Dosing & Uses
Dosage Forms & Strengths
lidocaine/prilocaine
cream (EMLA)
- (2.5%/2.5%)/30g
dental gel (Oraqix)
- 2.5%/2.5%
Dermal Procedures
Minor dermatological procedures
- Cream: Apply 2.5 g over 20-25 cm² of skin surface area for at least 1 hr
Painful dermatological procedures involving large areas (eg, split thickness skin graft harvesting)
- Cream: Apply 2 g/10 cm² of skin and allow to remain in contact with the skin for at least 2 hr
- Analgesia is achieved in 1 hr, reaches maximum in 2-3 hr, and persists 1-2 hr after removal
Topical Anesthetic on Genital Mucous Membranes
Superficial minor surgery on male genitalia and as pretreatment for infiltration anesthesia
- Cream: Apply 1 g/10 cm² of skin for 15 min
Minor procedures on the female external genitalia (eg, condylomata acuminata) as well as for use as pretreatment for anesthetic infiltration
- Cream: Apply 5-10 g for 5-10 min
Dental Procedures
Localized anesthesia in periodontal pockets during scaling and/or root planing
Dental gel: Apply one cartridge or less for one quadrant of dentition; do not exceed 5 cartridges per treatment session
Dosing Considerations
Cream
- Gently squeeze cream out of the tube as a narrow strip that is 1.5 inches long and 0.2 inches wide; 1 strip corresponds to 1 g
- Perform local anesthetic infiltration immediately after removal of cream
- Male genital skin: Analgesia will increase up to 3 hours under occlusive dressing and persist 1-2 hours after cream removal
- Female genital skin: Occlusive dressing is not necessary but will keep cream in place
Dental gel
- Anesthetic effect lasts approximately 20 minute; if effect wears off, reapply if needed; one cartridge or less is sufficient for one quadrant of dentition
Administration
Cream
- Apply a thick layer to intact skin and cover with occlusive dressing
- Female genital skin: Patient should be lying down during administration, especially if no occlusion is used
Dental gel
- Do not inject; only use product with blunt-tipped applicator
- Apply on gingival margin around selected teeth using the blunt–tipped applicator included in package; wait 30 seconds, and fill the periodontal pockets with gel using the blunt–tipped applicator until it becomes visible at the gingival margin; wait another 30 seconds before starting treatment
- If a gel has formed, place in refrigerator (do not freeze) until it becomes a liquid again; only administer when it is a liquid
Other Indications & Uses
Provides dermal analgesia through intact skin by release of local anesthetics through epidermis
Dosage Forms & Strengths
lidocaine/prilocaine
cream (EMLA)
- (2.5%/2.5%)/30g
dental gel (Oraqix)
- 2.5%/2.5%
Local Anesthetic Procedures
Cream
- Neonates (gestation age <37 weeks): Use not recommended
- <12 months: Do not use if receiving treatment with methemoglobinemia-inducing agents
- 0-3 months (or <5 kg): Do not exceed 1 g total dose/application area > 10 cm²/>1 hr application time
- 3-12 months (and >5 kg): Do not exceed 2 g total dose/application area > 20 cm²/>4 hr application time
- 1-6 years (and >10 kg): Do not exceed 10 g total dose/application area > 100 cm²/>4 hr application time
- 7-12 years (and >20 kg): Do not exceed 20 g total dose/application area > 200 cm²/>4 hr application time
Dosing Considerations
Cream
- If patient >3 months does not meet minimum weight requirement, total dose should correspond to patient’s weight
- Care must be taken to avoid accidental ingestion of cream; use secondary protective covering to present disruption of application site
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (5)
- bupivacaine liposome
lidocaine increases toxicity of bupivacaine liposome by Other (see comment). Contraindicated. Comment: Do not admix with other local nonbupivacaine-based local anesthetics; admixing results in a rapid increase in free (unencapsulated) bupivacaine; may administer after waiting at least 20 minutes following local administration of lidocaine.
- dofetilide
lidocaine increases effects of dofetilide by pharmacodynamic synergism. Contraindicated. Additive cardiac effects.
