Podcast
Questions and Answers
Which of the following is NOT a recognized antiresorptive agent used in osteoporosis drug management?
Which of the following is NOT a recognized antiresorptive agent used in osteoporosis drug management?
- Alendronate
- Denosumab
- Raloxifene
- Teriparatide (correct)
What is the mechanism of action of anabolic therapies for osteoporosis?
What is the mechanism of action of anabolic therapies for osteoporosis?
- Inhibiting osteoclast formation and activity
- Promoting calcium absorption in the intestines
- Stimulating bone formation by increasing osteoblast activity (correct)
- Decreasing bone turnover
What is the primary target when using antiresorptive medications?
What is the primary target when using antiresorptive medications?
- Osteoclast (correct)
- Osteoblast
- Osteocyte
- Bone marrow
A T-score of what value is indicative of osteoporosis?
A T-score of what value is indicative of osteoporosis?
Which of the following lifestyle factors is LEAST likely to contribute to the management of osteoporosis?
Which of the following lifestyle factors is LEAST likely to contribute to the management of osteoporosis?
Which of the following best describes the action of bisphosphonates in treating osteoporosis?
Which of the following best describes the action of bisphosphonates in treating osteoporosis?
How does Denosumab reduce bone resorption?
How does Denosumab reduce bone resorption?
Raloxifene, a Selective Estrogen Receptor Modulator (SERM), is often prescribed for postmenopausal women with osteoporosis. What is its primary mechanism of action on bone tissue?
Raloxifene, a Selective Estrogen Receptor Modulator (SERM), is often prescribed for postmenopausal women with osteoporosis. What is its primary mechanism of action on bone tissue?
What is a notable concern associated with the discontinuation of Denosumab?
What is a notable concern associated with the discontinuation of Denosumab?
For whom is Raloxifene most useful for?
For whom is Raloxifene most useful for?
What is a common recommendation regarding the use of bisphosphonates?
What is a common recommendation regarding the use of bisphosphonates?
What is the general recommendation regarding calcium and vitamin D supplementation for osteoporosis?
What is the general recommendation regarding calcium and vitamin D supplementation for osteoporosis?
Which of the following is NOT a typical side effect associated with bisphosphonates?
Which of the following is NOT a typical side effect associated with bisphosphonates?
What is the recommended administration frequency for Denosumab?
What is the recommended administration frequency for Denosumab?
Which of the following is a recognized anabolic agent used in the treatment of osteoporosis?
Which of the following is a recognized anabolic agent used in the treatment of osteoporosis?
What is the most probable action of Teriparatide (PTH) on bone?
What is the most probable action of Teriparatide (PTH) on bone?
What is the recommended approach following the cessation of teriparatide treatment?
What is the recommended approach following the cessation of teriparatide treatment?
What is a common reason for NOT recommending teriparatide?
What is a common reason for NOT recommending teriparatide?
Abaloparatide is similar to Teriparatide, but what is one key difference?
Abaloparatide is similar to Teriparatide, but what is one key difference?
Which of the following best characterizes Romosozumab's mechanism of action?
Which of the following best characterizes Romosozumab's mechanism of action?
Which intervention is recommended when discontinuing denosumab treatment to mitigate potential adverse effects?
Which intervention is recommended when discontinuing denosumab treatment to mitigate potential adverse effects?
How do bisphosphonates interfere with osteoclast function at a molecular level?
How do bisphosphonates interfere with osteoclast function at a molecular level?
A patient with osteoporosis has a history of atypical femoral fractures. Which medication should be avoided due to its potential to exacerbate this condition?
A patient with osteoporosis has a history of atypical femoral fractures. Which medication should be avoided due to its potential to exacerbate this condition?
Which antiresorptive agent is least likely to be characterized by a long biologic half-life or incorporation into bone?
Which antiresorptive agent is least likely to be characterized by a long biologic half-life or incorporation into bone?
Following long-term Denosumab treatment, what is recommended?
Following long-term Denosumab treatment, what is recommended?
Which of the following is a significant consideration when prescribing Romosozumab for osteoporosis?
