lidocaine/prilocaine (Rx)

Brand and Other Names:EMLA, Oraqix
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Dosing & Uses

AdultPediatric

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
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Interactions

Interaction Checker

and lidocaine/prilocaine

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            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.

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            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)

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            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
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            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.

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            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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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.