The clinical pharmacology of mexiletine.

Campbell, Norman P.S.; Kelly, J.G.; Adgey, A A; Shanks, R. G.

doi:10.1111/j.1365-2125.1978.tb00833.x

Cited by 129 publications

(50 citation statements)

References 8 publications

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“…Plasma therapeutic concentrations are within the range 0.75-2 ,ug/ml (Campbell et al, 1978a). Side effects increase at plasma levels greater than 2 pug/ml without improvement in the therapeutic efficacy.…”

Section: Introductionmentioning

confidence: 87%

Pharmacokinetics of mexiletine in renal insufficiency.

Allaf¹,

Henrard²,

Crochelet³

et al. 1982

Brit J Clinical Pharma

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1 The aim of this study was to evaluate the influence of renal insufficiency on the plasma pharmacokinetics of mexiletine, a new antiarrhythmic agent, in human beings. 2 Mexiletine was administered orally three times daily for 10 days to 15 patients with chronic renal failure (creatinine clearance lower than 30 ml/min) and to 9 subjects with normal renal function. 3 The use of low doses of mexiletine was possible owing to the development of a new fluorescence h.p.l.c. method with a limit of sensitivity lower than 20 gn/ml. 4 Our results clearly indicate that the plasma kinetics of mexiletine are not modified when the renal clearance of creatinine is higher than 10 ml/min.

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Section: Introductionmentioning

confidence: 87%

Pharmacokinetics of mexiletine in renal insufficiency.

Allaf¹,

Henrard²,

Crochelet³

et al. 1982

Brit J Clinical Pharma

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“…Less than 10% of an administered dose is recovered unchanged in urine (Prescott et al, 1977). An important cor-relation exists between the serum concentrations of the drug and both its antiarrhythmic and toxic effects (Talbot et al, 1973;Campbell et al, 1978a). However, considerable overlap has been observed between the therapeutic and toxic concentrations.…”

Section: Introductionmentioning

confidence: 99%

Stereoselective disposition of mexiletine in man.

Grech-Bélanger¹,

Turgeon²,

Gilbert³

1986

Brit J Clinical Pharma

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1 The pharmacokinetics of S-(+)-and R-(-)-mexiletine and of the corresponding conjugates were investigated in six healthy young volunteers after administration of a single 200 mg oral dose of racemic mexiletine hydrochloride.2 The values for the distribution rate constants as well as for the elimination half-lives of the two enantiomers were similar but the AUC of the S-(+)-enantiomer was always significantly higher (P < 0.01) than that of the opposite enantiomer. The mean R/S ratios for unchanged mexiletine in serum and in urine were 0.78 ± 0.12 (s.d.) and 0.80 + 0.21, respectively.3 Urinary excretion of mexiletine conjugates consisted mainly of the R-(-)-enantiomer; the mean R/S enantiomeric ratio over 48 h was 9.65 + 3.10. 4 Serum concentrations of the conjugates were measured in three subjects. The mean R/S AUC ratio was 2.94 ± 0.48 and the renal clearance of the R-(-)-enantiomer was significantly higher (P < 0.02) than that of the S-(+)-enantiomer.

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“…Following administration of antacid, tmax was significantly increased to a mean of 2.9 + 1.0 h (P < 0.02). (Prescott et al, 1977;Campbell et al, 1978a, Haselbarth etal., 1981.…”

Section: Rasmussen S and Nielsen Pe (1978)mentioning

confidence: 99%

“…Side effects of oral mexiletine therapy include gastrointestinal disturbances such as indigestion, vomiting, and nausea (Campbell et al, 1978a;Opie, 1980). Such symptoms are often treated with gastric antacids.…”

Section: Rasmussen S and Nielsen Pe (1978)mentioning

confidence: 99%