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商品名称:美国三唑仑
商品类别:迷香香水
商品编号:222222222
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库存数量:998
浏览次数:164
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上市时间:2018-4-16 17:38:14
市场价:¥1500
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Hypnotic
Triazolam is a benzodiazepine with a very short elimination half-life (about 3 hours). In sleep laboratory studies in man of 1 to 21 days duration, triazolam reduced sleep latency, increased duration of sleep and decreased the number of nocturnal awakenings. However, after 2 weeks of consecutive nightly administration, the drug's effect on total wake time is decreased, and the values recorded in the last third of the night approach baseline levels. On the first and/or second night after drug discontinuance (first or second post-drug night), total time asleep, and percentage of time spent sleeping frequently were significantly decreased, and sleep latency significantly increased when compared to baseline (predrug) nights. This effect is often called "rebound" insomnia. The duration of hypnotic effect and the profile of unwanted effects may be influenced by the alpha (distribution) and beta (elimination) half-lives of the administered drug and any active metabolites formed. When half-lives are long, the drug or metabolites may accumulate during periods of nightly administration and be associated with impairments of cognitive and motor performance during waking hours. If half-lives are short, the drug and metabolites will be cleared before the next dose is ingested, and carry-over effects related to sedation or CNS depression should be minimal or absent. However, during nightly use and for an extended period, pharmacodynamic tolerance or adaptation to some effects of benzodiazepine hypnotics may develop. If the drug has a very short elimination half-life, it is possible that a relative deficiency (i.e., in relation to the receptor site) may occur at some point in the interval between each night's use. This sequence of events may account for two clinical findings reported to occur after several weeks of nightly use of rapidly eliminated benzodiazepine hypnotics: (1) increased wakefulness during the last third of the night and (2) the appearance of increased day-time anxiety (see Warnings). When sedation and psychomotor performance were compared in healthy elderly and young subjects, in response to 0.125 and 0.25 mg doses of triazolam, the degree of sedation was greater and the impairment of psychomotor performance more pronounced in the elderly. The age dependent difference was closely associated with the correspondingly higher plasma triazolam concentrations measured in elderly subjects. Patients with severe liver disease also demonstrated greater psychomotor impairment than control subjects or patients with minimal liver dysfunction. Pharmacokinetics: Triazolam is rapidly absorbed and peak plasma levels are reached within 2 hours following oral administration. Peak plasma concentration (C (max)) and area under the plasma-concentration curve (AUC) increase in proportion to the dose, while the time to peak plasma concentration (T(max)), elimination half-life (t 1/2beta), and clearance are independent of dose. Triazolam has a short half-life; the range is reported to be 1.5 to 5.5 hours. Triazolam is metabolized via hepatic microsomal oxidation. The hydroxylated metabolites, which are inactive, are excreted primarily in the urine as conjugated glucuronides. The two primary metabolites account for approximately 80% of the urinary excretion. Repeated administration of triazolam for 7 days does not lead to accumulation and does not alter the rate of elimination. Pharmacokinetics in the elderly: The kinetics of triazolam are significantly influenced by age (see Table I). Following single oral doses of 0.125 mg and 0.25 mg of triazolam, peak plasma concentrations and area under the curve were significantly higher and clearance significantly lower in elderly subjects (mean age: 69 years) than in younger one (mean age: 30 years). Age, however, did not influence the time to peak plasma levels and differences in elimination half-life were small
 

 

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