Dermazyl (lidocaine/dimethicone)
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/dimethicone
Pronunciation: (LYE-doe-kane)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Dermazyl
Indications
No indications are available for this drug.
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.
There are no severe interactions for this drug.
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.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
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.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
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
Search health-plan coverage for this drug by ZIP code.
Choose the first character of a health plan name.
Last reviewed · Source: First Databank (FDB) drug data
On this page
Actions
Sign in to save favorites
Saving this drug requires a free Physicians Office Resource account.