Bisphosphonates for the treatment of osteoporosis

Bisphosphonates - what is it? Bisphosphonates for the treatment of osteoporosis

The musculoskeletal system performs one of the main functions in the human body. It is the support for all organs. The condition of bones plays an important role.

When there are malfunctions in the joints, spine, frequent fractures occur, then the quality of life of a person is significantly reduced.

One such disease, which is often accompanied by similar symptoms, is osteoporosis.

If you turn to a doctor in time, then there is an opportunity to significantly improve the patient's condition. Currently, bisphosphonates are used to treat osteoporosis. These drugs can give hope for recovery. Let's see what kind of medicines these are.

What are bisphosphonates

Its name was given to this group of medicines because of the two phosphonates in the structure. The mechanism of action proved effective because of the great similarity with pyrophosphonates, which have a great effect on the regulation of calcium content in the bones.

Having a similar structure, bisphosphonates inhibit enzymes that could utilize pyrophosphonates. They seem to bind calcium ions and draw them back into bone tissue.

Because of this action in the treatment of osteoporosis, it is possible to prevent the loss of calcium and phosphorus, which has a positive effect on treatment.

Varieties of bisphosphonates

Many still do not know about bisphosphonates. What it is? At present, the third generation of this group of medicines has already been developed.

Doctors continue to use the drugs of the first two generations.

Now many medications basically contain bisphosphonates, they can all be divided into two large groups:

1. Simple, not containing nitrogen.
2. A group of bisphosphonates, which include nitrogen-aminobisphosphonates.

The difference between the two groups is that they have a different effect on osteoclasts.

Nitrogen-Containing Bisphosphonates

What it is? These agents contain the following substances:

1. Ibandronic acid belongs to the third generation, it has been synthesized recently and has been used with great success to prevent osteoporosis in women, especially during the menopause.
2. Zolendronic acid selectively affects bone tissue, has a well-pronounced antitumor effect. On the basis of this substance, drugs such as "Zometa "Zolendronate" are produced.
3. Alendronate sodium refers to non-hormonal correctors of metabolism in bone tissue, contributes to the formation of the correct bone structure.
4. Ibandronate sodium, on the basis of which they produce: Bonviva, Boniva, Bondronate, inhibits the activity of osteoclasts, but does not affect their number. These bisphosphonates for the treatment of osteoporosis are quite effective, especially as a prophylactic tool in menopause in women.

It should be taken into account that you should not engage in self-medication, the medicine should be prescribed by a doctor.

Simple bisphosphonates

Nitrogen-free preparations of bisphosphonates in osteoporosis are also actively used. These include:

1. "Etidronate" in the form of tablets and injections. Often it is prescribed not only for osteoporosis, but also for Paget's disease, hypercalcemia, which occurs against the background of an oncological disease.
2. "Clodronate" is available in the form of capsules, tablets and solutions. Effective in osteoporosis and osteolysis.
3. "Tiludronate" is usually prescribed only to adults suffering from Paget's disease. To children it is contraindicated.

It is believed that these two groups of drugs have different effects on the female and male body, that's why for the beautiful ladies the drugs nitrogen containing are better suited. In any case, the choice should only be made by your doctor.

The effectiveness of drugs for various diseases

There is a whole list of diseases in which bisphosphonate therapy can have a positive effect.

For each of these diseases, only the doctor prescribes the drug, its dosage and duration of use. Doing self-medication, you can only harm the body.

Mechanism of action

Since bisphosphonate preparations for osteoporosis find the greatest application, it is necessary to find out the mechanism of their action.

All cells of our body are periodically updated, the same can be said about bone tissue.

In it, the balance is maintained with the help of osteoblasts, which are responsible for the synthesis of new tissue, as well as osteoclasts responsible for its destruction.

.

So, BF somehow miraculously inhibit the work of osteoclasts, and in some cases even trigger the mechanism of their self-destruction.

.

It is worth saying that at the present time scientists have not been able to fully understand how bisphosphonates manage to block the destruction of bone tissue. It is known only that these preparations can be combined with hydroxyapatite patches in the bones, as a result of which the bending of the bone tissue changes.

It can also be noted that if bisphosphonates have been used for the treatment of osteoporosis for a long time, then oncological diseases therapy on their basis is used relatively recently.

Bisphosphonates in metastases

When cancer develops, a stage occurs when cancer cells break away from their primary focus and spread throughout the body. In a new place, they attach and begin to expand, forming metastases.

Bone tissue is constantly updated, so the probability of infection with hematogenous path increases. When cancer cells enter the bone marrow, they disrupt the normal interaction between osteoclasts and osteoblasts, which leads to incorrect development of bone tissue.

Since it is difficult to determine the presence of metastases, since in the first stages this process proceeds practically without symptoms, then oncologists should undergo a thorough examination to identify secondary foci.

