Alendronate Na trihydrate.
Each tablet contains alendronate sodium trihydrate 91.37 mg equivalent to alendronic acid 70 mg.
It also contains the following excipients: Sorbitol, maize starch, sodium starch glycolate, stearic acid and magnesium stearate.
Alendronic acid is chemically described as (4-amino-1-hydroxybutylidene) bisphosphonic acid monosodium salt trihydrate.
Pharmacotherapeutic Group: Bisphosphonate, for the treatment of bone diseases.
Alendronic acid is a bisphosphonate that acts as a specific inhibitor of osteoclast-mediated bone resorption. Bisphosphonates are synthetic analogs of pyrophosphate that binds to the hydroxyapatite found in bone.
Pharmacology: Pharmacodynamics: Alendronate sodium trihydrate is a bisphosphonate that inhibits osteoclastic bone resorption with no direct effect on bone formation. Preclinical studies have shown preferential localisation of alendronate to sites of active resorption. Activity of osteoclast is inhibited, but recruitment or attachment of osteoclasts is not affected. The bone formed during treatment with alendronate is of normal quality.
Treatment of Postmenopausal Osteoporosis: Osteoporosis is defined as bone mineral density (BMD) of the spine or hip 2.5 standard deviation (SD) below the mean value of a normal young population, or as a previous fragility fracture, irrespective of BMD.
The therapeutic equivalence of alendronate 70 mg once weekly (n=519) and alendronate 10 mg daily (n=370) was demonstrated in a 1-year multicentre study of postmenopausal women with osteoporosis. The mean increases from baseline in lumbar spine BMD at 1 year were 5.1% (95% CI: 4.8%, 5.4%) in the 70-mg once weekly group and 5.4% (95% CI: 5.1%, 5.8%) in the 10-mg daily group. The mean BMD increases were 2.3% and 2.9% at the femoral neck, 2.9% and 3.1% at the total hip in the 70-mg once weekly and 10-mg daily groups, respectively. The 2 treatment groups were also similar with regards to BMD increases at other skeletal sites.
Pharmacokinetics: Absorption and Bioavailability: Relative to an IV reference dose, the oral mean bioavailability of alendronate in women was 0.64% for doses ranging from 5-70 mg when administered after an overnight fast and 2 hrs before a standardized breakfast. Bioavailability was decreased similarly to an estimated 0.46% and 0.39% when alendronate was administered 1 hr or ½ hr before a standardized breakfast.
Distribution: Concentrations of drug in plasma following therapeutic oral doses are too low for analytical detection (<5 ng/mL). Protein-binding in human plasma is approximately 78%.
Metabolism and Elimination: Biotransformation: There is no evidence that alendronate is metabolized in animals or humans.
Elimination: The terminal half-life in humans is estimated to exceed 10 years, reflecting release of alendronate from the skeleton. Alendronate is not excreted through the acidic or basic transport systems of the kidney in rats; thus, it is not anticipated to interfere with the excretion of other medicinal products by those systems in humans.
Toxicology: Preclinical Safety Data: Preclinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated-dose toxicity, genotoxicity and carcinogenic potential.
Treatment and prevention of postmenopausal osteoporosis.
Treatment of glucocorticoid-induced osteoporosis in men and women, Paget's bone disease in men and women, and to increase bone mass in men with osteoporosis.
Recommended Dose: 1 tab once weekly.
The recommended dose has not been investigated in the treatment of glucocorticoid-induced osteoporosis.
Renal Impairment: No dosage adjustment is necessary for patients with glomerular filtration rate (GFR) >35 mL/min. Alendronate is not recommended for patients with renal impairment where GFR is <35 mL/min, due to lack of experience.
Elderly: In clinical studies, there was no age-related difference in the efficacy or safety profiles of alendronate. Therefore, no dosage adjustment is necessary for the elderly.
Children: Alendronate has not been studied in children and should not be given to them.
Administration: To permit adequate absorption of alendronate: Maxlen-70 must be taken at least 30 min before the 1st food, beverage or medicinal product of the day with plain water only. Other beverages (including mineral water), food and some medicinal products are likely to reduce the absorption of alendronate (see Interactions).
