129318-43-0 Usage
Description
Alendronate sodium, also known as Alendros, is the fourth bisphosphonate to reach the market for the treatment of postmenopausal osteoporosis. It is a potent inhibitor of bone resorption, which significantly increases bone mineral density, reduces fracture risk, and is the first-line treatment for osteoporosis. Alendronate sodium is a resorption inhibitor of aminodiphosphonate bone, with a strong affinity for bone hydroxyapatite, allowing it to enter the bone matrix hydroxyapatite crystals. It is released during osteoclast dissolution of crystals, inhibiting osteoclast activity and indirectly exhibiting anti-bone resorption activity through the inhibition of bone resorption by osteoblasts. Alendronate sodium is more potent than other bisphosphonates such as clodronate, pamidronate, and etidronate, and has no deleterious effects on bone. It also reduces hypercalcemia in cancer patients.
Uses
Used in Pharmaceutical Industry:
Alendronate sodium is used as an anti-osteoporosis drug for the treatment of postmenopausal women with osteoporosis, as it significantly increases bone mineral density and reduces fracture risk.
Used in Oncology:
Alendronate sodium is used as a treatment to reduce pain and complications due to bone metastases in cancer patients, as it is a potent inhibitor of bone resorption.
Used in Paget's Disease Treatment:
Alendronate sodium is used as an effective treatment for Paget's disease, a condition characterized by excessive bone resorption and formation, as it inhibits bone resorption and reduces the associated symptoms.
Used in Hypercalcemia Management:
Alendronate sodium is used as a treatment to reduce hypercalcemia in cancer patients, as it has been shown to effectively lower calcium levels in the blood.
Synthesis of Alendronate
It uses gamma-aminobutyric acid (GABA), phosphorous acid, phosphorus trichloride as the raw material and uses the diphenyl ether as the solvent to prepare the alendronic acid, and then alkalesizes to obtain its monosodium salt. The synthesis is shown below:
Image 1: Synthesis of Alendronate sodium
Side effects
After medication tolerance well, a small number of patients can be seen gastrointestinal reactions, such as nausea, abdominal distension, abdominal pain, occasional headache, skeletal muscle pain, rare rash and erythema.
The overview of Alendronate sodium, synthesis, adverse reactions, precautions, etc. is edited by lookchem's Li Jie. (2016-01-22)
Taboo
1.Esophageal motility disorders, such as the disability of esophageal delay and the esophageal stricture are disabled.
2.Severe renal insufficiency is disabled.
3.Osteomalacia is disabled.
4.Allergies with the goods and other bisphosphonates, hypokalemia are disabled.
5.Pregnant, lactating women and children are disabled.
Note
1. At least 30 minutes before breakfast with 200ml warm water delivery; medication at least 30 minutes before eating.
2. Taking with orange juice and coffee at the same time will significantly affect the absorption of the product.
3. In taking this product before and after 30 minutes, drinking milk, dairy products and drinks with more calcium are not allowed. Immediately lying in bed after taking medicine may cause esophageal irritation or ulcerative esophagitis.
4. Gastrointestinal disorders, gastritis, esophageal discomfort, duodenitis, ulcer patients should use this drug with caution.
5, Mild to moderate renal dysfunction in patients should use this drug with caution.
6. Before starting to use this product treatment, calcium metabolism and mineral metabolism disorders, vitamin D deficiency and hypocalcemia must be corrected. Calcium supplements, antacids and some oral agents are likely to hinder the absorption of the product. Therefore, after taking this product, the time should be delayed at least half an hour and then taking other drugs.
7. If the food intake is not enough, all patients with osteoporosis should be added calcium and vitamin D.
Drug interactions
1. Antacids and cathartic agents will often affect the absorption of the drug for containing calcium or other metal ions such as magnesium, iron and so on.
2. Inducing hypocalcemia when in combination with aminoglycosides.
Originator
Istituto Gentili (Italy)
Pharmacokinetics
The second-generation agent alendronate sodium was the first bisphosphonate agent approved by the U.S.
FDA for the prevention and treatment of osteoporosis and Paget's disease of the bone and is 1,000-fold
more potent than etidronate. This derivative, when dosed continuously (5–10 mg/day for osteoporosis and 40
mg/day for Paget's disease) and given with oral calcium supplements (500 mg/day), produced well-mineralized
bone and significantly improved BMD (7% in the spine and 4% in the hip) within 18 months. In addition, the
vertebral fracture rate was shown to decrease by 47%. A side effect associated with alendronate, chemical
esophagitis, has been attributed to inadequate intake of water and lying down after taking the
medication. Specific patient instructions were developed to limit the incidence of upper gastrointestinal
problems and include: 1) taking the medication with 6 to 8 ounces of water on arising in the morning, 2)remaining in an upright position for at least 30 minutes after taking the medication, and 3) delaying drinking
other liquids/eating for at least 30 minutes, if not 1 to 2 hours, to allow maximal absorption of the agent. To
enhance absorption, calcium supplements and any aluminum- or magnesium-containing antacids should be
dosed separately from the agents in this class.
Clinical Use
The second-generation agent alendronate sodium was the first bisphosphonate agent approved by the U.S.
FDA for the prevention and treatment of osteoporosis and Paget's disease of the bone and is 1,000-fold
more potent than etidronate.
Check Digit Verification of cas no
The CAS Registry Mumber 129318-43-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,2,9,3,1 and 8 respectively; the second part has 2 digits, 4 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 129318-43:
(8*1)+(7*2)+(6*9)+(5*3)+(4*1)+(3*8)+(2*4)+(1*3)=130
130 % 10 = 0
So 129318-43-0 is a valid CAS Registry Number.
InChI:InChI=1/C4H13NO7P2.Na/c5-3-1-2-4(6,13(7,8)9)14(10,11)12;/h6H,1-3,5H2,(H2,7,8,9)(H2,10,11,12);/q;+1/p-1
