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Pharmacology > Osteoporosis > Flashcards

Osteoporosis Flashcards

1
Q

Bone resorption

A

removal of Ca and removal of old damaged bone tissue (osteoclasts) leaving small spaces

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2
Q

Bone formation

A

use Ca and P to fill spaces with new bones

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3
Q

Why does bone remodeling occur?

A

adjust bone according to mechanical strain, repair microfactures, provide access to mineral stores

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4
Q

How is bone remodeling regulated?

A

initiated by osteocytes (identify damage), sends signals to stimulate osteoclasts, secretes collagenases and proteinases, resorb bone matrix and release Ca, osteoblast begin formation, bone is mineralized

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5
Q

Mineralization occurs mostly with

A

CaPO4 deposition and requires the presence of vit D

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6
Q

3 functions of parathyroid hormone

A

increase renal Ca reabsorption and phosphate excretion, promote bone resorption to release Ca from bone, result in conversion of 25 hydroxyvit D to active metabolite be activating an enzyme in the kidney

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7
Q

Normalization of Ca results in a negative feedback signal causing

A

decreased release of PTH

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8
Q

Recommended amount of Calcium and Vit D in the diet (19-30 yo)

A

1000 mg/d and 600 IU/d

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9
Q

Calcitonin

A

made in thyroid gland and has major effect on bone, released when [Ca] increases and acts to inhibit bone breakdown and lower [Ca]

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10
Q

How does Calcitonin decrease plasma Ca levels

A

it is an antagonist to PTH, stimulated by increase in plasma Ca levels, target cell is the osteoclast, inhibits osteoclasts with rapid decrease in Ca caused by inhibition of bone resorption

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11
Q

Glucocorticoids

A

necessary for skeletal growth, excess steroid decrease Ca reabsorption and stimulate PTH secretion, causes bone loss

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12
Q

Adrogens and estrogens

A

result in diminished bone turnover rate, inhibiting osteoclast activity and increasing osteoblast activity. Estrogen causes Ca retention

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13
Q

Mechanism of osteoporosis

A

imbalance between rate of resorption and formation

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14
Q

Osteoporosis risk factors

A

gender, ethnicity, body composition, fam hx of osteoporosis, RA, thyroid/liver disease, spinal cord injury, physical activity level, low Ca, lifestyle habits, recurrent falls, smoking, thyroid replacement, coricosteroids, antacids, long term anti-convulsant use

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15
Q

Osteoporosis presentation

A

decrease ht, bent over, change in spine, slow gait, wide stance, clothes do not fit, crowding of internal organs

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16
Q

Non pharm approaches for osteoporosis

A

low calcium and vit D, fall prevention, exercise, smoking cessation, avoid alcohol

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17
Q

Calcium MOA

A

inhibit bone resorption to reduce bone loss, increase bone mass and reduce fx, increase bone mineral density

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18
Q

How to take calcium

A

take 1 tab TID with meals, not 3 tabs at once, vit D is required for absorption

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19
Q

ADRs of calcium

A

constipation, flatulence, upset stomach

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20
Q

Drug interactions with calcium

A

Ca is a clelator, problematic with antibiotics

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21
Q

Bisphosphonates

A

Alendronate (Fosamax), Ibandronate (Boniva), Risedronate (Actonel), Zoledronic acid (Reclast), Pamidronate (Aredia), Tiludronate (skelid), Clondronate, Etidronate

22
Q

Bisphosphanates MOA

A

inhibit bone resorption by binding to bone mineral surface, are taken up by osteoclast and induce osteoclast apoptosis, decreases [Ca] and [Phos]

23
Q

Clinical use of bisphosphonates

A

osteoporosis, hypercalcemia of malignancy, Paget’s disease, metastatic bone disease due to breast cancer, multiple myeloma, osteolytic bone lesions

24
Q

Pharmocokinetics of bisphosphonates

A

IV and PO, compromised with coffee/juice, avoid in pts w/ CrCl,30 ml/min, very long half life

