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CAS 3 > Drugs for Parathyroid Disorders > Flashcards

Drugs for Parathyroid Disorders Flashcards

1
Q

what is pagets disease

A

A bone disorder, of unknown origin, characterized by excessive bone destruction and disorganized repair. Complications include skeletal deformity, musculoskeletal pain, kidney stones, and organ dysfunction secondary to pressure from bony overgrowth

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2
Q

what is rickets

A

The same as osteomalacia, but occurs in the growing skeleton

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3
Q

nonhormonal regulators of bone mineral homeostasis

A
  • bisphosphonates
    -fluoride
    -calcmimetics
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3
Q

nonhormonal regulators of bone mineral homeostasis

A
  • bisphosphonates
    -fluoride
    -calcmimetics
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4
Q

PTH and 1,25(OH)2D ______ the input of calcium and phosphorus from bone into the serum and stimulate bone formation.
1,25(OH)2D also ________calcium and phosphate absorption from the gut.
In the kidney, 1,25(OH)2D _____ excretion of both calcium and phosphorus, whereas PTH _______ calcium but _______ phosphorus excretion.
FGF23 stimulates renal excretion of phosphate.
Calcitonin (CT) is a less critical regulator of calcium homeostasis, but in pharmacologic concentrations can reduce serum calcium and phosphorus by ______bone resorption and stimulating their renal excretion.

A

increase
increases
decreases
reduces
increases
inhibiting

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5
Q

what are 3 regulations of PTH hormone

A
  1. Serum calcium feeds back to parathyroid gland
  2. High calcium
    -Stimulates calcium-sensitive protease in gland
    -Stimulates calcium-sensing receptor (CaSR)
  3. Vitamin D
    -Suppresses PTH production
    -Induces CaSR
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6
Q

how does parathyroid control LOW serum calcium

A

Parathyroid releases PTH
Stimulates bone resorption
Increases calcium uptake from GI tract
Increases calcium reabsorption, hydroxylation of vitamin D by kidney
Decreases phosphate reabsorption by renal tubules ↑ Serum Ca

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7
Q

how does THYROID control LOW serum calcium

A

Thyroid decreases release of calcitonin
Decreased bone formation
Increased calcium uptake from GI tract
Increased calcium reabsorption by kidney

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8
Q

PTH effects on bone

A

Net effect of PTH favors bone resorption by osteoclasts
Low, intermittent doses favor bone formation

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9
Q

what is the MOA of Terparatide

A

1-34 active segment of human PTH
-Acts through PTH receptors to produce a net increase in bone formation

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10
Q

what is the MOA of Natpara

A

Genetic engineered full-length (1-84) human PTH

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11
Q

list 2 drugs that are PTH preparations

A

teriparatide
Natpara

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12
Q

describe the short-term process of PTH preparations

A

Short-term, intermittent –> Increased osteoblast number and function –> increased bone formation

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13
Q

describe the long-term process of PTH preparations

A

Long-term, continuous –> Increased osteoclast function —> increased bone resorption

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14
Q

what are the uses for PTH preparations

A

Osteoporosis in postmenopausal women & hypogonadal men
Other osteoporosis in patients at high risk of fracture
Severe osteoporosis not responsive to other drugs

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15
Q

what are the contraindications for PTH preparations

A

Patients at increased risk of bone tumors [osteosarcoma]
Paget’s disease of bone, elevated alkaline phosphatase

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16
Q

what are the Adverse effects for PTH preparations

A

Carcinogenesis (osteosarcoma)
Orthostatic hypotension
Kidney stones (assoc. with elevated serum calcium]
Diarrhea, nausea
GERD
Muscle cramps

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17
Q

what is the uses of Terparatide

A

osteoporosis

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18
Q

what is the adverse effects of Terparatide

A

Hypercalcemia, Hypercalciuria, Osteosarcoma in animals

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19
Q

How Does Teriparatide Useful in the Treatment of Osteoporosis?

A

Increases bone formation
Cessation associated with rapid bone loss
-Follow treatment with bisphosphonate or other anti-
resorptive agent
Especially useful in:
-Post-menopausal women with high fracture risk

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20
Q

calcitonin is secreted by

A

parafollicular (C) cells of thyroid gland

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21
Q

calcitonin mediates____________ effects of PTH

A

OPPOSITE

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22
Q

calcitonin mediates____________ effects of PTH

A

OPPOSITE

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23
Q

MOA of calcitonin

A

Inhibits bone resorption

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24
Q

uses of calcitonin

A

Osteoporosis

25
Q

adverse effects of calcitonin

A

rhinitis

26
Q

MOA for calcium & phosphate

A

Bone mineralization

27
Q

uses for calcium & phosphate

A

Osteoporosis, osteomalacia, Ca & P deficiencies

28
Q

adverse effects for calcium & phosphate

A

constipation

28
Q

adverse effects for calcium & phosphate

A

constipation

29
Q

MOA for Cholecalciferol [D], Ergocalciferol, Calcitriol [active D]

