Zoledronic acid, first patented by Swiss scientists from Novartis, is currently on sale under a variety of names. The drug is widely used as an element of the complex therapy of osteochondrosis. It is quite successfully used in the treatment of certain types of malignant neoplasms. The tool stops the processes of bone resorption. On sale are bottles containing white powder or a porous mass that absorbs well.
Pharmacology
As indicated in the instructions of zoledronic acid, the use of the drug is possible in a situation where aminobisphosphonates are indicated. These compounds, and especially the medication under consideration, have a pronounced selective effect in relation to bone tissue. Scientists have not yet found out exactly how the tool works, by what mechanism affects the human body, but it was possible to prove that the active substance is distinguished by its affinity for mineralized bones, which means it can inhibit degenerative processes. At the same time, clinical trials have shown that zoledronic acid does not show a negative effect on bone formation processes, does not correct its chemical composition, elasticity, and physical strength.
Once in the human body, the substance quickly affects the bone marrow at the microscopic level. This stops the development of atypical cell formations. According to the instructions for use, zoledronic acid simultaneously eliminates pain and fights tumors. In parallel, inhibition of the formation of endothelial cells is observed. If the cancer is associated with excess calcium, the concentration of this component under the influence of the agent in question gradually returns to normal, which improves the quality of the functioning of the vascular system.
Osteoporosis: effective and efficient
Zoledronic acid preparations are widely used in the treatment of osteoporosis in patients of different age groups. Proper medication helps to normalize metabolic processes. In a short time, indicators are stabilized to the biological human norm, then they are maintained in this state for a long period. On average, under the influence of the drug, the parameters of metabolic processes characteristic of premenopause are established. An annual infusion does not progress towards a decrease in the number of exchange markers in the tissues of the skeletal system.
Pharmacokinetics
Treatment with zoledronic acid involves the intravenous infusion of a powder dissolved in a special liquid (the acid is practically insoluble in water). Immediately after the start of the procedure, a sharp increase in the concentration of the substance in the blood plasma is observed. The highest rate is recorded at the time of completion of the infusion. The decrease in concentration is also rapid, only after a day, zoledronic acid decreases in concentration and reaches no more than one percent relative to the maximum value obtained at the time of infusion. A long time period in the circulatory system, the substance is present in an amount of 0.1% of the largest.
No cumulative effect is observed. The use of zoledronic acid must strictly comply with the rules of use of the drug. In this case, it is taken into account that the substance from the body is excreted in the urine. The process is three-stage. The first step is 0.25-1.87 hours, then the longer the second. The total elimination half-life is 146 hours.
When will it help?
The use of zoledronic acid is indicated for:
- Osteoporosis diagnosed after menopause.
- Osteoporosis caused by prolonged use of glucocorticosteroids.
- Osteodystrophy, provoking deformation.
In the period after menopause, zoledronic acid helps prevent fractures provoked by a decrease in skeletal strength.
Preparations based on this compound have shown good results as an element of the therapeutic course with an excess of calcium in the body. Often this is observed against the background of malignant tumor processes, cancer, which metastases to the bone tissue.
Categorically not
As indicated in the instructions, zoledronic acid is not used if the patient has an allergic reaction to this substance or hypersensitivity to it. It is unacceptable to undergo a course of treatment during the period of bearing a child, breastfeeding a baby. Zoledronic acid is not approved for the treatment of juvenile patients and persons whose body is deficient in calcium. You can not use the composition if the kidneys are not functioning actively enough, creatine clearance is estimated at 35 ml / min or less.
You can, but very carefully
The instructions for zoledronic acid contain indications of the possibility of using the medication for severe liver diseases, but only in conditions where it is possible to constantly monitor the patient's condition and take indicators of functioning that are important for life. Similar conditions apply to the use of a medication for aspirin bronchial asthma. In these cases, the doctor first analyzes how great the risks are for the patient and what positive aspects are associated with the use of this particular medication, then he introduces the patient to the possible dangers and consequences of the course of treatment. Only on the basis of a detailed analysis can a final decision be made on the reasonableness of the use of zoledronic acid in this case.
