Teikoku Seiyaku

Teikoku Seiyaku

Japan - Higashikagawa
Biotechnology

Focus: Poultices

Teikoku Seiyaku is a life sciences company focused on Poultices.

Neurology
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Products & Portfolio (1)

LIDODERM
lidocaine
LOE Approaching
TOPICAL · PATCH
CLINICAL PHARMACOLOGY Pharmacodynamics Lidocaine is an amide-type local anesthetic agent and is suggested to stabilize neuronal membranes by inhibiting the ionic fluxes required for the initiation and conduction of impulses. The penetration of lidocaine into intact skin after application of LIDOCAINE PATCH 5% is sufficient to produce an analgesic effect, but less than the amount necessary to produce a complete sensory block. Pharmacokinetics Absorption The amount of lidocaine systemically absorbed from LIDOCAINE PATCH 5% is directly related to both the duration of application and the surface area over which it is applied. In a pharmacokinetic study, three LIDOCAINE PATCH 5% patches were applied over an area of 420 cm of intact skin on the back of normal volunteers for 12 hours. Blood samples were withdrawn for determination of lidocaine concentration during the application and for 12 hours after removal of patches. The results are summarized in Table 1. Table 1 Absorption of lidocaine from LIDOCAINE PATCH 5% Normal volunteers (n = 15, 12-hour wearing time) LIDOCAINE PATCH 5% Application Site Area (cm) Dose Absorbed (mg) C max (mcg/mL) T max (hr) 3 patches (2100 mg) Back 420 64 ± 32 0.13 ± 0.06 11 hr When LIDOCAINE PATCH 5% is used according to the recommended dosing instructions, only 3 ± 2% of the dose applied is expected to be absorbed. At least 95% (665 mg) of lidocaine will remain in a used patch. Mean peak blood concentration of lidocaine is about 0.13 mcg/mL (about 1/10 of the therapeutic concentration required to treat cardiac arrhythmias). Repeated application of three patches simultaneously for 12 hours (recommended maximum daily dose), once per day for three days, indicated that the lidocaine concentration does not increase with daily use. 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 LIDOCAINE PATCH 5% patches simultaneously for 12 hours per day in healthy volunteers (n = 15). Figure 1 Distribution When lidocaine is administered intravenously to healthy volunteers, the volume of distribution is 0.7 to 2.7 L/kg (mean 1.5 ± 0.6 SD, n=15). At concentrations produced by application of LIDOCAINE PATCH 5%, lidocaine is approximately 70% bound to plasma proteins, primarily alpha‑1‑acid glycoprotein. At much higher plasma concentrations (1 to 4 mcg/mL of free base), the plasma protein binding of lidocaine is concentration dependent. Lidocaine crosses the placental and blood brain barriers, presumably by passive diffusion. Metabolism It is not known if lidocaine is metabolized in the skin. Lidocaine is metabolized rapidly by the liver to a number of metabolites, including monoethylglycinexylidide (MEGX) and glycinexylidide (GX), both of which have pharmacologic activity similar to, but less potent than that of lidocaine. A minor metabolite, 2, 6-xylidine, has unknown pharmacologic activity but is carcino
1999
30

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Interview Prep Quick Facts
Portfolio: 1 approved product
Top TAs: Neurology
Portfolio Health
LOE Approaching1 (100%)
1 total products
Therapeutic Area Focus
Neurology
1 marketed
Marketed
Pipeline