Nobela

Drug overview for NOBELA (lidocaine/tetracaine/benzocaine):

Generic name: LIDOCAINE/TETRACAINE/BENZOCAINE
Drug class: Topical Local Anesthetics
Therapeutic class: Dermatological

Benzocaine is a local anesthetic. Lidocaine, a nonselective voltage-gated sodium channel inhibitor, is an Tetracaine is an ester local anesthetic. amide-type local anesthetic.

Benzocaine is used topically for the temporary relief of pain and itching Lidocaine is used topically for the treatment of pain. Various topical associated with minor burns, sunburn, minor cuts or scrapes, insect bites, lidocaine products are commercially available. Lidocaine 1.8%

and 5% or minor skin irritations. Benzocaine is also used topically for the topical systems (i.e., patches) are FDA-labeled for the treatment of pain associated with postherpetic neuralgia (PHN). Lidocaine is also available temporary relief of pain and itching associated with episiotomy, pruritus in various over-the-counter (OTC) topical preparations for the temporary vulvae, or hemorrhoids and as a male genital desensitizer to aid in slowing the onset of ejaculation.

treatment of pain. Benzocaine has been used topically as a water-soluble lubricant for topical anesthesia on urinary catheters, laryngoscopes, proctoscopes, sigmoidoscopes, and vaginal specula. However, methemoglobinemia has been reported when the drug has been applied to mucous membranes.

DRUG IMAGES

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The following indications for NOBELA (lidocaine/tetracaine/benzocaine) have been approved by the FDA:

Indications:
None.

Professional Synonyms:
None.

The following dosing information is available for NOBELA (lidocaine/tetracaine/benzocaine):

Dosing
Administration
Dosing Information
Generic

Benzocaine preparations are applied topically in the form of aerosol sprays, creams, gels, lotions, ointments, and solutions.

For the temporary relief of pain and itching associated with various skin conditions, preparations containing 5-20% benzocaine are usually applied 3 or 4 times daily or as directed by a physician.

For male genital desensitization, a small amount of a preparation containing 3-7.5% benzocaine in a water-soluble base is applied to the head and shaft of the penis before intercourse; after intercourse, patients should wash off any remaining benzocaine to minimize the chance of an allergic reaction occurring.

For topical anesthesia and lubrication during instrumentation, benzocaine is applied to the exterior of the tube or instrument as a 20% water-soluble lubricant prior to use.

It isessential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

To produce local ophthalmic anesthesia, the usual dose is 1 drop topically in the eye(s) as needed.

Apply topically to the eye in the form of a 0.5% solution. Not for injection or intraocular use; do not use intracamerally.

Administer under the direct supervision of a healthcare provider; not intended for patient self-administration. Open package using standard aseptic technique. The dispenser may then be allowed to fall upon a sterile surface.

The entire outer surface of the dispenser and its contents are sterile. Each dispenser is for single patient use and does not contain a preservative; discard any unused portion. Store at 2degreesC to 8degreesC; protect contents from light.

Do not use if solution contains crystals, is cloudy, or discolored. 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 NOBELA (lidocaine/tetracaine/benzocaine):

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 NOBELA (lidocaine/tetracaine/benzocaine):

Overview
Contraindicated
Severe
Moderate

Drug contraindication overview.

None *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 NOBELA (lidocaine/tetracaine/benzocaine):

Overview
Severe
Less Severe

Adverse reaction overview.

Ocular adverse events: stinging, burning, conjunctival redness. 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 16 severe adverse reactions.

More Frequent	Less Frequent
None.	Dermatitis due to topical drug

Rare/Very Rare
Acute respiratory failure Anaphylaxis Angioedema Bradycardia Bronchospastic pulmonary disease Cardiac arrhythmia CNS toxicity Cyanosis Eyelid edema Headache disorder Hypotension Methemoglobinemia Respiratory depression Seizure disorder Unconsciousness

There are 20 less severe adverse reactions.

More Frequent	Less Frequent
None.	Blanching of skin Edema Erythema Pruritus of skin Skin rash Stinging of skin Urticaria

Rare/Very Rare
Acute cognitive impairment Apprehension Blurred vision Dizziness Drowsy Euphoria Muscle fasciculation Nervousness Sensation of cold Sensation of warmth Tinnitus Tremor Vomiting

The following precautions are available for NOBELA (lidocaine/tetracaine/benzocaine):

Pediatric
Pregnant
Lactation
Geriatric

Safety in the pediatric population has been demonstrated in clinical trials. Efficacy of tetracaine hydrochloride ophthalmic solution for use in pediatric patients has been extrapolated from adequate and well controlled clinical trials in the adult population. Safety and effectiveness in pediatric patients have not been established.

Contraindicated

None

Severe Precaution

None

Management or Monitoring Precaution

None

There are no adequate and well-controlled studies with tetracaine hydrochloride ophthalmic solution in pregnant women. Animal developmental and reproductive toxicity studies with tetracaine hydrochloride have not been reported in the published literature. 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.

There are no data to assess whether tetracaine hydrochloride ophthalmic solution is excreted in human milk or to assess its effects on milk production/excretion. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for the drug and any potential adverse effects on the breastfed child from tetracaine or from the underlying maternal condition. 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.

No overall differences in safety or effectiveness of tetracaine hydrochloride ophthalmic solution have been observed between elderly and younger patients. 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.