Aklasta - Instructions For Use, Indications, Doses, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Aklasta

Instructions for use:

1. 1. Release form and composition
2. 2. Indications for use
3. 3. Contraindications
4. 4. Method of application and dosage
5. 5. Side effects
6. 6. Special instructions
7. 7. Drug interactions
8. 8. Analogs
9. 9. Terms and conditions of storage
10. 10. Terms of dispensing from pharmacies

Prices in online pharmacies:

from 13 400 rub.

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Aklasta is a drug that inhibits bone resorption.

Release form and composition

The dosage form of Aklasta is a solution for infusion: a transparent, colorless liquid (in polyethylene bottles of 100 ml, 1 bottle in a cardboard box).

The composition of 1 bottle (100 ml) includes:

• Active ingredient: zoledronic acid (anhydrous) - 5 mg (zoledronic acid monohydrate - 5.33 mg);
• Auxiliary components: mannitol - 4950 mg; sodium citrate - 30 mg; water for injection - up to 100 ml.

Indications for use

• Postmenopausal osteoporosis (to reduce the risk of fractures of the vertebrae, femur and extravertebral fractures, as well as to increase bone mineral density);
• Osteoporosis caused by the use of glucocorticosteroids (treatment and prevention);
• Postmenopausal osteoporosis in women with osteopenia (prevention);
• Paget's bone disease;
• Prevention of new (subsequent) osteoporotic fractures in women and men with fractures of the proximal femur;
• Osteoporosis in men.

Contraindications

Absolute:

• Disorders of mineral metabolism in severe course, including hypocalcemia;
• Functional renal disorders in severe course (with creatinine clearance <35 ml / min);
• Pregnancy and breastfeeding period;
• Age up to 18 years (the safety profile of Aklasta in this category of patients has not been studied);
• Hypersensitivity to the components of the drug, as well as to any bisphosphonates.

Relative, Aklasta is used with caution in the presence of the following diseases / conditions:

• History of "Aspirin" bronchial asthma;
• Functional kidney disorders of moderate and mild severity;
• Concomitant cancer and history of chemotherapy;
• Severe dehydration;
• Combined use with drugs that can have a significant effect on renal function (for example, aminoglycoside antibiotics or diuretics that cause dehydration).

Method of administration and dosage

Aklasta's solution is administered as an intravenous infusion using a valve infusion system that provides a constant rate of solution infusion for at least 15 minutes.

Adequate hydration of the body must be ensured prior to infusion. This is especially important for elderly patients (≥65 years old), as well as for patients receiving diuretics.

Recommended application scheme:

• Treatment of osteoporosis in men and postmenopausal osteoporosis in women, as well as osteoporosis caused by the use of glucocorticosteroids: 100 ml of solution (5 mg) once a year. In cases where the intake of vitamin D and calcium from food is not enough, additional drugs are prescribed to cover this deficiency;
• Prevention of subsequent fractures in patients with fractures of the proximal femur: 100 ml of solution (5 mg) once a year. For recent (up to 3 months) fractures of the proximal femur, a single administration of high doses of vitamin D (50,000-125,000 IU orally or intramuscularly) is recommended 2 weeks before the first infusion. With a single administration of Aklasta, patients are recommended to take daily oral calcium (1000 mg per day) and vitamin D (800 IU per day) preparations for 14 days before the infusion. These drugs should be taken within one year of the infusion. The first infusion should be carried out 2 or more weeks after surgery;
• Prevention of postmenopausal osteoporosis: 100 ml of solution (5 mg) 1 time in 2 years. In order to decide whether to re-infuse, the risk of fractures and the clinical response to therapy must be assessed annually. In cases where the intake of vitamin D and calcium in the body from food is not enough, women are additionally prescribed drugs to cover this deficiency;
• Treatment of Paget's bone disease: 100 ml of solution (5 mg) once. Transient hypocalcemia may develop during the first 10 days after infusion. While using Aklasta, it is recommended to take a sufficient dose of vitamin D and an adequate dose of calcium (not less than 500 mg of elemental calcium 2 times a day) for at least the first 10 days after administration of the drug;
• Re-treatment of Paget's bone disease: re-administration of 100 ml of solution (5 mg) after 1 year or more from the start of therapy (the duration of the break is determined individually based on the effectiveness of the drug and the results of the study of the level of alkaline phosphatase (should be carried out every 6-12 months). signs of deterioration (in the form of bone pain and compression symptoms) and / or radiological signs of disease progression are absent, the next infusion can be carried out no earlier than 12 months after the first.

If creatinine clearance is ≥35 ml / min, liver dysfunction and elderly patients, dose adjustment is not required.

Aklast should not be mixed or administered together with any other drugs. Do not allow contact with solutions containing calcium or any other divalent cations.

For the administration of Aklasta, it is always necessary to use a separate infusion system.

