Drugs for Osteoporosis Flashcards
What are two types of drugs that are used to treat osteoporosis?
SERMS and bisphosphonates
Osteoporosis Drugs: SERMS stand for
Selective estrogen receptor modulators
Osteoporosis Drugs: What are three types of oral bisphosphonates?
Fosamax, Acetonel, Boniva
Osteoporosis Drugs: Example of SERMS drug
Raloxifene
Osteoporosis Drugs: Raloxifene Function
Activates estrogen receptors in bone.
Osteoporosis Drugs: FDA approved Raloxifene for what use?
For prevention of osteoporosis in postmenopausal women
Osteoporosis Drugs: What does Raloxifene not do?
Does not activate estrogen receptors in breast, thus helping to prevent breast cancer
Osteoporosis Drugs: Raloxifene is primarily used by what population? Why?
Used by women with osteporosis risk who also have risk for breast cancer (therefore are unable/unwilling to take estrogen)
Osteoporosis Drugs: Raloxifene alternate name
Evista
Osteoporosis Drugs: Evista (Raloxifene) is the only medication to reduce what two events?
- Reduce risk for spinal fractures due to osteoporosis
2. Reduce risk of invasive breast cancer in postmenopausal women with osteoporosis
Osteoporosis Drugs: What does Evista (Raloxifene) not do?
Does not treat breast cancer, prevent it from returning, or reduce the risk of all forms of breast cancer.
Osteoporosis Drugs: Evista (Raloxifene) summary of effects (3)
- Anti-resorptive action on bone
- Absence of vaginal bleeding
- Absence of endometrial and breast stimulation
Osteoporosis Drugs: Evista (Raloxifene) side effects
Hot flashes, leg cramps
Osteoporosis Drugs: MOA of Bisphosphonates
- Target osteoclasts
- Inhibit osteoclast formation and activity
What are the three oral bisphosphonates?
- Alendronate
- Risedronate
- Ibandronate
Function of oral bisphosphonates
Prevention and treatment of osteoporosis
What are the three IV bisphosphonates?
Etidronate
Pamidronate
Zoledronic acid
Tiludronate
Function of IV bisphosphonates
Treatment of bone pathologies
What is the IV bisphosphonate that is used for osteoporosis prevention
Zoledronic acid
What are some challenges of bisphosphonates?
- Low bio availability
- Take with full glass of water only
- Use with calcium but at different times
- Remain upright for 30 minutes to 1 hour after taking
Common Side effects of bisphosphonates
- Erosive esophagitis
- Headache
- GI distress
Oral complication of bisphosphonates
Osteonecrosis of the jaw
When are IV bisphosphonates used in most cases?
Given at higher doses for chemotherapy for cancers that have metastasized to the bone.
What are three examples of bisphosphonates given for chemotherapy and other bone pathologies
- Etidronate disodium
- Pamidronate
- Tiludronate
- Zoledronic acid
Bisphosphonates: Etidronate disodium uses
Paget’s disease, hypercalcemia (malignancy)
Bisphosphonates: Pamidronate Uses
Hypercalcemia (malignancy), bone cancers
Bisphosphonates: Tiludronate uses
Paget’s Disease
Bisphosphonates: Zoledronic acid uses
Hypercalcemia (malignancy), bone cancers
What is a complication of Bisphosphonates that occurs due to long-term use?
Increase prevalence of atypical fractures, especially in mid-shaft long bone and femur fractures
Two functions of calcitonin
Greatest effect in patients with rapid bone turnover.
Relieves osteoporotic bone pain
Teriparatide is a ____ derivative
Parathyroid
Teriparatide Is given to what population
- Postmenopausal osteoporotic women and hypogonadal osteoporotic men at high risk of fracture
- Glucocorticoid induced osteoporosis in men and women at high risk for fracture
Teriparatide Function
Stimulates osteoblasts, increases GI and kidney absorption of calcium.
Denosumab is not a Bisphosphonate but is an _____ _____
Monoclonal antibody
Denosumab Indications
Treatment of osteoporosis in men and postmenopausal women at high risk for fractures
Denosumab are used for patients with what two conditions?
Bone metasteses from solid tumors
Multiple myeloma
Prolia (Denosumab) is injected how often?
60 mg as a single dose every six months
Prolia (Denosumab) Function
Receptor blocker on osteoclasts
Prolia (Denosumab) MOA
Blocks interaction between ligand (RANKL) and receptor (RANK) located on osteoclast surfaces and prevents osteoclast formation
Prolia (Denosumab) leads to ______ bone resportion and ____ bone mass
Decreased; increased
Prolia (Denosumab) is associated with what oral complication?
Oral necrosis of the jaw
Prolia and Bisphosphonates share what common target?
Osteoclast inhibition
Calcium supplements dosage over 51
1200 mg/day
Calcium supplements for postmenopausal women without HRT
1500 mg/day
Calcium supplements max dose
2500 mg
Calcium supplement doses should be split into ____-_____ mg
500-600 mg
When should calcium supplements be taken?
At mealtime
Calcium is combined with what two other elements to become dietary calcium? What is it known as?
Carbon and oxygen; calcium carbonate
What happens when calcium carbonate is digested?
Carbon and oxygen breaks away to return to its elemental form
How much elemental calcium is in calcium carbonate?
40%
What are two types of calcium supplements?
Calcium carbonate and calcium citrate
Advantages of Calcium Carbonate
- 40% elemental calcium
- Inexpensive, requires few tablets
- Absorption is acid-dependent
Advantages of calcium citrate
- 24% elemental calcium
- Acid dependent
- better for those taking Tagamet and Prilosec
Total calcium intake and dietary calcium offer ____ protective effects
Cardiovascular
Calcium supplements are associated with an increased risk for ____ ____ events; what are some examples?
Adverse cardiac
MI, stroke, coronary artery calcification, mortality
Vitamin D is necessary for the absorption of ___ and _____
Calcium and phosphorus
Function of Vitamin D
- Increases bone mass
- Decreases fracture rate
Vitamin D decreases PTH which decreases ___
Resorption
VItamin D potentially increases ______ _____
Bone formation
What is the vitamin D preparation?
Ergocalciferol
The vitamin D2 supplement is known as
Ergocalciferol
Ergocalciferol has a _____ half-life and decreased _____
Short; decreased
The vitamin D3 supplement is known as
Cholecalciferol
Cholecalciferol is synthesized where?
In humans in skin
Cholecalciferol is more effective at raising and maintaing what?
Vitamin D test
Why would vegans not want to use vitamin D3?
Because supplements are derived from animal source
What is the normal vitamin D test?
30 to 74 ng/mL
Vitamin D Deficiency can be avoided by
Going outside
What is the right dose of vitamin D for preventing all cancer types?
Calcium 1400-1500 mg/day plus vitamin D3 1100 IU/day in postmenopausal women
What is the right dose of vitamin D for muscle pain caused by meds called “statins”?
vitamin d2 or d3 50,000 unites once a week
What is the right dose of vitamin D for preventing the flu?
vitamin D 12000 IU daily
Most vitamin supplements contain only ____ IU vitamin D
400
Vitamin D Dosage to prevent rickets/bone pain:
Birth through 50 years of age
200 IU
Vitamin D Dosage to prevent rickets/bone pain:
Adults 51 to 70 years old
400 IU
Vitamin D Dosage to prevent rickets/bone pain:
Adults greater than 70 years of age
600 IU