This article masters the usage, dosage and adverse reactions of 3 major types of osteoporosis drugs

*For medical professionals only, what are the differences between osteoporosis treatment drugs, and what are the tips for using drugs? All the stuff is here! Osteoporosis drug treatment is the use of drugs to achieve the purpose of treatment and prevent fractures
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Osteoporosis therapeutic drugs are classified into three categories: bone resorption inhibitors, bone formation promoters, and bone metabolism regulators
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According to the characteristics of the currently used drugs and with reference to domestic and foreign evidence, the recommended grades are given for the effectiveness of various drugs on bone mineral density, vertebral fractures, non-vertebral fractures, proximal femoral fractures and other disease states for your reference.

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Table 1 Recommended grades of osteoporosis drugs Bone resorption inhibitors ■01.
Bisphosphonates Key Point: Bisphosphonates are the first choice for osteoporosis drugs
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Pharmacodynamic mechanism: According to the structure of the side chain, it is divided into the first generation to the third generation; according to the presence or absence of nitrogen atoms in the side chain, the mechanism of bone resorption inhibition activity and pharmacological action are different, resulting in different pharmacological effects; only etidronic acid Disodium has no definite inhibitory effect on non-vertebral fractures
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Dosage: There are periodic intermittent dosing, daily dosing, once a week or even once a month
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In particular, the use of the once-weekly and once-monthly preparations reduces the complexity of requiring fasting administration and improves the patient's medication compliance (Table 2)
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There is little difference in the dosage of etidronate disodium for bone formation and bone inhibition.
In order to prevent bone calcification, periodic and intermittent administration is adopted
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For other drugs (alendronate, risedronate, and minodronate hydrate), the amount of bone formation inhibitory and bone resorption inhibitory effect varies widely, and patients can adjust and choose the dosage form according to their life>
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Adverse reactions: prodromal symptoms of atypical fractures, usually pain at the fracture site such as the thigh and groin; for patients with oral bisphosphonates for more than three years or at risk of osteonecrosis of the jaw, it is recommended before invasive dental treatment It is best to stop the drug for 3 months; the timing of resuming the drug is recommended to wait until the wound has healed
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Table 2 Dosage of bisphosphonates Figure 1 Basic structure of bisphosphonates therapeutic effect
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Table 3 The characteristic mechanism of action of estrogen drugs in the treatment of osteoporosis: estrogen drugs can inhibit the bone resorption effect of thyroid hormone
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At the same time, it can promote the absorption of calcium in the intestine, the reabsorption of calcium in the kidney, and promote the production of active vitamin D3
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Adverse reactions: If there is a long-term bedridden state such as surgery plan, it is recommended to stop the drug for a period of time, but the time of drug withdrawal is still inconclusive
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■ 03.
Selective Estrogen Receptor Modulator (SERM) Key Point: Due to the safety and convenience of taking the drug, SERM is currently recommended as the first choice for postmenopausal women with low fracture risk
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Selective estrogen receptor modulator (SERM) exhibits estrogen-like effects on bone and lipid metabolism, and exhibits anti-estrogen-like effects on breast and uterus, avoiding the most important role of female hormone drugs.
The problem is that it can play a role in inhibiting bone resorption
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Table 4.
Effectiveness and safety of SERM drugs for fracture prevention: ① In the prevention of non-vertebral fractures, raloxifene hydrochloride has certain advantages over bazedoxifene acetate
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② Both raloxifene hydrochloride and bazedoxifene acetate can increase the risk of deep vein thrombosis, and the incidence rates of the two drugs are similar
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③ Both raloxifene hydrochloride and bazedoxifene acetate caused a slight increase in the occurrence of hypoestrogenic symptoms such as vasodilation (hot flashes) and cramps of the calf, with little difference in incidence
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Adverse reactions: It is recommended to stop the drug for a period of time in anticipation of long-term immobility (surgery, long-distance bus, long-term flight overseas)
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■ 04.
Calcitonin Key Point: ①Used for bone pain cases with osteolysis and/or osteopenia caused by osteoporosis
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②It takes about 2 to 6 weeks for the pain improvement effect to appear
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Calcitonins, which we expect to relieve pain and improve quality of life, are the first choice for patients with bone deformity symptoms following osteoporotic fractures and vertebral bodies
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The mechanism of action of calcitonins is to exert analgesic effect by regulating the level of the central neurotransmitter serotonin, and at the same time, it can inhibit bone resorption by directly binding to the receptor of osteoclasts
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Adverse reactions are occasionally allergic symptoms, erythema, papules, etc.
