Effective drugs for the treatment of osteoporosis

Bisphosphonate drugs for the treatment of osteoporosis are a synthetic replacement for natural chemical compounds that strengthen human bone tissue by inhibiting bone resorption. Osteoporosis is a very terrible disease that makes human bones extremely fragile. People with this disease experience constant pain in their bone joints and fractures become more frequent.

carries a high risk of thinning bone tissue . A clinic where treatment is carried out using the most modern methods using the best drugs is the safest option for getting rid of this disease.

What is osteoporosis

Osteoporosis is a disease of skeletal tissue, characterized by a violation of the structure and strength of bones, as well as a decrease in bone mass. With this disease, bones become pathologically fragile and brittle. The literal translation of the Greek term “osteoporosis” means “porous bone.” The disease entails a violation of the integrity of the bones and spinal column, deformation and displacement of the vertebrae.

At the initial stage, a disease such as osteoporosis is hidden - patients do not complain because they do not experience pain or discomfort, while the mechanism of bone destruction has already been launched.

To diagnose osteoporosis, ultrasound examination and blood tests are used.

Preventive measures and timely treatment help prevent the development of progressive osteoporosis.

Vitamins for bones, joints and ligaments

First of all, let’s talk about the famous “calcium-vitamin D3” tandem. These are our bones' best friends! Calcium is a very important mineral that is responsible for their strength. But it cannot be fully absorbed without vitamin D3. Insufficient calcium intake, as well as vitamin D3 deficiency, increases the risk of developing a disease such as osteoporosis. At the same time, bone tissue loses strength, and a person risks a fracture at any time.

Important vitamins for joints and ligaments are C, A and E. With a lack of vitamin C, a person’s muscles and joints hurt, and the synthesis of a substance such as collagen, which ensures the strength and elasticity of cartilage tissue, is worse. But vitamins A and E help reduce the severity of inflammation in the joint and help improve their mobility.

The category “Vitamins for joints” also includes B vitamins. For example, nicotinic acid (vitamin B3) and pantothenic acid (vitamin B5) are very beneficial for cartilage. Together with other B vitamins, they help restore them and reduce the severity of pain.

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The best drugs for the treatment of osteoporosis

For the drug treatment of osteoporosis, drugs are used whose action is aimed at reconstructing the processes of bone tissue regeneration. According to the mode of action on bone tissue, drugs for osteoporosis can be divided into drugs that slow down degradation, as well as drugs that increase tissue synthesis, and complex effects. The list of relevant drug groups is quite extensive.

Calcitonins

Calcitonin has the property of slowing down the process of bone loss and preventing deformation of skeletal tissue. By acting on receptors for a similar substance in skeletal cells, calcitonin helps increase bone density and reduces vertebral fragility. This drug is prescribed as a nasal spray or subcutaneous injection. Calcitonin injections also have an analgesic effect. Oral administration of calcitonin is less effective: when it enters the gastrointestinal tract, part of the drug is destroyed. Undesirable side effects (digestive disorders, nausea or vomiting) are possible when using calcitonin.

Calcium salts

These substances increase bone turnover and improve its regulation. They are produced in the form of tablets - carbonates and citrates. Treatment with citrates is safer, since carbonates can provoke the development of urolithiasis. The indication for the use of calcium salts is senile osteoporosis. Having high absorption rates, these salts effectively help balance calcium balance in the body.

They are prescribed to be taken in small doses, during meals and before bed.

Vitamin D preparations

Vitamin D promotes the absorption of calcium and stimulates its absorption in the digestive tract. Therefore, it is advisable to take this vitamin simultaneously with calcium. It has been proven that a lack of vitamin D leads to low calcium levels in the blood. Vitamin D is indicated primarily in the treatment of osteoporosis in older people and in cases where the disease is caused by steroid drugs.

