Osterepar tablets 70mg, No. 4

Treatment of postmenopausal osteoporosis to prevent fractures of the spine and hip.

The drug is taken orally. The recommended dose is 70 mg once a week. To ensure optimal absorption, the drug should be taken in the morning on an empty stomach, 2 hours (at least 30 minutes) before the first meal or liquid, with plain drinking water. Other drinks, incl. mineral waters, food, a number of medicines can impair the absorption of alendronate. To avoid local irritation of the oral mucosa and esophagus in the morning, immediately after getting out of bed, you should drink at least 200 ml of plain water, then take a pill without chewing or letting it dissolve in your mouth, during the next 30 minutes you should not take a horizontal position of the body , after this period, breakfast should be taken.

Do not take the pill 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. Dose adjustment is not required in elderly patients. With CC> 35 ml / min, dose adjustment is not required. In renal failure with CC <35 ml / min, the drug should not be prescribed due to lack of clinical experience.

The tablets are white, oblong, biconvex.

1 tab. alendronate sodium trihydrate 91.37 mg, which corresponds to the content of alendronic acid 70 mg

Excipients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, colloidal anhydrous silicon dioxide.

• Anomalies of the esophagus and other factors that impede the patency of the esophagus (including achalasia, stricture);

• inability of the patient to remain upright, even if sitting, for 30 minutes;

• hypocalcemia;

• chronic renal failure (CC <35 ml / min);

• pregnancy;

• lactation period (breastfeeding);

• childhood;

• vitamin D deficiency;

• severe disorders of mineral metabolism;

• hypersensitivity to the components of the drug.

  The drug should be used with caution in diseases of the digestive tract in the acute phase (dysphagia, diseases of the esophagus, gastritis, duodenitis, ulcer, serious gastrointestinal disease in the previous 12 months, for example, peptic ulcer, gastrointestinal bleeding, surgery, except for operations on spastic pylorus).

pharmachologic effect

Bone resorption inhibitor. Alendronate sodium is a bisphosphonate, a synthetic analogue of pyrophosphate that binds hydroxyapatite in bone tissue. As a non-hormonal specific inhibitor of osteoclast activity, it prevents bone resorption. Does not affect the processes of bone formation. Stimulates osteogenesis, restores a positive balance between bone resorption and restoration. Progressively increases bone mineral density (regulates phosphorus-calcium metabolism), promotes the formation of bone tissue of normal composition and structure.

Pharmacokinetics

Suction

After a single dose of 70 mg in the morning on an empty stomach 2 hours before breakfast, absorption is 0.64%. With a shortened break between taking the drug and food - 0.46-0.39%. This decrease in absorption does not significantly affect the effectiveness of the drug. Simultaneous intake of coffee or orange juice reduces bioavailability by 60%.

Distribution

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

Metabolism

There is no data to support the metabolism of alendronate in humans.

Withdrawal

Alendronate absorbed but not incorporated into the bone tissue is rapidly excreted by the kidneys. Despite the lack of evidence, in kidney disease, a decrease in excretion of alendronate with increased accumulation in bone tissue is likely.