Which of the following is a significant consideration when prescribing Romosozumab for osteoporosis?
Calcium and Vitamin D supplementation should be considered with the following maximum daily intake?
Calcium and Vitamin D supplementation should be considered with the following maximum daily intake?
How does raloxifene reduce bone resorption?
How does raloxifene reduce bone resorption?
What is a similarity between Teriparatide and Abaloparatide?
What is a similarity between Teriparatide and Abaloparatide?
What is the primary reason why high-dose calcium supplementation is NOT universally recommended for older women?
What is the primary reason why high-dose calcium supplementation is NOT universally recommended for older women?
A 72-year-old female patient with osteoporosis, who has been on long-term bisphosphonate therapy, presents with a sudden onset of thigh pain after a minor fall. Radiographic examination reveals a transverse fracture pattern in the femoral shaft. Which of the following is the MOST likely diagnosis?
A 72-year-old female patient with osteoporosis, who has been on long-term bisphosphonate therapy, presents with a sudden onset of thigh pain after a minor fall. Radiographic examination reveals a transverse fracture pattern in the femoral shaft. Which of the following is the MOST likely diagnosis?
A postmenopausal woman with severe osteoporosis is being considered for Romosozumab. Which pre-existing condition would be the MOST concerning contraindication for this medication?
A postmenopausal woman with severe osteoporosis is being considered for Romosozumab. Which pre-existing condition would be the MOST concerning contraindication for this medication?
In an extremely rare scenario, what condition could be caused by an activating mutation of LRP5/6 receptor?
In an extremely rare scenario, what condition could be caused by an activating mutation of LRP5/6 receptor?
Which of the following is the most important assessment prior to initiating bisphosphonate therapy in a patient with osteoporosis?
Which of the following is the most important assessment prior to initiating bisphosphonate therapy in a patient with osteoporosis?
A patient reports persistent heartburn and difficulty swallowing after starting alendronate for osteoporosis. What guidance should the healthcare provider give the patient?
A patient reports persistent heartburn and difficulty swallowing after starting alendronate for osteoporosis. What guidance should the healthcare provider give the patient?
Which medication is an anabolic therapy?
Which medication is an anabolic therapy?
A key enzyme in the mevalonic acid pathway is the target for which drug?
A key enzyme in the mevalonic acid pathway is the target for which drug?
Which drug mimics osteoprotegerin?
Which drug mimics osteoprotegerin?
Which of the following drugs is a human parathyroid hormone related peptide?
Which of the following drugs is a human parathyroid hormone related peptide?
Which of the following is a primary goal of antiresorptive medications in osteoporosis treatment?
Which of the following is a primary goal of antiresorptive medications in osteoporosis treatment?
What is the structural basis of bisphosphonates?
What is the structural basis of bisphosphonates?
How does teriparatide affect bone remodeling to increase bone mass?
How does teriparatide affect bone remodeling to increase bone mass?
What is the recommended approach when discontinuing denosumab treatment?
What is the recommended approach when discontinuing denosumab treatment?
What is the role of sclerostin in bone remodeling?
What is the role of sclerostin in bone remodeling?
Which of the following is associated with high-dose calcium supplementation?
Which of the following is associated with high-dose calcium supplementation?
Which of the following lifestyle recommendations is crucial for individuals over 50 to maintain bone density?
Which of the following lifestyle recommendations is crucial for individuals over 50 to maintain bone density?
What is a key consideration when prescribing raloxifene to postmenopausal women?
What is a key consideration when prescribing raloxifene to postmenopausal women?
Which of the following best describes the action of anabolic agents in treating osteoporosis?
Which of the following best describes the action of anabolic agents in treating osteoporosis?
What is the general recommendation for calcium intake for individuals undergoing osteoporosis treatment?
What is the general recommendation for calcium intake for individuals undergoing osteoporosis treatment?
What is the impact of Sclerostin on bone formation?
What is the impact of Sclerostin on bone formation?
After the cessation of teriparatide treatment, what subsequent treatment is typically recommended and why?
After the cessation of teriparatide treatment, what subsequent treatment is typically recommended and why?
