Pamidronic acid

Last updated
Pamidronic acid
Pamidronic acid.svg
Clinical data
Trade names Aredia, Pamimed, among others
Other namesPamidronate disodium pentahydrate, pamidronate disodium
AHFS/Drugs.com International Drug Names
MedlinePlus a601163
Pregnancy
category
  • AU:B3
Routes of
administration
Intravenous
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability n/a
Protein binding 54%
Metabolism Nil
Elimination half-life 28 ± 7 hours
Excretion Renal
Identifiers
  • (3-amino-1-hydroxypropane-1,1-diyl)bis(phosphonic acid)
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.049.897 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C3H11NO7P2
Molar mass 235.069 g·mol−1
3D model (JSmol)
  • O=P(O)(O)C(O)(CCN)P(=O)(O)O
  • InChI=1S/C3H11NO7P2/c4-2-1-3(5,12(6,7)8)13(9,10)11/h5H,1-2,4H2,(H2,6,7,8)(H2,9,10,11) Yes check.svgY
  • Key:WRUUGTRCQOWXEG-UHFFFAOYSA-N Yes check.svgY
   (verify)

Pamidronic acid or pamidronate disodium or APD (marketed as Aredia among others), is a nitrogen-containing bisphosphonate used to prevent osteoporosis.

Contents

It was patented in 1971 and approved for medical use in 1987. [1]

Medical uses

It is used to prevent bone loss, and treat osteoporosis. It is also used to strengthen bone in Paget's disease, to prevent bone loss due to steroid use, and in certain cancers with high propensity to bone, such as multiple myeloma. Due to its ability to sequester calcium in bone, it is also used to treat high calcium levels. It is also used as an experimental treatment of the bone disorder osteogenesis imperfecta. It has been studied in the treatment of complex regional pain syndrome. [2]

Administration

Intravenous, usually 90 mg monthly. 30 mg, 60 mg, 90 mg and for hospitals, 120 mg vials are available, mixed with mannitol.

Side effects

Common side effects include bone pain, low calcium levels, nausea, and dizziness. Osteonecrosis of the jaw is a rare complication which has been associated with the use of bisphosphonates, including pamidronate. [3]

Pamidronate activates human γδ T cells in vitro and in vivo , which may lead to flu-like symptoms upon administration.

Pharmacology

Relative potency [4]
BisphosphonateRelative potency
Etidronate 1
Tiludronate 10
Pamidronate100
Alendronate 100-500
Ibandronate 500-1000
Risedronate 1000
Zoledronate 5000

Related Research Articles

<span class="mw-page-title-main">Osteoporosis</span> Skeletal disorder

Osteoporosis is a systemic skeletal disorder characterized by low bone mass, micro-architectural deterioration of bone tissue leading to bone sterility, and consequent increase in fracture risk. It is the most common reason for a broken bone among the elderly. Bones that commonly break include the vertebrae in the spine, the bones of the forearm, the wrist, and the hip. Until a broken bone occurs there are typically no symptoms. Bones may weaken to such a degree that a break may occur with minor stress or spontaneously. After the broken bone heals, the person may have chronic pain and a decreased ability to carry out normal activities.

<span class="mw-page-title-main">Phossy jaw</span> Disease caused by phosphorus exposure

Phossy jaw, formally known as phosphorus necrosis of the jaw, was an occupational disease affecting those who worked with white phosphorus without proper safeguards. It was most commonly seen in workers in the matchstick industry in the 19th and early 20th centuries. It was caused by white phosphorus vapor, which destroys the bones of the jaw. Modern occupational hygiene practices have since eliminated the working conditions that caused this disease.

Hypercalcemia, also spelled hypercalcaemia, is a high calcium (Ca2+) level in the blood serum. The normal range is 2.1–2.6 mmol/L (8.8–10.7 mg/dL, 4.3–5.2 mEq/L), with levels greater than 2.6 mmol/L defined as hypercalcemia. Those with a mild increase that has developed slowly typically have no symptoms. In those with greater levels or rapid onset, symptoms may include abdominal pain, bone pain, confusion, depression, weakness, kidney stones or an abnormal heart rhythm including cardiac arrest.

<span class="mw-page-title-main">Bisphosphonate</span> Pharmaceutical drugs for preventing bone loss

Bisphosphonates are a class of drugs that prevent the loss of bone density, used to treat osteoporosis and similar diseases. They are the most commonly prescribed drugs used to treat osteoporosis. They are called bisphosphonates because they have two phosphonate groups. They are thus also called diphosphonates.

<span class="mw-page-title-main">Paget's disease of bone</span> Disease affecting bone remodeling

Paget's disease of bone is a condition involving cellular remodeling and deformity of one or more bones. The affected bones show signs of dysregulated bone remodeling at the microscopic level, specifically excessive bone breakdown and subsequent disorganized new bone formation. These structural changes cause the bone to weaken, which may result in deformity, pain, fracture or arthritis of associated joints.

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

Alendronic acid, sold under the brand name Fosamax among others, is a bisphosphonate medication used to treat osteoporosis and Paget's disease of bone. It is taken by mouth. Use is often recommended together with vitamin D, calcium supplementation, and lifestyle changes.

<span class="mw-page-title-main">Avascular necrosis</span> Death of bone tissue due to interruption of the blood supply

Avascular necrosis (AVN), also called osteonecrosis or bone infarction, is death of bone tissue due to interruption of the blood supply. Early on, there may be no symptoms. Gradually joint pain may develop, which may limit the person's ability to move. Complications may include collapse of the bone or nearby joint surface.

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

Zoledronic acid, also known as zoledronate and sold under the brand name Zometa by Novartis among others, is a medication used to treat a number of bone diseases. These include osteoporosis, high blood calcium due to cancer, bone breakdown due to cancer, Paget's disease of bone and Duchenne muscular dystrophy (DMD). It is given by injection into a vein.

