A Single-Dose Crossover Pharmacokinetic Comparison Study of Oral, Rectal and Topical Quetiapine in Healthy Adults

Jonathan G. Leung, Sarah Nelson, Julie L. Cunningham, Virginia H. Thompson, William V Bobo, Simon Kung, Ross A. Dierkhising, Matthew F. Plevak, Maria Isabel Lapid

Research output: Contribution to journalArticle

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Abstract

Introduction: Quetiapine is an oral atypical antipsychotic drug commonly used to treat a large number of neuropsychiatric disorders and conditions. However, a substantial number of patients who may benefit from treatment with quetiapine are unable to ingest quetiapine or other medications by mouth and thus require alternative routes of administration. There are currently no studies evaluating non-oral compounded dosage forms of quetiapine. Methods: We conducted a single-dose open-label crossover pharmacokinetic study in 10 healthy adults to determine whether quetiapine compounded as a rectal suppository or a topical cream achieved absorption similar to that achieved by a commercially available oral formulation. Results: Rectal quetiapine produced an area under the plasma concentration–time curve from time zero to infinity (AUC) approximately 90 % greater than that produced by an equal (milligram per milligram) dose of oral quetiapine (15,333 ng/mL versus 8118.8 ng/mL, p = 0.005). However, only two of ten subjects who received topical quetiapine had detectable serum levels. When detected, serum levels achieved with topical quetiapine were delayed and low in comparison with those produced by the oral and rectal dosage forms. Conclusion: Our results suggest that rectal, but not topical, quetiapine may be useful in clinical settings. Clinical outcome studies of rectal quetiapine are needed.

Original languageEnglish (US)
Pages (from-to)1-6
Number of pages6
JournalClinical Pharmacokinetics
DOIs
StateAccepted/In press - Feb 12 2016

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Pharmacokinetics
Dosage Forms
Quetiapine Fumarate
Suppositories
Serum
Cross-Over Studies
Antipsychotic Agents
Area Under Curve
Mouth
Outcome Assessment (Health Care)

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology

Cite this

A Single-Dose Crossover Pharmacokinetic Comparison Study of Oral, Rectal and Topical Quetiapine in Healthy Adults. / Leung, Jonathan G.; Nelson, Sarah; Cunningham, Julie L.; Thompson, Virginia H.; Bobo, William V; Kung, Simon; Dierkhising, Ross A.; Plevak, Matthew F.; Lapid, Maria Isabel.

In: Clinical Pharmacokinetics, 12.02.2016, p. 1-6.

Research output: Contribution to journalArticle

Leung, Jonathan G. ; Nelson, Sarah ; Cunningham, Julie L. ; Thompson, Virginia H. ; Bobo, William V ; Kung, Simon ; Dierkhising, Ross A. ; Plevak, Matthew F. ; Lapid, Maria Isabel. / A Single-Dose Crossover Pharmacokinetic Comparison Study of Oral, Rectal and Topical Quetiapine in Healthy Adults. In: Clinical Pharmacokinetics. 2016 ; pp. 1-6.
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