Author/Editor     Gobec, Stanislav
Title     Bisfosfonati
Translated title     Bisphosphonates
Type     članek
Source     Farm Vestn
Vol. and No.     Letnik 51, št. 2
Publication year     2000
Volume     str. 263-8
Language     slo
Abstract     Bisphosphonates are stable analogs of inorganic pyrophosphate. They bind to bone mineral and inhibit the resorption of living bone. Several bisphosphonates are established as effective treatments for diseases as Paget's disease, hypercalcemia of malignancy, metastatic bone disease and osteoporosis. Bisphosphonates are poorly absorbed following oral administration but have a high affinity for bone. They probably inhibit bone resorption by interfering with the action of osteoclasts. The first generation bisphosphonates can be incorporated into analogs of ATP that may inhibit ATP-dependent intracellular enzymes. More potent nitrogen-containing bisphosphonates can inhibit enzymes of the mevalonate pathway.
Summary     Bisfosfonati so stabilni analogi pirofosfata. Vežejo se na kostni hidroksiapatit in zavirajo kostno resorbcijo. Več bisfosfonatov je že v uporabi za zdravljenje Pagetove bolezni, maligne hiperkalcemije, kostnih metastaz in osteoporoze. Po peroralni aplikaciji se slabo absorbirajo, vendar imajo visoko afiniteto do kostnih mineralov. Kostno resorbcijo zavirajo najverjetneje zaradi vpliva na delovanje osteoklastov. Bisfosfonati prve generacije se metabolizirajo do citotoksičnih analogov ATP, ki lahko zavirajo od ATP odvisne intracelulame encime. Učinkovitejši in novejši bisfosfonati z dušikom pa verjetno zavirajo encime vključene v pot mevalonata.
Descriptors     DIPHOSPHONATES
BONE RESORPTION
OSTEOPOROSIS
OSTEOCLASTS
OSTEITIS DEFORMANS
HYPERCALCEMIA