Alendronic acid

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

Pharmaceutical form, composition and packaging

Pills white or nearly white, lenticular, without risk.

Excipients: low substituted hydroxypropyl cellulose, hydroksypropyltsellyuloza, colloidal silicon dioxide, stearil sodium fumarate.

10 PC. – blisters (3) – packs cardboard.

Pills white or nearly white, round, flat, chamfered, Engraved “T” on one side and flat – with another.

Excipients: microcrystalline cellulose, sodium croscarmellose, magnesium stearate.

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

Pharmacological action

Bone resorption inhibitor, belongs to the group of aminobisphosphonates – synthetic analogs of pyrophosphate, binding to hydroxyapatite, part of the bone tissue. Increases the mineral density of the bones of the spine and other bones of the skeleton. The mechanism of antiresorbent action is associated with the suppression of osteoclast function. Promotes the formation of bone tissue with normal histological structure.

Pharmacokinetics

Absorption

When taken orally on an empty stomach in a dose range from 5 to 70 mg directly behind 2 h before breakfast, the bioavailability of alendronic acid in women is 0.64%, males – 0.6%. The bioavailability of alendronic acid is reduced by 40% when taken on an empty stomach for 1-1.5 hours before breakfast. After drinking coffee and orange juice, bioavailability decreases by about 60%.

Distribution

The binding of alendronic acid to blood plasma proteins is about 78%. The drug is distributed into soft tissues, and then quickly redistributes to bones, where does it commit, or excreted in urine.

The concentration of the drug in blood plasma after oral administration in a therapeutic dose is below the possible detection limit (<5 ng / ml).

Metabolism

Does not undergo biotransformation.

Deduction

Excreted unchanged. The elimination process is characterized by a rapid decrease in the concentration of alendronic acid in the blood plasma and an extremely slow release from the bones.

The final T_1/2 more than 10 years, which reflects the release of the drug from the bone tissue.

Testimony

- treatment of postmenopausal osteoporosis;

- Osteoporosis, caused by the use of GCS.

Dosage regimen

To ensure normal absorption of the drug and reduce the risk of adverse reactions, recommendations for use and dosage should be strictly followed.

Tevanat drug^® appointed interior 1 tab. 10 mg 1 time / day or 1 tab. 70 mg 1 once a week.

The pill is taken whole, with a glass of water for at least 30 min before the first meal, drinks or other medicines. The drug is washed down only with plain water, since other drinks (including mineral water), foods and certain drugs can reduce the bioavailability of alendronic acid. Tablets should not be chewed or sucked..

After taking the drug, the patient must maintain an upright position (standing or sitting) for not less than 30 m. Do not take medication before bedtime or before the morning lifting from the bed.

Side effect

From the digestive system: stomach ache, dyspeptic symptoms (constipation or diarrhea, flatulence, nausea and vomiting), dysphagia, ulcerative lesions of the esophageal mucosa, disorders of the stomach, ground, heartburn; rarely – esophagitis, erosion of the esophageal mucosa, ulceration of the mucous membranes of the mouth, throat, stomach and duodenum.

On the part of the musculoskeletal system: myalgia, arthralgia, ossalgia.

Metabolism: asymptomatic hypocalcemia, gipofosfatemiя.

On the part of the organ of vision: rarely – uveitis, scleritis.

CNS: headache; rarely – irritability.

Dermatological reactions: rarely – эritema, dermahemia.

Allergic reactions: rarely – skin rash.

Contraindications

- Hypocalcemia;

- State, lead to slower moving food to the esophagus (incl. strictures or achalasia of the esophagus);

- inability of the patient to stand or sit upright for at least 30 m;

- Severe renal insufficiency (CC less than 35 ml / min);

- Severe disorders of mineral metabolism;

- Children's age;

- Pregnancy;

- Lactation (breast-feeding);

- Hypersensitivity to the drug.

Pregnancy and lactation

The drug is contraindicated in pregnancy and lactation (breast-feeding).

Cautions

The possibility of any signs of adverse reactions from the esophagus should be especially carefully monitored.. The patient should be informed about the need to stop taking the drug and consult a doctor if dysphagia develops., pain when swallowing, chest pain or heartburn.

It is necessary to inform the patient about the possible risk of damage to the esophageal mucosa if the instructions for use are not followed..

The drug should be used with caution in case of gastrointestinal diseases in the acute phase. (dysphagia, esophagitis, gastrit, duodenitis, gastric ulcer and duodenal ulcer), hypovitaminosis D.

In patients with hypocalcemia before starting Tevanat^® correction of mineral metabolism disorders is necessary, incl. hypovitaminosis D. During treatment, a slight asymptomatic decrease in serum calcium and phosphate concentration is possible due to the positive effect of alendronic acid on bone mineral density, what is of particular importance to patients, receiving corticosteroids, as they may have reduced calcium absorption.

When taking Tevanat^® (especially with GKS) it is necessary to ensure an adequate intake of calcium and vitamin D with food or in the form of drugs.

The absorption of bisphosphonates is greatly reduced with concurrent food intake.

Effects on ability to drive vehicles and operate machinery

The drug does not affect the ability to drive vehicles and work with mechanisms.

Overdose

Symptoms: possible hypocalcemia, gipofosfatemiя, diarrhea, heartburn, esophagitis, erosive and ulcerative lesions of the gastrointestinal tract.

Treatment: taking milk or an antacid to bind alendronic acid. Due to the risk of esophageal irritation, do not induce vomiting.. The patient must be in an upright position.

Drug Interactions

Combined use of alendronic acid (but not simultaneous reception) with estrogen preparations, is not accompanied by a change in their action and the development of side effects.

Simultaneous reception of alendronic acid with drugs is not allowed, containing calcium, antacids or other medicinal products for oral use due to a possible decrease in the absorption of alendronic acid. In this regard, it is necessary to observe the interval, at least, 30 minutes after taking alendronic acid and before taking other drugs orally.

Oral prednisolone intake is not accompanied by clinically significant changes in the bioavailability of alendronic acid.

NSAIDs increase the side effects of alendronic acid on the gastrointestinal tract.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children at or above 30 ° C. Shelf life of the drug in tablet form 10 mg – 3 year, in the form of tablets 70 mg – 2.5 year.