When a person's bones become brittle and brittle, and this happens with some diseases of the bone tissue, the quality of life is sharply reduced. Frequent fractures, pain in the joints, spine and limbs begin to accompany a person everywhere, because of which you can completely stop feeling the joy of being and plunge into complete despair.
But fortunately for us, there are special preparations in the modern world that can effectively strengthen bone tissue. It is about them that will be discussed in our article. These drugs are called "bisphosphonates" - drugs, reviews of which can give hope for recovery to many desperate people. Believe me, there are many! We will tell you about the history of the creation of these funds, why they are so good, what their healing effect is based on, we will publish the names of bisphosphonates, which are the most popular and effective.
The article will be useful to absolutely everyone. After all, even if today everything is in order with the he alth of you and your loved ones, then, unfortunately, this does not mean that it will always be so. Years go by, with themthe addition of diseases becomes more and more. So information about modern medicines will not be superfluous. But enough introductions! Let's move on to a more serious study of the topic of our article.
Bisphosphonates for bone he alth
A group of synthetic selective drugs that have the ability to block the activity of osteoclasts (cells that destroy bone tissue) in the body and restore bone structure is called bisphosphonates.
These drugs are currently used primarily to help patients with osteoporosis and other diseases that cause brittle bones. The most valuable property of bisphosphonates is that they can be used in oncological diseases characterized by the formation of tumors in the bone tissue. In these cases, the drugs described in our article prevent the spread of metastases and reduce pain in such patients.
Mechanism of action of bisphosphonates in the treatment of osteoporosis
You learned from the previous chapter that bisphosphonates are drugs that promote bone he alth. It is time to talk in more detail about the mechanism of their action. The cells of our body have a remarkable ability to renew and remodel from time to time. Bones are no exception. The balance of their structures is constantly maintained, on the one hand, by osteoblast cells, which are responsible for the construction of new tissue, and on the other hand, by osteoclasts, which are responsible for its destruction. BFs are endowed with the power to inhibit the work of osteoclasts andeven trigger the mechanism of their self-destruction. The treatment of osteoporosis with bisphosphonates is based on this remarkable property.
It must be said that to date, scientists have not yet fully understood the mechanism of blocking bone destruction with the help of bisphosphonates. It is known for certain that these substances are able to bind to hydroxyapatite areas of the bone, due to which they can change its bending and at the same time reduce the concentration of hydroxyproline and phosphatase in the blood.
Sometimes BF preparations can be prescribed in the treatment of even such diseases as hernia or protrusion of the intervertebral discs, as painkillers. And a little more information: bisphosphonates for osteoporosis have been used for a long time, but for oncological diseases they began to be used relatively recently. With the help of research, it was found that when entering the body, where there is an active tumor process, bisphosphonates do not allow tumor cells to fuse with the bone matrix and thereby block the formation of metastases. This will be discussed in more detail in a separate chapter.
A bit of history
It turns out that bisphosphonates were discovered by scientists a long time ago, back in the 19th century. For the first time, the synthesis of the first BPs was carried out in Germany. It is surprising that initially these substances were used only in various industrial sectors (in the production of mineral fertilizers, fabrics, oil refining, etc.) and had nothing to do with medicine.
For medical purposes - for the treatment of bonetissues - bisphosphonates began to be used only in the middle of the twentieth century, when their amazing property was discovered to influence the processes of both calcification and decalcification. Bisphosphonates for osteoporosis have been widely used since then around the world.
Classification of bisphosphonates
Today, pharmacology has developed the third generation of biosphosphonates. But this does not mean that doctors have completely abandoned the use of first and second generation drugs, which were invented much earlier. By no means! Today, there are many drugs based on bisphosphonates. All this variety of drugs is divided into two groups: nitrogen-free drugs and nitrogen-containing drugs. Their action on osteoclast cells has a different mechanism. Below we will look at both groups in more detail.
Nitrogen-containing bisphosphonates
These are preparations of the bisphosphonate group containing the following active ingredients:
- Ibandronate acid. This substance was synthesized recently, therefore it is a third-generation drug. It is used most successfully in the treatment and prevention of osteoporosis in women who have entered the difficult period of postmenopause. Men are not recommended to take this drug. Ibandronate acid is also used for abnormally high calcium levels in the blood (hypercalcemia).
