Information about ABALOPARATIDE
Abaloparatide is a synthetic peptide used for the treatment of severe osteoporosis, postmenopausal osteoporosis, and increased fracture risk.
Active ingredients: Abaloparatide (34 amino acid peptide)
Therapeutic category: Hormonal preparation, Bone anabolic agent
Chemical structure: Peptide with 41% homology to parathyroid hormone and 76% homology to PTHrP(1-34) peptide
Mechanism of action: Abaloparatide acts as an activator of the PTH1 receptor, stimulating the formation of new bone in both trabecular and cortical bone. It promotes osteoblastic activity while causing limited and transient increases in bone resorption, leading to increased bone density.
History of the drug
Abaloparatide was developed as an alternative treatment to teriparatide for osteoporosis management. According to research by Yang et al., abaloparatide is the second anabolic drug made available for osteoporosis treatment. The drug is specifically designed to selectively mimic the beneficial actions of parathyroid hormone on bones while minimizing adverse effects associated with excessive PTH1 receptor stimulation.
The clinical development of the drug included extensive studies evaluating its efficacy and safety in the treatment of postmenopausal osteoporosis, with a particular focus on reducing fracture risk.
Instructions for Use/Indications for ABALOPARATIDE (Abaloparatide)
Abaloparatide is administered subcutaneously once daily at a dose of 80 micrograms. It is recommended to administer it at the same time each day. The duration of treatment should not exceed 24 months, as there is insufficient data for longer use.
Main indications:
- Treatment of severe postmenopausal osteoporosis
- Reduction of vertebral and non-vertebral fracture risk
- Increase in bone density in women at high fracture risk
Contraindications and Precautions
Absolute contraindications:
- Pre-existing hypercalcemia
- Severe renal impairment
- Metabolic bone diseases
- Unexplained increase in alkaline phosphatase
- Previous radiation therapy to bones
- Skeletal malignancies
Relative contraindications:
- Active or recent urolithiasis
- Cardiovascular diseases
- Orthostatic hypotension
Special warnings for the elderly, children, and pregnant women
Elderly:
No dosage adjustment is required for elderly patients. However, careful monitoring of renal function and calcium levels is recommended.
Children and adolescents:
Safety and efficacy in individuals under 18 years of age have not been established. Use in pediatric patients is not recommended.
Pregnancy and breastfeeding:
Use during pregnancy and breastfeeding is contraindicated. Women of childbearing potential should use effective contraception during treatment.
As found in a study by Lewiecki et al., the administration of abaloparatide via a transdermal system offers an alternative route of administration with comparable efficacy.
Dosage and administration
The recommended dosage of abaloparatide is 80 micrograms subcutaneously once daily. The injection should be administered in the lower abdominal area. The injection site should be rotated daily to avoid local reactions.
According to a comprehensive analysis by Xu et al., the systematic administration of the recommended dose shows optimal results in reducing fracture risk.
What to do if I miss a dose of abaloparatide?
If a dose is missed, it should be administered as soon as possible within 12 hours of the scheduled administration time. If more than 12 hours have passed, the dose should be skipped, and the next dose should be administered the following day as usual. Two doses should not be administered on the same day to make up for the missed dose.
Overdose
In case of overdose, symptoms such as:
- Nausea and vomiting
- Dizziness and headache
- Hypercalcemia
- Orthostatic hypotension
Immediate medical monitoring and supportive treatment are required. Monitoring of serum calcium levels and appropriate hydration are recommended.
Side effects
Common side effects (>1/100):
- Redness and pain at the injection site
- Dizziness and headache
- Nausea
- Palpitations
- Fatigue
Less common side effects (1/100 to 1/1000):
- Hypercalcemia
- Tachycardia
- Musculoskeletal pain
- Arthralgia
Rare side effects (<1/1000):
- Severe allergic reactions
- Nephrolithiasis
- Severe hypotension
Interactions
Understanding the interactions of abaloparatide with other drugs and foods is vital for safe and effective treatment. Sahbani et al. documented the particular importance of monitoring calcium levels during treatment, as abaloparatide can affect calcium homeostasis in the body.
Drug-drug interactions
Abaloparatide requires special attention when co-administered with digoxin or other cardiotonic glycosides, as it may affect serum calcium levels. Regular monitoring of calcium levels and renal function is required. Concurrent administration with diuretics may increase the risk of hypercalcemia and requires careful monitoring. As noted in a study by Marino et al., co-administration with other drugs affecting calcium metabolism needs special attention.
Drug-food interactions
The absorption of abaloparatide is not significantly affected by food, but it is recommended to take it at a consistent time of day, preferably in the morning. Adequate intake of calcium and vitamin D through diet is essential for the optimal effectiveness of the drug. Excessive consumption of alcohol and caffeine should be avoided, as they may negatively affect bone density. Adequate protein intake is also important for the optimal action of the drug in bone remodeling.
Additional important information
Abaloparatide represents a significant advancement in osteoporosis treatment, with a unique mechanism of action that differentiates it from conventional therapies. Its selective action on PTH1R receptors offers an improved safety and efficacy profile.
