lidocaine/tetracaine (Rx)

Brand and Other Names:Synera, Pliaglis
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

lidocaine/tetracaine

transdermal patch

  • 70mg/70mg (Synera)

topical cream

  • 7%/7% (Pliaglis)

Local Dermal Analgesia

Venipuncture or IV cannulation

  • Patch: Apply patch to intact skin 20-30 minutes prior to procedure

Superficial dermatological procedures (eg, excision, electrodessication, shave biopsy)

  • Patch: Apply patch to intact skin for 30 minutes prior to procedure

Topical cream

  • Indicated for use on intact skin in adults to provide topical local analgesia for superficial dermatological procedures (eg, dermal filler injection, pulsed dye laser therapy, facial laser resurfacing, laser-assisted tattoo removal)
  • Apply to intact skin 20-30 minutes prior to superficial dermatological procedures (eg, dermal filler injection, facial laser ablation)
  • Apply 60 minutes prior to procedures for laser-assisted tattoo removal or similar procedures
  • Dosage amount determined by surface area of treatment site (see prescribing information for details)

Dosing Considerations

Patch: Contains integrated, oxygen-activated heating component so do not cut patch or remove top cover due to risk of thermal injury; do not cover holes on top side of patch as it will not heat properly

Administration

Patch: Use immediately after opening pouch; only apply to intact skin; wash hands after handling patch

Dosage Forms & Strengths

lidocaine/tetracaine

transdermal patch

  • 70mg/70mg (Synera)

Local Dermal Analgesia

Venipuncture or IV cannulation

  • <3 years: Safety and efficacy not established
  • >3 years (patch): Apply patch to intact skin 20-30 minutes prior to procedure

Superficial dermatological procedures (eg, excision, electrodessication, shave biopsy)

  • <3 years: Safety and efficacy not established
  • >3 years (patch): Apply patch to intact skin for 30 minutes prior to procedure
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Interactions

Interaction Checker

and lidocaine/tetracaine

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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

              tetracaine, 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 (90)

            • acetaminophen

              tetracaine, acetaminophen. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • acetaminophen IV

              tetracaine, acetaminophen IV. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • acetaminophen rectal

              tetracaine, acetaminophen rectal. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • 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.

            • amyl nitrite

              tetracaine, amyl nitrite. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • armodafinil

              armodafinil will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • atogepant

              lidocaine will increase the level or effect of atogepant by affecting hepatic/intestinal enzyme CYP3A4 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.

            • bupivacaine implant

              tetracaine, bupivacaine implant. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Local anesthetics may increase the risk of developing methemoglobinemia when concurrently exposed to drugs that also cause methemoglobinemia.

            • 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.

            • chloroquine

              tetracaine, chloroquine. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • 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.

            • dapsone

              tetracaine, dapsone. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • 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, tetracaine. 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.

              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.

            • isavuconazonium sulfate

              lidocaine will increase the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • isosorbide dinitrate

              tetracaine, isosorbide dinitrate. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • isoniazid

              isoniazid will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • isosorbide mononitrate

              tetracaine, isosorbide mononitrate. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • 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 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.

            • nirmatrelvir

              nirmatrelvir will increase the level or effect of lidocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution warranted. Monitor lidocaine therapeutic concentrations if available.

            • nirmatrelvir/ritonavir

              nirmatrelvir/ritonavir will increase the level or effect of lidocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution warranted. Monitor lidocaine therapeutic concentrations if available.

            • nitrofurantoin

              tetracaine, nitrofurantoin. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • nitroglycerin IV

              tetracaine, nitroglycerin IV. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • nitroglycerin PO

              tetracaine, nitroglycerin PO. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • nitroglycerin sublingual

              tetracaine, nitroglycerin sublingual. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • nitroglycerin topical

              tetracaine, nitroglycerin topical. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • nitroglycerin transdermal

              tetracaine, nitroglycerin transdermal. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • nitroglycerin translingual

              tetracaine, nitroglycerin translingual. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • nitroprusside sodium

              tetracaine, nitroprusside sodium. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • 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 (DSC)

              ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) 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

              tetracaine, phenobarbital. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              phenobarbital will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • phenytoin

              tetracaine, phenytoin. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • pindolol

              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 increases levels of lidocaine by decreasing elimination. Use Caution/Monitor. Risk of hypertension and bradycardia. Consider selective beta 1 blocker (e.g., metoprolol).

            • pipemidic acid

              pipemidic acid will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • ponatinib

              ponatinib increases levels of lidocaine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • primaquine

              tetracaine, primaquine. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • 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).

            • quinine

              tetracaine, quinine. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • 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.

            • ruxolitinib topical

              lidocaine will increase the level or effect of ruxolitinib topical 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.

            • sulfadiazine

              tetracaine, sulfadiazine. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • sulfisoxazole

              tetracaine, sulfisoxazole. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

            • 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

            Minor (27)

            • 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.

