Pharmacokinetics of bisphosphonates in rabbits

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Luurila, S. (författare)

Pharmacokinetics of bisphosphonates in rabbits

Artikel/kapitelEngelska1999

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2017-02-03
Blackwell Munksgaard,1999
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LIBRIS-ID:oai:DiVA.org:mdh-55606
https://urn.kb.se/resolve?urn=urn:nbn:se:mdh:diva-55606URI
https://doi.org/10.1111/j.1600-0773.1999.tb02106.xDOI

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Språk:engelska
Sammanfattning på:engelska

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Clodronate, pamidronate and etidronate are commonly used bisphosphonates, which accumulate extensively in arteries and some other tissues. We compared their pharmacokinetics in rabbits with those of tiludronate, the drug newly introduced to clinical use. The 14C-labelled drugs were given intravenously and plasma drug levels were monitored for up to 24 hr. The dose-related plasma concentrations of tiludronate and etidronate were clearly higher and decreased more slowly than those of clodronate and pamidronate (P<0.001). Already at 5 min., the concentrations of tiludronate and etidronate were higher than those of clodronate and pamidronate (P=0.016). At 24 hr, plasma concentration of tiludronate was 12 ± 6.6%, of etidronate 18 ± 2.5%, of clodronate 0.8 ± 0.2%, and of pamidronate 1.4 ± 0.4% of the dose per body weight. With the same dose (25 mg/kg), absolute AUC(0-24hr) for tiludronate and etidronate was 9-11 times larger than for clodronate. AUC(0-24hr) for pamidronate (2.5 mg/kg) was 11% of that for clodronate. Plasma clearance of tiludronate and etidronate was 9- 15 times slower than that of clodronate and pamidronate. At 24 hr, the mean tissue-to-plasma ratio of tiludronate for aorta was 1.2-1.6. For bone, spleen, liver and kidneys the ratio varied from 5.4 to 52.6. The results suggest that 1) tiludronate and etidronate are removed from plasma much slower than clodronate and pamidronate, and 2) the potential of filudronate to concentrate in arteries and bone is generally smaller than previously found with the other bisphosphonates.

Ämnesord och genrebeteckningar

MEDICIN OCH HÄLSOVETENSKAP Hälsovetenskap Folkhälsovetenskap, global hälsa, socialmedicin och epidemiologi hsv//swe
MEDICAL AND HEALTH SCIENCES Health Sciences Public Health, Global Health, Social Medicine and Epidemiology hsv//eng
clodronic acid
etidronic acid
pamidronic acid
tiludronic acid
animal experiment
animal tissue
area under the curve
article
drug blood level
drug clearance
male
nonhuman
osteolysis
osteoporosis
priority journal
rabbit
Animalia
Oryctolagus cuniculus

Biuppslag (personer, institutioner, konferenser, titlar ...)

Kautiainen, Susanna (författare)
Ylitalo, P. (författare)
Ylitalo, R. (författare)

Sammanhörande titlar

Ingår i:Pharmacology and Toxicology: Blackwell Munksgaard84:1, s. 24-280901-99281600-0773

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Av författaren/redakt...: Luurila, S.; Kautiainen, Susa ...; Ylitalo, P.; Ylitalo, R.

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MEDICIN OCH HÄLSOVETENSKAP: MEDICIN OCH HÄLS ...; och Hälsovetenskap; och Folkhälsovetensk ...

Artiklar i publikationen: Pharmacology and ...

Av lärosätet: Mälardalens universitet

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