Bisphosphonates (preparations): description, instructions, testimonials. Bisphosphonates in the treatment of osteoporosis

When the bones of a person become brittle and brittle, and this happens with some diseases of bone tissue, the quality of life is sharply reduced. Frequent fractures, pains in the joints, spine and limbs begin to accompany the person everywhere, because of what you can completely stop feeling the joy of being and plunge into complete despair.

But our luck with you is in the modern world, special drugs that can effectively strengthen bone tissue. It is about them that will be discussed in our article. These drugs are called "bisphosphonates" - drugs, reviews about which can inspire hope for the recovery of many desperate people. Believe me, there are many such! We will tell you about the history of creating these funds, about how they are so good, on what their healing effect is based, we will publish the names of bisphosphonates that are the most popular and effective.

The article will be useful to everyone. After all, even if today you and your close people have good health, unfortunately, this does not mean that it will always be like this. Years go by, with their adding 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 - preparations for bone health

A group of synthetic selective drugs that have the ability to block the activity of osteoclasts (cells that destroy bone tissues) in the body and restore the structure of bones is called bisphosphonates.

These drugs are currently used primarily to help patients with osteoporosis and other diseases that cause bone fragility. The most valuable property of bisphosphonates is also the fact that they can be used in cancer diseases characterized by the formation of tumors in bone tissue. In these cases, the medicines, which our article tells us, do not allow spreading metastases and reduce the pain syndrome in such patients.

The mechanism of action of bisphosphonates in the treatment of osteoporosis

From the previous chapter, you learned that bisphosphonates are drugs that help improve bones. It is time to talk more about the mechanism of their action. The cells of our body have a remarkable ability to be updated from time to time and reconstructed. Bone tissues are no exception. The equilibrium of their structures is constantly supported, on the one hand, by osteoblastic cells responsible for the construction of new tissue, on the other - osteoclasts, which are responsible for its destruction. BF are endowed with the power to inhibit the work of osteoclasts and even trigger the mechanism of their self-destruction. On this remarkable property, the treatment of osteoporosis with bisphosphonates is based.

I must say that for today, scientists have not yet fully studied the mechanism of blocking the destruction of bones with the help of bisphosphonates. It is known for certain that these substances are able to bind to the hydroxyapatite regions of the bone, whereby they can change its bend and reduce the concentration of oxyproline and phosphatase in the blood.

Sometimes BF preparations can be prescribed in the treatment of even such diseases as hernias or protrusions of intervertebral discs, as an anesthetic. And some more information: bisphosphonates from osteoporosis have been used for a long time, but now they have been used relatively recently for oncological diseases. With the help of research, it was found that, when ingested into an organism where there is an active tumor process, bisphosphonates do not allow the cells of the tumor to fuse with the bone matrix and thereby block the formation of metastases. More about this will be discussed in a separate chapter.

A bit of history

It turns out that bisphosphonates were discovered by scientists long ago, back in the XIX century. The first BF synthesis was first carried out in Germany. It is surprising that initially these substances were used only in various industrial branches (in the production of mineral fertilizers, fabrication, processing of oil, etc.) and had nothing to do with medicine.

For medical purposes - for the treatment of bone tissue - 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 from osteoporosis have been applied since then all over the world very actively.

Classification of bisphosphonates

Nowadays the third generation of biophosphonates has been developed by pharmacology. But this does not mean that doctors completely abandoned the use of drugs of the first and second generation, which were invented much earlier. By no means! Today, there are many drugs based on bisphosphonates. All this variety of medicines is divided into two groups: nitrogen-free drugs and nitrogen-containing drugs. Their effect on osteoclast cells has a different mechanism. Below we consider both groups in more detail.

