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Abaloparatide

Pronunciation

(a bal oh PAR a tide)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Pen-injector, Subcutaneous:

Tymlos: 3120 mcg/1.56 mL (1.56 mL) [contains phenol]

Brand Names: U.S.

  • Tymlos

Pharmacologic Category

  • Parathyroid Hormone Analog

Pharmacology

Abaloparatide is an analog of human parathyroid hormone related peptide (PTHrP[1-34]), which acts as an agonist at the PTH1 receptor (PTH1R). This results in stimulation of osteoblast function and increased bone mass (Harslof 2016; Leder 2017).

Distribution

Vd: ~50 L

Metabolism

Hepatic (nonspecific proteolysis)

Excretion

Urine (as peptide fragments)

Time to Peak

0.51 hours (range: 0.25 to 0.52 hours)

Half-Life Elimination

1.7 hours

Protein Binding

~70%

Special Populations: Renal Function Impairment

Maximum serum concentration increased 1-, 1.3- and 1.4-fold in patients with mild, moderate and severe renal impairment, respectively. AUC increased 1.2-, 1.7- and 2.1-fold in patients with mild, moderate and severe renal impairment, respectively.

Use: Labeled Indications

Osteoporosis: 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.

Limitations of use: Use of abaloparatide and parathyroid hormone analogs for >2 years is not recommended.

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Dosing: Adult

Osteoporosis: SubQ: 80 mcg once daily

Dosing: Geriatric

Refer to adult dosing

Dosing: Renal Impairment

No dosage adjustment necessary.

Dosing: Hepatic Impairment

There is no dosage adjustment provided in the manufacturer's labeling

Administration

Inject subcutaneously 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 intravenously or intramuscularly. Initial doses should occur under circumstances in which the patient may sit or lie down, in the event of orthostasis.

Storage

Store refrigerated at 2°C to 8°C (36°F to 46°F). Do not freeze or heat. After first use, store for up to 30 days at 20°C to 25°C (68°F to 77°F).

Drug Interactions

There are no known significant interactions.

Adverse Reactions

>10%:

Endocrine & metabolic: Increased uric acid (25%)

Genitourinary: Hypercalciuria (11% to 20%)

Immunologic: Antibody development (49%; neutralizing antibodies: 68%; antibody formation was not found to have any clinical significance)

Local: Erythema at injection site (58%)

1% to 10%:

Cardiovascular: Palpitations (5%), orthostatic hypotension (1% to 4%), sinus tachycardia (≤2%), tachycardia (≤2%)

Central nervous system: Dizziness (10%), headache (8%), fatigue (3%)

Endocrine & metabolic: Hypercalcemia (3%)

Gastrointestinal: Nausea (8%), upper abdominal pain (3%)

Local: Swelling at injection site (10%), pain at injection site (9%)

ALERT: U.S. Boxed Warning

Osteosarcoma

Abaloparatide caused a dose-dependent increase in the incidence of osteosarcoma, a malignant bone tumor, in male and female rats. The effect was observed at systemic exposures to abaloparatide ranging from 4 to 28 times the exposure in humans receiving the 80 mcg dose. It is unknown whether abaloparatide will cause osteosarcoma in humans.

Use of abaloparatide is not recommended in patients at increased risk for osteosarcoma including those with Paget's 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 parathyroid hormone analogs (eg, teriparatide) for more than 2 years during a patient's lifetime is not recommended.

Warnings/Precautions

Concerns related to adverse effects:

• Hypercalcemia: May cause or exacerbate hypercalcemia; use is not recommended in patients with preexisting hypercalcemia or with an underlying hypercalcemic disorder (eg, primary hyperparathyroidism).

• Orthostatic hypotension: May cause orthostatic hypotension. Transient orthostatic hypotension usually occurs within 4 hours of dosing.

• Osteosarcoma: [US Boxed Warning]: In animal studies, abaloparatide has been associated with an increase in osteosarcoma; risk was dependent on both dose and duration. Avoid use in patients with an increased risk of osteosarcoma (including Paget disease, bone metastases or skeletal malignancies, hereditary disorders predisposing to osteosarcoma, unexplained elevation of alkaline phosphatase, prior external beam or implant radiation therapy involving the skeleton, or in patients with open epiphyses).

Disease-related concerns:

• Urolithiasis: Use may cause hypercalciuria; use with caution in patients with active or recent urolithiasis because of risk of exacerbation.

Other warnings/precautions:

• Appropriate use: [US Boxed Warning]: Use for >2 years during a patient's lifetime is not recommended.

Monitoring Parameters

Orthostatic hypotension; urinary calcium (patients with suspected active urolithiasis or preexisting hypercalciuria); bone mineral density (BMD) should be evaluated 1 to 2 years after initiating therapy and every 2 years thereafter (NOF [Cosman 2014]); serum calcium; consider measuring biochemical markers of bone turnover

Pregnancy Considerations

Abaloparatide is not indicated for use in women of reproductive potential. Animal reproduction studies have not been conducted.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience headache, loss of strength and energy, abdominal pain, or injection site irritation. Have patient report immediately to prescriber signs of high calcium (weakness, confusion, fatigue, headache, nausea and vomiting, constipation, or bone pain), signs of a kidney stone (back pain, abdominal pain, or hematuria), bone pain, skin edema, lump, persistent pain, severe dizziness, passing out, tachycardia, abnormal heartbeat, severe nausea, vomiting, or painful urination (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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