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ChapterDrugsusedforthetreatmentofosteoporosisDepartmentofpharmacologyLimingzhou2015.9ContentsOsteoporosis

Antiresorptivedrugs

Bone-formingdrugs

MineralizationdrugsOsteoporosis

Osteoporosisisadiseasecharacterizedbylowbonemass(bonethinning)thatleadstofragilebonesandanincreasedriskoffracturesofthehip,spine,andwrist.Normal

OsteoporosisSevereosteoporosisOsteoporosis

—symptomsCommonsymptoms:BackpainStoopedpostureFracturesOsteoporosis—types

PrimaryosteoporosisSecondaryosteoporosisIdiopathicosteoporosisPostmenopausalosteoporosisSenileosteoporosis[Osteoporosis—riskfactors

FactorsyoucannotchangeGenderAge;Bodysize;Ethnicity;FamilyhistoryFactorsyoucanchangeSexhormones;Anorexianervosa;(神经性厌食症)CalciumandvitaminDintake;Medicationuse;Lifestyle;Cigarettesmoking;AlcoholintakeOsteoporosis—diagnosis

TheBoneMineralDensityTest(BDT)DetectlowbonedensitybeforeafractureoccursConfirmanosteoporosis

diagnosisifyoualreadyhaveoneormorefracturesPredictyourchancesofhavingfracturesinthefutureDetermineyourrateofbonelossandmonitortheeffectsoftreatmentOsteoporosis—diagnosisBoneMassDensityTheNationalOsteoporosisFoundationRecommendsaBDTif:YouusemedicationsthatcauseosteoporosisYouhavetypeIdiabetes,liverdisease,kidneydiseaseorafamilyhistoryYouexperienceearlymenopauseYouarepostmenopauseover50andhaveatleastoneriskfactorYouarepostmenopauseover65andneverhadatestOsteoporosis—treatmentComprehensivetreatmentfor

osteoporosisdealswith:

PropernutritionExerciseSafetyissuestopreventfallsMedicationsOsteoporosis—medicationsAntiresorptivedrugs:Bisphosphonates,calcitonin,estrogenBone-formingdrugs:Parathyroidhormone,androgenMineralizationdrugs:CalciumandvitaminDBisphosphonates(双磷酸盐)—PharmacologicalSlowbonelossIncreasebonedensityReducetheriskfracturesAntiresorptivedrugsBisphosphonate—clinicalapplicationOsteoporosisinmenandpostmenopausalwomenPreventingandtreatingosteoporosisduetoglucocorticoidsteroidmedicationsTreatinghighblood

calcium

levelsduetocancer

Treating

multiplemyeloma

orsolidtumorcancersthathavespreadtotheboneBisphosphonate—sideeffects

Nausea,abdominalpainandindigestion

Rashanditchyskin

Atemporaryincreaseinparathyroidhormone

andserumtransaminase(血转氨酶)

CalcitoninCalcitoninanalogues(whicharemanufacturedversionsofcalcitonin)canbeusefulfortreatingosteoporosisbyslowingthebreakdownofbone.Calcitoninisadelicatemoleculethatwouldbedestroyedbythedigestivetract,itmustbetakenbynasalsprayorbyinjectionWithsideeffectsofnausea,vomitingandallergic

rashetal.EstrogenTherapy—application

Estrogentherapy(ET)reduceboneloss,increase

bonedensity

inboththespineandhip,andreducetheriskofhipandspinefracturesinpostmenopausalwomen.

ETis

approvedforpreventingpostmenopausalosteoporosis

andaremostcommonlyadministeredintheformofatabletorskinpatch(经皮吸收).

EstrogenTherapy—sideeffectsTakingestrogenaloneincreasesawoman'sriskofdevelopingcanceroftheuterinelining(endometrialcancer).Toreducethisrisk,womenwhostillhaveauterus(whohavenothadahysterectomy(子宫切除))shouldusuallytakeaprogestinincombinationwithestrogenSelectiveestrogenreceptormodulators(SERMS)aredrugsthatactlikeestrogenatsomereceptorsItactslikeestrogenforpreventingbonelossandimprovingcholesterol.Currently,onlyraloxifene(雷洛昔芬)thatisapprovedtopreventandtreatosteoporosis.SelectiveEstrogenReceptorModulatorsBone-formingdrugsParathyroidhormone(PTH)—mechanismWithbothcatabolicandanabolicactions

Lowdose:PTHstimulateboneturnoverandisassociatedwithboneformation(成骨作用)

Highdose:PTHincreasetherateofboneresorptionfollowedbyslowerrateofboneformation(破骨作用)Parathyroidhormone(PTH)—application

OsteoporosisPrimaryparathyroidfunctiondecline

(Intake

vitaminsDandcalciumtogether)

GenerallyappliesonlytofirstaidAndrogenandanabolichormone—mechaismAndrogencanpromotethesynthesisofproteinandcollagen,stimulateboneformationandretentionofcalcium,phosphorus,andpotassium.Androgenandanabolichormone—applicationmaleosteoporosisSideeffectisbigger,thedoseoftreatmentandtheprosandconsofrelationshipisstillinthefurtherresearchMineralizationdrugsCalciumAddingbonemineralandpromotingbonemineralizationvitaminD3

Increasetheabsorptionofdietarycalciumandphosphorus,maintainthebalanceofcalciumandphosphorusandincreasetheactivityofosteoblastsCalcium—applicationAcuteorchronichypocalcemia;Tetanydisease(手足抽搐)Rickets(佝偻病);Osteomalacia(软骨病),osteoporosis,parathyroidfunctionimpairmentMagnesiumpoisoningcounterpoison(镁中毒解救)(Onekeypieceofadviceistotakeyourcalciuminseveralsmalldosesthroughouttheday).vitaminD3—applicationOsteoporosisChronicrenalfailureFortreatmentandpreventionofvitaminDdeficiencyPsoriasis(银屑癣)Osteoporosisisadiseaseofbonethatcommonlyoccursinelderlypeople,andischaracterizedbythedegenerationofbonesuperstructure,adecreaseofbonestrength,anincreaseofbonefragilityandthusanincreasedriskoffracture.Drugsava

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