Lidocaine disposition—Sex differences and effects of cimetidine

Wing, Lindon; Miners, John O.; Birkett, D. J.; Foenander, T.; Lillywhite, K. J.; Wanwimolruk, Sompon

doi:10.1038/clpt.1984.97

Cited by 56 publications

(22 citation statements)

References 1 publication

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Verapamil concentrations were measured by the method of Harapat & Kates (1980); sulphinpyrazone concentrations were measured by a modification of the procedure described by Wong et al (1978) using phenprocoumon as the internal standard; and cimetidine concentrations were measured by a method previously described from our laboratory (Wing et al, 1984).…”

Section: Methodsmentioning

confidence: 99%

Verapamil disposition‐effects of sulphinpyrazone and cimetidine.

Wing¹,

Miners²,

Lillywhite³

1985

Brit J Clinical Pharma

View full text Add to dashboard Cite

The effects of separate 7 day pretreatments with sulphinpyrazone (800 mg daily) and cimetidine (1 g daily) on the disposition of (+/‐)‐ verapamil have been examined in eight healthy volunteers (four male, four female). Each subject received single oral (80 mg) and intravenous (0.15 mg/kg) doses of verapamil on different occasions before and after each pretreatment. Following sulphinpyrazone pretreatment, verapamil apparent oral plasma clearance (CLpo) increased from 4.27 to 13.77 l h‐ 1 kg‐1 (s.e. mean 0.51‐ANOVA) (P less than 0.001); CL increased from 1.05 to 1.20 l h‐1 kg‐1 (s.e. mean 0.05) (P less than 0.05) and Fpo decreased from 27 to 10% administered dose (s.e. mean 2) (P less than 0.001). Vss and t1/2,z were unchanged. There was no sex difference for any dispositional parameter in the control phase, but the increase in CLpo following sulphinpyrazone pretreatment was more marked in males (4.04 to 17.33 l h‐1 kg‐1) than in females (4.49 to 10.21 l h‐1 kg‐1) (s.e. mean 0.72) (P less than 0.01). There was no significant change in any verapamil disposition parameter following cimetidine pretreatment. Verapamil unbound fraction in plasma was 0.157 (s.e. mean 0.001, n = 40). There was no alteration in verapamil plasma protein binding associated with increasing verapamil concentration (25‐250 micrograms l‐ 1) or addition of sulphinpyrazone (50‐500 mg l‐1) or cimetidine (0.5‐5 mg l‐1). The results suggest that sulphinpyrazone induces the metabolic clearance of (+/‐)‐verapamil with a sex difference in the response.(ABSTRACT TRUNCATED AT 250 WORDS)

show abstract

Section: Methodsmentioning

confidence: 99%

Verapamil disposition‐effects of sulphinpyrazone and cimetidine.

Wing¹,

Miners²,

Lillywhite³

1985

Brit J Clinical Pharma

View full text Add to dashboard Cite

show abstract

“…The fraction of drug unbound in blood was calculated as fu p /R B , where fu p is the fraction unbound in plasma and R B is the blood/plasma concentration ratio. For PHEN, fu p was taken as 0.60 (Vesell et al, 1975) and R B as 1.01 (Shibata et al, 2002), whereas for LID fu p was 0.30 (Wing et al, 1984) and R B was 0.84 (Shibata et al, 2002). These values provided unbound fractions of PHEN and LID in blood of 0.59 and 0.36, respectively.…”

Section: Inhibition Of Phenacetin O-deethylation By Fatty Acidsmentioning

confidence: 99%

Effect of Albumin on Human Liver Microsomal and Recombinant CYP1A2 Activities: Impact on In Vitro-In Vivo Extrapolation of Drug Clearance

Wattanachai¹,

Tassaneeyakul²,

Rowland³

et al. 2012

Drug Metab Dispos

View full text Add to dashboard Cite

ABSTRACT:Long-chain unsaturated fatty acids inhibit several cytochrome P450 and UDP-glucuronosyltransferase (UGT) enzymes involved in drug metabolism, including CYP2C8, CYP2C9, UGT1A9, UGT2B4, and UGT2B7. Bovine serum albumin (BSA) enhances these cytochrome P450 and UGT activities by sequestering fatty acids that are released from membranes, especially with human liver microsomes (HLM) as the enzyme source. Here, we report the effects of BSA on CYP1A2-catalyzed phenacetin (

show abstract

“…Plasma lignocaine concentrations were determined by a specific gas-liquid chromatographic procedure employing nitrogen-phosphorous detection (Wing et al, 1984).…”

Section: Analyticalmentioning

confidence: 99%

Failure of ‘therapeutic’ doses of beta‐adrenoceptor antagonists to alter the disposition of tolbutamide and lignocaine.

Miners¹,

Wing²,

Lillywhite³

et al. 1984

Brit J Clinical Pharma

View full text Add to dashboard Cite

The effects of separate 1 week pre‐treatments with each of the beta‐ adrenoceptor antagonists, propranolol (80 mg every 12 h), metoprolol (100 mg every 12 h) and atenolol (50 mg once daily), on the disposition of a single i.v. dose of tolbutamide were studied in six healthy volunteers. In addition, the effects of a 1 week pre‐treatment with metoprolol (100 mg every 12 h) and atenolol (50 mg once daily) on the disposition of orally and i.v. administered lignocaine were determined in seven healthy subjects. Tolbutamide clearance, half‐life, volume of distribution and plasma protein binding were not altered by the beta‐ adrenoceptor blocker pre‐treatments. Similarly, neither metoprolol nor atenolol had a significant effect on the systemic clearance, apparent oral clearance or other dispositional parameters of lignocaine. ‘Therapeutic’ plasma concentrations of the beta‐adrenoceptor blockers were confirmed on each study day. It is concluded that the inhibition of oxidative drug metabolism previously reported for lipophilic beta‐ adrenoceptor blockers may be selective for different forms of cytochrome P450 and possible concentration‐dependent.

show abstract

Lidocaine disposition—Sex differences and effects of cimetidine

Cited by 56 publications

References 1 publication

Verapamil disposition‐effects of sulphinpyrazone and cimetidine.

Verapamil disposition‐effects of sulphinpyrazone and cimetidine.

Effect of Albumin on Human Liver Microsomal and Recombinant CYP1A2 Activities: Impact on In Vitro-In Vivo Extrapolation of Drug Clearance

Failure of ‘therapeutic’ doses of beta‐adrenoceptor antagonists to alter the disposition of tolbutamide and lignocaine.

Contact Info

Product

Resources

About