A

Regulates gene transcription via the vitamin D receptor to produce the effects

30
Q

USES for Cholecalciferol [D], Ergocalciferol, Calcitriol [active D]

A

prophylaxiss & Rx. Vitamin D deficiency, Osteoporosis, Osteomalacia, Psoriasis, calcium def. (renal insufficiency (must use calcitriol)

31
Q

adverse effects for Cholecalciferol [D], Ergocalciferol, Calcitriol [active D]

A

Hypercalcemia
Hypercalciuria (kidney stones)
Cholestyramine inhibits absorption
Phenytoin and barbiturates increase metabolism

32
Q

MOA of Alendronate [Bisphosphonate]

A

Inhibition of osteoclast mediated bone resorption

33
Q

uses of Alendronate [Bisphosphonate]

A

Osteoporosis, Paget’s disease

34
Q

adverse effects of Alendronate [Bisphosphonate]

A

Esophageal irritation, osteonecrosis of the jaw

35
Q

adverse effects of Denosumab

A

Osteonecrosis of the jaw, risk of infection

36
Q

uses of Denosumab

A

osteoporosis

37
Q

MOA of Denosumab

A

Immunoglobulin G2 monoclonal antibody against RANKL
Prevents RANK activation of NF-𝜅B
Inhibits gene expression for formation of osteoclasts
Inhibits osteoclast function
Mimics osteoprotegerin [OPG]
Increases osteoclast apoptosis

38
Q

MOA of Raloxifene

A

Selective Estrogen Receptor Modifier - SERM
Estrogen agonist effect in bone + antagonist in breast and endometrium

39
Q

uses of Raloxifene

A

Osteoporosis in postmenopausal women

40
Q

adverse effects of Raloxifene

A

Hot flashes, thromboembolism
Menopausal symptoms
Increased risk of stroke, PE, DVT

41
Q

MOA of Cinacalcet

A

Increases sensitivity of calcium sensing receptor (CaSR) of parathyroid gland

↓PTH for a given level of serum calcium (reduced sensitivity)

↓ PTH & serum calcium

42
Q

uses of Cinacalcet

A

Hyperparathyroidism

43
Q

adverse effects of Cinacalcet

A

Hypocalcemia

44
Q

vit D2

A

ergocalciferol , plant source

45
Q

cholecalciiferol

A

Vit D3

46
Q

1,25 dihydroxy vitamin D

A

calcitrol

47
Q

________ stimulates the renal alpha 1 hydroxylation of vit. D

A

PTH

48
Q

Calcium carbonate & Calcium citrate drug interactions:

A

Decrease the absorption of ciprofloxacin, fluoride, phenytoin, levothyroxine, and tetracycline, so calcium supplements should be taken at least 2 hours before or after taking these drugs.

49
Q

1st/ 2nd or 3rd gen Etidronate

A

First Generation (least potent)

50
Q

1st/ 2nd or 3rd gen:
Alendronate
Pamidronate
Risedronate
Tiludronate

A

Second Generation (~100X more potent)

51
Q

1st/ 2nd or 3rd gen:
Ibandronate
Zoledronic Acid

A

Third Generation (~1000X more potent)

52
Q

MOA for Tiludronate

A

Causes osteoclast to detach from bone by inhibiting tyrosine phosphatase
Reduces proton pump activity

53
Q

Bisphosphonates (Inhibit Osteoclast Activity) SIDE EFFECTS (5)

A
  1. Esophageal erosion
    - Remain upright after ingestion
  2. GI distress
    - Pamidronate most common, alendronate, risedronate least
  3. Atypical femur fractures with long-term use
    - Preceded by dull, aching pain in thigh or groin
  4. Osteonecrosis of jaw
    - High doses and poor oral health
  5. Calcium supplements and antacids decrease absorption
    - 2-hour rule
54
Q

MOA of sodium fluoride

A

Increases bone crystal size and makes more resistant to resorption
Increases bone formation

Limited use
Tends to cause osteosclerosis
No effect on osteoporotic fractures

55
Q

MOA of sodium fluoride

A

Increases bone crystal size and makes more resistant to resorption
Increases bone formation

Limited use
Tends to cause osteosclerosis
No effect on osteoporotic fractures

56
Q

what drug : Antagonizing vitamin D-stimulated intestinal calcium transport - Osteoporosis

A

glucocorticoids

57
Q

what drug : Promotes osteoclast apoptosis and increases bone formation

A

Strontium Ranelate

58
Q

Gallium Nitrate MOA

A

Managing the hypercalcemia in malignancies and Paget’s disease. It acts by inhibiting bone resorption.
Adverse effect: Nephrotoxicity

59
Q

Plicamycin (mithramycin -uses)

A

Used to reduce serum calcium and bone resorption in Paget’s disease and hypercalcemia
Adverse effects: Thrombocytopenia, hemorrhage, hepatic and renal damage

60
Q

what is the function of Sevelamer

A

The phosphate-binding gel is used in combination with calcium supplements and dietary phosphate restriction to treat hyperphosphatemia, a common complication of renal failure, hypoparathyroidism, and vitamin D intoxication.

CAS 3 (10 decks)

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