It is advisable to use the solution immediately after opening the bottle. If the solution is cooled, it is recommended to keep it indoors until it reaches room temperature before administration.

Side effects

Adverse events in the treatment of osteoporosis in men, postmenopausal osteoporosis in women, Paget's bone disease, prevention of subsequent fractures in patients with fractures of the proximal femur, treatment and prevention of osteoporosis associated with the use of glucocorticosteroids, as a rule, are mild to moderate in nature.

Most often, the development of disorders lasting no longer than 3 days was noted in the form of fever, myalgia, flu-like syndrome, arthralgia and headache. With the repeated administration of Aklasta, the severity of adverse reactions significantly decreased.

The frequency of development of disorders can be assessed on a scale: very often (≥1 / 10); often (≥1 / 100, <1/10); infrequently (≥1 / 1,000, <1/100); rarely (≥1 / 10,000, <1/1,000); very rare (<1/10 000); with an unknown frequency (according to separate reports from clinical practice).

Violations, possibly associated (in the opinion of the attending physicians) with the introduction of Aklasta in the treatment of Paget's bone disease, various types of osteoporosis, prevention of new fractures in patients with fractures of the proximal femur:

• Digestive system: often - vomiting, nausea, diarrhea; infrequently - pain in the upper abdomen, dyspepsia, anorexia, loss of appetite, abdominal pain, esophagitis, dry mouth, gastroesophageal reflux, constipation, toothache, gastritis (against the background of glucocorticosteroid therapy);
• Musculoskeletal system and connective tissue: often - myalgia, arthralgia, pain in the bones, limbs and back; infrequently - neck pain, muscle cramps, swelling in the joints, pain in the shoulder girdle and chest (of musculoskeletal origin), muscle weakness, stiffness in the joints and muscles, musculoskeletal pain, arthritis; with an unknown frequency - osteonecrosis of the jaw;
• Urinary system: infrequently - pollakiuria, increased blood creatinine, proteinuria; with an unknown frequency - renal failure;
• Respiratory system: infrequently - cough, shortness of breath;
• Nervous system: often - headache, dizziness; infrequently - lethargy, fainting, paresthesia, tremor, drowsiness, dysgeusia;
• Hematopoietic system: infrequently - anemia;
• Cardiovascular system: often - atrial fibrillation; infrequently - sudden facial flushing, increased blood pressure, palpitations; with an unknown frequency - a pronounced decrease in blood pressure (in the presence of risk factors);
• Subcutaneous tissue and skin: infrequently - rash, itching, hyperhidrosis, erythema;
• Sense organs: often - hyperemia of the sclera; infrequently - eye pain, conjunctivitis, vertigo; rarely - uveitis, episcleritis, iritis; with an unknown frequency - inflammation of the orbit and sclera;
• Invasions and infections: infrequently - flu, nasopharyngitis;
• Psyche: infrequently - insomnia;
• The body as a whole and disorders at the injection site: very often - an increase in body temperature; often - reactions at the infusion site, chills, flu-like syndrome, fatigue, pain, asthenia, general malaise; infrequently - a feeling of thirst, peripheral edema, acute phase reactions, chest pain (not associated with heart disease); with an unknown frequency - dehydration (occurs secondary to post-infusion symptoms such as vomiting, fever and diarrhea).

When conducting separate studies, the following adverse events were recorded, the frequency of which in Aklasta's group was lower than in patients who did not receive the drug: hypocalcemia, reactions at the injection site, redness of the eyes, gastritis, increased content of C-reactive protein, toothache, dysgeusia, feeling of palpitations.

When using Aklasta in women with postmenopausal osteoporosis, the development of atrial fibrillation was noted (this violation has not been confirmed by other clinical studies of zoledronic acid).

The general safety profile when using Aklasta in postmenopausal osteoporosis (for prophylactic purposes) is comparable to that in the treatment of postmenopausal osteoporosis, except for adverse reactions observed within 3 days after infusion (in the form of pain, fever, chills, myalgia, nausea, headache, increased fatigue, arthralgia), the frequency of which was higher in patients who used the drug for prophylaxis. Most often, these adverse reactions were mild to moderate and resolved on their own within 3 days after onset. With repeated use of Aklasta, the severity of these adverse events was significantly reduced.

Adverse reactions possibly associated with the use of Aklasta for the prevention of postmenopausal osteoporosis (according to the attending physicians):

• Digestive system: very often - nausea; often - anorexia, constipation, pain in the abdomen and upper abdomen;
• Nervous system: very often - headache; often - lethargy, tremor; infrequently - dysgeusia, decreased sensitivity;
• Musculoskeletal system and connective tissue: very often - myalgia; often - pain in the chest area of musculoskeletal origin, muscle spasm, pain in the jaw and neck; infrequently - pain in the side;
• Psyche: infrequently - anxiety;
• Skin and subcutaneous tissue: often - increased sweating at night;
• Organ of vision: often - eye pain, conjunctivitis, iritis; infrequently - blurred vision;
• The body as a whole and disorders at the injection site: very often - chills, pain; often - reactions at the injection site, peripheral edema, non-cardiac chest pain.

