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Pharma 1 Flashcards

(55 cards)

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1
Q

Primary (essential reglators) hormone regulators of Ca+ metabolism

A

1) Parathroid hormone
2) Vitamin D (calcitriol)
3) Fibroblast growth factor-23 (FGF-23)

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2
Q

Secondary (modulatory reglators) hormone regulators of Ca+ metabolism

A

1) Calcitonin
2) Estrogen
3) Glucocorticoids

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3
Q

The sectretion of PTH is controlled by

A

The level of serum Ca+ (low)

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4
Q

Mechanism of action and effects of PTH

A

PTH acts on specific receptors in bone and kidney, leading to ↑ serum Ca²⁺ and ↓ PO₄³⁻ through:
i. Bone: ↑ bone resorption
ii. Intestine: ↑ Ca²⁺ absorption (through activation of vitamin D)
iii. Kidney: ↑ Ca²⁺ reabsorption and ↑ PO₄³⁻ excretion

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5
Q

Therapeutic uses of PTH

A

Synthetic PTH (teriparatide) in low and intermittent doses may stimulate bone formation and can be used for treatment of osteoporosis

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6
Q

Synthetic PTH is also know as

A

Teriparatide

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7
Q

Vitamin D is a fat soluble vitamin found in two forms

A

Vitamin D2 (ergoclciferol), plants
&
Vitamin D3 (cholecalciferol), animals and synthesized in human skin by UV rays

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8
Q

The two forms of vitamin D must be activated by

A

Two hydroxylations…

At site 25 (liver) and then at site 1 (kidney)

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9
Q

Active form of vitamin D

A

1,25 (OH)2 D3 (Calcitriol)

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10
Q

If a patient with renal failure/ renal disease has vitamin deficiency, what form of vitamin D should be given

A

Active form of Vitamin D

1,25 (OH)2 D3 (Calcitriol)

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11
Q

Mechanism of action of vitamin D

A

Vitamin D acrs on nuclear (DNA) receptors to synthesize protiens necessary for Ca+ transport

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12
Q

Effects of vitamin D

A

1) On bone
In deficent to usual range, it restores bone mineralization of osteoid
In excess, bone resorption

2) Intestine
↑ Ca²⁺ absorption

3) Kidney
↑ Ca²⁺ and PO₄³⁻ reabsorption

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13
Q

Theraputic uses of Vitamin D

A

1) Hypocalcemia and hypophosphatemia
2) Osteoporosis
3) Rickets (children)
4) Osteomalacia (adults)

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14
Q

Drug interactions of vitamin D

A

1) Phenytoin & phenobarbitone (antiepipleptic drugs)
2) Cholestyramine
3) Thiazides

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15
Q

Effects of Phenytoin and phenobarbitone (antiepileptic drugs) on vitamin D

A

Stimulates hepatic microsomal enzymes, increases the rate viamin D metabolism…
Epileptic patients on long-term therapy may develop osteomalacia or rickets

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16
Q

Effects of cholestyramine on vitamin D

A

Decreases vitamin D absorption

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17
Q

Effects of thiazides on vitamin D

A

Increases the hypercalcemic effects of vitamin D

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18
Q

Mechanism of action of FGF-23

A

Inhibits 1,25 (OH) 2D production
&
Inhibits phosphate reabsorption in the kidney (Hypophosphatemia)

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19
Q

Monoclonal antibody to FGF23

A

Burosumab

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20
Q

Used for the treatment of hyophosphatemic rickets

A

Burosumab

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21
Q

A single-chain polypeptide secreted by the C-cells of the thyroid

A

Calcitonin (CT)

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22
Q

The secretion of CT is controlled by

A

The level of serum Ca²(high)⁺and vitamin D

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23
Q

Mechanism of action and effect of calcitonin

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A

Calcitonin acts on specific receptors in bone and kidney, leading to ↓ serum Ca²⁺ and PO₄³⁻ through:
i. Bone: ↓ bone resorption
ii. Intestine: ↓ Ca²⁺ absorption
iii. Kidney: ↓ reabsorption of Ca²⁺ and PO₄³⁻

24
Q

Theraputic uses of CT

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A

1) Treatment of hypercalcemia
2) Treatment of osteoporosis
3) Treatment of Paget’s disease of bone

