OSTALON

Active material: Alendronate
When ATH: M05BA04
CCF: An inhibitor of bone resorption in osteoporosis
ICD-10 codes (testimony): M80, M81.0, M81.1, M81.4
When CSF: 16.04.04.01
Manufacturer: RICHTER RICHTER Ltd. (Hungary)

Pharmaceutical form, composition and packaging

Pills, coated white, round, lenticular, Engraved “M14” on one side.

Excipients: microcrystalline cellulose, colloidal silicon dioxide, Croscarmellose sodium, magnesium stearate.

The composition of the shell: Chandelier CLEAR PM 103 (microcrystalline cellulose, karraginan, macrogol 8000)

4 PC. – blisters (1) – packs cardboard.

Pharmacological action

An inhibitor of bone resorption in osteoporosis. Alendronate sodium is a bisphosphonate, a synthetic analogue of pyrophosphate, binding hydroxyapatite bone.

As a non-hormonal specific inhibitor of osteoclast activity, inhibits bone resorption. No effect on the formation of bone tissue. It stimulates bone formation, restores a positive balance between resorption and bone repair. Progressive increases bone mineral density (regulates calcium and phosphorus metabolism), promotes the formation of normal bone structure and structure.

Pharmacokinetics

Absorption

After a single oral dose in the morning on an empty stomach (for 2 hours before breakfast) dose 35 mg or 70 mg of absorption 0.64%; with a shortened interval between taking the drug and food – 0.46-0.39%. This decrease in absorption has no significant impact on the effectiveness of the drug. Simultaneous treatment with coffee or orange juice reduced bioavailability of alendronate sodium 60%.

Distribution

After oral alendronate sodium temporarily distributed in soft tissues, then rapidly embedded in the bone tissue. Plasma protein binding – 78%.

Metabolism

Data, supporting metabolism of alendronate in humans, no.

Deduction

Absorbirovannыy, but it is not embedded in the bone alendronate sodium is rapidly excreted in the urine. The maximum satiating power of bone tissue in animals was unable to establish with a / in the introduction of the cumulative daily dose, of equal 35 mg / kg. Despite the lack of evidence, kidney diseases likely to decrease clearance of alendronate with increased accumulation in the bone.

Testimony

- Treatment of osteoporosis in postmenopausal women (reducing the risk of fractures of the spinal vertebrae, head hipbone);

- Treatment of osteoporosis in men (reducing the risk of fractures of the spinal vertebrae, pelvic bones);

- Osteoporosis, caused by prolonged use of corticosteroids.

Dosage regimen

The drug should be taken on 70 mg 1 once a week. For optimal absorbability Ostalon^® It should be taken in the morning on an empty stomach 2 no (no less 30 m) before the first ingestion of food or liquid, drank plain drinking water. Other drinks (in t. no. mineral water), food, a number of drugs may impair the absorption of alendronate.

To avoid local irritation of the oral cavity and esophagus in the morning, immediately after getting out of bed should drink at least 200 ml of plain water, then take the pill, not liquid and not allowing it to dissolve in your mouth, during subsequent 30 min should not take the horizontal position of the body. On expiry of this period breakfast.

You can not take a pill in the morning, to rise from the bed or in the evening, after bedtime.

Treatment with alendronate should be complemented by the use of calcium and vitamin D.

In elderly patients correction dose is not required.

At CC > 35 ml / min, dose adjustment is not required, at severe renal insufficiency prescribed the drug is not recommended due to lack of clinical experience.

Side effect

From the digestive system: often (≥1/100, <1/10) – stomach ache, dyspepsia, constipation, diarrhea, flatulence, esophageal ulcer, dysphagia, abdominal distention, heartburn; sometimes (≥1/1000, <1/100) – nausea, vomiting, gastritis, esophagitis, erosion of the esophagus, ground; rarely (≥1/10 000, <1/1000) – esophagostenosis, orofaringealynaya ulcer, perforation of the upper gastrointestinal tract, ulcer, bleeding (relationship to treatment is not always straightforward).

