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system and ' or the stimulating action of .eta 4 adrenergic receptor epinephrine when present" 0he net effect is normally a modest hypotension when the recommended dosages are not e/ceeded" 0his is Page & 9ecem.er 4&:&% Pharmaco8inetics and meta.olism: Information derived from diverse formulations, concentrations andUsages reveal that lidocaine is completely a.sor.ed following parenteral administration, its rate of a.sorption depending, for e/ample, upon various factors such as the site of administration and the presence or a.sence of a vasoconstrictor agent" 6/cept for intravascular administration, the highest .lood levels are o.tained following intercostal nerve .loc8 and the lowest after su.cutaneous administration" 0he .inding of lidocaine depends on the plasma concentration of the drug , and reduces the fraction .ound with increasing concentration" At concentrations of % to : mcg of free .ase per ml , ,! to *! percent of the lidocaine is .ound to protein " ;inding is also dependent on the plasma concentration of 4 % 4 alpha acid glycoprotein" Lidocaine crosses the .lood4.rain and placental .arriers, presuma.ly .y passive diffusion" Lidocaine is rapidly meta.oli3ed in the liver, and meta.olites and unchanged drug are e/creted .y the 8idneys" ;iotransformation includes o/idative 24 deal8ylation, ring hydro/ylation, cleavage of the amide lin8age , and conjugation " 24 9eal8ylation, a major pathway of .iotransformation, yields the glycine/ylidide monoethyl glycine/ylidide and meta.olites" 0he pharmacological ' to/icological action of these meta.olites is similar to, .ut less potent than those of lidocaine" Appro/imately <!$ of the lidocaine administered is e/creted in the form of various meta.olites, and less than %! $ is e/creted unchanged" 0he primary meta.olite in the urine is a conjugate of : 4 hydro/yl 4 &, , 4 dimethylaniline" 0he elimination half4life after an intravenous lidocaine .olus injection is typically %"# to &"!hours" ;ecause of the speed with which lidocaine is meta.oli3ed , any condition that affects liver functioncan alter the 8inetics of lidocaine " 0he half4life may .e prolonged .y twice or more in patients with liverdysfunction " =enal dysfunction does not affect lidocaine 8inetics .ut may increase the accumulation of meta.olites" >actors such as acidosis and the use of stimulants and 2S depressants affect the 2S levels of apparent lidocaine re5uired to produce systemic effects" 1.jective adverse manifestations .ecome increasingly evident with increasing venous plasma
levels a.ove ,"! mcg free .ase per ml" In rhesusmono %*4&% mcg ' ml arterial .lood levels have .een shown to .e threshold for convulsive activity" INDICATIONS AND USAGE Lidocaine Hydrochloride Injection, USP is indicated for production of local or regional anesthesia infiltration techni5ues such as percutaneous injection and intravenous regional anesthesia .y peripheralnerve .loc8 techni5ues such as .rachial ple/us and intercostal and .y central neural techni5ues such as lum.ar and caudal epidural .loc8s , when the accepted procedures for these techni5ues as descri.ed in the standard te/t.oo8s are o.served" ontraindications Lidocaine is contraindicated in patients with a history of hypersensitivity to local anesthetics of the amide"
-ahendra hemicals is an US >9A approved IS1 <!!%:&!!* certified lidocaine hydrochloride and Lidocaine" Pharmaceutical -anufacturer suppliers
and a.ility to synthesi3e new API, Local Anesthetics"