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Pharmacology II > Agents that affect Calcium/Bone Homeostasis > Flashcards

Agents that affect Calcium/Bone Homeostasis Flashcards

1
Q

what are the conditions that can lead ot hypercalcmemia?

A
  • hyperparathyroidism
    • parathyroid adenoma / carcinoma / hyperplasia
  • Cancers +/- bone metastasis
  • Hypervitaminosis (Vit D)?
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2
Q

what are the conditions that can lead to hypocalcemia?

A
  • Hypoparathyroidism (autoimmune, psuedohypothyroidism)
  • insufficient gut Ca++ absorption:
    • Vitamin D deficiency (rickets, osteomalacia)
      • CKD? but its secondary hyperthyroidism?
    • other reason for alabsorption - Ca++ not absorbed in gut
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3
Q

what is osteoporosis?

how does it present?

A

a generalized loss of bone mass and strength from excessive bone resorbption

increased risk of fractures

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4
Q

what is pagets disease of the bone?

how does it present?

A

localized increases in bone turnover due to excessive bone resorption, followed by replacement with structurally abnormal bone

presentation: skeletal deformities (misshapen bones) + fractures

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5
Q

what is the role of

  • estrogen
  • calicitonin
  • PTH

in bone metabolism?

A
  • inhibits osteoclast activity, PREVENTING bone resorption:
    • estrogen:
      • (this is why estrogen loss in women during age weakens bones)
    • calticonin
  • promotes osteoclast activity, INDUCING bone resorption
    • PTH
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6
Q

what two major classes of drugs are used to treat osteoporosis?

A
  1. anti-resorptive agents
  2. anabolic agents
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7
Q

what are the anti-resorbtive agents used to treat osteoporosis?

in what situations are they used?

what do they all have in common?

A
  • bisphophonates - 1st line
  • denosumab - 1st line
  • raloxifene - 1st in in post-menopausal
  • calcitonin - in post-menopausal (not first line)

all suppress osteoclast activity

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8
Q

what are the anabolic hormones used to treat osteoporosis?

A
  • teriparatide (PTH analog)
  • sclerostin inhibitor
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9
Q

bisphosphonates

incudes what drugs?

A

“dronate and dronic”

  • - dronate: alendronate, risedronate, ibandronate, pamidronate
  • zoledronic acid
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10
Q

bisophosphonate MOA

A

anti-resorptive agent

  • inhibit bone resorbtion by suppressing osteoclasts
    1. permanently incorporate into bone* - have effects post discontuation
    2. induce osteocast apoptosis
    3. disrupt osteoclast activity
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11
Q

bisphosphonates - clinical uses

A
  • osteoporosis - 1st line tx
  • Paget’s disease
  • bone metastasis / hypercalcemia of malignancy
  • reduction of bone fracture risk
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12
Q

bisphosphonates AEs / CIs

A
  • AEs
    • esophageal & gastric irratitation / ulcers
    • hypocalcemia & related consequences:
      • jaw osteonecrosis (ONJ)
      • atypical femur fracturefs (AFF)
  • C/I:
    • esophgeal disorders / peptic ulcers
    • severe hypocalcemia (renal disease)
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13
Q

bisphosphonates - pharmokinetics

A

poor oral absorption that is inhibited by food.

pt must take in FASTED STATE (water only)

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14
Q

alendronate

what kind of drug?

available in what forms?

A

bisphosphonate

  • oral: daily, weekly
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15
Q

risendonrate

what kind of drugs?

available in what forms?

A

bisphosphonate

  • oral: daily, weekly
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16
Q

ibandrate

what kind of drug?

available in what forms?

A

bisphosphonate

  • oral: daily, monthly
  • IV: quarterly
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17
Q

pamidronate

what kind of drug?

available in what forms?

A

bisphosphonate

  • IV only: monthly injection
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18
Q

zoldronic acid

what kind of drug?

available in what forms?

A

bisphosphonate

  • IV only: given yearly or (for osteoporosis prevention) once every 2 years
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19
Q

how should a patient be instructed to take an oral bisphosphonate?

A
  • dronates
  • take it fasting (water only) - bisphosphonates have poor oral bioavability
  • sit upright for 30 min after taking - prevents formation of gastric & esophageal ulcers
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20
Q

denosumab

what kind of drug?

MOA?

