Osteoporosis drugs for menopause

Osteoporosis is a bone disease in which, due to the formation of voids in the bones, they lose strength, become brittle and fragile, and bone mass decreases. Women are twice as susceptible to this disease as men. Women during menopause are at increased risk. Studies have shown that only in the first 5 years after the onset of menopause, the bone mass of the spine decreases by 3%. This is due to the fact that during menopause, the production of the hormone estrogen, which increases the rate of formation of so-called osteoclasts (cells that remove bone tissue), is significantly reduced.

During a woman's reproductive age, there is a balance between osteoclasts and osteoblasts (cells that create new bone tissue). Violation of this balance leads to osteoporosis. As a result, calcium is "washed out" of the body's bones, which makes them rarefied and porous. The disease manifests itself in frequent fractures, back pain due to joint deformation. Osteoporosis drugs during menopause are intended to play a role in preventing fractures.

Bisphosphonates in the treatment of osteoporosis in menopause

The primary task of medicine is to correct the synthesis of osteoclasts and osteoblasts in the bone tissues of a woman's body. Pharmacology helps to solve it, having introduced into medical drug practice a group of drugs called bisphosphonates. In action, they are similar to natural pyrophosphates, which participate in the regulation of metabolic processes in bone tissue. Bisphosphonates inhibit the production of osteoclasts, put a barrier between them and osteoblasts, and also have an antitumor and analgesic effect.

Bisphosphonates have been on the pharmacological market for about 60 years and are deservedly recognized in the field of treatment of osteoporosis in women during menopause and its prevention. They are well tolerated by patients, they have few side effects. The release form is mainly in tablets, but a newer generation of bisphosphonates is produced in powders for injections. The chemical composition of bisphosphonates can be simple and nitrogen-containing, the effectiveness of the latter is much higher. The most commonly used nitrogen-containing bisphosphonates include alendronate, risedronate, ibandronate, zoledronic acid. The duration of taking bisphosphonates is very long (3-5 years).

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Bisphosphonates in tablet form

Alendronate is a drug in the form of tablets of 10 mg and 70 mg, has proven high efficiency, reduces the risk of local fractures by 50% and multiple fractures by 90%. The pharmacodynamics of the drug is to suppress osteoclasts in the bone, which will lead to the restoration of the balance between the removal of bone tissue and the formation of new, increasing the density, and therefore the strength of the bone. Pharmacokinetics indicates low bioavailability of the drug, so it is taken in the morning on an empty stomach and washed down with plenty of water (a glass or one and a half). After taking alendronate, you must not eat anything for at least an hour and not lie down horizontally. For treatment, you need to take a tablet of 70 mg once a week, or 10 mg daily. If you take it once a week, you must stick to the same day. The drug is excreted from the body unchanged. Contraindicated in pregnant women, with hypersensitivity to the components of the drug, renal failure. It is necessary to approach the drug intake with caution in case of vitamin D deficiency and gastrointestinal diseases. Side effects in the form of nausea, vomiting, heartburn, allergic reactions, malaise, general weakness are possible. In case of overdose, there may be diarrhea, nausea, ulceration and erosion in the gastrointestinal tract.

When alendronate is taken simultaneously with calcium preparations, the absorption of alendronic acid, which is part of its composition, is reduced. Non-steroidal anti-inflammatory drugs, including acetylsalicylic acid, can increase the negative impact of alendronic acid on the gastrointestinal tract.

It is recommended to store the drug for no more than 2 years in a dry place at a temperature not exceeding 25°C.

Risedronate is a tablet packaged in 35 mg and 75 mg, coated with an orange shell. Suppresses osteoclasts, promotes an increase in bone mass, strengthens the skeleton, thereby reducing the risk of fractures in postmenopause. A tablet of 35 mg is taken once a week, on the same day, 75 mg - two days in a row, one tablet on the same days each month. Do not crush the tablet, drink it whole in the morning half an hour before meals, washing it down with plenty of water, do not lie down for 30 minutes after taking it. The maximum concentration of the drug in the body occurs an hour after taking it. Half of the absorbed dose is excreted in the urine within 24 hours. The unabsorbed drug is excreted unchanged in the feces. Risedronate can have side effects in the form of headache, nausea, diarrhea, depression, insomnia, allergic reactions. Contraindicated for pregnant women, children and adolescents under 18, in case of renal failure, in case of inability to take a vertical position. Overdose may cause hypocalcemia – low calcium content in the blood. No studies on the reaction with simultaneous administration with other drugs have been conducted, but it is assumed that drugs and food containing aluminum, magnesium, iron, calcium can reduce the absorption of risedronic acid. The shelf life of the drug is 3 years, at a temperature not exceeding 25°C in a dry place. Available on prescription.

