Bioavailability of Triprolidine as a Single Agent or in Combination With Pseudoephedrine: A Randomized, Open-Label Crossover Study in Healthy Volunteers.

Clinical Pharmacology in Drug Development
Salvatore FebbraroAna Santos Cravo

Abstract

Antihistamines have been in clinical use for more than 70 years to treat allergic and nonallergic symptoms including relief from cold and flu symptoms. Despite their widespread use, pharmacokinetic (PK) data are sparse for older, first-generation antihistamines. This phase 1 single-center open-label, randomized, single-dose, 3-way crossover trial evaluated the PK profiles of 2 doses of film-coated triprolidine caplets (2.5 and 5 mg) compared with a reference combination tablet (triprolidine 2.5 mg + pseudoephedrine 60 mg) in 24 healthy adults. Blood samples were collected predose and at specified intervals across a 24-hour period after administration, and triprolidine was quantified using liquid chromatography-tandem mass spectrometry. Maximum plasma concentration of triprolidine for the 2.5 mg and dose-normalized 5 mg single-agent tablets were comparable (8.4 versus 7.1 ng/mL, respectively) and higher for the combination tablet (9.5 ng/mL). PK parameters, including time to maximum plasma concentration (∼1.5 hours) and elimination half-life (∼4 hours), were comparable between the 3 treatment arms. The safety profile of this sedating antihistamine was as expected; however, adverse effects were reported in a markedly higher propo...Continue Reading

References

Jun 1, 1977·Journal of Pharmaceutical Sciences·R L DeAngelisR M Welch
Jun 1, 1990·Journal of Clinical Pharmacology·M V MilesM F Frosolono
May 1, 1989·Clinical Pharmacokinetics·H FriedmanR I Shader
Jan 1, 1985·European Journal of Clinical Pharmacology·A F CohenA W Peck
Nov 1, 1985·Clinical Pharmacokinetics·D M Paton, D R Webster
Jan 1, 1989·Clinical Pharmacology and Therapeutics·F GengoJ K Miller
Feb 1, 1986·The Journal of Allergy and Clinical Immunology·K J SimonsF E Simons
Oct 1, 1984·Journal of Pharmaceutical Sciences·J W FindlayR M Welch
May 1, 1995·The Journal of Allergy and Clinical Immunology·E O Meltzer
Aug 1, 1995·Clinical Pharmacology and Therapeutics·S U YasudaR L Woosley
May 1, 1994·Drug Safety : an International Journal of Medical Toxicology and Drug Experience·F E Simons
Oct 6, 2001·Clinical Infectious Diseases : an Official Publication of the Infectious Diseases Society of America·P S Muether, J M Gwaltney
Mar 28, 2008·Journal of Neurochemistry·Gianluigi TandaJonathan L Katz
Apr 24, 2009·Clinical Pharmacokinetics·Offie P Soldin, Donald R Mattison
Jan 15, 2010·Basic & Clinical Pharmacology & Toxicology·José Augusto Guimarães Morais, Maria do Rosário Lobato
Jun 4, 2010·Anais Brasileiros De Dermatologia·Paulo Ricardo CriadoCarlos d'Apparecida Machado Filho
Nov 1, 2011·The Journal of Allergy and Clinical Immunology·F Estelle R Simons, Keith J Simons
Jun 1, 2013·Indian Journal of Dermatology·Martin K Church, Diana S Church
Apr 14, 2016·Pharmacology Research & Perspectives·Sara PlanèsMichel Mallaret
Mar 7, 2017·The International Journal of Pharmacy Practice·Olufunmilola AbrahamSteven M Albert

❮ Previous
Next ❯

Citations

Mar 17, 2020·The Cochrane Database of Systematic Reviews·Zhirong YangQian Zhang
Mar 27, 2021·Journal of Clinical Pharmacology·Ana Santos CravoTim Shea

❮ Previous
Next ❯

Software Mentioned

Sciex
MacQuan
STAT
SAS
Sciex MassChrom
COSTART
WinNonlin Pro

Related Concepts

Related Feeds

Allergy and Asthma

Allergy and asthma are inflammatory disorders that are triggered by the activation of an allergen-specific regulatory t cell. These t cells become activated when allergens are recognized by allergen-presenting cells. Here is the latest research on allergy and asthma.