Alendronate Sodium:- Alendronate Sodium is a bisphosphonate that act as a potent specific inhibitor of osteoclast mediated bone resorption. Alendronate shows preferential localization at sites of bone resorption, specifically under osteoclast. The osteoclasts adhere normally to the bone surface but lack the ruffled border that is indicative of active resorption. Alendronate dose not interfere with osteoclast recruitment or attachment, but inhibits osteoclast activity.
Studies showed that normal bone was formed over alendronate which is incorporated inside the matrix. Alendronate is not pharmacologically active, so Alendronate must be continuously administrered to suppress osteoclasts on newly formed resorption surfaces, Histomorphometry showed that Alendronate treatment reduces bone turnover in addition, bone formation exceeds bone resorption at these remodeling sites, leading to progressive gains in bone mass.
Cholecalciferol:- is a secosterol that is the natural precursor of calcium-regulating hormone, vitamin D3 is produced in the skin by photochemical conversion of 7-dehydrocholesterol to previtamin D3 by ultraviolet light. This is followed by non-enzymatic isomerization to vitamin D3 in skin and dietary vitamin D3 is converted to 25-hydroxy vitamin D3 to increase intestinal absorption of both calcium and phosphate and regulate serum calcium and phosphate excretion, bone formation and bone resorption. Vitamin D3 is required for normal bone formation, vitamin D3 insufficiency develops when both sunlight exposure and dietary intake are inadequate. Insufficiency is associated with negative calcium balance, increased parathyroid hormone levels, bone loss, and increased risk of skeletal fracture in severe cases, deficiency result is more severe hyperparathyroidism, hypophosphatemia, proximal muscle weakness, bone pain and osteomalacia
Absorption: Alendronate sodium is effective when administered at least 30 minutes before breakfast. Concomitant administration of alendronate with coffee or orange juice reduce bioavailability by approximately 60% and the bioavailability of the 2800 I.U. vitamin D3 in Egydronate is similar to 2800 I.U vitamin D3 administered alone
Distribution: Alendronate sodium plasma concentrations following therapeutic oral doses are too low for analytical detection, its protein binding in human plasma is approximately 78% after absorption, Vitamin D3 is rapidly distributed mostly to the liver, lesser amounts are distributed to adipose tissue and stored as vitamin D3 at these sites for later release into the circulation, circulating vitamin D3 is bound to vitamin D3-binding protein.
Metatobolism: there is no evidence that alendronate is metabolized in animals or humans and vitamin D3 is rapidly metabolized in the kidney to its active form, further hydroxylation and small amount of glucouronidation occur prior to elimination,
Excretion: the half- life in humans is estimated to exceed 10 years, probably reflecting release of alendronate from the skeleton it is estimated that after 10 years of oral treatment with Egydronate the amount of alendronate released daily from the skeleton is approximately 25% of that absorbed from the gastrointestinal tract and the mean half-life of vitamin D3 in the serum following an oral dose of Egydronate is approximately 14 hours.
- Interavenous ranitidine was shown to double the bioavailability of oral alendronate & that occur in patients given oral H2-antagonists.
- Oral prednisone (20mg three times daily for five days ) does not produce a clinically meaningful change in the oral bioavailability of alendronate
- Products containing calcium and other multivalent cations are likely to prefere with absorption of alendronate
- Olestra, mineral oils, orlistat, and bile acid sequestrates may impair the absorption of vitamin D3
- Anticonvulsants, cimetidine and thiazides may increace the catabolism of vitamin D3
- Treatment of osteoporosis in postmenopausal women.
- Treatment to increase bone mass in men with osteoporosis
Egydronote must be taken at least half an hour before the first food, beverage, or medication of the day with plain water only.
Egydronote should be swallowed upon arising for the day with a full gloss of water and patient should not lie down for at least 30 minutes and until otter their first food of the day.
The recommended dosage is one tablet (70mg/2800IU) once weekly.
Abnormalities of the esophagus, which delay esophageal emptying such as stricture or achalasia.
Inability to stone or sit upright for at least 30 minutes.
Hypersensitivity to any component of this product.
Hypersensitivity reactions including urticarial rarely angioedema, esophageal ulcers. Gastric or duodenal ulcers, oropharyngeal ulceration, localized osteonecrosis of the jaw, bone one joint and muscle pain, pruritus, rarely severe skin reactions Including Stevens-Johnson syndrome and toxic epidermal necrolysis.
The use of Egydronate in cases of osteoporosis other than estrogen deficiency, aging, and glucocorticoid should be considered.
Hypocalcaemia must be corrected before initiating therapy with Egydronate and other disorders affecting mineral metabolism should be monitored during therapy with egydronate
Egydronate only should not be used to treat vitamin D3 deficiency and patients at increased risk for vitamin D3 insufficiency should receive vitamin D3 supplementation in addition to that provided in Egydronate.
Patients with gastrointestinal malabsorption syndrome way require higher dose of Vitamin D3 supplementation and measurement of 25-hydroxy vitamin D3 should be considered.
Caution should be taken when Egydronate is given to patients with active upper gastrointestinal problems.
Patients who develop osteonecrosis of jaw while on therapy should receive care by oral surgeon.
Egydronate is not recommended for patients with severe renal insufficienc
Physicians should instruct their patients to read the insert before starting therapy with Egydronate and It is very Important that the full dosing instructions are provided to, and understood by the patients in patients who cannot comply with dosing instructions due to mental disability, therapy with Egydronate should be used under appropriate supervision.
Patients should be instructed to take calcium supplement if intake is inadequate and take vitamin D3 supplement in Vitamin D3 insufficiency.
Weight-bearing exercise should be considered along with the modification of certain behavior factors such as cigarette smoking and/or excessive alcohol consumption.
Patients should be instructed that if they miss a dose of Egydronote, they should return to take a tablet once a week, as originally scheduled on their chosen day.
Patients must wait at least half an hour after taking Egydronate before taking any other oral medications.
The incidence of upper gastrointestinal adverse events was increased in patients receiving concomitant therapy with daily doses of Egydronate.
NSAJO use is associated with gastrointestinal irritation so caution should be taken during concomitant use with Egydronate.
Safety and effectiveness in pediatric patients have not been established.
Egydronate should be used during pregnancy only if the potential benefit
Justifies the potential risk to the mother and foetus.
Cholecalciferol and some of Its active metabolites pass Into breast milk so caution should be taken when Egydronate is administered to nursing women .
Hypocalcaemia, hypophosphatemia and upper gastrointestinal adverse events such as upset stomach , heart bum. oesophagitis, gastritis , hypercalciuria. anorexia, nausea. vomiting, polyuria, polydipsia, Weakness result from oral over dosage
Milk ex antacid should be given . Due to the risk of esophageal irritation. vomiting should not be induced & the patient should remain full up right, standard therapy includes restriction of dietary calcium , hydration and systemic glucocorticoids In patients with severe hypercalcemia.
Dialysis to remove Vitamin D3 wouldn't be beneficial .
A box contains a blister of 2 tablets.
Store below 25C . Protect from light&humidity
. Keep out ot the reach of children