- eliglustat
lidocaine increases levels of eliglustat by affecting hepatic enzyme CYP2D6 metabolism. Contraindicated. If coadministered with strong or moderate CYP2D6 inhibitors, reduce eliglustat dose from 84 mg BID to 84 mg once daily in extensive and intermediate metabolizers; eliglustat is contraindiated if strong or moderate CYP2D6 inhibitors are given concomitantly with strong or moderate CYP3A inhibitors.
- flibanserin
lidocaine will increase the level or effect of flibanserin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration of flibanserin with moderate or strong CYP3A4 inhibitors is contraindicated. Severe hypotension or syncope can occur.
- lomitapide
lidocaine increases levels of lomitapide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Increases lomitapide levels several folds.
Serious - Use Alternative (5)
- abametapir
abametapir will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP1A2 substrates. If not feasible, avoid use of abametapir.
- axitinib
lidocaine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration with moderate CYP3A4 inhibitors, monitor closely and reduce dose if necessary .
- bosutinib
lidocaine increases levels of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- bupivacaine implant
prilocaine, bupivacaine implant. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid additional local anesthetic administration within 96 hr following bupivacaine implantation. If use of additional local anesthetics is unavoidable based on clinical need, monitor for neurologic and cardiovascular effects related to local anesthetic systemic toxicity.
- cobimetinib
lidocaine will increase the level or effect of cobimetinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concurrent short term (14 days or less) use of moderate CYP3A inhibitors is unavoidable for patients who are taking cobimetinib 60 mg, reduce the cobimetinib dose to 20 mg. After discontinuation of a moderate CYP3A inhibitor, resume cobimetinib 60 mg. Use an alternative to a moderate CYP3A inhibitor in patients who are taking a reduced dose of cobimetinib (40 or 20 mg daily).
Monitor Closely (73)
- amiodarone
amiodarone increases levels of lidocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Higher doses of amiodarone (ie, 600 mg BID) were shown to significantly increase lidocaine levels.
- amobarbital
amobarbital will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- armodafinil
armodafinil will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- avapritinib
lidocaine will increase the level or effect of avapritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- bosutinib
bosutinib increases levels of lidocaine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- brexpiprazole
lidocaine will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP2D6 inhibitor PLUS a strong/moderate CYP3A4 inhibitor.
lidocaine will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor. - butabarbital
butabarbital will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- butalbital
butalbital will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- cabozantinib
lidocaine will increase the level or effect of cabozantinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- cannabidiol
cannabidiol, lidocaine. affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Owing to the potential for both CYP1A2 induction and inhibition with the coadministration of CYP1A2 substrates and cannabidiol, consider reducing dosage adjustment of CYP1A2 substrates as clinically appropriate.
- carbamazepine
carbamazepine will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- cigarette smoking
cigarette smoking will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- cimetidine
cimetidine will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- ciprofloxacin
ciprofloxacin will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Lidocaine plasma levels may be elevated, increasing the risk of toxicity. Monitor cardiac function and symptoms of toxicity.
- cobicistat
cobicistat will increase the level or effect of lidocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Clinical monitoring is recommended upon coadministration with antiarrhythmics.
- darunavir
darunavir increases levels of lidocaine by decreasing metabolism. Use Caution/Monitor. Clinical monitoring is recommended upon coadministration with antiarrhythmics.
- disopyramide
disopyramide, lidocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Risk of arrhythmia, heart failure in predisposed pts.
- duvelisib
duvelisib will increase the level or effect of lidocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with duvelisib increases AUC of a sensitive CYP3A4 substrate which may increase the risk of toxicities of these drugs. Consider reducing the dose of the sensitive CYP3A4 substrate and monitor for signs of toxicities of the coadministered sensitive CYP3A substrate.
- eliglustat
eliglustat increases levels of lidocaine by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Monitor therapeutic drug concentrations, as indicated, or consider reducing the dosage of the P-gp substrate and titrate to clinical effect.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of lidocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Cobicistat is a CYP3A4 inhibitor; contraindicated with CYP3A4 substrates for which elevated plasma concentrations are associated with serious and/or life-threatening events.