How does denosumab administration differ from that of oral bisphosphonates, such as alendronate?
How does denosumab administration differ from that of oral bisphosphonates, such as alendronate?
What is the role of Vitamin D in osteoporosis?
What is the role of Vitamin D in osteoporosis?
Which of the following is a potential side effect of bisphosphonates that requires careful consideration?
Which of the following is a potential side effect of bisphosphonates that requires careful consideration?
Which statement accurately describes the mechanism of action of Romosozumab?
Which statement accurately describes the mechanism of action of Romosozumab?
Which of the following is a crucial aspect of managing osteoporosis in postmenopausal women?
Which of the following is a crucial aspect of managing osteoporosis in postmenopausal women?
What is a key difference in the actions of teriparatide (PTH) and abaloparatide (PTHrP)?
What is a key difference in the actions of teriparatide (PTH) and abaloparatide (PTHrP)?
What is the rationale behind limiting teriparatide use to 18 months?
What is the rationale behind limiting teriparatide use to 18 months?
What is the primary reason calcium supplements should be used cautiously in elderly individuals who are not institutionalized?
What is the primary reason calcium supplements should be used cautiously in elderly individuals who are not institutionalized?
A patient with osteoporosis is prescribed denosumab. What is the most important counseling point to emphasize?
A patient with osteoporosis is prescribed denosumab. What is the most important counseling point to emphasize?
How do bisphosphonates induce osteoclast apoptosis?
How do bisphosphonates induce osteoclast apoptosis?
What is the primary rationale behind the use of anti-resorptive agents in osteoporosis management?
What is the primary rationale behind the use of anti-resorptive agents in osteoporosis management?
Which of the following is a non-pharmacological recommendation for osteoporosis management?
Which of the following is a non-pharmacological recommendation for osteoporosis management?
Alendronate, risedronate, and zoledronic acid belong to which class of anti-resorptive agents?
Alendronate, risedronate, and zoledronic acid belong to which class of anti-resorptive agents?
What is the recommended frequency of administration for denosumab?
What is the recommended frequency of administration for denosumab?
How does raloxifene contribute to bone health in postmenopausal women?
How does raloxifene contribute to bone health in postmenopausal women?
Which of the following is an anabolic agent used in the treatment of osteoporosis?
Which of the following is an anabolic agent used in the treatment of osteoporosis?
What is the term for a synthetic human parathyroid hormone-related peptide?
What is the term for a synthetic human parathyroid hormone-related peptide?
What is a potential concern associated with discontinuing denosumab treatment without a follow-up therapy?
What is a potential concern associated with discontinuing denosumab treatment without a follow-up therapy?
What is a common side effect associated with raloxifene?
What is a common side effect associated with raloxifene?
What potential risk should clinicians consider when prescribing Romosozumab for osteoporosis?
What potential risk should clinicians consider when prescribing Romosozumab for osteoporosis?
What is the typical timeframe for improvements in BMD after initiating anabolic therapies?
What is the typical timeframe for improvements in BMD after initiating anabolic therapies?
What should be done after completion of a course of Abaloparatide?
What should be done after completion of a course of Abaloparatide?
What is meant when Romosozumab can be described as having 'dual action'?
What is meant when Romosozumab can be described as having 'dual action'?
What is the main reason an osteoporosis patient might prefer Denosumab over oral bisphosphonates such as alendronate?
What is the main reason an osteoporosis patient might prefer Denosumab over oral bisphosphonates such as alendronate?
What is the relationship between Osteocytes and Sclerostin?
What is the relationship between Osteocytes and Sclerostin?
Other than falls, why might someone with Oestrogen and Vitamin D deficiency develop osteoporosis?
Other than falls, why might someone with Oestrogen and Vitamin D deficiency develop osteoporosis?
What is the primary goal of osteoporosis management?
What is the primary goal of osteoporosis management?
Which of the following is a common risk factor for osteoporosis that is related to lifestyle?
Which of the following is a common risk factor for osteoporosis that is related to lifestyle?
Which type of exercise is most beneficial for improving bone density in individuals over 50?
Which type of exercise is most beneficial for improving bone density in individuals over 50?