Special occasion
Zoledronic acid cannot be used to treat juvenile patients, since there is no official information to support its safety. There is no information confirming the effectiveness of drugs based on this substance. For similar reasons, the drug is not used in the treatment of pregnant, lactating mothers. There is no information about what the consequences of the use of the medication can provoke for patients suffering from impaired renal function, liver. In general, acid treatment is not recommended, although occasionally doctors can offer such an option, but only by arguing it with really important arguments.
According to reviews, zoledronic acid is used in the treatment of individuals with kidney abnormalities. If at the same time the creatine clearance exceeds the parameter of 35 ml / min, you can safely use the medication without adjusting the standard scheme.
Negative effects
It is known that the use of the described medication can cause a negative response of the body. From medical practice, the following side effects are possible with zoledronic acid:
- It hurts, dizzy.
- The patient is worried, worried.
- Temporary blurred consciousness.
- Sleep disturbance.
- Shortness of breath and coughing.
- Violation of the stool, abdominal pain.
- Inflammatory processes of the mucosa.
- Deterioration in vision.
From the reviews formulated by experts: zoledronic acid can cause taste disorders, lethargy, anorexia, glaucoma. There are cases when the drug provoked skin rashes, kidney failure, allergic reactions. Under the influence of the active component, there may be a violation of pressure (in the upper or lower side relative to the norm), weakening of the heart rhythm.
More often the negative response of the body is felt at the beginning of the therapeutic course. As is evident from the patient reviews, zoledronic acid first becomes the cause of a fever, pain, which disappears within 72 hours after the first injection of the substance.
How to use?
The most commonly used drug, as mentioned above, in the treatment of osteoporosis, in oncology. Zoledronic acid should be used strictly under the supervision of a doctor. Do not use this compound at home. It is not allowed to use acid-based medicines on your own.
According to the rules, the substance is injected into a vein, the infusion lasts more than a quarter of an hour. The solution should be prepared in absolute sterility. The standard dose involves the dilution of 4 g of the substance in 5 ml of liquid. The finished product is mixed with 100 ml of saline or dextrose (concentration - 5%). The finished product must be used immediately, storage is not allowed. The composition is recommended to be used once a year.
Important aspects
As can be seen from the patient reviews, zoledronic acid in oncology, the treatment of osteoporosis is used strictly under the supervision of a doctor, otherwise the likelihood of side effects and worsening of the patient's condition is high. Before starting the procedure, the doctor checks that the patient has consumed a sufficient amount of drink. This is required in the treatment process. It is important to ensure the flow of fluid in an adequate volume, avoiding its overabundance, so the drinking process is under the supervision of a doctor, and specific quantities are calculated taking into account the individual characteristics of the patient.
It is necessary to analyze the diet of the patient. If with food a person receives insufficient vitamin D, calcium, it is important to provide an additional influx of these compounds to prevent their insufficiency.
Too much!
With the introduction of too much, there are signs of an overdose. Zoledronic acid negatively affects the functioning of the kidneys, laboratory tests show a lack of magnesium, phosphorus, calcium deficiency. The main task of the doctor is the symptomatic treatment of a lack of minerals in the tissues of the body. Injections of the patient urgently injected with magnesium sulfate, calcium gluconate, potassium, sodium phosphate. Calcium can be used orally.
Combine: how to?
It is unacceptable to mix zoledronic acid and other substances and compounds in a syringe. When using the drug and some types of diuretics, there is a likelihood of mineral deficiency, therefore it is important to monitor the patient's condition. A similar effect is observed when combined with aminocyclitols.
If plasmacytoma is diagnosed in a generalized form, and the therapeutic course involves the use of Thalidomide, the use of zoledronic acid with a high degree of probability can cause a failure of renal functionality.
It is unacceptable to drink alcohol during treatment.
Note!
As a solvent for zoledronic acid, it is not allowed to use substances that contain calcium cations. During therapy, the doctor must monitor the patient's condition, check the concentration of phosphorus, calcium, magnesium in the body. It is necessary to regularly take an analysis of creatine clearance. It is important to inform the patient how the deficiency of minerals in the body is expressed, how to behave at the first suspicion of such changes. If the patient is at risk for mineral deficiency, it is important to constantly monitor the condition of the client.
