Active substanceAlendronic acidAlendronic acid
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: sodium alendronate trihydrate - 91.36 mg (corresponding to 70 mg of alendronic acid);

    Excipients: lactose monohydrate 128.64 mg, microcrystalline cellulose 65.00 mg, croscarmellose sodium 15.00 mg, magnesium stearate 3.00 mg, silicon dioxide colloidal anhydrous 2.00 mg.

    Description:

    Tablets are white, oblong, biconvex.

    Pharmacotherapeutic group:Bone resorption inhibitor-bisphosphonate
    ATX: & nbsp

    M.05.B.A.04   Alendronic acid

    Pharmacodynamics:

    Inhibitor of bone resorption. Refers to a group of bisphosphonates that, localized in areas of active bone resorption, under osteoclasts, inhibit the process of bone resorption caused by osteoclasts without directly affecting the formation of new bone tissue. Since bone resorption and the appearance of new bone tissue are interrelated, bone formation also decreases, but to a lesser extent than resorption, which leads to a progressive increase in bone mass. During treatment with alendronate, normal bone tissue is formed, in the matrix of which alendronate is incorporated, remaining pharmacologically inactive. In therapeutic doses, alendronate does not cause osteomalacia.

    Pharmacokinetics:

    Suction

    After oral administration in doses of 5-70 mg on an empty stomach no later than 2 hours before a standard breakfast, the bioavailability of alendronate is 0.64% in women and 0.6% in men.

    After taking alendronate on an empty stomach 1-1.5 h before the standard breakfast, bioavailability is reduced by approximately 40%.

    In patients with osteoporosis, Osterepar® is effective when applied on an empty stomach no later than 30 minutes before the first meal or liquid.

    The bioavailability of alendronate is insignificant when administered simultaneously with food intake or within 2 hours after ingestion. Simultaneous reception with coffee or orange juice reduces the bioavailability of the drug by approximately 60%.

    When taking prednisolone at a dose of 20 mg 3 times / day for 5 days, there is no clinically significant change in the bioavailability of alendronate.

    Distribution

    The average volume of distribution of alendronate in the equilibrium state (excluding bone tissue) is at least 28 liters. When taken in therapeutic doses, the concentration of the drug in the blood plasma is negligible (less than 5 ng / ml). The binding of alendronate to plasma proteins is approximately 78%.

    Metabolism

    There is no evidence that alendronate is metabolized in humans or animals.

    Excretion

    After a single intravenous (iv) introduction of alendronate labeled with carbon atoms [14C], approximately 50% of the drug is excreted in the urine for 72 hours; excretion of the labeled drug with feces was insignificant or not determined.

    After a single intravenous injection of alendronate in a dose of 10 mg, its renal clearance is 71 ml / min. After 6 hours after IV maintenance, the concentration in the blood plasma is reduced by more than 95%. Finite T1/2 exceeds 10 years, which reflects the release of the drug from bone tissue. Alendronate does not interfere with the excretion of drugs through the acid and basic transport systems of the kidneys.

    Floor. The bioavailability of alendronic acid does not differ significantly between men and women.

    Elderly age. Bioavailability and excretion of alendronic acid are similar in the elderly and young patients.

    Race. Pharmacokinetic differences on the basis of race were not studied.

    Violation of the function of the liver. In patients with impaired liver function, there is no need to correct the dose of alendronic acid, since it is not metabolized and is not excreted with bile.

    Indications:

    - Treatment of osteoporosis in postmenopausal women in order to prevent the development of fractures, incl. hip fractures and compression fractures of the spine;

    - treatment of osteoporosis in men in order to prevent the occurrence of fractures.

    Contraindications:

    - Pincreased sensitivity to the components of the drug;

    - abnormalities of the esophagus and other factors that impede the passage of the esophagus (achalasia, stricture, etc.);

    - the patient's inability to remain in a vertical position, even if sitting, for 30 minutes;

    - hypocalcemia;

    - chronic renal failure (creatinine clearance (CK) <35 mL / min);

    - pregnancy, the period of breastfeeding;

    - childhood;

    - vitamin deficiency D;

    - severe disturbances in mineral metabolism.

    - deficiency of lactase, intolerance to galactose, glucose-galactose malabsorption (the preparation contains lactose).

    Carefully:

    Diseases of the digestive tract in the phase of exacerbation (dysphagia, esophageal diseases, gastritis, duodenitis, ulcer, serious gastrointestinal disease in the previous 12 months, for example, peptic ulcer, gastrointestinal bleeding, surgery, except for operations on the spastic gastric gatekeeper) .

