Ostepam

Ostepam Uses, Dosage, Side Effects, Food Interaction and all others data.

Ostepam is a second generation, nitrogen containing bisphosphonate similar to neridronic acid and alendronic acid. Ostepam was first described in the literature in 1977. The second generation bisphosphonates are less common as third generation bisphosphonates, such as ibandronic acid, zoledronic acid, minodronic acid, and risedronic acid are becoming more popular.

Ostepam was granted FDA approval on 31 October 1991.

Ostepam is a second generation, nitrogen containing bisphosphonate that inhibits osteoclast mediated bone loss It has a wide therapeutic index and a long duration of action as it can be given every 3-4 weeks for certain indications. Patients should be counselled regarding the risk of elevated blood urea nitrogen, renal tubular necrosis, and nephrotoxicity.

Trade Name Ostepam
Generic Pamidronic acid
Pamidronic acid Other Names Acide pamidronique, Acido pamidronico, Acidum pamidronicum, Pamidronate, Pamidronic acid
Type
Formula C3H11NO7P2
Weight Average: 235.0695
Monoisotopic: 235.001074735
Protein binding

Pamidronate is approximately 54% protein bound in serum.

Groups Approved
Therapeutic Class
Manufacturer
Available Country France, Tunisia
Last Updated: September 19, 2023 at 7:00 am
Ostepam
Ostepam

Uses

Ostepam is a bisphosphonate used to treat Paget's disease, to treat hypercalcemia of malignancy, and to treat osteolytic bone lesions.

Pamidronate is indicated to treat moderate to severe hypercalcemia of malignancy, moderate to severe Paget's disease of bone, osteolytic bone metastases of breast cancer, and osteolytic lesions of multiple myeloma.

Ostepam is also used to associated treatment for these conditions: Hypercalcemia of Malignancy, Osteolytic lesion, Paget’s Disease, Osteolytic Bone metastases

How Ostepam works

Bisphosphonates are taken into the bone where they bind to hydroxyapatite. Bone resorption by osteoclasts causes local acidification, releasing the bisphosphonate, which is taken into the osteoclast by fluid-phase endocytosis. Endocytic vesicles become acidified, releasing bisphosphonates into the cytosol of osteoclasts where they act.

Osteoclasts mediate resorption of bone. When osteoclasts bind to bone they form podosomes, ring structures of F-actin. Disruption of the podosomes causes osteoclasts to detach from bones, preventing bone resorption.

Nitrogen containing bisphosphonates such as pamidronate are known to induce apoptosis of hematopoietic tumor cells by inhibiting the components of the mevalonate pathway farnesyl diphosphate synthase, farnesyl diphosphate, and geranylgeranyl diphosphate. These components are essential for post-translational prenylation of GTP-binding proteins like Rap1. The lack of prenylation of these proteins interferes with their function, and in the case of Rap1, leads to apoptosis. pamidronate also activated caspases 3 and 9 which further contribute to apoptosis.

Toxicity

Patients experiencing and overdose may present with hypocalcemia, fever, hypotension, and taste perversion. Overdose can be managed by symptomatic and supportive treatment which may include the administration of steroids and intravenous calcium.

Food Interaction

No interactions found.

Elimination Route

In patients with a creatinine clearance >90mL/min, a 90mg intravenous dose reached a Cmax of 1.92±1.08µg/mL, with a Tmax of 4h, and an AUC of 10.2±6.95µg*h/mL.

In patients with a creatinine clearance 61-90mL/min, a 90mg intravenous dose reached a Cmax of 1.86±0.50µg/mL, with a Tmax of 4h, and an AUC of 10.7—3.91µg*h/mL.[A203264

In patients with a creatinine clearance 30-60mL/min, a 90mg intravenous dose reached a Cmax of 1.84±0.58µg/mL, with a Tmax of 4h, and an AUC of 10.1±3.38µg*h/mL.

In patients with a creatinine clearance max of 1.93±0.53µg/mL, with a Tmax of 4h, and an AUC of 34.0±8.37µg*h/mL.

Half Life

The mean elimination half life of pamidronate is 28±7 hours.

Clearance

The mean total clearance of pamidronate is 107±50mL/min and the mean renal clearance is 49±28mL/min.

Elimination Route

Pamidronate is exclusively eliminated in the urine. By 120 hours after administration, 46±16% of the dose has been eliminated in the urine.

Innovators Monograph

You find simplified version here Ostepam

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0000264
http://classyfire.wishartlab.com/tax_nodes/C0000419
http://classyfire.wishartlab.com/tax_nodes/C0000327
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http://classyfire.wishartlab.com/tax_nodes/C0001302
http://classyfire.wishartlab.com/tax_nodes/C0001852
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0000400
http://classyfire.wishartlab.com/tax_nodes/C0000323
http://classyfire.wishartlab.com/tax_nodes/C0003940
http://classyfire.wishartlab.com/tax_nodes/C0000469
http://classyfire.wishartlab.com/tax_nodes/C0004150
http://www.hmdb.ca/metabolites/HMDB0014427
http://www.genome.jp/dbget-bin/www_bget?drug:D07281
http://www.genome.jp/dbget-bin/www_bget?cpd:C07395
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https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504823
https://www.chemspider.com/Chemical-Structure.4512.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=12581
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=11473
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=7903
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL834
https://zinc.docking.org/substances/ZINC000003812862
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP001416
http://www.pharmgkb.org/drug/PA450767
https://www.ebi.ac.uk/pdbe-srv/pdbechem/chemicalCompound/show/210
http://www.rxlist.com/cgi/generic/aredia.htm
https://www.drugs.com/cdi/pamidronate.html
https://en.wikipedia.org/wiki/Pamidronic_acid
*** Taking medicines without doctor's advice can cause long-term problems.
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