Aclasta solution 50mcg/ml 100ml

Aclasta user manual

Reed more and buy Aclasta on this page

Composition

As part of the solution for infusions, Aclasta contains the active ingredient zoledronic acid monohydrate and additional components: sodium citrate, mannitol, water for injections.

Form of issue

The medicine is in the form of a solution for infusions. It is a clear liquid without color, which is contained in 100 ml polyethylene bottles. The bottles are packed in cardboard boxes.

pharmachologic effect

The drug produces an inhibitory effect of bone resorption. The active substance - zoledronic acid refers to amino bisphosphonates and mainly affects bone tissue, suppressing the resorption of bone tissue and the activity of osteoclasts.
The selective effect of bisphosphonates on bone tissue is based on the affinity for mineralized bone tissue. After the drug Aclasta is administered intravenously, zoledronic acid is actively redistributed into bone tissue and is mainly localized in remodeling sites, like other bisphosphonates. In general, at the molecular level, zoledronic acid in the osteoclast acts on the enzyme farnesyl pyrophosphate synthetase. Also other mechanisms of action of this tool are not excluded.
Zoledronic acid inhibits bone resorption, while not adversely affecting the formation of bone tissue, its mechanical properties and mineralization. The active ingredient dose-dependent decreases the activity of osteoclasts and the frequency of new foci of remodeling in the cortical and trabecular parts of the bone, without provoking the formation of fibrous bone tissue and aberrant accumulation of the osteoid.
If we exclude the anti-resorptive effect, zoledronic acid acts on bone tissue in the same way as other bisphosphonates.
In the treatment of patients with postmenopausal osteoporosis with the drug Aclasta, a decrease in the probability of vertebral fractures by 70% (statistically significant) was noted by the end of the third year of treatment. Also by 60-70%. the risk of manifestation of repeated and new vertebral fractures decreased. In women aged 75 years and over, suffering from osteoporosis, the risk of vertebral fractures decreased by 61%.
In people who used the drug Aclasta, the relative risk of untebral fractures of different localization decreased by 33%. The use of the agent for three years by patients with postmenopausal osteoporosis led to an increase in bone mineral density (BMD) of the lumbar vertebrae, femur.
Treatment for 3 years contributed to a reduction in the period of immobilization in patients with osteoporosis in postmenopausal women and a decrease in the severity of pain.
If the drug Aclasta was administered to a patient with fractures of the proximal femur, there was a 35% decrease in the incidence of osteoporotic fractures in the future.
The use of Aclasta by patients with femoral fractures for two years led to an increase in the BMD of the femur.
A marked increase in the BMD of the lumbar vertebrae was noted in men with primary or secondary osteoporosis, provided that the drug was applied once a year.
Also, BMD increased after Aclasta therapy in people suffering from osteoporosis caused by the use of GCS. At the same time, there was no negative effect on bone structure and mineralization on bone structure.
Positive effects of treatment on patients who suffered from Paget's bone disease, as well as those who had previously been treated with oral bisphosphonates, were noted.
There is evidence that the majority of patients on whom zoledronic acid is administered retain a therapeutic response throughout the treatment period. At the sixth month of treatment, a marked decrease in the pain syndrome after the administration of Aclasta once in a dose of 5 mg is the same as with the administration of 30 mg / day. risedronic acid.

Pharmacokinetics and pharmacodynamics

Pharmacokinetics does not depend on the dose of the drug. As the drug Aclasta is gradually introduced to the patient, a rapid increase in the concentration of zoledronic acid occurs in the plasma. The maximum concentration is achieved at the end of the injection. After the infusion is complete, the level of active substance in the blood begins to decrease. Further, over an extended period, a low concentration of the active component is noted in the plasma. If the infusion time increases from 5 to 15 minutes, the concentration of zoledronic acid at the end of the injection is reduced by 30%, but the bioavailability of the drug remains unchanged. With blood proteins binds to 43-55%, these indices do not depend on concentration. In the body it binds to the bone tissue.
Removal of the medicine occurs through the kidneys. First, a rapid two-phase elimination occurs with a half-life of 0.24 hours and 1.87 hours. Further, a prolonged phase is noted where the final half-life is 146 hours. It is excreted unmodified.
There is no cumulation after repeated use every 28 days.