<span class="mw-page-title-main">Osteopenia</span> Medical condition

Osteopenia, known as "low bone mass" or "low bone density", is a condition in which bone mineral density is low. Because their bones are weaker, people with osteopenia may have a higher risk of fractures, and some people may go on to develop osteoporosis. In 2010, 43 million older adults in the US had osteopenia. Unlike osteoporosis, osteopenia does not usually cause symptoms, and losing bone density in itself does not cause pain.

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

Risedronic acid, often used as its sodium salt risedronate sodium, is a bisphosphonate. It slows down the cells which break down bone. It's used to treat or prevent osteoporosis, and treat Paget's disease of bone. It is taken by mouth.

Hypercalciuria is the condition of elevated calcium in the urine. Chronic hypercalciuria may lead to impairment of renal function, nephrocalcinosis, and chronic kidney disease. Patients with hypercalciuria have kidneys that excrete higher levels of calcium than normal, for which there are many possible causes. Calcium may come from one of two paths: through the gut where higher than normal levels of calcium are absorbed by the body or mobilized from stores in the bones. After initial 24 hour urine calcium testing and additional lab testing, a bone density scan (DSX) may be performed to determine if the calcium is being obtained from the bones.

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

Ibandronic acid is a bisphosphonate medication used in the prevention and treatment of osteoporosis and metastasis-associated skeletal fractures in people with cancer. It may also be used to treat hypercalcemia. It is typically formulated as its sodium salt ibandronate sodium.

<span class="mw-page-title-main">Osteonecrosis of the jaw</span> Medical condition

Osteonecrosis of the jaw (ONJ) is a severe bone disease (osteonecrosis) that affects the jaws. Various forms of ONJ have been described since 1861, and a number of causes have been suggested in the literature.

<span class="mw-page-title-main">Denosumab</span> Human monoclonal antibody

Denosumab is a human monoclonal antibody for the treatment of osteoporosis, treatment-induced bone loss, metastases to bone, and giant cell tumor of bone.

Senile osteoporosis has been recently recognized as a geriatric syndrome with a particular pathophysiology. There are different classification of osteoporosis: primary, in which bone loss is a result of aging and secondary, in which bone loss occurs from various clinical and lifestyle factors. Primary, or involuntary osteoporosis, can further be classified into Type I or Type II. Type I refers to postmenopausal osteoporosis and is caused by the deficiency of estrogen. While senile osteoporosis is categorized as an involuntary, Type II, and primary osteoporosis, which affects both men and women over the age of 70 years. It is accompanied by vitamin D deficiency, body's failure to absorb calcium, and increased parathyroid hormone.

<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.

Steroid-induced osteoporosis is osteoporosis arising from the use of glucocorticoids analogous to Cushing's syndrome but involving mainly the axial skeleton. The synthetic glucocorticoid prescription drug prednisone is a main candidate after prolonged intake. Bisphosphonates are beneficial in reducing the risk of vertebral fractures. Some professional guidelines recommend prophylactic calcium and vitamin D supplementation in patients who take the equivalent of more than 30 mg hydrocortisone, especially when this is in excess of three months. The use of thiazide diuretics, and gonadal hormone replacement has also been recommended, with the use of calcitonin, bisphosphonates, sodium fluoride or anabolic steroids also suggested in refractory cases. Alternate day use may not prevent this complication.

<span class="mw-page-title-main">Medication-related osteonecrosis of the jaw</span> Medical condition

Medication-related osteonecrosis of the jaw is progressive death of the jawbone in a person exposed to a medication known to increase the risk of disease, in the absence of a previous radiation treatment. It may lead to surgical complication in the form of impaired wound healing following oral and maxillofacial surgery, periodontal surgery, or endodontic therapy.

<span class="mw-page-title-main">C-terminal telopeptide</span> Chemical compound

The C-terminal telopeptide (CTX), also known as carboxy-terminal collagen crosslinks, is the C-terminal telopeptide of fibrillar collagens such as collagen type I and type II. It is used as a biomarker in the serum to measure the rate of bone turnover. It can be useful in assisting clinicians to determine a patient's nonsurgical treatment response as well as evaluate a patient's risk of developing complications during healing following surgical intervention. The test used to detect the CTX marker is called the Serum CrossLaps, and it is more specific to bone resorption than any other test currently available.

Parish P. Sedghizadeh is a clinician-scientist, and a clinical and surgical oral and maxillofacial pathologist. He is a Professor of Clinical Dentistry, and Section Chair of Diagnostic Sciences in the Division of Periodontology, Diagnostic Sciences & Dental Hygiene at the Herman Ostrow School of Dentistry, University of Southern California. He is also the Director of the Oral Pathology and Radiology Distance Learning Program at the University of Southern California.

References

  1. Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 523. ISBN   9783527607495.
  2. Kubalek I, Fain O, Paries J, Kettaneh A, Thomas M (December 2001). "Treatment of reflex sympathetic dystrophy with pamidronate: 29 cases". Rheumatology. 40 (12): 1394–1397. doi: 10.1093/rheumatology/40.12.1394 . PMID   11752511.
  3. Zarychanski R, Elphee E, Walton P, Johnston J (January 2006). "Osteonecrosis of the jaw associated with pamidronate therapy". American Journal of Hematology. 81 (1): 73–75. doi: 10.1002/ajh.20481 . PMID   16369966. S2CID   11830192.
  4. Tripathi KD (2013-09-30). Essentials of medical pharmacology (Seventh ed.). New Delhi: Jaypee Brothers Medical Publishers Pvt. Limited. ISBN   9789350259375. OCLC   868299888.