Instructions for Alendra tablets 70 mg blister No. 4
Composition
active ingredient: alendronic acid;
1 tablet contains alendronate sodium equivalent to 70 mg alendronic acid;
Excipients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate, colloidal anhydrous silicon dioxide.
Dosage form
Pills.
Main physicochemical properties: oval, biconvex tablets of white or almost white color.
Pharmacotherapeutic group
Drugs affecting bone structure and mineralization. ATX code M05B A04.
Pharmacological properties
Pharmacodynamics
Sodium alendronate belongs to the group of aminobisphosphonates. It is a synthetic analogue of natural pyrophosphate. It inhibits the precipitation of calcium phosphate, blocks its transformation into hydroxyapatite, delays the aggregation of apatite crystals with the formation of larger crystals and accelerates the reverse dissolution of these crystals. The selective action is due to the high affinity of bisphosphonates with the mineral components of bones. It acts as an effective non-hormonal specific inhibitor of osteoclast-mediated bone resorption. The exact mechanisms of this process are not fully understood. It restores a positive balance between resorption and bone regeneration. It increases the mineral density of the bones of the spine and pelvis, promotes the formation of bone tissue with a normal histological structure. It prevents the appearance of new bone fractures. It reduces the level of calcium in the blood serum by inhibiting bone resorption and reducing the release of calcium from bone tissue. The calcium-lowering effect of the drug, mediated by osteoclast inhibition, is observed after 1-2 days.
Pharmacokinetics
Alendronate sodium is absorbed from the gastrointestinal tract by 25%. Absolute bioavailability for tablets (5 to 10 mg) taken on an empty stomach 2 hours before a meal is 0.64% for women and 0.59% for men. Bioavailability is reduced (by approximately 40%) when alendronate sodium is taken half an hour to an hour before a normal breakfast. The bioavailability of alendronate sodium is insignificant when taken with food or within two hours after a meal. Concomitant administration of alendronate sodium with other drinks (including mineral water, coffee, orange juice) reduces its bioavailability by 60%. Studies in animals have shown that when administered intravenously at a dose of 1 mg/kg, alendronate sodium is temporarily distributed in soft tissues, but then redistributed rapidly. Half of the absorbed dose is excreted mainly by the kidneys unchanged within 72 hours, and the rest accumulates in bone tissue for a long time, eliminated very slowly due to binding to bone tissue. The half-life of alendronate sodium from bones is several years.
Alendronate is approximately 78% bound to plasma proteins and is not metabolized. Plasma concentrations are negligible (less than 5 ng/mL) and decline by 95% within 6 hours after intravenous infusion.
After a single intravenous administration of 10 mg alendronate, its renal clearance was 71 mL/min, and systemic clearance did not exceed 200 mL/min.
Indication
Treatment of postmenopausal osteoporosis. The drug reduces the risk of fractures of the spine and hip.
Contraindication
Hypersensitivity to alendronate sodium or to any other component of the drug;
Esophageal pathology (stricture or achalasia) that causes delayed evacuation of esophageal contents;
inability to stand or sit upright for at least 30 minutes;
hypocalcemia;
severe renal failure (creatinine clearance < 35 ml/min).
Interaction with other medicinal products and other types of interactions
The absorption of alendronate sodium may be impaired when taken simultaneously with food, drinks (including mineral water), calcium preparations (including food additives), antacids and some other drugs for oral administration. The interval between taking alendronate sodium and other drugs taken orally should be at least 30 minutes (see section "Method of administration and dosage").
Estrogens
No negative effects of simultaneous administration of alendronate sodium and estrogen-containing drugs have been identified.
Nonsteroidal anti-inflammatory drugs (NSAIDs)
NSAIDs may cause irritation of the gastrointestinal mucosa. Caution should be exercised when alendronate sodium and NSAIDs are used concomitantly.
No other drug interactions of clinical significance are expected.
Application features
Alendronate sodium may cause local irritation of the upper gastrointestinal mucosa. Since there is a risk of exacerbation of the underlying disease, the drug should be prescribed with caution to patients with dysphagia, esophageal diseases, gastritis, duodenitis, peptic ulcer disease, as well as patients who have had severe gastrointestinal diseases within the last year (gastric ulcer, acute gastrointestinal bleeding, surgical interventions in the upper gastrointestinal tract, except pyloroplasty).
Patients with Barrett's esophagus should be prescribed the drug individually, provided that the expected benefit outweighs the risk.
Since the drug may cause esophagitis (inflammation of the esophagus), ulcers or erosions of the esophagus, which in exceptional cases may be complicated by the appearance of esophageal stricture, it is necessary to carefully monitor the occurrence of any manifestations of such effects. If symptoms such as dysphagia, pain when swallowing, retrosternal pain, heartburn (the appearance of heartburn or worsening of existing heartburn) occur, the drug should be discontinued and consult a doctor.