They can be combined with radiation and chemotherapy. When using such drugs, a decrease in the incidence of metastases in bone tissue in breast cancer, as well as myeloma, was revealed.

When hypercalcemia develops, which is almost the norm in cancer diseases, the most effective drugs are injections and injections.

.

An excellent result showed such tools as "Zolendronic acid "Pamidronate".

.

A few days after the start of treatment, the tests show a normalization of the calcium content in the blood, and the effect can last up to several days.

Special recommendations for the use of bisphosphonates

If you have not heard about bisphosphonates, what it is, the doctor will tell you. The intake of these drugs should be carried out according to certain rules:

• Take medication after waking up, at least an hour before meals.
• Wash down with plenty of water.
• Do not use for liquids other liquids, for example, juice, tea, coffee. They interfere with the absorption of bisphosphonates.
• After eating the pill can not lie down, you need about an hour and a half to stay in an upright position, so that the effect on the esophagus is minimal.
• It is not recommended to combine BF with calcium, magnesium, iron and aluminum.

If you comply with all these recommendations, the use of bisphosphonates will not bring undesirable side effects.

Bisphosphonates in osteoporosis: the pros and cons

In the treatment, bisphosphonates from osteoporosis are widely used. The drugs are equally successful in both men and women. The main advantages of these medicines include:

• Do not contain hormones.
• Do not contribute to the development of cardiovascular diseases.
• Malignant tumors with BF do not progress.

But in any barrel of honey you can always find a fly in the ointment. Bisphosphonates, despite their effectiveness in the treatment of osteoporosis, are far from perfect. Excessive enthusiasm for their reception can give the following side effects:

• Negatively affect the liver and kidneys.
• If administered intravenously, it is likely the development of hypocalcemia.
• An ulcer of the esophagus or stomach may occur.
• Appear rashes on the body.
• Some have general weakness, malaise and nausea.
• Muscle pain.
• Problems with eyesight.
• Diarrhea or diarrhea.

It can not be asserted that all these undesirable effects will necessarily appear in every patient, but it is necessary to know about them. If you are prescribed bisphosphonates, what is it, the doctor will explain, he will choose the dosage of the drug and the duration of treatment.

Such medications are quite effective in the treatment of osteoporosis, as well as other diseases.

Before appointing a medicine, the doctor will certainly conduct a survey to find out the state of the exchange substances in bone tissue and homeostasis of calcium, so do not prescribe yourself drugs of this group.

In order not to resort to the help of drug therapy, it is necessary to lead a healthy lifestyle, follow all the recommendations of doctors, eat right. Only in this case your bone system will be in order.

A source: http://.ru/article/196520/bisfosfonatyi-chto-eto-takoe-bisfosfonatyi-dlya-lecheniya-osteoporoza

The use of bisphosphonates in the treatment of osteoporosis

Since the end of the last century, doctors around the world are actively using bisphosphonates for the treatment of osteoporosis.

Diseases of the musculoskeletal system - extremely painful and unpleasant ailments that prevent living full life and entail a lot of negative consequences up to the loss of ability move.

One of such dangerous diseases is osteoporosis - pathological brittleness of bones, leading to frequent fractures and difficulty recovery after them. The risk group is a person after 50 years of age, with women falling ill more often than men.

Bisphosphonates (diphosphonates) are called so because the molecules of these substances contain two phosphonates (PO3). These chemical compounds are the closest analogs to natural pyrophosphates, which do not undergo cleavage by enzymes present in the human body.

The main purpose of pharmaceutical preparations of bisphosphonates is stabilization of the skeleton in diseases accompanied by rapid loss of bone mass.

We will understand how this happens. Normally, the body produces two types of cells with different functions:

1. Osteoclasts - promote resorption (destruction) of the old cells of the skeleton.
2. Osteoblasts - are involved in the process of forming a new tissue.

In osteoporosis, the latter simply can not cope with their task, while osteoclasts continue to routinely dispose of old cells.

Prevention of osteoporosis and treatment is based on the effect of bisphosphonates on osteoclasts, which is to inhibit their growth and start the process of their self-destruction, as a result of which it is suspended thinning of bones. Another important point: the drugs hold up in the bones the calcium and phosphorus they need so much.

In addition, bisphosphonates are used in complex therapy for cancer patients in the treatment and prevention the occurrence of metastases, affected bone in breast, lung, prostate, kidney, thyroid glands. Entering the body and accumulating, drugs:

• reduce the high content of calcium in the blood - hypercalcemia, which is a concomitant sign of metastatic bone damage;
• prevent the formation of new foci of disease - metastasis;
• have an analgesic effect.

The undoubted advantage is that these drugs are non-hormonal and do not overload the cardiovascular system. A significant drawback is the poor solubility, which makes it difficult for the body to digest.

