Preferred Bisphosphonates for Osteoporosis

Suffix associated with Bisphosphonates

Bisphosphonates that treat post menopausal osteoporosis, osteoporosis in men, glucocorticoid-induced osteoporosis, Paget disease, as well as treatment of bone metastases and hypercalcemia of maligancy.

Bind to hydroxyapatite in decrease Osteoclastic bone resorption causing small increase in bone mass and decrease risk of fractures

A Bisphosphonate that where Beneficial effects increase exponentially over several years of therapy, but discontinuation needs to gradual loss of effects

First Line Therapy for Paget’s Disease r/t high efficacy and once-yearly dosing. Has very high affinity for mineralized bone and decreases bone resorption up to 1 year after a single IV dose.

Bisphosphonates that are dosed daily, weekly, or monthly depending on the drug.

They are cleared rapidly from the plasma (r/t binding of hydroxyapatite). Once bound to bone, they are cleared via kidneys over a period of hours to years.

Patients unable to tolerate oral Bisphosphonates receive?

Contraindications of Bisphosphonates

Diarrhea, Abdominal and Musculoskeletal Pain are common side effects

Esophagitis and Esophageal Ulcers are common side effects

ONJ and Atypical Femur Fractures are uncommon adverse effects

Absorption is poor (<1%) and food and other medications interfere with its absorption

How much water should you take with Bisphosphonates?

How much water should you take with Risedronate ER?

How long should you remain upright after taking Bisphosphonates?

How long should you remain upright with Ibandronate?

Bisphosphonate that is taken orally (daily or weekly); effervescent tab (taken weekly)

Bisphosphonate that is taken orally (monthly); IV (taken every 3 months)

Bisphosphonate that is taken yearly by IV

How many years of Bisphosphonate oral therapy until a drug holiday?

How many years of Bisphosphonate Zolendronic Acid IV therapy until a drug holiday?

Bisphosphonate therapy should not be discontinued in women who are high risk of

Drugs that contribute to bone loss

Drugs that contribute to bone loss

Alternative first line RANKL for postmenopausal osteoporosis, particularly with patients with higher risk of fractures, and osteoporosis in men and glucocorticoid-induced osteoporosis

Monoclonal antibody targets receptor activator of nuclear factor kappa-B ligand (RANKL). By binding to RANKL, it prevents activation of RANK receptors on onsteoclasts, thereby inhibiting osteoclast formation and reducing done resorption.

GI upset, bone pain, increased risk of infection, skin reactions, hypocalcemia

Adverse effects of Denosumab

How is Denosumab administered?

Parathyroid agent that is a recombinant form of human parathyroid hormone

Analog of parathyroid hormone-related peptide

Acts as an agoinist at the parathyroid hormone receptor in stimulation of osteoclastic activity thereby increasing bone formation and strength

Contraindications for Teriparatide and Abalparatide

Hyperuricemia can occur with?

Injection site reactions, hypercalcemia, and orthostatic hypotension

Should be reserved for patients for high risk for fractures and those who have failed or cannot tolerate other osteoporosis therapies

Cumulative therapy should not last more than 2 years, and following therapy another anti-resorptive agent for osteoporosis should be initiated to maintain bone density and prevent loss

Monoclonal antibody and inhibitor of Sclerostin

Binds to Sclerostin (regulator factor that inhibits bone formation) and inhibits it’s action, thereby promoting osteoblast activity and bone formation. Secondry action - to decrease bone resorption.

Contraindications for Sclerostin Inhibitors

Adverse drug effects include arthralgias, headache, and injection site reactions

Indicated for postmenopausal women at high risk of fractures. Two SQ injections are given yearly.

SERMs for postmenopausal women with osteoporosis

Estrogen-like affects on bone and estrogen antagonist, affects on breast and endometrial tissue causing increases in bone density without increasing of endometrial cancer, and decreases risk of invasive breast cancer

Contraindications for SERMs

Hot flashes, leg cramps, and increased risk of DVT

Because it has not been shown to reduce non-vertebral or hip fractures, this drug should be used as an alternative for postmenopausal women who cannot take Bisphosphonates or Denosumab

Peptide secreted by the thyroid gland that binds to osteoclasts inhibits their resorptive activity thereby by reducing bone resorption

Rhinitis and injection site reactions are adverse reactions

Indicated for postmenopausal women who are at least five years postmenopausal but is less effective than other osteoporosis medications

Given intranasally or by injection (IM or SQ). For postmenopausal women who are at least 5 years postmenopausal. Is less effective than other osteoporosis medications, and should only be used if other agents not tolerated or appropriate. Has higher risk of new malignancy with long term use.