Bisphosphonates

The action of bisphosphonates prevents bone loss and improves skeletal density. Bisphosphonates also reduce the likelihood of fractures. They are indicated for the treatment of steroid-induced osteoporosis, as well as osteoporosis in women. Bisphosphonates are used both orally (capsules, solutions) and intravenously (in the form of injections).

Bisphosphonates in tablet form can cause gastrointestinal side effects, so it is best to take them 30 minutes before meals.

Anabolic steroid

During the treatment of osteoporosis, anabolic steroids are responsible for restoring the process of bone tissue formation and improving its mineral density. The effectiveness of anabolic steroids is obvious in the treatment of postmenopausal osteoporosis. Medicines of this type reduce the risk of fractures by almost half. The disadvantage of the drug is a side effect: patients may experience an increase in body weight.

Active metabolites of vitamin D

In the treatment of osteoporosis, active metabolites of vitamin D are prescribed. In particular, they are used for steroid and senile osteoporosis, and for damage to skeletal tissues. They stimulate better absorption of calcium and protect the spine from fractures. These drugs should be used with caution: taking them too often can cause kidney stones.

Fluoride preparations

Patients with osteoporosis are recommended to take fluoride supplements. These safe and effective products stimulate bone tissue regeneration and help increase bone density. The drugs have a particularly positive effect on the condition of the spine. They are prescribed for steroid osteoporosis and women during menopause.

Non-opioid analgesics

The course of osteoporosis of the spine is accompanied by the presence of a characteristic pain syndrome in the back. Pain can be acute or chronic and lead to psychological disorders (increased anxiety, depression). The use of non-opioid analgesics helps to avoid such phenomena. These drugs have analgesic, relaxation and neuroprotective effects.

Estrogens

In the treatment of osteoporosis, the use of tablets containing estrogen is indicated. Their use is effective during menopause and has proven to be a necessary hormonal therapy. Taking estrogen strengthens the bones of the spine, reducing the risk of displacement of the vertebrae, femur and other bones. However, such a drug is best used in the initial stages of the disease or for prevention purposes - breast cancer may be an undesirable effect.

Restoration of bone and cartilage tissue in an experimental model of osteoporosis under the influence of a new economical phytotherapeutic composition (Phytocost New)

Volkov E.E.1, Korsun V.F. 4, Izvolskaya M.S.2 Vasilenko A.M.3

1LLC HuangDi Medical Center, Moscow, Russia; 2FGBUN Institute of Developmental Biology named after. N.K. Koltsov RAS, Moscow, Russia. 3FGBU "National Medical Research Center for Rehabilitation and Balneology of the Ministry of Health of the Russian Federation", 4FGAUHE "Peoples' Friendship University of Russia"

The recovery of bone and cartilage in an experimental model of osteoporosis under the action of a new cost-effective phytotherapeutic composition (Fitokost New)

Volkov EE, Korsun VF, Izvolskaia MS, Vasilenko AM

Summary.

The urgency of the problem is determined by the widespread prevalence of osteoporosis, the lack of effectiveness and iatrogenic effects of drug therapy. Against the backdrop of many different herbal medicine recipes from the field of traditional medicine, scientific data on its use in osteoporosis is scarce and is presented mainly by foreign researchers. Previously, we showed that the multicomponent domestic herbal medicine Fitokost corrects disorders in cartilage and bone tissues caused by prednisolone in an experimental model of osteoporosis.

Purpose of the study: to determine the effectiveness of the new, more economical phytocomposition “Phytocost New” on the course of experimental osteoporosis.

Materials and methods. Experiments were carried out on 3-month-old Balb/c mice as a model of osteoporosis. The animals were divided into 6 groups: 1 – control group – intact animals. Animals of groups 2-6 were intramuscularly injected with prednisolone (1.0 mg/mouse) daily for 14 days. Animals of group 2 were sacrificed at the end of the last injection of prednisolone. Animals of the 3rd group did not receive the herbal medicine for 30 days. Animals of the 4th group received the previously obtained phytopreparation Fitokost (50 mg/mouse) orally daily for 30 days. Animals of groups 5 and 6 received the new phytocomposition Phytocost New in doses of 50 and 5 mg/mouse, respectively, for 30 days.