- Zolendronic acid. Also belongs to the third generation of bisphosphonates. Able to selectively affect bone tissue. Due to this, it is effectively used for the treatment of osteoporosis. selective actionzoledronic acid on bone structure is based on its high affinity to the bone lattice, which provides excellent inhibition of osteoclasts. Another important property of this drug is a pronounced antitumor effect. Based on zoledronic acid, the popular bisphosphonates "Zometa", "Zolendronate" are produced.
- Alendronate Sodium is a second generation bisphosphonate. It is a non-hormonal specific corrector of bone tissue metabolism, forms the correct bone structure. Indicated for use in osteoporosis in both women and men.
- Sodium ibandronate ("Bonviva", "Bondronat", "Boniva" - bisphosphonates, preparations made on its basis) - the third generation of drugs. Suppresses the activity of osteoclasts, without affecting their number. It does not have a harmful effect on the formation of bone cells, while effectively reducing their destruction. Good for postmenopausal women as a prophylactic against bone fractures.
Preparations that do not contain nitrogen
And now we will talk about what nitrogen-free bisphosphonates are. The drugs you are about to read are first-generation bisphosphonates:
- "Clodronate". Prevents both osteolysis and the development of hypercalcemia. Forms complex bonds with bone tissue hydroxyapatite, changes the crystal lattice and actively counteracts the separation of calcium moleculesand phosphates. With bone metastases, it inhibits their development and blocks the birth of new formations.
- "Sodium etidronate". Promotes the restoration of bones in women diagnosed with osteoporosis. Also used for Paget's disease, hypercalcemia, etc.
- "Tiludronate sodium". Mineralizes and strengthens bone tissue, accumulating molecular compounds of phosphates and calcium in it, inhibits the destruction of bones. It is prescribed for patients diagnosed with osteodystrophy deformans or Paget's disease, it can be prescribed instead of hormones.
Bisphosphonates - the drugs we have published - are sold by prescription only, because they are potent substances. Using them at your own discretion can be hazardous to he alth! Remember that BF is not harmless vitamins or calcium supplements. These drugs actively interfere with the processes occurring in the body, and if used incorrectly, they can be harmful instead of helping.
Admission rules
Bisphosphonates drugs are rather difficult to digest by the gastrointestinal tract, their absorption is difficult. Therefore, the instruction strongly prescribes to drink these drugs exclusively on an empty stomach, about 30 minutes before a meal - this rule helps the absorption of active medicinal substances. Patients should be aware that this group of drugs can cause inflammation and erosion in different parts of the gastrointestinal tract. To avoid such complications, after taking the pills, you should try not tolie down and stay upright. The dosage is selected by the attending physician.
Typically, when prescribing bisphosphonates, the doctor also prescribes the patient to ingest large doses of calcium. So, the simultaneous reception of both is excluded. Calcium supplements should not be taken after taking a bisphosphonate until two hours have passed, and not before. Another important recommendation: BF should not be washed down with tea, milk, juice or coffee, but with plain water (large amounts).
Use of bisphosphonates in cancer
Let's talk more about the treatment with bisphosphonates of diseases accompanied by the growth of tumors of various nature. The occurrence of bone metastases goes hand in hand with a reciprocal interaction between tumor cells and metabolically active bone tissue. In turn, the dynamic development of metastases is accompanied by adhesion of tumor cells to bone structures, as well as invasion, proliferation, and neoangiogenesis. Numerous preclinical studies have allowed scientists to assume that BP inhibit each of the listed stages of pathogenesis.
Several research programs have evaluated the effect of the bisphosphonate Clodronate on the development of bone metastases in women diagnosed with breast cancer. Excellent results were obtained: the drug helped to reduce the frequency of formation and growth of new metastases in the bone tissues of patients. Currentlyresearch in this direction is actively ongoing. Bisphosphonates can really help with bone metastases.
Malignant tumors are often accompanied by hypercalcemia (release of calcium from the bones). With the defeat of bone metastases, rapid loss of calcium occurs due to its destruction by osteoclasts. In addition, hypercalcemia in cancer can occur due to the effect of the peptide on the tumor. Further activation of osteoclasts occurs, which leads to hypercalcemia. This process is further complicated and accelerated by reduced kidney function.