Drug Groups

There are two main types of bisphosphonates that differ in the way they affect osteoclasts:

• Bezazotnye, or means of the first generation. Suffice to actively use such drugs based on them, such as Etidronate, Clodronate, Tiludronate. The destructive effect on osteoclasts is due to absorption by the latter. Etidronate and Clodronate are successfully used in the complex treatment of oncology.
• Aminobisphosphonates, containing nitrogen, second-generation drugs. More effective because of their selectivity when acting on osteoclasts and prolonged action, which can have, because They are not absorbed by osteoclasts, unlike non-nitrogen ones. These are drugs such as Pamidronate and Alendronate. Effective in osteoporosis due to menopause in women, in the treatment of cancer patients with metastases in the bones.

Nitrogen-containing products have already been introduced, which experts attribute to the third generation of bisphosphonates. Their active substances are ibandronate and zolendronic acids. Among the most common medicines they include Bonviva, Bondronat, Zometa.

Zometa (Zoledronate) has a special molecular structure (the presence of two nitrogen atoms in the side chain), which determines a higher the potential of zoledronic acid, and causes a sharp increase in the activity of the drug in comparison with the preparations of the previous one generation.

What you need to know when treating bisphosphonates

As you know, everything in the spoon represents a medicine in a cup can become a poison.

Therefore, when using bisphosphonates it is important to follow the dosage instructions and carefully read the list of contraindications and other necessary information specified in the annotation.

From the same considerations self-medication is dangerous.
Drugs can only be used as prescribed by your doctor!

Since bisphosphonates are sufficiently serious medical preparations, fraught with side effects, it is recommended to follow certain rules when applying them:

1. Take in the morning on an empty stomach, at the same time with a lot of water.
   To consume food after this is allowed no earlier than an hour.
2. Drink exclusively with ordinary still water. All other drinks will inhibit the action of the drug.
3. Within one and a half hours after taking, if possible, keep the vertical position. During this time, the medicine will reach the intestine, which minimizes its irritating effect on the walls of the esophagus and stomach.
4. It is advisable to take calcium or vitamin D in parallel with the bisphosphonate course, but use them with observance of two-hour time intervals. Simultaneous reception of these funds is excluded.

Parenteral bisphosphonates are administered intravenously by infusion (drop) method for 2-3 hours.

Rapid jet administration of drugs may cause acute renal failure, which can lead to death in the background of hypercalcemia accompanying oncological diseases.

Limitations for the use of bisphosphonates are:

• pregnancy,
• lactation period,
• age to 18 years,
• individual intolerance,
• renal failure,
• Gastrointestinal illness in acute phase.

If you strictly follow these tips, you will avoid complications or mitigate possible side effects of medications during treatment.

Osteogenone is a new effective drug used to treat osteoporosis and accelerate recovery after fractures of bones: http://pomogispine.com/lechenie/lekarstva/osteogenon.html.

Often, when you change the position of the body, in the hip joint outside sounds are audible: a crunch and clicks. Sometimes it is accompanied by pain. About the reasons, read the article.

Conventional X-ray examination can only reveal a strong degree of thinning of bone tissue, then how densitometry gives accurate results about the condition of the skeleton, so it is so important in diagnosing osteoporosis.

Side effects

Among the frequently occurring adverse effects of bisphosphonate administration are:

• in the digestive system - irritation of the gastric mucosa and duodenum, gastritis, bleeding, nausea, stomach pain, flatulence and constipation;
• headaches and muscle pains;
• arthralgia;
• kidney and liver diseases due to accumulation of toxic substances;
• hypocalcemia - lack of calcium in the blood;
• allergic symptoms.

If bisphosphonates are used unauthorized and uncontrolled, more serious complications, such as fibrillation - desynchronization of the heart, osteonecrosis of the jaw, susceptible fractures of the femoral bones.

However, the manifestation of all these undesirable symptoms is not observed in all patients. Correctly calculated course of treatment and adherence to the regimen helps to avoid the appearance of side effects and minimize the risk of complications.

Reviews

Since the introduction of bisphosphonates on the pharmacological market, these funds have earned a lot of positive feedback from both patients and professionals. Let us cite a few of them.

Svetlana, 56 years old:
"The doctor prescribed Bondronate six months ago. Already in the first month, pain in the knees and spine calmed down, the dream returned to normal. I'm happy with the drug, I do not have any side effects. "

Alexandra, 60 years old:
"During the menopause, I drank zoledronic acid, the doctor appointed. For three days my muscles ached and my head ached, my symptoms were the same as with the flu. She was saved by paracetamol. Saw the pills as expected, according to the regime. Nothing else bothered. "

Preparations of the third generation are very good.

However, they should be used with caution, strictly following the recommendations of the doctor for greater effectiveness and reducing the risk of side effects. "

Alexey, a rheumatologist:
"Bisphosphonates are an excellent remedy for those suffering from osteoporosis.