Nitrogen-Containing Bisphosphonates

These are preparations of the bisphosphonate group containing the following active substances:

• Ibandronic acid. This substance was synthesized recently, therefore it is a preparation of the third generation. It is used most successfully in the treatment and prevention of osteoporosis in women who have entered a difficult period of postmenopause. Men should not take this medication. Ibandronate acid is also used in the pathological increase in blood levels of calcium (hypercalcemia).
• Zolendronic acid. It also applies to the third generation of bisphosphonates. It is able to selectively affect bone tissue. Due to this, it is effectively used for the treatment of osteoporosis. The selective effect of zolendronic acid on the 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 popular bisphosphonates "Zometa", "Zolendronate" are produced.
• Alendronate sodium is a remedy from the second generation of bisphosphonates. It is a non-hormonal specific corrector of bone tissue metabolism, forms the correct bone structure. It is indicated for use in osteoporosis for both women and men.
• Ibandronate sodium ("Bonviva", "Bondronate", "Boniva" - bisphosphonates, preparations made on its basis) is the third generation of medicines. Suppresses the activity of osteoclasts without affecting their number. Does not have a harmful effect on the formation of bone cells, while effectively reducing their destruction. Well helps women in postmenopause as a preventive remedy for bone fractures.

Drugs that do not contain nitrogen

And now we are going to talk about what are nitrogen-free bisphosphonates. Preparations, the names of which you will now read, refer to the first generation of bisphosphonates:

• "Clodronate." It interferes with both osteolysis and the development of hypercalcemia. Forms complex bonds with hydroxyapatite of bone tissue, changes the crystal lattice and actively counteracts the separation of calcium and phosphate molecules. With metastases in the bones, their development slows down and blocks the birth of new formations.
• "Ethidronate sodium." Promotes the restoration of bones in women diagnosed with "osteoporosis." It is also used for Paget's disease, hypercalcemia, etc.
• "Tiludronate sodium." Minerals and strengthens bone tissue, accumulating in it the molecular compounds of phosphates and calcium, inhibits the destruction of bones. It is prescribed to patients with diagnoses "deforming osteodystrophy" or "Paget's disease", can be prescribed instead of hormones.

Bisphosphonates - drugs, the list of which we published - are sold only on prescription, since they are potent substances. Use them at your own discretion may be hazardous to health! Remember that BF - is not harmless vitamins or supplements with calcium. These drugs actively interfere with the processes occurring in the body, and with illiterate application can harm instead of help.

Rules of admission

Medicines bisphosphonates are quite difficult to digest by the gastrointestinal tract, their absorption is difficult. Therefore, the instruction urgently prescribes to drink these preparations only on an empty stomach, about 30 minutes before a meal - this rule helps to absorb active drugs. Patients should be aware that this group of medicines can cause inflammation and erosion in different parts of the gastrointestinal tract. To avoid such complications, after taking the tablets you should try not to lie down for an hour, but stay in a vertical position. The dosage is chosen by the attending physician.

Usually, when prescribing bisphosphonates, the doctor prescribes to the patient the intake of large doses of calcium. So, the simultaneous reception of both is excluded. Preparations containing calcium can be taken after taking bisphosphonate only after two hours, and not before. Another important recommendation: BF should be washed down not with tea, milk, juice or coffee, but with plain water (plenty).

The use of bisphosphonates in tumor diseases

Let's talk in more detail about the treatment of bisphosphonates with diseases accompanied by the growth of tumors of various nature. The emergence of metastases in bone tissues goes side by side with the reciprocal interaction between tumor cells and the metabolic active bone tissue. In turn, the dynamic development of metastases is accompanied by adhesion of tumor cells to bone structures, as well as by invasion, proliferation and neoangiogenesis. Numerous preclinical studies have allowed scientists to make the assumption that BF inhibits each of the listed stages of pathogenesis.

Several research programs evaluated the effect of the bisphosphonate "Clodronate" on the development of metastases in bone tissues in women with diagnosed 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. Currently, research in this direction is actively continuing. Bisphosphonates with bone metastases are really capable of helping.

Malignant tumors are often accompanied by hypercalcemia (release of calcium from the bones). When bone metastases are affected, a rapid loss of calcium occurs due to the destruction of the osteoclasts by it. In addition, hypercalcemia in cancer can arise due to the effect on the tumor of the peptide. Further, activation of osteoclasts occurs, which leads to hypercalcemia. This process is complicated and accelerated also due to a decrease in the function of the kidneys.