25
Q

Contraindications

A

hypocalcemia, esophageal abnormalities delay esophageal emptying

26
Q

ADRs of bisphosphonates

A

fatigue, HA, insomnia, hypocalcemia, GI mucosa irritation, erosions, esophagitis, ulcers, dysphagia, osteonecrosis of the jaw

27
Q

How to combat GI adr in bisphosphonates

A

pt should take first thing in the morn, 30 min before breakfast and glass of plain water, remain upright 30 min after administration

28
Q

Alendronate (Fosamax)

A

first one marketed, 10 year T1/2, PO only, once a week, given daily sometimes, less expensive

29
Q

Ibandronate (Boniva)

A

T1/2 37-157 hours, PO given once monthly, coated tablet (decrease GI irritation), IV given every 3 months

30
Q

Risedronate (Actonel)

A

T1/2 480-561 hours, coat tablet (decrease GI irritaton), IV, once weekly or monthly

31
Q

Zoledronic acid

A

reclast- ostroporosis (given once a year), Zometa- all other indications, largely onc related, T1/2 146 hours, suspected to be nephrotoxic, only available IV

32
Q

Pamidronate (Aredia)

A

not for osteoporosis, only hypercalcemia, paget’s and onc related uses, T1/2: 21-35 hours, IV, only one with data for use in renal failure

33
Q

Conjugated estrogen (Premarin) MOA

A

inhibits bone resorption, often considered most efficacious but patient selectionis critically important due to ADR profile, PO and transdermal patch

34
Q

Clinical use of conjugated estrogen (Premarin)

A

menopause symptoms, Prevention of postmenopausal osteoporosis in high risk women, low estrogen, and others

35
Q

Contraindications in estrogen

A

genital bleeding, Br CA, estrogen-dependent malignancy, VTE, arterial thromboembolic disease, pregnancy

36
Q

ADRs of estrogen

A

increased risk of CV events, HTN, MI, stroke, pulmonary emboli, DVT, DC 4-6 weeks prior to surgeries, CV risk w/ estrogen remains controversial, increased risk of Br CA, dementia, nausea, HA, edema, migraines, endometrial CA

37
Q

Things to consider before starting estrogen

A

menopausal sx, osteoporosis risk, CVD risk, Br Ca risk, thromboembolic risk, dementia risk

38
Q

Estrogen receptor modulators

A

Ralocifene (Evista)

39
Q

MOA of Ralocifene (Evista)

A

non-hormonal agent which inhibits bone resorption similar to estrogen, very specific to bone, antagonist to breast and uterus

40
Q

Ralocifene (Evista) clinical use

A

prevention or treatment of osteoporosis, prevention of br CA in high risk pts, PO, chronic therapy

41
Q

Ralocifene (Evista) contraindications

A

active or past h/o VTE, lactating/ pregnancy

42
Q

Ralocifene (Evista) ADRs

A

hot flashes, wt gain, edema, decrease LDL, decreased endometrial activity, decrease risk of breast CA

43
Q

Calcitonin (Calcimar)

A

subcut or IM injection

44
Q

Salmon-calcitonin (Miacalcin)

A

nasal spray

45
Q

Calcitonin MOA

A

inhibit osteoclastic bone resorption, 10 x more potent than endogenous calcitonin, has analgesic properties

46
Q

Calcitonin clinical uses

A

osteoporosis (Miacalcin) for pt who can’t take bisphosphonates, hypercalcemia (calcimar), off label for pain control for bone metastasis

47
Q

Calcitonin ADRs

A

intranasal- rhinitis, epistaxis, dryness, nasal irritation, Subcut: flushing, nausea, injection site reaction

48
Q

Teriparatide (Forteo) MOA

A

recombinant PTH, principal regulator of Ca, increases/stimulates osteoblast function, once daily, $$$

49
Q

Teriparatide (Forteo) clinical uses

A

reserved for failures of antiresorptive therapy, treatment of postmenopausal osteoporosis, increase BMD in men w. osteoporosis associated with hypogonadism

50
Q

Teriparatide (Forteo) ADRs and contraindications

A

postural hypotension and several

Pharmacology (61 decks)

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