A
  • an anti-resorptive drug (thus, suppresses osteoclasts)
    • MOA: is an RANKL-antibody that binds RANK-L, inhibiting its binding with RANK receptors on osteoclasts. this inhibits osteoclast activation
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21
Q

denosumab - clinical uses

A

= RANK-L inhibitor

  • osteoporosis - 1st choice - used as an alternative to bisphosphonates
  • hypercalcemic malignancy

(similar to bisphosphonates)

22
Q

denosumab

is available in what form?

A
  • injections (subcutucaneous) - given every 6 mos
23
Q

denosumab- AEs / CIs?

A
  • AE
    • hypocalcemia & related effects
      • jaw osteonecrosis (ONJ)
      • atypical femur fractures (AFF)
  • CI
    • hypocalcemia

(similar to bisphosphonates)

24
Q

which osteoporosis drug can cause an increase in bone mass density (BMD) that persists beyond discontinuation of therapy?

why?

A

bisphosphonates (dronates & zoldedronic acid)

this is because they permanently incorporate themselves into bone

25
Q

raloxifene

  • what kind of drug?
  • MOA?
A
  • is an antiresorptive drug
    • MOA: specifically a SERP: selective estrogen receptor modulator
      • ​raloxifene is an agonist in some tissue but an antagonist in others
        • agonism in certain tissues (bone) serves to stimulate estrogen, thus inhibiting osteoclasts activity
        • antagonism in certain tissues (breast, endometrium) serves to inhibit estrogen, preventing cancer development
26
Q

raloxifene -clinical uses?

A

= SERM (selective estrogen receptor modulator)

  • to prevent/treat osteoporosis in postmenopausal females
27
Q

raloxefine - AEs / CIs?

A

= SERM (selective estrogen receptor modifiers)

  • AEs:
    • leg - arthralgia /cramps / muscle spasms
    • increases risk of thromboembolism
    • hot flashes
  • CI:
    • in pts with hx/current venous thromboembolitic disorders*
28
Q

compare and contrast bisphosphonates to RANK-L inhibitors

(what are the drug names in each of these classes?)

A

bisphosphonates: - dromate (oral/IV), zoledronic acid (IV only)

RANK-L inhibitor: denosumab (injection)

  • both:
    • are anti-resorptive drugs
    • treat
      1. osteoporosis (1st line)
      2. bone metastasis / hypercalcemia malignancy
    • AEs
      • hypocalcemia (+ ONJ, AFF)
    • C/I in: severe hypocalcemia
  • only bisphosphonates:
    • increase BMD after drug discontinuation
    • can treat: Paget’s disease
    • can cause: esophageal / gastric ulcers irritation
    • C/I in: hx of esophgeal / gastric disorders
    • must taken while fasting & while pt is upright for 30 min*
29
Q

estrogens

  • MOA
  • have what clinical uses?
  • AEs /CIs?
A
  • MOA: antiresorptive via osteoclast supression
  • uses:
    • to treat osteoporosis in postmenopausal women - NOT first choice
    • to relief other postmenopausal symptoms
  • AEs:
    • endometrial / breast carcinoma
    • venous thrombombolism
30
Q

calcitonin

  • what kind of “drug”?
  • MOA?
  • clinical uses?
  • available in what forms?
  • AEs / CI?
A
  • grouped with resorptive drugs
  • MOA:
    • secreted by thyroid in response to hypercalcemia
      • lowers both Ca and PO4
  • clinical uses:
    • postmenopausal osteoporosis - not first line
    • paget’s disease - not 1st line
    • hypercalcemia
  • formulations:
    • human calcitonin
    • “salmon” calcitonin = intranasal / sc / im; longer half life
  • AEs:
    • hypersensitivity / flushing
    • nausea / GI cramps
31
Q

what are the AEs of calcitonin?

A
  • hypersensitivity / flushing
  • nausea / GI cramps
32
Q

what drugs are specifically indicated for postemenopausal osteoporosis? how are they different?

A
  • estrogen & raloxafine (SERM) -
    • both: are risk factors for a venous thromboembolism (stroke)
      • raloxifene - 1st choice
      • estrogen - NOT first choice
        • is also a factor for breast/emdometrial cancer

calcitonin also used for postemenopausal osteoporosis (amongst other things). not 1st choice

33
Q

which drugs are used to treat Paget’s disease?

which one is first choice?

