Clodronic acid

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Clodronic acid
Clodronic acid.png
Clinical data
AHFS/Drugs.com International Drug Names
ATC code
Legal status
Legal status
Identifiers
  • (Dichloro-phosphono-methyl)phosphonic acid
CAS Number
PubChem CID
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KEGG
ChEBI
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ECHA InfoCard 100.031.090 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula CH4Cl2O6P2
Molar mass 244.88 g·mol−1
3D model (JSmol)
  • ClC(Cl)(P(=O)(O)O)P(=O)(O)O
  • InChI=1S/CH4Cl2O6P2/c2-1(3,10(4,5)6)11(7,8)9/h(H2,4,5,6)(H2,7,8,9) Yes check.svgY
  • Key:ACSIXWWBWUQEHA-UHFFFAOYSA-N Yes check.svgY
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Clodronic acid (INN) or clodronate disodium (Na2CH2Cl2O6P2) (USAN) is a first generation (non-nitrogenous) bisphosphonate. It is an anti-osteoporotic drug approved for the prevention and treatment of osteoporosis in post-menopausal women and men to reduce vertebral fractures, hyperparathyroidism, hypercalcemia in malignancy, multiple myeloma and fracture related pain because of its anti-inflammatory effects shown as a reduction in inflammatory markers like IL-1β, IL-6, and TNF-α. [1]

Contents

Medical uses

A study comparing the analgesic effect of clodronic acid versus acetaminophen in osteoporotic vertebral fractures showed that clodronic acid provided more analgesia than 3 grams/day of acetaminophen. [2]

Clodronic acid is also used in experimental medicine to selectively deplete macrophages.

Clodronic acid is approved for human use in Canada and Australia, the United Kingdom, where it is marketed as Bonefos, Loron, Clodron and in Italy as Clasteon, Difosfonal, Osteostab and several generics. In other countries is prescribed as a bone resorption inhibitor and antihypercalcemic agent. It is not approved for use in the United States, because it has too many adverse effects.

Veterinary uses

Clodronic acid is approved for use in horses under the trade name Osphos, for treatment of bone resorptive processes of navicular syndrome. It is given by intramuscular injection at one point in time, with the total dose divided into 2-3 sites on the horse. Clinical effects (e.g. improvement of lameness) after a single treatment can be seen up to 6 months post-treatment.

Adverse effects

Clodronic acid has been shown to have several adverse effects. These include: [3]

Related Research Articles

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<span class="mw-page-title-main">Strontium ranelate</span> Chemical compound

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<span class="mw-page-title-main">Tiludronic acid</span> Chemical compound

Tiludronic acid is a bisphosphonate used for treatment of Paget's disease of bone in human being medicine. It has the tradename Skelid. In veterinary medicine, tiludronic acid is used to treat navicular disease and bone spavin in horses. Its tradenames are Tildren and Equidronate. It is approved for treatment of navicular disease and distal, tarsal osteoarthritis in Europe, and was approved for treatment of navicular disease in the United States in 2014.

<span class="mw-page-title-main">Meclofenamic acid</span> Chemical compound

Meclofenamic acid is a drug used for joint, muscular pain, arthritis and dysmenorrhea. It is a member of the anthranilic acid derivatives class of nonsteroidal anti-inflammatory drugs (NSAIDs) and was approved by the US FDA in 1980. Like other members of the class, it is a cyclooxygenase (COX) inhibitor, preventing the formation of prostaglandins.

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The treatment of equine lameness is a complex subject. Lameness in horses has a variety of causes, and treatment must be tailored to the type and degree of injury, as well as the financial capabilities of the owner. Treatment may be applied locally, systemically, or intralesionally, and the strategy for treatment may change as healing progresses. The end goal is to reduce the pain and inflammation associated with injury, to encourage the injured tissue to heal with normal structure and function, and to ultimately return the horse to the highest level of performance possible following recovery.

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References

  1. Pennanen N, Lapinjoki S, Urtti A, Mönkkönen J (June 1995). "Effect of liposomal and free bisphosphonates on the IL-1 beta, IL-6 and TNF alpha secretion from RAW 264 cells in vitro". Pharmaceutical Research. 12 (6): 916–22. doi:10.1023/A:1016281608773. PMID   7667201. S2CID   46332840.
  2. Rovetta G, Monteforte P, Balestra V (2000). "Intravenous clodronate for acute pain induced by osteoporotic vertebral fracture". Drugs Under Experimental and Clinical Research. 26 (1): 25–30. PMID   10761534.
  3. U.S. Food and Drug Administration. "FDA Provides Equine Veterinarians with Important Information about TILDREN and OSPHOS for Navicular Syndrome in Horses". Food and Drug Administration . Retrieved 3 January 2015.