The clinical pharmacokinetics of buflomedil in normal subjects after intravenous and oral administration

Gundert‐Remy, Ursula; Weber, E; Lam, Gilbert N.; Chiou, Win L.; Mann, W.C.; Aynilian, G.H.

doi:10.1007/bf00542100

Cited by 21 publications

(11 citation statements)

References 9 publications

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“…Buflomedil has been used for the treatment of periph eral vascular disease [1,2]. Studies by Fagrell and Hermansson [3] have shown that buflomedil is effective in the treatment of patients with acral gangrene, and Triibestein et al [4] demonstrated an improvement in the claudica tion distance in patients with chronic arterial disease.…”

Section: Introductionmentioning

confidence: 99%

Effects of Buflomedil on Spontaneous Vasomotion and Mean Arteriolar Internal Diameter in the Hamster Cheek Pouch

Cyrino¹

1994

J Vasc Res

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Intravital microscopy of the hamster cheek pouch microvasculature was used for in vivo studies on the effects of buflomedil, phentolamine (α-adrenergic receptor antagonist) and norepinephrine on the mean internal arteriolar diameter and spontaneous vasomotion. All drugs were applied topically. The vasomotor activity was studied in 125 arterioles (internal diameter range 18.0–62.0 µm) of 34 preparations. Addition of buflomedil (10^–9 to 10^–5M) did not affect the arteriolar diameter significantly (from 100.7 ± 3.5 to 106.4 ± 1.8%, values expressed in percent of the initial diameter as mean ± SE), but increased the vasomotion frequency and amplitude by approximately 20% (from 7.5 ± 0.3 to 9.2 ± 0.2 cpm) and 30% (from 7.3 ± 0.3 to 10.0 ± 0.5 µm), respectively. Phentolamine (10^–9 to 10^–5M) dose-dependently increased the microvascular diameter (from 102.3 ± 1.2 to 139.1 ± 4.3%) and reduced the vasomotion frequency and amplitude (from 8.0 ± 0.3 to 1.9 ± 0.5 cpm and from 9.0 ± 2.1 to 3.1 ± 0.2 µm, respectively). Addition of buflomedil (10^–7M) reduced the vasodilation evoked by phentolamine (from 103.3 ± 0.7 to 127.0 ± 1.5%) and potentiated its depressive effect on vasomotion frequency and amplitude (from 7.6 ± 0.1 to 1.0 ± 0.3 cpm and from 9.0 ± 0.3 to 1.9 ± 0.6 µm, respectively). Norepinephrine (10^–9 to 10^–5M) dose-dependently decreased to arteriolar diameter (from 102.3 ± 0.7 to 69.6 ± 1.6%) and the vasomotion frequency and amplitude (from 8.4 ± 0.2 to 0.4 ± 0.3 emp and from 8.7 ± 0.2 to 0.5 ± 0.4 µm, respectively). Addition of buflomedil (10^–7 M) reduced the vasoconstriction elicited by norepinephrine (from 103.2 ± 0.9 to 82.9 ± 3.9%) and restored the vasomotion frequency and amplitude (from 8.4 ± 0.3 to 7.8 ± 0.4 cpm and from 8.6 ± 0.2 to 7.8 ± 0.3 µm, respectively). The effects observed with buflomedil on the hamster cheek pouch microcirculation suggest a direct action on the smooth muscle excitability and further support its properties as a competitive inhibitor of α-adrenergic receptors and as a weak calcium antagonist.

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Section: Introductionmentioning

confidence: 99%

Effects of Buflomedil on Spontaneous Vasomotion and Mean Arteriolar Internal Diameter in the Hamster Cheek Pouch

Cyrino¹

1994

J Vasc Res

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“…It is especially well adapted for the management of buflomedil poisoning yielding concentrations generally above the therapeutic range (20 mg/mL; Gunder- Remy et al, 1981;Zecca et al, 1989). Under the chromatographic conditions, buflomedil and metoclopramide (IS) were sufficiently resolved from endogenous plasma compounds and their retention times were t r = 2.31 AE 0.30 min for metoclopramide and t r = 4.05 AE 0.42 min for buflomedil.…”

Section: Resultsmentioning

confidence: 98%

Rapid HPLC measurement of buflomedil in plasma in poisoning cases

Forfar‐Bares

Péhourcq²,

Jarry

2002

Biomedical Chromatography

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A rapid high-performance liquid chromatographic method for the determination of buflomedil in human plasma is described. It requires a single liquid-liquid extraction step from 1 mL of plasma with diethyl ether followed by chromatography on a Nova Pak C(18) reversed-phase column and detection by ultaviolet light. Metoclopramide was used as internal standard. The method is sensitive with a quantification limit at 500 ng/mL. It was used for the determination of buflomedil in biological fluids in poisoning cases.

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“…The detection limit (10 ng/spot) and the quantification limit (27 ng/spot) were estimated according to Knoll's theory [4] 1 Introduction The mobile phase was a 10% solution of dichloromethane in acetonitrile (UV grade, Merck). The reagents for extraction were: ethanol p.a.…”

Section: Resultsmentioning

confidence: 99%

Determination of pentachlorophenol by high performance thin layer chromatography

Pérez

Barrios

Saelzer

et al. 1989

J. High Resol. Chromatogr.

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The clinical pharmacokinetics of buflomedil in normal subjects after intravenous and oral administration

Cited by 21 publications

References 9 publications

Effects of Buflomedil on Spontaneous Vasomotion and Mean Arteriolar Internal Diameter in the Hamster Cheek Pouch

Effects of Buflomedil on Spontaneous Vasomotion and Mean Arteriolar Internal Diameter in the Hamster Cheek Pouch

Rapid HPLC measurement of buflomedil in plasma in poisoning cases

Determination of pentachlorophenol by high performance thin layer chromatography

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