These processes are observed in malignant tumors such as squamous cell carcinoma, multiple myeloma, breast cancer, renal cell carcinoma and some types of lymphomas. For cancer-induced hypercalcemia, intravenous bisphosphonates are the most effective drugs. Bisphosphonates such as Zoledronic acid and Pamidronate have proven themselves well in these cases.
Observations show that within a few days after the start of intravenous administration of these drugs to patients, the concentration of calcium in the blood normalizes, and the effect continues for quite a long time (from one to two weeks).
List of diseases for which bisphosphonates have been successfully used
- Osteoporosis.
- Myeloma.
- Disorders in bone formation.
- Paget's disease (deforming osteodystrophy).
- Primary hyperparathyroidism.
- Tumours and bone metastases, especially those associated with hypercalcemia.
Side effects
Unfortunately, active treatment with bisphosphonates can be anything but harmless. Especially when it comes to intravenous administration of these drugs. They may cause the following negative side effects:
- With intravenous administration - hypocalcemia.
- Able to adversely affect the kidneys, cause intoxication.
- Sometimes taking amine-containing bisphosphonates provokes the development of osteonecrosis of the jaws.
- Contribute to the development of ulcers in the esophagus and stomach.
- May cause constipation or diarrhea, and in rare cases, difficulty swallowing.
- General malaise, weakness, nausea.
- Muscle pain.
- Vision problems.
- Rashes on the body.
Yes, bisphosphonates can cause all these troubles. The drugs whose names you meet in our article cannot be prescribed to yourself on your own, so as not to inadvertently cause irreparable harm to the body. We deliberately repeat this in the text several times! Judging by the reviews that can be read on various forums, people actively share information about certain BFs with each other and willingly recommend them to others. This is somewhat unethical. It is necessary to take such potent drugs only on the recommendation of the attending doctor and always under his supervision.
Bisphosphonates - reviews of doctors and patients
Did you know that every year, on October 20,Does every country celebrate World Osteoporosis Day? This disease has become truly epidemic in recent years. Although some experts believe that the relevance of the problem of osteoporosis is somewhat exaggerated, because this disease is not fatal in itself. Nevertheless, the percentage of elderly people who die after a hip fracture, which often happens precisely with progressive osteoporosis, is very high. Therefore, a huge number of people have a special hope for bisphosphonates. Feedback from patients who received hope for recovery thanks to these medicines is permeated with gratitude to doctors and modern pharmacology, which was able to provide them with timely assistance.
Dr. med. Svetlana Rodionova, PhD, Professor and Head of the Scientific and Clinical Center for Osteoporosis, believes that the situation with osteoporosis in Russia is quite difficult. A well-known doctor says that nowadays, when the diet of most people is inadequate (lack of calcium), bad habits such as smoking, drug and alcohol use are widespread, and physical activity is rapidly approaching zero, many young people, mainly women are doomed to become ill with osteoporosis in more mature years. So the need for good effective drugs to help cure this disease is very great.
As for the frequent prescription of bisphosphonates by doctors, the professor is of the opinion that this is not always justified. Bisphosphonates - drugseffective, but before prescribing a particular prescription to a patient, the doctor must take into account factors such as bone metabolism and calcium homeostasis. With thoughtless and uncontrolled treatment with bisphosphonates, serious complications can occur: atrial fibrillation, osteonecrosis of the jaw, subtrochanteric fractures of the femur.
According to the respected doctor, bisphosphonates are not a universal panacea, their use should be approached with caution. Meanwhile, the He alth program is being broadcast on TV screens, where Elena Malysheva convinces the audience with a sweet smile that there is nothing easier than treating osteoporosis with third-generation bisphosphonates. Do not trust the advertising show too much. For some people, taking BF is strictly contraindicated. For example, patients with severe kidney disease.
Now for the feedback on how bisphosphonates work for bone metastases. The opinion of doctors is unequivocal: these drugs are really capable of stopping the growth of malignant cells in bone tissues, which, of course, helps patients overcome one of the most serious ailments that exists in the world.
Conclusion
Now you know what it is - bisphosphonates. The instructions for their use set forth here, as well as the list of medicines, are not given by us as recommendations and are for informational purposes only - please pay special attention to this! In case of serious he alth problems, you do not need to self-medicate, the best thing is to quickly consult a doctor,for him to prescribe medication for you. We wish everyone good he alth and happiness!