The risk of severe esophageal adverse reactions is higher in individuals who do not take alendronate sodium properly and/or continue to take the drug after symptoms of esophageal irritation appear. Therefore, the patient should strictly follow the doctor's recommendations regarding dosage and administration of the drug (see section "Method of administration and dosage").
Although no increased risk of gastric and duodenal ulcers was identified in the pre-marketing period, rare cases of these diseases have been reported in the post-marketing period; some of them were severe with complications.
Osteonecrosis of the jaw
In general, osteonecrosis of the jaw has been associated with tooth extraction and/or the presence of local infection (including osteomyelitis) in cancer patients receiving intravenous bisphosphonates. Most of these patients were receiving chemotherapy and corticosteroids. Cases of osteonecrosis of the jaw have also been reported in patients with osteoporosis receiving oral bisphosphonates.
When assessing an individual's risk of osteonecrosis of the jaw, the following risk factors should be considered:
potency of the bisphosphonate (highest in zoledronic acid), route of administration (see above), and cumulative dose;
cancer, chemotherapy, radiotherapy, corticosteroids, angiogenesis inhibitors, smoking;
a complicated dental history, inadequate oral hygiene, invasive dental procedures, insufficiently tight fit of dentures.
Patients with poor oral hygiene should have a dental examination and receive appropriate preventive dental care before starting bisphosphonate treatment. During treatment, such patients should avoid invasive dental procedures whenever possible.
In patients who develop osteonecrosis of the jaw while receiving bisphosphonate therapy, dental surgery may worsen the condition. There is no additional evidence to suggest that discontinuation of bisphosphonate therapy reduces the risk of osteonecrosis of the jaw in patients who require dental surgery. The clinical decision to treat the patient should be based on an individual benefit/risk assessment.
During bisphosphonate therapy, all patients should maintain good oral hygiene, have regular dental check-ups, and report any dental symptoms (pain, swelling, tooth mobility).
Osteonecrosis of the external auditory canal
Cases of osteonecrosis of the external auditory canal have been reported with bisphosphonate therapy, mainly in association with long-term treatment (see section 4.8). Possible risk factors for osteonecrosis of the external auditory canal include steroid hormone therapy and chemotherapy, and/or local risk factors such as infection or trauma. The possibility of osteonecrosis of the external auditory canal should be assessed in patients receiving bisphosphonates and presenting with ear symptoms (ear pain or discharge from the external auditory canal and chronic ear infections).
Musculoskeletal pain
Bone, joint, and/or muscle pain has been reported in patients taking bisphosphonates. In rare cases, these symptoms have been severe and/or have affected the ability to perform daily activities. The time from initiation of bisphosphonate treatment to onset of symptoms has ranged from one day to several months. In most patients, symptom relief occurred after discontinuation of treatment. Recurrence of symptoms has occurred with re-administration of the same drug or a different bisphosphonate.
Atypical femur fractures
These fractures can occur anywhere along the femur (from the lesser trochanter to the epicondyles) with or without minimal trauma. Some patients may experience hip or groin pain for a period of weeks to months before a fracture is detected. Fractures are often bilateral. Therefore, if a patient receiving bisphosphonates has a diaphyseal fracture in one limb, the other limb should be examined to rule it out. It should be noted that these fractures do not heal well. Therefore, the decision to discontinue bisphosphonates in patients suspected of having atypical femoral fractures should be made by the physician based on an individual benefit/risk assessment. In addition, patients receiving bisphosphonates should be advised to promptly report any groin, hip, or hip pain to their physician. If such symptoms occur, the patient should be examined for a femur fracture.
Severe skin adverse reactions
In the post-marketing period, serious skin adverse reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported.
Missed dose
The patient should be warned that in case of missing a dose of the drug, it is necessary to take 1 tablet in the morning of the next day. Then continue taking it as usual - the next tablet should be taken on the day chosen for taking from the very beginning of treatment (see the section "Method of administration and dosage").
Kidney failure
Alendronate sodium is contraindicated in patients with severe renal impairment, particularly those with creatinine clearance < 35 ml/min (see section "Contraindications").
Mineral metabolism and hypocalcemia
Attention should be paid to possible causes of osteoporosis other than estrogen deficiency and age-related changes. Hypocalcemia should be corrected before starting therapy with alendronate sodium (see section "Contraindications"). Other disorders of mineral metabolism (such as vitamin D deficiency and hypoparathyroidism) should also be effectively treated. In patients with such conditions, serum calcium levels and symptoms of hypocalcemia should be monitored during treatment with the drug.
Due to the increase in bone mineralization under the influence of alendronate sodium, hypocalcemia and hypophosphatemia may develop, especially in patients taking glucocorticoids (due to reduced calcium absorption). Usually hypocalcemia is mild and asymptomatic. However, cases of hypocalcemia with clinical symptoms (in some cases severe) may occur, especially in patients with risk factors for calcium metabolism disorders (e.g. hypoparathyroidism, vitamin D deficiency, calcium malabsorption/impaired absorption). Therefore, ensuring adequate calcium and vitamin D intake is particularly important for patients taking glucocorticoids.
