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Elimination of brotizolam in elderly patients after multiple doses

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Summary

Plasma brotizolam levels were measured in 5 elderly patients given 0.25 mg daily. The half-life of brotizolam elimination was 6.0 h after a single dose and 6.9 h after continuous administration for 3 weeks. The brotizolam concentration in plasma 2 h after the dose was 3.5 and 3.4 ng/ml, respectively, on the first and last days of the study. Brotizolam levels measured several times during the study 10 h after dosing were between 1.2 and 1.8 ng/ml.

Thus, administration of brotizolam 0.25 mg/d to elderly patients for 3 weeks led neither to its accumulation nor to faster elimination. The half-life of brotizolam elimination in elderly patients was in the upper range of that found in young volunteers.

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References

  1. Kohn RR (1963) Human aging and disease. J Chronic Dis 16, 5–12

    Google Scholar 

  2. Ritschel WA (1980) Disposition of drugs in geriatric patients. Trends Pharm Int 1: 226–230

    Google Scholar 

  3. Klotz U, Avant GR, Hoyumpa A, Scheuber S, Wilkinson GR (1975) The effects of age and liver disease on the disposition and elimination of diazepam in adult man. J Clin Invest 55: 347–359

    Google Scholar 

  4. Greenblatt DJ, Divoll M, Abernethy DR, Moschitto LJ, Smith RB, Shader RI (1983) Alprazolam kinetics in the elderly. Arch Gen Psychiatry 40, 287–290

    Google Scholar 

  5. Greenblatt DJ, Shader RI (1980) Kinetics of diazepam and lorazepam in the elderly. Psychopharmacol Bull 16: 56–57

    Google Scholar 

  6. Greenblatt DJ, Divoll M, Harmatz JS, Shader RI (1980) Oxazepam kinetics: Effects of age and sex. J Pharmacol Exp Ther 215, 86–91

    Google Scholar 

  7. Estal RE (1978) Drug use in the elderly: A review of problems and special considerations. Drugs 16: 358–382

    Google Scholar 

  8. Greenblatt DJ, Shader RI (1981) Pharmacokinetics in old age: Principles and problems of assessment. In: Jarvik LF, Greenblatt DJ, Harman DF (eds) Clinical pharmacology and the aged patient. Raven Press, New York

    Google Scholar 

  9. Saletu B, Grünberger J, Volavka J, Berner P (1979) Classification and bioavailability studies with We 941 by quantitative pharmaco-EEG and clinical analysis. Arzneimittelforsch 29: 700–704

    Google Scholar 

  10. Kubicki S (1979) Elektroenzephalographische Dosis- und Schlafprofil-Beurteilung eines Hypnotikums aus der Reihe der Triazolothienodiazepine. Z EEG-EMG 10: 95–100

    Google Scholar 

  11. Nicholson AN, Stone BM, Pascoe PA (1980) Studies on sleep and performance with a triazolo-1,4-thieno-diazepin (brotizolam). Br J Clin Pharmacol 10: 75–81

    Google Scholar 

  12. Fink M, Irwin P (1981) Pharmaco-EEG study of brotizolam, a novel hypnotic. Clin Pharmacol Ther 30: 336–342

    Google Scholar 

  13. Bechtel WD, Mierau J, Stiasni M, Richter I (1986) Absorption, distribution, metabolite pattern, and excretion of [14C]brotizolam (We 941), a new hypnotic, in rats, dogs and monkeys. Arzneimittelforsch 36: 568–574

    Google Scholar 

  14. Bechtel WD, van Wayjen RGA, von den Ende A (1986) Blood level, excretion, and metabolite pattern of [14C]-brotizolam (We 941) in humans. Arzneimittelforsch 36: 575–578

    Google Scholar 

  15. Bechtel WD (1983) Pharmacokinetics and metabolism of brotizolam in animals. Br J Clin Pharmacol 16: 261 S-266 S

    Google Scholar 

  16. Bechtel WD (1983) Pharmacokinetics and metabolism of brotizolam in humans. Br J Clin Pharmacol 16: 279 S-283 S

    Google Scholar 

  17. Jochemsen R, Wesselman JGJ, Hermans J, van Boxtel CJ, Breimer DD (1983) Pharmacokinetics of brotizolam in healthy subjects following intravenous and oral administration. Br J Clin Pharmacol 16: 285 S-290 S

    Google Scholar 

  18. Bechtel WD, Weber KH (1985) Brotizolam radioimmunoassay: Development, evaluation, and application to human plasma samples. J Pharm Sci 74: 1265–1269

    Google Scholar 

  19. Greenblatt DJ, Locniskar A, Shader RI (1983) Pilot pharmacokinetic study of brotizolam, a thienodiazepine hypnotic, using electron-capture gas-liquid chromatography. Sleep 6: 72–76

    Google Scholar 

  20. Jochemsen R, Nandi KL, Corless D, Wesselman JGJ, Breimer DD (1983) Pharmacokinetics of brotizolam in the elderly. Brit J Clin Pharmacol 16: 299 S-307 S

    Google Scholar 

  21. Bechtel WD, Mierau J, Brandt K, Förster HJ, Pook KH (1986) Metabolic fate of [14C]brotizolam (We 941) in the rat, dog, monkey and man. Arzneimittelforsch 36: 578–586

    Google Scholar 

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Authors and Affiliations

  1. Department of Biochemistry, Boehringer Ingelheim KG, Ingelheim, Federal Republic of Germany

    W. D. Bechtel

  2. Department of Medicine, Boehringer Ingelheim KG, Ingelheim, Federal Republic of Germany

    E. Goetzke

Authors
  1. W. D. Bechtel
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  2. E. Goetzke
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Additional information

Preliminary results were reported at the Brotizolam Symposium, Bad Schachen, FRG, 1982. (Br J Clin Pharmacol (1983) 16 [Suppl 2]: 201 S–442 S)

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Bechtel, W.D., Goetzke, E. Elimination of brotizolam in elderly patients after multiple doses. Eur J Clin Pharmacol 31, 243–245 (1986). https://doi.org/10.1007/BF00606668

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  • DOI: https://doi.org/10.1007/BF00606668

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