Introduction
Elcatonin acetate, a physicochemically and biologically stable synthetic derivative of calcitonin transformed from eel's calcitonin by changing the S-S bond into the stable C-N bond, is consisting of 31 amino acids with the molecular formula C148H244N42O47, which are widely used for the treatment of osteoporosis in Asia country, such as China and Japan etc. it has been reported that elcatonin acetate suppresses bone resorption through direct action on the calcitonin receptors of osteoclasts and exhibits potent analgesic effects. Therefore, it is effective analgesic for acute and severe back pain secondary to fractures.
Pharmacologic action
When adopted the bone strength, bone cortical amplitude, bone mineral density, bone calcium content and hydroxyproline excretion in urine as indicators, the elcatonin acetate shows preventive effect for the experimental osteoporosis induced by low calcium diet, prednisolone therapy and ovarian extraction (rats, dogs). It inhibits bone resorption in normal young rats and rabbits with carcinoma and decreases the calcium in bone transfer into blood. Elcatonin inhibits intraosseous calcium dissociation induced by various bone resorption promoters in the bone cultures system of rat and mouse.
Function
The elcatonin acetate inhibits the activity and proliferation of osteoclasts and promotes the growth of osteoblasts, which is similar to that of calcitonin. It also can restrain the levels of interleukin-6 (il-6) and tumor necrosis factor- α (TNF- α), and promote the levels of insulin-like growth factor (IGF) -1 and osteocalcin (BGP), which are the key factors for the formation of the bone. Moreover, elcatonin can stimulate the release of corticotropin (ACTH) and β-endorphin from the pituitary gland and directly affect the hypothalamus and achieve the central analgesic effect. What's more, the elcatonin shows effectively prevention effect for bone calcium loss which is a typical symptom in elderly patients with osteoporosis.
Pharmacokinetics and metabolism
The drug effect is more stable in human serum than in vitro, and the residual activity rate can still be preserved by 50% after 3 days of medication, achieving a better therapeutic effect. Moreover, the serum drug concentration of healthy adults reaches the peak 30 minutes after intramuscular injection of ecalcitonin (0.5 μ g/kg) and lasts 120 minutes. The elimination half-life of intramuscular injection is 4.8 hours.
References:
1. Tsukamoto M, Menuki K, Murai T, et al. Elcatonin prevents bone loss caused by skeletal unloading by inhibiting preosteoclast fusion through the unloading-induced high expression of calcitonin receptors in bone marrow cells.[J]. Bone, 2016, 85:70-80.
2. Fujita T, Ohue M, Nakajima M, et al. Comparison of the effects of elcatonin and risedronate on back and knee pain by electroalgometry using fall of skin impedance and quality of life assessment using SF-36.[J]. Journal of Bone & Mineral Metabolism, 2011, 29(5):588-597.
3. Li Y, Xuan M, Wang B, et al. Comparison of parathyroid hormone (1-34) and elcatonin in postmenopausal women with osteoporosis: an 18-month randomized, multicenter controlled trial in China.[J]. Chinese Medical Journal, 2013, 126(3):457-463.
4. Endo N, Fujino K, Doi T, et al. Effect of elcatonin versus nonsteroidal anti-inflammatory medications for acute back pain in patients with osteoporotic vertebral fracture: a multiclinic randomized controlled trial.[J]. Journal of Bone & Mineral Metabolism, 2017:1-10.
5. Hongo M, Miyakoshi N, Kasukawa Y, et al. Additive effect of elcatonin to risedronate for chronic back pain and quality of life in postmenopausal women with osteoporosis: a randomized controlled trial.[J]. Journal of Bone & Mineral Metabolism, 2015, 33(4):432-439.
6. Ji Z, Shi C, Huang S, et al. Elcatonin attenuates disuse osteoporosis after fracture fixation of tubular bone in rats[J]. Journal of Orthopaedic Surgery & Research, 2015, 10(1):103.
7. Tanaka S, Yoshida A, Kono S, et al. Effectiveness of elcatonin for alleviating pain and inhibiting bone resorption in patients with osteoporotic vertebral fractures[J]. Journal of Bone & Mineral Metabolism, 2017, 35(5):544-553.