25
Synthetic form of calcitonin
Salmon CT
26
Prolonged administration of glucocorticoids can cause osteoporosis in adults and retarded growth in children due to...
1) ↑ renal Ca²⁺ excretion 2) ↓ bone formation 3) Antagonize intestinal vitamin D–stimulated Ca²⁺ absorption
27
Theraputic use of glucocorticoids
Can be used to treat hypercalcemia associated with lymphomas and sarcoidosis
28
Mechanism of action of estrogen
1) ↑ blood levels of vitamin D 2) ↓ bone resorption
29
Theraputic uses of estrogen
Used in the treatmen of postmenopausal osteoporosis
30
The cons of using estrogen
Not recommended for long use as it may cause many side effects (e.g. breast cancer and endometrial carcinoma)
31
Selective estrogen receptor modulators SERMs were developed to...
1) Stimulate esrpgen receptors in bone 2) Block estrogen receptors in the breast and uterus (mixed agonist-anatogist)
32
A Selective Estrogen Receptor Modulators (SERMs)
Raloxifene
33
Secondary regulators modulate...
Modulate the actions of primary regulators (PTH, vitamin D) and overall calcium balance
34
Examples of Bisphosphonates
Risedronate & zoledronic acid
35
Bisphosphonates are analongs of pyrophospahte in which....
The P–O–P bond is replaced by the stable P–C–P bond.
36
Pharmacokinetics of Bisphosphonates
After oral administration, all bisphosphonates have very poor oral absorption (1–3%), which is decreased by food. Predominant elimination by the kidney (avoided in severe renal impairment).
37
Recommended method of administration of bisphosphonates
Administer on an empty stomach with a full glass of water and remain standing for 30 minutes to avoid Erosive esophagitis
38
Mechanism of action of bisphosonates
Bind to hydroxyapatite crystals in the bone and inhibit osteoclastic activity →↓ bone resorption
39
Theraputic uses of Bisphosphonates
1) Hypercalcemia associated with malignancy 2) Osteoporosis 3) Paget’s disease
40
Side effects of Bisphosphonates
1) Diarrhea, abdominal pain. 2) Esophagitis and esophageal ulcers 3) Renal impairment 4) Rare: osteonecrosis of the jaw 5) Risk for atypical fractures with long-term use
41
Mechanism of action of Thiazides
Thiazides increase Ca²⁺ reabsorption directly in the distal convoluted tubule →↓Ca2+ excretion
42
Theraputic uses of Thiazides
▪ Idiopathic hypercalciuria & renal stones ▪ Hypocalcemia
43
Mechanism of action of Fluoride
Accumulates in bone and teeth stabilization of hydroxyapatite crystals.
44
Theraputic use of Fluoride
Prophylaxis of dental caries (added to toothpaste)
45
Mechanism of action of Denosumab
Denosumab is a receptor Activator of Nuclear Factor-κB Ligand (RANKL) monoclonal antibody acts through the inactivation of gene transcription required for osteoclast viability and function, so decreases bone resorption.
46
Method of administration of denosumab
Given by subcutaneous injection
47
Theraputic uses of Denosumab
▪ Treatment of osteoporosis. ▪ Prevention of fractures and spinal cord compression in patients with bone metastases
48
Side effects of Denosumab
▪ Increase the risk of infections ▪ Hypocalcemia ▪ Rarely, osteonecrosis of the jaw, and atypical fractures
49
A monoclonal antibody to sclerostin
Romosozumab
50
Theraputic uses of romosozumab
Treatment of osteoporosis (promotes bone formation and inhibits bone resorption)
51
Side effects of romosozumab
Increase risk for myocardial infarction and stroke
52
Mechanism of action of calcimimetics
Activates the calcium-sensing receptor (CaSR) in the parathyroid gland→ inhibits PTH secretion
53
Theraputic uses of cinacalcet
▪ 2ry hyperparathyroidism in chronic kidney disease ▪ Parathyroid carcinoma
54
Management of hypercalcemia
1) Diuresis Aggressive IV isotonic saline guided by volume status, followed by loop diuretics if needed to increase urine flow and enhance Ca2+ excretion 2) IV bishosphantes 3) Calcitonin 4) Hemodialysis especially when renal failure is present
55
Management of hypocalcemia
1) Diet rich in calcium and low in phosphate 2) Calcium gluconate: slowly i.v. (in acute conditions) 3) Vitamin D: to ↑ Ca+2 absorption from intestine 4) Thiazide diuretics
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