To facilitate delivery to the stomach, and thus reduce the potential for local and oesophageal irritation/adverse experiences (see Precautions): Maxlen-70 should only be swallowed upon arising for the day with a full glass of water (not less than 200 mL or 7 fl oz).
Patients should not chew the tablet or allow the tablet to dissolve in the mouth because of potential for oropharyngeal ulceration.
Patient should not lie down until after the 1st food of the day which should be at least 30 min after taking Maxlen-70.
Maxlen-70 should not be taken at bedtime or before arising for the day. Patients should receive supplemental calcium and vitamin D if dietary intake is inadequate (see Precautions).
Symptoms: Hypocalcaemia, hypophosphataemia and upper gastrointestinal adverse events eg, upset stomach, heartburn, oesophagitis, gastritis or ulcer, may result from oral overdosage.
Treatment: No specific information is available on the treatment of overdosage with alendronate. Milk or antacids should be given to bind alendronate. Owing to the risk of oesophageal irritation, vomiting should be induced and the patient should remain fully upright.
Hypersensitivity to alendronate sodium trihydrate or to any of the excipients of Maxlen-70.
Patients with abnormalities of the oesophagus and other factors which delay oesophageal emptying eg, stricture or achalasia; inability to stand or sit upright for at least 30 min; hypocalcemia (see Precautions).
Alendronate can cause local irritation of the upper gastrointestinal mucosa. Because there is a potential for worsening of the underlying disease, caution should be used when alendronate is given to patients with active upper gastrointestinal problems eg, dysphagia, oesophageal disease, gastritis, duodenitis, ulcers, or with a recent history (within the previous year) of major gastrointestinal disease eg, peptic ulcer or active gastrointestinal bleeding, or surgery of the upper gastrointestinal bleeding or surgery of the upper gastrointestinal tract other than pyloroplasty (see Contraindications).
Oesophageal reactions (sometimes severe and requiring hospitalization) eg, oesophagitis, oesophageal ulcers and oesophageal erosions, rarely followed by oesophagitis stricture, have been reported in patients receiving alendronate. Physicians should therefore be alert to any signs or symptoms signaling a possible oesophageal reaction, and patients should be instructed to discontinue alendronate and seek medical attention if they develop symptoms of oesophageal irritation eg, dysphagia, pain or swallowing, or retrosternal pain, new or worsening heartburn. The risk of severe oesophageal adverse experiences appears to be greater in patients who fail to take alendronate properly and/or who continue to take it after developing symptoms suggestive of oesophageal irritation. It is very important that the full dosing instructions are provided to, and understood by the patient (see Dosage & Administration). Patients should be informed that failure to follow these instructions may increase the risk of oesophageal problems. While no increase risk was observed in extensive clinical trials, there have been rare (post-marketing) reports of gastric and duodenal ulcers, severe, bad and with complications. A causal relationship cannot be ruled out.
Osteonecrosis of the jaw generally associated with tooth extraction and/or local infection (including osteomyelitis) has been reported in patients with cancer receiving treatment regimen including primarily intravenously administered bisphosphonates. Many of these patients were also receiving chemotherapy and corticosteroids. Osteonecrosis of the jaw has also been reported in patients with osteoporosis receiving oral bisphosphonates.
A dental examination with appropriate preventive dentistry should be considered prior to treatment with bisphosphonates in patients with concomitant risk factors (eg, cancer, chemotherapy, radiotherapy, corticosteroids, poor oral hygiene).
While on treatment, these patients should avoid invasive dental procedures if possible. For patients who develop osteonecrosis of the jaw while on bisphosphonate therapy, dental surgery may exacerbate the condition. For patients requiring dental procedures, there are no data available to suggest whether discontinuation of bisphosphonate treatment reduces the risk of osteonecrosis of the jaw.
Clinical judgement of the treating physician should guide the management plan of each patient based on individual benefit/risk assessment.
Bone, joint and/or muscle pain has been reported in patients taking bisphosphonates. In post-marketing experience, these symptoms have rarely been severe and/or incapacitating (see Adverse Reactions).
