Polygraphic study in man to differentiate sleep-inducing action of hypnotics

Fernández-Guardiola, Augusto; Tejada, Aguilar; Contreras, Carlos M.; Salgado, Alejandro Stilmann; Ayala, Fructuoso

doi:10.1007/bf00422704

Psychopharmacologia

1972

DOI: 10.1007/bf00422704

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Polygraphic study in man to differentiate sleep-inducing action of hypnotics

Augusto Fernández-Guardiola¹,

Aguilar Tejada²,

Carlos M. Contreras³

et al.

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1975

1989

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Cited by 7 publications

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Pharmacokinetics and relative bioavailability of heptabarbital and heptabarbital sodium after oral administration to man

Breimer

Boer

1975

Eur J Clin Pharmacol

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A method has been developed for the quantitative determination of heptabarbital [5-(1-cyclohepten-1-yl)-5-ethylbarbituric acid] in human plasma after administration of single therapeutic doses of the drug. It involves a single extraction step followed by gas chromatography with alkali flame ionization detection, and the results were linear in the concentration range 0.125 - 5.0 mug/ml plasma. The pharmacokinetics and relative bioavailability of heptabarbital and heptabarbital sodium were studied in a crossover design in 7 healthy volunteers after oral administration of 20 tablets containing 200 mg heptabarbital and hard gelatine capsules containing an equivalent amount of its sodium salt. Heptabarbital concentrations in plasma were determined at regular intervals. The absorption of heptabarbital from the tablets absorbed more rapidly and peak concentrations occurred between 1/3 and 2 h. In all cases the elimination of heptabarbital could be described by a single first-order process with an average half-life of 7.6 h (range 6.1 - 11.2 h). The half-life of the drug in each individual was about the same in the two trials. The relative bioavailability in each volunteer was estimated by comparing the areas under the plasma concentration curves. The sodium salt had an average bioavailability of 83% relative to the free acid. In some volunteers urinary excretion of unchanged heptabarbital was measured; cumulative excretion amounted to 0.16 - 0.30% of the administered dose. Four volunteers received one tablet each night for eight or ten days, but no accumulation was found. In three volunteers the half-life of the drug prior to and after these experiments did not change, whereas in the other volunteer the half-life decreased from 7.1 to 4.6 h. The possibility of enzyme induction should be considered when heptabarbital is taken regularly. It was concluded that heptabarbital was a suitable drug for the treatment of insomnia, since its half-life was rather short. Heptabarbital sodium may be used for induction of sleep, whereas Medomin tablets, i.e. heptabarbital free acid, may be prescribed when the maintenance of sleep is the primary reason for treatment with a hypnotic drug.

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Pharmacokinetics and relative bioavailability of heptabarbital and heptabarbital sodium after oral administration to man

Breimer

Boer

1975

Eur J Clin Pharmacol

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Effects of 1 week administration of two benzodiazepines on the sleep and early daytime performance of normal subjects

1989

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This study analyzed the effects of 1 week administration of alprazolam (AL; 0.25 mg), lorazepam (LO; 1 mg) and placebo (PL) on sleep as well as their residual effects on attention upon awakening. Under a crossed, double-blind design, six healthy male volunteer subjects between 19 and 30 years of age were studied. After two habituation sessions and a control session, each substance was given orally, twice a day for 7 days, with a 1-week washout period between administrations. At the end of each administration period, sleep studies were conducted from 2300 to 0700 hours. Evaluation of attention was carried out by means of a simple visuomotor reaction time (RT) task, and a time estimation (TE) task, that started at 0700 hours, lasting 1 h. Neither drug significantly affected any sleep variable. Both benzodiazepines tended to increase RT, but only LO did so significantly at the beginning of the attention test. No significant changes in predictive and failure responses during the RT task were produced by either drug. Also, no significant changes were observed in the TE. Even though only LO produced a significant increase of RT at the selected doses and with 1 week administration, it is suggested that both benzodiazepines could have residual effects on attention.

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Normal human subjects with slow reaction times and larger time estimations after waking have diminished delta sleep

Jurado

Luna-Villegas

Buela-Casal

1989

Electroencephalography and Clinical Neurophysiology

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Polygraphic study in man to differentiate sleep-inducing action of hypnotics

Cited by 7 publications

References 3 publications

Pharmacokinetics and relative bioavailability of heptabarbital and heptabarbital sodium after oral administration to man

Pharmacokinetics and relative bioavailability of heptabarbital and heptabarbital sodium after oral administration to man

Effects of 1 week administration of two benzodiazepines on the sleep and early daytime performance of normal subjects

Normal human subjects with slow reaction times and larger time estimations after waking have diminished delta sleep

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