Results. A dose-dependent reparative effect of Fitokost New was revealed in the form of a decrease in the number of chondroblasts and restoration of bone tissue, similar to the drug Fitokost.

Conclusion. The effectiveness of Fitokost New, which has a significantly smaller number of components compared to the previously obtained drug Fitokost, is not inferior to it in its activity in restoring cartilage and bone tissue in a model of osteoporosis.

Key words : osteoporosis, prednisolone, Phytocost New, cartilage and bone tissue.

Abstract

Background. The urgency of the problem is determined by the wide prevalence of osteoporosis, insufficient effectiveness and iatrogenic effects of drug therapy. Against the background of many different recipes of herbal medicine from the field of traditional medicine, scientific data on its use in osteoporosis are scarce and presented mainly by foreign researchers. Previously we have shown that multi-component domestic phytopreparation Fitokost corrigiruet disturbances in cartilage and bone tissues caused by prednisone in experimental models of osteoporosis. The purpose of the study was to determine the effectiveness of a new, more efficient creation of phyto compositions “Fitokost New” on the course of experimental osteoporosis. Materials and methods . The experiments were carried out on 3-month mice of Balb/c line on osteoporosis model. The animals were divided into 6 groups: 1 – control group – intact animals. Animals of groups 2-6 were administered daily intramuscular injection of prednisolone (1.0 mg/mouse) for 14 days. Animals of the 2nd group were slaughtered at the end of the last injection of prednisolone. Animals of the 3rd group did not receive phytopreparation within 30 days. Animals of the 4th group received daily oral previously obtained phytopreparation Fitokost (50 mg/mouse) for 30 days. Animals 5 and 6 groups received new fitokompozitsiya the New Fitokost in doses of 50 and 5 mg/mouse, respectively, for 30 days. Results. Revealed dose-dependent reparative effect Fitokost New reduction in the number of chondroblasts and bone regeneration like a drug Fitokost. Conclusion. The effectiveness of the New Fitokost, which have significantly fewer components, compared to previously obtained drug Fitokost, not inferior to it in their activity in the regeneration of cartilage and bone tissue in a model of osteoporosis.

Key words: osteoporosis, prednisone, Fitokost New, cartilage and bone tissue

Introduction. The growing prevalence, insufficiently effective treatment methods, and the personal and public socioeconomic burden of osteoporosis [1-3] necessitate the search for new and improvement of already known approaches to its prevention and treatment [4-6]. However, the optimistic expectations associated with the widespread introduction into practice of many modern pharmaceuticals for its treatment are not fully justified. This is due to the high level of drug iatrogenicity [5], the high price and insufficient effectiveness of drugs. Therefore, the search for complementary approaches to correcting disorders observed in osteoporosis, including in the arsenal of naturopathic remedies, remains relevant.

In connection with medicinal iatrogenies, interest in herbal medicine (PT) has begun to revive, which is recognized as one of the safest methods of treating acute and chronic diseases, provided that the treatment is carried out by a specialist and not by the patient himself. However, data on the scientific basis and practice of using PT for osteoporosis are currently most widely presented in foreign, and primarily Chinese, literature [7-15] and to a lesser extent by domestic researchers [16, 17]. Among several patented domestic PT compositions intended for the treatment and prevention of osteoporosis [18-19], their effectiveness has been assessed for only one composition [20], called “Fitokost”. This composition includes components from more than 60 medicinal plants that have the most pronounced effect on individual parts of the pathogenesis of osteoporosis.

