Ostalon^® (Tablets) Instructions for Use

ATC Code

M05BA04 (Alendronic acid)

Active Substance

Alendronic acid (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Bone resorption inhibitor for osteoporosis

Pharmacotherapeutic Group

Bone resorption inhibitor – bisphosphonate

Pharmacological Action

Alendronate sodium is a bisphosphonate, a synthetic analogue of pyrophosphate that binds to bone hydroxyapatite.

Being a non-hormonal specific inhibitor of osteoclast activity, it prevents bone resorption. It does not affect bone formation processes. It stimulates osteogenesis, restoring a positive balance between bone resorption and restoration.

It progressively increases bone mineral density (regulates phosphorus-calcium metabolism), and promotes the formation of bone tissue of normal composition and structure.

Pharmacokinetics

Absorption

After a single oral dose taken in the morning on an empty stomach (2 hours before breakfast) at a dose of 35 mg or 70 mg, absorption is 0.64%; with a shortened interval between drug intake and food – 0.46-0.39%.

Such a decrease in absorption does not significantly affect the drug’s efficacy. Simultaneous intake of coffee or orange juice reduces the bioavailability of alendronate sodium by 60%.

Distribution

After oral administration, alendronate sodium is temporarily distributed in soft tissues, then rapidly incorporates into bone tissue. Plasma protein binding is 78%.

Metabolism

There are no data confirming the metabolism of alendronate in the human body.

Excretion

Absorbed alendronate sodium that is not incorporated into bone tissue is rapidly excreted by the kidneys.

The maximum saturating capacity of bone tissue in animals could not be established with intravenous administration of a cumulative daily dose equal to 35 mg/kg.

Despite the lack of evidence, in renal disease, the excretion of alendronate is likely reduced with increased accumulation in bone tissue.

Indications

• Treatment of postmenopausal osteoporosis (reduction of the risk of spinal and hip fractures);
• Treatment of osteoporosis in men (reduction of the risk of spinal and pelvic fractures);
• Osteoporosis caused by long-term use of glucocorticoids.

ICD codes

Dosage Regimen

Tablets

The drug should be taken at a dose of 70 mg once a week. To ensure optimal absorption, Ostalon^® should be taken in the morning on an empty stomach at least 30 minutes (preferably 2 hours) before the first meal or liquid, washed down with plain drinking water.

Other beverages (including mineral water), food, and a number of medications may impair the absorption of alendronate.

To avoid local irritation of the oral mucosa and esophagus, in the morning, immediately after getting out of bed, drink at least 200 ml of plain water, then take the tablet without chewing or letting it dissolve in the mouth; for the next 30 minutes, you should not assume a horizontal position.

After this period, you should have breakfast.

Do not take the tablet in the morning before getting out of bed or in the evening after going to bed.

Treatment with alendronate should be supplemented with calcium and vitamin D intake.

In elderly patients, dose adjustment of the drug is not required.

For CrCl >35 ml/min, dose adjustment is not required; in severe renal impairment, the use of the drug is not recommended due to lack of clinical experience.

Due to the lack of clinical data, the drug is not prescribed to children.

Adverse Reactions

From the digestive system Common (≥1/100, <1/10) – abdominal pain, dyspepsia, constipation, diarrhea, flatulence, esophageal ulcer, dysphagia, abdominal distension, heartburn; Uncommon (≥1/1000, <1/100) – nausea, vomiting, gastritis, esophagitis, esophageal erosion, melena; Rare (≥1/10,000, <1/1000) – esophageal stricture, oropharyngeal ulcer, upper GI perforation, ulcer, bleeding (the relationship with treatment is not always clear).

From the musculoskeletal system Common (≥1/100, <1/10) – bone pain, arthralgia, myalgia.

From the nervous system Common (≥1/100, <1/10) – headache, irritability.

From the organ of vision Rare (≥1/10,000, <1/1000) – uveitis, scleritis.

Dermatological reactions Uncommon (≥1/1000, <1/100) – itching, skin hyperemia, rash; Rare (1/10,000, <1/1000) – photosensitivity.

