Lidocaine-Prilocaine

Drug overview for LIDOCAINE-PRILOCAINE (lidocaine/prilocaine):

Generic name: LIDOCAINE/PRILOCAINE (LYE-doe-kane/PRILL-oh-cane)
Drug class: Topical Local Anesthetics
Therapeutic class: Dermatological

Lidocaine, a nonselective voltage-gated sodium channel inhibitor, is an Prilocaine hydrochloride is an intermediate-acting local anesthetic of the amide type. amide-type local anesthetic.

Lidocaine is used topically for the treatment of pain. Various topical Prilocaine hydrochloride is used in dentistry for infiltration anesthesia and for nerve block anesthesia. lidocaine products are commercially available.

Lidocaine 1.8% and 5% topical systems (i.e., patches) are FDA-labeled for the treatment of pain associated with postherpetic neuralgia (PHN). Lidocaine is also available in various over-the-counter (OTC) topical preparations for the temporary treatment of pain.

DRUG IMAGES

LIDOCAINE-PRILOCAINE CREAM

The following indications for LIDOCAINE-PRILOCAINE (lidocaine/prilocaine) have been approved by the FDA:

Indications:
Administration of local anesthesia

Professional Synonyms:
None.

The following dosing information is available for LIDOCAINE-PRILOCAINE (lidocaine/prilocaine):

Dosing
Administration
Dosing Information
Generic

Prilocaine hydrochloride may be administered by infiltration or by peripheral nerve block. Partially used dental cartridges of the drug should be discarded. Dosage of prilocaine hydrochloride varies with the anesthetic procedure, the degree of anesthesia required, and individual patient response.

The smallest dose required to produce the desired effect should be used. Resuscitative equipment and drugs which may be required for treatment of adverse reactions should be immediately available when prilocaine is administered. For specific procedures and techniques of administration, specialized references should be consulted.

For most routine dental procedures either by infiltration or major nerve block in adults, an initial dose of 1-2 mL (40-80 mg) of a 4% prilocaine hydrochloride solution is usually sufficient. A single dose in adults should not exceed 600 mg (8 mg/kg), and no more than 600 mg should be administered within a 2-hour period in healthy adults. Children younger than 10 years of age rarely require more than 1 mL of a 4% solution (40 mg).

The maximum dose in children younger than 10 years of age who have normal lean body mass and body development may be determined using standard pediatric dose formulas (e.g., Clark's rule).

Lidocaine patches are applied topically to intact skin. Applyimmediately after removal from the protective envelope. Patches may be cut into smaller sizes with scissors prior to removal of therelease liner.

Up to 3 patches may be applied at one time as prescribed; application of more than the recommended number of patches or for longer durations than recommended can result in increased blood concentrations of lidocaine, resulting in adverse reactions. Advise patients on proper application of the patches. Clothing may be worn over the area ofapplication.

If irritation or a burning sensation occurs during application, remove the patch(es) and do not reapply until the irritation subsides. Lidocaine 5% (Lidoderm(R)) patches may not stick if they get wet. The manufacturer states to avoid contact with water, such as bathing,swimming or showering.

The manufacturer of Ztlido(R) states that the patches may be used during moderate exercise, such as biking for 30 minutes and may be exposed to water, such as showering, for 10 minutes or immersion for 15 minutes. To dry the topical system after water exposure, gently pat the skin; do not rub the skin or topical system. Do not apply external heat sources, such as heating pads or electric blankets,directly to lidocaine patches, since this may increase plasma lidocaine levels.

The manufacturer of Ztlido(R) states that the patches can beapplied to an administration site after moderate heat exposure, such as15 minutes of heating pad exposure on a medium setting. Topical lidocaine (Lidoderm(R)and generics; Ztildo(R)) patches should be stored at 20-25degreesC with excursions permitted to 15-30degreesC.

No dosing information available.

No generic dosing information available.

The following drug interaction information is available for LIDOCAINE-PRILOCAINE (lidocaine/prilocaine):

Contraindicated
Severe
Moderate

There are 0 contraindications.

There are 1 severe interactions. These drug interactions can produce serious consequences in most patients. Actions required for severe interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration scheduling, and providing additional patient monitoring. Review the full interaction monograph for more information.

Drug Interaction	Drug Names
Long-acting Bupivacaine/Local Anesthetics SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Concurrent use of other local anesthetics or use of other local anesthetics within 96 hours following long-acting bupivacaine may result in additive neurologic and cardiovascular effects. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also increase the risk of methemoglobinemia.(1,2) Non-liposomal bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally.(1) CLINICAL EFFECTS: Concurrent or use of local anesthetics with 96 hours of use of long-acting bupivacaine may result in neurologic and cardiovascular toxicity. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also result in methemoglobinemia.(1,2) Non-liposomal bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally.(1) PREDISPOSING FACTORS: Use of additional agents that are associated with methemoglobinemia may further increase the risk of methemoglobinemia.(1) Patients who are at increased risk of developing methemoglobinemia include those 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. If local anesthetics must be used in these patients, close monitoring for symptoms and signs of methemoglobinemia is recommended.(1) PATIENT MANAGEMENT: Avoid the use of other local anesthetics within 96 hours following the administration of long-acting bupivacaine. In patients for whom use is required, monitor for neurologic and cardiovascular effects. Also monitor for methemoglobinemia with use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine.(1,2) Non-liposomal bupivacaine may be administered in the same syringe as bupivacaine liposomal or injected immediately before bupivacaine liposomal as long as the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Lidocaine may be administered 20 minutes or more prior to bupivacaine. It is unknown if other local anesthetics may be used without compromising the release characteristic of bupivacaine liposomal.(1) DISCUSSION: Concurrent use of other local anesthetics or use of other local anesthetics within 96 hours following long-acting bupivacaine may result in additive neurologic and cardiovascular effects. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also increase the risk of methemoglobinemia.(1,2) Non-liposome bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally. Lidocaine may be administered 20 minutes or more prior to bupivacaine. It is unknown if other local anesthetics may be used without compromising the release characteristic of bupivacaine liposomal.(1)	BUPIVACAINE LIPOSOME, EXPAREL, XARACOLL, ZYNRELEF

Drug Interaction

Drug Names

Long-acting Bupivacaine/Local Anesthetics

SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.