Using a model of osteoporosis induced in mice by the administration of prednisolone, it was shown that the Phytocost composition causes restoration of bone and cartilage tissue in the hip joints of animals [21]. A more pronounced effect was observed under the influence of phytocost with cyclodextrin [22]. The studied domestic phytocompositions differ from a number of foreign analogues in a significantly larger number of components included in it. The multicomponent nature of Phytocost is due to a wide range of pathogenetic mechanisms of osteoporosis and the desire for their total overlap. This approach is appropriate for polyetiological osteoporosis, but can also be considered as polypharmacy in other situations. The goals for the development of any therapeutic agents, along with ensuring their effectiveness and safety, should also include affordability for the general public. Based on this, we have developed a new PT composition for the treatment of osteoporosis “Fitokost New”, containing 20 components.

Purpose of the work: to study the effect of the new phytocomposition Phytocost New on the restoration of cartilage and bone tissue in an experimental model of osteoporosis.

Materials and methods

The Phytocost New composition was obtained by extracting 20 phytocomponents using a previously described method [20]. It contains such substances as the fruits of Caucasian Sophora, the grass of Astragalus wooliflorum, the roots of cinquefoil, the roots of common dandelion, the roots of comfrey, the grass of knotweed, the grass of European sage, the rhizomes of bergenia, the bark of gray aspen, the thallus of Icelandic moss, the leaves of nettle. dioecious, meadowsweet herb, salvia officinalis leaves, calendula officinalis flowers, corn silk, chaga mushroom, lemon balm leaves, maclea cordate herb, licorice roots, dihydroquercetin with arabinogalactan (6-10%). Dihydroquercetin is a bioflavonoid obtained from the butt part of the Siberian larch, an active antioxidant with anti-inflammatory, analgesic and immunomodulatory effects. Arabinogalactan is a polysaccharide, also obtained from larch wood, used to increase the absorption of drugs characterized by low bioavailability. It has antioxidant and anti-inflammatory effects, helps restore the structure of connective tissue [23].

According to test report No. 19066.05.03 dated July 13, 2018, Phytocost New complies with the technical regulations of the Customs Union TR CU 022/2011; TR TS 029/2012; TRTS 021/2011. Registration number of the declaration of conformity: EAEU No. RU D-RU.NA30.V.03475. Date of registration of the declaration of conformity: 08/02/2018.

Experiments were carried out on Balb/c mice, females, 3 months old, weighing 20-23 g (Stolbovaya nursery, Russian Academy of Sciences). The mice were kept under standard conditions, 5 individuals per cage, with controlled temperature (24o C) and lighting (for 12 hours) and with free access to water and food. To model osteoporosis, mice were administered intramuscular (IM) daily prednisolone at a dose of 1.0 mg/mouse for 14 days. The dose of administered prednisolone was selected based on our previously obtained data [21].

All animals were divided into 6 groups of 10 animals each: 1 control group – intact animals. Animals of groups 2-6 were administered prednisolone daily for 14 days. Animals of the 2nd group were sacrificed on the 14th day after the last injection of prednisolone. Animals of the 3rd group did not receive the herbal medicine for 30 days. Animals of groups 2 and 3 served as comparison groups. Animals of the 4th group received the previously obtained phytopreparation Fitokost orally daily at an active dose of 50 mg/mouse for 30 days. Animals of groups 5 and 6 received Phytocost New in doses of 50 and 5 mg/mouse, respectively, for 30 days.

Mice were killed by cervical dislocation and femurs were removed. The bones were fixed in 10% formaldehyde prepared in phosphate-buffered saline (0.02 M, pH7.6) for 24 hours at room temperature. Decalcified in 5% trichloroacetic acid for 24-48 hours. They were washed in phosphate-buffered saline (0.02 M, pH 7.6) and frozen in isopentane at -400 C. Next, sections 10 µm thick were prepared on a Leyca cryostat (Germany). The sections were dried at room temperature for 1 hour and stained with hematoxylin and eosin. Hematoxylin - 5 sec, differentiated in running water for 10 min, eosin - 15 sec, washed in distilled water, dried, cleared in xylene and embedded with synthetic resin. Analysis of the preparations was carried out on an Olympus Vanox AH BT3 microscope (Germany) magnification (x 100) and (x 40). The images were photographed and morphological analysis of the cells in the field of view was performed. To determine the significance of differences between the experimental and control groups of animals, the nonparametric two-sided Mann-Whitney test (U-test) was used.

