Bone Pharm

77問 • 1年前

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Preferred Bisphosphonates for Osteoporosis

Alendronate, Risedronate, Zolendronic Acid

Suffix associated with Bisphosphonates

-dronate

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.

Alendronate, Risedronate, Zoledronic Acid, Etidronate, Ibandronate, Pamidronate

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

Mechanism of Action for Bisphosphonates

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

Alendronate

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.

Zolendronic Acid

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

Alendronate, Risedronate, and Ibandronate

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.

Bisphosphonates

Patients unable to tolerate oral Bisphosphonates receive?

Ibandronate or Zolendronic Acid IV

Contraindications of Bisphosphonates

Avoid with severe renal impairment

Diarrhea, Abdominal and Musculoskeletal Pain are common side effects

Bisphosphonates

Esophagitis and Esophageal Ulcers are common side effects

Alendronate, Risedronate, Ibandronate

ONJ and Atypical Femur Fractures are uncommon adverse effects

Bisphosphonates

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

Bisphosphonates

How much water should you take with Bisphosphonates?

6-8 oz water only

How much water should you take with Risedronate ER?

At least 4 oz of water only

How long should you remain upright after taking Bisphosphonates?

At least 30 minutes

How long should you remain upright with Ibandronate?

At least 60 minutes

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

Alendronate

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

Ibandronate

Bisphosphonate that is taken yearly by IV

Zolendronic Acid

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

5 years

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

3 years

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

Fractures

Drugs that contribute to bone loss

Aluminum antacids, Anticonvulsants (phenytoin), arommatase inhibitors, furosemide, glucocorticoids

Drugs that contribute to bone loss

Heparin, medroxyprogesterone, PPIs, SSRIs, thiazolidinediones, thyroid (excessive)

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

Denosumab

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.

Mechanism of action for Denosumab

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

Common side effects of Denosumab

Adverse effects of Denosumab

ONJ and atypical fractures

How is Denosumab administered?

SQ injection every 6 months

Parathyroid agent that is a recombinant form of human parathyroid hormone

Teriparatide

Analog of parathyroid hormone-related peptide

Abalparatide

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

Mechanism of action of Teriparatide and Abalparatide

Contraindications for Teriparatide and Abalparatide

Patients at risk of osteosarcoma

Hyperuricemia can occur with?

Abalparatide

Injection site reactions, hypercalcemia, and orthostatic hypotension

Adverse drug reactions for Teriparatide and Abalparatide

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

Parathyroid Agents

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

Parathyroid Agents

Monoclonal antibody and inhibitor of Sclerostin

Romosozumab

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.

Romosozumab

Contraindications for Sclerostin Inhibitors

Patients with a history of MI or stroke

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

Romosozumab

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

Romosozumab

SERMs for postmenopausal women with osteoporosis

Raloxifene and Bazedoxifene

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

Mechanism of action for SERMs

Contraindications for SERMs

Patients with a history of DVT and PE

Hot flashes, leg cramps, and increased risk of DVT

Adverse drug effects for SERMs

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

Raloxifene

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

Calcitonin

Rhinitis and injection site reactions are adverse reactions

Calcitonin

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

Calcitonin

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.

Calcitonin

Suffix for Parathyroid Agents

-paratide

Suffix for SERMs

-oxifene

How is Risedronate delayed-release tablet taken?

Immediately after breakfast

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?

Prednisone

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

T-score </= -2.5 or history of fragility fracture

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

Food or other medications greatly impair absorption of 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?

Alendronate

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?

Atypical femur fractures

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

RANKL inhibitor

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

Teriparatide

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

History of multiple vertebral fractures

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?

Zoledronic Acid

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?

Erosive esophagitis

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?

Female gender

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?

Alendronate 70 mg weekly

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?

Denosumab 60 mg SQ every 6 months

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?

Renal disease

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?

Denosumab 60 mg SQ every 6 months

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?

Stair climbing and Running

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?

Vitamin D3 [Calcitriol] 0.5 mcg daily for 8 weeks, then 5,000 IU thereafter

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?

ONJ

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

Atypical fractures

Preferred Bisphosphonates for Osteoporosis

Alendronate, Risedronate, Zolendronic Acid

MPLE

ユーザ名非公開 · 41問 · 13日前

MPLE