Nasal Mucosal Inflammation Has No Effect on the Absorption of Intranasal Triamcinolone Acetonide

Abstract

The potential for enhanced systemic absorption of intranasal triamcinolone acetonide was explored in patients with inflamed nasal mucosa. Twelve allergic rhinitis patients with documented nasal inflammation, and 12 healthy volunteers, each received a single, therapeutic, 400-micrograms dose of triamcinolone acetonide in each nostril. Blood was obtained at fixed time points after the dose, and plasma concentrations of triamcinolone acetonide were determined by radioimmunoassay. There were no statistically significant differences in any of the derived pharmacokinetic parameters (maximum plasma triamcinolone acetonide concentrations [Cmax], time to maximum plasma triamcinolone concentrations [Tmax], elimination half-life [t1/2], and area under the plasma concentration-time curve [AUC0-12] from 0 to 12 hours) between treatment groups. A once-a-day, chronic regimen (6 weeks) of triamcinolone acetonide was also administered to five patients with allergic rhinitis. Pharmacokinetic parameters were similar to the parameters derived from healthy volunteers after acute administration. There was no evidence of drug accumulation. The results of this study indicate that acute and chronic intranasal administration. The results of this study indicate that acute and chronic intranasal administration of therapeutic doses of triamcinolone acetonide to patients with inflamed nasal mucosa does not result in enhanced systemic drug absorption or accumulation.

Dissolution in nasal fluid, retention and anti‐inflammatory activity of fluticasone furoate in human nasal tissue ex vivo

“…Likewise, after nasal spray doses of 800 μg FP and MF C max levels of 27.7 and 25.5 pg/mL, respectively, were detected in humans [44]. In contrast, systemic absorption rates have been shown to be higher for the more hydrophilic TCA with a C max of 320 pg/mL after repeated administration of 800 μg doses [45]. Intranasal administration of Bud resulted in mean C max levels of 426 pg/mL (dose 400 μg; aqueous preparation), 220 pg/mL (dose 800 μg; pMDI) and 432 pg/mL (dose 800 μg; dry powder formulation) [38].…”

Iatrogenic Cushing Syndrome after Epidural Triamcinolone Injections in an HIV Type 1–Infected Patient Receiving Therapy with Ritonavir‐Lopinavir

“…Triamcinolone acetonide is typically rapidly metabolized, with an estimated half life of 2–3 hours (3); the acetonide version is less water soluble than other glucocorticoid derivatives, and absorption from intra-articular sites has been reported to continue for 2–3 weeks following injection (4). In this patient, the rate of decline in triamcinolone acetonide levels (Figure 1) from days 22–62 following the last dose of epidural injection approximated linear decay kinetics (slope 0.0154 μg/day, r 2 =0.992) with a calculated half life of 21.3 days.…”

Iatrogenic Cushing's syndrome after triamcinolone plus ritonavir-boosted atazanavir

“…9 Serum half-life of triamcinolone is approximately 2-3 hours. 10 However, intraarticular triamcinolone acetonide may be systemically absorbed for 2-3 weeks after injection. 11 Adrenal suppression may last as long as 30-40 days after intraarticular injection.…”