Rezoclastin FS concentrate for a solution of 5 mg ml 6.25 ml
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Active ingredients
Zoledronic acid
Release form
Concentrate
Composition
Zoledronic acid 800 mcg
Pharmacological effect
Resoclastin FS has an inhibitory effect on bone resorption.
Pharmacokinetics
After the start of the infusion, the concentration of zoledronic acid in the plasma increases rapidly, reaching Cmax 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% of Cmax before re-infusion on the 28th day. Zoledronic acid, introduced into / in, is excreted by the kidneys in 3 stages: rapid two-phase elimination from the systemic circulation with T1 / 2 0.24 h and 1.87 h and a long phase with a final T1 / 2 constituting 146 h. Not noted cumulation with repeated administrations every 28 dney.Zoledronovaya acid is not metabolised systemically and excreted by the kidneys in unchanged form. 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 minutes leads to a decrease in the concentration of zoledronic acid by 30% at the end of the infusion, but does not affect the AUC. Less than 3% is excreted in the feces. The kidney clearance of zoledronic acid positively correlates with CK. blood. Plasma protein binding is low (about 50%) and does not depend on the concentration of zoledronic acid.
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 (for reducing the risk of pathological fractures; spinal cord compression; hypercalcemia; , and reducing the need for radiotherapy); postmenopausal form of primary osteoporosis; senile form of primary osteoporosis; secondary osteoporosis; bone disease Pe jet
Contraindications
Hypersensitivity to zoledronic acid, other bisphosphonates or any other components,part of the drug Rezoclastin FS; severe renal failure (Cl creatinine - ≤30 ml / min); pregnancy; breastfeeding period; childhood and adolescence (safety and efficacy have not been established). With caution should be used in such conditions as: renal dysfunction, severe hepatic impairment (no data on the use), bronchial asthma (if patients have hypersensitivity to acetylsalicylic acid).
Use during pregnancy and lactation
Contraindicated in pregnancy and lactation.
Dosage and administration
Resoklastin FS is administered intravenously, for at least 15 minutes. In postmenopausal and senile primary osteoporosis, as well as in secondary osteoporosis to increase bone mineral density, prevent fractures of the vertebral bodies and other skeletal bones, the recommended dose of Rezoklastina 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 bone disease and Paget's recommended single intravenous injection of the drug at a dose of 5 mg. 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 rate 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 later 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: in case of accidental overdose of the drug, the patient should be under constant medical supervision. In the event of hypocalcemia, accompanied by clinical manifestations, it is shown to carry out the infusion of calcium gluconate. Treatment: It is shown to carry out the infusion of calcium gluconate.
Interaction with other drugs
Solutions containing calcium or any divalent cations, in particular Ringer's lactate solution, cannot be used as solvents. When used simultaneously with antineoplastic drugs, diuretics, antibiotics, analgesics, there are no clinically significant interactions. Bisphosphonates and aminoglycosides have a unidirectional effect on serum calcium concentration blood, therefore, with their simultaneous appointment increases the risk of hypocalcemia and hypomagnesemia. It is recommended Care should be taken when using zoledronic acid with drugs that have potentially nephrotoxic effects. Patients with multiple myeloma may have an increased risk of developing renal dysfunction when IV is administered with bisphosphonates in combination with thalidomide. Rezoclastin FS should not be mixed with other drugs.
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.