What is the primary action of antiresorptive medications in treating osteoporosis?
What is the primary action of antiresorptive medications in treating osteoporosis?
Which of the following is a potential side effect associated with raloxifene?
Which of the following is a potential side effect associated with raloxifene?
What is the method of administration of denosumab?
What is the method of administration of denosumab?
What is a key recommendation regarding bisphosphonate use?
What is a key recommendation regarding bisphosphonate use?
What strategy is recommended to mitigate the risk of rebound fractures after discontinuing denosumab?
What strategy is recommended to mitigate the risk of rebound fractures after discontinuing denosumab?
Which of the following best characterizes the mechanism of action of bisphosphonates?
Which of the following best characterizes the mechanism of action of bisphosphonates?
What is a significant consideration when prescribing romosozumab?
What is a significant consideration when prescribing romosozumab?
What is the role of PTHrP (parathyroid hormone related peptide) in Abaloparatide?
What is the role of PTHrP (parathyroid hormone related peptide) in Abaloparatide?
For whom is raloxifene most appropriate?
For whom is raloxifene most appropriate?
For whom is teriparatide NOT recommended?
For whom is teriparatide NOT recommended?
How does denosumab reduce bone resorption at the molecular level?
How does denosumab reduce bone resorption at the molecular level?
After cessation of teriparatide treatment, which treatment is typically recommended?
After cessation of teriparatide treatment, which treatment is typically recommended?
What is the general recommendation for calcium and vitamin D supplementation in osteoporosis treatment?
What is the general recommendation for calcium and vitamin D supplementation in osteoporosis treatment?
What is the mechanism of action of romosozumab?
What is the mechanism of action of romosozumab?
Why might Denosumab be preferred over oral bisphosphonates?
Why might Denosumab be preferred over oral bisphosphonates?
What is a potential concern associated with high-dose calcium supplementation in older women?
What is a potential concern associated with high-dose calcium supplementation in older women?
What is the primary reason for limiting teriparatide use to 18 months?
What is the primary reason for limiting teriparatide use to 18 months?
What is the role of sclerostin in bone remodeling, and how does romosozumab affect this process?
What is the role of sclerostin in bone remodeling, and how does romosozumab affect this process?
A patient with osteoporosis is being considered for teriparatide. Which pre-existing condition would be a contraindication for this medication?
A patient with osteoporosis is being considered for teriparatide. Which pre-existing condition would be a contraindication for this medication?
Raloxifene is known to not increase risk of cancer in which organ?
Raloxifene is known to not increase risk of cancer in which organ?
What characterizes the mechanism of action of anabolic agents in treating osteoporosis?
What characterizes the mechanism of action of anabolic agents in treating osteoporosis?
What is the significance of FRAX score in the management of osteoporosis?
What is the significance of FRAX score in the management of osteoporosis?
A patient who has been on long-term bisphosphonate therapy is at increased risk of what?
A patient who has been on long-term bisphosphonate therapy is at increased risk of what?
A patient has been prescribed alendronate, what needs to be assessed?
A patient has been prescribed alendronate, what needs to be assessed?
Which of the following best describes how bisphosphonates affect osteoclasts in order to reduce bone resorption?
Which of the following best describes how bisphosphonates affect osteoclasts in order to reduce bone resorption?
Romosozumab has a high binding affinity to which?
Romosozumab has a high binding affinity to which?
The risk windows for osteonecrosis of the jaw (ONJ) and atypical femoral fractures (AFF) in patients on long-term bisphosphonate therapy are primarily related to what factor?
The risk windows for osteonecrosis of the jaw (ONJ) and atypical femoral fractures (AFF) in patients on long-term bisphosphonate therapy are primarily related to what factor?
Why might individuals living away from sunlight develop osteoporosis?
Why might individuals living away from sunlight develop osteoporosis?
Why are falls bad even if someone isn't osteoporotic?
Why are falls bad even if someone isn't osteoporotic?
What advice might you give a smoker to prevent osteoporosis?
What advice might you give a smoker to prevent osteoporosis?
What is the FRAX tool used for?
