When a person’s bones become brittle and brittle, and this happens with some bone diseases, the quality of life decreases sharply. Frequent fractures, pains in the joints, spine and limbs begin to accompany a person everywhere, because of which you can completely stop feeling the joy of life and become immersed in complete despair.
But for our happiness, 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 inspire hope for many desperate people to recover. Believe me, there are many of them! We will tell you about the history of the creation of these funds, about how 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. Indeed, even if everything is in order with the health of you and your loved ones today, unfortunately, this does not mean that it will always be so. Years go by, with their addition of diseases becomes more and more. So the information on modern medicines will not be superfluous. But enough intros! Let's move on to a more serious study of the topic of our article.
Bisphosphonates - bone health products
A group of synthetic selective drugs with 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 bone fragility. Another valuable property of bisphosphonates is that they can be used for oncological diseases characterized by the formation of tumors in bone tissue. In these cases, the drugs our article talks about do not allow metastases to spread and reduce pain 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 promote bone healing. It is time to talk in more detail about the mechanism of their action. The cells in our body have a remarkable ability to renew and reconstruct from time to time. Bone tissue is no exception. The equilibrium of their structures is constantly maintained, on the one hand, osteoblast cells responsible for the construction of new tissue, and on the other hand, osteoclasts that are responsible for its destruction. BFs are endowed with the power to slow down the work of osteoclasts and even start the mechanism of their self-destruction. The treatment of osteoporosis with bisphosphonates is based on this remarkable property.
I must say that to date, scientists have not yet fully understood the mechanism of blocking bone destruction using bisphosphonates. It is known for certain that these substances are able to bind to the hydroxyapatite areas of the bone, due to which they can change its bend and at the same time reduce the concentration of oxyproline and phosphatase in the blood.
Sometimes BF drugs can be prescribed in the treatment of even diseases such as hernias or protrusions of the intervertebral discs, as painkillers. And some more information: bisphosphonates from osteoporosis have been used for a long time, but now they have been used relatively recently for cancer. With the help of studies, it was found that getting into the body where an active tumor process is available, bisphosphonates do not allow tumor cells to merge 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. The synthesis of the first BPs was first carried out in Germany. It is surprising that initially these substances were used only in various industrial sectors (in the production of mineral fertilizers, the manufacture of fabrics, oil refining, 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. Since bisphosphonates from osteoporosis have been used very actively around the world since then.
Classification of Bisphosphonates
Today, 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. Not at all! Today, there are many drugs based on bisphosphonates. All this variety of drugs is divided into two groups: nitrogen-free drugs and nitrogen-containing. 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 bisphosphonates group containing the following active substances:
- Ibandronate acid. This substance has been 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 a pathological increase in blood levels of calcium (hypercalcemia).
- Zolendronic acid. Also applies to the third generation of bisphosphonates. Able to selectively affect bone tissue. Thanks to this, it is effectively used to treat osteoporosis. The selective effect of zolendronic acid on the bone structure is based on its high affinity for the bone lattice, which provides excellent inhibition of osteoclasts. Another important property of this drug is a pronounced antitumor effect. Based on zollendronic acid, the popular bisphosphonates Zometa and Zolendronate are produced.
- Sodium alendronate is a second-generation bisphosphonate drug. It is a non-hormonal specific corrector of bone tissue metabolism, forms the correct bone structure. Indicated for use in osteoporosis for both women and men.
- Sodium ibandronate (Bonviva, Bondronat, Boniva - bisphosphonates, preparations based on it) - the third generation of drugs. Suppresses the activity of osteoclasts, without affecting their number. It has no harmful effect on the formation of bone cells, while effectively reducing their destruction. It helps women in postmenopausal women as a prophylactic against bone fractures.
Nitrogen Free Products
And now we will talk about what nitrogen-free bisphosphonates are. The drugs, the names of which you will now read, belong to the first generation of bisphosphonates:
- "Clodronate." Prevents both osteolysis and the development of hypercalcemia. It forms complex bonds with bone hydroxyapatite, changes the crystal lattice and actively counteracts the separation of calcium and phosphate molecules. With bone metastases, it inhibits their development and blocks the birth of new formations.
- "Ethidronate sodium." Promotes bone repair in women diagnosed with osteoporosis. It is also used for Paget's disease, hypercalcemia, etc.
- "Sodium tiludronate." It mineralizes and strengthens bone tissue, accumulating molecular compounds of phosphates and calcium in it, and inhibits bone destruction. It is prescribed to patients with diagnoses of "deforming osteodystrophy" or "Paget's disease", can be prescribed instead of hormones.
Bisphosphonates - the drugs we have published a list of - are sold only by prescription, because they are potent substances. Using them at your own discretion can be hazardous to your health! Remember that BFs are not harmless vitamins or calcium supplements. These drugs actively intervene in the processes occurring in the body, and if used improperly, they can be harmful instead of helping.
Admission Rules
Medication bisphosphonates are quite difficult to digest by the gastrointestinal tract, their absorption is difficult. Therefore, the instruction urges you to drink these drugs exclusively on an empty stomach, about 30 minutes before eating - this rule helps the absorption of active drugs. Patients should know that this group of medicines can cause inflammation and erosion in different parts of the gastrointestinal tract. To avoid such complications, after taking the pills, you need to try not to go to bed for an hour, but to remain upright. The dosage is selected by the attending physician.