Development of resistance
No development of resistance to abaloparatide has been observed over time. However, as highlighted in research by the Ebina et al. laboratory, the effectiveness of the drug may decrease after prolonged use, leading to the recommendation to limit treatment to 24 months.
Preclinical and Clinical Studies
Extensive research data support the efficacy of abaloparatide. In studies conducted under the supervision of Pan et al., the drug’s ability to protect against bone mass loss under conditions of reduced mechanical loading was demonstrated. Additionally, data from the Ozgurel et al. team confirmed the superiority of abaloparatide in restoring bone mass compared to other therapeutic options.
Post-marketing studies, Pharmacovigilance, and Pharmacokinetic characteristics
The pharmacokinetic characteristics of abaloparatide include rapid absorption after subcutaneous administration, with peak plasma concentration within 30-60 minutes. The drug’s bioavailability is approximately 40%, with a half-life of about 1-2 hours. The pharmacovigilance system has recorded minimal serious adverse events, confirming the drug’s good safety profile in clinical practice.
Preclinical and Clinical Studies
Preclinical studies of abaloparatide extensively investigated its effect on bone metabolism and bone density. The results showed a significant increase in bone mass and improvement in bone microarchitecture. The mechanism of action was studied at the cellular level, revealing the selective activation of osteoblasts and the promotion of bone remodeling. The research team of Wang et al. found that abaloparatide maintains normal blood calcium levels through the vitamin D and osteocalcin signaling pathway.
Post-marketing studies, Pharmacovigilance, and Pharmacokinetic characteristics
Post-marketing studies have confirmed the favorable safety profile of abaloparatide in clinical practice. As found by the Recknor et al. team, the use of transdermal delivery systems shows comparable efficacy to subcutaneous administration. The pharmacokinetic characteristics include linear pharmacokinetics within the therapeutic dose range, with rapid clearance from circulation and minimal tissue accumulation. The pharmacovigilance system has recorded a limited number of serious adverse events, mainly related to cardiovascular system disorders and calcium metabolism.
Comparative effectiveness
The comparative evaluation of the effectiveness of abaloparatide with other therapeutic options has demonstrated its superiority in specific areas. Laboratory findings by Zhu et al. indicate significant improvement in bone density and reduction in vertebral fracture risk. The McAndrews et al. team highlighted the increased effectiveness of abaloparatide in restoring bone mass compared to teriparatide.
Systematic reviews and meta-analyses
Systematic reviews have confirmed the safety and efficacy of abaloparatide in the treatment of postmenopausal osteoporosis. According to the meta-analysis by Czerwinski et al., a significant reduction in fracture risk and improvement in bone density at multiple anatomical sites were observed.
Current research directions and future prospects
Research continues to optimize the administration of abaloparatide and develop new delivery forms. The exploration of alternative delivery routes, such as transdermal systems, promises improved patient compliance. Additionally, the potential for combination therapy with other agents to enhance effectiveness in osteoporosis treatment is being studied.
Summary
The active substance abaloparatide (Abaloparatide) is a therapeutic option for the management of severe postmenopausal osteoporosis when fracture risk is increased. It is administered subcutaneously at a dose of 80 micrograms daily, with a maximum treatment duration of 24 months. It is contraindicated in cases of hypercalcemia, severe renal impairment, and in patients with skeletal malignancies. The most common adverse effects include local reactions at the injection site, dizziness, nausea, and arthralgia. Regular monitoring of calcium levels and renal function is required during treatment.
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WARNING: Never take medication without consulting a doctor. Always read the medication leaflet. This encyclopedic article refers to the specific active substance and does not replace the instructions of your doctor or pharmacist.
Bibliography
- Clinical effects of teriparatide, abaloparatide, and romosozumab in postmenopausal osteoporosis. K Ebina, Y Etani, T Noguchi, K Nakata. Journal of Bone and Mineral Metabolism, 2024.
- Efficacy and safety of transdermal Abaloparatide in postmenopausal women with osteoporosis: a randomized study. EM Lewiecki, E Czerwinski, C Recknor. Journal of Bone and Mineral Research, 2023.
- Abaloparatide maintains normal rat blood calcium level in part via 1, 25-dihydroxyvitamin D/osteocalcin signaling pathway. Y Yang, WJ Tseng, B Wang. Endocrinology, 2023.
- Abaloparatide is more potent than teriparatide in restoring bone mass and strength in type 1 diabetic male mice. S Marino, SU Ozgurel, K McAndrews, M Cregor. Bone, 2024.
- Abaloparatide prevents immobilization‐induced cortical but not trabecular bone loss after spinal cord injury. K Sahbani, J Pan, M Zaidi, CP Cardozo. The FASEB Journal, 2023.
- The safety and efficacy of abaloparatide on postmenopausal osteoporosis: a systematic review and meta-analysis. F Xu, Y Wang, X Zhu. Clinical Therapeutics, 2024.
