Alendronat

General characteristics. Structure:

Active agent:

Alendronat of 10 mg. Contains active agent of an alendronat of sodium of trihydrate of 13,05 mg, in terms of alendronovy acid of 10,00 mg

Alendronat of 70 mg. Contains active agent of an alendronat of sodium of trihydrate of 91,36 mg, in terms of alendronovy acid of 70,00 mg.

Excipients: starch corn (C*Pharm 93000), lactose (sugar moyolochny), magnesium stearate, cellulose microcrystallic.

Description

Tablets of white or almost white color, ploskotsilindrichesky form with a facet or with a facet and risky (a dosage of 70 mg). The insignificant mramornost is allowed.

Pharmacological properties:

Pharmacodynamics. Non-hormonal specific inhibitor of an osteoklastichesky bone resorption (from group of aminobisfosfonat — synthetic analogs of the pyrophosphate connecting the hydroxyapatite which is in a bone), suppresses osteoclasts. Recovers polozhiyotelny 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 with normal histologic structure.

Pharmacokinetics. Bioavailability of alendronovy acid at reception on an empty stomach in 2 hours prior to food — 0,64% (at women) and 0,6% (at men); at reception on an empty stomach in 1–1,5 hours prior to food decreases by 40%. Coffee and orange juice reduces bioavailability by 60%.

Distribution:

The average volume of distribution in a condition of equilibrium concentration (except for bones) at the person makes, at least, 28 l. Concentration of drug in a blood plasma after oral administration in a therapeutic dose is too small for analiticheyosky definition (<5 ng/ml). Linkng with proteins of a blood plasma makes pribliziyotelno 78%.

Metabolism:

 In a human body it is not metabolized.

Removal:

It is removed in not changed look. Process of removal is characterized bystry snizheniyoy concentration of alendronovy acid in a blood plasma and extremely slow vysvobozhyodeniye from bones. At peroral introduction in 6 h concentration in plasma decreases more than by 95%. An elimination half-life — about 10 years that indicates removal of an alendronat from a bone tissue. Absorbed, but not built in kostyony fabric алендронат, it is quickly removed by kidneys. Renal clearance — 71 ml/min., sisyotemny — 200 ml/min.

Indications to use:

- osteoporosis at women in a postmenopause (prevention of fractures of bones, including a hip and a backbone);
- osteoporosis at men;
- the osteoporosis caused by prolonged use of glucocorticosteroid drugs; Pedzhet's disease.

Route of administration and doses:

Alendronat is applied inside, 1 time a day, without chewing, on an empty stomach, not less than in 30 minutes) before the first meal, water or other lekarstvenyony drugs is desirable in 2 hours (but. It is necessary to wash down only with usual water as other drinks, including mineral water, coffee, tea, orange juice reduce absorption. Tablets cannot be chewed or rassasyvat.

After Alendronat's reception the patient has to keep vertical position of a body (standing or sitting) within not less than 30 minutes. It is impossible to accept Alendronat before going to bed or before morning rise from a bed.

The recommended dose makes 1 tablet (10 mg) inside once a day or 1 tablet (70 mg) inside once a week.

For treatment of osteoporosis at women (in a postmenopause) and at men, and also the osteoporosis caused by prolonged use of glucocorticosteroid drugs, Alendronat is accepted on 10 mg/days or on 70 mg once a week.

At Pedzhet's disease it is applied in a dose of 40 mg/days within 6 months. At the accidental admission of administration of drug in the mode once a week it is necessary при­нять one tablet in the morning of the next day. It is not necessary to take two pill in one day, but in the subsequent it is necessary to continue to accept on one tablet in that day of the week which was chosen for reception from the very beginning of treatment.

Features of use:

It is necessary to wash down Alendronat only with usual water as other drinks (including mineral water, coffee, tea, orange juice) reduce absorption of an alendronovy kiyoslota.

Absorption of bisfosfonat substantially decreases at a concomitant use of food.

For reduction of the irritating influence on a gullet Alendronat it is necessary to accept right after morning rise, washing down with a full glass of water. After reception it is necessary to be in vertical position (standing or sitting) within 30 minutes (it is dangerous приме­нять drug in case of inability of the patient to stand or sit directly during ukayozanny time). Alendronat's reception before going to bed or in horizontal position poyovyshat risk of development of an esophagitis.

The patient has to be informed on need of the termination of reception of Alendroyonat and the address to the doctor at development of a dysphagy, emergence of pains when swallowing, pains behind a breast or when developing heartburn.

At a hypocalcemia it is necessary to carry out its correction prior to treatment. Including it is necessary to eliminate the disturbances of mineral exchange leading to a hypocalcemia (deficit of vitamin D, a hypoparathyrosis, calcium malabsorption). Therapy should be provoyodit against the background of the diet enriched with calcium salts.

At reception of bisfosfonat (especially at the accompanying therapy by glyukokortikostero-idny drugs) it is necessary to provide receipt of adequate quantities a kalyyotion and vitamin D with food or in the form of medicines.