- encorafenib
encorafenib, lidocaine. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.
- erythromycin base
erythromycin base will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- erythromycin stearate
erythromycin stearate will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- fexinidazole
fexinidazole will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- finerenone
lidocaine will increase the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or weak CYP3A4 inhibitors. Adjust finererone dosage as needed.
- fostamatinib
fostamatinib will increase the level or effect of lidocaine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of P-gp substrates. Monitor for toxicities of the P-gp substrate drug that may require dosage reduction when given concurrently with fostamatinib.
- glecaprevir/pibrentasvir
glecaprevir/pibrentasvir will increase the level or effect of lidocaine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- hawthorn
hawthorn increases effects of lidocaine by pharmacodynamic synergism. Use Caution/Monitor.
- hyaluronidase
hyaluronidase, lidocaine. Other (see comment). Use Caution/Monitor. Comment: Hyaluronidase hastens the onset of local analgesia and reduces swelling, but increases systemic absorption of anesthetic. This decreases the duration of action and increases incidence of systemic reaction.
- isoniazid
isoniazid will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- ivacaftor
ivacaftor increases levels of lidocaine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Ivacaftor and its M1 metabolite has the potential to inhibit P-gp; may significantly increase systemic exposure to sensitive P-gp substrates with a narrow therapeutic index.
ivacaftor increases effects of lidocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - lemborexant
lidocaine will increase the level or effect of lemborexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Lower nightly dose of lemborexant recommended if coadministered with weak CYP3A4 inhibitors. See drug monograph for specific dosage modification.
- letermovir
letermovir increases levels of lidocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lomitapide
lomitapide increases levels of lidocaine by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Consider reducing dose when used concomitantly with lomitapide.
- mefloquine
lidocaine will increase the level or effect of mefloquine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mexiletine
mexiletine will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- midazolam intranasal
lidocaine will increase the level or effect of midazolam intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of mild CYP3A4 inhibitors with midazolam intranasal may cause higher midazolam systemic exposure, which may prolong sedation.
- modafinil
modafinil will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- nadolol
nadolol, lidocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Increased effects of epinephrine in anesthetic; risk of hypertension and bradycardia. Do NOT D/C chronic beta blocker Tx prior to anesthetic administration. Consider selective beta 1 blocker (e.g., metoprolol).
nadolol, prilocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Use extreme caution during concomitant use of bupivacaine and antihypertensive agents.
nadolol increases levels of lidocaine by decreasing elimination. Use Caution/Monitor. Risk of hypertension and bradycardia. Consider selective beta 1 blocker (e.g., metoprolol). - nevirapine
nevirapine will decrease the level or effect of lidocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- phenazopyridine
phenazopyridine increases toxicity of prilocaine by Other (see comment). Modify Therapy/Monitor Closely. Comment: Phenazopyridine may significantly increase risk of methemoglobinemia when coadministered with prilocaine. Monitor patients closely.
- oliceridine
lidocaine will increase the level or effect of oliceridine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. If concomitant use is necessary, may require less frequent oliceridine dosing. Closely monitor for respiratory depression and sedation and titrate subsequent doses accordingly. If inhibitor is discontinued, consider increase oliceridine dosage until stable drug effects are achieved. Monitor for signs of opioid withdrawal.
- ombitasvir/paritaprevir/ritonavir & dasabuvir
ombitasvir/paritaprevir/ritonavir & dasabuvir will increase the level or effect of lidocaine by decreasing metabolism. Modify Therapy/Monitor Closely. Caution is warranted and therapeutic concentration monitoring (if available) is recommended for antiarrhythmics when coadministered with Viekira Pak
- palbociclib
lidocaine will increase the level or effect of palbociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- peginterferon alfa 2a
peginterferon alfa 2a will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- pentobarbital
pentobarbital will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- phenobarbital
phenobarbital will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- pindolol
pindolol increases levels of lidocaine by decreasing elimination. Use Caution/Monitor. Risk of hypertension and bradycardia. Consider selective beta 1 blocker (e.g., metoprolol).
pindolol, lidocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Increased effects of epinephrine in anesthetic; risk of hypertension and bradycardia. Do NOT D/C chronic beta blocker Tx prior to anesthetic administration. Consider selective beta 1 blocker (e.g., metoprolol).
pindolol, prilocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Use extreme caution during concomitant use of bupivacaine and antihypertensive agents. - pipemidic acid
pipemidic acid will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- propranolol
propranolol, prilocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Use extreme caution during concomitant use of bupivacaine and antihypertensive agents.