Suffix for Parathyroid Agents

Suffix for SERMs

How is Risedronate delayed-release tablet taken?

A 52-year old woman has a history of RA, DM, HTN, and heartburn. Her medications include methotrexate, prednisone, metformin, hydrochlorothiazide, lisiniopril and calcium carbonate. She is worried about the risk of osteoprosis as she approaches menopause. Which of her medications is most likely to contribute to the risk of developing osteoporosis?

What are one of two criteria needed to be met for a diagnosis of osteoporosis?

Which of the following is correct reguarding the pharmacokinetics of the bisphosphonates?

A 56 year old womand who has been diagnosed with postmenopausal ostoeporosis has no history of fractures and no other pertinent medical conditions. Which of the following is most appropriate for the management of her osteoporosis?

A patient has been taking Alendronate for postmenopausal osteoporsis for 5 years with slight increase in bone mineral density and no occurrence of fracures. Risk of which adverse effect might warrant consideration of a drug holiday from Alendronate in this patient?

Which of the following best describes the mechanism of action of Denosumab in the treatment of osteoporosis?

Use of which agent for osteoporosis should be limited to no more than 2 years?

Which of the following characteristics would make a patient the most appropriate candidate for Abaloparatide treatment for postmenopausal osteoporosis?

A 55 year old man is diagnosed with Paget disease. He has no other significant medical history. Which agent would be most appropriate for treatment of Paget disease in this patient?

A 67 year old woman complains of severe back pain and is found to have multiple verterbral fractures related to osteoporosis. The patient has a past medical history of HTN, CKD, and MI 6 months ago. Which of the following would exclude the use of Romosozumab in this patient?

A 55 year old woman with postmenopausal osteoporosis has a past medical history of alcohol use disorder, alcoholic liver disease, erosive esophagitis, and hypothyroidism. Which is the primary reason oral Bisphosphonates should be used with caution in this patient?

45 year old African American woman who was a previous smoker has a BMI of 32 kg/m2. She is currently on a 1 week taper of Prednisone for an asthma flair. She is also taking Lisinopril 20 mg for HTN. Which of the following is associated with the most INCREASED risk for her developing osteoporosis in this patient?

72 y/o woman with a history of vertebral compression fracture and a DEXA T score of -2.7 in the left hip. What is the best initial therapy for this patient?

75 y/o woman with newly diagnosed osteoporosis, being discharged after total hip replacement due to right hip fracture. She has never been medication for osteoporosis. PMH is significant for severe GERD, DVT [20 years ago], atrial fibrillation and family history of breast cancer. Which therapy may offer the MOST benefit in this patient?

68 y/o post menopausal woman with a history of T2DM, CAD, dyslipidemia, GERD, OA of knees, stage 3 CKD. Recent EGD was unremarkable. DEXA scan showed t score of -3 of the left hip. Which of the following precludes the used of a bisphosphonate?

53 y/o woman with history of esophageal stricture—recently treated successfully with dilatation—from longstanding GERD, and vasomotor symptoms of menopause. A recent DEXA showed a T score of -2.5 of the LS spine and -2.6 in the left hip. Which therapy is MOST appropriate?

38 y/o woman who is at a health fair. She asks what she can do to maintain her bone health. Her mum had sever osteoporosis with vertebral fractures, spinal kyphosis, hip fracture and limited mobility. Your patient is 64 inches tall and weighs 115 pounds. She is postmenopausal. Her meds include OCP and a multivitamin daily; her DEXA scan shows a T score of -1.3 and a Z score of -.8. which exercise regimen is going to be most helpful to improve her bone health?

68 y/o man with several risk factors for osteoporosis— cigarette smoking, drinking 3-5 alcoholic drinks/day, low body weight and sedentary lifestyle. Labs reveal a 25 Vitamin D level of 18 mcg. Of the following, what will you recommend?

Higher dose, longer duration of therapy, IV administration, dental extractions or implants, use of glucocorticoids, diabetes, and smoking put patients on bisphosphonates at increased risk for?

Long term use of bisphosphonates put patients at increased risk for?

Preferred Bisphosphonates for Osteoporosis