Drugs/Physiology: Osteoporosis, DM, Endocrine Flashcards
Raloxifene
Selective estrogen receptor modulator (SERM)
Bisphosphonate Action
The “dronate’s”- Impair osteoclast function (decrease differentiation/increase apoptosis) via inhibiting farnesyl pyrophosphate (FPP) synthase in mevalonate pathway > disrupts protein prenylation > cytoskeletal abnormalities
Increase bone mineral density (BMD)/decrease fractures
Bisphosphonate SEs
Esophagitis with orals, flu like symptoms with IV, bone/muscle pain (rare), hypocalcemia
Long Term SEs: atypical subtrochanteric fractures > micro cracks- avoid via “drug holidays”, micro cracks can also lead to osteonecrosis of jaw +/- infection
Contraindicated if Creatinine clearance
Alendronate
Bisphosphonate: PO
Risedronate
Bisphosphonate: PO
Ibandronate
Bisphosphonate: PO, IV
Xolendronic acid (zolendronate)
Bisphosphonate: IV
Selective Estrogen Receptor Modulator (SERM) Action
Binds to estrogen receptor:
Agonist in bone > inhibit osteoclast
Antagonist in Breast tissue > reduced BC risk
SERM SEs
DVT, hot flushes
Denosumab
Monoclonal Antibody, SubQ injection/6 months
Denosumab Action
directly binds to RANKL (secreted via osteoblasts and responsible for osteoclast activation), similar to osteoprotegerin (OPG) > blocks maturation of osteoclast
Denosumab SEs
Hypocalcemia, potential neoplastic due to lymphocytes requiring RANKL
NO renal restrictions (can treat Creatinine
Teriparatide (human recombinant PTH-34)
Anabolic (unique in respect to osteoporosis drugs): stimulates osteoblast activity
Teriparatide Action
Induces differentiation/maturation of osteoblast, reduces osteoblast apoptosis (given daily SubQ)
Teriparatide SEs
Increase uric acid (3% of patients), hypercalcemia, osteosarcoma (seen in lab only > 2 yr treatment limit)
Contraindicated at high risk osteosarcoma (Paget, radiation, open epiphyses), cancer diagnosis in past 5 yrs, elevated PTH
Cinacalcet
Calcium mimetic > binds to CaSR on parathyroid gland > decrease Ca release from bone but DOES NOT normalize PTH
SE: nausea
Calcitriol
1,25 OH2 Vitamine D: treat hypoparathyroidism > attempt to get Ca levels to 8.5-9.5 to prevent hypercalciuria
Propanonlol
B-blocker: used to treat sympathetic symptoms of hyperthyroidism (only necessary treatment to thyroiditis)
Methimazole
Thionamide used in hyperthyroidism to decrease production of T4
Propylthiouracil
Thionamide used in hyperthyroidism to decrease production of T4
Most common treatment modality for Grave’s disease
Radioactive iodine (I-131) > radiation ablates thyroid gland and follow with supplemental thyroid hormone SEs: don't give to patients with proptosis > can worsen May cause iodine-induced thyroiditis initially
Thioamide SEs
Thionamides = proplythiouracil and methimazole
Rash, agranulocytosis (neutr), cholestasis, fulminant liver failure with PTU, Methimazole - teratogenic during 1st trimester (use PTU during 1st then Methimazole for remaining)
How do you treat primary adrenal insufficiency?
Glucocorticoid (prednisone or hydrocortisone) + mineralcorticoid (fludrocortisone)
Metyrapone
Inhibit cortisol synthesis (used in ectopic Cushing’s)
Ketoconazole
Inhibit cortisol synthesis (used in ectopic Cushing’s)
Mifepristone
Cortisol receptor blocker (used in ectopic Cushing’s)
What Abs are found in Hashimot’s thyroiditis?
Thyroid peroxidase antibodies (TPO)
Levothyroxine
T4- treatment of primary hypothyroidism