Clinical Pharmacokinetics of Alprazolam

@article{Greenblatt1993ClinicalPO,
  title={Clinical Pharmacokinetics of Alprazolam},
  author={David J Greenblatt and C. Eugene Wright},
  journal={Clinical Pharmacokinetics},
  year={1993},
  volume={24},
  pages={453-471}
}
SummaryAlprazolam is a triazolobenzodiazepine that is extensively prescribed in the Western world for the treatment of anxiety and panic disorders. Its benzodiazepine receptor binding characteristics are qualitatively similar to those of other benzodiazepines. The drug is metabolised primarily by hepatic microsomal oxidation, yielding α-hydroxy- and 4-hydroxy-alprazolam as principal initial metabolites. Both have lower intrinsic benzodiazepine receptor affinity than alprazolam and appear in… Expand
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References

SHOWING 1-10 OF 75 REFERENCES
Alprazolam: Pharmacokinetics, Clinical Efficacy, and Mechanism of Action
TLDR
Its primary side effect, drowsiness, is less than that produced by diazepam at comparable doses, and alprazolam seems to be at least comparable to other benzodiazepines. Expand
Alprazolam kinetics in the elderly. Relation to antipyrine disposition.
TLDR
Old age is associated with impaired capacity to oxidize alprazolam, but this effect is far more apparent in men than in women, and a test of antipyrine half-life and clearance may help identify slow or rapid metabolizers of alpazolam. Expand
Determination of biological activity of alprazolam, triazolam and their metabolites
The benzodiazepines are psychoactive drugs with wide therapeutic applications as anxiolytics, anticonvulsants, and muscle relaxants (Zbinden 8: Randall 1967). Their site and mechanism of action haveExpand
Inhibitors of alprazolam metabolism in vitro: effect of serotonin-reuptake-inhibitor antidepressants, ketoconazole and quinidine.
TLDR
Ketoconazole was a potent inhibitor of ALP metabolism in vitro, suggesting that ALP hydroxylation is mediated by the cytochrome P450-3A sub-family, and fluoxetine and sertraline were weak inhibitors. Expand
Pharmacokinetics and Clinical Effects of Alprazolam Following Single and Multiple Oral Doses in Patients With Panic Disorder
TLDR
Alprazolam clearance is independent of dose and plasma concentration up to daily doses of at least 9 mg/d, with steady‐state plasma level proportional to dosing rate. Expand
Clinical Pharmacokinetics of Anxiolytics and Hypnotics in the Elderly
TLDR
The weight of evidence indicates that old age is associated with impaired clearance of the benzodiazepines which are biotransformed by microsomal oxidation, which may lead to altered pharmacokinetics of sedative-anxiolytic drugs, causing higher plasma concentrations after single or multiple doses. Expand
Chronic benzodiazepine administration. IV. Rapid development of tolerance and receptor downregulation associated with alprazolam administration.
TLDR
The results indicate that behavioral tolerance and receptor downregulation develop rapidly during chronic alprazolam administration, and were similar to those associated with lorazepam administration but occurred more rapidly and with different regional specificity. Expand
Benzodiazepine Receptor Binding of Triazolobenzodiazepines In Vivo: Increased Receptor Number with Low‐Dose Alprazolam
TLDR
In vivo receptor binding, as defined by the specific uptake of [3H]Ro 15–1788, decreased with increasing doses of estazolam and triazol am, a finding indicating dose‐related increases in receptor occupancy due to these compounds, but alprazolam appears to be anomalous in that low brain concentrations increase benzodiazepine receptor number. Expand
Interaction of propoxyphene with diazepam, alprazolam and lorazepam.
TLDR
Propoxyphene significantly impairs the clearance of alprazolam, biotransformed mainly by the oxidative reaction of aliphatic hydroxylation, and has far less effect on the oxidation of diazepam by N-demethylation and has no apparent influence on lorazepam conjugation. Expand
Alprazolam Pharmacokinetics in Alcoholic Liver Disease
TLDR
The changes in elimination half‐life and clearance indicate that the metabolism of the drug is slowed in patients with alcoholic liver disease. Expand
...
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3
4
5
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