Abaloparatide is an analog of human Parathyroid hormone-related peptide that activates the Parathyroid hormone receptors and activates osteoblasts. It is therefore used to increase bone mass in patients with osteoporosis. It is approved for the treatment of osteoporosis in postmenopausal osteoporosis who are at high risk for fracture. In clinical trials, it demonstrated significant reductions in both vertebral and non-vertebral fractures High-risk patients include:
- Patients with a history of osteoporotic fracture
- Those with multiple risk factors for fracture
- Patients who have failed to respond adequately to other therapies or are intolerant to other therapies.
Note: Use of Abaloparatide for more than 2 years is not recommended.
Contraindicatiob to Abaloparatide
There are no contraindications mentioned in the manufacturers labeling.
Warnings and precautions:
- Patients with hypercalcemia should avoid its use. Furthermore, normocalcemic patients should monitor their calcium levels as it can cause a rise in calcium levels.
- It may cause orthostatic hypotension within 4 hours of administration of the drug.
- Osteosarcoma (US Boxed warning): Abaloparatide use has been associated with an increased risk of developing osteosarcoma especially when used for a longer duration (>2 years) and in those at risk of developing osteosarcoma ( Paget's disease, Bone metastasis, skeletal malignancies, prior radiation and in those with open epiphysis).
- The risk of urolithiasis is increased as it may cause hypercalciuria
Note: Prolonged use i.e. more than 2 years of a patient's lifetime is not recommended.
Abaloparatide Dose in Adults
Abaloparatide dose in postmenopausal females with osteoporosis:
- 80 mcg subcutaneously once daily (should not be used for more than 2 years)
Abaloparatide Dose in Childrens
Not recommended for use in children
Abaloparatide Dose in Renal Disease:
No dose adjustment is required in kidney disease patients
Abaloparatide Dose in Liver Disease:
The manufacturer has not provided any dose adjustment in patients with liver disease
How to Adminisrter Abaloparatide?
- It should be injected into the skin like insulin injections around the umbilicus.
- It should be injected at the same time of the day and the site of injections should be rotated.
- The patient should be asked to sit or lie down for some time if he/ she develops blackouts or orthostasis.
Pregnancy Risk Factor D
It is not indicated for pregnant females. It should be avoided by breastfeeding women. It is not known if it can be absorbed into breast milk.
Common side effects of Abaloparatide:
- Hyperuricemia
- Hypercalciuria
- Antibody formation
- Redness at the injection site
Uncommon side effects:
- Cardiovascular side effects: Palpitation, orthostatic hypotension, and tachycardia
- CNS side effects: Dizziness, headache, and fatigue
- Endocrine: Hypercalcemia
- Gastrointestinal side effects: Nausea and abdominal pain
- Local injection site side effects: Swelling and pain at the injection site
Monitor:
- Blood Pressure (orthostatic hypotension)
- Calcium levels and urinary calcium levels
- Bone mineral density, and
- Biochemical markers of bone turn over
Mechanism of action of Abalaoparatide:
- It is an analog to human Parathyroid hormone-related Peptide that stimulates osteoblasts and increases bone mineral density.
Protein binding: 70%
Metabolism is via the liver
Half-life elimination is 1.7 hours Time to peak action is 0.51 hours
International Brands of Abaloparatide:
Pricing: US
- Solution Pen-injector (Tymlos Subcutaneous):
Brands:
Tymlos injection
Abaloparatide Brands in Pakistan:
It is not available in Pakistan