The therapeutic effect is manifested in the reduction of pain syndrome, strengthening of bone structure, harmonization of regenerative processes.

.

It does not do without side effects, which, however, in most cases, soon disappear with proper application. "

.

The main inconvenience is considered to be a complicated procedure for the use of the drug, however, this trouble is completely compensated for by the therapeutic effect produced.

Thus, bisphosphonates are truly effective in the treatment of osteoporosis, but require scrupulous following all the recommendations of specialists and are prescription drugs.

A source: http://pomogispine.com/zabolevaniya/osteoporoz/bisfosfonaty.html

Bisphosphonates for the successful treatment of osteoporosis

Bisphosphonates for the treatment of osteoporosis help to successfully cope with the manifestations of this pathology.

Thanks to them, it is possible to strengthen the structure of bone tissue, but at the same time to prevent hypercalcemia.

Drugs of this kind are successfully combined with hormone therapy, and therefore often recommended in the postmenopausal period.

What are bisphosphonates and how do they work with osteoporosis?

Bisphosphonates constitute a group of medical drugs that have been widely used in osteoporosis.

This name of the drug is deserved due to its special molecular structure, it contains 2 phosphonates, ie organic compounds that are saturated with phosphorus.

In medicine, bisphosphonates have been used since the beginning of the XIX century. Before that time, they were actively used in the chemical and industrial sectors.

Without the drugs of this group, the treatment of bone diseases actually never does.

Clinically proven that taking bisphosphonates in osteoporosis, it is possible to reduce the probability of bone fractures by at least 30-50%.

This is made possible by the fact that drugs are able to prevent the destruction of bone tissue.

Under the influence of certain constituents, the molecules of phosphonates and calcium ions are bound. Together they are absorbed into the bone.

Preparations of this group inhibit those enzymes that destroy pyrophosphonates.

The advantage of drugs is that they can only affect those parts of the bone where excess calcium is noted. Bisphosphonates are also similar with hydroxyapatite.

They also make it possible to avoid loss of phosphorus and calcium by the bone tissue. In the place of active reconstruction of bone tissue, osteoclasts absorb bisphosphonates. This ensures the absorption of the first, and then the reduction in the destruction of bones.

.

This characteristic is very important in the case of a patient with osteoporosis.

.

Some drugs of this type are able to change the relationship between osteoblasts and osteoclasts. As a result, a kind of chemical barrier arises that does not allow contact with osteoclasts and bones. Bisphosphonates are divided into 2 main groups:

• Simple, which in its composition do not contain nitrogen;
• aminobisphosphonates containing nitrogen in their composition.

Simple bisphosphonates

A group of nitrogen-free, so-called simple bisphosphonates, is represented by four basic preparations. This is Etidronate, Tiludronate, Ibandronate sodium and clondronate. Etidronate in its composition contains the following components:

• ethyldric acid;
• didronel;
• pleostat;
• ksidifon;
• sodium ethidronate.

It is suitable for use in osteoporosis and in cases of hypercalcemia. It has several forms of release (tablets, concentrate for oral use, solution for injections). Together with it, calcium and vitamin D preparations are used.

Tiludronate is prescribed to patients in the case when the bones are too soft, deformed, often break. Can improve bone density.

Klondronate has its constituents:

• clobber;
• bonnefos;
• sodium clodronate;
• syndronate;
• clodronic acid.

The drug prevents the development of osteolysis, can reduce pain. Getting into the patient's body, the drug combines with hydroxyapatite of bone tissue, then changes the crystal structure and prevents the destruction of phosphate-calcium crystals.

In fact, 80% of the absorbed acid is excreted by the kidneys of the patient, so people who already have problems with the urinary system should take the drug with caution.

It is available in the form of capsules for oral use and in the form of a solution for injection.

What are aminobisphosphonates and what is their advantage?

Aminobisphosphonates are those drugs that are indispensable in the treatment of osteoporosis, contain nitrogen in their composition.

They are more effective than non-nitrogen drugs, with particular caution they should be used by women. Aminobisphosphonates can not be taken in long courses.

The list of the best medicines of this type can be made the following:

1. Zoledronate. The bone tissue affects very selectively, only in the place where the bones are subjected to degenerative changes. The agent is capable of causing bone resorption by affecting osteoclasts. However, the agent can not negatively affect the mineralization. The main active substance in this case is zoledronic acid. Sold in the form of a concentrate for infusions.
2. Bondronate. In its composition contains ibandronic acid, which has a positive effect in the treatment of osteoporosis. It is appropriate to use this drug for the prevention of osteoporosis. Can be used by women after menopause. Successfully combined with sexual tableted hormones. Men are discharged in cases when there are real clinical manifestations of the disease. Bondronate can be used when a biochemical blood test recorded hypercalcemia.
3. Alendronic acid. A non-hormonal drug that is able to successfully correct bone metabolism. The agent is able to effectively stimulate osteogenesis. Sold in the form of tablets. It is accepted once a week. The duration of treatment is determined by the doctor in accordance with the patient's state of health.
4. Clodronic acid. Today is one of the drugs of experimental medicine, it is able to selectively reduce microphages. In pharmaceutics is produced under the names of Clodron and Bonefos. It plays the role of inhibitor of bone resorption. Reduces the likelihood of fractures, has analgesic effect.

