Rezoclastin Pharmstandard concentrate solution for infusion 4mg 5ml fl
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Active ingredients
Zoledronic acid
Release form
Solution
Composition
per 1 ml of concentrate for preparing a solution for infusion active substance: zoledronic acid monohydrate 0.85 mg (corresponds to anhydrous zoledronic acid - 0.80 mg), excipients: D-mannitol 44.0 mg, sodium citrate dihydrate 5.5 mg, water for injection up to 1.0 ml
Pharmacological effect
Rezoclastin FS has a bone resorption inhibitory effect
Pharmacokinetics
After the start of the infusion, serum concentrations increase rapidly, reaching a peak at the end of the infusion, followed by a rapid decrease in concentration by 10% after 4 hours and by less than 1% after 24 hours with a consistently prolonged period of low concentrations not exceeding 0.1% from maximum to repeated infusion on the 28th day. Zoledronic acid, introduced into / in, is excreted by the kidneys in 3 stages: rapid two-phase elimination of the drug from the systemic circulation with T1 / 2 0.24 h and 1.87 h and a long phase with a final T1 / 2 of 146 h. No cumulation is noted with repeated administrations every 28 days. Zoledronic acid does not undergo systemic metabolism and is excreted by the kidneys unchanged. During the first 24 hours, 39 ± 16% of the administered dose is detected in the urine. The remaining amount is mainly associated with bone tissue. Then, slowly, the back release of zoledronic acid from the bone tissue into the systemic circulation and its excretion by the kidneys. Total plasma clearance is 5.04 ± 2.5 l / h. An increase in the infusion time from 5 to 15 min leads to a decrease in the concentration of zoledronic acid by 30% at the end of the infusion, but does not affect the AUC. With feces less than 3% is excreted.
Indications
Hypercalcemia (serum calcium corrected for albumin - ≥12 mg / dL or 3 mmol / L) induced by malignant tumors; metastatic bone lesions in malignant solid tumors and myeloma (to reduce the risk of pathological fractures; compression of the spinal cord; hypercalcemia caused by the tumor, and reduce the need for radiotherapy); postmenopausal primary osteoporosis; senile form of primary osteoporosis; secondary osteoporosis; Paget's bone disease
Contraindications
Hypersensitivity to zoledronic acid, other bisphosphonates, or any other components that make up Resoclastin FS; severe renal failure (Cl creatinine - ≤30 ml / min); pregnancy; breastfeeding period; children and adolescents (safety and efficacy not established)
Precautionary measures
It should be used with caution in such conditions as: renal dysfunction; severe liver failure (no application data); bronchial asthma (in patients with hypersensitivity to acetylsalicylic acid).
Use during pregnancy and lactation
Contraindicated
Dosage and administration
Resoclastin FS is administered intravenously, for at least 15 minutes. For postmenopausal and senile primary osteoporosis, as well as for secondary osteoporosis in order to increase bone mineral density, prevent vertebral body fractures and other skeletal bones, the recommended dose of Resoclastine FS is 5 mg once a year. If the intake of calcium and vitamin D with food is not enough, patients with osteoporosis should also be given calcium and vitamin D supplements. For the treatment of Paget's disease of the bone, a single intravenous administration of the drug in a dose of 5 mg is recommended. Since Pedzhet's bone disease is characterized by a high level of bone metabolism, all patients with this disease are advised to take a daily intake of calcium and vitamin D during the first 10 days after administration of zoledronic acid. Repeated treatment with Paget's disease of zoledronic acid. After the first injection of the drug, there is a long period of remission. Currently, there is no specific data on the re-treatment of Paget's disease of the bone. However, the possibility of repeated administration of the drug can be considered if a disease recurrence is found in patients based on the following criteria: the lack of normalization of serum alkaline phosphatase activity, an increase in its activity over time, and the presence of clinical signs of Paget's disease of the bone detected by medical examination 12 months after the first dose of zoledronic acid
Side effects
Anemia, headache, conjunctivitis, nausea, vomiting, anorexia, bone pain, myalgia, arthralgia, generalized pain, renal dysfunction, Local reactions. Hypophosphatemia, increased serum concentrations of creatinine and urea, hypocalcemia, flu-like syndrome (including general malaise, chills, fever).
Overdose
Symptoms: increased symptoms of hypocalcemia. Treatment: Calcium Gluconate Injection
Interaction with other drugs
With the simultaneous use of bisphosphonates and aminoglycosides, the level of calcium in the serum may remain reduced longer than is required, since an additive effect on the concentration of calcium in the blood serum is possible. With simultaneous use with drugs that potentially have a nephrotoxic effect increases the risk of renal function deterioration.
special instructions
Before infusion should be excluded the presence of dehydration in the patient. If necessary, the introduction of saline is recommended before, during or after the infusion of zoledronic acid. Patient overhydration should be avoided due to the risk of cardiovascular complications. When deciding on the use of Rezoclastin FS in patients with hypercalcemia caused by a malignant tumor, on the background of renal dysfunction, it is necessary to assess the patient's condition and to conclude that the ratio of the potential benefits and possible risks of treatment. After the introduction of the drug requires constant monitoring of the concentration of calcium, magnesium, phosphorus and creatinine in the serum. Against the background of zoledronic acid therapy, kidney function should be carefully monitored. The risk factors for impaired renal function include dehydration, previous renal failure, repeated administration of zoledronic acid or other bisphosphonates, as well as the use of nephrotoxic drugs, and too rapid administration of the drug Rezoclastin FS. It should be borne in mind that the appointment of other bisphosphonates to patients with bronchial asthma, hypersensitive to acetylsalicylic acid, there have been cases of bronchospasm, however, when using zoledronic acid, such cases have not yet been registered.In oncological patients, during treatment with bisphosphonates, including zoledronic acid, cases of osteonecrosis of the jaw are described, and therefore, prior to treatment, it is necessary to provide for a dental examination and in case of risk factors (anemia, coagulopathy, infection, poor hygiene or diseases of the oral cavity, concomitant chemotherapy or radiation therapy, treatment with corticosteroids) to conduct appropriate preventive procedures. During treatment with zoledronic acid, patients with risk factors should, if possible, avoid dental surgery. To reduce the frequency of adverse reactions after infusion of Rezoclastin FS, patients should be prescribed paracetamol or ibuprofen immediately after the introduction of the drug