In the course of treatment owing to positive impact of alendronovy acid on the mineral density of a bone tissue insignificant bessimptomyony decrease in concentration of calcium and phosphates in blood serum can be observed.

Before purpose of therapy of a bisfosfonatama patients with concurrent factors of risk (for example, cancer, chemotherapy, radiation therapy, reception of glucocorticosteroid prepayorat, insufficient hygiene of an oral cavity) need to undergo dental inspection with the corresponding preventive dental care. The patients who are on treatment of a bisfosfonatama should avoid invasive dental procedures whenever possible. It was reported about a jaw osteonecrosis, usually connected with an odontectomy and/or a local infection (including osteomyelitis) at the onkoloyogichesky patients receiving bisfosfonata intravenously (much of them also nayoznachatsya chemotherapy and glucocorticosteroid drugs). There are messages on development of an osteonecrosis of a jaw in patients with osteoporosis against the background of use of bisfo-sonat inside.

At patients, with a jaw osteonecrosis, and the being on therapy of a bisfosfonatama, stoyomatologichesky surgical interventions can lead to an aggravation of symptoms. In need of carrying out surgical interventions it is necessary to consider that the decrease in risk of development of an osteonecrosis of a jaw given about an opportunity after cancellation of a bisfosfonat are absent.

Appointments and recommendations of the attending physician have to be based on individual assessment of a ratio advantage/risk for each patient.

Side effects:

From digestive tract: dysphagy, esophagitis, abdominal pain, heartburn, dyspepsia, lock, diarrhea, meteorism. Seldom — nausea, vomiting, gastritis, a melena, a stricture of a gullet, an ulcer of a mucous membrane of an oral cavity and throat, a gullet ulcer, perforation of a yazyova of a gullet with bleeding.

From a musculoskeletal system: ostealgia, muscles and joints. From a nervous system: headache. From an organ of sight: uveitis, sclerite.

Allergic reactions: seldom — a small tortoiseshell, a Quincke's disease; it was reported about ediyonichny cases of emergence of syndromes of Stephens — Johnson and Layell.

Others: rash, itch, erythema, photodermatosis, symptomatic hypocalcemia. Cases of development of an osteonecrosis upper and a mandible generally at patsiyenyot with oncological diseases against the background of antineoplastic treatment, включающе­го bisfosfonata are described. Risk factors of development of an osteonecrosis are oncological zayobolevaniye, chemotherapy, radiation therapy, treatment by glucocorticosteroids, nedostayotochny hygiene of an oral cavity, local infectious and inflammatory process, vklyuyochy osteomyelitis. In the majority of the described cases the patient against the background of treatment of a bisfosfo-natama made extraction of teeth.

Data of laboratory researches: insignificant and passing decrease in a kontsentrayotion of calcium and phosphates.

Typical symptoms in an initiation of treatment — a mialgiya, an indisposition and, seldom — fever.

Interaction with other medicines:

Simultaneous use of drugs of calcium (including antacids), reduces an abyosorbtion of alendronovy acid. The interval between reception of alendronovy acid and druyogy medicines has to make not less than 30 min.

Non-steroidal anti-inflammatory drugs (including an acetilsalicylic kisloyota) can strengthen side effects of alendronovy acid from a GIT. Reception of glucocorticosteroid drugs inside is not followed by clinically znayochimy changes of bioavailability of alendronovy acid.

Contraindications:

 hypersensitivity to drug components;
- hypocalcemia;
- inability of the patient is in vertical position (to stand or sit пря­мо) within not less than 30 min.;
- heavy renal failure (clearance of creatinine less than 35 ml/min.);
- heavy disturbances of mineral exchange;
- strictures or achalasias of a gullet and other states leading to difficulty of advance of food on a gullet;
- heavy hypoparathyrosis;
- calcium malabsorption;
- lactose intolerance, deficit of lactase, glyukozo-galaktozny malabsorption;
- pregnancy;
- lactation period;
- children's age.

With care:
Diseases of the digestive tract (DT) in an aggravation phase (a dysphagy, an esophagitis, gastritis, a duodenitis, a peptic ulcer of a stomach and a 12-perstny gut), deficit of vitamin D.

Overdose:

Symptoms: a hypocalcemia, a hypophosphatemia, side reactions from the gastrointestinal expenditure (GE) — heartburn, an esophagitis, GIT erosive cankers, diarrhea.

Treatment: milk or kaltsiysoderzhashchy antacids for binding of an alendronovy kisloyota. Owing to risk of emergence of irritation of a gullet it is not necessary to cause vomiting. The patient has to be in vertical position.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 2 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets of 10 mg and 70 mg.

On 10 tablets (for dosages of 10 mg and 70 mg) or 30 tablets (for a dosage of 10 mg) in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.

On 1, 3, 6 blister strip packagings on 10 tablets or on 1, 2 planimetric yacheykoyovy packagings on 30 tablets together with the application instruction place in a pack from a cardboard.