Instructions for Rezoclastin (Zoledronic acid)
Concentrate for solution for infusion
Release form:
Infusion solution concentrate
Description:
Infusion solution concentrate 1 ml
zoledroic acid 800μg
ATC codes
M05BA08 Zoledronic acid
Clinical-pharmacological groups / Group affiliation
Bone resorption inhibitor for bone metastases
Active substance:
zoledroic acid
Pharmacotherapy
Bone resorption inhibitor-bisphosphonate
Pharmacological effect:
Bone resorption inhibitor, nitrogen-containing bisphosphonate. It acts mainly on bone, suppresses osteoclasts and bone resorption.
The selective effect of bisphosphonates on bone tissue is based on a high affinity for mineralized bone tissue. Zoledronic acid is rapidly redistributed into bones and, like other bisphosphonates, is localized predominantly in bone remodeling sites.
The main molecular target of zoledronic acid in osteoclast is the enzyme farnesyl pyrophosphate synthetase (FPS)
While the possibility of other mechanisms of action is not excluded. The long period of action is determined by a high affinity for the active FPS centre and a pronounced affinity for mineralized bone tissue.
With the exception of high antiresorbative action, the effects of Zoledronic acid on bone tissue are similar to those of other bisphosphonates.
In addition to the inhibitory effect on bone resorption, Zoledronic acid has antitumor properties that provide therapeutic efficacy in bone metastases.
In vivo: inhibition of osteoclastic bone resorption, changing the microenvironment of the bone marrow, leading to a decrease in the growth of tumor cells; antiangiogenic activity. Suppression of bone resorption is also clinically accompanied by a pronounced decrease in pain.
In vitro: inhibition of osteoblast proliferation, direct cytotoxic and proapoptic activity, synergistic cytostatic effect with antitumor drugs Rezoclastin; antiadhesive/invasive activity.
Zoledronic acid, suppressing proliferation and inducing apoptosis, has a direct antitumor effect on human myeloma cells and breast cancer, and also reduces the penetration of breast cancer cells through the extracellular matrix, which indicates the presence of antimetastatic properties. In addition, Zoledronic acid inhibits the proliferation of human endothelial cells and in animals causes an antiangiogenic effect.
In patients with hypercalcemia caused by a tumor, it was shown that the action of Zoledronic acid is characterized by a decrease in the concentration of calcium in the serum and a decrease in its excretion in the urine.
Testimony Rezoclastin:
Postmenopausal osteoporosis (to reduce the risk of fractures of the femur, vertebrae and extra-vertebrate fractures, to increase bone mineral density); prevention of subsequent (new) osteoporotic fractures in men and women with proximal femoral fractures; osteoporosis in men; Prevention and treatment of osteoporosis caused by the use of GCS; Prevention of postmenopausal osteoporosis (in patients with osteopenia); Pejet's bone disease.
Osteolytic, osteoblastic and mixed bone metastases of solid tumors and osteolytic lesions in multiple myeloma, as part of combination therapy; hypercalciemia caused by a malignant tumor.
Method of administration, course and dosage:
Enter in / in drip.
The dose and treatment regimen depend on the indications from the indications, the treatment regimen used, the therapeutic effectiveness.
Drug Rezoclastin interaction
When both bisphosphonates and aminoglycosides are applied simultaneously, the serum calcium level may remain reduced for longer than required, as an additive effect on the serum calcium concentration is possible.
When used together with preparations potentially having a nephrotoxic effect, the risk of deterioration of kidney function is increased.
Use in pregnancy and breastfeeding
Use in pregnancy and during breastfeeding is contraindicated.
Side Effect:
From the side of the ventilation system: Not often - anaemia.
By metabolism: infrequently, reduced appetite; Incidence unknown - dehydration (resulting from post-exposure events such as fever, vomiting and diarrhea), hypophosphatemia.
From the nervous system: often - headache, dizziness; Not often - inhibition, paresthesia, drowsiness, tremors, fainting, hypestesia, dysgevsia.
Mental disorders: Insomnia and anxiety are rare.
From the viewpoint of: infrequently - conjunctivitis, pain in the eyes, vertigo; Rarely - uveiit, episclerit, irit.
From the side of the hearing and labyrinthine disorders: not often - vertigo.
On the cardiovascular side: infrequently- raised AD, sudden redness of the face; frequency unknown - a marked decrease in AD (in patients with risk factors).
From the respiratory system: Cough, shortness of breath are not common.
From the skin and subcutaneous tissues: Not often - skin rash, hyperhidrosis, skin itching, erythema.
On the digestive side: Often - nausea, vomiting, diarrhea; Not often - dyspepsia, upper abdominal pain, abdominal pain, gastroesophageal reflux, constipation, dry mouth, esophagitis.
From the side of the musculoskeletal system and connective tissue: Often - arthralgia, myalgia, bone pain, back and limb pain; infrequently - neck pain, muscle stiffness, joint swelling, muscle cramps, chest pain of bone-muscle origin, bone-muscle pain, joint stiffness, arthritis, muscle weakness; frequency unknown - osteonecrosis of the jaw.
From the urinary system: Not often - increase of blood creatinine, pollakiuria, proteinuria concentration.
Infectious and parasitic diseases: Not often - flu, nasopharyngitis.
From the immune system: hypersensitivity reactions including anaphylactic reaction, anaphylactic shock, angioedema, bronchospasm, urticaria.
General reactions and disturbances at the site of administration: very often - fever; often - flu-like syndrome, chills, increased fatigue, asthma, pain, general malaise;
Not often - peripheral edema, thirst, acute phase reaction, non-cardiogenic chest pain.
Contraindications for use:
Severe mineral exchange disorders, including hypocalciemia; severe kidney dysfunction (CC <35 ml/min); pregnancy; Breastfeeding period;
Age up to eighteen years; It also has increased sensitivity to zoledronic acid or bisphosphonates.
Nosology (ICD codes) Rezoclastin
C79.5
Secondary malignancy of bones and bone marrow
C90.0
Multiple myeloma
E83.5
Calcium metabolism disorders
M80.0
Postmenopausal osteoporosis with pathological fracture
M80.1
Osteoporosis with pathological fracture after ovarian removal
M80.4
Drug Rezoclastin osteoporosis with pathological fracture
M80.5
Idiopathic osteoporosis with pathological fracture
M81.0
Postmenopausal osteoporosis
M81.1
Osteoporosis after ovarian removal
M81.4
Drug osteoporosis
M81.5
Idiopathic osteoporosis
M81.8
Other osteoporosis (senile osteopause)
M88
Paget's disease (bones) [deformative osteitis]
Dosage form
solution for infusions
