Brain uptake of nonsteroidal anti-inflammatory drugs: ibuprofen, flurbiprofen, and indomethacin.

Brain uptake of nonsteroidal anti-inflammatory drugs: ibuprofen, flurbiprofen, and indomethacin. Research Abstract Details 

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Brain uptake of nonsteroidal anti-inflammatory drugs: ibuprofen, flurbiprofen, and indomethacin. Abstract Text:

Jagan Mohan R Parepally,Haritha Mandula,Quentin R Smith,

PURPOSE: To determine the roles of blood-brain barrier (BBB) transport and plasma protein binding in brain uptake of nonsteroidal anti-inflammatory drugs (NSAIDs)-ibuprofen, flurbiprofen, and indomethacin. METHODS: Brain uptake was measured using in situ rat brain perfusion technique. RESULTS: [14C]Ibuprofen, [3H]flurbiprofen, and [14C]indomethacin were rapidly taken up into the brain in the absence of plasma protein with BBB permeability-surface area products (PS(u)) to free drug of (2.63 +/- 0.11) x 10(-2), (1.60 +/- 0.08) x 10(-2), and (0.64 +/- 0.05) x 10(-2) mL s(-1) g(-1) (n = 9-11), respectively. BBB [14C]ibuprofen uptake was inhibited by unlabeled ibuprofen (Km = 0.85 +/- 0.02 mM, Vmax = 13.5 +/- 0.4 nmol s(-1) g(-1)) and indomethacin, but not by pyruvate, probenecid, digoxin, or valproate. No evidence was found for saturable BBB uptake of [3H]flurbiprofen or [14C]indomethacin. Initial brain uptake for all three NSAIDs was reduced by the addition of albumin to the perfusion buffer. The magnitude of the brain uptake reduction correlated with the NSAID free fraction in the perfusate. CONCLUSIONS: Free ibuprofen, flurbiprofen, and indomethacin rapidly cross the BBB, with ibuprofen exhibiting a saturable component of transport. Plasma protein binding limits brain NSAID uptake by reducing the free fraction of NSAID in the circulation.

Brain uptake of nonsteroidal anti-inflammatory drugs: ibuprofen, flurbiprofen, and indomethacin. Publishing Authors By Initials

JM Parepally,H Mandula,QR Smith,

For similar proteins: albumins: serum albumin: serum albumin, bovine research abstracts see: proteins: albumins: serum albumin: serum albumin, bovine research

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Brain uptake of nonsteroidal anti-inflammatory drugs: ibuprofen, flurbiprofen, and indomethacin. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Pharmaceutical research

VOLUME: 23

Page Numbers: 873-81

Journal Abbreviation: Pharm. Res.

ISSN: 0724-8741

DAY: 2

MONTH: 05

YEAR: 2006

Brain uptake of nonsteroidal anti-inflammatory drugs: ibuprofen, flurbiprofen, and indomethacin. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 8406521

Brain uptake of nonsteroidal anti-inflammatory drugs: ibuprofen, flurbiprofen, and indomethacin. Keywords Mesh Terms:

KEYWORDS: Serum Albumin, Bovine

MESH TERMS: metabolism

Chemical & Substance for Abstract: Brain uptake of nonsteroidal anti-inflammatory drugs: ibuprofen, flurbiprofen, and indomethacin. Information

Substance Name: Indomethacin

Registry Number: 53-86-1

Grant and Affiliation Information for Brain uptake of nonsteroidal anti-inflammatory drugs: ibuprofen, flurbiprofen, and indomethacin.

AFFILIATION: Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University Health Sciences Center, 1300 Coulter, Amarillo, Texas 79106, USA.

Country: United States

AGENCY: United States NINDS

GRANT: NS052484

ACRONYM: NS

MEDLINETA: Pharm Res

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