    Pregnancy and lactation:

    Pregnancy: There is no data on the use of alendronic acid in pregnant women.

    In animal studies, there was a disturbance in the formation of fetal bone tissue with high doses of alendronic acid,dysfunction of labor related to hypokalemia. The use of alendronic acid during pregnancy is contraindicated.

    Breastfeeding period: there is no data on the penetration into breast milk; the intake of alendronic acid during breastfeeding is contraindicated.

    Dosing and Administration:

    Inside, without chewing, drinking with drinking water, at least 30 minutes before the first meal, liquid or medicines. Other beverages (including mineral water), food and some medicines can reduce the absorption of Ostherepar®.

    To reduce the risk of esophageal irritation, Osterepar® should be taken with the following rules: take in the morning immediately after getting up from bed; drink a full glass of water to facilitate the intake of the tablet in the stomach; Do not chew tablets and do not dissolve them in the mouth due to the possible formation of ulcers in the mouth and throat; patients should not lie down until the first meal, which should be made at least 30 minutes after taking Osterepar®; Osterepar® should not be taken before bedtime or before going to bed.

    Patients should additionally take calcium and vitamin preparations D, if the supply of these substances with food is not enough.

    Treatment of osteoporosis in postmenopausal women: the recommended dose is 1 tablet 70 mg once a week.

    Treatment of osteoporosis in men: the recommended dose is 1 tablet 70 mg once a week.

    The optimal duration of the drug is not established. The need for continuation of bisphosphonate therapy should be evaluated on a regular basis, especially after 5 years of use.

    For elderly patients and patients with mild and moderate renal insufficiency (CK from 35 to 60 ml / min), dose adjustment is not required. Osterhepar® is not recommended for patients with severe renal insufficiency (CK <35 mL / min) due to a lack of experience with these patients.

    Childhood: Because of the lack of clinical data, the drug is not prescribed for children.

    Side effects:

    Alendronic acid safety profile for use in postmenopausal women at a dose of 70 mg per week and a dose of 10 mg / day, according to a one-year clinical trial, was similar.

    In two three-year clinical trials, the use of alendronic acid in postmenopausal women at a dose of 10 mg / day showed that the general safety profiles of alendronic acid and placebo are similar.

    Table 1 shows the undesirable reactions, the association of which with the administration of alendronic acid is possible, probable or unquestionable if they were observed at a frequency of not less than 1% in the group receiving alendronic acid at a dose of 70 mg per week in a one-year study, or at a frequency of not less than 1 % in the group receiving alendronic acid at a dose of 10 mg / day in three-year studies.

    Table 1.


    One-year

    Three-year



    study

    research



    70 mg in

    10

    10

    Placebo



    week,

    mg / day,

    mg / day,




    (n= 519)

    (n= 370)

    (n= 196)

    (n= 397)



    %

    %

    %

    %


    From the digestive system






    stomach ache

    3,7

    3,0

    6,6

    4,8


    dyspepsia

    2,7

    2,2

    3,6

    3,5


    sour belch

    1,9

    2,4

    2,0

    4,3


    nausea

    1,9

    2,4

    3,6

    4,0


    bloating

    1,0

    1,4

    1,0

    0,8


    constipation

    0,8

    1,6

    3,1

    1,8


    diarrhea

    0,6

    0,5

    3,1

    1,8


    dysphagia

    0,4

    0,5

    1,0

    0,0


    flatulence

    0,4

    1,6

    2,6

    0,5


    gastritis

    0,2

    1,1

    0,5

    1,3


    gastric ulcer

    0,0

    1,1

    0,0

    0,0


    oesophageal ulcer

    0,0

    0,0

    1,5

    0,0


    From the musculoskeletal system






    pain in the bones, muscles, joints

    2,9

    3,2

    4,1

    2,5


    muscle cramps

    0,2

    1,1

    0,0

    1,0

    From the central nervous system (CNS)





    headache

    0,4

    0,3

    2,6

    1,5

    In the broad clinical practice (including clinical trials and post-marketing data), the following adverse effects have been reported, which are classified according to their frequency of development (WHO classification): very often (≥1 / 10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10,000, <1/1000), very rarely (<1/10 000, including individual messages):

    Allergic reactions: rarely - hypersensitivity reactions, including hives, angioedema.

    From the laboratory indicators: rarely symptomatic hypocalcemia (especially in the presence of risk factors).