MECHANISM OF ACTION: Concurrent use of other local anesthetics or use of other local anesthetics within 96 hours following long-acting bupivacaine may result in additive neurologic and cardiovascular effects. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also increase the risk of methemoglobinemia.(1,2) Non-liposomal bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally.(1)

CLINICAL EFFECTS: Concurrent or use of local anesthetics with 96 hours of use of long-acting bupivacaine may result in neurologic and cardiovascular toxicity. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also result in methemoglobinemia.(1,2) Non-liposomal bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally.(1)

PREDISPOSING FACTORS: Use of additional agents that are associated with methemoglobinemia may further increase the risk of methemoglobinemia.(1) Patients who are at increased risk of developing methemoglobinemia include those 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. If local anesthetics must be used in these patients, close monitoring for symptoms and signs of methemoglobinemia is recommended.(1)

PATIENT MANAGEMENT: Avoid the use of other local anesthetics within 96 hours following the administration of long-acting bupivacaine. In patients for whom use is required, monitor for neurologic and cardiovascular effects. Also monitor for methemoglobinemia with use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine.(1,2)

Non-liposomal bupivacaine may be administered in the same syringe as bupivacaine liposomal or injected immediately before bupivacaine liposomal as long as the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Lidocaine may be administered 20 minutes or more prior to bupivacaine. It is unknown if other local anesthetics may be used without compromising the release characteristic of bupivacaine liposomal.(1)

DISCUSSION: Concurrent use of other local anesthetics or use of other local anesthetics within 96 hours following long-acting bupivacaine may result in additive neurologic and cardiovascular effects. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also increase the risk of methemoglobinemia.(1,2) Non-liposome bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1)

Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally. Lidocaine may be administered 20 minutes or more prior to bupivacaine. It is unknown if other local anesthetics may be used without compromising the release characteristic of bupivacaine liposomal.(1)

BUPIVACAINE LIPOSOME, EXPAREL, XARACOLL, ZYNRELEF

There are 0 moderate interactions.

The following contraindication information is available for LIDOCAINE-PRILOCAINE (lidocaine/prilocaine):

Overview
Contraindicated
Severe
Moderate

Drug contraindication overview.

*Known history of sensitivity to local anesthetic of the amide type, or to any other component of the product.

There are 2 contraindications. Absolute contraindication.

Contraindication List
Large open wound
Methemoglobinemia

There are 6 severe contraindications. Adequate patient monitoring is recommended for safer drug use.

Severe List
Cardiac arrhythmia
Glucose-6-phosphate dehydrogenase (g6Pd) deficiency
Heart block
Hemolytic anemia from pyruvate kinase and g6PD deficiencies
Sepsis
Shock

There are 3 moderate contraindications. Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.

Moderate List
Disease of liver
Respiratory depression
Seizure disorder

The following adverse reaction information is available for LIDOCAINE-PRILOCAINE (lidocaine/prilocaine):

Overview
Severe
Less Severe

Adverse reaction overview.

Common adverse effects of lidocaine 1.8 and 5% patches include mild and transient application site reactions (e.g., blisters, bruising, burning sensation, depigmentation,dermatitis, discoloration, edema, erythema, exfoliation, irritation, papules, petechia,pruritus, vesicles). Systemic adverse reactions following topical use of lidoderm patch are unlikely due to minimal drug absorption.

There are 8 severe adverse reactions.

More Frequent	Less Frequent
None.	None.

Rare/Very Rare
Bradycardia CNS toxicity Drowsy Headache disorder Hypotension Methemoglobinemia Respiratory depression Seizure disorder

There are 6 less severe adverse reactions.

More Frequent	Less Frequent
Localized edema Pallor Pruritus of skin Skin rash Treatment site sequelae Vasodilation of blood vessels	None.

Rare/Very Rare
None.

The following precautions are available for LIDOCAINE-PRILOCAINE (lidocaine/prilocaine):

Pediatric
Pregnant
Lactation
Geriatric

Safety and effectiveness in pediatric patients have not been established.

Contraindicated

None

Severe Precaution

None

Management or Monitoring Precaution

None

Lidocaine 5% patch has not been studied in pregnancy. The limited human data with the 1.8% patch are insufficient to inform a drug-associated risk for major birth defects and miscarriage.

Animal reproductionstudies found that subcutaneous administration of the drug at doses higher than recommended human doses during the period of organogenesis resulted in lower fetal weights. Some manufacturers recommend that lidocaine patches should be used during pregnancy only if clearly needed. Lidoderm patches have not been studied and are contraindicated in labor and delivery. If lidocaine patches are used concomitantly with other productscontaining lidocaine, total doses contributed by all formulations must be considered.

Lidocaine is excreted into humanmilk in low concentrations following topical application. Caution should be exercised whenlidocaine is administered to a nursing woman, especially when administered with other local anesthetics.

Clinical studies of lidocaine 1.8% patch did not include sufficient number of patients >=65 years of age to determine whether they respond differently from younger patients. No differences in response have been identified in other clinical experience.