Ostalon

General characteristics. Structure:

Active components: an alendronata of sodium trihydrate - 91,35 mg (there correspond 70 mg of alendronovy acid).

Excipients. Kernel: cellulose microcrystallic, silicon dioxide colloid, croscarmellose sodium, magnesium stearate.
Cover: To a chandelier Klear of HP 103 (consists of cellulose microcrystallic, каррагинан, a macrogoal 8000).

Pharmacological properties:

Pharmacodynamics. Alendronat of sodium is bisfosfonaty, a synthetic analog of the pyrophosphate connecting a hydroxyapatite of a bone tissue. Being non-hormonal specific inhibitor of activity of osteoclasts, interferes with a resorption of a bone tissue. Does not influence processes of formation of a bone tissue. Stimulates bone formation, recovers positive balance between a resorption and recovery of a bone. Progressively increases the mineral density of bones (regulates phosphorus-calcium exchange), promotes formation of a bone tissue of normal structure and structure.

Pharmacokinetics. Absorbability after a single dose of 35 or 70 mg on an empty stomach for 2 h till a breakfast makes in the morning 0,64%. At the shortened break between administration of drug and food: 0,46-0,39%. Similar decrease in absorbability has no significant effect on efficiency of drug. The concomitant use of coffee or orange juice reduces bioavailability by 60%.
Distribution: after intake it is temporarily distributed in soft tissues, then quickly built in a bone tissue. Communication with proteins of plasma ~ 78%.
Metabolism: the data confirming metabolism of an alendronat in a human body no.
Removal:
Absorbed, but not built in a bone tissue алендронат quickly it is removed by kidneys. The maximum sating ability of a bone tissue at animals it was not succeeded to establish 35 mg/kg at intravenous administration of a cumulative daily dose equal. Despite the absence of proofs, at diseases of kidneys decrease in removal of an alendronat with strengthening of accumulation in a bone tissue is probable.

Indications to use:

Treatment of osteoporosis in a postmenopause (decrease in risk of development of fractures of back vertebras and a head of a coxofemoral bone). Treatment of osteoporosis at men (decrease in risk of development of fractures of back vertebras and pelvic bones).

Route of administration and doses:

The recommended dose: 70 mg once a week. For ensuring optimum absorbability drug should be taken in the morning on an empty stomach, for 2 h (not less than 30 min.) before the first meal or liquid, washing down with simple drinking water. Other drinks, including mineral waters, food, a number of medicines can worsen absorbability of an alendronat.
In order to avoid local irritation of a mucous oral cavity and a gullet in the morning, at once after rise from a bed it is necessary to drink not less than 200 ml of simple water, then to take a pill, without chewing and without allowing it to be dissolved in a mouth, within the next 30 minutes it is impossible to accept horizontal position of a body, after this term it is necessary to accept a breakfast. It is impossible to take a pill in the morning, before rise from a bed or in the evening, after withdrawal to a dream.
Treatment alendronaty should be added with reception of calcium and vitamin D.

Elderly patients: dose adjustment is not required.
Renal failure: if renal filtering> 35 ml/min., correction of a dose is not required, in heavier stages of insufficiency of function of kidneys it is not recommended to appoint drug due to the lack of clinical experience.

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

Features of use:

Alendronat can cause local irritation mucous a digestive tract. The course of diseases of upper parts of a trust can worsen during treatment alendronaty.
Cases of the side reactions from a gullet (an esophagitis, an ulcer or an erosion of a gullet) sometimes proceeding in a severe form, demanding hospitalization, and which were complicated by formation of a stricture are known. It is necessary to draw especially the attention of patients that at emergence of signs of irritation of a gullet (a dysphagy, a retrosternal pain when swallowing, emergence or deterioration in a current of attacks of heartburn), administration of drug it is necessary to stop and see a doctor. The risk of damage of a gullet is higher at the patients who are not following Regulations of Admission of drug, or continuing treatment contrary to emergence of signs of irritation of a gullet. It is extremely important to inform timely patients on value of observance of rules on administration of drug and to be convinced that the patient understood it.
It is necessary to warn patients that in case of the admission of the next dose of drug, the passed pill should be taken the next morning; it is not necessary to take two pill in one day at all.
Treatment can be begun only after elimination of a hypocalcemia, disturbances of mineral and vitamin exchanges (for example, insufficiency of vitamin D). Reception of an alendronat leads to increase in content of mineral salts in a bone tissue, process can be followed by asymptomatic change of levels of calcium and phosphorus. Ensuring the corresponding reception of calcium and vitamin D especially important in case of treatment of the patient with glucocorticosteroid hormonal drugs.
Treatment should be combined with the diet enriched with calcium salts.