Advantages and disadvantages of bisphosphonates

Long-term studies of the effect of bisphosphonates on the human body make it possible to state the high effectiveness of these drugs. They are effective for the treatment of osteoporosis of any stage.

Particularly useful, these medicines are for women after the full completion of the menstrual cycle.

A sharp cessation of the development of hormones that are habitual for the female body leads to fragility of bones, and therefore the body needs protection.

If osteoporosis occurs accompanied by cancerous tumors or metastasis of bones, bisphosphonates can reduce severe pain.

Other advantages of this type of medication are their good tolerability, and if the patient takes into account the contraindications and recommendations of the doctor, then they do not give any negative consequences.

Drugs in this group do not cause drowsiness or fatigue. There is no need to abandon the management of vehicles or complex technical processes after using these drugs. Bisphosphonates also have some drawbacks. These include:

1. Low bioavailability. The destination does not fall to the entire dose of the medicine, but only a small part of it, the other is naturally withdrawn with feces and urine.
2. Inconvenience of admission. The medicine provides for certain rules for their use. The patient should take them on an empty stomach and stay up for at least 1-2 hours after taking. Do not drink with a large amount of liquid.
3. Probability of allergic reaction. It is possible to overcome this deficiency with the help of antihistamines.

Possible side effects

Bisphosphonate preparations should be taken with extreme caution, because they can lead to serious side effects with regard to different systems:

1. Since most of the active substances of the drugs are excreted by the urinary system, the kidneys have a significant effect. When using aminobisphosphonates there is a high risk of toxic organ damage.
2. With too long use of medicines, pain, nausea, diarrhea or constipation, heartburn may occur. Less common is a violation of swallowing, erosive diseases of the esophagus, bleeding in the upper esophagus, gastritis, prolonged flatulence, lack of appetite, sensation of acid in the mouth.
3. There is a high probability of atrial fibrillation, tachycardia, arrhythmia. Increased risk of adverse reactions from the heart in the case of existing problems with the cardiovascular system.
4. Most often after taking bisphosphonates, hypocalcemia occurs. Occurs in cases where the dosage exceeds a doctor's defined rate or when the withdrawal of bisphosphonates into a vein becomes more complicated. With prolonged use of aminobisphosphonates, osteonecrosis of the jaw can develop - a disease accompanied by insufficient blood supply to bone tissue and destruction of the latter. In this case, the patient complains of very severe pain. Zoledronate is able to cause hip fractures. This is a consequence of blocking the restoration of bone tissue.
5. Problems with vision and eyes arise after taking bisphosphonates is not very common. In some cases, pain in the eyes, conjunctivitis or scleritis may occur.
6. Allergies can occur if the patient's body is sensitive to the components of the drugs. Most often there is redness of the skin, itching, a small rash. In more difficult situations, it is possible to develop eczema, urticaria, and Quincke edema.
7. General reactions. Bisphosphonates from osteoporosis can cause prolonged muscle pain, fever, general weakness, headache. All this is due to too rapid activation of T-lymphocytes.

Features of use

Bisphosphonates are those drugs that can not be used alone. Appoint and monitor their use should only be an expert. Drugs of this group are poorly absorbed in the gastrointestinal tract.

That's why doctors advise taking them on an empty stomach and at least an hour before a meal. But do not forget that bisphosphonates have an extremely negative effect on the stomach. Therefore, a person should help as quickly as possible to digest the remedy.

Do not hold the horizontal position after entering the tablet.

Because of poor absorption, the drug should be taken with caution. It is better to take calcium-containing drugs 2-3 hours after using bisphosphonates.

The next injections will not give such a strong reaction or will not manifest themselves at all. Given the temporary negative impact, there is no need to treat such symptoms.

For greater effectiveness of bisphosphonates, therapy with them should be performed in combination with calcium and vitamin D.

The main contraindication to the use of such drugs is renal failure. Before the beginning of treatment the patient must undergo a detailed examination.

It is forbidden to use bisphosphonates in the period of gestation or feeding the baby with breast milk, and even with:

• serious diseases of the cardiovascular system;
• pathologies and severe erosive diseases of the gastrointestinal tract;
• sensitivity to the drug.

Do not use bisphosphonates in pediatrics. For better effectiveness, the drug should be used at the same time.

