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Lidoderm (Lidocaine Patch 5%): Uses, Dosage, Side Effects, Interactions, Warning
05
Aug
Aug
CLINICAL PHARMACOLOGY
Pharmacodynamics
Lidocaine is an amide-type local anaesthetic agentive role and is suggested to stabilize neural membranes by inhibiting the ionic fluxes required for the initiation and conduction of impulses .
The penetration of lidocaine into intact bark after application of LIDODERM is sufficient to produce an analgesic consequence, but less than the amount necessity to produce a complete sensory block .
Pharmacokinetics
Absorption
The sum of lidocaine systemically absorbed from LIDODERM is directly related to both the duration of application and the surface area over which it is applied. In a pharmacokinetic study, three LIDODERM patches were applied over an sphere of 420 cm² of integral hide on the back of normal volunteers for 12 hours. blood samples were withdrawn for decision of lidocaine assiduity during the lotion and for 12 hours after removal of patches. The results are summarized in table 1 .
Table 1 : Absorption of lidocaine from LIDODERM Normal
volunteers (n= 15, 12-hour wearing time)
| LIDODERM Patch | Application Site | Area (cm²) | Dose Absorbed (mg) | Cmax (μg/mL) | Tmax (hr) |
| 3 patches (2100 mg) | Back | 420 | 64 ± 32 | 0.13 ± 0.06 | 11 hr |
When LIDODERM is used according to the recommended dose instructions, lone 3 ± 2 % of the dose applied is expected to be absorbed. At least 95 % ( 665 milligram ) of lidocaine will remain in a use while. Mean point lineage concentration of lidocaine is about 0.13 μg/mL ( about 1/10 of the curative concentration required to treat cardiac cardiac arrhythmia ). Repeated lotion of three patches simultaneously for 12 hours ( recommend maximal daily dose ), once per day for three days, indicated that the lidocaine assiduity does not increase with daily consumption. The mean plasma pharmacokinetic profile for the 15 healthy volunteers is shown in Figure 1 .
Figure 1 : Mean lidocaine blood concentrations after
three consecutive daily applications of three LIDODERM patches simultaneously
for 12 hours per day in healthy volunteers (n = 15).
 |
Distribution
When lidocaine is administered intravenously to healthy volunteers, the volume of distribution is 0.7 to 2.7 L/kg ( think of 1.5 ± 0.6 SD, n=15 ). At concentrations produced by application of LIDODERM, lidocaine is approximately 70 % boundary to plasma proteins, chiefly alpha-1 -acid glycoprotein. At much higher plasma concentrations ( 1 to 4 μg/mL of free base ), the plasma protein bind of lidocaine is assiduity pendent. Lidocaine crosses the placental and blood genius barriers, presumably by passive voice diffusion .
Metabolism
It is not known if lidocaine is metabolized in the skin. Lidocaine is metabolized quickly by the liver-colored to a number of metabolites, including monoethylglycinexylidide ( MEGX ) and glycinexylidide ( GX ), both of which have pharmacologic action alike to, but less potent than that of lidocaine. A minor metabolite, 2, 6-xylidine, has unknown pharmacological activity but is carcinogenic in rats. The lineage concentration of this metabolite is negligible following application of LIDODERM ( lidocaine patch 5 % ). Following intravenous administration, MEGX and GX concentrations in serum range from 11 to 36 % and from 5 to 11 % of lidocaine concentrations, respectively.
Excretion
Lidocaine and its metabolites are excreted by the kidneys. Less than 10 % of lidocaine is excreted unaltered. The half life of lidocaine elimination from the plasma following IV administration is 81 to 149 minutes ( beggarly 107 ± 22 SD, north = 15 ). The systemic clearance is 0.33 to 0.90 L/min ( bastardly 0.64 ± 0.18 SD, newton = 15 ) .
Clinical Studies
Single-dose treatment with LIDODERM was compared to treatment with vehicle bandage ( without lidocaine ), and to no treatment ( observation only ) in a double-blind, crossing clinical trial with 35 post-herpetic neuralgia patients. Pain intensity and annoyance relief scores were evaluated sporadically for 12 hours. LIDODERM performed statistically better than vehicle patch in terms of pain intensity from 4 to 12 hours .
Multiple-dose, two-week treatment with LIDODERM was compared to vehicle bandage ( without lidocaine ) in a double-blind, crossover voter clinical trial of withdrawal-type design conducted in 32 patients, who were considered as responders to the open-label use of LIDODERM prior to the learn. The constant type of pain was evaluated but not the trouble induced by sensational stimuli ( dysesthesia ). Statistically significant differences favoring LIDODERM were observed in terms of time to exit from the test ( 14 versus 3.8 days at p-value < 0.001 ), daily median trouble relief, and affected role 's preference of discussion. About half of the patients besides took oral medicine normally used in the treatment of post-herpetic neuralgia. The extent of use of attendant medication was like in the two treatment groups .