A
  1. bisphosphonates (dromate, zoledronic acid)- 1st choice
  2. calcitonin - NOT first choice
34
Q

PTH

  • has what key physiological affects?
  • how does it mediate these effects?
A

PTH acts at

  1. bone:
    • inc Ca reabsorption (via osteoclast activation)
    • inc PO4 reabsorption (released along w/ Ca)
  2. kidney:
    • inc Ca reabsorption
    • dec PO4 reabsorption

net effect: raise plasma calcium and lower plasma phosphate

35
Q

teriparatide

  • what kind of drug?
  • MOA?
A
  • an anabolic hormone
    • ​MOA: is a PTH analog - that, when administered intermittently, induces osteoclast activity (by inducing RANK-L secretion by osteoblasts) that is immediately followed by bone deposition (by osteoblasts) - having the net effect of bone building (“anabolic effect”)
36
Q

teriparatide - clinical uses

A

treatment of osteoporosis in pts with a high fracture risk who have failed the antiresorptive agents (bisophosphonates, denosumab, reloxifene, calcitonin)

37
Q

teriparatide - PK

A
  • dosing is: intermittent (once daily) - this timing is imperative for a net anabolic effect.
    • continuous/high circulating of PTH = bone resorbption > bone formation
38
Q

teriparatide - AEs/CIs

A
  • AEs
    • it teraparatide is givin with continuous administration then circulating PTH levels become too high and reabsorptive effets > anabolic effects, and related AEs present:
      • hypercalcemia / hyperuricemia
      • dizziness / fatigue
      • cramps / arthralgia
  • CI:
    • hypercalcemia / hyperparathyroidism
    • Pagets
39
Q

vitamin D preparations come in what forms?

A

oral supplements

  • ergocalciferol
  • cholecalciferol
  • calitriol
40
Q

Vitamin D supplements

clinical uses?

A
  • rickets / osteomalacia
  • hypocalcemia (d/t hypoparathyroidism)
  • renal osteodystrophy d/t CDK)
  • osteoporosis
41
Q

which Vitamin D supplement is especially useful in hypocalcemia due to chonic kidney disease?

A

calcitriol

is the active form of Vit D, which is useful in patients with CDK, form whom the final step in vitamin D synthesis is impaired

42
Q

which Vitamin D analog can be used to treat psoriasis?

A

calcipotriene

43
Q

Vit D drug drug interactions

A
  • phenobarticals/phenytoin - inc metabolism
  • mineral oil/resins - impair absorption
44
Q

Vit D AEs?

A
  • hypercalcemia / calciuria
  • hyperphosphatemia
45
Q

Vitamin D C/I

A
  • hypercalcemia
  • hyperparathyroidism
  • pregnancy*
  • sarcoidosis
46
Q

contrst PK of ergocalciferol (D2) vs cholecalciferol (D3)

A

cholecalciferol = more potent & longer half life (6 weeks > 1 week)

47
Q

calcium preparations

include what drugs?

A

various calcium carbonates: calium carbonate, calcium gluconate, ect

48
Q

calcium supplements (preparations)

  • clinical uses
  • formulations
  • PK (& drug-drug interactions)
  • AE
A

Ca-carbonate, Ca-gluconate

  • clinical uses: given w/ Vit D for:
    • prevention of osteoporosis:
      • oral supplement + dietary Ca + Vit D
    • hypocalcemia
      • oral / IV supplement + Vit D
  • formulations: IV & oral
  • PK:
    • requires acidic environment for dissolution
    • drug-drug: absorption reduced by anti-acids & laxatives
  • AEs:
    • constipations / GI upset
    • kidney stone risk*
49
Q

calcimimetics

  • MOA
  • clinical uses
A
  • MOA: is a Ca++ analog that binds parathyroid cells on the parathyroid gland to decrease synthesis of PTH
  • clinical uses:
    • primary hyperparathyroidism in pts who can’t undergo surgery
    • secondary hyperparathyroidism in chronic renal dz
    • parathyroid carcinoma
50
Q

romosozumab

  • what kind of drug?
  • MOA?
  • clinical uses?
  • AE?
A
  • anabolic drug: scerlostin inhibitor
  • MOA: increases bone formation for 12 months
  • clinical uses: osteoporosis in _post meno-pausal female_s at high bone fracture risk
  • AE
    • cardiovascular: MI / stroke
51
Q

what drugs can be used to treat osteoporosis in post-menopausal women?

what are their individual AEs?

A
  • estrogen - thromboembolism / breast & uterine cancer
  • raloxifene (SERM) - thromboembolism
  • calcitonin - hypersensitivity / flushing
  • romosuzumab (clerostin inhibitor) - MI / stroke / CV death

Pharmacology II (5 decks)

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