RESUMO
The bioavailability, pharmacokinetics, and effects on performance of lormetazepam (1 mg) have been compared using soft gelatin capsule and tablet formulations. Lormetazepam was more rapidly absorbed from the soft gelatin capsule (tmax = 1.0 +/- 0.2 h) than from the tablet (tmax = 2.4 +/- 0.4 h), and the plasma concentration-time curve for the capsule was shifted to the left. Bioavailability and elimination kinetics did not differ between the formulations. The number of substitutions in the digit symbol test was reduced between 0.5 and 1.5 h for both formulations (P less than 0.001), but the degree of impairment at 0.5 h was greater after the capsule than after the tablet (P less than 0.01). Visuo-motor co-ordination was impaired from 0.5 to 1.5 h after the tablet and the capsule (P less than 0.01), and extended to 5.5 h after the tablet (P less than 0.05). These observations reflect the differences in the plasma concentration-time curves.
Assuntos
Ansiolíticos/metabolismo , Benzodiazepinas , Lorazepam/análogos & derivados , Absorção , Adolescente , Adulto , Ansiolíticos/administração & dosagem , Ansiolíticos/sangue , Ansiolíticos/farmacologia , Disponibilidade Biológica , Cápsulas , Humanos , Cinética , Lorazepam/administração & dosagem , Lorazepam/sangue , Lorazepam/metabolismo , Lorazepam/farmacologia , Masculino , Pessoa de Meia-Idade , ComprimidosRESUMO
In an open, multicentre study, the short-acting benzodiazepine hypnotic lormetazepam (Loramet) was administered nightly (1-2 mg p.o.) for a period of 7 nights to 665 out-patients with various types of sleep disturbances. The patients assessed the efficacy and acceptability of lormetazepam with the aid of a simple diary card and a set of visual analogue scales. The results showed that about 75% of the patients reported a significant improvement in their sleep pattern. The time to onset of sleep was decreased, the number of nocturnal wakings was reduced and the patients reported waking in the morning more refreshed and co-ordinated. The effects were significant after the first night and there were further significant improvements by the seventh night on the drug. In patients who had prior experience of other hypnotics, twice as many preferred lormetazepam to temazepam and three times as many preferred lormetazepam to nitrazepam. Nine patients withdrew from the study due to lack of efficacy and only fifteen patients dropped out following the occurrence of side-effects, mainly drowsiness and light-headedness. It was concluded that lormetazepam is an effective and highly acceptable hypnotic in patients with sleep disturbances.
Assuntos
Ansiolíticos , Benzodiazepinas , Hipnóticos e Sedativos/uso terapêutico , Lorazepam/análogos & derivados , Transtornos do Sono-Vigília/tratamento farmacológico , Administração Oral , Adolescente , Adulto , Idoso , Ensaios Clínicos como Assunto , Feminino , Humanos , Lorazepam/administração & dosagem , Lorazepam/efeitos adversos , Lorazepam/uso terapêutico , Masculino , Pessoa de Meia-Idade , Pacientes AmbulatoriaisRESUMO
An open, multi-centre study was carried out in 804 patients complaining of sleep disorders to assess the effectiveness and acceptance of temazepam as a hypnotic. Patients received between 10 mg and 30 mg (mean 16.4 mg) temazepam each night for a week. Subjective assessments using a self-administered questionnaire were made daily of the quality and quantity of sleep. The results showed that sleep induction was rapid and most patients enjoyed a relatively uninterrupted night's sleep, and awakened feeling refreshed. Patient acceptance was good and there was a low incidence of residual or other adverse effects of treatment.