    From the side of the central nervous system: often - headache, dizziness; infrequently - a violation of taste sensations.

    From the side of the organ of vision: infrequently - uveitis, scleritis, episcleritis.

    From the organs of hearing and balance: often - imbalance.

    From the digestive system: often - abdominal pain, indigestion, constipation, diarrhea, esophagus ulcer, dysphagia, bloating, acidic eructation; infrequently - nausea, vomiting, gastritis, melena, esophagitis, erosion of the esophagus; rarely - stricture of the esophagus, ulceration of the oropharynx, perforation, ulcers, bleeding from the upper sections of the gastrointestinal tract.

    From the skin and skin appendages: often - itching, alopecia; infrequently - skin rash, erythema; rarely - a rash with photosensitivity, severe skin reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis.

    From the musculoskeletal system: very often - myalgia, pain in the bones, pain in the joints (sometimes - heavy flow); often - swelling of the joints; rarely - osteonecrosis of the lower jaw, atypical fractures of the body of the femur.

    On the part of the body as a whole: often - asthenia, peripheral edema; infrequent - transient symptoms of acute phase reaction at the beginning of treatment (myalgia, malaise, less often - fever), usually at the beginning of treatment.

    Overdose:

    Symptoms: abdominal pain, dyspeptic disorders, dysphagia, heartburn, esophagitis, gastritis; hypocalcemia and hypophosphataemia may develop.

    Treatment: symptomatic. The use of milk and antacid preparations for the binding of alendronate is shown. In connection with the risk of esophageal injury, do not induce vomiting, the patient should be in an upright position.

    Interaction:

    Calcium, antacids, some oral preparations, food, drinks, incl. The mineral waters affect the absorption of alendronate; medicines can be taken orally no earlier than 1 hour after taking alendronate.

    Ranitidine increases bioavailability (clinical significance is unknown). With the joint use of Ostherepar® and hormone replacement therapy (estrogen ± progestin), the safety and tolerability of combination therapy are consistent with those of each of these drugs alone.In clinical studies of Ostherepar® in men, postmenopausal women and patients taking glucocorticosteroids, there was no clinically significant drug interaction with respect to effects on protein binding, renal excretion, and metabolism. The incidence of adverse events from the upper part of the gastrointestinal tract (GIT) increases with the combination of Osterepar® in a dose of more than 10 mg / day with preparations containing acetylsalicylic acid. However, this effect was not observed when taking Osteverpar ® in a dose of 70 mg once a week.

    Osterhepar® can be administered with caution (due to the risk of developing gastrointestinal bleeding) to patients taking non-steroidal anti-inflammatory drugs, however, according to the results of the clinical study, there was no clinically significant drug interaction and an increase in the incidence of side effects when drugs were used together.

    Special instructions:

    Osterepar®, like other bisphosphonates, can cause local irritation of the mucous membrane of the upper gastrointestinal tract.Patients treated with Osterepar® receive side effects such as esophagitis, esophageal ulcers, and erosion of the esophagus, which occasionally lead to the development of strictures or perforation of the esophagus. In some cases, these undesirable phenomena may be severe and require hospitalization, so you should carefully monitor any symptoms that indicate possible abnormalities on the part of the esophagus. Patients should be cautioned to stop taking Ostaperpar® and seek medical attention if dysphagia, swallowing pain or chest pain occurs, or if heartburn occurs.

    The risk of severe adverse events on the side of the esophagus is higher in patients who violate the recommendations for taking the drug and / or continue to take it when symptoms of esophageal irritation appear. It is especially important that the patient has recommendations for taking the drug, understood them and was informed that the risk of developing an esophageal lesion increases if these recommendations are not followed.

    There are rare cases of the occurrence of gastric and duodenal ulcers, sometimes severe and complicated (the cause-and-effect relationship with taking the drug is not established).

    Osterepar® The drug should be used with caution in patients with exacerbations of upper gastrointestinal diseases, such as dysphagia, oesophageal disease, gastritis, duodenitis and ulcers due to possible irritating effect of the drug on the mucosa of the upper gastrointestinal tract and the worsening of the underlying disease.

    The decision to perform treatment should be taken individually for each patient after a thorough assessment of the risk / benefit ratio, especially for patients with Barrett's esophagus.

    There are cases of local osteonecrosis of the jaw associated mainly with the previous extraction of the tooth and / or a local infection (including osteomyelitis), often with a slow recovery.

