Alendronic Acid + Vitamin D3

Uses

Alendronic Acid & Vitamin D3 is used for:

• is used for the treatment of osteoporosis in postmenopausal women and to increase bonemass in men with osteoporosis. Alendronic Acid & Vitamin D3 alone should not be used to treat vitamin D deficiency.

Alendronic Acid + Vitamin D3 is also used to associated treatment for these conditions: Osteogenesis Imperfecta (OI), Osteoporosis, Osteoporosis caused by glucocorticoid, Paget’s Disease

How Alendronic Acid + Vitamin D3 works

Alendronic acid binds to bone hydroxyapatite. Bone resorption causes local acidification, releasing alendronic acid which is that taken into osteoclasts by fluid-phase endocytosis. Endocytic vesicles are acidified, releasing alendronic acid to the cytosol of osteoclasts where they induce apoptosis. Inhibition of osteoclasts results in decreased bone resorption which is shown through decreased urinary calcium, deoxypyridinoline and cross-linked N-telopeptidases of type I collagen.

Dosage

Alendronic Acid + Vitamin D3 dosage

Treatment of osteoporosis in postmenopausal women: One tablet once weekly.Treatment to increase bonemass in men with osteoporosis: One tablet once weekly.Dosing in elderly and renal insufficiency: No dosage adjustment is necessary for the elderly or for patients with mild-to-moderate renal insufficiency (creatinine clearance 35 to 60 mL/min). Bonemass D is not recommended for patients with more severe renal insufficiency (creatinine clearance <35 mL/min) due to lack of experience.Bonemass D must be taken at least one to half hour before the first food, beverage, or medication of the day with plain water only. Other beverages (including mineral water), food, and some medications are likely to reduce the absorption of Alendronate. To facilitate delivery to the stomach and thus reduce the potential for esophageal irritation, Bonemass D should only be swallowed upon arising for the day with a full glass of water and patients should not lie down for at least 30 minutes and until after their first food of the day. Bonemass D should not be taken at bedtime.

To permit adequate absorption, Alendronate & Colecalciferol must be taken at least 30 minutes before the first food, beverage or medication of the day with plain water only. Other beverages (including mineral water), food and some medications are likely to reduce the absorption of Alendronate. To facilitate delivery to the stomach and thus to reduce the potential for esophageal irritation, Alendronate & Colecalciferol tablet should only be swallowed upon rising for the day with a full glass of water. Patients should not lie down for at least 30 minutes after taking Alendronate until after their first food of the day. Alendronate & Colecalciferol should not be taken at bed time.

Side Effects

The most common side-effect is digestive reactions from Bonemass D. These reactions include irritation, inflammation, or ulcers of the esophagus, which may sometimes bleed. This may occur especially if patients do not drink a full glass of water with Bonemass D or if they lie down in less than 30 minutes or before their first food of the day. Less common side-effects are nausea, vomiting, a full or bloated feeling in the stomach, constipation, diarrhea, black or bloody stools, gas, headache, a changed sense of taste, and bone, muscle, or joint pain.

Toxicity

In clinical studies, ≥3% of patients experience abdominal pain, acid regurgitation, constipation, diarrhea, dyspepsia, musculoskeletal pain, and nausea.

No information for treatment of overdose is available, however patients should be given milk or antacids to bind alendronic acid and vomiting should not be induced. Patients may experience hypocalcemia, hypophosphatemia, and upper gastrointestinal events..

There are currently no studies for safety and efficacy in pregnancy, though studies in pregnant rats show fetal and maternal complications at 4 times the clinical dose and pregnant rabbits do not show complications at as high as 10 times the clincal dose.

Excretion in breast milk, and therefore safety in lactation, is unknown.

Alendronic acid has been studied for use in pediatric patients. The oral bioavailability is similar to that in adult patients, but an increase in the portion of patients experiencing vomiting.

There is no significant difference in efficacy or safety of alendronic acid in geriatric populations, though there is potential for even greater sensitivity in patients at a further advanced age than those in the study.

Alendronic acid is not recommended for patients with creatinine clearance Label.