Allergic reactions Rare (≥1/10,000, <1/1000) – urticaria, angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From metabolism Rare (≥1/10,000, <1/1000) – temporary, mild asymptomatic hypocalcemia and hypophosphatemia.

Other Rare (≥1/10,000, <1/1000) – transient symptoms resembling an acute-phase reaction (myalgia, malaise, fever, rarely – high body temperature), most often developing at the beginning of treatment.

Contraindications

• Abnormalities of the esophagus and other factors that delay esophageal emptying (including achalasia, stricture);
• Hypocalcemia;
• Chronic renal failure (CrCl <35 ml/min);
• Vitamin D deficiency;
• Severe disturbances of mineral metabolism;
• Inability of the patient to stand or sit upright for at least 30 minutes;
• Pregnancy;
• Lactation period;
• Childhood;
• Hypersensitivity to the components of the drug.

With caution GI diseases in the acute phase (dysphagia, esophageal disease, gastritis, duodenitis, ulcer; within the previous 12 months – peptic ulcer, gastrointestinal bleeding, surgery, except for surgery on the pylorus).

Use in Pregnancy and Lactation

Due to the lack of necessary clinical experience, the use of alendronate during pregnancy is contraindicated.

There are no data on excretion in breast milk; the use of alendronate during breastfeeding is contraindicated.

Use in Renal Impairment

The use of the drug in chronic renal failure (CrCl <35 ml/min) is contraindicated.

Pediatric Use

Contraindicated in childhood.

Geriatric Use

In elderly patients, dose adjustment of the drug is not required.

Special Precautions

Alendronate may cause local irritation of the GI mucosa. The course of diseases of the upper GI tract may worsen during treatment with alendronate.

Cases of adverse reactions from the esophagus (esophagitis, esophageal ulcer or erosion) have been reported, sometimes severe, requiring hospitalization, and complicated by the formation of strictures.

Patients should be specifically advised that if signs of esophageal irritation appear (dysphagia, retrosternal pain on swallowing, appearance or worsening of heartburn attacks), the drug should be discontinued and a doctor should be consulted.

The risk of esophageal damage is higher in patients who do not follow the rules for taking the drug, or who continue treatment despite the appearance of signs of esophageal irritation.

It is extremely important to inform patients in a timely manner about the importance of following the rules for taking the drug and to ensure that the patient understands this.

The patient should be warned that if a dose is missed, the missed tablet should be taken the next morning. Under no circumstances should two tablets be taken in one day.

Treatment can only be started after hypocalcemia, disturbances in mineral and vitamin metabolism (e.g., vitamin D deficiency) have been corrected.

The use of alendronate leads to an increase in the mineral salt content in bone tissue; the process may be accompanied by an asymptomatic change in calcium and phosphorus levels.

Ensuring adequate intake of calcium and vitamin D is especially important in the case of simultaneous treatment of the patient with glucocorticoids.

Treatment should be combined with a diet enriched with calcium salts.

Effect on ability to drive vehicles and operate machinery

The drug does not affect the ability to drive a car and perform work associated with a high risk of injury, however, in the presence of adverse reactions from the organ of vision, driving a car and operating machinery is contraindicated until the adverse reactions completely disappear.

Overdose

Symptoms hypocalcemia, hypophosphatemia, adverse reactions from the upper GI tract (heartburn, esophagitis, gastritis, ulcer).

Treatment there is no specific treatment, intake of milk, antacids is recommended. To avoid irritation of the esophagus, vomiting should not be induced; the patient should be placed in an upright position (standing or sitting).

Drug Interactions

Calcium, antacids, some oral medications, food, beverages (including mineral water) affect the absorption of alendronate – medications can be taken orally no earlier than 1 hour after taking Ostalon^®.

Other interaction, except for changes in absorption, is unlikely.

Ranitidine increases bioavailability (clinical significance is unknown).

NSAIDs enhance the adverse effects of alendronic acid.

Special drug interaction studies have not been conducted, however, patients receiving other oral drugs participated in studies with alendronate. No adverse effects associated with the simultaneous use of other drugs were observed.

Storage Conditions

The drug should be stored out of the reach of children at a temperature between 15°C (59°F) and 30°C (86°F).

Shelf Life

The shelf life is 4 years. Do not use after the expiration date.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.