            • hydromorphone

              lidocaine increases toxicity of hydromorphone by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • levorphanol

              lidocaine increases toxicity of levorphanol by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • lily of the valley

              lidocaine, lily of the valley. Either increases toxicity of the other by pharmacodynamic synergism. Minor/Significance Unknown.

            • meperidine

              lidocaine increases toxicity of meperidine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • methadone

              lidocaine increases toxicity of methadone by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • morphine

              lidocaine increases toxicity of morphine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • nalbuphine

              lidocaine increases toxicity of nalbuphine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • omeprazole

              omeprazole will decrease the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

            • opium tincture

              lidocaine increases toxicity of opium tincture by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • oxycodone

              lidocaine increases toxicity of oxycodone by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • oxymorphone

              lidocaine increases toxicity of oxymorphone by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • papaveretum

              lidocaine increases toxicity of papaveretum by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • pentazocine

              lidocaine increases toxicity of pentazocine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • sufentanil

              lidocaine increases toxicity of sufentanil by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • tapentadol

              lidocaine increases toxicity of tapentadol by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

            • tramadol

              lidocaine increases toxicity of tramadol by pharmacodynamic synergism. Minor/Significance Unknown. Risk of increased CNS depression.

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            Adverse Effects

            >10%

            Localized erythema (71%)

            Localized blanching (12%)

            Localized edema (12%)

            1-10%

            Other application site reactions (contact dermatitis, rash, skin discoloration) (<4%)

            <1%

            Rash

            Application site reactions

            Pruritus

            Dizziness

            Headache

            Pain

            N/V

            Contact dermatitis

            Infection

            Skin discoloration

            Somnolence

            Allergic reaction

            Blister

            Paresthesia

            Urticaria

            Vesiculobullous rash

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            Warnings

            Contraindications

            Hypersensitivity to drug, components or PABA

            Cautions

            Severe hepatic or pseudocholinesterase deficiency

            Do not use on broken skin or mucous membranes

            Use caution if applied for longer period than recommended

            Produces mild localized warming of skin to facilitate drug absorption

            Simultaneous/successive patches not recommended due to risk of serious adverse effects caused by increased systemic absorption

            Do not apply near eyes as loss of protective reflexes can permit corneal irritation and potential abrasion

            Severe hepatic or pseudocholinesterase deficiency due to increased risk of toxic plasma concentrations of lidocaine/tetracaine

            Lidocaine and prilocaine have been shown to inhibit viral and bacterial growth

            Integrated heating component contains iron; remove patch prior to MRI

            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

            There are no available data on use in pregnant women to determine drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes; available data from an epidemiologic study and case series with parenteral lidocaine use in pregnant women have not identified drug-associated risk of major birth defects, miscarriage or other adverse maternal or fetal outcomes

            Published data on tetracaine use in pregnant women are not sufficient to determine any drug-associated risks; the amount of lidocaine and tetracaine systemically absorbed is low compared to parenteral route of administration and is not expected to result in significant fetal exposure; systemic exposure of drug combination is directly related to both duration of application and surface area over which it is applied

            Animal data

            • In a published animal reproduction study, pregnant rats administered lidocaine by continuous subcutaneous infusion during period of organogenesis resulted in lower fetal body weights at doses approximately 1.3 times the maximum recommended human dose (MRHD) during period of organogenesis
            • In published animal reproduction study, pregnant rats administered lidocaine, containing 1:100,000 epinephrine, injected into masseter muscle of the jaw or into gum of lower jaw on gestation Day 11 at 0.02 times MRHD resulted in developmental delays in neonates
            • Subcutaneous administration of tetracaine to pregnant rats and rabbits during organogenesis did not produce adverse embryofetal effects at 0.03 times the MRHD

            Lactation

            There are no data on presence of tetracaine in human milk, effects on a breastfed infant, or on milk production; published studies on parenterally administered lidocaine have reported presence of lidocaine in human milk with milk:plasma ratios ranging between 0.4 to 1.1

            Available data on lidocaine’s effects on breastfed child have not revealed a consistent pattern of associated adverse effects; amount of lidocaine present in human milk following topical administration is unknown, but systemic absorption from topical lidocaine is low

            Consider developmental and health benefits of breastfeeding along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from therapy or mother’s underlying condition

            Advise breastfeeding women not to apply drug combination directly to nipple and areola to avoid direct infant exposure

            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)

            Distribution

            Vd (IV administration): 0.8-1.3 L/kg (lidocaine)

            Protein bound: 75% (lidocaine)

            Metabolism

            Unknown if metabolized in skin

            Systemic metabolism: hepatic (lidocaine); plasma esterases (tetracaine)

            Metabolites: ester- and amide-type local anesthetics

            Elimination

            t1/2 (IV administration): 1.8 hr (lidocaine)

            Excretion (IV administration): Urine (98%) [lidocaine]

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            Images

            No images available for this drug.
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            Patient Handout

            A Patient Handout is not currently available for this monograph.
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            Formulary

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
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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.