The time to onset of symptoms varied from 1 day to several months after starting treatment. Most patients had relief of symptoms after stopping. A subset had recurrence of symptoms when rechallenged with the same drug or another bisphosphonate.
Patients should be instructed for a missed dose of Maxlen-70. Take 1 tablet on the morning as remembered. Two tablets should not be taken on the same day but should return to taking 1 tablet once weekly, as originally scheduled on the chosen day. Alendronate is not recommended for patients with renal impairment where GFR is <35 mL/min (see Dosage & Administration).
Causes of osteoporosis other than oestrogen deficiency and ageing should be considered. Hypocalcaemia must be corrected before initiating therapy with alendronate (see Contraindications).
Other disorders affecting mineral metabolism (eg, vitamin D deficiency and hypoparathyroidism) should also be effectively treated. In patients with these conditions, serum calcium and symptoms of hypocalcaemia should be monitored during therapy with Maxlen-70. Due to positive effects of alendronate in increasing bone mineral, decreases in serum calcium and phosphate may occur. These are usually small and asymptomatic. However, there have been reports of symptomatic hypocalcaemia, which occasionally have been severe and often occurred in patients with predisposing conditions (eg, hypoparathyroidism, vitamin D deficiency and calcium malabsorption). Ensuring adequate calcium and vitamin D intake is particularly important in patients receiving glucocorticoids.
Effects on the Ability to Drive or Operate Machinery: No effects on ability to drive and use machines have been observed.
Use in pregnancy & lactation: There are no adequate data for the use of alendronate in pregnant women.
It is not known whether alendronate is excreted into human breast milk. Given the indication, alendronate should not be used by breastfeeding women.
There are no adequate data for the use of alendronate in pregnant women.
It is not known whether alendronate is excreted into human breast milk. Given the indication, alendronate should not be used by breastfeeding women.
The following adverse experiences have also been reported.
[Common (approximately 1/100, <1/10), uncommon (approximately 1/1000, <1/100), rare (approximately 1/10,000, <1/1000), very rare (<1/10,000) including isolated cases.]
Immune System Disorders: Rare: Hypersensitivity reactions including urticaria and angioedema.
Metabolism and Nutrition Disorders: Rare: Symptomatic hypocalcaemia, often in association with predisposing conditions.
Nervous System Disorders: Common: Headache.
Eye Disorders: Rare: Uveitis, scleritis, episcleritis.
Gastrointestinal Disorders: Common: Abdominal pain, dyspepsia, constipation, diarrhea, flatulence, oesophageal ulcer, dysphagia, abdominal distention, acid regurgitation. Uncommon: Nausea, vomiting, gastritis, oesophagitis, oropharyngeal ulceration, upper gastrointestinal perforation, ulcers, bleeding (PUBs).
Skin and Subcutaneous Tissue Disorders: Uncommon: Rash, pruritus, erythema. Rare: Rash with photosensitivity. Very Rare: Isolated cases of severe skin reactions including Stevens-Johnson syndrome and toxic epidermal necrolysis.
Musculoskeletal, Connective Tissue and Bone Disorders: Common: Musculoskeletal (bone, muscle or joint) pain. Rare: Osteonecrosis of the jaw has been reported in patients treated by bisphosphonates.
If taken concomitantly, it is likely that food and beverages (including mineral water), calcium supplements, antacids, and some oral medicinal products will interfere with absorption of alendronate. Therefore, patients must wait at least 30 min after taking alendronate before taking any other oral medicinal product (see Pharmacokinetics under Actions and Dosage & Administration).
No other interactions with medicinal products of clinical significance are anticipated. A number of patients in the clinical trials received oestrogen (intravaginal, transdermal or oral) while taking alendronate. No adverse experiences to the concomitant use were identified.
Although, specific interaction studies were not performed, in clinical studies, alendronate was used concomitantly with a wide range of commonly prescribed medicinal products without evidence of clinical adverse interactions.
Incompatibilities: Not applicable.
Store below 25°C, in a dry place. Protect from light and moisture.
Shelf-Life: 36 months.
M05BA04 - alendronic acid ; Belongs to the class of bisphosphonates. Used in the treatment of bone diseases.
Tab 70 mg (cylindrical white, with a one face groove) x 1 x 4's.
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