It can be argued that bisphosphonates are a good option for fighting osteoporosis. With their help, it is possible to solve the basic problems with bone tissue damage.

But given the possible serious adverse reactions, it is not worth using these medications as a prophylaxis.

A source: https://OrtoCure.ru/kosti-i-sustavy/osteoporoz/bisfosfonaty-dlya-lecheniya.html

Review of bisphosphonates - preparations for the treatment of osteoporosis

articles:

Bisphosphonates - a group of drugs that have the ability to slow the destruction of bone tissue. The main direction of using these medicines is the treatment of diseases, accompanied by increased brittleness and brittle bones, such as osteoporosis.

Fosamax is the first medicine for osteoporosis approved by the US Food and Drug Administration 10 years ago. This bisphosphonate quickly restores bone tissue with a minimum of side effects

Bisphosphonates for the treatment of osteoporosis of any form (primary and secondary) are prescribed as the main drugs used in the first place (first-line drugs).They are indispensable in therapy, and their effectiveness is high and proven clinically - taking bisphosphonates 30-50% reduces the risk of bone fractures.

Let us consider in more detail what bisphosphonates are, how they function, what are the features of their use and the possible negative effects of treatment.

Mechanism of action

The name bisphosphonates was obtained because of the structure of the molecule, which includes two phosphonates - phosphorus-containing organic compounds.

Schematic representation of a bisphosphonate molecule

After taking the drug, the molecules of the active substance bind to calcium and penetrate into the bone tissue, accumulating and prolonged lingering in it. There bisphosphonates disrupt the work of special cells - osteoclasts.

Osteoclasts are normally involved in physiological processes of resorption and destruction (resorption) of old bone tissue and work simultaneously with osteoblasts forming new bone tissue. But with osteoporosis this interaction is broken: osteoblasts "do not have time" to create a new tissue, and osteoclasts quickly destroy the old, so the bones become thinner and become brittle.

If bisphosphonates are incorporated into the bone tissue, they reduce the activity of osteoclasts, prevent them growth, stimulate the process of self-destruction of osteoclasts, suppress signals that trigger their destructive act. This is how osteoporosis is treated: the bones do not thinner and can recover.

Click on photo to enlarge

Types of bisphosphonates

Bisphosphonates in composition are divided into nitrogen-containing and nitrogen-free.

Bezazotistye drugs (first generation)

This medication tidronate, tiludronate, clodronate.

Nitrogen-containing drugs (second generation)

This medication is pamidronate, alendronate, ibandronate. These drugs are more effective, the best among them is the modern zoledronate preparation, which includes two nitrogen atoms.

Zolendronate and ibandronate are convenient in use - zolendronate should be taken only once a year, and ibandronate - once a month (or you can inject ibandronate intravenously - once a quarter).

Also produced are two-component preparations containing alendronate and calcium, or alendronate and vitamin D.

Pros of drugs

Numerous studies have shown that long-term use of bisphosphonates helps to increase bone density and reduce the likelihood of fracture. They are relatively safe, well tolerated and have few negative side effects.

Minuses

But there are disadvantages to bisphosphonates.

disadvantages

• Low bioavailability - only a small fraction of the medication taken orally penetrates into the site of action.
• Inconvenience of taking: to reduce the risk of side effects of the drug, it must be drunk in the morning strictly on an empty stomach, washed down with a large amount of water (250-400 ml), and after intake for a minimum of 40 minutes you can neither eat nor drink to go to bed. Such rules for patients are difficult to fulfill and quickly tire them. According to patients' reviews, many of them refused permanent treatment with bisphosphonates or disrupted the regimen (and a violation of the regime led to an increase in the frequency of side effects).

Side effects

The main side effect is a negative effect on the gastrointestinal tract.

The drug can cause:

• inflammation of the mucosa and erosion in the lower part of the esophagus;
• gastritis, erosion and stomach ulcers;
• bleeding from the upper gastrointestinal tract;
• stomach ache;
• nausea, decreased appetite;
• heartburn;
• flatulence;
• constipation or diarrhea.

On the background of treatment of osteoporosis, there may be headaches, pains in muscles and bones.

Possible rashes on the skin and the development of allergic reactions.

Long-term treatment of osteoporosis with these drugs can lead to hypocalcemia (a decrease in the level of calcium in the blood), so bisphosphonates are necessary Combine with calcium preparations or vitamin D (but at different times of the day, sharing a bisphosphonate and calcium or vitamin D intake with a gap of at least 2 hours).

Conclusion

Bisphosphonates are effective drugs for the treatment of osteoporosis.

remember, thatThese are serious medicinal substances that have a multifaceted impact and interfere with the complex processes of the human body.

They are indispensable in the treatment, but in no case can they be taken independently and uncontrolled.