What is the FRAX tool used for?
Name a drug that requires sequential treatment
Name a drug that requires sequential treatment
What is a difference between osteoporosis and osteopenia?
What is a difference between osteoporosis and osteopenia?
What causes bone mineral density to decrease following the cessation of teriparatide treatment?
What causes bone mineral density to decrease following the cessation of teriparatide treatment?
What factor reduces bone turnover?
What factor reduces bone turnover?
What is a condition that means that teriparatide should not be used?
What is a condition that means that teriparatide should not be used?
Both Abaloparatide and Teriparatide are administered via which method?
Both Abaloparatide and Teriparatide are administered via which method?
What is true of Abaloparatide?
What is true of Abaloparatide?
Which of the following is an example of an antiresorptive medication?
Which of the following is an example of an antiresorptive medication?
Which medication directly inhibits sclerostin to increase bone formation?
Which medication directly inhibits sclerostin to increase bone formation?
A patient with a history of vertebral fractures is prescribed raloxifene. What is the primary mechanism of action for this medication?
A patient with a history of vertebral fractures is prescribed raloxifene. What is the primary mechanism of action for this medication?
Which of the following is a significant concern associated with discontinuing denosumab without transitioning to another osteoporosis therapy?
Which of the following is a significant concern associated with discontinuing denosumab without transitioning to another osteoporosis therapy?
Which characteristic distinguishes raloxifene from traditional hormone replacement therapy (HRT) in treating osteoporosis?
Which characteristic distinguishes raloxifene from traditional hormone replacement therapy (HRT) in treating osteoporosis?
What is a typical recommendation regarding the duration and monitoring of bisphosphonate use for osteoporosis?
What is a typical recommendation regarding the duration and monitoring of bisphosphonate use for osteoporosis?
What is the general recommendation regarding calcium supplementation for individuals undergoing osteoporosis treatment?
What is the general recommendation regarding calcium supplementation for individuals undergoing osteoporosis treatment?
How is denosumab typically administered to patients with osteoporosis?
How is denosumab typically administered to patients with osteoporosis?
Which of the following should a doctor consider before prescribing Romosozumab?
Which of the following should a doctor consider before prescribing Romosozumab?
What is the primary action of anabolic agents in treating osteoporosis?
What is the primary action of anabolic agents in treating osteoporosis?
What type of activity is most beneficial for improving bone density in individuals over 50?
What type of activity is most beneficial for improving bone density in individuals over 50?
What is a potential risk associated with high-dose calcium supplementation in older women?
What is a potential risk associated with high-dose calcium supplementation in older women?
What is the key target of action for bisphosphonates?
What is the key target of action for bisphosphonates?
Which agent is a synthetic form of parathyroid hormone-related protein?
Which agent is a synthetic form of parathyroid hormone-related protein?
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Study Notes
Antiresorptive Agents
- Bisphosphonates include alendronate, risedronate, and zoledronic acid
- Denosumab is another antiresorptive agent
- Selective Oestrogen Receptor Modulators (SERMs) like raloxifene are also used
Anabolic Therapies
- Teriparatide (PTH) is a parathyroid hormone
- Abaloparatide (PTHrP) is a parathyroid hormone-related peptide
- Romosozumab targets sclerostin
Learning Outcomes
- Understand osteoporosis management and pharmacologic treatments.
- Differentiate between antiresorptive and anabolic therapies.
- Describe the actions/uses of antiresorptive and anabolic agents
- Know the issues/side effects of current osteoporosis therapies.
- Discuss calcium and vitamin D supplementation benefits for osteoporosis/osteopenia.
