1. Chapter Drugs used for the treatment of osteoporosis
Department of pharmacology
Liming zhou
2018.9

2. Contents Osteoporosis Antiresorptive drugs Bone-forming drugs
Mineralization drugs

4. Osteoporosis
Osteoporosis is a disease characterized by low bone mass (bone thinning) that leads to fragile bones and an increased risk of fractures of the hip, spine, and wrist.
Normal
Osteoporosis
Severe osteoporosis

5. Osteoporosis —symptoms
Common symptoms :
Back pain
Stooped posture
Fractures

6. [ Osteoporosis—types Primary osteoporosis Secondary osteoporosis
Postmenopausal osteoporosis
Primary osteoporosis
Senile osteoporosis
Secondary osteoporosis
Idiopathic osteoporosis

7. Osteoporosis—risk factors
Factors you cannot change
Gender Age; Body size ;Ethnicity; Family history
Factors you can change
Sex hormones ; Anorexia nervosa; Calcium and vitamin D intake; Medication use; Lifestyle; Cigarette smoking; Alcohol intake

8. Osteoporosis—diagnosis
The Bone Mineral Density Test (BDT)
Detect low bone density before a fracture occurs
Confirm an osteoporosis diagnosis if you already have one or more fractures
Predict your chances of having fractures in the future
Determine your rate of bone loss and monitor the effects of treatment

9. Osteoporosis—diagnosis
Bone Mass Density
The National Osteoporosis Foundation Recommends a BDT if: You use medications that cause osteoporosis
You have type I diabetes ,liver disease, kidney disease or a family history
You experience early menopause
You are postmenopause over 50 and have at least one risk factor
You are postmenopause over 65 and never had a test

10. Osteoporosis—treatment
Comprehensive treatment for osteoporosis deals with:
  Proper nutrition
Exercise
Safety issues to prevent falls
Medications

11. Osteoporosis—medications
Antiresorptive drugs: Bisphosphonates, calcitonin, estrogen
Bone-forming drugs: Parathyroid hormone, androgen
Mineralization drugs: Calcium and vitamin D

12. Antiresorptive drugs Bisphosphonates(双磷酸盐）—Pharmacological
Slow bone loss
Increase bone density
Reduce the risk fractures

13. Bisphosphonate—clinical application
Osteoporosis in men and postmenopausal women
Preventing and treating osteoporosis due to glucocorticoid steroid medications
Treating high blood calcium levels due to cancer 
Treating multiple myeloma or solid tumor cancers that have spread to the bone

14. Bisphosphonate—side effects
Nausea ,abdominal pain and indigestion
 Rash and itchy skin
 A temporary increase in parathyroid hormone and serum transaminase（血转氨酶）

15. Calcitonin
Calcitonin analogues (which are manufactured versions of calcitonin) can be useful for treating osteoporosis by slowing the breakdown of bone.
Calcitonin is a delicate molecule that would be destroyed by the digestive tract, it must be taken by nasal spray or by injection
With side effects of nausea , vomiting and allergic rash et al.

16. Estrogen Therapy—application
Estrogen therapy (ET) reduce bone loss, increase bone density in both the spine and hip, and reduce the risk of hip and spine fractures in postmenopausal women.
ET is approved for preventing postmenopausal osteoporosis and are most commonly administered in the form of a tablet or skin patch（经皮吸收）.  

17. Estrogen Therapy—side effects
Taking estrogen alone increases a woman's risk of developing cancer of the uterine lining (endometrial cancer).
To reduce this risk, women who still have a uterus (who have not had a hysterectomy（子宫切除）) should usually take a progestin in combination with estrogen

18. Selective Estrogen Receptor Modulators
Selective estrogen receptor modulators (SERMS) are drugs that act like estrogen at some receptors
It acts like estrogen for preventing bone loss and improving cholesterol.
Currently, only raloxifene （雷洛昔芬）that is approved to prevent and treat osteoporosis .

19. Bone-forming drugs Parathyroid hormone(PTH)—mechanism
With both catabolic and anabolic actions
Low dose: PTH stimulate bone turnover and is associated with bone formation（成骨作用）
High dose: PTH increase the rate of bone resorption followed by slower rate of bone formation（破骨作用）

20. Parathyroid hormone(PTH) —application
Osteoporosis
Primary parathyroid function decline
(Intake  vitamins D and calcium together)
Generally applies only to first aid

21. Androgen and anabolic hormone
—mechaism
Androgen can promote the synthesis of protein and collagen, stimulate bone formation and retention of calcium, phosphorus, and potassium.

22. Androgen and anabolic hormone —application
male osteoporosis
Side effect is bigger, the dose of treatment and the pros and cons of relationship is still in the further research

23. Mineralization drugs Calcium
Adding bone mineral and promoting bone mineralization
vitamin D3
Increase the absorption of dietary calcium and phosphorus, maintain the balance of calcium and phosphorus and increase the activity of osteoblasts

24. Calcium—application
Acute or chronic hypocalcemia; Tetany disease（手足抽搐）Rickets（佝偻病）; Osteomalacia（软骨病）, osteoporosis, parathyroid function impairment
Magnesium poisoning counterpoison（镁中毒解救）
(One key piece of advice is to take your calcium in several small doses throughout the day) .

25. vitamin D3—application
Osteoporosis
Chronic renal failure
For treatment and prevention
of vitamin D deficiency
Psoriasis （银屑癣）

27. Key Concepts
Osteoporosis is a disease of bone that commonly occurs in elderly people, and is characterized by the degeneration of bone superstructure, a decrease of bone strength , an increase of bone fragility and thus an increased risk of fracture.
Drugs available for the prevention and treatment of osteoporosis are catalogued into three types in terms of their actions on affecting calcification and boneover.

28. Key Concepts
Antiresorptive agents, including bisphosphonates, calcitonin, estrogen and iprioavone which decrease the rate of bone loses through inhibiting the activity osteoclasts（破骨细胞）.
The second group agents including fluoride,parathyroid hormone and androgens that promote bone formation by stimulating the activity of osteoblasts（成骨细胞） . .

29. Review questions
Please describe the classification and characteristic of osteoporosis drugs?