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alendronate

 
Dictionary: a·len·dro·nate   (ə-lĕn'drə-nāt') pronunciation
n.
A synthetic drug analogue of pyrophosphate that acts primarily on bone to inhibit its resorption and is used to treat and prevent osteoporosis in postmenopausal women.

[Probably A(MINO) + (buty)l(id)en(e), a bivalent hydrocarbon radical (BUTYL + -ID(E) + -ENE) + (HY)DR(OXY) + (phosph)onate, chemical compound name (PHOSPHON(IUM) + -ATE2).]


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Drug Info: Alendronate
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Brand names: Fosamax®

Chemical formula:



Alendronate oral solution

What is alendronate oral solution?

ALENDRONATE (Fosamax®) reduces calcium loss from bones. It helps prevent bone loss and increases production of normal healthy bone in patients with osteoporosis. It may also be used for other conditions which place someone at risk for bone loss, including after menopause in females or from the long-term use of corticosteroids (like prednisone) in men or women. Generic alendronate oral solution is not yet available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• dental disease
• kidney disease
• low level of blood calcium
• stomach, intestinal, or esophageal problems, like acid-reflux or GERD
• problems swallowing
• vitamin D deficiency
• an unusual or allergic reaction to alendronate, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Follow the directions on the prescription label. Alendronate oral solution is taken once a week. Make sure you take the medicine on the same day every week. Use a specially marked spoon or container to measure the oral solution. Ask your pharmacist if you do not have one; household spoons are not always accurate.

Take alendronate oral solution by mouth in the morning, after you have risen for the day. Swallow the oral solution with 2 fluid ounces (1/4 cup) of plain water first thing in the morning. Do not take the solution with any other type of liquid except plain water. Do not take with orange juice, coffee, or other fluids as these may decrease the absorption of alendronate. Do not eat or drink anything before you take your solution and do not eat breakfast, drink, or take any other medicines for at least 30 minutes after taking alendronate. If you can wait for 2 hours before eating, your body will absorb even more of the medicine. After taking this medicine, remain sitting or standing upright (do not lie down or bend over) for at least 30 minutes. This will help to avoid irritation of your throat and esophagus (tube connecting mouth to stomach). Do not take this medicine at the same time as antacids, calcium, magnesium or iron supplements, or vitamins with minerals; if you take these medications, take them later in the day. Do not take your medicine more often than directed.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What if I miss a dose?

If you miss a your weekly dose of alendronate, take the dose on the morning after you remember. Then return to taking your dose just once a week, as originally scheduled on your regular chosen day of the week. Never take 2 doses of the oral solution on the same day. Do not take double or extra doses.

What drug(s) may interact with alendronate?

• aluminum hydroxide
• antacids
• anti-inflammatory drugs like ibuprofen, naproxen, and others
• aspirin
• calcium supplements
• iron supplements
• magnesium supplements
• parathyroid hormone
teriparatide
• vitamins with minerals

Tell your prescriber or health care professional about all other medicines you are taking including non-prescription medicines. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These can affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking alendronate?

Visit your prescriber or health care professional for regular checks on your progress. Do not stop taking alendronate except on your prescriber's advice. Low blood levels of phosphorus and calcium can occur but usually do not cause serious problems. Your prescriber or health care professional may order regular blood tests to check for these problems.

It is very important to take alendronate with 2 ounces (1/4 cup) of plain water. Do not take with orange juice, coffee, or other fluids as these may decrease the absorption of alendronate. Do not take alendronate with food. Wait at least 30 minutes or longer after taking alendronate before you eat, drink or take other medicines.

Because alendronate may irritate your throat, remain sitting or standing upright for at least 30 minutes after taking alendronate. Do not lie down. Do not bend over while you are sitting, standing, or walking.

If you begin to have pain when swallowing, difficulty swallowing, heartburn or stomach pain, call your prescriber or health care professional right away.