At the beginning of the therapeutic course, specialized drugs can be taken to alleviate side effects after the first injection. The most common and effective are substances based on ibuprofen and paracetamol. The first on the pharmacy shelves are presented under the trade names "Nurofen", "Mig", the second category is "Panadol" and its analogues.
Since zoledronic acid can have a negative effect on the central nervous system, it is wise to refuse to control transport during treatment with this drug, and also to avoid tasks that require increased care and concentration.
Analogs
Zoledronic acid is an active ingredient in pharmaceutical products:
In some cases, experts advise you to opt for the Belklast drug.
Choosing a specific name, you should consult with your doctor.
In some cases, zoledronic acid can be replaced by other agents from the group of bisphosphonates. On the pharmacy shelves they are presented under the trade names "Bonefos", "Bonviva". A good reputation is the drug "Ibandronate-Teva." In no case can you independently replace the prescribed zoledronic acid with these funds, be sure to coordinate this step with your doctor.
Fighting cancer: going to the next level
According to reviews, zoledronic acid in oncology was almost a breakthrough. Of particular note is the product on the shelves of pharmacies presented as "Rezoskan." This drug is the first on our planet from the category of commercial radiopharmaceuticals, created specifically to detect pathologies of the skeletal system through modern nuclear technology. The main substance "Rezoskana" is the considered zoledronic acid. From all other radiopharmaceutical medicines, Rezoskan differs in its main component. As a targeted carrier, the manufacturer used an acid that has the highest level (when compared with other bisphosphonates) of affinity for regions of high resorption. This helps to quickly and accurately establish the presence of metastases, localize them. "Rezoskan" shows reliable results in the study of patients with different types of neoplasms, provoked by various factors and developed in different areas of the body.
Osteoscintigraphy
Using "Rezoskan", it is possible to quickly detect lytic metastasis, conducting an initial diagnosis. This is especially true if a neoplasm is established in the prostate gland. Based on the information obtained during the study, zoledronic acid can be prescribed in the form of injections. This allows you to start therapy in a timely manner, which means to achieve the maximum effect, to prevent the appearance of metastases in the future.
Using "Rezoskan", it is possible to differentially diagnose degenerative changes due to oncology and other factors. The accuracy of such information is the key to a successfully selected therapeutic course. Diagnostic methods involving the use of Rezoskan help to accurately identify all the features of the patient’s condition if destructive processes in bone tissue are associated with factors that have nothing to do with oncology. This makes the tool an important assistant for the doctor in identifying features of articular pathologies, diseases of the spine.
Oncology: how does it work?
The use of zoledronic acid in the treatment of cancer patients shows good results with a timely started course. In some cases, drugs on this substance are the main component of therapy, but can act as an auxiliary point in the rehabilitation period after chemotherapy.
Like other bisphosphonates, zoledronic acid simultaneously suppresses the growth of atypical cells and prevents bone destruction processes. However, it was not possible to detect negative changes in the tissues of the body caused by the substance. It is believed that zoledronic acid is safe if used in accordance with the instructions, given contraindications. Indeed, the technique is often associated with side effects, but they are all short-lived and quickly go away, the cumulative effect is not observed.
In the treatment of cancer, zoledronic acid is prescribed by the course, the duration of the program is up to a month. Features should be chosen by the doctor, focusing on the type of malignant neoplasm, the patient's condition and the body's response to therapy. In some cases, the duration is up to nine months and a half years. If excess calcium is detected in the body, the frequency of procedures is reduced.
Advantages and disadvantages
Reviews indicate that zoledronic acid quickly shows a positive effect. With oncological diseases, the positive aspects are most pronounced if the patient has previously undergone chemotherapy.
Many patients treated with this remedy note that the most significant drawback is too high a price. Zoledronic acid costs between five and fifteen thousand per bottle. The specific values depend on the manufacturer, the point of sale.