solution for SC injection
Dosage Forms & Strengths
80mcg/40mcL (available as a prefilled pen that delivers 30 daily doses of 80mcg)
Osteoporosis
Indicated for the treatment of postmenopausal women with osteoporosis at high risk for fracture, defined as a history of osteoporotic fracture, multiple risk factors for fracture, or patients who have failed or are intolerant to other available osteoporosis therapy
In postmenopausal women with osteoporosis, clinical trials showed abaloparatide reduces the risk of vertebral fractures and nonvertebral fractures
80 mcg SC qDay
Cumulative use of abaloparatide and parathyroid hormone (PTH) analogs for >2 yr not recommended (see Dosing Considerations and Black Box Warnings)
Patients should receive supplemental calcium and vitamin D if dietary intake is inadequate
Dosing Considerations
Limitations of use: Because of the unknown relevance of the rodent osteosarcoma findings to humans, cumulative use of abaloparatide and PTH analogs (eg, teriparatide) for >2 yr during a patient’s lifetime is not recommended
Adverse Effects
>10%
Injection site redness (58%)
Hypercalciuria (11%)
1-10%
Dizziness (10%)
Injection site edema (10%)
Nausea (8%)
Headache (8%)
Palpitations (5%)
Orthostatic hypotension (4%)
Fatigue (3%)
Upper abdominal pain (3%)
Hypercalcemia (3%)
Vertigo (2%)
Tachycardia (2%)
Black Box Warnings
Abaloparatide caused a dose-dependent increase in the incidence of osteosarcoma (a malignant bone tumor) in male and female rats; this effect was observed at systemic exposures to abaloparatide ranging from 4-28 times the exposure in humans receiving the 80-mcg dose
It is unknown if abaloparatide causes osteosarcoma in humans
Use is not recommended in patients at increased risk of osteosarcoma, including those with Paget disease of bone or unexplained elevations of alkaline phosphatase, open epiphyses, bone metastases or skeletal malignancies, hereditary disorders predisposing to osteosarcoma, or prior external beam or implant radiation therapy involving the skeleton
Cumulative use of abaloparatide and PTH analogs (eg, teriparatide) for >2 yr during a patient’s lifetime is not recommended
Cautions
Dose-dependent increase in incidence of osteosarcoma in rats observed (see Black Box Warnings)
May cause orthostatic hypotension, typically within 4 hr after injection; instruct patient to sit or lie down for the first several doses if necessary
May cause hypercalcemia; not recommended with preexisting hypercalcemia or in patients who have an underlying hypercalcemic disorder (eg, primary hyperparathyroidism) because of the possibility of exacerbating hypercalcemia
May cause hypercalciuria; unknown whether the drug may exacerbate urolithiasis in patients with active or a history of urolithiasis; if active urolithiasis or preexisting hypercalciuria is suspected, measurement of urinary calcium excretion should be considered
Pregnancy
Not indicated for females of reproductive potential
Lactation
Not indicated for females of reproductive potential
Pregnancy Category Definitions
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
Mechanism of Action
Synthetic peptide analog of human parathyroid hormone-related protein (hPTHrP); hPTHrP is a naturally occurring hormone that, among other functions, regulates bone formation
Elicits anabolic effect on bone, demonstrated by increases in bone mineral density and content that correlated with increases in bone strength at vertebral and/or nonvertebral sites
Absolute bioavailability: 36%
Absorption
Peak plasma time: 0.51 hr
Peak plasma concentration: 312 pg/mL
AUC: 1622 pg·hr/mL
Distribution
Protein bound: 70%
Vd: ~50 L
Metabolism
No specific metabolism or excretion studies have been performed
Metabolism is consistent with nonspecific proteolytic degradation into smaller peptide fragments, followed by elimination by renal clearance
Elimination
Half-life: 1.7 hr
Excretion: Primarily in urine
SC Preparation
Clear and colorless solution
Visually inspect for particulate matter and discoloration prior to administration
Do not use if solid particles appear or if the solution is cloudy or colored
Provide appropriate training and instruction to patients and caregivers on the proper use of the pen
SC Administration
Administer as a SC injection into the periumbilical region of the abdomen
Rotate the site of the injection every day and administer at approximately the same time every day
Do not administer IV or IM
Administer the first several doses where the patient can sit or lie down if necessary, in case symptoms of orthostatic hypotension occur
Before first use: Refrigerate between 2-8°C (36-46°F)
Storage
After first use: Store for up to 30 days at 20-25°C (68-77°F)
Do not freeze or subject to heat
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