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Bisphosphonates in other forms of release

Taking the above-described bisphosphonates requires punctuality in taking the drugs from the patient, so it does not always lead to clinical effectiveness. Currently, new highly effective bisphosphonates have appeared on the market of medical drugs, which are taken less often and have different routes of administration, i.e. different forms of release. These include ibandronate and zoledronic acid.

Ibandronate - in the form of tablets of 150 mg is taken once a month according to a regimen similar to taking alendronate and risedronate, and in the form of intravenous injections - once every three months, the dose is 3 mg.

Zoledronic acid is a white powder or porous mass in a vial, weighing 4 mg. The contents of the vial are dissolved in 5 ml of water for injection, the resulting liquid is diluted with a glucose solution (5%), or 100 ml of sodium chloride (0.9%). The injection is done once a year (5 mg) from a freshly prepared preparation and has minimal negative consequences, since it is similar to the mineral component of bone tissue. Contraindicated for pregnant women, lactating women, and renal failure. Side effects are similar to those inherent in other bisphosphonates and are observed in a third of patients. But there are also peculiarities, after the injection, flu-like symptoms may be observed for three days: fever, chills, bone pain. No significant reactions have been noted when interacting with other drugs, except that it is used with caution simultaneously with diuretics. The shelf life of the drug is 2 years, store in a place protected from light at a temperature not exceeding 25°C.

A combination of bisphosphonates and vitamin D is also successfully used to treat osteoporosis during menopause. These drugs include fosavans and ostalon calcium. In addition to alendronic acid, they also contain calcium. The regimen is similar to alendronate.

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Other drugs in the treatment of osteoporosis during menopause

Strontium ranelate - corrects metabolism in bone and cartilage tissues, restoring the balance between the synthesis and removal of bone tissue from the bone in favor of the former. Release form - powder 2 mg, for administration dissolve in 250 ml of water and drink once a day at night, but not earlier than 2 hours after calcium and vitamin D, in combination with which it is prescribed. The shelf life of the prepared solution is no more than a day. It has contraindications for pregnant women, nursing mothers, patients with renal failure, venous thromboembolism, bedridden patients and temporarily bedridden after surgery. Side effects include nausea, vomiting, skin rashes, muscle pain. If the instructions for taking the drug in combination with food are violated, the absorption of strontium ranelate decreases. When taking the recommended dose, overdose symptoms were not observed.

Denosumab is a biological drug, an antibody produced by the immune system and used to suppress osteoclasts. It is administered subcutaneously and is convenient to use, as it is injected once every six months. Good tolerability of the drug is noted.

Salmon calcitonin is a hormone that regulates calcium metabolism in the body by blocking its release into the blood from bone tissue. At the same time, an analgesic effect on the patient's body was also established. It is available in the form of an injection solution. It can be administered both subcutaneously and intramuscularly. It has the property of being quickly absorbed into the blood, reaching a maximum concentration in an hour and a half. It is excreted from the body by the kidneys. It has contraindications in case of intolerance to the components of the drug. There have been cases of decreased calcium levels in the blood. It is not recommended for use by pregnant women and during lactation. The dose of the drug is determined by the doctor depending on the severity of the disease and ranges from 50 to 100, sometimes up to 400 IU (international unit of action of the substance) per day. The duration of treatment is from two weeks to six months. Side effects may include nausea, headache, diarrhea, decreased visual acuity, joint and muscle pain. Injection ampoules are stored for no more than three years.

Estrogen-gestagens - their action is aimed at replacing the lack of estrogen during menopause, and this is accompanied by an increase in bone mineral density. However, the drug is effective only during the intake, after stopping its intake, all indicators return to the previous level.

Recently, homeopathic remedies consisting of at least 5 components have appeared for the treatment of osteoporosis during menopause. However, they have not been sufficiently studied to provide clear recommendations for their use, and they are very expensive.

As we can see, the pharmacological market for the treatment of osteoporosis during menopause is quite extensive, but most drugs are intended for very long-term use, which often leads to interruption of treatment. Women are encouraged by the emergence of new drug forms (in the form of injections), which make it possible not to strain themselves in tracking the intervals of drug intake, but to make 1-2 injections per year.