Drugs Affecting Bone Mineralization (online) Flashcards
What is the key molecule that causes formation, activation and maintenance of osteoclasts and is highly regulated by multiple systems in the body
NF-kB ligand RANKL is
what is the purpose of RANK ligand would inhibition of RANK ligand would do to overall bone balance?
since RANK ligand stimulates bone resorption, inhibition of RANK ligand would favor overall bone building as osteoclast activity would be less than osteoblast activity.
What are the three MAJOR regulators of calcium homeostasis?
PTH, vitamin D and FGF-23.
What effects does PTH have on the kidneys?
increase calcium reabsorption and decreases phosphorous reabsorption
What effect does PTH have in the gut?
increases BOTH calcium and phosphorous to reabsorption.
Net effect of PTH on serum calcium and Phosphorus levels
increase Calcium, decrease phosphorus
what is Teriparatide (Forteo)?
a subunit of amino acids 1-34 of human PTH
What is the MOA of Teriparatide?
stimulator of bone formation
What does intermittent PTH treatment do to bones?
stimulates osteoblastic bone formation with
Side effects of teriparatide include (6)
nausea, dizziness, headache, joint pain, mild hypercalcaemia, and orthostatic hypotension.
Teriparatide currently a drug of choice for treating? Why? .
osteoporosis and this is because it is currently the only drug with a primary mechanism of action of increasing bone formation.
Teriparatide is also used in the prevention and treatment of ?
pathological fractures
Where is Vitamin D first hydroxylated? to form? (aka)
in the liver to form 25-hydroxyvitamin D which is also called calcifediol calcidiol
After the liver, what organ converts vitamin D metabolites to what? (aka)
in kidney, 25-hydroxyvitamin D is further converted to 1,25-hydroxyvitamin D (aka calcitrol) = the activated form of vitamin D
PTH has what effect on Vit D mtb
PTH stimulates the production of 1,25-hydroxyvitamin D = calcitrol
what enzyme in the kidney converts 25-hydroxyvitamin D into 1,25-hydroxyvitamin D?
1-a hydroxylase
Three activities of vitamin D and their locations ***
- bone mineralization (via increased Ca and P)
- facilitates calcium absorption in the small intestine.
- helps to decrease calcium excretion in the kidneys.
viramin D is used to treat what 4 diseases
rickets and osteomalacia, hypocalcemia. and hypoparathyroidism
How does Vitamin D increase serum Ca levels? what is the implication for it’s administration?
stimulates intestinal calcium absorption–> so it is often given with calcium supplements
analogues of Vitamin D that are nonhypercalcemic are used in what case?
used in secondary hyperparathyroidism
What is the MOA of the (2) vitamin D analogues and what are they called?
Both paricalcitol and doxercalciferol may lower plasma PTH levels without significantly raising plasma calcium levels
What is the side effect condition of vitamin D toxicity and it’s sx? (7)
hypercalcemia
constipation, depression, weakness, fatigue, kidney stones, or even renal failure
What is the main role of FGF-23? (acting where?)
The main role of FGF-23 is to inhibit 1,25 hydroxy vitamin D formation in the kidney.