Effect of drug on ability to drive the car and mechanisms
does not influence ability to drive the car and to perform the works connected with high risk of traumatism, however in the presence of side reactions from an organ of sight driving and working mechanisms contraindicated until total disappearance of side reactions.

Side effects:

The following side effects are possible. Often (1/100, <1/10):
- From the alimentary system: abdominal pains, dyspepsia, lock, diarrhea, meteorism, gullet ulcer, dysphagy, abdominal distention, heartburn.
- From a musculoskeletal system: ostalgiya, arthralgia, mialgiya.
- From a nervous system: headache, irritability.
Not often (1/1000, <1/100):
The general: itch, rash, dermahemia.
- From the alimentary system: nausea, vomiting, gastritis, esophagitis, gullet erosion, melena. Seldom (1/10000, <1/1000):
The general: allergic reactions (small tortoiseshell, angiodema, syndrome Stephens-Johnson, toxic epidermal necrolysis); the passing symptoms reminding a phase of acute reaction (a mialgiya, weakness, feeling sick, it is rare - high temperature of a body) most often develop in an initiation of treatment; rash; photosensitivity; a hypocalcemia (it is frequent accompanied by the contributing factors).
- From the alimentary system: an esophageal stenosis, an oropharyngeal ulcer, perforation of upper parts of digestive tract, an ulcer, bleeding, however, communication with treatment is not always unambiguous.
- From sense bodys: uveitis, sclerite.
Laboratory indicators: the temporary, poorly expressed symptomless hypocalcemia and a hypophosphatemia.

Interaction with other medicines:

Calcium, antacids, some peroral drugs, food, drinks, including mineral waters influence absorbability of an alendronat; medicines can be accepted inside not earlier than in 1 h after reception of an alendronat.
Other, except for change of absorbability, interactions are a little probable.
Ranitidine increases bioavailability (clinical value is unknown). Non-steroidal anti-inflammatory drugs strengthen adverse effects of alendronovy acid.
Special researches on medicinal interactions were not conducted, however the patients who were at the same time accepting other peroral medicines participated in researches with alendronaty. At the same time they did not observe the side effects connected with a concomitant use of other medicines.

Contraindications:

Hypersensitivity to any of drug components; anomalies of a gullet and other factors complicating passability of a gullet (an achalasia, a stricture, etc.); inability of the patient to remain in vertical position, at least sitting, within 30 minutes; hypocalcemia, chronic renal failure (clearance of creatinine <35 ml/min.), pregnancy, lactation period, children's age, deficit of vitamin D, heavy disturbances of mineral exchange.

With care: diseases of a digestive tract in an aggravation phase (a dysphagy, gullet diseases, gastritis, a duodenitis, an ulcer, a serious disease of digestive tract in the previous 12 months, for example, a round ulcer, gastrointestinal bleeding, surgical intervention, except for operations on a spastic pylorus).

Pregnancy: in view of lack of necessary clinical experience use of an alendronat during pregnancy is contraindicated.
Breastfeeding period: there are no data on penetration into breast milk; reception of an alendronat during feeding by a breast is contraindicated.

Overdose:

Overdose signs: a hypocalcemia, a hypophosphatemia, side reactions from upper parts of a digestive tract (heartburn, an esophagitis, gastritis, an ulcer).
There is no specific treatment. Reception of milk, antacids is recommended. In order to avoid irritation of a gullet it is impossible to cause vomiting, the patient it is necessary to arrange in vertical position (standing or sitting).

Storage conditions:

To store at a temperature of 15-30 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets coated 70 mg.
4 tablets in A1/A1 the blister.
One blister in a cardboard pack with the enclosed application instruction.