Zoledronic acid - instructions for use, dose, side effects, contraindications

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.

Pharmacokinetics:

After intravenous administration, it is distributed in an equilibrium state, followed by deposition in bone and cartilage tissue. The connection with plasma proteins is 43-55%.

Not exposed to metabolism.

The half-life of plasma is 146 hours. Elimination of the kidneys unchanged.

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.M81.0 Postmenopausal osteoporosis

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

XIII.M80-M85.M81.4 Medicinal osteoporosis

XIII.M86-M90.M89.5 Osteolysis

Contraindications:

Chronic renal failure, vitamin D deficiency, abnormalities and pathologies of the gastrointestinal tract, accompanying the obstruction of the esophagus, individual intolerance, children under 18 years of age.

Carefully:

Hypovitaminosis D, 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 D. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Intravenously, drop by 5 mg (in 1 vial - 100 ml of solution) once a year.

The highest daily dose: 5 mg.

The highest single dose: 5 mg.

Side effects:

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.

Overdose:

Hypocalcemia: arterial hypotension, tetany, paresthesia.

Treatment: intravenous administration of calcium gluconate.

Interaction:

Simultaneous use of aminoglycosides increases the risk of hypocalcemia.

Drugs containing divalent cations (Ca, Fe, Mn, Mg, etc.), easily form bonds with zoledronic 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.

Special instructions:

After the infusion of the drug throughout the year, patients should take calcium and vitamin D preparations.

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

Instructions

Zoledronic acid (Acidum zoledronicum)