Bisphosphonates for the treatment of osteoporosis and othersgroups of drugs for osteoporosis

Update: December 2018

Osteoporosis is a decrease in bone density leading to
fragility and bone fractures, which leads to a tendency to
fractures. After 35 years bone mass (bone density)
begins to gradually decline, the process is significantly accelerated after
the entry of women into menopause. This condition
requires pharmacological correction with drugs for treatment
osteoporosis, without which the quality of life is significantly reduced and
developing disability.

ATыраженность и скорость прогрессирования заболевания зависит
from:

  • genetic factors
  • degree of physical exertion
  • lack of or excess calcium and ergocalciferol
  • individual history of fractures throughout life
  • tobacco smoking
  • alcohol abuse
  • rheumatoid arthritis
  • also low body weight.

Often, osteoporosis does not manifest itself, and the patient does not even
guesses it until a bone fracture occurs (see symptoms
and causes of osteoporosis). You can diagnose the disease on the basis of
densitometry data (level of bone mineral density),
which is measured by magnetic resonance imaging,
X-ray, ultrasound, CT and MSCT (multispiral computer
tomography).

What is osteoporosis and why is it so important
to treat?

Osteoporosis is a gradual decrease in bone density due to
leaching of minerals, which leads to a decrease in its strength and
повышению хрупbones. ATначале развивается незначительное уменьшение
bone density (osteopenia) and then it becomes
abnormally porous and compressible like a sponge. Such a violation
структуры скелета приводит к частым fractures.

Bone is made up of protein, collagen and calcium – substances that
ensuring its strength (see products containing calcium). With
imbalance of the listed components occur injuries, in
the form of cracks (fracture of the femoral neck) or fracture (compression
vertebral fracture of the spine). Some patients throughout
few years do not even know about the presence of damage.
You can suspect the development of the disease by the following symptoms:

  • chronic pain, localized at the fracture site;
  • reduction of height, curvature of the spine, slouch;
  • fractures with minimal physical activity, falling from
    heights of growth that are localized mainly in the region
    ribs, hips, spine, feet and wrists.
  • slow bone splicing.

Osteoporosis is not only medical, but also
a socio-economic problem that affects all layers
population around the world.

  • Hip fracture occurs more often in people 75-80 years old; other
    types of fractures are characteristic for 50-59 year olds and are reduced from
    by age.
  • Loss of 10% bone density increases fracture risk
    spine 2 times, femoral neck – 2.5 times.
  • By 2050, hip fractures in men will be 310%, and in women
    240% more than now.
  • Every 3 seconds a world is diagnosed with a fracture
    provoked by osteoporosis; spinal compression fracture
    – every 22 seconds.
  • The vast majority of patients at high risk of injury,
    associated with increased bone fragility (about 80%), including
    who have already had at least one fracture, are not aware of their
    diseases and do not take pills for osteoporosis.
  • Mortality after hip fracture in both sexes
    increases with age and is most likely within a year after
    injury and is about 20%. The main task in therapy
    osteoporosis is the prevention of fractures, by reducing
    loss of bone mass, increase its density and recovery
    bone strength. Early detection and timely initiated
    specific treatment significantly reduces the risk of injury and other
    complications of the disease.

About 200 million women suffer from this disease.
the world;

  • every tenth woman aged 60
  • fifth at the age of 70
  • two out of five after 80
  • two out of three after 90.

Modern drugs for the treatment of osteoporosis

AT настоящее время для предупреждения и лечения остеопороза
widely used medications that provide
antiresorptive effect and reduce the excretion of calcium from the bones
(see also the treatment of osteoporosis folk remedies). Bone
is a living, constantly updated structure. When speed
bone resorption (destruction) prevails over its speed
recovery (reconstruction) develop osteoporosis.
Consider drugs that prevent the violation of this
balance.

Bisphosphonates

Use of bisphosphonates for the treatment of osteoporosis is based
on their ability to inhibit osteoclast activity and slow down
bone loss, which allows osteoblasts to work more
efficiently. ATсе это приводит к укреплению кости и предотвращению
fractures (including the femoral neck, wrist, spine) in
people with osteoporosis:

  • Withем препаратов показан за 30 минут -2 часа до еды или через
    two hours after.
  • Drink a full glass water.
  • With этом всасывается не более 10 процентов препарата, которых
    enough to quickly begin the suppression of the pathological
    рассасывания bones.
  • Большая часть препарата откладывается в виде депо в bones. Than
    the older the patient, the worse the absorbability of his bisphosphonates.

This group includes drugs based on the following
active components:

Alendronat

Alendronic acid inhibits bone resorption by binding
hydroxyapatite, especially effective in postmenopausal
osteoporosis. Withменяются только по назначению врача. It is effective
for all types of osteoporosis and also for the prevention of primary
osteoporosis.