You should make sure you get enough calcium and vitamin D in your diet while you are taking alendronate, unless directed otherwise by your health care provider. Discuss your dietary needs with your health care professional or nutritionist.

If you get bone pain, or a worsening of bone pain, check with your doctor. However, many patients have improvement in their bone pain during and after treatment with alendronate.

If you are taking an antacid, a mineral supplement like calcium or iron, or a vitamin with minerals, wait to take them at least 30 minutes, and preferably 2 hours after you take alendronate. Do not take them at same time.

Limit your time in sunlight or other UV exposure, such as tanning beds, while taking alendronate. Alendronate may cause a rash that is worsened by exposure to the sun.

What side effects might I notice from taking alendronate?

Side effects that you should report to your prescriber or health care professional as soon as possible:
More common
• stomach pain
• heartburn
• pain or difficulty swallowing
Rare or uncommon:
• black or tarry stools
• constant jaw pain, especially burning or cramping
• eye inflammation, pain or change in vision
• skin rash, itching (hives)
• swelling of the lips, arms, legs, face, tongue, or throat
• vomiting
• allergic reactions such as hives, swelling of the face, lips or tongue

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• diarrhea or constipation
• headache
• stomach gas or fullness
• nausea
• changes in taste
• bone, muscle or joint pain
• rash, which may be made worse by prolonged exposure to sunlight

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store at room temperature between 15—30 degrees C (59—86 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Wikipedia: Alendronic acid
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Alendronic acid
Systematic (IUPAC) name
sodium [4-amino-1-hydroxy-1-(hydroxy-oxido-phosphoryl)- butyl]phosphonic acid trihydrate
Identifiers
CAS number 121268-17-5
ATC code M05BA04
PubChem 2088
DrugBank APRD00561
ChemSpider 2004
Chemical data
Formula C4H18NNaO10P2 
Mol. mass 325.124
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 0.6%
Metabolism excreted unchanged
Half life 126 months
Excretion renal
Therapeutic considerations
Pregnancy cat.

C

Legal status

POM (UK), Rx-only (US)

Routes Oral

Alendronic acid (INN) or alendronate sodium (USAN, sold as Fosamax by Merck) is a bisphosphonate drug used for osteoporosis and several other bone diseases. It is marketed alone as well as in combination with vitamin D (2,800 U and 5600 U, under the name Fosamax+D). Merck's U.S. patent on alendronate expired in 2008 and Merck lost a series of appeals to block a generic version of the drug from being certified by the U.S. Food and Drug Administration (FDA).

On February 6, 2008, the US FDA approved the first generic versions of alendronate, which are being marketed by Barr Pharmaceuticals and Teva Pharmaceuticals USA. Teva Pharmaceuticals will make generic alendronate in 5-milligram, 10-milligram, and 40-milligram daily doses, and in 35-milligram and 70-milligram weekly doses, while Barr will make generic alendronate in 70-milligram tablets, which are taken once a week. Teva and Barr have already begun shipping their generic versions of alendronate to stores.[1]

Contents

Pharmacokinetics

As with all potent bisphosphonates, the systemic bioavailability after oral dosing is low, averaging only 0.6–0.7 % in women and in men under fasting conditions. Intake together with meals and beverages other than water further reduces the bioavailability. The absorbed drug rapidly partitions, with approximately 50% binding to the exposed bone surface; the remainder is excreted unchanged by the kidneys. Unlike most drugs, the strong negative charge on the two phosphate moieties limits oral bioavailability, and in turn, the exposure to tissues other than bone is very low. After absorption in the bone, alendronate has an estimated terminal half-life of 10 years.[2]

Pharmacology

Alendronate inhibits osteoclast-mediated bone-resorption. Like all bisphosphonates it is chemically related to inorganic pyrophosphate, the endogenous regulator of bone turnover. Whereas pyrophosphate and the first bisphosphonate, etidronate, are capable of inhibiting both osteoclastic bone resorption as well as the mineralization of the bone newly formed by osteoblasts, alendronate and the other potent N-containing bisphosphonates such as risedronate and ibandronate and zoledronate specifically inhibit bone resorption without any effect on mineralization at pharmacalogically achievable doses. Its inhibition of bone-resorption is dose-dependent and approximately 1,000 times stronger than the equimolar effect of etidronate. Under therapy normal bone tissue develops, and alendronate is deposited in the bone-matrix in pharmacologically inactive form. For optimal action enough calcium and vitamin D are needed in the body in order to promote normal bone development. Hypocalcemia should therefore be corrected before starting therapy.