, and severe shock has also been reported
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■ 05.
Isoflavones Key Point: Female estrogen-like effects, play a role in bone resorption and bone formation promotion; patients with peptic ulcer and the past medical history should be used with caution
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There have been no reports of efficacy trials of the drug since 2001, and questionable evidence of its fracture-inhibiting effect continues to emerge
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Osteoporosis is currently treated with ipriflavone less frequently than other treatments
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Adverse reactions: Allergies, gastrointestinal symptoms, neurological symptoms, etc.
occur frequently
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In particular, patients with a history of peptic ulcers may induce ulcers or exacerbate symptoms, requiring special attention
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Cases of gynecomastia have also been reported occasionally
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Bone formation promoter ■ 01.
Parathyroid hormone drug (PTH) Key Point: PTH is mainly aimed at osteoporosis patients with high fracture risk; it is currently the second choice for osteoporosis treatment drugs
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Mechanism of action: Persistent PTH excess state leads to hypermetabolism and decreased bone mass
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On the other hand, intermittent subcutaneous injection once a day or once a week induces osteocyte differentiation and inhibits apoptosis, and promotes bone formation and increases bone mass, but the mechanism of action is not yet clear
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Table 5.
Dosage and usage of parathyroid hormones Combination therapy: Combination of teriparatide and alendronate will weaken the effect of the drug on promoting bone formation
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At present, there is no clear evidence to prove the advantages of these drugs in combination with bone resorption inhibitors, and it is not recommended to use them in combination with bone resorption inhibitors
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Adverse reactions: For nausea and vomiting caused by PTH drugs, antiemetic drugs should be given to support treatment; PTH drugs should not be given to cancer patients
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■ 02.
Anabolic hormones There is little clinical research evidence for the use of these drugs in the treatment of osteoporosis, and the frequency of use is also relatively low
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In terms of adverse reactions, the frequency of liver function damage is about 50%, and it will improve after stopping the drug
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Occasionally, masculinization symptoms such as hirsutism and voice change occurred, which were relieved after drug withdrawal
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■ 03.
Vitamin K2 Key Point: for patients with vitamin K2 deficiency; determine whether patients have vitamin K2 deficiency by measuring the concentration of undercarboxylated osteocalcin in blood
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Dynamic drug interactions in vivo: The drug relies on bile absorption and should be taken after meals; warfarin exerts an anticoagulant effect by antagonizing vitamin K and inhibiting coagulation factors, so patients who are using warfarin should not use this drug
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Bone metabolism regulating drug ■ 01.
Calcium agent Key Point: When administering, pay attention to the different calcium content of different preparations; it is recommended to choose organic salt calcium agent with better absorption
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Table 6 Adverse reactions of calcium content of different calcium preparations: constipation is a sign of dose reduction; calcium intake is associated with an increased risk of cardiovascular disease, and it is recommended that calcium intake should not exceed 500 mg per time
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■ 02.
Active vitamin D3Key Point: Alfacalcidol and calcitriol reduce the risk of falling, especially suitable for elderly patients; compared with other drugs, alcalcidol has the effect of increasing bone density and preventing fractures.
There are advantages to the effect
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Table 7 Adverse reactions compared with active vitamin D3 drugs: it may lead to hypercalcemia and renal insufficiency, and it is necessary to monitor the blood calcium value regularly; pay attention to observe and monitor nausea, vomiting, thirst, polyuria, muscle weakness and other hypercalcemia The initial symptoms of hyperemia; combined with digitalis drugs, the serum calcium concentration will increase, enhance the effect of digitalis drugs, and easily cause arrhythmia
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References: [1] Fleisch H: Bisphosphonates in bone disease, From the Laboratory to the Patient, 4th Ed, Academie Press, San Diego, 2000.
[2] Schildcher J et al: Bisphosphonate use and atypical fractures of the femoral shaft.
N Engl Med: 364: 1728-1737, 2011.
[3] Park-Wyllie LY et al: Bisphosphonate use and the risk of subtrochanteric or femoral fractures in older women.
JAMA 305: 783-789, 2011.
[4] Rossouw JE et al: Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principle results From the Women's health Initiative randomized controlled trial.
JAMA 288: 321-333, 2002.
[5] Journal of Bone Metabolism 3: 93-109, 1985 .
[6]Prevention and Treatment of Bone Thickness, 2011 Edition, ライフサイエンス, 2011.