Lecture № 14

Drugs effecting on osteoporosis

Abdullaev Dzhumadil, pharmD

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International Medical University
Bone is a mineralized connective tissue that exhibits four types of cells: osteoblasts, bone lining cells,
osteocytes, and osteoclasts . Bone exerts important functions in the body, such as locomotion, support
and protection of soft tissues, calcium and phosphate storage, and harboring of bone marrow .
Bones are mostly made of the protein collagen, which forms a soft framework. The mineral calcium
phosphate hardens this framework, giving it strength. More than 99 percent of our body’s calcium is
held in our bones and teeth.

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Osteoporosis is a health condition that weakens bones, making them fragile and
more likely to break. It develops slowly over several years and is often only
diagnosed when a fall or sudden impact causes a bone to break (fracture).
The most common injuries in people with osteoporosis are:
• broken wrist
• broken hip
• broken spinal bones (vertebrae)
However, breaks can also happen in other bones, such as in the arm or pelvis.
Sometimes a cough or sneeze can cause a broken rib or the partial collapse of one
of the bones of the spine.
Osteoporosis is not usually painful until a bone is broken, but broken bones in the
spine are a common cause of long-term pain. Although a broken bone is often the
first sign of osteoporosis, some older people develop the characteristic stooped
(bent forward) posture. It happens when the bones in the spine have broken,
making it difficult to support the weight of the body.

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Losing bone is a normal part of ageing, but some people lose bone much faster than normal. This
can lead to osteoporosis and an increased risk of broken bones.Women also lose bone rapidly in
the first few years after the menopause. Women are more at risk of osteoporosis than men,
particularly if the menopause begins early (before the age of 45) or they've had their ovaries
removed. However osteoporosis can also affect men, younger women and children.

Many other factors can also increase the risk of developing osteoporosis, including:

• taking high-dose steroid tablets for more than 3 months •

other medical conditions – such as inflammatory conditions, hormone-related conditions, or
malabsorption problems •
a family history of osteoporosis – particularly a hip fracture in a parent •
long-term use of certain medicines that can affect bone strength or hormone levels, such as
anti-oestrogen tablets that many women take after breast cancer
• having or having had an eating disorder such as anorexia or bulimia •
having a low body mass index (BMI) • not
exercising regularly • heavy
drinking and smoking -5-
Many diseases and disorders have been associated with osteoporosis. For some, the
underlying mechanism influencing the bone metabolism is straightforward, whereas for
others the causes are multiple or unknown.
• Hypogonadal states can cause secondary osteoporosis. Women, estrogen deficiency,
men, testosterone deficiency.
• Endocrine disorders that can induce bone loss include Cushing's syndrome,
hyperparathyroidism, hyperthyroidism, hypothyroidism, diabetes mellitus type 1 and 2
• Malnutrition, parenteral nutrition and malabsorption.
• People with rheumatologic disorders such as rheumatoid arthritis, ankylosing
spondylitis, systemic lupus erythematosus and polyarticular juvenile idiopathic arthritis.
• Chronic kidney disease can lead to renal osteodystrophy.
• Hematologic disorders.
• Several inherited disorders.
• People with scoliosis.
• People with Parkinson's disease. -6-
 Osteoporosis occurs when bones lose minerals, such as calcium,
more quickly than the body can replace them, leading to a loss of
bone thickness (bone mass or density). As a result, bones
become thinner and less dense, so that even a minor bump or
accident can cause serious fractures. These are known as
fragility or minimal trauma fractures. Two thirds of fractures of
the spine are not identified or treated, even though they nearly
all cause pain and some disability.
Osteoporosis can be easily diagnosed on a special type of x-ray
known as a Dexa scan. This machine determines bone mineral
density (BMD).
Bone Densitometry (DEXA), uses a very small dose of
radiation to produce pictures of the inside of the body to
measure bone mineral density or bone mass.

Normal bones → osteopenia → osteoporosis

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 Class drugs effecting on osteoporosis
1.Biophosphonates:
Clodronate 4.Parathyroid hormone:
Alendronate (Binosto, Fosamax) Teriparatide (Forteo). 
Ibandronate (Boniva) Abaloparatide (Tymlos)
Zoledronic acid (Reclast, Zometa)
2.Monoclonal antibody medications: 5.Calcitonin (Miacalcin, )
Denosumab (Prolia, Xgeva)
Romosozumab (Evenity). 6.Calcium and vitamin D supplements
(Fortical)
3.Hormone-related therapy:
Raloxifene (Evista) ( Estrogen replacement therapy).
Testosterone (Testosterone replacement therapy).

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 RANKL (receptor activator of nuclear factor
Monoclonal antibody medications kappa-B ligand)
Prolia® is an antiresorptive RANK Ligand inhibitor, and its mechanism is
as an essential mediator of osteoclast activity, increased RANK Ligand may lead to increased bone loss
Prolia® targets and binds RANK Ligand, inhibiting osteoclast formation, function, and survival
Treatment Of Postmenopausal Women With Osteoporosis
At High Risk For Fracture
Treatment To Increase Bone Mass In Men With
Osteoporosis
Treatment Of Glucocorticoid-Induced Osteoporosis
Treatment Of Bone Loss In Men Receiving Androgen
Deprivation Therapy For Prostate Cancer
Treatment Of Bone Loss In Women Receiving Adjuvant
Aromatase Inhibitor Therapy For Breast Cancer
Injection given by a health
care provider twice a year