- ponatinib
ponatinib increases levels of lidocaine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- primidone
primidone will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- procainamide
lidocaine, procainamide. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Either suppresses myocardial conduction by increasing electrical stimulation threshold of the ventricle and His-Purkinje fibers.
- propranolol
propranolol, lidocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Increased effects of epinephrine in anesthetic; risk of hypertension and bradycardia. Do NOT D/C chronic beta blocker Tx prior to anesthetic administration. Consider selective beta 1 blocker (e.g., metoprolol).
propranolol increases levels of lidocaine by decreasing elimination. Use Caution/Monitor. Risk of hypertension and bradycardia. Consider selective beta 1 blocker (e.g., metoprolol). - rifampin
rifampin will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- rucaparib
rucaparib will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP1A2 substrates, if clinically indicated.
- ruxolitinib
lidocaine will increase the level or effect of ruxolitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- secobarbital
secobarbital will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- sevelamer
sevelamer decreases levels of lidocaine by increasing elimination. Use Caution/Monitor.
- smoking
smoking will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- sonidegib
lidocaine will increase the level or effect of sonidegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of sonidegib with moderate CYP3A4 inhibitors. If a moderate CYP3A inhibitor must be used, administer the moderate CYP3A inhibitor for <14 days and monitor closely for adverse reactions, particularly musculoskeletal adverse reactions.
- stiripentol
stiripentol, lidocaine. affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP1A2 inhibitor and inducer. Monitor CYP1A2 substrates coadministered with stiripentol for increased or decreased effects. CYP1A2 substrates may require dosage adjustment.
- suvorexant
lidocaine will increase the level or effect of suvorexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Decrease suvorexant starting dose to 5 mg HS if coadministered with moderate CYP3A4 inhibitors
- tamsulosin
lidocaine increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Dose reduction may be needed for coadministered drugs that are predominantly metabolized by CYP3A.
lidocaine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. - tazemetostat
lidocaine will increase the level or effect of tazemetostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- timolol
timolol, lidocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Increased effects of epinephrine in anesthetic; risk of hypertension and bradycardia. Do NOT D/C chronic beta blocker Tx prior to anesthetic administration. Consider selective beta 1 blocker (e.g., metoprolol).
timolol increases levels of lidocaine by decreasing elimination. Use Caution/Monitor. Risk of hypertension and bradycardia. Consider selective beta 1 blocker (e.g., metoprolol).
timolol, prilocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Use extreme caution during concomitant use of bupivacaine and antihypertensive agents. - tinidazole
lidocaine will increase the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tobacco use
tobacco use will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- tofacitinib
lidocaine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- verapamil
verapamil will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- zileuton
zileuton will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
Minor (13)
- alfentanil
lidocaine increases toxicity of alfentanil by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
- belladonna and opium
lidocaine increases toxicity of belladonna and opium by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
- buprenorphine
lidocaine increases toxicity of buprenorphine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
- buprenorphine buccal
lidocaine increases toxicity of buprenorphine buccal by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
- butorphanol
lidocaine increases toxicity of butorphanol by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
- codeine
lidocaine increases toxicity of codeine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
- dextromoramide
lidocaine increases toxicity of dextromoramide by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
- diamorphine
lidocaine increases toxicity of diamorphine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
- difenoxin hcl
lidocaine increases toxicity of difenoxin hcl by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
- diphenoxylate hcl
lidocaine increases toxicity of diphenoxylate hcl by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
- dipipanone
lidocaine increases toxicity of dipipanone by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
- hyaluronidase
hyaluronidase, prilocaine. Other (see comment). Minor/Significance Unknown. Comment: Hyaluronidase hastens the onset of local analgesia and reduces swelling, but increases systemic absorption of anesthetic. This decreases the duration of action and increases incidence of systemic reaction.
