Bone Mineral Drugs Flashcards
What is the MOA of Vitamin D and its analogs?
• side effects?
- *Vitamin D/Vit D analogs:**
- *MOA:** works via intracellular and extracellular Vit. D receptors to increase BOTH calcium and phosphate reabsorption in the intestines, kidney, and to increase bone turnover.
Toxicity: All predicatable - Hypercalcemia, Hyperphosphatemia, Hypercalciuria
What forms of Vitamin D are used to treat vitamin D deficiency?
• where can these be found naturally?
Ricketts:
Cholecalicferol/Ergocalciferol – non-hydroxylated Vit D. for Vitamin D Deficiency
Note: Cholecalicferol is the form of Vitamin D found in fish liver oil – it can remain in your fat stores for a long time
What types of Vitamin D are used in the treatment of Hyperparathyroidism?
• Which can also treat hyperparathyroidism?
• which of these analogs are activated?
- *Calcitriol** – ACTIVATED vitamin D used as tx for:
1. Secondary Hyperparathyroidism (CKD) 2. Hypoparathyriodism as tx for hypocalcemia
Doxercalciferol (– ½ Activated Vitamin D used for Secondary Hyperparathyroidism (CKD)
Paricalcitriol – Calcitriol analog (ACTIVATED) – for Secondary Hyperparathyroidism (CKD)
22-oxacalcitriol
What vitamin D-based drug is used in the treament of psoriasis?
Calcipotriene (ala Calcipotriol) – Calcitriol analog (activated>) – for Psoriasis
What type of Vitamin D is used in the treatment of osteoporosis?
Osteoporosis:
Dihydrotachysterol – much less potent than Calcitriol but is more effective at high doses
***Can be given as an injection or nasal spray***
Bisphosphonates:
• Administration**
• MOA
Bisphosphonates
Administration: Oral but very poorly absorbed, take with glass of H2O and do not eat or do activities for 30 min to allow for absorption and to prevent esophageal problems.
MOA: Suppression of osteoclast activity and bone resorption
Bisphosphonates:
• Toxicity
Bisphosphonates
Toxicity: increases as drug strength increases (3rd gen most toxic)
Adynamic bone
Esophageal Irritation
Osteonecrosis of the Jaw
What are the features of osteonecrosis of the Jaw and who is at the highest risk?
Bisphosphonates
Clinical Features of Jaw Osteonecrosis: pain, exposed bone under teeth, inability to correct surgically, superimposed infection
Risk Factors: dental extraction (80% of cases), often in patients on chemo
(bisphosphonates are often given to prevent bone loss from cancer tx – esp BREAST and PROSTATE)
What are the 1st generation bisphosphonates?
• compare strength to other generations
Strength Increases with 10-100+x with each Generation
1st Etidronate
2nd Pamidronate, Alendronate, Ibandronate
3rd Risedronate, Zoledronate
What are the 2nd generation bisphosphonates?
• how does strength change with subsequent generations?
Strength Increases with 10-100+x with each Generation
1st Etidronate
2nd Pamidronate, Alendronate, Ibandronate
3rd Risedronate, Zoledronate
What are the 3rd generation bisphosphonates?
• how does strength change with each additional generation?
Strength Increases with 10-100+x with each Generation
1st Etidronate
2nd Pamidronate, Alendronate, Ibandronate
3rd Risedronate, Zoledronate
What conditions are commonly treated with bisphosphonates?
- *Paget’s Treatment** = EAR (etidronate, alendronate, risedronate)
- *Osteoporosis** = Aldendronate
What bisphosphonates are used in the treatment of Paget’s?
Paget’s Treatment = EAR (etidronate, alendronate, risedronate)
Osteoporosis = Aldendronate
What bisphosphonates are used in the treatment of osteoporosis?
Paget’s Treatment = EAR (etidronate, alendronate, risedronate)
Osteoporosis = Aldendronate
Compare the effect of bisphosphonates on bone in comparison to agents like Vitamin D, Sr2+, and PTH.
Estrogen and the Bisphonates have less of an effect on increasing bone density relative to Vitamin D, PTH, and Sr2+
**Note: any prevention of loss is really the most important thing
What are the thyroid hormone analogs?
Parathyroid Hormone Analogs – Teripartide
Teripartide:
• Administration
• MOA
Teripartide
Administration: SC; PTH used in osteoporosis is administered in low-intermitent doses which leads to increased bone synthesis and less degradation by altering gene expression.
MOA: Just like PTH they increase renal reabsorption of Ca2+ and reduce reabsorption of phosphate. Additionally, they act directly on osteoblasts to increase bone turnover. Finally, they induce vitamin D synthesis to increase calcium and phosphate uptake in the intestines.
Teripartide
• Toxicity
• Indication
Parathyroid Hormone Analogs – Teripartide
Toxicity: Same as hyperparathyroidism: hypercalcemia, hypercalcinuria (moans, stones, bones, groans)
Indication: Hypoparathyroidism, Women with Osteoporosis following tx with bisphosphonates
What drug works as a selective estrogen receptor blocker?
Selective Estrogen Receptor Modulator – Raloxifene
Raloxifene
• Administration
• MOA
Selective Estrogen Receptor Modulator – Raloxifene
Administration: Oral
MOA: works on estrogen receptors without binding estrogen receptors in the breasts
Raloxifene
• Toxicity
Selective Estrogen Receptor Modulator – Raloxifene
Toxicity: Hot Flashes, Thromboembolism
What drug works by preventing differentiation of monocytes into osteoclasts?
Denosumab
Denosumab
• Administration
• MOA
Denosumab
Administration: SC
MOA: Anti-RANKL antibody blocking the stimulation of monocytes to become osteoclasts
Denosumab
• Toxicity
• Indication
Denosumab
Toxicity: Blocking RANK compromises Immune function
Indication: increases bone mass in patients with breast and prostate cancer
What are the drug names for calcitonin?
Calcitonin: Calcimar, Miacalcin (from Salmon)
Calcimar
• Administration
• MOA
Calcitonin: Calcimar, Miacalcin (from Salmon)
Administration: SC, Intranasal – can only be administered for a few days to weeks because antibodies are easily developed against it.
MOA: Induces synthesis of Calbindin and increases Ca2+ uptake in the duodenum,
Calcimar
• Toxicity
• Indication
Calcitonin: Calcimar, Miacalcin (from Salmon)
Toxicity: Rhinitis from nose spray
Indication: Paget’s, Osteoporosis, Acute Hypercalcemia
Miacalcin
• Administration
• MOA
Calcitonin: Calcimar, Miacalcin (from Salmon)
Administration: SC, Intranasal – can only be administered for a few days to weeks because antibodies are easily developed against it.
MOA: Induces synthesis of Calbindin and increases Ca2+ uptake in the duodenum,
Miacalcin
• Toxicity
• Indication
Calcitonin: Calcimar, Miacalcin (from Salmon)
Toxicity: Rhinitis from nose spray
Indication: Paget’s, Osteoporosis, Acute Hypercalcemia
What is the use of glucocorticoids in bone health?
Glucocorticoids:
• useful in reversing lymphoma-induced hypercalcemia
What drugs act as calcimimetics?
Calcimimetics – Cinacalcet
Cinacalcet
• MOA
• Toxicity
Calcimimetics – Cinacalcet
MOA: acts on CaSR (calcium sensing receptor) to reduce the threshold of Ca2+ in the serum needed to activate the receptor and thus suppress PTH secretion from chief cells
Toxicity: Nausea, Hypocalcemia, Adynamic Bone
Cinacalcet
• Indication
Calcimimetics – Cinacalcet
Indication: Hyperparathyroidism