Precaution

Alendronate Sodium: Hypocalcemia must be corrected before initiating therapy with Bonemass D. Other disorders affecting mineral metabolism (such as vitamin D deficiency) should also be effectively treated. In patients with these conditions, serum calcium and symptoms of hypocalcemia should be monitored during therapy with Bonemass D.

Colecalciferol: Bonemass D alone should not be used to treat vitamin D deficiency. Patients at increased risk for vitamin D insufficiency (e.g. those who are nursing home bound, chronically ill, over the age of 70 years) should receive vitamin D supplementation in addition to that provided in Bonemass D.

Interaction

Calcium supplement, antacids and some oral medications will interfere with absorption of Alendronate if taken at the same time. Intravenous ranitidine makes the bioavailability of oral Alendronate double. Incidence of upper gastro-intestinal adverse events associated with NSAID and aspirin appears to be greater with concomitant administration of Alendronate. Mineral oils, orlistat, and bile acid sequestrants (e.g., cholestyramine, colestipol) may impair the absorption of vitamin D. Anticonvulsants, cimetidine, and thiazides may increase the catabolism of vitamin D.

Volume of Distribution

28L.

Elimination Route

Mean oral bioavailability of alendronic acid in women is 0.64% and in men is 0.59%. Bioavailability of alendronic acid decreases by up to 40% if it is taken within an hour of a meal.

Half Life

Due to alendronic acid being incorporated into the skeleton, the terminal half life is estimated to be over 10 years.

Clearance

71mL/min.

Elimination Route

Administration of radiolabeled alendronic acid results in 50% recovery in urine within 72 hours. No alendronic acid is recovered in the feces. Men excrete less alendronic acid than women, though race and advanced age do not affect elimination.

Pregnancy & Breastfeeding use

There is no studies in pregnant women. should be used during pregnancy only if the potential benefit justifies the potential risk to the mother and fetus. Colecalciferol and some of its active metabolites pass into breast milk. It is not known whether Alendronate is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when it is administered to nursing women. This is not indicated for use in children.

Contraindication

• Abnormalities of the esophagus which delay esophageal emptying, such as stricture or achalasia.
• Inability to stand or sit upright for at least 30 minutes.
• Hypersensitivity to any component of this product.
• Hypocalcaemia.

Special Warning

Dosing in elderly and renal insufficiency: No dosage adjustment is necessary for the elderly or for patients with mild-to-moderate renal insufficiency (creatinine clearance 35 to 60 mL/min). Alendronic Acid + Vitamin D3 (Colecalciferol) is not recommended for patients with more severe renal insufficiency (creatinine clearance<35 mL/min) due to lack of experience.

Acute Overdose

Hypocalcemia, hypophosphatemia, and upper gastrointestinal adverse events, such as upset stomach, heartburn, esophagitis, gastritis, or ulcer, may result from oral overdosage. Signs and symptoms of vitamin D toxicity include hypercalcemia, hypercalciuria, anorexia, nausea, vomiting, polyuria, polydipsia, weakness, and lethargy.

Alendronate Sodium: No specific information is available on the treatment of overdosage with Alendronate. Hypocalcemia, hypophosphatemia, and upper gastrointestinal adverse events, such as upset stomach, heartburn, esophagitis, gastritis, or ulcer, may result from oral overdosage. Milk or Antacids should be given to bind Alendronate. Due to the risk of esophageal irritation, vomiting should not be induced and the patient should remain fully upright.

Colecalciferol: There is limited information regarding overdosage of Colecalciferol associated with acute toxicity. Signs and symptoms of vitamin D toxicity include hypercalcemia, hypercalciuria, anorexia, nausea, vomiting, polyuria, polydipsia, weakness, and lethargy. Serum and urine calcium levels should be monitored in patients with suspected vitamin D toxicity. Standard therapy includes restriction of dietary calcium, hydration, and systemic glucocorticoids in patients with severe hypercalcemia.

Storage Condition

Store in a cool and dry place. Protect from light & moisture. Keep out of the reach of children.

Innovators Monograph

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