Assign and select the optimal drug, the duration of the course and dosage should only your doctor (this may be a rheumatologist, endocrinologist, traumatologist).

Svetlana Agrineeva

A source: http://SustavZdorov.ru/raznoe/bisfosfonaty-dlya-lecheniya-osteoporoza-244.html

Bisphosphonates from osteoporosis

Osteoporosis is a fairly common pathology of bone tissue.

It is characterized by a decrease in bone density, acceleration of the processes of their destruction, and an increased risk of fractures.

Most often this disease develops in women during menopause, it can also arise due to hormonal intake.

For the treatment of osteoporosis, different drugs are used. The most effective are those that slow down the destruction of bone tissue and increase its strength.

Bisphosphonates are especially often used for osteoporosis.

This group of phosphorus-containing drugs, which have a positive effect on metabolic processes in bone tissue.

Features of the action

Bisphosphonates are organic chemicals that have been used by humans since the 19th century. But first they were used only in the oil industry and for the production of fertilizers.

And only by the middle of the 20th century they found their beneficial effect on the processes of metabolism in bone tissue and began to be used to treat pathologies of the musculoskeletal system.

Received their name bisphosphonates because of their special structure: they contain two molecules of phosphonate, a phosphorus-containing compound.

.

In the bones, the processes of destruction and creation of new tissue are constantly occurring. This is controlled by special cells: osteoblasts and osteoclasts. In a healthy person, they are in balance.

.

But with some pathologies, for example, with osteoporosis, osteoclasts work more actively and destroy bone tissue.

Osteoblasts do not have time to restore it, so fragility and fragility of bones develop, they become thinner, gradually destroyed.

But the use of bisphosphonates allows to normalize this process.

Due to this, bone tissue has time to recover and become less fragile. In addition, these drugs have analgesic and antitumor effect.

When applied

Features of the action of bisphosphonates allow treating with their help diseases that are accompanied by increased brittleness of bones.

Often they are prescribed to women in menopause for the prevention of fractures. Especially need bisphosphonates in patients who are contraindicated taking estrogen.

They do not replace hormones, but help to slow the loss of bone calcium tissue.

.

These drugs are effective in all pathologies, which are accompanied by thinning and destruction of bones. This can be Paget's disease, hyperparathyroidism, imperfect osteogenesis, multiple myeloma, as well as the development of metastases in bone malignant tumors.

.

But most often used bisphosphonates from osteoporosis. They are drugs prescribed for this disease most often. Clinical studies have proven their effectiveness. Against the backdrop of such treatment, the risk of fractures in osteoporosis is halved.

Bisphosphonates are prescribed for any pathology accompanied by destruction of bone tissue, but most often - with osteoporosis

Advantages and disadvantages

Clinical studies of the use of bisphosphonates in osteoporosis have proven their high efficacy. With regular use according to the scheme recommended by the doctor, such drugs significantly reduce the risk of fractures, reduce pain, increase bone density.

But bisphosphonates have their drawbacks, which do not allow them to be used by some patients:

• a fairly high price - from 300 rubles for 4 tablets to 2 thousand per solution, especially since it takes a long time to take them;
• drugs in the form of tablets have low bioavailability;
• inconvenient features of their reception: in order to reduce the risk of side effects, you need to drink tablets with plenty of water, and then you can not go to bed 30-40 minutes;
• these agents often cause irritation of the mucosa of the gastrointestinal tract;
• Apply them a long time - usually several years, but the desired result for this time can not always be achieved.

In addition, the use of bisphosphonates is justified only with rapid loss of bone mass. After all, often these substances completely slow down the metabolism in the bones. That is, not only the processes of cell destruction stop, but also their recovery.

There are many different drugs from the group of bisphosphonates, only the doctor can choose what is needed for treatment

Types of drugs

All bisphosphonates used to treat osteoporosis can be divided into two groups. The first is nitrogen-free compounds, which appeared earlier.

To this group of simple bisphosphonates are such drugs as "Tiludronate "Tidronate "Clodronate" and others.

In addition, there are modern complex products containing, in addition to bisphosphonates, calcium or vitamin D. These drugs are based on alendronic acid - "Fosavans" and "Ostalon calcium."

"Zoledronate"

This preparation on the basis of zoledronic acid is a solution for infusions. With this composition, several drugs are produced: "Zometa "Aklasta "Desrotron "Metacoz "Zolendran" and others. All these drugs have one feature - they need to be used only once a year.

Intravenous infusion, containing 5 ml of the drug, lasts from 15 minutes to half an hour. Getting into bone tissue, zoledronic acid acts on osteoclasts, greatly slowing the process of cell destruction. But this substance does not influence the mechanical properties of bones or their mineralization.

These drugs are very serious, so they often cause side effects. Basically, these are headaches, fever, muscle aches, general malaise.