- hydromorphone
lidocaine increases toxicity of hydromorphone by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.
Adverse Effects
>10%
Pallor/blanching (37%)
Application site erythema/pain (30%)
Genital mucous membrane burning sensation (17%)
Oral cavity, periodontal formulation (15%)
1-10%
Alterations in temperature sensations (7%)
Application site edema (6-10%)
Itching (2%)
<1%
Rash
Myocardial dysfunction (rare)
Methemoglobinemia (rare)
Depression/excitation (rare)
Seizure (rare)
Frequency Not Defined
Localized discrete purpuric or petechial reactions (rare)
Localized hyperpigmentation (rare)
Allergic reactions (eg, urticaria, angioedema, bronchospasm, shock)
Warnings
Contraindications
Hypersensitivity to components, amide-type local anesthetics
Cautions
Do not apply on open wounds
Monitor child closely after administration; if child becomes very dizzy, excessively sleepy, or develops duskiness of the face or lips, remove cream immediately
Exercise caution when applying over large areas for >2 hours due to risk of systemic absorption and adverse effects
Monitor patients treated with class III anti-arrhythmic drugs (eg, amiodarone, bretylium, sotalol, dofetilide) due to additive cardiac effects; consider ECG monitoring
Use of cream is not recommended in any clinical situation when penetration or migration beyond tympanic membrane into middle ear is possible due to ototoxic effects observed in animal studies
Avoid in patients with congenital/idiopathic methemoglobinemia, infants <12 months receiving treatment with methemoglobin-inducing agents, patients on drugs associated with drug-induced methemoglobinemia; monitor Met-Hb levels before, during and after application in patients <3 months; treatment with IV methylene blue may be effective
Monitor acutely ill, debilitated, or elderly patients closely if administering repeated doses
Do not apply near eyes as loss of protective reflexes can permit corneal irritation and potential abrasion
Patients with history of drug sensitivities (eg, allergy to paraaminobenzoic acid derivatives)
Severe hepatic disease due to increased risk of toxic plasma concentrations of lidocaine/prilocaine
Lidocaine and prilocaine have been shown to inhibit viral and bacterial growth
Instruct patient to avoid irritating or exposing treated area to extreme temperatures until complete sensation has returned
Methemoglobinemia
- Use of local anesthetics may cause methemoglobinemia, a serious condition that must be treated promptly; 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
- Advise patients or caregivers to seek immediate medical attention if patient experiences the following signs or symptoms: pale, gray, or blue colored skin (cyanosis); headache; rapid heart rate; shortness of breath; lightheadedness; or fatigue; discontinue Bicillin C-R and any other oxidizing agents; depending on severity of signs and symptoms, patients may respond to supportive care, including oxygen therapy and hydration; a more severe clinical presentation may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen
Pregnancy & Lactation
Pregnancy Category: B
Lactation: Excreted in breast milk; use not recommended
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
Mechanism of Action
Amide-type local anesthetics stabilize neuronal membranes and prevent generation/conduction of nerve impulses by reducing sodium permeability and increasing action potential threshold
Absorption
Positively correlated to degree of systemic absorption
Peak plasma concentrations: 148-641 ng/mL (lidocaine); 40-346 ng/mL (prilocaine)
Distribution
Vd (IV administration): 1.1-2.1 L/kg (lidocaine); 0.7-4.4 L/kg (prilocaine)
Protein bound: 70% (lidocaine); 55% (prilocaine)
Metabolism
Unknown if metabolized in skin
Systemic metabolism: hepatic (lidocaine); hepatic/renal (prilocaine)
Metabolites: ester- and amide-type local anesthetics
Elimination
t1/2 (IV administration): 65-150 min (lidocaine); 10-150 min (prilocaine)
Excretion (IV administration): Urine (98%) [lidocaine]
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