Clinical data

Treatment of post-menopausal women with Fosamax has demonstrated normalization of the rate of bone turnover, significant increase in BMD (bone mineral density) of the spine, hip, wrist and total body, and significant reductions in the risk of vertebral (spine) fractures, wrist fractures, hip fractures, and all non-vertebral fractures. In the women with the highest risk of fracture (by virtue of pre-existing vertebral fractures) in the Fracture Intervention Trial, treatment with Fosamax 5 mg/day for two years followed by 10 mg/day for the third year (plus calcium and vitamin D) resulted in approximately 50% reductions in fractures of the spine, hip and wrist compared with the control group taking placebos plus calcium and vitamin D.

Uses

  • Prophylaxis and treatment of female osteoporosis
  • Treatment of male osteoporosis
  • Prevention and treatment of corticosteroid-associated osteoporosis together with supplements of calcium and vitamin D
  • Paget's disease

Contraindications and precautions

  • Acute inflammations of the gastrointestinal tract (esophagitis, gastritis, ulcerations)
  • Clinically manifest osteomalacia
  • Certain malformations and malfunctions of the esophagus (strictures, achalasia)
  • Inability to stand, walk, or sit for 30 minutes after oral administration
  • Renal impairment with a creatinine clearance below 30ml/min
  • Hypersensitivity to alendronate or another ingredient
  • Hypocalcemia
  • Pregnancy and breastfeeding
  • Patients below 18 yrs. of age, because no clinical data exists

Side-effects

  • Gastrointestinal tract: ulceration of the esophagus; this may require hospitalization and intensive treatment. Gastric and duodenal ulceration may also occur. December 31, 2008, FDA reported alendronate and related drugs, may carry an increased risk for esophageal cancer.[1]
  • General: infrequent cases of skin rash, rarely manifesting as Stevens-Johnson syndrome and toxic epidermal necrolysis, eye problems (uveitis, scleritis) and generalized muscle, joint, and bone pain [2] (rarely severe) have been seen. In laboratory tests decreased calcium and phosphate values may be obtained but reflect action of the drug and are harmless.
  • Osteonecrosis of the Jaw - Deterioration of the Temporomandibular Joint (TMJ) may occur while on this drug, if dental work of any kind is carried out. Although osteonecrosis is uncommon, it occurs primarily in patients being administered intravenous biphosphonates, with most cases being reported in cancer patients.[citation needed]
  • Neurological: Rare instances of auditory hallucinations and visual disturbances have been associated with alendronate and other bisphosphonates.[3]
  • Bone: reported increases in osteoclast numbers, cellular morphology and nuclear morphology. At this point, it's unclear what these findings mean in the "real world". Right now, we're just learning these nuances. said Dr. James Liu, chairman of the department of obstetrics and gynecology at MacDonald Women's Hospital at Case Medical Center. Whether these findings will signal future problems is an open question said study lead author Dr. Robert S. Weinstein, at Central Arkansas Veterans Healthcare System and a professor of medicine at University of Arkansas for Medical Sciences. [4]

Interactions

  • Milk, diet and drugs containing high amounts of calcium, magnesium or aluminium (antacids): the resorption of alendronate is decreased. At least half an hour should pass after intake of alendronate before taking the supplement or drug.
  • Highly active vitamin D analogues or fluorides: no data is available. Concomitant treatment should be avoided.
  • The additional beneficial effect of HRT (hormone replacement therapy) with estrogens/progestins or raloxifene in postmenopausal women remains to be elucidated, but no interactions have been seen. The combination is therefore possible.
  • Intravenous ranitidine increases the oral bioavailability of alendronate. No clinical consequences are known.
  • The combination of NSAIDs and alendroate may increase the risk of gastric ulcers. Both these drugs have the potential to irritate the upper gastro-intestinal mucosa.