In postmenopausal osteoporosis during therapy, there have been cases of a decrease in serum calcium concentration without clinical signs of hypocalcemia. In the treatment of Paget's bone disease, the development of transient hypocalcemia, accompanied by clinical manifestations, was noted in approximately 1% of cases.

During the use of zoledronic acid, cases of renal dysfunction with an increase in the concentration of creatinine in the blood were noted, which were sometimes accompanied by acute renal failure (care must be taken when using Aklasta in patients with concomitant oncological diseases and chemotherapy).

Cases of osteonecrosis (in most episodes - jaw) mainly occurred in cancer patients after tooth extraction or other dental procedures. As a rule, they showed symptoms of a local infectious and inflammatory process, including osteomyelitis.

Also during therapy, the following undesirable effects were noted (a causal relationship with the use of Aklasta has not been established): hypersensitivity reactions, including in rare cases urticaria, bronchoconstriction, angioedema, anaphylactic reactions / shock.

In some cases, in clinical practice, the development of functional renal disorders, including renal failure, which required hemodialysis, or deaths, was noted, especially in patients with additional risk factors (for example, concomitant therapy with diuretics and nephrotoxic drugs, advanced age or severe dehydration) or a history of renal disease.

special instructions

Patients need to know the main manifestations of hypocalcemia. The condition of the patients at risk should be monitored regularly.

Patients with Paget's bone disease should be prescribed therapy only by qualified specialists with experience in treating this disease.

To reduce the incidence of adverse reactions that occur within 3 days after the administration of Aklasta, it is possible to use paracetamol or ibuprofen shortly after the infusion.

In case of hypocalcemia, before starting the use of the drug, treatment with adequate doses of calcium and vitamin D should be carried out. For other disorders of mineral metabolism (for example, developed after operations on the parathyroid and thyroid glands, with hypoparathyroidism or decreased absorption of calcium in the intestine), therapy should also be carried out.

To reduce the likelihood of kidney dysfunction, follow these guidelines:

1. Aklasta should not be prescribed to patients with severely impaired renal function (due to limited data on the safety of therapy in this category of patients);
2. When combined with drugs / substances that can have a significant effect on renal function, care must be taken;
3. Before the introduction of Aklasta, creatinine clearance should be determined. When using the drug in patients who have risk factors for the development of renal disorders, it is necessary to determine the serum creatinine content regularly;
4. Before the introduction of the solution, it is necessary to ensure adequate hydration of the body, especially for patients over 65 years of age, as well as patients receiving diuretic therapy;
5. A single dose should not exceed 5 mg. The drug should be administered for at least 15 minutes.

Risk factors for osteonecrosis include cancer, concomitant therapy (eg, radiation therapy, chemotherapy, glucocorticosteroid treatment), and other comorbidities (eg, infections, anemia, coagulopathies, a history of dental disease). Before the introduction of Aklasta, it is necessary to conduct a dental examination and, if there are risk factors, perform the necessary preventive procedures in advance.

There is evidence of cases of atypical diaphyseal and subtrochanteric fractures of the femur in patients receiving bisphosphonates for a long time. These fractures usually develop spontaneously or after minor trauma and may be accompanied by poor healing. The decision to discontinue the use of Aklasta in patients with suspected atypical fractures of the femur should be made individually by the physician based on an assessment of the benefit-risk ratio.

Care must be taken when performing potentially dangerous types of work, since dizziness may develop during the use of the drug.

Drug interactions

Special studies to study the interaction of zoledronic acid with other drugs have not been conducted.

Care must be taken when using Aklasta in combination with drugs / substances that significantly affect renal function.

In case of functional disorders of the kidneys, the combination of Aklasta with drugs that are excreted mainly by the kidneys can lead to an increase in the systemic effect of these drugs.

Aklasta's solution is incompatible with solutions that contain calcium or other divalent cations (for example, in the same system for intravenous drip).

Analogs

Aklasta's analogues are: Zoledronate-Teva, Blaztera, Zoledrex, Zoleriks, Zometa, Rezoklastin FS.

Terms and conditions of storage

Keep out of reach of children at temperatures up to 25 ° C.

The shelf life is 3 years.

The solution after opening the bottle remains stable for 24 hours when stored at a temperature of 2-8 ° C.

Terms of dispensing from pharmacies

Dispensed by prescription.

Aklasta: prices in online pharmacies

Drug name Price Pharmacy

Aklasta 50 μg / ml solution for infusion 100 ml 1 pc. 13 400 RUB Buy

Aklasta rr d / inf. 5mg / 100ml No. 1 13719 RUB Buy

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!