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BisphosphonatesAka: Alendronate, Risedronate, Actonel, Pamidronate, Aredia, Ibandronate, Boniva, Fosamax, Etidronate, Didronel, Tiludronate, Skelid

Indications
1. Osteoporosis
2. Metabolic bone disease (e.g. Paget's Disease of Bone)
Contraindications
1. Delayed gastric emptying
Efficacy
1. Decreases rate of bone resorption
2. Reduces risk of vertebral Fracture: 8.8%
3. Reduces risk of non-vertebral Fracture (5.6%)
4. Reference
  1. Black (1996) 348:1535
Adverse effects
1. Bone, joint or muscle pain
  1. Consider stopping medication if persists
2. Significant Gastrointestinal risks
  1. Esophageal Erosions or Esophageal ulcers
    1. Appears to occur more with Alendronate
  2. Take with over 8 ounces water
  3. Stay upright for at least 30 minutes after dose
  4. Take at least 60 minutes before breakfast
Pharmacokinetics: Absorption inhibited if taken with food
1. Wait 1-2 hours before eating
Agents: Osteoporosis and Metabolic Bone Disease
1. See Adverse effects for patient instructions
2. Alendronate (Fosamax or Fosamax plus D)
  1. Osteoporosis
    1. Prophylaxis: 5 mg PO qd or 35 mg PO qWeek
    2. Treatment: 10 mg PO qd or 70 mg PO qWeek
  2. Paget's Disease: 40 mg PO qd for 6 months
3. Risedronate (Actonel)
  1. Osteoporosis: 5 mg PO qd or 35 mg PO qWeek
  2. Paget's Disease: 30 mg PO qd for 2 months
4. Ibandronate (Boniva) for Osteoporosis
  1. Daily: 2.5 mg orally
  2. Monthly: 150 mg orally (same cost as for daily)
  3. Chestnut (2004) J Bone Miner Res 19:1241
5. Zoledronic Acid (Reclast)
  1. Approved for Post-menopausal Osteoporosis and Paget's Disease
  2. Contraindicated in Hypocalcemia or where GFR <35 ml/min
  3. Adverse effects: Acute phase reaction with fever, myalgias, Headache
  4. Dosing: 5 mg IV infused over 15 minutes once yearly
  5. Black (2007) N Engl J Med 356(18):1809
Agents: Metabolic bone disease
1. Etidronate (Didronel)
  1. Paget's Disease: 5-10 mg/kg PO qd for 6 months
  2. Hypercalcemia: 7.5 mg/kg in 250 cc NS IV qd x3 days
    1. Given slowly over >2 hours
2. Tiludronate (Skelid)
  1. S-Containing agent
  2. No effect on Fracture risk
  3. Indicated for Paget's Disease of Bone
  4. Dose: 40 mg PO qd
3. Pamidronate (Aredia)
  1. Dose: 40-80 mg IV slowly over >2 hours every 4 months
  2. Indications
    1. Paget's Disease of Bone
    2. Hypercalcemia of Malignancy
    3. Osteolytic bone lesions (e.g. Multiple Myeloma)
References
1. Greenspan (2000) Am Fam Physician 61(9):2371

pamidronate (C0043603)
Definition (NCI)	An amino- bisphosphonate with anti-resorptive and anti-hypercalcemic activities. Pamidronic acid binds to and adsorbs onto hydroxyapatite crystals in the bone matrix, thereby preventing osteoclast resorption. This agent also binds to and inhibits farnesyl pyrophosphate synthase, an enzyme that plays an important role in the mevalonate pathway. This inhibits the formation of isoprenoid metabolites that are substrates for protein prenylation. This prevents farnesylation and geranylgeranylation of proteins essential for osteoclast function, leading to the induction of apoptosis of osteoclasts. By preventing osteoclast-mediated bone resorption, pamidronic acid decreases bone turnover rate, stabilizes the bone matrix and reduces hypercalcemia.
Definition (PDQ)	A synthetic bisphosphonate agent. Although its mechanism of action is not completely understood, pamidronate appears to adsorb to calcium phosphate crystals in bone, blocking their dissolution by inhibiting osteoclast-mediated bone resorption. This agent does not inhibit bone mineralization and formation. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39149&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39149&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1345" NCI Thesaurus)
Concepts	Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH	C019248
English	AHPrBP, amidronate, aminohydroxypropylidene diphosphonate, aminopropanehydroxydiphosphonate, APD, pamidronate, PAMIDRONATE PREPARATION, Pamidronic acid
Spanish	acido pamidronico, pamidronato
Parent Concepts	Diphosphonates (C0012544), Bone resorption inhibitor (C0521941), pamidronate (C0043603), [HS900] HORMONES/SYNTHETICS/MODIFIERS, OTHER (C0991612)
Sources	CSP, MSH, MTH, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF Derived from the NIH UMLS (Unified Medical Language System)

Etidronate (C0086268)
Definition (CSP)	ethane-1-hydroxy-1,1-diphosphonate; a diphosphonate compound that affects calcium metabolism and inhibits the resorption and deposition of hydroxyapatite crystals in bone.
Definition (NCI)	A drug that belongs to the family of drugs called bisphosphonates. Bisphosphonates are used as treatment for hypercalcemia (abnormally high levels of calcium in the blood) and for cancer that has spread to the bone (bone metastases).
Concepts	Organophosphorus Compound (T115) , Pharmacologic Substance (T121)
MSH	D012968
English	EHDP, Ethanehydroxydiphosphonate, Ethanehydroxyphosphate, Etidronate, Etidronate -RETIRED-, HEDP, Hydroxyethanediphosphonate
Spanish	etidronato, etidronato-RETIRADO-
Parent Concepts	alkylphosphate (C0596068), calcification inhibitor (C0596231), Etidronic Acid (C0015121), Diphosphonates (C0012544), Reason not stated concept (C1276325)
Sources	CSP, MSH, MTH, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF Derived from the NIH UMLS (Unified Medical Language System)

