Aspercreme (lidocaine)
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
Pronunciation: (LYE-doe-kane)
Therapeutic class: Dermatological
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Aspercreme
Indications
The following indications are listed for Aspercreme:
- Postherpetic Neuralgia
Also known as: Post Herpetic Neuralgia, Postherpetic Neurodynia.
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.
Salicylates/Influenza Virus Vaccine Live
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Use of salicylates during influenza infection has been associated with Reye's Syndrome.(1,2)
CLINICAL EFFECTS: Use of the live influenza virus vaccine in children and adolescents (patients age 2-17 years) receiving salicylate therapy may increase the risk of Reye's Syndrome.(1,2) Symptoms of Reye's syndrome include drowsiness, confusion, seizures, coma. In severe cases, Reye's syndrome can result in death.
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: The use of live influenza virus vaccine in children and adolescents (patients age 2-17 years) receiving salicylate therapy is contraindicated.(1,2) Use of salicylates should be avoided for 4 weeks after administration of live influenza vaccine.(1)
DISCUSSION: Because the use of salicylates during influenza infection has been associated with Reye's Syndrome, the use of live influenza virus vaccine in children and adolescents (patients age 2-17 years) receiving salicylate therapy is contraindicated.(1,2)
Topical Salicylates/Slt Anticoagulants (Vit K Antagonists)
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Multiple processes are involved: 1) Salicylate doses greater than 3 gm daily decrease plasma prothrombin levels. 2) Salicylates may also displace anticoagulants from plasma protein binding sites. 3) Aspirin is an irreversible platelet inhibitor. Salicylates impair platelet function, resulting in prolonged bleeding time. 4) Salicylates may cause gastrointestinal(GI) bleeding due to irritation.
CLINICAL EFFECTS: The concurrent use of anticoagulants and salicylates leads to blockade of two distinct coagulation pathways and may increase the risk for bleeding.
PREDISPOSING FACTORS: The risk for bleeding episodes may be greater in patients with disease-associated factors (e.g. thrombocytopenia). Drug associated risk factors include concurrent use of multiple drugs which inhibit anticoagulant/antiplatelet metabolism and/or have an inherent risk for bleeding (e.g. NSAIDs).
PATIENT MANAGEMENT: Avoid concomitant administration of these drugs. When aspirin is required for cardioprotection, a low dose (< 100 mg daily) is recommended to decrease the risk for aspirin-induced GI bleeding. If concurrent therapy is warranted, monitor patients receiving concurrent therapy for signs of blood loss, including decreased hemoglobin, hematocrit, fecal occult blood, and/or decreased blood pressure and promptly evaluate patients with any symptoms. When applicable, perform agent-specific laboratory test (e.g. INR, aPTT) to monitor efficacy and safety of anticoagulation. Discontinue anticoagulation in patients with active pathologic bleeding. Instruct patients to report any signs and symptoms of bleeding, such as unusual bleeding from the gums or nose; unusual bruising; red or black, tarry stools; red, pink or dark brown urine; acute abdominal or joint pain and/or swelling.
DISCUSSION: Topical use of methyl salicylate has been reported to increase the effects of warfarin.(1-7) In a case series on 11 patients who used significant amounts of methyl salicylate (2-4 g of ointment for previous 2 weeks), all had significant increases in INR and positive blood levels of salicylates. Two patients experienced diffuse bruising and one experienced gastrointestinal bleeding.(1) A self-controlled case study of 1,622 oral anticoagulant-precipitant drug pairs were reviewed and found 14% of drug pairs were associated with a statistically significant elevated risk of thromboembolism. Concurrent use of warfarin and diflunisal resulted in a ratio of rate ratios (RR) (95% CI) of 3.85 (1.34-11.03); and warfarin and aspirin ratio of RR 2.13 (1.72-2.64).
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.
- Aspirin exacerbated respiratory disease
- Hemolytic anemia from pyruvate kinase and g6PD deficiencies
There are no severe contraindications for this drug.
- Peripheral vascular disease
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.
Rare or Very Rare
- Anaphylaxis
- Burns
- Dyspnea
- Facial edema
- Hypersensitivity drug reaction
- Periorbital edema
- Pharyngeal edema
- Skin ulcer
- Superficial skin ulcer
- Syncope
- Throat constriction
- Urticaria
More Frequent
- Stinging of skin
Less Frequent
- Dry skin
- Skin irritation
Rare or Very Rare
- Pruritus of skin
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
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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