To reduce such symptoms, doctors recommend taking Ibuprofen.

In addition, to avoid loss of calcium, a few days before the infusion, you need to start taking calcium and vitamin D.

Pamidronic acid

Based on this bisphosphonate, such drugs are produced: "Pamidronate "Pamifos "Pamirid "Pamidia 90". They are a powder for the preparation of a solution.

These drugs are also used for intravenous injections. But they are done once a month.

.

It is necessary to inject the solution drip slowly, so that local negative reactions do not develop.

.

All funds based on pamidronic acid are well tolerated by patients. Side effects are rare. Basically it is a fever and flu-like symptoms. Therefore, these drugs are contraindicated only in pregnancy, lactation and individual intolerance.

The most common drug for the treatment of osteoporosis is Alendronate

Alendronate

One of the most effective aminobisphosphonates is alendronic acid.

This substance is contained in the preparations Alendronate, Alendra, Londromax, Ostemax, Fosamax, Ostalon and others. They are produced mainly in the form of tablets of 70 mg.

They are taken once a week. You need to take the pill in the morning, one hour before breakfast or taking other medications, always on the same day of the week.

Read more: How to cure osteoporosis

Alendronic acid has a strong irritant effect on the digestive tract, so you can not chew tablets, drink them with a lot of water - not less than a glass.

In addition, it is not recommended 30-40 minutes after taking the drug to go to bed.

In addition to the negative effect on the gastrointestinal tract, when taking these drugs, these side effects are possible:

• headaches, dizziness;
• weakness, malaise;
• pain in the joints and muscles;
• decrease in the amount of calcium in the blood;
• allergic reactions.

Bondronate

This drug is often prescribed for the prevention of osteoporosis in women during menopause.

It is also effective for treating this disease, as it stops the destruction of bone tissue.

In addition, "Bondronate" is able to normalize the level of calcium in the blood, therefore, its reception is indicated for hypercalcemia.

Etidronate

Analogues of this drug containing etidronic acid are Didronel, Pleoostat, and Xidiphon.

Most often, these funds are prescribed for Paget's disease, hypercalcaemia against a background of cancer or osteoporosis.

It is recommended to use them together with calcium and vitamin D.

Produced by means of etidronic acid in tablets or solution. Moreover, there are varieties of solution for oral administration and for intravenous administration.

To prevent fractures and reduce pain in osteoporosis, preparations based on clodronic acid

«Clodronate»

It is prescribed for osteoporosis, as well as for the prevention of bone metastases in certain forms of cancer.

Analogues of "Clodronate" are preparations "Klobir "Bonefos "Clodron" and "Sindronat".

These drugs have analgesic effect, slow down the activity of osteoclasts, stopping the destruction of bone tissue. Against the background of their administration, the probability of fractures is significantly reduced.

Ibandronate

Means based on ibandronic acid are used for various pathologies, accompanied by destruction of bone tissue. In addition to "Ibanronata this is "Bonviva" and "Bonnronat".

These drugs are produced in the form of tablets and a solution for infusions. Tablets are taken daily, and intravenous administration is shown once a month.

These funds are often prescribed to women during menopause on the background of hormone therapy.

Risedronate

This drug on the basis of risedronic acid is tolerated by patients well.

Therefore, it is often prescribed for osteoporosis, especially for women in menopause. "Risedronate" take 1 tablet a week, preferably always in one day.

An analogue of this drug with the same composition and reception characteristics is the medicine "Actonel".

Most bisphosphonates adversely affect the digestive system

Contraindications and side effects

In addition to the characteristics of each drug, they have common properties. All bisphosphonates have a damaging effect on the mucosa of the digestive tract.

When they are taken, these side effects may occur:

• nausea, vomiting;
• pain in the abdomen;
• flatulence, bloating, heartburn;
• the occurrence of erosion on the mucosa of the digestive tract or inflammation;
• development of gastritis or stomach ulcers;
• gastric bleeding;
• narrowing of the esophagus;
• an intestinal disorder.

In addition, any preparations of the bisphosphonate group can develop allergic reactions, most often - skin rashes.

It is also possible the appearance of headaches, dizziness, unpleasant sensations in the muscles and joints. Sometimes ulcers develop on the oral mucosa or even osteonecrosis of the jawbone.

Side effects of these drugs include also a violation of kidney function, and sometimes cardiac activity

.

All preparations of the bisphosphonate group are contraindicated in pregnancy, during breastfeeding, and also with individual intolerance. In addition, due to the fact that these substances are excreted from the body through the kidneys, they can not be taken if the functions of the urinary system are impaired.

.

Bisphosphonates are serious drugs, which in no case can not be taken alone. These substances interfere with metabolic processes in the body and, with uncontrolled application, can cause severe complications.

A source: http://MoyaSpina.ru/medikamenty/bisfosfonaty-osteoporoza