Alendronat 4 шт. 300 rub. Alenthal 20 pcs. 300 rub Ostepar 4 pcs 330 rub Forosa 4 pcs. 650 rub.
Alendrokern 4 pcs. 470 rub Ostalon 4 pcs. 480 rub. Tevanat 4 pcs. 760 rubles

Withменение: Обычно рекомендуется принимать по 10 мг лекарства в
day. This should be done no later than half an hour before use.
fluid, food, or another drug. The tablet needs to be washed down with the full
a glass of water (preferably distilled), after which you can not take
horizontal position for 30 minutes. ATсе это необходимо для
normal absorption of alendronate. Contraindications: Medicinal
The remedy is not prescribed to people suffering from contraction or disorder.
peristalsis of the esophagus, with a deficiency of calcium in the blood, allergies to
active substance, those who are not able to stand, and
pregnant and lactating women. Побочные эффекты: Alendronat может
cause dyspeptic disorders, epigastric pain, heartburn,
damage to the lining of the esophagus, flatulence, violation of swallowing
reflex, upset stool, headache and muscle pain,
allergic rashes, reduced blood concentrations of calcium and
phosphates.

Risedronate

  • Risedronic acid (Actonel, Rizendros 4 pcs. 880 rub.)

A drugы на основе данного действующего вещества являются
best drugs for osteoporosis caused by
corticosteroids are successfully applied also during menopause.
Risedronic Acid-Based Drugs Less
aggressively affect the esophageal mucosa and have more
pronounced anti-sparing effect on bone tissue than
alendronates.

Ibandronate

  • Bonviva 1 tab. 150 mg. 1800 rub., 1 syringe 5500 rub.
  • Boldronate 50 mg. 28 pcs. 13500 rub.

Ibandronic acid refers to nitrogen-containing bisphosphonates,
highly effective in suppressing bone destruction and activating
osteoclasts. Selectively affects bone tissue, thanks to
large affinity to its mineral components. Much
reduces the likelihood of skeletal complications when
malignant neoplasms. Prevents the release of factors
the growth of cancer associated with the functioning of osteoclasts suppresses
division and distribution of cancer cells. He is a drug
выбора для постменопаузального osteoporosis.

With использовании радиоактивного тетрациклина, ибандронат
contributes to its removal from bone tissue. Does not wash out minerals
from bone, and with hypercalcemia helps to normalize
calcium concentrations, both in blood and in urine. Discouraged
destructive changes in bone tissue caused by various
reasons.

Показания: A drug назначают для профилактики переломов при
bone metastases of a malignant breast tumor,
hypocalcemia, reducing the severity of pain, reducing
radiotherapy dosages; for the prevention of hypercalcemia with
various forms of cancer. Withменение: Особенности употребления
ibandronate tablets are the same as alendronates.
The recommended daily intake is 50 mg. Pill follows
swallow whole to prevent mucosal ulceration
surface of the oral cavity and esophagus. Ibandronic acid in the form
the solution is administered intravenously drip once a month. Infusion 6 mg
drug diluted in 100 ml of nat. p-ra should last no less
15 minutes. Contraindications: The drug is not prescribed to children, persons with
allergic to its components, as well as pregnant and lactating
moms.

Zoledronate

Zoledronic acid – bisphosphonate, with pronounced
anti-resistance properties that inhibits
osteoclast activity. The mechanism of this process is not completely
understandable. It is established that the drug does not cause demineralization.
bone tissue does not affect its formation and does not violate
mechanical bone functionality. Suppresses cell division
malignant neoplasm of the breast and myeloma, prevents
the growth of pathological tissues and the induction of apoptosis (death
cells). It has antimetastatic properties.

Blaster 3800 rub. Aklast 18900rub. Zometa 9800 rub. Resorb 7000 rub. Резокластин 4300 rub.

Показания: Zoledronate назначают для терапии остеопороза
of various etiologies, Paget’s disease, prevention of repeated
fractures and bone damage in patients with recent
stages of cancer. Shown as an early appointment (in the first 3 months
after hip fracture) and after joint replacement.
Withменение: 4 мг золендроната, разведенного в 100 мл физ. the solution
be introduced once every 3 to 4 weeks heated to room temperature
temperature view. Manipulation should last at least 15 minutes.
Drug treatment requires correction of vitamin D and calcium levels.
with diet or nutritional supplements. Contraindications: not
It is recommended to administer the drug to patients with hypercalcemia,
allergic reaction to its components, as well as during pregnancy
and during breastfeeding. Side effects: use
Zoledronic acid may be accompanied by:

  • pancytopenia (reduction of leukocytes, platelets and
    red blood cells), reducing the level of phosphate, calcium, magnesium and
    an increase in creatinine, urea, potassium and sodium in
    blood;
  • disorder of taste perception;
  • headache and abdominal pain;
  • violation of tactile sensitivity, tremor,
    dizziness;
  • increased anxiety, sleep disturbance;
  • dyspepsia, anorexia and stool;
  • respiratory distress, cough;
  • inflammation of episcleral tissue, conjunctiva and vessels of the eye,
    clouding of the vitreous body;
  • increased sweating, itching and rash, edema
    Quincke;
  • pain in muscles, joints, bones, cramps, stiffness
    joints;
  • heart rhythm disorder, hypertension;
  • acute renal failure;
  • the presence in the urine of blood and proteins;
  • local inflammatory reaction, localized in
    injections.

