abaloparatide (Rx)

>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%)

Postmarketing Reports

Abdominal distension, abdominal pain

Constipation, diarrhea, vomiting

Asthenia, lethargy, malaise

Insomnia

Hypersensitivity and anaphylactic reactions, dyspnea (in the context of allergic reactions)

Pruritus, rash

Generalized pain and pain in bone, joint, back, and extremity

Muscle spasms of the leg and back

Injection site reactions including bruising, hemorrhage, pruritus, and rash

Contraindications

History of systemic hypersensitivity to drug or components of product formulation

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; associated symptoms may include dizziness, palpitations, tachycardia or nausea; instruct patient to sit or lie down for first several doses if necessary; administer where patient can sit or lie down 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 Categories

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.

NA: Information not available.

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

Absorption

Absolute bioavailability: 36%

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

Storage

Before first use: Refrigerate between 2-8°C (36-46°F)

After first use: Store for up to 30 days at 20-25°C (68-77°F)

Do not freeze or subject to heat