Pharm Flashcards
Teriparatide
-Human recombinant of PTH (SC once a day)
-give in extreme osteoporosis when bisphosphonates don’t work and several fractures have been observed. Also in glucocorticoid induced osteoprosis
-The only drug that increases the osteoblast activity rather than decrease bone resorption.
-BBB: increases osteosarcoma in rats
AE: hypercalcemia, constipation, muscle weakness, and low energy.
Parathyroid hormone
- Increases cAMP levels
- In bone, continuous exposure causes bone resorption but pulsatile exposure causes bone formation.
- In kidney: increases Ca resorption but excretion of Pi
- in Gut: increases both Ca and Pi uptake
Vitamin D2, D3
Paricalcitol
calcipotriene
Calcitriol
-in the skin by UVL it is made into cholecalciferol, in the liver it turns to calcidiol and in the kidney it is activated to calcitriol
-directly (via gene expression) and indirectly(via increase in Ca) inhibits PTH
-causes bone formation (increases Ca and Pi absorption and inhibits their excretion in kidneys)
-inhibits proliferation, stimulation of skin and malignant cells.
-give for rickets, osteomalacia, vit. D deficiency hypoparathyrodism
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Paricalcitol: it is more selective than calcitriol. It decreases PTH synthesis but doesnt do it by inducing hypercalcemia. This is great for patients with secondary hyperparathyrodism of renal failure.
- recall it needs fat to be absorbed, excreted in bile
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Calcipotriene: use for Psoriasis
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Calcitriol: give for osteoprosis, secondary hyperparathyrodism of renal failure, vit. D dependent or resistant rickets.
Calcitonin
- Tones the Ca and pi down
- Secreted from parafollicular cells of thyroid in response to too much Ca so antagonizes the PTH
- salmon calcitonin has a higher half life than human
- Relives bone pain in osteoporosis (unique characteristics)
- Used in paget’s dz, hyperparathyrodism, osteoprosis in post menopausal women, idiopathic juveniile hypercalcemia, vit. D intoxication, osteolytic bone disorder.
- If on it for a longer period of time, antibodies develop against it.
- Due to safety issues not recommended by FDA and is banned in CA and Europe
- AE: Anaphylaxis, rhinitis, nasal mucosa irritation, headache, nausea, flushing
Bisphosphanates
All the drontaes
-bind the hydroxyapetite and kill the osteoclasts so increase bone density and reduce fractures. Also inhibit proton pump in osteoclasts
-give in paget’s disease (Pamidronate (IV)), FIRST LINE FOR menopausal osteoprosis, glucocorticoid indices osteoprosis, hypercalcemia, other bone diseases
-Risedronate and Alendronate inhibit Farnesyl pyrophosphate which is required for osteoclastic activity.
-very poor oral absorption and iron messes up with absorption
AE: esophagitis (give on empty stomach with a glass of PLAIN water one hour b4 breakfast and sit upright for 30 mins), GI disturbance, jaw ostenonecrosis
-Contraindicated in renal failure because it is eliminated by kidneys
cinacalcet
Regulator of PTH
-A calcium sensing receptor (CaSR) on chief cells of parathyroid, senses Ca and regulates PTH depending on the Ca level. Cinacalcet is an agonist for this receptor. Increases the affinity for Ca and therefore decreases PTH.
Uses: primary and secondary hyperparathyrodism
AE: Hypocalcemia, nausea, vomitting, diarrhea, arthralgia, myalgia
Sevelamer
-A phosphate binder
-binds dietary phosphate in the GI and decreases both PTH and phosphate
USE: hyperphosphatemia in ESRD patients
AE: GI disturbances
Denosumab
monoclonal antibody against RANKL so inhibits ostecolast
-IM every 6 months
-good for postmenopausal osteoprosis, giant cell tumor of bone, multiple myeloma, RA
AE: hypocalcemia, jaw osteonecrosis
Very $$$$$$$ compared to bisphosphanates
Raloxifene
-SERM(selective estrogen receptor modulator)
in the bones it increases bone density and in the breast it decreases breast cancer risk (good for younger postmenopausal women)
**first line after bisphosphanates if the patient is intolerant to bisphosphonates
