (Xolido) 4%
- (AneCream, LidoStat, LMX4, Xolido)
- 5% (AneCream5)
topical ointment
- 5%
topical lotion
- 3%
topical spray
- 2% (Regenecare HA)
- 4% (Derma Numb, Lidocoll)
topical solution, mouth/throat
- 2%
- 4% (Xylocaine Solution)
Anesthetic Lubricant for Intubation
Indicated as an anesthetic lubricant for oral or nasal endotracheal intubation
Jelly (2%): Apply moderate amount to external surface of endotracheal tube shortly before use
Ointment: Apply to tube prior to intubation
Children aged <10 years: Not to exceed 4.5 mg/kg per 12 hr
Older children/adolescents: Not to exceed 600 mg/12 hr
Skin Irritation
Indicated for temporary relief of pain and itching caused by minor skin irritations (eg, sunburn, minor burns, minor cuts, scrapes, insect bites, minor skin irritations)
<2 years: Safety and efficacy not established
≥2 years: Apply topically to affected area TID/QId
Lioderm, Xylocaine Jelly (lidocaine topical) adverse (side) effects
Frequency not defined
Cardiovascular (with excessive systemic absorption): CV depressant effect characterized by bradycardia, hypotension, and cardiovascular collapse, which may lead to cardiac arrest
Allergic: Cutaneous lesions, urticaria, edema, or anaphylactoid reactions
Central nervous system
- CNS manifestations are excitatory and/or depressant and may be characterized by 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
- 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
Warnings
Black box warnings
Significant systemic absorption may occur with topical use
Twenty-two case reports have shown evidence of serious adverse reaction when viscous lidocaine 2% is used in young children to treat mouth pain
Resulting reactions include seizures, severe brain injury, and cardiovascular depression characterized by bradycardia, hypotension, and cardiovascular collapse, which may lead to cardiac arrest
Contraindications
Hypersensitivity to drug or amide type anesthetic
Cautions
Some formulations may contain sulfites
Contact with eye may cause severe eye irritation; if eye contact occurs, immediately wash out the eye with water or saline and protect eye until sensation returns
Patients with severe hepatic disease are at greater risk of developing toxic blood concentrations of lidocaine due to inability to metabolize lidocaine normally
When used concomitantly with other products containing local anesthetic agents, the amount of lidocaine absorbed from all formulations must be considered
Dispose of used lidocaine patches properly to avoid toxicity in small children or pets; used lidocaine patches contains a large amount of lidocaine (at least 665 mg)
Application to broken or inflamed skin, although not tested, may result in higher blood concentrations of lidocaine from increased absorption; apply only to intact skin
Jelly for endotracheal use
- When used for endotracheal tube lubrication care should be taken to avoid introducing the jelly 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
Excessive systemic absorption
- External heat sources (eg, heating pads, electric blanket) may increase systemic absorption from transdermal patch
- Sepsis, severely traumatized mucosa, or open wounds in the area of application (potential for rapid systemic absorption)
- Doses applied to large surface areas that remain on the skin for >2 hr
- Repeated doses with short dosing intervals
2% Viscous solution
- Parents and caregivers should be cautioned about the following:
- Use special care for patients <3 years of age to accurately measure prescribed dose and not to administer product more often than prescribed
- Use a measuring device to carefully measure correct volume
- Use product for prescribed indication only
- Keep product container should be tightly closed and product stored well out of reach of all children immediately after each use
- If patient shows signs of systemic toxicity (e.g., lethargy, shallow breathing, seizure activity) seek emergency medical attention immediately with no additional product administered
- Discard unused product in manner that prevents possible exposure to children and pets
- When topical anesthetics used in mouth or throat, production of topical anesthesia may impair swallowing and thus enhance danger of aspiration; food should not be ingested for 60 min following use of local anesthetic preparations in mouth or throat area especially in children because of their frequency of eating; numbness of tongue or buccal mucosa may increase danger of biting trauma (food and/or chewing gum should not be used while mouth or throat area is anesthetized)
Pregnancy and lactation
Pregnancy category: B
Lactation: Distributed in human breast milk; caution advised
Pregnant or breastfeeding patients should seek advice of health professional before using OTC drugs
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Lioderm, Xylocaine Jelly (lidocaine topical)
Mechanism of action
Elicits local anesthesia; stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action
Absorption
Onset of action: 3-5 minutes (eg, gel, cream, ointment)
Peak plasma time (transdermal patch): 11 hr
Peak plasma concentration (3 transdermal patches): 0.13 mcg/mL
Distribution
Protein bound: 70% (transdermal patch)
Vd: 0.7-2.7 L/kg (transdermal patch)
Metabolism
It is not known if lidocaine is metabolized in the skin
Lidocaine is metabolized rapidly by the liver to a number of metabolites, including monoethylglycinexylidide (MEGX) and glycinexylidide (GX), both of which have pharmacologic activity similar to, but less potent than that of lidocaine
Elimination
Half-life: 81-149 minutes (IV)
Total body clearance: 0.33-0.9 L/min
Excretion: Kidneys (<10% unchanged)
