Bisphosphonates: A review of their pharmacokinetic properties

Lin, Jiunn H.

doi:10.1016/8756-3282(95)00445-9

Cited by 841 publications

(682 citation statements)

References 56 publications

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“…Bioavailability of oral bisphosphonates is poor due to low intestinal absorption rates [51]. The correct intake of a poorly absorbed bisphosphonate tablet is even more important if it is only given once per week.…”

Section: Smaller Increases In Bmd Due a False Intake Of Generic Alendmentioning

confidence: 99%

Differences in persistence, safety and efficacy of generic and original branded once weekly bisphosphonates in patients with postmenopausal osteoporosis: 1-year results of a retrospective patient chart review analysis

Ringe

Möller

2009

Rheumatol Int

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Section: Smaller Increases In Bmd Due a False Intake Of Generic Alendmentioning

confidence: 99%

Differences in persistence, safety and efficacy of generic and original branded once weekly bisphosphonates in patients with postmenopausal osteoporosis: 1-year results of a retrospective patient chart review analysis

Ringe

Möller

2009

Rheumatol Int

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“…Bisphosphonates are used clinically to inhibit osteoclastmediated bone resorption associated with many pathologic processes of bone [10,11,18,19,25]. They bind tightly to One or more of the authors (CM, JHH) has received funding from the Orthopaedic Research and Education Foundation; the Musculoskeletal Transplant Foundation; and the Biomet Oncology Fellowship.…”

Section: Introductionmentioning

confidence: 99%

“…the hydroxyapatite crystals in mineralized bone [14,23] with a half-time measured in years and matching the bone's turnover period [18]. Frozen and freeze-dried cortical bulk allografts are not vascularized, and thus systemically administered bisphosphonates must passively diffuse into them from adjacent tissues.…”

Section: Introductionmentioning

confidence: 99%

Bisphosphonate Delivery to Tubular Bone Allografts

DiResta

Manoso

Naqvi

et al. 2008

Clin Orthop Relat Res

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Large structural allografts used for reconstruction of bone defects after revision arthroplasty and tumor resection fracture up to 27% of the time from osteolytic resorption around the fixation screw holes and tendon or ligament attachment sites. Treating structural allografts before implantation with bisphosphonates may inhibit local osteoclastic processes and prevent bone resorption and the development of stress risers, thereby reducing the long-term fracture rate. Taking advantage of allografts' open-pore structure, we asked whether passive soaking or positive-pressure pumping was a more efficient technique for delivering bisphosphonates. We treated matched pairs of ovine tibial allografts with fluids containing Tc-99m pamidronate and toluidine blue stain to facilitate indicator distribution analysis via microSPECT-microCT imaging and light microscopy, respectively. Surfactants octylphenoxy polyethoxy ethanol or beractant were added to the treatment fluids to reduce flow resistance of solutions pumped through the allografts. Indicator distribution after 1 hour of soaking produced a thin ring around periosteal and endosteal surfaces, while pumping for 10 minutes produced a more even distribution throughout the allograft. Flow resistance was reduced with octylphenoxy polyethoxy ethanol but unaffected with beractant. Pumped allografts displayed a more homogeneous indicator distribution in less time than soaking while surfactants enhanced fluid movement.

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“…BPs are also highly ionized at physiological pH, which leads to their low oral bioavailability and poor cellular uptake in soft tissues. 4 BPs' affinity for bone depends highly on their structure. 5 The binding is mainly mediated by the two phosphonate groups, but other properties are thought to contribute to the binding affinity as well, for example, a hydroxyl group as substituent R 1 or a primary amine group in the substituent R 2 .…”

mentioning

confidence: 99%

Structural Requirements for Bisphosphonate Binding on Hydroxyapatite: NMR Study of Bisphosphonate Partial Esters

Puljula

Turhanen

Vepsäläinen

et al. 2015

ACS Med. Chem. Lett.

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Eighteen different bisphosphonates, including four clinically used bisphosphonate acids and their phosphoesters, were studied to evaluate how the bisphosphonate structure affects binding to bone. Bisphosphonates with weak bone affinity, such as clodronate, could not bind to hydroxyapatite after the addition of one ester group. Medronate retained its ability to bind after the addition of one ester group, and hydroxy-bisphosphonates could bind even after the addition of two ester groups. Thus, several bisphosphonate esters are clearly bone binding compounds. The following conclusions about bisphosphonate binding emerge: (1) a hydroxyl group in the geminal carbon takes part in the binding process and increases the bisphosphonate's ability to bind to bone; (2) the bisphosphonate's ability to bind decreases when the amount of ester groups increases; and (3) the location of the ester groups affects the bisphosphonate's binding ability.

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Bisphosphonates: A review of their pharmacokinetic properties

Cited by 841 publications

References 56 publications

Differences in persistence, safety and efficacy of generic and original branded once weekly bisphosphonates in patients with postmenopausal osteoporosis: 1-year results of a retrospective patient chart review analysis

Differences in persistence, safety and efficacy of generic and original branded once weekly bisphosphonates in patients with postmenopausal osteoporosis: 1-year results of a retrospective patient chart review analysis

Bisphosphonate Delivery to Tubular Bone Allografts

Structural Requirements for Bisphosphonate Binding on Hydroxyapatite: NMR Study of Bisphosphonate Partial Esters

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