Indications for use

The drug Aclasta is prescribed to patients suffering from postmenopausal osteoporosis, in order to reduce the likelihood of fractures of the vertebrae, femur, and extravertebral fractures. Also, the drug is prescribed in the following cases:
    to improve bone mineral density;
    in the case of osteoporosis in men;
    to prevent fractures in patients who have already had fractures of the proximal femur;
    with the goal of preventing postmenopausal osteoporosis in women with osteopenia;
    for the treatment and prevention of osteoporosis, provoked by SCS;
    with bone disease Paget.

Contraindications

The remedy should not be taken in such cases:
    at a high level of sensitivity to the components of this agent, as well as to other bisphosphonates;
    during pregnancy and lactation;
    with severe forms of disturbance of mineral metabolism, with hypocalcemia;
    patients under the age of 18, since the safety of taking this remedy has not been studied;
    with severe kidney disease.

Side effects of Aclasta

In the case of intravenous administration of Aclasta in a dose of 5 mg once a year, most adverse reactions in patients were mild or moderate. The most common side effects are those lasting not more than three days:
    fever;
    influenza-like syndrome;
    myalgia, arthralgia;
    headache.
When the drug was administered, the severity of these side effects was significantly reduced.
In the process of treatment, other side effects of Aclasta also appeared, which, according to experts, are related to the use of the drug:
    nervous system: dizziness and headache, paresthesia, tremor, retardation, drowsiness;
    respiratory system: cough and shortness of breath;
    sensory organs: pain in the eyes, conjunctivitis, vertigo;
    digestion: vomiting, nausea, diarrhea, impaired appetite, anorexia, dyspepsia, dry mouth, abdominal pain, esophagitis, constipation;
    skin, subcutaneous tissue: hyperhidrosis, rash, erythema, itching;
    musculoskeletal system, connective tissue: myalgia, arthralgia, back pain, limbs and bones, muscle spasms, shoulder and chest pain, stiffness and weakness in muscles, arthritis;
    hemopoiesis: anemia;
    urinary system: pollakiuria, increased blood creatinine, proteinuria;
    heart and blood vessels: increased blood pressure, redness of the face;
    Infection, infection: influenza, nasopharyngitis;
    other manifestations: influenza-like syndrome, fever, chills, severe fatigue, asthenia, general malaise, peripheral edema, thirst, strong excitability.
In rare cases, local reactions are noted in places where Aclasta is administered in the form of swelling, redness, and soreness.

Aclasta, instructions for use (Method and dosage)

In the appointment of the drug Aclasta instructions for use should be carefully observed by the patient. The solution is administered to the patient intravenously, while a valve infusion system is used, which ensures a constant rate of administration of at least 15 minutes. Before you enter the medicine, you should conduct hydration of the body. This point is especially important in the treatment of people who are already 65 years of age, as well as when injecting the solution to patients who are treated with diuretics.
In order to treat osteoporosis in men and postmenopausal osteoporosis in women, it is recommended to administer 5 mg IV once a year. If the patient receives a little vitamin D and calcium with food, he is additionally prescribed drugs containing these components.
In order to prevent fractures in people with fractures of the proximal femur, a similar dose of medication should be administered intravenously once a year. Those who have had such a recent breakthrough are recommended to take a single dose of vitamin D (up to 125,000 ME) two weeks before the introduction of Aclasta, and also take vitamin D and calcium every day for two weeks. After the infusion over the course of the year, it is necessary to continue taking these medications. It is recommended that Aclasta be administered between 6 and 12 weeks after the operation associated with a fracture of the femur.
In order to treat osteoporosis, which is associated with the treatment of SCS, it is recommended to administer 5 mg of the drug once a year intravenously. Additionally, it is possible to prescribe calcium, vitamin D.
To ensure the prevention of postmenopausal osteoporosis, it is recommended to inject intravenously 5 mg of medication every two years.
Patients with Paget's bone disease are injected intravenously with 5 mg of Aclasta's solution. For ten days after the infusion, people with this diagnosis are recommended to take calcium and vitamin D in a daily dose.
Repeated administration of the solution with Paget's disease is possible only after examinations and appointment of a doctor.
People with liver and kidney disease, as well as elderly patients, do not need to adjust the dosage.
When you apply the solution, you must carefully observe all the rules of asepsis. Do not use the medicine if its color has changed, or there are undissolved particles. The solution should be at room temperature before injection.
Aclasta can not be administered with other medicines, a separate system for intravenous administration should be used to administer the drug. Do not use a solution that remained in the vial after infusion.

