Abaloparatide

Abaloparatide:

Generic name: abaloparatide
Brand name: Tymlos
Drug class: Parathyroid hormone and analogs
Dosage form: subcutaneous solution (3120 mcg/1.56 mL)
Chemical name: l-Alanyl-l-valyl-l-seryl-l-α-glutamyl-l-histidyl-l-glutaminyl-l-leucyl-l-leucyl-l-histidyl-l-α-aspartyl-l-lysylglycyl-l-lysyl-l-seryl-l-isoleucyl-l-glutaminyl-l-α-aspartyl-l-leucyl-l-arginyl-l-arginyl-l-arginyl-l-α-glutamyl-l-leucyl-l-leucyl-l-α-glutamyl-l-lysyl-l-leucyl-l-leucyl-2-methylalanyl-l-lysyl-l-leucyl-l-histidyl-l-threonyl-l-alaninamide
Molecular formula: C₁₇₄H₃₀₀N₅₆O₄₉
Protein Average Weight: 3961.0 Da
Half-life: 1 hour
CAS number: 247062-33-5

Used for:

It is used to treat postmenopausal women who has high risk of bone fracture (Osteoporosis). It can be also used by men with osteoporosis and to treat people who cannot use another treatment for osteoporosis.

It is a synthetic peptide N-terminal analog of parathyroid hormone-related protein (PTHrP) and an agonist at the parathyroid hormone type 1 (PTH1) receptor. It is a synthetic 34 amino acid peptide with 41% homology to human parathyroid hormone 1-34 and human PTHrP 1-34. Abaloparatide and PTHrP share the first 21 amino acids and the receptor-activating domain. It is an osteoanabolic agent that stimulates bone formation. The mean half-life of abaloparatide is approximately one hour. It was first approved by the FDA on April 28, 2017, for the treatment of osteoporosis in postmenopausal women and is also used to increase bone density in men with osteoporosis. In October 2022, the EMA's Committee for Medicinal Products for Human Use (CHMP) recommended abaloparatide be granted marketing authorization in Europe and the drug was fully authorized by the European Commission on December 19, 2022

Side effects:

Consult your doctor if you have any allergic reactions like

• A light-headed feeling, like you might pass out (may occur within 4 hours after injection)
• Bone pain, unusual body aches, hives
• Difficulty in breathing, swelling of your face, lips, tongue, or throat
• A new or worsening lump or swelling under your skin
• Pounding heartbeats or fluttering in your chest
• High calcium levels--confusion, tiredness, nausea, vomiting, loss of appetite, constipation, increased thirst or urination, weight loss, or
• Signs of a kidney stone--pain in your side or lower back, blood in your urine, painful or difficult urination.

Common Adverse Effects include:

• Osteoporosis in postmenopausal women (≥2%): hypercalciuria, dizziness, nausea, headache, palpitations, fatigue, upper abdominal pain, and vertigo.
• Osteoporosis in men (≥2%): injection site erythema, dizziness, arthralgia, injection site swelling, injection site pain, confusion, nausea, diarrhea, abdominal distension, abdominal pain, and bone pain.

Precautions:

• Avoid use of abaloparatide in patients with increased baseline risk of osteosarcoma Cumulative use of abaloparatide for >2 years during a patient's lifetime not recommended.
• Orthostatic Hypotension may occur, generally within 4 hours of administration. Symptoms may include dizziness, palpitations, tachycardia, or nausea, and may resolve by having the patient recline.
• Not recommended for patients with hypercalcemia and other related disorders because of the possibility of worsening hypercalcemia. It is also not recommended for patients with urolithiasis and hypercalciuria.

Drug Interactions:

Drug interactions may change how your medications work and what products you use which may increase your risk for serious side effects. However, this document does not contain all possible drug interactions. Keep a list of all the products or medications you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

Dosage:

The required dosage for patients with osteoporosis is 80 mcg/day. It is also recommended for the Patients with less/inadequate dietary intake should receive supplemental calcium and vitamin D.

Toxicity:

If the patient is given/taken more dose than original, The patient experiences asthenia, headache, nausea, and vertigo. Serum calcium may be normal or very high. Other symptoms of overdose may include hypercalcemia, nausea, vomiting, dizziness, tachycardia, orthostatic hypotension, and headache. Since there is no specific antidote for abaloparatide overdose, it is recommended that overdose is managed with drug discontinuation, monitoring of serum calcium and phosphorus, and implementation of appropriate supportive measures, such as hydration.