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 The recommended dose for osteoporosis
is 60 mg orally each day.
Estrogen replacement therapy
The mechanism of action of raloxifene
Most common documented adverse effects of
occurs through binding to estrogen
raloxifene are hot flashes, flu-like symptoms,
receptors. This binding results in
muscle spasm, arthralgia. Less common effects
activation of estrogenic pathways
are insomnia, vomiting, sinusitis, deep venous
(estrogen-agonistic effect) and blockade
thrombosis
(estrogen-antagonistic effect) in tissues
that express estrogen receptors.
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 Testosterone Replacement Therapy 
In some studies, osteoporotic men undergoing TRT
have been shown to have increased bone density,
though BMD does not reach normal adult male levels.
Mechanism of action
Testosterone and its androgenic metabolite,
dihydrotestosterone, exert biological effects directly
through binding to the androgen receptor and indirectly
through aromatization of testosterone to estradiol, which
allows action via binding to the estrogen receptor (ER).
Side• Irritation, redness, pain, tenderness, swelling, 1 capsule a day
toughening, or blistering of gums
effects•
stinging or swelling of lips
• unpleasant or bitter taste in mouth
• difficulty tasting food
• headache
• acne IM 1ml once
• breast pain or enlargement - 12 - a month
Class Drug Dosing How it works Risks/side effects
gastrointestinal problems,
such as trouble swallowing,
Bisphosphonates Alendronate daily or weekly tablet or strengthens bones by inflammation of the
(Fosamax, weekly effervescent tablet slowing the rate at esophagus, and
Binosto) that shoud dissolve in which osteoclasts ulcersosteonecrosis (death
water remove bone of bone tissue) in the jaw
(rare)
Ibandronate monthly tablet or injection strengthens bones by
(Boniva) every three months slowing the rate at fracture of the thighbone
which osteoclasts (femur) with more than five
remove bone years of use (rare)
 

Risedronate daily, weekly, or monthly strengthens bones by irritation at the injection

(Actonel, Atelvia) tablet slowing the rate at siteflu-like symptoms—
which osteoclasts headache, muscle aches,
remove bone feverfracture of the
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thighbone (rare)
 
Class
  Drug
  Dosing
  How
  it works Risks/side
  effects
Calcitonin calcitonin daily nasal inhibits bone allergic reactionssmall
(Miacalcin, spray or removal by increase in cancer risk
Fortical) injection osteoclasts, and
increases the rate of
new bone formation
by osteoblasts
Parathyroid teriparatide daily increases the leg cramps nausea
hormone (Forteo) injection number of bone- dizziness
forming osteoblasts
Monoclonal denosumab injection prevents the low blood calcium skin
antibody (Prolia) given by a development of infections and rash
health care bone-removing osteonecrosis of the jaw
provider osteoclasts (rare)
twice a year fracture of the thighbone
(rare)

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 Teriparatide is manufactured using a strain of Escherichia
coli modified by recombinant DNA technology.
Teriparatide (recombinant human parathyroid
hormone) is a potent anabolic agent used in the
treatment of osteoporosis.

FORTEO is a prescription medicine used to treat

postmenopausal women who have osteoporosis
who are at high risk for having broken bones
(fractures) or who cannot use other osteoporosis
treatments.
Common side effects of Forteo include:
Each cartridge, pre-assembled into a delivery • nausea
device, delivers 20 mcg of teriparatide per dose • joint aches
each day for up to 28 days . • pain
 Abaloparatide 
Brand name: Tymlos
80mcg/40mcL (prefilled pen delivers 30 daily doses of 80mcg)

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Calcitonin is a hormone that is produced in humans by the parafollicular cells of
the thyroid gland. Calcitonin is involved in helping to regulate levels of calcium
and phosphate in the blood, opposing the action of parathyroid hormone. This
means that it acts to reduce calcium levels in the blood. However, the
importance of this role in humans is unclear, as patients who have very low or
very high levels of calcitonin show no adverse effects.
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 Calcium D3 Nycomed Forte
regulates calcium and phosphorus
metabolism in the body (bones,
teeth, nails, hair, muscle).
Decreases resorption (resorption)
and increases bone density, filling
the lack of calcium and vitamin
D3 in the body is required for
mineralization of teeth.
chewable pills 1 pill 2 times a day
for treatment and prevention of
osteoporosis
Calcium is involved in the regulation of nerve conduction, muscle contraction and is a
component of the blood coagulation system. Vitamin D3 increases calcium absorption in the
intestine. The use of calcium and vitamin D3 prevents the increase in the production of
parathyroid hormone (PTH), which is a stimulator of increased bone resorption (leaching
calcium from the bones).
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 M
Bishkek city
Manas street 6

Rp Zoledronic acid 4 mg-5ml.

D.t.d № 1
Sig: 5ml IM once a year

17.05.2021
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 M
Bishkek city
Manas street 6

Rp: Prolia 60 mg -1ml.

D.t.d № 1
Sig: 1 ml IM twice a year.

17.05.2021
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 M
Bishkek city
Manas street 6

Rp: Evista 60 mg tab.

D.t.d № 28
Sig: 1tab. a day

17.05.2021
 M
Bishkek city
Manas street 6

Rp: Forteo 20 mcg-2.4ml pen.

D.t.d № 1
Sig: 1dose (20mcg) a day

17.05.2021
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 M
Bishkek city
Manas street 6

Rp Calcitonin Salmon 3.7 ml.

nasal spray
D.t.d № 1
Sig: 1 spray into one nostril a day

17.05.2021
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 M
Bishkek city
Manas street 6

Rp: Calcium-D3 nicomed tab.

D.t.d № 100

Sig: 1 pill 2 times a day

17.05.2021
 Thank you for your attention !

Abdullaev Dzhumadil, pharmD

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International Medical University