Alendronate (C0102118)
Definition (CSP)	bone resorption inhibitor.
Definition (MSH)	A nonhormonal medication for the treatment of postmenopausal osteoporosis in women. This drug builds healthy bone, restoring some of the bone loss as a result of osteoporosis.
Concepts	Organophosphorus Compound (T115) , Pharmacologic Substance (T121)
MSH	D019386
English	AHBUTBP, Alendronate, ALENDRONATE PREPARATION, Aminohydroxybutane Bisphosphonate
Spanish	alendronato
Parent Concepts	antagonists & inhibitors (C0003139), Diphosphonates (C0012544), [HS900] HORMONES/SYNTHETICS/MODIFIERS, OTHER (C0991612)
Sources	CSP, MSH, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF Derived from the NIH UMLS (Unified Medical Language System)

Aredia (C0104018)
Concepts	Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH	C019248
English	Aredia, Novartis brand of pamidronate disodium salt
Sources	CSP, MSH, NCI, PDQ, RXNORM Derived from the NIH UMLS (Unified Medical Language System)

Tiludronate (C0145942)
Concepts	Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH	C058651
English	Tiludronate, TILUDRONATE PREPARATION
Spanish	tiludronato
Parent Concepts	tiludronic acid (C0043611), [HS900] HORMONES/SYNTHETICS/MODIFIERS, OTHER (C0991612), Diphosphonates (C0012544)
Sources	MSH, MTH, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF Derived from the NIH UMLS (Unified Medical Language System)

Risedronate (C0246719)
Definition (NCI)	(ris-ED-roe-nate) A substance that is being studied in the prevention and treatment of osteoporosis. It belongs to the family of drugs called bone resorption inhibitors.
Definition (PDQ)	A synthetic pyridinyl bisphosphonate agent. Risedronate binds to hydroxyapatite crystals in bone and inhibits osteoclast-dependent bone resorption Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=256445&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=256445&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1528" NCI Thesaurus)
Concepts	Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH	C073008
English	RISE, Risedronate, RISEDRONATE PREPARATION
Spanish	risedronato
Parent Concepts	risedronic acid (C0140610), [HS900] HORMONES/SYNTHETICS/MODIFIERS, OTHER (C0991612), Diphosphonates (C0012544)
Sources	MSH, MTH, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF Derived from the NIH UMLS (Unified Medical Language System)

Fosamax (C0376569)
Concepts	Organophosphorus Compound (T115) , Pharmacologic Substance (T121)
MSH	D019386
English	Fosamax
Sources	CSP, MSH, NCI, PDQ, RXNORM Derived from the NIH UMLS (Unified Medical Language System)

Ibandronate (C0379199)
Definition (PDQ)	A synthetic nitrogen-containing bisphosphonate. Ibandronate inhibits farnesyl pyrophosphate synthase, resulting in a reduction in geranylgeranyl GTPase signaling proteins and apoptosis of osteoclasts. This agent increases bone mineral density, decreases bone remodeling, inhibits osteoclast-mediated bone resorption, and reduces metastases-related and corticosteroid-related bone pain. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=365963&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=365963&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1670" NCI Thesaurus)
Concepts	Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH	C073007
English	Ibandronate, IBANDRONATE PREPARATION
Spanish	ibandronato
Parent Concepts	[HS900] HORMONES/SYNTHETICS/MODIFIERS, OTHER (C0991612), Unclassified Ingredients (C1372954), Diphosphonates (C0012544)
Sources	MSH, MTH, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, VANDF Derived from the NIH UMLS (Unified Medical Language System)

Didronel (C0591373)
Concepts	Organophosphorus Compound (T115) , Pharmacologic Substance (T121)
MSH	D012968
English	Didronel
Sources	MSH, NCI, PDQ, RXNORM Derived from the NIH UMLS (Unified Medical Language System)

Skelid (C0592793)
Concepts	Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH	C058651
English	Skelid
Sources	MSH, NCI, RXNORM Derived from the NIH UMLS (Unified Medical Language System)

Actonel brand of risedronate sodium (C0718248)
Concepts	Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH	C073008
English	Actonel, Actonel brand of risedronate sodium
Sources	MSH, MTH, NCI, PDQ, RXNORM Derived from the NIH UMLS (Unified Medical Language System)

Boniva (C1541222)
Concepts	Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH	C073007
English	Boniva
Sources	MSH, NCI, PDQ, RXNORM Derived from the NIH UMLS (Unified Medical Language System)

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BisphosphonatesAka: Alendronate, Risedronate, Actonel, Pamidronate, Aredia, Ibandronate, Boniva, Fosamax, Etidronate, Didronel, Tiludronate, Skelid

pamidronate (C0043603)

Etidronate (C0086268)

Alendronate (C0102118)

Aredia (C0104018)

Tiludronate (C0145942)

Risedronate (C0246719)

Fosamax (C0376569)

Ibandronate (C0379199)

Didronel (C0591373)

Skelid (C0592793)

Actonel brand of risedronate sodium (C0718248)

Boniva (C1541222)

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