Overdose

There is limited information about an overdose of the drug. It is important that after receiving a dose that exceeds the allowable, the patient is under the supervision of a specialist.
In the case of an overdose of zoledronic acid, serious impairment of kidney function can develop, including kidney failure, hypomagnesemia, hypophosphatemia, hypocalcemia. With such manifestations, the patient needs to inject intravenously solutions that contain phosphates, magnesium ions, calcium.

Interaction

There have been no studies, during which the interaction of zoledronic acid with other drugs would be studied.
It is noted incompatibility of the solution with preparations containing calcium, so these medicines can not be used in one system for infusion.
Care should be taken with drugs that have a marked impact on kidney function.

Storage conditions

Store the solution of Aclasta at temperatures up to 25 ° C. After the vial has been opened, it is stored for 24 hours, while the temperature should be 2-8 ° C. Keep out of the reach of children.
Shelf life - 3 years. After the expiry of this period, do not use.

special instructions

Aclasta therapy of people who suffer from Paget's bone disease should be practiced exclusively by specialists who already have experience in the treatment of this ailment.
To reduce the severity and frequency of negative symptoms that occur during the course of the medication in the first three days, immediately after IV drugs, patients may be prescribed Ibuprofen or Paracetamol.
As part of the Zometa medicine, which is used to treat cancer patients, zoledronic acid is also active. But these two drugs can not replace each other. At the same time, they should not be used.
People suffering from hypocalcemia should take vitamin D and calcium preparations before starting therapy. It is also important to provide treatment for other disorders of mineral metabolism.
It is not recommended to apply to Aclasta people suffering from severe impairment of kidney function.
Before the infusion, it is important to determine the level of creatinine in the blood plasma. In patients with kidney disease, the creatinine content should be determined regularly.
With a single infusion, the dose of the drug should not be above 5 mg, the period of administration should last no less than 15 minutes.
To date, there has been no confirmation of the connection of the osteonecrosis of the jaw with the use of bisphosphonates, but it is recommended that dental surgical procedures should not be performed in the treatment of Aclasta, since after such operations the recovery period may increase. Complete dental research and preventive procedures should be performed before starting therapy with bisphosphonates.
There is no evidence that the use of Aclasta influences the patient's response, but in view of the likelihood of negative effects, it is recommended that the vehicle be transported cautiously and perform all actions that require a quick reaction.

Children

Patients under 18 years of age are not prescribed.

In pregnancy and lactation

Do not administer to pregnant women and nursing mothers. There is evidence of a teratogenic effect of the active substance on one of the rodent species.

Reviews about Aclasta

There are very different reviews about Aclasta in the forums, where they discuss problems related to osteoporosis. Often patients who have undergone fractures and have practiced treatment with this drug, write that after receiving it the condition improved. This was confirmed by the results of the examinations and the general condition of the patients. At the same time, many people say that the administration of the medicine is difficult to bear: the body temperature rises, chills, vomiting.
There are also opinions that Aclasta is not an effective remedy, since patients after treatment did not feel better.