Results and discussion.

After a 14-day administration of prednisolone to mice, a significant increase in chondroblast proliferation was observed in the femoral head of mice (Fig. 1B), which persisted for 30 days (Fig. 1C), compared to the control group of animals that did not receive prednisolone injections (Fig. 1A) . After daily administration of the Phytocost New phytocomposition for 30 days at a dose of 50 mg/mouse, restoration of the cellular composition of hyaline cartilage to its previous state was observed, similar to the effect of the Phytocost composition administered at the same dose (Figure 1D, E). At the same time, the number of chondroblasts in the field of view decreased to the control level (group 1) and the number of chondrocytes began to increase (table). After taking Phytocost New at a dose of 5 mg/mouse, the number of chondroblasts also decreased significantly, but to a lesser extent than at a dose of 50 mg/mouse (Fig. 1 E).

In the group of animals that did not receive the phytocomposition (group 3), after 30 days, violations of its integrity and chaotic orientation of collagen fibers were revealed in the bone tissue (Fig. 2B), as well as changes in cellular composition compared to the 1st control group ( table). After taking herbal medicines at a dose of 50 mg/mouse (groups 4, 5), the structure of bone tissue was almost restored to the control level (Fig. 2A, D, E). In addition, in the bone tissue of animals taking herbal medicines, a decrease in the number of osteoblasts and an increase in the number of osteocytes was observed compared to comparison group 3 (table). After taking Fitokost New at a dose of 5 mg/mouse, bone tissue breaks also completely disappeared (Fig. 2E) and the cellular composition changed, similar to the effect of the drug at a high dose, although less pronounced (table). A decrease in the number of chondroblasts in cartilage tissue and an increase in osteocytes in bone tissue under the influence of Phytocost New at a dose of 5 mg/mouse indicate a positive effect of this dose, which will appear fully, apparently, at a later date. It should also be noted that the appearance and behavior of animals that received the herbal medicine differed favorably from those that did not take it.

Conclusion. The new economical phytocomposition Phytocost New provides high efficiency in the restoration of cartilage and bone tissue in an experimental model of osteoporosis. Reducing the number of components of the presented composition causes a reduction in the cost of its production.

Table. The influence of phytocompositions Fitokost and Fitokost New on the cellular composition of cartilage and bone tissue.

Groups of animals, doses of herbal medicines, mg/mousechondroblasts
(M ± SEM)

n= 10

osteoblasts
(M ± SEM)

n=10

osteocytes
(M ± SEM)

n=10

1 gr. intact (control) 18 ± 38 ± 241 ± 3
2 gr. 14 days after administration of prednisolone 112 ± 726 ± 38 ± 2
3 gr. 30 days after administration of prednisolone 83 ± 622 ± 315 ± 3
4 gr. Phytocost, 50.0 mg\mouse 28 ± 3*13 ± 2*33 ± 3*
5 gr. Phytocost New 50.0 mg/mouse 25 ± 3*12 ± 2*34 ± 5*
6 gr. Phytocost New 5.0 mg\mouse 37 ± 4*16 ± 2 **21 ± 4**

Note: significance of the difference between the experimental and control groups: M±SEM; * p < 0.05 compared with groups 2 and 3; ** p < 0.05 compared with group 2; n – number of animals in each group.

