Alendros - General Information
Pharmacology of Alendros
Alendros, a second-generation bisphosphonate is the first member of a group of drugs which strengthens bone. Alendros is used to reduce hypercalcemia in tumor-induced bone disease, to treat corticosteroid-induced osteoporosis and Paget's disease, and to prevent osteoporosis in postmenopausal women.
Alendros for patients
Physicians should instruct their patients to read the patient package insert before starting therapy with FOSAMAX and to reread it each time the prescription is renewed. Patients should be instructed to take supplemental calcium and vitamin D, if daily dietary intake is inadequate. Weight-bearing exercise should be considered along with the modification of certain behavioral factors, such as cigarette smoking and/or excessive alcohol consumption, if these factors exist.
Patients should be instructed that the expected benefits of FOSAMAX may only be obtained when it is taken with plain water the first thing upon arising for the day at least 30 minutes before the first food, beverage, or medication of the day. Even dosing with orange juice or coffee has been shown to markedly reduce the absorption of FOSAMAX. To facilitate delivery to the stomach and thus reduce the potential for esophageal irritation patients should be instructed to swallow each tablet of FOSAMAX with a full glass of water (6-8 oz). To facilitate gastric emptying patients should drink at least 2 o (a quarter of a cup) of water after taking FOSAMAX oral solution. Patients should be instructed not to lie down for at least 30 minutes and until after their first food of the day. Patients should not chew or suck on the tablet because of a potential for oropharyngeal ulceration. Patients should be specifically instructed not to take FOSAMAX at bedtime or before arising for the day. Patients should be informed that failure to follow these instructions may increase their risk of esophageal problems. Patients should be instructed that if they develop symptoms of esophageal disease (such as difficulty or pain upon swallowing, retrosternal pain or new or worsening heartburn) they should stop taking FOSAMAX and consult their physician. Patients should be instructed that if they miss a dose of once weekly FOSAMAX, they should take one dose on the morning after they remember. They should not take two doses on the same day but should return to taking one dose once a week, as originally scheduled on their chosen day.
Intravenous ranitidine was shown to double the bioavailability of oral alendronate.
The clinical significance of this increased bioavailability and
whether similar increases will occur in patients given oral H2-antagonists
is unknown; no other specific drug interaction studies were performed.
Products containing calcium and other multivalent cations likely will interfere
with absorption of alendronate.
· Abnormalities of the esophagus which delay esophageal emptying such as stricture or achalasia
· Inability to stand or sit upright for at least 30 minutes
· Patients at increased risk of aspiration should not receive FOSAMAX oral solution.
· Hypersensitivity to any component of this product
Additional information about Alendros
Alendros Indication: For the treatment and prevention of osteoporosis in women and Paget's disease of bone in both men and women.
Mechanism Of Action: The action of Alendros on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Alendros also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate and zoledronate) appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.
Drug Interactions: Not Available
Food Interactions: Take with a full glass of water Take 30-60 minutes before breakfast.
Generic Name: Alendronate
Synonyms: Acide Alendronique [Inn-French]; Acido Alendronico [Inn-Spanish]; Acidum Alendronicum [Inn-Latin]; Alendronate Sodium; Alendronic acid
Drug Category: Antiresorptives; Bisphosphonates; Antihypocalcemic Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Alendronate: Adronat; Alendros; Arendal; Fosamax; Onclast;
Absorption: Relative to an intravenous (IV) reference dose, the mean oral bioavailability of alendronate in women was 0.7% for doses ranging from 5 to 40 mg when administered after an overnight fast and two hours before a standardized breakfast. Oral bioavailability of the 10 mg tablet in men (0.59%) was similar to that in women (0.78%) when administered after an overnight fast and 2 hours before breakfast.
Toxicity (Overdose): Alendronate can damage the esophagus both by toxicity from the medication itself and by nonspecific irritation secondary to contact between the pill and the esophageal mucosa, similar to other cases of "pill esophagitis."
Protein Binding: 78%
Biotransformation: There is no evidence that alendronate is metabolized in humans or animals.
Half Life: >10 years
Dosage Forms of Alendros: Tablet Oral
Chemical IUPAC Name: (4-amino-1-hydroxy-1-phosphonobutyl)phosphonic acid
Chemical Formula: C4H13NO7P2
Alendronate on Wikipedia: http://en.wikipedia.org/wiki/Alendronate
Organisms Affected: Humans and other mammals