Usually, when prescribing bisphosphonates, the doctor also prescribes the patient to take large doses of calcium inside. 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 not be washed down with tea, milk, juice or coffee, but plain water (plenty).
The use of bisphosphonates in tumor diseases
Let's talk more about the treatment of diseases with bisphosphonates, accompanied by the growth of tumors of various nature. The occurrence of metastases in bone tissue goes side by side with reciprocal interaction between tumor cells and metabolic 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 make the assumption that BP inhibit each of the listed stages of pathogenesis.
Several research programs have evaluated the effect of Clodronate bisphosphonate on the development of bone metastases in women with identified breast cancer. Excellent results were obtained: the drug helped reduce the frequency of formation and growth of new metastases in the bone tissues of patients. Currently, research in this direction is actively ongoing. Bisphosphonates with bone metastases can really help.
Malignant tumors are often accompanied by hypercalcemia (the release of calcium from the bones). When bone metastases are affected, rapid calcium loss occurs due to its destruction by osteoclasts. In addition, hypercalcemia in cancer can occur due to exposure to the tumor peptide. Next, activation of osteoclasts occurs, which leads to hypercalcemia. This process is complicated and accelerated by a decrease in kidney function.
These 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 caused by cancer, the most effective drugs are bisphosphonates for intravenous infusion. In these cases, bisphosphonates such as Zolendronic Acid and Pamidronate have proven themselves well.
Observations show that already a few days after the start of the administration of these drugs to patients, the concentration of calcium in the blood normalizes, and the effect lasts for quite a long time (from one to two weeks).
List of diseases in which bisphosphonates are successfully used
- Osteoporosis.
- Myeloma
- Disorders of bone tissue formation.
- Paget's disease (deforming osteodystrophy).
- Primary hyperparathyroidism.
- Tumors and metastases in bone tissue, especially combined with hypercalcemia.
Side effects
Unfortunately, active treatment with bisphosphonates can be far from harmless. Especially when it comes to the intravenous administration of these drugs. They can cause the following negative side effects:
- With intravenous administration, hypocalcemia.
- Able to adversely affect the kidneys, cause intoxication.
- Sometimes, the intake of amino-containing biophosphonates provokes the development of osteonecrosis of the jaws.
- Contribute to the development of ulcers in the esophagus and stomach.
- May cause constipation or diarrhea, in rare cases, difficulty swallowing.
- General malaise, weakness, nausea.
- Muscle pain.
- Vision problems.
- Rashes on the body.
Yes, all these troubles can cause bisphosphonates. The drugs, the names of which you find in our article, can not be assigned to yourself, so as not to inadvertently cause the body irreparable harm. We intentionally repeat this several times in the text! Judging by the reviews that can be read on various forums, people are actively sharing information about various BFs with each other and willingly recommend them to others. This is somewhat unethical. It is necessary to take such potent drugs solely on the recommendation of the attending doctor and always under his supervision.
Bisphosphonates - reviews of doctors and patients
Do you know that every year, October 20, all countries celebrate World Osteoporosis Day? 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 fatal. Nevertheless, the percentage of elderly people dying after a hip fracture, which often happens with progressive osteoporosis, is very large. Therefore, a huge number of people have special hope in bisphosphonates. The reviews of patients who received hope of recovery thanks to these drugs are imbued with gratitude to the doctors and modern pharmacology, which was able to provide them with timely help.
Doctor honey. Sci., Professor and Head of the Scientific and Clinical Center for Osteoporosis Svetlana Rodionova believes that the situation with osteoporosis in Russia is quite difficult. A well-known doctor says that today, when the majority of people’s nutrition is inadequate (calcium deficiency), bad habits like smoking, using drugs and alcohol are becoming widespread, and physical activity is rapidly approaching zero, many young people, mainly women who are doomed to osteoporosis in more mature years. So the need for good effective drugs to help cure this ailment is very great.
As for the frequent prescription of bisphosphonates by doctors, the professor expresses the opinion that this is not always justified. Bisphosphonates are effective drugs, but before prescribing a particular prescription to the patient, the doctor must take into account factors such as bone metabolism and calcium homeostasis. Serious complications can arise with rash and uncontrolled treatment with bisphosphonates: atrial fibrillation, osteonecrosis of the jaw, subrochanteric fractures of the femur.
Judging by the opinion of a respected doctor, bisphosphonates are not a universal panacea, their use should be approached with caution. Meanwhile, the Health program is being broadcast on television, where Elena Malysheva, with a sweet smile, convinces the audience that there is nothing easier than to treat third-generation bisphosphonates for osteoporosis. Do not trust the advertising show too much. For some people, taking BF is strictly contraindicated. For example, patients with severe kidney disease.
Now about the reviews regarding how bisphosphonates act in bone metastases. The opinion of doctors is unambiguous: these drugs are really able to stop 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 described here, as well as the list of medicines, were not given as recommendations and are for informational purposes only - please draw your attention to this! If you have serious health problems, you do not need to self-medicate, the best thing is to consult a doctor as soon as possible so that he picks you up medications. We wish everyone good health and happiness!