Alendronic acid + Kololecalciferol - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Correctors of bone and cartilage tissue metabolism

Included in the formulation

Fosavans®

pills inwards

MERC SHARP and DOMA IDEA, Inc. Switzerland

АТХ:

M.05.B.B.03 Alendronic acid and colcalciferol

Pharmacodynamics:

Combined drug for the treatment of osteoporosis.

Alendronic acid

Refers to the group of bisphosphonates, inhibits bone resorption in malignant tumors and bone metastases. It suppresses the activity of osteoclasts, causes damage to their structure, decreases in size and quantity.

Selectively affects the bone tissue. Reduces the severity of pain in osteoporosis and metastatic bone damage. Effectively reduces the level of calcium in the blood plasma, preventing the development of clinical signs of hypercalcemia and hypercalcaemic coma.

In the treatment of osteoporosis, the mass of bone tissue increases by the end of the first year of therapy, especially in the spine. As an alternative to hormone replacement therapy can be used in postmenopausal osteoporosis. When an overdose affects osteoblasts, and the mineralization of bone tissue (osteomalacia) is disturbed.

Kolekaltsiferol

Increases the permeability of the intestinal mucosa for calcium and phosphorus ions, promotes their deposition in bone tissue. Participates in the process of reabsorption of phosphates in the renal tubules.

Pharmacokinetics:

Alendronic acid

After oral administration, an empty stomach is absorbed up to 25% in the gastrointestinal tract, followed by deposition in bone and cartilage tissue. The connection with plasma proteins is 78%.

Not exposed to metabolism.

The half-life of plasma is 6 hours, of bone tissue - more than 10 years. Elimination by the kidneys and with feces.

Kolekaltsiferol

After oral administration, up to 90% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 12 hours.

Metabolism in the liver to 25-hydroxyvitamin D₃, which circulates in the blood, associated with vitamin D-binding protein.

The half-life is 24 hours. Elimination by the kidneys in the form of metabolites.

Indications:

It is used for the treatment of Paget's disease and in osteoporosis: in postmenopause, in order to prevent fractures in men, due to prolonged use of glucocorticosteroids.

ICD-10

XIII.M80-M85.M80 Osteoporosis with pathological fracture

XIII.M80-M85.M81.4 Medicinal osteoporosis

XIII.M80-M85.M81.1 Osteoporosis after removal of ovaries

XIII.M80-M85.M81.0 Postmenopausal osteoporosis

XIII.M86-M90.M89.5 Osteolysis

Contraindications:

Chronic renal failure, hypervitaminosis D, abnormalities and pathologies of the gastrointestinal tract, accompanied by obstruction of the esophagus, individual intolerance, children under 18 years of age.

Carefully:

Diseases of the gastrointestinal tract: dysphagia, gastritis, duodenitis, peptic ulcer in the acute stage, active gastrointestinal bleeding or surgical operation on the upper divisions gastrointestinal tract in the anamnesis.

Pregnancy and lactation:

Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside for 1 tablet (70 mg / 70 mcg) 1 time per week.

The highest daily dose: (70 mg / 70 μg).

The highest single dose: (70 mg / 70 mcg).

Side effects:

Alendronic acid

Central and peripheral nervous system: headache, dizziness, agitation, insomnia or drowsiness, impaired orientation, convulsions, visual hallucinations.

Hemopoietic system: anemia, leukopenia, thrombocythemia.

The cardiovascular system: exacerbation of heart disease, increase or decrease in blood pressure.

Digestive system: anorexia, abdominal pain, dyspepsia, rarely gastritis.

Musculoskeletal system: pain in the lower back, in the bones, myalgia, arthralgia.

Sense organs: conjunctivitis, scleritis, rarely xantopsy.

urinary system: development of acute renal failure, hematuria, urinary tract infection.

Allergic reactions.

Kolekaltsiferol

Central and peripheral nervous system: dizziness, fatigue, weakness, drowsiness.

The cardiovascular system: tachycardia.

Digestive system: dry mouth, nausea, vomiting, anorexia, discomfort in the epigastric region, constipation.

urinary system: Hyphosphatemia.

Dermatological reactions: itching, skin rash.

Allergic reactions.

Overdose:

Alendronic acid

Hypocalcemia: arterial hypotension, tetany, paresthesia.

Treatment: intravenous administration of calcium gluconate.

Kolekaltsiferol

Chronic overdose: anorexia, pathological demineralization of bones, calcium deposition in vessels, heart, kidneys, intestines.

Acute overdose: fever, headache, arrhythmia, hypercalcemia, proteinuria, leukocyturia, cylindruria.

In hypercalcemic crisis intravenous administration of 0.9% sodium chloride solution with addition of loop diuretics (ethacrynic acid or furosemide) is indicated. Effective dialysis.

Interaction:

Alendronic acid

Simultaneous use of aminoglycosides increases the risk of hypocalcemia.

Drugs containing divalent cations (Ca, Fe, Mn, Mg, etc.), easily form bonds with alendronic acid, so these drugs can not be taken concurrently.

Ranitidine improves bioavailability.

Mineral water and juices degrade the absorption of the drug.

Nonsteroidal anti-inflammatory drugs increase side effects.

Kolekaltsiferol

Strengthens the action of cardiac glycosides.

Simultaneous reception of barbiturates and anticonvulsants reduces the effect of dihydrotachysterol.

Vitamin A, tocopherol, ascorbic acid, thiamine, pantothenic acid, riboflavin weaken the toxic effect of colcalciferol.

Special instructions:

Alendronic acid

To avoid irritation of the mucosa of the esophagus, it is recommended to take the tablet with ordinary water in an amount of not less than 200 ml and Do not take the horizontal position of the body.

During treatment, you need to consume enough fluids and restrict the intake of foods that contain calcium.

Kolekaltsiferol

With prolonged use, it is necessary to monitor the concentration of calcium ions in blood plasma and urine. The serum calcium level should be 1.9-2.5 mmol / l.

In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

Instructions

Alendronic acid + Kololecalciferol (Acidum alendronicum + Colecalciferolum)