Rice. 1. Histological study of the effect of herbal preparations Fitokost and Fitokost New on the cartilage tissue of the head of the hip joint of mice in a model of osteoporosis induced by prednisolone. (A) – intact; (B) – after intramuscular administration of prednisolone at a dose of 1 mg/mouse after 14 and (C) 30 days; (D) – after daily oral administration of the Phytocost phytocomposition at a dose of 50.0 mg/mouse for 30 days; (D) - after daily oral administration for 30 days of the phytocomposition Fitokost New at a dose of 50.0 mg/mouse and (E) at a dose of 5.0 mg/mouse. Hemotoxylin-eosin staining. Analysis of the preparations was carried out on an Olympus Vanox AH BT3 microscope (Germany), magnification (x 100) and (x 40).

Rice. 2. Histological study of the effect of herbal preparations Fitokost and Fitokost New on the femoral bone tissue of mice in a model of osteoporosis induced by prednisolone.

(A) – intact; (B) – after intramuscular administration of prednisolone at a dose of 1 mg/mouse after 14 and (C) 30 days; (D) – after daily oral administration of the Phytocost phytocomposition at a dose of 50.0 mg/mouse for 30 days; (D) - after daily oral administration for 30 days of the phytocomposition Fitokost New at a dose of 50.0 mg/mouse and (E) at a dose of 5.0 mg/mouse. Hemotoxylin-eosin staining. Analysis of the preparations was carried out on an Olympus Vanox AH BT3 microscope (Germany), magnification (x 100) and (x 40).

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4. Rudenko E.V., Buglova A.E., Rudenko E.V., Samokhovets O.Yu. Drug treatment of osteoporosis in adults. Educational and methodological manual, Minsk: BelMAPO, 2011—22 p. .

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13. Siu WS, Wong HL, Lau CP, Shum WT, Wong CW, Gao S, Fung KP, Lau CB, Hung LK, Ko CH, Leung PC. The effects of an antiosteoporosis herbal formula containing epimedii herba, ligustri lucidi fructus and psoraleae fructus on density and structure of rat long bones under tail-suspension, and its mechanisms of action. Phytother Res. 2013 Apr;27(4):484-92. doi: 10.1002/ptr.4743.

14. Shu B, Shi Q, Wang YJ. Shen (Kidney)-tonifying principle for primary osteoporosis: to treat both the disease and the Chinese medicine syndrome. Chin J Integr Med. 2015 Sep;21(9):656-61. doi:10.1007/s11655-015-2306-z.

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18. Trifonov V.N., Elistratova Yu.A., Elistratov K.G., Kurus N.V., Khomyakova I.V., Elistratova T.V. Composition for the treatment and prevention of osteoarthritis, osteoporosis and osteoarthritis of the joints. RF patent No. 2521227. application: 2013-03-28, patent publication: 06.27.2014. .

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23. Babkin V.A. Theoretical foundations and practical development of new drugs for medicine based on extractive substances of larch biomass. Chemistry of plant materials. 2014. No. 3: 111-119.

Consequences of osteoporosis

Among the consequences of osteoporosis, the following pathologies are most likely:

  • injuries of the musculoskeletal system - compression and other fractures (damage to the spine and peripheral bones);
  • neurological disorders up to loss of limb mobility (the reason for this is compression of the spinal cord due to osteoporosis);
  • osteoporosis interferes with human growth (in rare cases, the disease also affects children; in adults, osteoporosis reduces height by 3-4 cm annually);
  • poor posture (fragility and deformation of the vertebrae lead to curvature of the spine in the thoracic region).

These complications, which are consequences of a progressive disease, can be avoided by timely diagnosis and treatment of osteoporosis.

Satisfy your vitamin hunger

Many factors play a role in maintaining healthy bones, joints and ligaments, including adequate intake of vitamins. But, alas, even a balanced diet often does not meet the need for them 100%. In this situation, a proven vitamin and mineral complex will come to the rescue as an additive to the daily diet. Prevention and treatment of many diseases of the musculoskeletal system often cannot be done without them. By the way, such products are actively used by athletes, because with many types of physical activity, bones, joints and ligaments work to the limit and need support.

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