Dosage

  • Prophylaxis of osteoporosis in women: 5-10 mg daily or 35-70 mg weekly.
  • Therapy of osteoporosis in women and men : 10 mg daily or 70 mg weekly.
  • Osteoporosis under corticosteroids: 5-10 mg daily or 35-70 mg weekly in men and premenopausal women or those receiving concomitant HRT. In postmenopausal women not receiving HRT the recommended dose is 10 mg daily or 70 mg weekly.
  • Paget's Disease: 40 mg daily for 6 months.

The drug is to be taken only upon rising for the day with three swallows of water, not to exceed 6-8 oz. Stand, walk or sit and remain fasting for 30-45 minutes afterwards, then eat breakfast. Lying down or reclining prior to eating breakfast may cause gastroesophageal reflux and esophageal irritation. At least 30 minutes should be allowed to pass before meals or other beverages than water are taken in.

On December 31, 2008, a letter in the New England Journal of Medicine, cited a finding by the U.S. Food and Drug Administration that 23 cases of esophageal cancer, possibly linked to the use of the drug, have been seen since Fosamax's 1995 market debut.[3]

Dosage forms

  • Fosamax solution 70 mg/75ml
  • Fosamax tablets 5 mg, 10 mg, 35 mg, 40 mg, and 70 mg

Litigation

By 2000 the FDA had received 139 spontaneous reports through the MedWatch system of osteonecrosis of the jaw (ONJ) in cancer patients treated with intravenous (IV) bisphopshonates, either IV pamidronate (Aredia) or IV zolendronate (Zometa).

At the 2004 ODAC meeting the number of spontaneous reports had increased since 2000, and although almost all of the reports remained in cancer patients treated with one of the IV bisphosphonates 13 of the reports were in patients taking oral alendronate or risedronate, most of which were reported on September 24, 2004, in the Journal of Oral and Maxillofacial Surgery. Although this small number of reports does not remotely indicate causality, given the millions of patients who have been treated with alendronate and risedronate, in order to be cautious the FDA asked the manufacturers of the oral bisphosphonates to issue a warning to health care professionals of the potential that bisphosphonates might increase the risk of ONJ.

Despite the fact that no data links the oral bisphosphonates causally to ONJ, product liability attorneys immediately filed suit maintaining that their claimants' ONJ is a direct result of the use of alendronate. Merck has stated the "underlying cause" of osteonecrosis of the jaw is "uncertain", though it might be triggered by a traumatic event like tooth extraction or oral surgery. As of May 13, 2007, hundreds of cases had been filed against Merck alleging Fosamax-induced ONJ. The first case is set to be tried in late 2008.

Bis-phossy jaw

The term given by scientists to the link between bisphosphonates and jaw necrosis is 'bis-phossy jaw.' This is derived from the 19th-century term phossy jaw, given its name after workers in match factories working with white phosphorus developed osteonecrosis of the jaw.

References

  1. ^ "First Generic Fosamax OK'd by FDA". http://www.rxlist.com/script/main/art.asp?articlekey=87025. Retrieved on 2008-02-21. 
  2. ^ Shinkai, I; Ohta, Y (Jan 1996). "New drugs--reports of new drugs recently approved by the FDA. Alendronate". Bioorganic & medicinal chemistry 4 (1): 3–4. doi:10.1016/0968-0896(96)00042-9. ISSN 0968-0896. PMID 8689235.  edit
  3. ^ http://abcnews.go.com/Health/ActiveAging/story?id=6558069&page=1

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Copyrights:

Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.  Read more
Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Alendronic acid" Read more