Estimation of phenytoin in body fluids in the presence of sulphonyl urea compounds

Thurkow, Ineke; Wesseling, H; Meijer, Dirk

doi:10.1016/0009-8981(72)90476-7

Cited by 6 publications

(1 citation statement)

References 5 publications

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“…They are used as seizure control drugs [10] [11] and preferred over barbiturate but in no way can reverse the effect of barbiturate as they have the same clinical action. Tolazamide which is an oral anti-diabetic drug has been documented to interfere with barbiturate [12] [13] . This is highly probable due to the fact that they both target similar active site found in this study.…”

Section: Discussionmentioning

confidence: 99%

Folate and Tolazamide: Potential competitive inhibitors of barbiturate by in-silico molecular docking

Sharp¹

2020

Preprint

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Barbiturates are the first line drugs for treatment of epilepsy for adults and children in the developing world because of its low cost and proven effectiveness. Due to their adverse effects, no effective management of toxicity and difficulty in determining correct dosage, benzodiazepines are preferred over them. It is also used as a recreational drug, thereby contributing to cases of overdose. My present study was to find the inhibitors of barbiturates by in-silico molecular docking. This approach can highlight only competitive inhibitors as molecules in-silico are rigid and do not produce conformational changes in structure by allosteric binding. 450 FDA-approved drugs were docked to active site of barbiturate of Gleobacter ligand-gated ion channel (GLIC). Drug interactions were visualized, literature search was done to bring out the final results. Tolazamide, an oral anti-diabetic drug and 5-methyltetrahydrofolate, active metabolite of folic acid produced desired results. These results should be used clinically for validation.

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Section: Discussionmentioning

confidence: 99%

Folate and Tolazamide: Potential competitive inhibitors of barbiturate by in-silico molecular docking

Sharp¹

2020

Preprint

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Interaction of diphenylhydantoin (DPH) and tolbutamide in man

Wesseling

Mols-Thürkow

1975

Eur J Clin Pharmacol

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The influence of tolbutamide administration on the plasma concentrations of diphenylhydantoin (DPH) was investigated in seventeen long-stay patients with epilepsy. Tolbutamide, 0.5 g 2-3x daily, considerably increased the proportion of non-protein-bound DPH in plasma (mean: 44.6% of control values). The increase was transient, unlike the decrease found in total plasma DPH-concentration (approx. 10% of control values). In vitro experiments confirmed that the interaction between DPH and tolbutamide was due to displacement of DPH from plasma proteins. Some factors that limit the capacity to metabolise DPH in the liver are discussed; they may increase the risk of DPH-intoxication in patients who take sulphonyl-ureas.

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Effect of sulphonylureas (tolazamide, tolbutamide and chlorpropamide) on the metabolism of diphenylhydantoin in the rat

Wesseling

Thurkow

Mulder

1973

Biochemical Pharmacology

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Estimation of phenytoin in body fluids in the presence of sulphonyl urea compounds

Cited by 6 publications

References 5 publications

Folate and Tolazamide: Potential competitive inhibitors of barbiturate by in-silico molecular docking

Folate and Tolazamide: Potential competitive inhibitors of barbiturate by in-silico molecular docking

Interaction of diphenylhydantoin (DPH) and tolbutamide in man

Effect of sulphonylureas (tolazamide, tolbutamide and chlorpropamide) on the metabolism of diphenylhydantoin in the rat

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