Pharmacokinetic differences hypnotics ...

Pharmacokinetic differences of three generations of hypnotics are determined by their main characteristics as the rate of absorption, half life, the presence of active metabolites, the type of metabolization and other general provisions in this regard, approximating an ideal hypnotic for ? ?, is the need to increase the absorption (rate the onset of sleep), limiting the therapeutic effect of normal sleep duration (short half-life), lack of active metabolites (predictability), a simpler form of metabolization (conjugation) and other high-speed suction different number of drugs both second and third generations of zolpidem, zopiclone , flunitrazepam, triazolam, flurazepam. However, only a third-generation hypnotics advised to take even while lying in bed. Accumulation of hypnotic and its subsequent ability to cause prolonged action and daytime sedation was determined primarily by the measure of half-life and total metabolic clearance. Obviously, at the rate of the drug half-life affected by the presence of active metabolites and their level of elimination. If the half-life of the drug and its active metabolite is short, there is minimal accumulation of drug. Thus, there is the least possibility of daytime sleepiness and reduced performance. The half-life of drugs of the third generation is as short (eg, 2,5 hours of zolpidem, zopiclone 5 hours), whereas the majority of benzodiazepine hypnotics are characterized by long half-life (eg flurazepam 80 hours, 28 hours, Nitrazepam, flunitrazepam 19 hours, estazolam 17 hours). Differences of three generations of hypnotics on the quantitative parameters to assess their actions lies in the expression of their influence on: the length of time to sleep, sleep duration, number of nighttime awakenings, frequency of dreams. This assessment is usually carried out by means of quantified methods of assessment (eg, rating scale Spiegel). One of the quantitative evaluation of hypnotics is to assess the effectiveness of sleep, which is defined as the quotient of sleep duration on the time spent in bed. In this case, the greater the degree of this figure is close to unity as a result of a hypnotic (sleep duration when fully corresponds to the time spent in bed), so its effectiveness. Differences of three generations of hypnotics on the quality parameters to assess their actions lies in the degree of normalization of sleep quality (including the architectonics of sleep, subjective assessment of sleep), waking the quality (lack of aftereffect, the normalization of psycho-physiological parameters, subjective evaluation of awakening), the individual rhythm sonbodrstvovanie. It should be emphasized that quality of sleep, but not its quantitative indicators (duration or frequency of awakenings), has a paramount impact on the wellbeing of the next day, the normal daytime functioning of patients, lack of discomfort, ie includes the range of problems that focus the concept of quality life.