Parathyroid drugs Flashcards
Alendronate (Fosamax), Risedronate (Actonel)
Class: Bisphosphonate
Mech: Reduce osteoclastic bone resorption
Thera: Hypercalcemia; osteoporosis; Paget’s disease of bone; prevention of fractures in osteogenesis imperfecta
Other SE’s: Esophageal irritation
Misc: Oral formulation; patient must be sitting upright, fasting, for 30 minutes; takes several days to see effect
Ibandronate (Boniva)
Class: Bisphosphonate
Mech: Reduce osteoclastic bone resorption
Thera: Hypercalcemia; osteoporosis; Paget’s disease of bone; prevention of fractures in osteogenesis imperfecta
Other SE’s: Esophageal irritation
Misc: Oral and IV formulations; patient must be sitting upright, fasting, for 30 minutes; takes several days to see effect
Pamidronate (Aredia)
Class: Bisphosphonate
Mech: Reduce osteoclastic bone resorption
Thera: Hypercalcemia of malignancy; Paget’s disease of bone; prevention of fractures in osteogenesis imperfecta
Important SE’s: Serum creatinine elevation
Other SE’s: Fever, flu-like symptoms
Misc: Bypasses GI tract (given IV); takes several days to see effect for lowering calcium
Zoledronic acid (Reclast)
Class: Bisphosphonate
Mech: Reduce osteoclastic bone resorption
Thera: Hypercalcemia of malignancy; Paget’s disease of bone; prevention of fractures in osteogenesis imperfecta
Important SE’s: Serum creatinine elevation
Other SE’s: Fever, flu-like symptoms
Misc: Bypasses GI tract (given IV); takes several days to see effect for lowering calcium
Cinacalcet (Sensipar)
Class: Calcimimetic
Mech: Reduces PTH and serum calcium levels
Thera: Secondary hyperparathyroidism from renal disease; parathyroid carcinoma; hypercalcemia in primary hyperparathyroidism not treatable by surgery
Calcitonin (Miacalcin)
Class: Amino acid peptide
Mech: Increases urinary calcium excretion, inhibits bone reabsorption (modest effect)
Thera: Short-term relief of hypercalcemia; osteoporosis (reduce vertebral fractures); Paget’s disease of bone
Other SE’s: Minimal (e.g., rhinitis)
Misc; No longer recommended for use in nasal spray form because of increased cancer risk. Can still use SQ or IM. Tachyphylaxis in 2-3 days; often used to bridge treatment for other medication
Teriparatide (Forteo)
Class: PTH analog
Mech: Short bursts given SQ, stimulating bone resorption and bone formation via osteoblasts
Thera: Osteoporosis (high risk patients who have failed other treatments)
Other SE’s: Transient mild hypercalcemia
Misc: Contraindicated in those with increased chance of osteosarcoma (e.g., Paget’s disease of the bone, radiation exposure)
Raloxifene (Evista)
Class: Selective estrogen receptor modulator
Mech: Selectively activates certain estrogen receptors, but blocks others
Thera: Osteoporosis
Important SE’s: Increase risk of hot flashes, DVT
Corticosteroids
Mech: Decreases production of 1,25 vitamin D; may inhibit growth of neoplastic lymphoid tissue
Thera: Hypercalcemia from vitamin D intoxication, granulomatous diseases, hematologic malignancies
Denosumab (Prolia)
Class: Monoclonal antibody
Mech: RANK ligand inhibitor (targets early effect of osteoclasts on bone)
Thera: Osteoporosis
Misc: can give at any GFR but need to exclude other causes of renal osteodystrophy
Calcium carbonate, Calcium acetate, Sevelamer (Renvela)
Mech: Binds phosphate
Thera: Secondary hyperparathyroidism from renal disease
Cortical bone predominates in the _____; trabecular bone predominates in the _____
shafts of the long bones;
vertebral bodies, ribs, pelvis, ends of long bones
The inorganic matrix of bone is largely composed of _____, a mineral composed of
hydroxyapatite;
Ca and P
Biologic activity of PTH resides in _____; it is secreted by what? Its secretion is controlled by what?
first 34 residues; the four parathyroid glands;
serum IONIZED Ca, such that if Ca is low, PTH is stimulated, but if Ca is high, PTH suppressed
Discuss percentages regarding Ca in the body:
99% in skeleton, 1% in ECF; 3 forms: 1. ionized Ca (50%) 2. protein bound Ca (40%) 3. Complexed to bicarb, citrate, phos (10%)