Lidocaine (lidocaine)
Topical Local Anesthetics Topical Cream (Gram)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Lidocaine, a nonselective voltage-gated sodium channel inhibitor, is an amide-type local anesthetic.
Lidocaine is an amide-type local anesthetic that blocks sodium ion channels required for the initiation and conduction of neuronal impulses. The analgesic effects of lidocaine are thought to result from these effects. Penetration of lidocaine into intact skin is sufficient to produce an analgesic effect; however, the amount is insufficient to produce a complete sensory block.
Ztlido(R) (lidocaine topical system) 1.8% is a single-layer, drug-in-adhesive, topical deliverysystem comprised of an adhesive material containing 36 mg lidocaine, which is applied toa pliable nonwoven cloth backing and covered with a polyethylene terephthalate (PET) filmrelease liner. Lidoderm(R) transdermal patch is composed of an adhesive material containing 5%lidocaine, which is applied to a nonwoven polyester felt backing and covered with aPET film release liner. The release liner is removed prior toapplication of both the Ztlido(R) and Lidoderm(R) patches.
The amount of lidocaine that is systemically absorbed from a lidocaine patch is directly related toboth the duration of application and the surface area over which it is applied. There is minimal systemic absorption (approximately 3%) when the 5% patches are used topically as recommended and maximum blood concentrations are about 1/10 of the therapeutic concentration required to treat cardiac arrhythmias. In apharmacokinetic study evaluating lidocaine 5% patches, 3 patches (total of 2100 mg) were applied over an area of 420 cm2of intact skin on the backs of normal volunteers for 12 hours.
The total dose absorbed was approximately 64 mg and time to peak plasma concentration was 11 hours. Mean lidocaine blood concentrations after 3 consecutive days of daily use (3 patches applied at the same time for 12 hours once daily for 3 days) remained the same. In a pharmacokinetic study evaluating the 1.8% patches, 3 patches (total dose of 108 mg) were applied over an area of 420 cm2of intact skin on the backs of normal volunteers for 12 hours.
Time to peak plasma concentration was approximately 14 hours. Mean lidocaine blood concentrations after 3 consecutive days of daily use (3 patches applied at the same time for 12 hours once daily for 3 days) remained the same.
Lidocaine is approximately 70% bound to plasma proteins (primarily alpha-1-acid glycoprotein) at concentrations achieved from topical application; at higher concentrations, plasma protein binding is concentration dependent. Lidocaine crosses the placental and blood brain barriers, presumably by diffusion. It is not known if lidocaine is metabolized in the skin.
However, lidocaine is extensively metabolized in the liver to several pharmacologically active metabolites and is excreted by the kidneys (less than 10% as unchanged drug).
Lidocaine 1.8% patches (Ztlido(R)) are bioequivalent to lidocaine 5% patches (Lidoderm(R) and generics).
Lidocaine is used topically for the treatment of pain. Various topical 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.
Generic name: lidocaine
Drug class: Topical Local Anesthetics
Therapeutic class: Dermatological
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Lidocaine
Indications
The following indications are listed for Lidocaine:
- Hemorrhoids
- Proctitis
- Pruritus Ani
- Rectal Pain
Also known as: Proctalgia, Rectitis.
Dosing
No dosing information is available for this tab.
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 is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
Local Anesthetics/Long-Acting Bupivacaine
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)
There are no moderate interactions for this drug.
Contraindications
*Known history of sensitivity to local anesthetic of the amide type, or to any other component of the product.
- Large open wound
- Methemoglobinemia
- Glucose-6-phosphate dehydrogenase (g6Pd) deficiency
- Heart block
- Hemolytic anemia from pyruvate kinase and g6PD deficiencies
- Sepsis
- Shock
- Disease of liver
- Respiratory depression
- Seizure disorder
Adverse reactions
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.
Less Frequent
- Dermatitis due to topical drug
Rare or 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
Less Frequent
- Blanching of skin
- Edema
- Erythema
- Pruritus of skin
- Skin rash
- Stinging of skin
- Urticaria
Rare or Very Rare
- Acute cognitive impairment
- Apprehension
- Blurred vision
- Dizziness
- Drowsy
- Euphoria
- Muscle fasciculation
- Nervousness
- Sensation of cold
- Sensation of warmth
- Tinnitus
- Tremor
- Vomiting
Precautions
No enhanced messaging available.
Safety and effectiveness in pediatric patients have not been established.
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.
Select dosage with caution in geriatric patients, usually starting at the low end of the dosing range (e.g., a single topical system).
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.
