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Pharmacokinetic and Pharmacodynamic Evaluation of the Inhibition of Alprazolam by Citalopram and Fluoxetine

2003· article· en· W2067493036 on OpenAlexaff
Judith Hall, Claudio A. Naranjo, Beth Sproule, Nathan Herrmann

Bibliographic record

VenueJournal of Clinical Psychopharmacology · 2003
Typearticle
Languageen
FieldPharmacology, Toxicology and Pharmaceutics
TopicPharmacogenetics and Drug Metabolism
Canadian institutionsSunnybrook Health Science Centre
FundersH. Lundbeck A/S
KeywordsCitalopramAlprazolamSerotonin reuptake inhibitorPharmacologyFluoxetineReuptake inhibitorSerotonin Uptake InhibitorsAntidepressantPharmacokineticsDrug interactionCYP3APharmacodynamicsCYP3A4ChemistryCytochrome P450MedicineSerotoninInternal medicineMetabolismPsychiatryReceptor

Abstract

fetched live from OpenAlex

The selective serotonin reuptake inhibitor antidepressant fluoxetine inhibits alprazolam metabolism in vivo by inhibition of the cytochrome P450 3A4 enzyme. Citalopram is a selective serotonin reuptake inhibitor antidepressant that has not yet been fully evaluated with respect to its potential for cytochrome P450 3A4-mediated drug interactions in vivo. Building on the existing in vitro and in vivo evidence that suggest a minimal effect of citalopram on cytochrome P450 3A4, we hypothesized that therapeutic doses of citalopram (20 mg/d), as compared with fluoxetine (20 mg/d), would cause less impairment in the metabolism of the probe drug alprazolam (1 mg) through inhibition of the cytochrome P450 3A4 isozyme as measured by pharmacokinetic and pharmacodynamic parameters in vivo. We found that fluoxetine prolonged the half-life of alprazolam by 16% and increased the area under the curve 0-infinity of alprazolam by 32%, while citalopram did not affect these parameters, although the time of maximum concentration of alprazolam was prolonged by 30 minutes after citalopram administration. Neither selective serotonin reuptake inhibitor significantly affected the pharmacodynamic profile of alprazolam. This experiment suggests differential effects by citalopram and fluoxetine on alprazolam kinetics.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.011
metaresearch head score (Gemma)0.001
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMeta-epidemiology (narrow), Insufficient payload (model declined to judge)
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.256
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0110.001
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0010.000
Bibliometrics0.0000.000
Science and technology studies0.0000.001
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.002
Insufficient payload (model declined to judge)0.0010.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.149
GPT teacher head0.535
Teacher spread0.386 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations28
Published2003
Admission routes1
Has abstractyes

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