Comparative Pharmacokinetics of Chlorphenesin Carbamate and Methocarbamol in Man

Forist, Arlington A.; Judy, Ray W.

doi:10.1002/jps.2600601121

Cited by 21 publications

(3 citation statements)

References 15 publications

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“…A peak mean (fSD) level of I (9.29 f 3.62 pg/ml) was observed a t 1 hr postadministration, indicating rapid drug absorption from hard-filled gelatin capsules. The serum drug disappearance half-life, a s estimated graphically from the average serum drug concentrations, was 4.6 hr, showing good agreement with the calculated half-lives (2.32-4.30 hr) following single-dose oral administration of 2-3 g drug (17). The combined results from these investigations show that the GLC method can be used for: (a) determining serum I concentrations after therapeutic doses (2400 mg) of drug, (b) evaluating the pharmacokinetics, and (c) selecting an optimum dosage regimen for I administration to humans.…”

supporting

confidence: 63%

GLC Determination of Chlorphenesin Carbamate in Serum

Kaiser

Shaw

1974

Journal of Pharmaceutical Sciences

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supporting

confidence: 63%

GLC Determination of Chlorphenesin Carbamate in Serum

Kaiser

Shaw

1974

Journal of Pharmaceutical Sciences

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“…For example, one large oral dose administrated in the human body, of carbamate (chlorphenesin) reached serum concentrations, with mean lag times and half-lives for absorption of a one compartmental model (Forist and Judy 1971). A study using pyridinol carbamate obtained a similar result (Sassard et al 1979).…”

Section: Distribution Of Carbamatesmentioning

confidence: 88%

Evaluation of novel carbamate insecticides for neurotoxicity to non-target species

Jiang

Swale

Carlier

et al. 2013

Pesticide Biochemistry and Physiology

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Malaria (vector: Anopheles gambiae) is a major infectious disease that kills about 1 million people each year. For the improvement of its treatment and vector control during the past decades, several issues such as high medicine cost, insecticide resistance, and lack of an effective vaccine have prevented adequate control of malaria. Additionally, the low selectivity of malaria vector insecticides also presents a public health problem. The purpose of developing novel carbamate insecticides in our laboratory is to offer effective and selective insecticide options to achieve the ultimate goal of malaria control.First, 50% inhibition concentration (IC 50 ) data was collected from three mammalian AChEs with eight commercial carbamate insecticides by using the Ellman assay. The IC 50 values varied from 57 nM to 7358 nM. The AChE sensitivity pattern and level were shown to be similar between the recombinant mouse and ICR male mouse brain cortex homogenate (slope = 0.99, R 2 = 0.96).Then eight novel carbamate insecticides that are possible malaria vector control agents were selected for further neurotoxicity testing in non-target organisms. Neurotoxic esterase (NTE) assay showed that the novel carbamates did not significantly inhibit NTE, inhibition of which underlies a significant hazard for anticholinesterases, especially organophosphates, in several nontarget vertebrate organisms. The NTE activity in the presence of novel carbamate insecticides ranged from 93% to 116% of the control, while in the commercial group, bendiocarb significantly inhibited NTE, leaving only 76.5% of the initial reactivity at 1 mM inhibitor concentration.Further in vivo bioassay using Daphnia magna was conducted to compare the aquatic toxicity of commercial and novel carbamates. The data showed that except for PRC331 (3-tertbutylphenylmethylcarbamate), all novel carbamates were of similar potency as bendiocarb (LC 50 = 611 nM) for aquatic toxicity, and their LC 50 values ranged from 172 nM (PRC331) to 1109 nM.In conclusion, the novel carbamate insecticides would appear to be an improvement over commercial carbamate insecticides because of greater selectivity, negligible NTE inhibition capacity, but in some cases with potent in vivo toxicity to Daphnia magna. However, since the envisioned usage of these compounds is in bednets or as indoor residual sprays (IRS), any environmental exposures to nontarget aquatic organisms are expected to be minimal.iv ACKNOWLEDGEMENTS

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“…Traditional techniques for detection of methocarbamol in biological samples include thin-layer chromatography (TLC) (5), carbon-14-1abeled drug use (3), spectrophotometric determination of the formaldehyde derivative of methocarbamol (6), and HPLC with refractive index detection (7). HPLC with IN and photodiode array detection (4,(8)(9)(10)(11) has been the method of choice recently for the detection of this drug in forensic toxicology.…”

Section: Introductionmentioning

confidence: 99%

Determination of Methocarbamol in Equine Serum and Urine by High-Performance Liquid Chromatography with Ultraviolet Detection and Atmospheric Pressure Ionization-Mass Spectrometric Confirmation*

Koupai-Abyazani¹,

Esaw²,

Laviolette³

1997

Journal of Analytical Toxicology

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Urine and serum samples collected from four standard-bred mares after and oral regimen administration of methocarbamol were extracted and analyzed. The method consisted of enzyme hydrolysis followed by a one-step liquid-liquid extraction, separation on a reversed-phase (RP-18) column, and detection using an ultraviolet (UV) detector. The confirmation was carried out using a liquid chromatography-atmospheric pressure ionization-mass spectrometry (LC-API-MS) system. Maximum methocarbamol concentrations of 1498, 1734, 1547, 2322 micrograms/mL in urine and 4.9, 1.7, and 3.6 micrograms/mL in serum were observed. The peak concentrations of the drug were detected 1-4 h (urine) and 10-60 min (serum) after administration to four horses. The method validation results and drug elimination profiles for both urine and serum are presented and discussed.

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Comparative Pharmacokinetics of Chlorphenesin Carbamate and Methocarbamol in Man

Cited by 21 publications

References 15 publications

GLC Determination of Chlorphenesin Carbamate in Serum

GLC Determination of Chlorphenesin Carbamate in Serum

Evaluation of novel carbamate insecticides for neurotoxicity to non-target species

Determination of Methocarbamol in Equine Serum and Urine by High-Performance Liquid Chromatography with Ultraviolet Detection and Atmospheric Pressure Ionization-Mass Spectrometric Confirmation*

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