    In most cases, osteonecrosis of the jaw in patients receiving bisphosphonates occurs in cancer patients treated with bisphosphonates in /. Known risk factors for osteonecrosis of the jaw include a cancer concomitant therapy (e.g., chemotherapy, radiotherapy, corticosteroids), poor oral hygiene and associated pathology (e.g., periodontal diseases and / or other dental diseases, anemia, coagulopathy, infection), and smoking.Patients who develop osteonecrosis of the jaw must be provided with specialized medical care by the maxillofacial surgeon, and the question of the abolition of bisphosphonate therapy should be considered based on an individual assessment of the risk / benefit ratio. Dental surgery can lead to a worsening of the condition.

    The tactics of treating each patient who needs an invasive dental intervention (for example, tooth extraction, implantation), including bisphosphonate therapy, should be based on the clinical judgment of the attending physician and / or maxillofacial surgeon and the individual risk / benefit ratio. There have been reports of pain in the bones, joints and / or muscles in patients receiving bisphosphonates. These symptoms are rarely severe and / or lead to disability. The time to onset of symptoms varies from one day to several months from the start of therapy. In most patients, after the cessation of therapy, symptoms recede, but some patients appear again after the resumption of the same drug or other bisphosphonate.Reported on the emergence of pathological (i.e., under the influence of minor force or spontaneous) susceptible fractures or fractures of the proximal parts of the femoral diaphysis in a small number of patients taking bisphosphonates. Some of the fractures were classified as stressful (also known as stress fracture, march fracture, Deutscheland fracture) that occur in the absence of trauma. Some patients experienced prodromal pains in the affected area weeks or months before the onset of a complete fracture, often associated with a characteristic radiographic picture of a stress fracture. The number of reports was very small, in addition, stress fractures with similar clinical features occur in patients who do not take bisphosphonates. Patients with stress fractures should be examined with an assessment of known causes and risk factors (eg, vitamin deficiency D, infringement of absorption, use of corticosteroids, stress fracture in anamnesis, arthritis or fracture of lower limb, excessive or increased loads, diabetes, chronic alcoholism) and provide them with proper orthopedic care.Approximately one-third of stress fractures were bilateral; accordingly, in patients who underwent fracture of the femoral bone, the contralateral femur should be examined. Prior to receiving the results of the survey, consideration should be given to stopping the use of bisphosphonates in patients with stress fractures, based on an assessment of the benefit / risk ratio in each specific case.

    Patients should be warned that if they miss a dose of Osterepar® once a week, they should take one pill in the morning of the next day. You should not take two doses in one day, but in the future you should return to reception the drug once a week on the day of the week that was selected at the beginning of the treatment. Other causes of osteoporosis should be taken into account, in addition to estrogen deficiency, age and treatment with glucocorticoids.

    In the presence of hypocalcemia, the level of calcium in the blood should be normalized before starting treatment with Osterepar®. Other disorders of mineral metabolism (eg, vitamin deficiency D) should also be eliminated. In patients with these disorders it is necessary to monitor the calcium content in the blood and the symptoms of hypocalcemia.

    Because Ostherepar® increases the mineral content in the bones, there may be a slight asymptomatic decrease in serum calcium and phosphate levels, especially in the case of Paget's bone disease, with initially significantly increased metabolic rate of bone tissue, as well as in patients receiving glucocorticoids, which is accompanied by a possible a decrease in calcium absorption. It is especially important to ensure adequate intake of calcium and vitamin in the body D in these patients.

    In rare cases, hypocalcemia can be severe, usually in patients with a predisposition to this complication (hypoparathyroidism, vitamin deficiency D, malabsorption of calcium).

    The preparation contains lactose. Patients with a deficiency of lactase, intolerance to galactose, glucose-galactose malabsorption should refrain from using the drug.

    Effect on the ability to drive transp. cf. and fur:

    Data on the effect of the drug on the ability to drive and other mechanisms do not. However, some of the side effects observed after taking alendronate may in some patients worsen the ability to drive vehicles and service mechanisms.

    Form release / dosage:

    Tablets of 70 mg.

    Packaging:

    4 tablets per foil blister A1/PVC.

    1 blister together with instructions for use are placed in a cardboard box.

    Storage conditions:

    At a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-007042/09
    Date of registration:07.09.2009 / 18.03.2014
    Expiration Date:Unlimited
    The owner of the registration certificate:Pharmaceutical factory "POLFARMA" JSCPharmaceutical factory "POLFARMA" JSC Poland
    Manufacturer: & nbsp
    Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia
    Information update date: & nbsp15.06.2017
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