Antiresorptive (preventing bone loss),
obsolete

Calcitonin

Calcitonin (Миакальцик 5 амп. 1100 руб) является гормоном
thyroid gland and is used to treat osteoporosis. AT
pharmaceutical industry synthesize recombinant
human calcitonin, as well as pig and salmon calcitonin.

Side Effects: With the nasal route of administration may
nasal bleeding, runny nose, mucosal irritation occur,
nausea or vomiting. When using the injection form
Calcitoninа может появиться воспаление в месте укола.

The drug was previously used as antiresorptive (interfering
bone resorption). Had a rather modest probative
base, slightly reducing the frequency of vertebral fractures and arresting acute
pain associated with osteoporotic fractures. In recent years
accumulated data on the increase in the frequency of newly registered
oncopathology in patients using myocalcium. Drug removed
of the recommendations for osteoporosis treatment, remaining on the market in
as a means. Reducing pain in fractures
vertebrae with osteoporosis and for the treatment of Paget’s disease.

Raloxifene (Evista)

Raloxifene is a selective receptor modulator
estrogen ІІ generation, abbreviated as SERIER. The drug has
estrogen-like effect in bone tissue, but behaves like
antiestrogen in the endometrium. This allows you to warn him
possible side effects, including the risk of cancer.

Side Effects: Enhancement with Raloxifene is Possible.
severity of tides; risk of thrombosis, including
deep vein thrombosis and pulmonary embolism. Danger of occurrence
unwanted reactions are more likely during the first four
months of use.

To date, the effectiveness of the drug is not proven, as not proven
and reducing their risk of non-vertebral fractures.

Effective antiresorptive

Denosumab (Prolia)

Denosumab (60 mg. 22000 rub) is a human
antibody (IgG2), which blocks the formation and activity
osteoclasts that are responsible for bone resorption. Prolia
strengthens bones, increasing their mineral density, prevents
fractures. The drug is administered twice a year under the skin in the thigh area.
or belly. Assigned to eliminate osteoporosis:

  • in women after climacteric changes with a tendency to
    fractures of various localization;
  • in men with reduced bone density and fracture risk
    vertebrae on the background of hormone suppressive therapy.

Denosumab is the drug of choice in case of high
multi-factor fracture risk, as well as intolerance to other
methods of treatment of osteoporosis.

The drug is administered 1 time in six months. Investigated in clinical
trials since 2004. In parallel with osteoporosis, has been studied for
treatment of metastatic tumor lesions of bones. AT отличие от
bisphosphonate is not contraindicated in patients with renal
insufficiency.

Drugs that increase bone mass

Teriparatide (Forteo)

The drug is the only effective anabolic that stimulates growth.
bones. Shown in postmenopausal, primary, senile
osteoporosis and idiopathic forms in men. The course of therapy from 12 to
18 months. Is the drug of choice for inefficiency
bisphosphonates. AT России выпускается под наименованием Форстео.

Forteo (250 mkg. 26000 rub). is a synthetic
analogue of the human parathyroid hormone which
involved in the regulation of calcium metabolism. AT отличие от других
osteoporosis drugs that reduce bone resorption
tissue, teriparatide promotes the growth of new bone tissue.

This medicine is used to treat cases of severe
osteoporosis in women and men of various etiologies. A drug
stimulates the activity of osteoblasts, promotes the formation of new
костной ткани, делает кости прочнее и предупреждает fractures.

Method of application: the recommended dose is 20 mg per day.
Teriparatide is injected subcutaneously in the thigh or abdomen.

Forteo should not be used:

  • allergic to its ingredients;
  • children and adolescents;
  • pregnant or lactating;
  • in malignant neoplasms of bones;
  • during or after radiation therapy;
  • with hypercalcemia;
  • hyperparathyroidism and Paget’s disease;
  • severe kidney disease.

ATсе перечисленные в этой статье препараты относятся к
prescription drugs and are not intended to
self treatment Because of the potential for serious harm to health,
Before using these medicines, you must obtain
consultation of the doctor.

Prevention of osteoporosis

  • Stop smoking and abuse alcohol
  • Give enough physical activity (pool,
    bicycle)
  • For persons over 65 – exercise indoors in a sitting position and
    lying down
  • Adequate intake of calcium and vitamin D for adults
    700-800 mg of calcium in foods or in the form of carbonate or citrate and
    400 IU of vitamin D

    • For persons over 60 years old and people at risk (those taking GCS,
      those whose parents suffered from osteoporosis, women from early
      menopause, late menarche, prolonged lactation or episodes
      hyperprolactinemia, people with low physical activity or
      asthenic physique, men with hormonal disorders,
      persons with rheumatologic pathologies, cancer patients, individuals with
      hypogonadism, Itsenko-Cushing syndrome or thyrotoxicosis) 800
      IU of vitamin D and 1200 mg of calcium.
    • Persons taking systemic glucocorticoids, 1500 mg of calcium
      per day and 800 IU of vitamin D.

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