Side effect

From the digestive system: often (1/100, <1/10) - abdominal pain, dyspepsia, constipation, diarrhea, flatulence, esophageal ulcer, dysphagia, bloating, heartburn; infrequently (1/1000, <1/1000) - nausea, vomiting, gastritis, esophagitis, esophageal erosion, melena; rarely (1/10 000, <1/1000) - narrowing of the esophagus, oropharyngeal ulcer, perforation of the upper gastrointestinal tract, ulcer, bleeding, however, the relationship with treatment is not always clear. From the musculoskeletal system: often (1/100, <1/10) - ostalgia, arthralgia, myalgia. From the nervous system: often (1/100, <1/10) - headache, irritability. On the part of the skin: infrequently (1/1000, <1/1000) - itching, rash, flushing of the skin; rarely (1/10 000, <1/1000) - photosensitization. Allergic reactions: rarely (1/10 000, <1/1000) - urticaria, angioedema, Stevens-Johnson syndrome,toxic epidermal necrolysis; transient symptoms resembling an acute reaction phase (myalgia, weakness, feeling unwell, rarely - high body temperature) most often develop at the beginning of treatment. From the side of metabolism: rarely (1/10 000, <1/1000) - hypocalcemia (often accompanied by predisposing factors). From the senses: rarely (1/10 000, <1/1000) - uveitis, scleritis. Laboratory indicators: rarely (1/10 000, <1/1000) - temporary, mild asymptomatic hypocalcemia and hypophosphatemia.1/1000) - hypocalcemia (often accompanied by predisposing factors). From the senses: rarely (1/10 000, <1/1000) - uveitis, scleritis. Laboratory indicators: rarely (1/10 000, <1/1000) - temporary, mild asymptomatic hypocalcemia and hypophosphatemia.1/1000) - hypocalcemia (often accompanied by predisposing factors). From the senses: rarely (1/10 000, <1/1000) - uveitis, scleritis. Laboratory indicators: rarely (1/10 000, <1/1000) - temporary, mild asymptomatic hypocalcemia and hypophosphatemia.

Application during pregnancy and lactation

Due to the lack of the necessary clinical experience, the use of OstereparЃ during pregnancy is contraindicated. There is no data on the penetration of alendronate into breast milk. Taking OstereparЃ during breastfeeding is contraindicated.

Application for impaired renal function

No dose adjustment is required at a glomerular filtration rate> 35 ml / min. In renal failure with a glomerular filtration rate <35 ml / min, the drug should not be prescribed due to lack of clinical experience.

Application in children

Children's age: due to the lack of clinical data, the drug is not prescribed to children.

special instructions

Alendronate may cause local irritation to the lining of the digestive tract. The course of diseases of the upper digestive tract may worsen during treatment with alendronate. There are known cases of adverse reactions from the esophagus (esophagitis, ulcer or erosion of the esophagus), sometimes severe, requiring hospital treatment, and complicated by the formation of a stricture. Particular attention should be paid to patients that when signs of irritation of the esophagus appear (dysphagia, chest pain when swallowing, the appearance or worsening of heartburn attacks), the drug should be discontinued and consult a doctor. The risk of damage to the esophagus is higher in patients who do not follow the rules for taking the drug, or continue treatment despite signs of irritation of the esophagus.It is extremely important to inform patients in a timely manner about the importance of adhering to the rules for taking the drug and to make sure that the patient understands this. Treatment can be started only after elimination of hypocalcemia, disorders of mineral and vitamin metabolism (for example, vitamin D deficiency). Taking alendronate leads to an increase in the content of mineral salts in the bone tissue, the process may be accompanied by asymptomatic changes in the levels of calcium and phosphorus. Ensuring adequate intake of calcium and vitamin D is especially important in the case of treatment of a patient with GCS. Treatment should be combined with a diet enriched with calcium salts. Patients should be warned that if the next dose of the drug is missed, the missed pill should be taken the next morning; in no case should you take 2 tablets on the same day.Use in pediatrics Due to the lack of clinical data, the drug is not prescribed for children.

Influence on the ability to drive vehicles and use mechanisms

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

Overdose

Symptoms: hypocalcemia, hypophosphatemia, side reactions from the upper gastrointestinal tract (heartburn, esophagitis, gastritis, ulcer). Treatment: no specific treatment. It is recommended to take milk, antacids. In order to avoid irritation of the esophagus, vomiting should not be induced; the patient must take an upright position (standing or sitting).

Drug interactions

Calcium, antacids, some oral medications, food, drinks, incl. mineral waters affect the absorption of alendronate. Medicines can be taken orally no earlier than 1 hour after taking alendronate. Interactions other than changes in absorption are unlikely. Ranitidine increases the bioavailability of alendronate (clinical significance is unknown). NSAIDs enhance the adverse effects of alendronic acid. Special studies on drug interactions were not carried out, however, patients who were simultaneously taking other oral drugs participated in studies with alendronate. At the same time, they did not have any adverse reactions associated with the simultaneous administration of other drugs.