ICD codes
| Code | Type | Description |
|---|---|---|
| Hemorrhoids | ||
| K64.0 | ICD10CM | First degree hemorrhoids |
| K64.8 | ICD10CM | Other hemorrhoids |
| K64.9 | ICD10CM | Unspecified hemorrhoids |
| O22.4 | ICD10CM | Hemorrhoids in pregnancy |
| O22.40 | ICD10CM | Hemorrhoids in pregnancy, unspecified trimester |
| O22.41 | ICD10CM | Hemorrhoids in pregnancy, first trimester |
| O22.42 | ICD10CM | Hemorrhoids in pregnancy, second trimester |
| O22.43 | ICD10CM | Hemorrhoids in pregnancy, third trimester |
| O87.2 | ICD10CM | Hemorrhoids in the puerperium |
| Proctitis | ||
| K62.7 | ICD10CM | Radiation proctitis |
| K62.89 | ICD10CM | Other specified diseases of anus and rectum |
| Pruritus ani | ||
| L29.0 | ICD10CM | Pruritus ani |
| L29.3 | ICD10CM | Anogenital pruritus, unspecified |
| Pruritus of skin | ||
| L29.8 | ICD10CM | Other pruritus |
| L29.81 | ICD10CM | Cholestatic pruritus |
| L29.89 | ICD10CM | Other pruritus |
| L29.9 | ICD10CM | Pruritus, unspecified |
| Rectal pain | ||
| K62.89 | ICD10CM | Other specified diseases of anus and rectum |
| Skin irritation | ||
| L24 | ICD10CM | Irritant contact dermatitis |
| L24.0 | ICD10CM | Irritant contact dermatitis due to detergents |
| L24.1 | ICD10CM | Irritant contact dermatitis due to oils and greases |
| L24.2 | ICD10CM | Irritant contact dermatitis due to solvents |
| L24.3 | ICD10CM | Irritant contact dermatitis due to cosmetics |
| L24.4 | ICD10CM | Irritant contact dermatitis due to drugs in contact with skin |
| L24.5 | ICD10CM | Irritant contact dermatitis due to other chemical products |
| L24.6 | ICD10CM | Irritant contact dermatitis due to food in contact with skin |
| L24.7 | ICD10CM | Irritant contact dermatitis due to plants, except food |
| L24.8 | ICD10CM | Irritant contact dermatitis due to other agents |
| L24.81 | ICD10CM | Irritant contact dermatitis due to metals |
| L24.89 | ICD10CM | Irritant contact dermatitis due to other agents |
| L24.9 | ICD10CM | Irritant contact dermatitis, unspecified cause |
| L24.A | ICD10CM | Irritant contact dermatitis due to friction or contact with body fluids |
| L24.A0 | ICD10CM | Irritant contact dermatitis due to friction or contact with body fluids, unspecified |
| L24.A1 | ICD10CM | Irritant contact dermatitis due to saliva |
| L24.A2 | ICD10CM | Irritant contact dermatitis due to fecal, urinary or dual incontinence |
| L24.A9 | ICD10CM | Irritant contact dermatitis due friction or contact with other specified body fluids |
| L24.B | ICD10CM | Irritant contact dermatitis related to stoma or fistula |
| L24.B0 | ICD10CM | Irritant contact dermatitis related to unspecified stoma or fistula |
| L24.B1 | ICD10CM | Irritant contact dermatitis related to digestive stoma or fistula |
| L24.B2 | ICD10CM | Irritant contact dermatitis related to respiratory stoma or fistula |
| L24.B3 | ICD10CM | Irritant contact dermatitis related to fecal or urinary stoma or fistula |
| L25 | ICD10CM | Unspecified contact dermatitis |
| L25.0 | ICD10CM | Unspecified contact dermatitis due to cosmetics |
| L25.1 | ICD10CM | Unspecified contact dermatitis due to drugs in contact with skin |
| L25.2 | ICD10CM | Unspecified contact dermatitis due to dyes |
| L25.3 | ICD10CM | Unspecified contact dermatitis due to other chemical products |
| L25.4 | ICD10CM | Unspecified contact dermatitis due to food in contact with skin |
| L25.5 | ICD10CM | Unspecified contact dermatitis due to plants, except food |
| L25.8 | ICD10CM | Unspecified contact dermatitis due to other agents |
| L25.9 | ICD10CM | Unspecified contact dermatitis, unspecified cause |
| L30.9 | ICD10CM | Dermatitis, unspecified |
| R21 | ICD10CM | Rash and other nonspecific skin eruption |
ICD code information from First Databank (FDB).
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Last reviewed · Source: First Databank (FDB) drug data
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