135459-87-9 Usage
Description
Strontium ranelate, a divalent strontium salt of ranelic acid, has been developed and launched for the treatment of osteoporosis. It enhances pre-osteoblastic cell replication, inhibits pre-osteoclast differentiation, and suppresses the bone-resorbing activity of osteoclasts. Strontium ranelate is supplied in a 2 g sachet and is evenly suspended in water prior to consumption.
Uses
Used in Pharmaceutical Industry:
Strontium ranelate is used as a bone metabolism modulator for inhibiting bone resorption while maintaining bone formation. It is an antiosteoporotic agent, mainly used for the treatment and prevention of osteoporosis in postmenopausal women and significantly reduces the risk of occurrence of vertebral fractures and hip fractures.
Additionally, Strontium ranelate (Protelos) is used as a strontium(II) salt of ranelic acid for (-)-desmethoxyverapamil binding to calcium channels with an IC50 of 0.5 mM.
Drug for the treatment of osteoporosis
Strontium ranelate is a drug for the treatment of osteoporosis with its appearance being white to light yellow powder or crystalline powder. It is odorless and slightly soluble in water but almost insoluble in ethanol and easily soluble in dilute hydrochloric acid. It was first studied and developed by the French Servier Company and had first entered into market in November 2004 in Ireland and entered into market in UK in December of same year. Japan's Fujisawa Pharmaceutical Company has owned the authorization of development, production and marketing right of this product in Japan. It is clinically mainly used for the treatment and prevention of osteoporosis in postmenopausal women with significantly reducing the risk of occurrence of vertebral fractures and hip fractures.
Strontium ranelate has dual pharmacological inhibitory effects of both inhibiting bone absorption and promoting bone formation. On the one hand, in the osteoblast-enriched cells, it can increase the synthesis of collagen and non-collagen proteins and promote the osteoblast-mediated bone formation mediated by osteoblasts through enhancing the proliferation of pre-osteoblast. On the other hand, through decreasing the osteoclast differentiation and reabsorbing activity and further reduction of bone absorption, it achieves the rebalance of bone turnover, further boosting the bone formation.
Strontium ranelate mainly exerts its pharmacological effects through its strontium atoms. Strontium is an alkaline earth metal element which is cognate with calcium and located under the calcium in the element periodic table. Its absorption, distribution, excretion is similar with calcium. After oral administration of 2g, the absolute bioavailability of strontium is 27%. Large doses of strontium cause abnormalities of bone mineral metabolism with low doses of strontium being able to the enhance the pre-osteoblast replication, increasing the number of osteoblasts to stimulate bone formation while reducing the activity of osteoclasts, reducing osteoclast quantity as well as reducing the rate of bone absorption. The results are consistent with the results found in animal and human in vivo studies.
s (OP) is a progressive skeletal disease, characterized by reduced bone mineral density (BMD) and degenerative changes in bone tissue microstructure. It is exhibited as bone fragility and fracture-prone with the latter most commonly happening in the spine, hip and wrist. For women, when after surgical removal of the ovaries or menopause, the body stops producing bone to maintain strong estrogen, thus, primary OP is particularly common in post-menopausal or menopausal women.
There are currently two major kinds of drugs used in the treatment of osteoporosis: one kind includes those drugs that inhibits osteoclast activity and therefore inhibiting bone absorption such as bisphosphonates, estrogen and calcitonin; the second category includes those drugs which promote the osteoblast activity, and thereby stimulating bone formation and there are currently only a product, human recombinant parathyroid hormone 1-34, that has entered into market. It however requires injection with high drug prices.
The above information is edited by the lookchem of Dai Xiongfeng.
Originator
Fujisawa (Japan)
Clinical Use
Treatment of post menopausal osteoporosis and men at
high risk of fractures
Drug interactions
Potentially hazardous interactions with other drugs
Calcium-containing compounds: separate
administration by at least 2 hours.
Antacids: separate administration by at least 2 hours.
Antibiotics: strontium can reduce absorption of oral
tetracycline and quinolones - suspend strontium
therapy during treatment.
Metabolism
Strontium ranelate has a high affinity for bone tissue. It is
not metabolised, and excretion occurs via the kidneys and
gastrointestinal tract.
Check Digit Verification of cas no
The CAS Registry Mumber 135459-87-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,5,4,5 and 9 respectively; the second part has 2 digits, 8 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 135459-87:
(8*1)+(7*3)+(6*5)+(5*4)+(4*5)+(3*9)+(2*8)+(1*7)=149
149 % 10 = 9
So 135459-87-9 is a valid CAS Registry Number.
InChI:InChI=1/C12H10N2O8S.7H2O.2Sr/c13-2-6-5(1-7(15)16)10(12(21)22)23-11(6)14(3-8(17)18)4-9(19)20;;;;;;;;;/h1,3-4H2,(H,15,16)(H,17,18)(H,19,20)(H,21,22);7*1H2;;/q;;;;;;;;2*+2/p-4