Osteoporosis Recap
- Loss of bone integrity leads to increased fracture risk
- Minimal trauma fractures occur from standing height, affecting the spine, hip, or forearm
- Low bone mineral density is characteristic
- A T-score of -2.5 or worse indicates osteoporosis, while -1.0 to -2.5 suggests osteopenia
- Osteoporosis is under-diagnosed but common in women and men, increasing fracture-related morbidity/mortality
Management of Osteoporosis
- A healthy lifestyle includes managing age, postmenopausal status, smoking, physical activity, BMI, and nutrition
- Assess risk factors like family history, BMD, and FRAX score
- Treat secondary causes such as increased PTH, glucocorticoid use, autoimmune conditions, and hypogonadism
- Manage calcium/Vit D deficiency, renal disease, aromatase inhibition in breast cancer, and androgen deprivation in prostate cancer
- Specific osteoporosis therapies include antiresorptive and anabolic options
Bisphosphonates
- Alendronate, risedronate, and zoledronic acid are bisphosphonates
- Bisphosphonates are structurally linked to inorganic pyrophosphate, consisting of two phosphate groups, and bind to bone
- Nitrogen-containing R2 side chains are second & third generation bisphosphonates
- Oral bisphosphonates include alendronate, risedronate, ibandronate, etidronate, and clodronate.
- Intravenous bisphosphonates include ibandronate and zoledronate
Bisphosphonates Action
- Anti-resorptive
- High affinity for hydroxyapatite in the inorganic phase of bone
- Cause osteoclast apoptosis after resorption
- Inhibit farnesyl pyrophosphate synthase (FPPS), a key enzyme in the mevalonic acid pathway
- Interfere with small GTP-binding proteins involved in osteoclast function
Bisphosphonates Use
- Prevent vertebral fractures in women with osteopenia (>10 years postmenopause)
- Reduce vertebral and non-vertebral fractures in women and men over 50 at high risk
- Use for 5 years then reassess
Bisphosphonates Side Effects
- Esophageal ulceration, mainly with oral forms
- Musculoskeletal pain
- Hypocalcemia with intravenous zoledronic acid
- Fever, especially with IV zoledronic acid
- Osteonecrosis of the jaw (ONJ) is related to a disruption in bone remodeling, not allowing osteoclasts to clean damaged bone
- Atypical femoral fractures (AFFs) are spontaneous and progress into a full fracture
- Adynamic bone disease
Denosumab
- IgG2 monoclonal antibody which inhibits RANKL
- Inhibits bone resorption by mimicking osteoprotegerin (OPG)
- Prevents RANKL from binding to RANK, thus reducing osteoclast development, survival, and bone resorption
- Recommended to treat osteoporosis in postmenopausal women/men
- Used for minimal trauma fracture risk
- Alternative for bisphosphonates
- Administered subcutaneous as 60mg every six months and well-tolerated
Denosumab: Osteoclast Differentiation
- Denosumab decreases the differentiation of osteoclasts
Denosumab Side Effects
- Cellulitis(Skin infections).
- Hypocalcemia (chronic kidney disease)
- Osteonecrosis of the jaw(ONJ)
- Atypical femoral fracture
- Multiple vertebral fractures upon discontinuation (rebound)
- Short half-life
- With the short half-life, the RANKL-starved cells are primed and do more damage than usual
- Oral treatments have compliance issues
Denosumab vs Bisphosphonates
- Denosumab is not characterized by a long biologic half-life nor is it incorporated into the bone, unlike bisphosphonates
- The antiresorptive effect of denosumab ceases after the treatment ends
- A concern is a drug “rebound” can occur, resulting in vertebral fractures following discontinuation
- Re-evaluation of risk should be assessed after five years
Denosumab Discontinuation
- Transition to oral bisphosphonates is recommended
- Do this for at least 12 months, starting 4 weeks after the missed dose
Selective Estrogen Receptor Modulators (SERMs)
- Raloxifene is a 2nd Gen SERM
- Synthetic non-steroidal agents
- Act as estrogen agonists & antagonists, and have anti-fracture efficacy
- Found in osteoclasts/osteoblasts and estrogen-depletion leads to bone loss
Raloxifene Action
- Decreases osteoclast activity leading/reducing bone resorption
Raloxifene Use and Administration
- Treatment for postmenopausal women with osteoporosis especially with vertebral fractures
- Others are poorly tolerated
- Effective in younger PM women at risk of vertebral fracture and who have a prior/family history of breast cancer
- Given orally at 60mg per day
Raloxifene Side Effects
- Oestrogen Replacement: Raises risk of invasive breast cancer, coronary heart disease, and thromboembolic events.
