Zoledronic acid-Farmex (zoledronic acid) concentrate for infusions 4 mg/5 ml. vial №1

Description

Zoledronic acid-Farmex concentrate for infusions 4 mg/5 ml. vial №1

Composition

active substance: zoledronic acid;

5 ml of concentrate contain 4 mg of zoledronic acid anhydrous, corresponding to 4.26 mg of zoledronic acid monohydrate;

Excipients: mannitol (E 421), sodium citrate (E 331), water for injections.

Dosage form

Concentrate for solution for infusion.

Basic physical and chemical properties: transparent colorless solution.

Pharmacotherapeutic group

Agents that affect the structure and mineralization of bones. Bisphosphonates. ATX code M05B A08.

Pharmacological properties

Zoledronic acid-Farmex belongs to a new class of bisphosphonates that have a specific effect on bone tissue. It is one of the most potent inhibitors of osteoclast bone resorption known today.

The selective action of bisphosphonates on bone is based on their high affinity for mineralized bone tissue, but the molecular mechanism that leads to inhibition of osteoclast activity has not yet been elucidated. Animal studies have shown that zoledronic acid inhibits bone resorption without adversely affecting bone formation, mineralization and mechanical properties.

In addition to inhibiting osteoclast bone resorption, zoledronic acid has a direct antitumor effect on cultured myeloma cells and human breast cancer by inhibiting cell proliferation and inducing apoptosis. This indicates that zoledronic acid may have antimetastatic properties. The following properties have been demonstrated in preclinical studies:

in vivo – inhibition of osteoclast bone resorption, which acts on the structure of the microcrystalline matrix of bone, which reduces tumor growth, has antiangiogenic (vascular effect, which reduces the blood supply to the tumor) and analgesic effect;

in vitro – inhibition of osteoblast proliferation, cytostatic action, proapoptostatic action on tumor cells, synergistic cytostatic effect with other antitumor drugs, antiadhesive and antiinvasive action.

Indication

Prevention of symptoms associated with bone lesions (pathological fractures, spinal cord compression, complications after surgery and radiation therapy, or hypercalcemia due to malignancy) in patients with late-stage malignancies.
Treatment of hypercalcemia caused by malignant tumor.

Contraindication:

• hypersensitivity to the active substance (zoledronic acid), other bisphosphonates or to any of the excipients;
• pregnancy or breastfeeding.

Method of application and dosage

Zoledronic acid-Farmex is used only by doctors who have experience in intravenous bisphosphonates.

Before administration, 5 ml of concentrate containing 4 mg of zoledronic acid is diluted in 100 ml of 0.9% sodium chloride solution or 5% glucose solution. The reconstituted solution for infusion is administered as a single intravenous infusion over at least 15 minutes.

The concentrate of this medicinal product Zoledronic acid-Farmex must not be mixed with solutions for infusion containing calcium or other divalent cations, such as lactated Ringer’s solution, it must be administered as a single intravenous infusion using a separate infusion system.

Children

The safety and efficacy of zoledronic acid in children have not been established.

Overdose

Clinical experience in the treatment of acute zoledronic acid overdose is limited. Misuse of zoledronic acid at doses up to 48 mg has been reported. Patients who receive more than the recommended dose should be under constant medical supervision, as possible renal impairment (including renal failure), changes in serum electrolytes (including calcium, phosphate and magnesium) . In case of hypocalcemia, infusion of calcium gluconate is indicated according to clinical indicators. Treatment is symptomatic.

Side effects

Acute reactions, symptoms of which included bone pain, fever, weakness, arthralgia, myalgia, chills, and arthritis with swollen joints, were commonly reported within three days of drug administration. These symptoms usually disappear within a few days.

The following important side effects have been identified with zoledronic acid: renal impairment, jaw necrosis, acute reactions, hypocalcemia, visual impairment, atrial fibrillation, anaphylaxis, interstitial lung disease.

• from the blood and lymphatic system: – anemia;
• from the nervous system: headache;
• from the eyes: conjunctivitis;
• from the gastrointestinal tract: nausea, vomiting, anorexia;
• from the musculoskeletal system, connective tissue: bone pain, myalgia, arthralgia, generalized pain;
• from the kidneys and genitourinary system: renal disorders;
• general disorders and administration site conditions: often fever, flu-like condition (including fatigue, chills, malaise and hot flushes);
• deviations of laboratory parameters: hypophosphatemia, increased creatinine and urea in the blood, hypocalcemia.