The listed processes are observed in such malignant tumors as squamous cell carcinoma, multiple myeloma, breast cancer, renal cell carcinoma and some types of lymphomas. With hypercalcemia, triggered by cancer, the most effective drugs are bisphosphonates for intravenous infusion. Well-proven in these cases, such drugs-bisphosphonates, as "Zolendronic acid" and "Pamidronate."

Observations show that in a few days after the introduction of these drugs intravenously to patients, the concentration of calcium in the blood is normalized, and the effect continues for a sufficiently long time (one to two weeks).

List of diseases in which bisphosphonates are successfully used

• Osteoporosis.
• Myeloma.
• Disturbances in the formation of bone tissue.
• Paget's disease (deforming osteodystrophy).
• Primary hyperparathyroidism.
• Tumors and metastases in bone tissue, especially combined with hypercalcemia.

Side effects

Unfortunately, active treatment with bisphosphonates may not be harmless. Especially when it comes to intravenous administration of these drugs. They can cause the following negative side effects:

• With intravenous administration - hypocalcemia.
• They are able to negatively affect the kidneys, cause intoxication.
• Sometimes the use of amino-containing biophosphonates provokes the development of osteonecrosis of the jaws.
• Promote the development of ulcers in the esophagus and in the stomach.
• Can cause constipation or diarrhea, in rare cases - difficulty in swallowing.
• General malaise, weakness, nausea.
• Muscle Pain.
• Problems with eyesight.
• Rashes on the body.

Yes, all these troubles can cause bisphosphonates. Preparations, the names of which you meet in our article, can not be assigned to yourself, so as not to accidentally cause irreparable harm to the body. We deliberately repeat this in the text several times! Judging by the responses that can be read in various forums, people actively share information about one or another BF with each other and readily recommend them to others. This is somewhat unethical. To take such potent medicines is necessary only on the recommendation of the treating doctor and necessarily under his supervision.

Bisphosphonates - reviews of doctors and patients

Did you know that every year, October 20, all countries celebrate World Day against Osteoporosis? This disease in recent years has become truly epidemic. Although some experts believe that the relevance of the problem of osteoporosis is somewhat exaggerated, because this disease is not in itself deadly. And yet, the percentage of elderly people dying after a fracture of the neck of the hip, which often happens precisely with progressive osteoporosis, is very large. Therefore, a huge number of people have a special hope for bisphosphonates. Feedback from patients who have received the hope of recovery through these medicines are permeated with gratitude to doctors and modern pharmacology, which was able to provide them with timely assistance.

Doctor honey. Sci., Professor and head of the Scientific and Clinical Center of Osteoporosis Svetlana Rodionova believes that the situation with the disease of osteoporosis in Russia is quite severe. A well-known doctor says that nowadays, when most people's nutrition is inadequate (lack of calcium), such bad habits as smoking, drug and alcohol use are getting widespread, and physical activity is rapidly approaching zero, many young people, mostly Women, are doomed in more mature years to develop osteoporosis. So the need for good effective drugs that help to cure this ailment is very great.

As for the frequent appointment of bisphosphonates by physicians, the professor expresses the opinion that this is not always justified. Bisphosphonates are effective drugs, but before prescribing a prescription for a patient, the doctor must take into account factors such as bone metabolism and calcium homeostasis. With unreasonable and uncontrolled treatment with bisphosphonates, serious complications can occur: atrial fibrillation, jaw bone osteonecrosis, and susceptible fractures of the femur.

Judging by the opinion of the esteemed doctor, bisphosphonates are not a universal panacea, their use must be treated with caution. Meanwhile, the TV program broadcasts the program "Health", where Elena Malysheva with a sweet smile convinces the audience that there is nothing easier than to be treated for osteoporosis by bisphosphonates of the third generation. Do not trust the ad show too much. For some people, BF is categorically contraindicated. For example, patients with severe kidney disease.

Now about the feedback on how bisphosphonates work in bone metastases. The doctors' opinion is unequivocal: these drugs are really capable of stopping the growth of malignant cells in the bone tissues, which certainly helps patients overcome one of the most serious ailments that exist 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 given to us not as recommendations, but are only for informational purposes - we ask you to pay special attention to this! If you have serious health problems, you do not need to self-medicate, the best thing is to see your doctor as soon as possible so that he can choose the medicines for you. We wish you all good health and happiness!