- Raloxifene: May increase hot flushes, thromboembolic events(2.5X) but not heart disease/risk of stroke, and has little effect on the endometrium
Teriparatide
- Analog of parathyroid hormone(PTH)(1-34)
Teriparatide Action
- Anabolic
- Binds to the PTH Type 1 receptor (PTH1R) which is a G-protein coupled receptor(GPCR) expressed on osteoblasts
- Increases new bone formation by osteoblasts while increasing osteoblasts survival
Teriparatide Mechanism
- Intermittent PTH helps in bone formation
Teriparatide Use
- Used on patients who have have a low bone mass density
- used to decrease vertebral and non-vertebral fractures in postmenopausal osteoporosis with prior fracture
- Patients with a BMD T-Score of ≤-3.0, had two or more fractures due to minimal trauma, or experienced at least one symptomatic new fracture after at least 12-month continuous therapy
- Administered (Subcutaneous 20µg daily (intermittent stimulation)
Teriparatide Side Effects
- Dizziness and Leg cramps.
- Nausea and Headache.
- Can cause Transient hypercalcaemia
- Can lead to increased Mild levels of uric acid and the risk osteogenic sarcoma.
Abaloparatide
- Agonist at the PTH1 receptor(PTH1R) , with a anabolic action.
Abaloparatide Action
- Increases bone formation by osteoblasts.
- Reduced bone resorption by an unknown mechanism?
Abaloparatide Use
- Patients with a very high risk that cannot respond to other drugs
- once-daily 80µg subcutaneous injection for 18 months then switch to antiresorptive
Abaloparatide Side Effects
- hypercalciuria and dizziness.
- Nausea,palpitations, headace and fatigue
- Risk osteosarcoma .
Dosing and Fracture Risk Reduction
- Alendronate:47%reduction of fracture (spine). Given 35-70mg weekly, orally
- Risedronate: 41% reduction of fracture(spine). Given150mg monthly, orally
- Zoledronic acid: 70% reduction of fracture(spine). Given 5 mg Yearly, intravenously
- Denosumab:68% reduction of fracture(spine). Given anti-resorptive therapy, subcutaneously
- Raloxifene: 35-42%reduction of fracture(spine). Given orally
- Abaloparatide: 86% reduction of fracture(spine). Given 80ug daily,subcutaneously
- Teriparatide: 66% reduction of fracture(spine). Given 20ug daily,subcutaneously
- Romosozumab: Given 210 subcutaneous injection
Current Anti-resorptive vs Anabolic Therapies
-
Anti-resorptives are administered late, resulting in osteopenic/osteoporotic . Leads to :poor compliance and Atypical Subtrochanteric femoral fractures(AFF) and Osteonecrosis of the Jaw (ONJ
-
Anabolics are Expensive, leads to Invasive daily subcutaneous injections , fracture efficacy gets limited after and anti-resorptive cycle. Poses risks with osteosarcoma.
New Therapies: Anti-Sclerostin
- Sclerostin : a SOST gene used in to inhibit canonical Wnt signalling
- Wnt signally pathway in osteoblasts : is responsible for bone formation and sensitive to Osteocytes
Romosozumab
- Humanised monoclonal antibody
- EVENITY
- Inhibits the “inhibitor of bone formation”
- Stimulates canonical WNT signalling in osteoblasts
- Increased bone formation and reduced fracture risk
- Used for severe osteoporosis with at least 2 fractures
- Administered monthly
- Side Effects from Stroke
Romosozumab Action
- Inhibit Sclerostin, leads to WNT OFF and Bone inhibition
Romosozumab: Dual Action
- Affects bone turnover markers
Calcium and Vitamin D
- Calcium and vitamin D supplements should not be used routinely in non-institutionalised elderly people
- The absolute benefit of calcium and vitamin D supplements in terms of fracture reduction is low
- They are beneficial in people at risk of deficiency, particularly institutionalised individuals
- Calcium and vitamin D supplements are beneficial to people taking osteoporosis treatments if their dietary calcium intake is <1300 mg per day
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