On the part of the musculoskeletal system: often (≥1/100, <1/10) – ostalgiya, arthralgia, myalgia.

CNS: often (≥1/100, <1/10) – headache, irritability.

From the senses: rarely (≥1/10 000, <1/1000) – uveitis, scleritis.

Dermatological reactions: sometimes (≥1/1000, <1/100) – itch, dermahemia, rash; rarely (1/10 000, <1/1000) – photosensitivity.

Metabolism: rarely (≥1/10 000, <1/1000) – hypocalcemia (often accompanied by predisposing factors), gipofosfatemiя.

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

Other: rarely (≥1/10 000, <1/1000) – transient symptoms, resembling an acute phase reaction (myalgia, weakness, bad feeling, rarely – high body temperature), most often develop in early treatment.

Contraindications

- Abnormalities of the esophagus and other factors, obstruct the esophagus (incl. axalazija, stricture);

- Hypocalcemia;

- Chronic renal failure (CC<35 ml / min);

- Vitamin D deficiency;

- Severe disorders of mineral metabolism;

- The inability of the patient to remain in an upright position, even sitting, during 30 m;

- Pregnancy;

- Lactation (breast-feeding);

- Children's age;

- Hypersensitivity to the drug.

FROM caution use in patients with gastrointestinal diseases in acute phase (dysphagia, esophageal disease, gastritis, duodenitis, ulcer; in the previous 12 months – pepticheskaya ulcer, gastrointestinal bleeding, surgical intervention, except for operations on spastic pylorus).

Pregnancy and lactation

Application Ostalona^® during pregnancy and lactation is contraindicated.

Cautions

Alendronate can cause local irritation of the gastrointestinal tract. The flow of upper gastrointestinal diseases may worsen during treatment Ostalonom^®.

There are cases of adverse reactions on the part of the esophagus (esophagitis, ulcer or erosion of the esophagus), sometimes be severe, requiring hospital treatment, and is complicated by the formation of strictures. It should pay special attention to the patients, that when the signs of irritation of the esophagus (dysphagia, chest pain when swallowing, the emergence or worsening bouts of heartburn) should stop taking the drug and seek medical advice. The risk of esophageal higher in patients, do not comply with the rules of the drug, or to continue treatment despite the appearance of signs of irritation of the esophagus.

It should warn patients, that in case of missing the next dose, missed tablet should be taken the following morning. In no case should not be taken 2 Tablets in one day.

Treatment can be started only after the elimination of hypocalcemia, disorders of mineral and vitamin exchanges (eg, vitamin D deficiency). Use of alendronate increases the content of mineral salts in the bone, It may be accompanied by a change in asymptomatic levels of calcium and phosphorus. Providing appropriate intake of calcium and vitamin D is particularly important in the case of simultaneous treatment of the patient GCS.

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

Effects on ability to drive vehicles and management mechanisms

The drug does not affect the ability to drive and perform the work, associated with a high risk of injury, However, the presence of adverse reactions from the body of driving and operating mechanisms are contraindicated until the complete disappearance of adverse reactions.

Overdose

Symptoms: hypocalcemia, gipofosfatemiя, adverse reactions from the upper gastrointestinal tract (heartburn, esophagitis, gastritis, ulcer).

Treatment: No specific treatment, recommended intake of milk, Antacids. To avoid irritation of the esophagus do not induce vomiting, the patient should be given a vertical position (standing or sitting).

Drug Interactions

Calcium, antacids, certain drugs for oral administration, food, beverages (incl. mineral water) affect the absorption of alendronate – drugs can be taken orally Minimum, than 1 h after administration Ostalona^®.

Other, except that the absorbability, Interaction unlikely.

Ranitidine increases the bioavailability (the clinical significance is unknown).

NSAIDs increase the adverse effects of alendronate.

Specific drug interaction studies have not performed, However, this study involved patients with Alendronate, who received other drugs inside. There were no side effects, associated with the simultaneous reception of other drugs.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at temperature from 15 ° to 30 ° C. Shelf life – 2 year.