Excipients
This medicine contains lactose. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicine.
Use during pregnancy or breastfeeding
The drug is contraindicated during pregnancy and breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
Alendronate sodium has no known effect on the ability to drive or use machines. However, certain adverse reactions reported with the use of the drug may affect the ability of some patients to drive or use machines. Individual reactions to alendronate sodium may vary.
Method of administration and doses
Recommended dose: 1 tablet of 70 mg once a week.
The optimal duration of bisphosphonate treatment for osteoporosis has not been established. The decision on the need to continue treatment with alendronate sodium is made by the doctor individually for each patient based on a periodic assessment of the benefit/risk ratio (especially after 5 or more years of use of the drug).
The tablet should be taken with water at least 30 minutes before the first food, drink or other medicines. Other drinks (including mineral water), food and some medicines may reduce the absorption of alendronate sodium (see section "Interaction with other medicines and other types of interactions")
To facilitate the entry of the drug into the stomach and thus reduce its irritating effect on the mucous membrane of the oral cavity, pharynx, and esophagus, it is necessary:
take the drug with a glass of water (at least 200 ml) in the morning after waking up;
do not chew the tablet due to the possibility of oral and throat ulcers;
the first meal of the day – only 30 minutes after taking the pill;
after taking the tablets, patients should not lie down for at least 30 minutes;
The drug should not be taken before bedtime or before getting out of bed in the morning.
The interval between taking alendronate and other oral medications should be at least 30 minutes.
The drug should be taken on the same day of the week. If you accidentally miss a dose, take 1 tablet the next morning. Then continue taking it as usual - take the next tablet on the day that was chosen for taking it from the very beginning of treatment (see the section "Peculiarities of use").
Use in elderly patients.
There is no need to adjust the dose for elderly patients.
Kidney failure.
For patients with creatinine clearance greater than 35 ml/min, no dose adjustment is necessary.
Alendronate is not recommended for patients with creatinine clearance less than 35 ml/min due to the lack of experience with the drug in the treatment of such patients.
The drug has not been studied in the treatment of osteoporosis caused by corticosteroids.
Children
Do not use in children under 18 years of age.
Overdose
Symptoms: hypocalcemia, hypophosphatemia and upper gastrointestinal adverse reactions (gastric dysfunction, heartburn, esophagitis, gastritis or gastric ulcer).
Treatment: Milk or antacids should be taken to bind alendronate. Due to the risk of esophageal irritation, vomiting should not be induced and the patient should be kept in an upright position.
Side effects
Immune system disorders: Hypersensitivity reactions, including urticaria, allergic reactions and angioedema.
From the nervous system: headache, dizziness, taste disturbance (bitter or unusual taste in the mouth after taking the drug).
From the organ of vision: uveitis, scleritis, episcleritis.
From the organ of hearing and balance: vertigo, osteonecrosis of the external auditory canal (belongs to the adverse reactions characteristic of bisphosphonates).
Gastrointestinal: abdominal pain, dyspepsia, constipation, diarrhea, flatulence, ulcers of the oral cavity, pharynx and esophagus, dysphagia, abdominal wall tension, heartburn, regurgitation of gastric contents, nausea, vomiting, gastritis, esophagitis, esophageal erosion, esophageal strictures, perforation, ulcer, gastrointestinal bleeding (including oral cavity, pharynx, esophagus, stomach), melena.
Skin and subcutaneous tissue disorders: rash, itching, erythema (redness); rashes aggravated by exposure to light (photosensitivity reactions); severe skin reactions including Stevens-Johnson syndrome and toxic epidermal necrolysis; hair loss (alopecia).
Musculoskeletal and connective tissue disorders: bone, muscle or joint pain, osteonecrosis of the jaw, atypical femoral fractures, joint swelling.
Metabolic disorders: hypocalcemia with corresponding clinical symptoms, often in connection with the presence of provoking factors.
General disorders: transient symptoms (muscle pain, malaise and in rare cases fever), which usually occur at the beginning of treatment, asthenia, peripheral edema.
Investigations: hypocalcemia, hypophosphatemia (when treated with alendronate 10 mg/kg per day).
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C in the original packaging.
Keep out of reach of children.
Packaging
4 tablets in a blister. 1 blister in a cardboard box.
Vacation category
According to the recipe.
Producer
KUSUM HEALTHCARE PVT LTD/KUSUM HEALTHCARE PVT LTD.
Address
SP-289 (A), RIICO Industrial area, Chopanki, Bhiwadi, Dist. Alwar (Rajasthan), India/SP-289 (A), RIICO Industrial area, Chopanki, Bhiwadi, Dist. Alwar (Rajasthan), India.
