Drugs for Osteoporosis and Gout Flashcards

1
Q

Where are the following found:

Ergocalciferol
Cholecalciferol

A

Ergocalciferol: D2 - occurs in plants and used in fortified foods.
Cholecalciferol: D3 - produced in skin exposed to sunlight, or as a prescription drug.

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2
Q

What is the MOA of Calcitonin-salmon?

What is the indication?

What are the adverse-effects?

A

Similar to endogenous calcitonin, but has a longer half-life and greater potency. It decreases bone resorption.

Only used for the treatment of established osteoporosis, not in prevention.

Very few - considered to be safe.

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3
Q

What is the MOA of Bisphosphonates-alendronate?

What is the indication?

What are the adverse-effects? (3)

A

Structural analogs of pyrophosphate (normal bone constituent) and inhibits bone resorption.

1st choice for essentially every kind of osteoporosis.

Esophagitis
Osteonecrosis of jaw*
Atypical femoral fractures

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4
Q

Aside from Alendronate, what are the other bisphosponates? (4)

A

Risedronate (PO)
Ibandronate (PO, IV)
Tiludronate (PO)
Zolendronic acid (IV 1x/year) - avoids GI problems, but associated with osteonecrosis of jaw.

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5
Q

What is the MOA of Raloxifene?

What is the indication?

What are the adverse-effects? (3)

A

SERM that is an agonist at bone and an antagonist in the breast and uterus.

Primarily post-menopausal osteoporosis.

DVT, PE and stroke.

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6
Q

What is the MOA of Teriparatide?

What is the unique frequency that it is given?

What are the indications?

How is it administered?

What are the adverse-effects?

A

A variant of PTH that increases bone formation (only osteoporosis drug that can do this).

It’s given in a pulsatile fashion so that osteoblast responses dominate.

OP: Post-menopausal, men, GC-induced.

Once-daily admin, by using pre-filled injectors.

Well-tolerated, but may cause nausea, HA, myalgias and cramps. Possibly elevated Ca++, Mg++ and uric acid levels.

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7
Q

What is the MOA of Denosumab?

What are the indications? It should be taken with…

How often is it given?

What are the adverse-effects? (3)

A

mAb that is an inhibitor of RANKL. This decreases the formation and function of osteoclasts (reduced bone resorption).

Post-menopausal OP at high risk for fractures, bone metastases from solid tumors.
Should be taken with Vit. D to prevent hypoglycemia.

Injected subQ every 6 mo.

Delays in fracture healing, new fractures and osteonecrosis of the jaw.

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8
Q

What is a major risk of treating osteoporosis in men?

What is the drug of choice for men with osteoporosis?

A

Hypogonadism, so testosterone replacement is important.

Bisphosphonates (1st), Denosumab (2nd).
They tend to respond to similar drugs as women.

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9
Q

What is the MOA of Cinacalcet?

What are the indications?

What are the adverse-effects?

A

A “calcimimetic” drug that binds in the PT glands and increases its sensitivity to extracellular Ca++ and decreases PTH secretion.

Hypercalcemia:

  • primary hyperparathyroidmism (parathyroid CA).
  • secondary hyperparathyroidism due to CKD.

N/V/D.

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10
Q

What topical NSAID is useful in OA?

What can be given for pain-resistant therapy? (3)

A

1% diclofenac gel.

Duloxetine (SNRI)
Opioid analgesics
Intra-articular: hyaluranons, glucocorticoids, PRP injections.

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11
Q

What are the 4 major antibiotics used to treat Osteomyelitis?

How long is it treated?

A

Clindamycin
Rifampin
TMP/SMX
Fluoroquinolone

Approx. 4-6 wks.

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12
Q

What are the causes of Primary Hyperuricemia due to the following:

Uric acid underexcretion (90%)

Urate overproduction (10%)

A

Uric acid underexcretion (90%): lower fractional excretion of filtered urate.

Urate overproduction (10%): metabolic disorders, idiopathic.

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13
Q

What are the causes of Secondary Hyperuricemia due to the following:

Uric acid underexcretion (90%)

Urate overproduction (10%)

A

Uric acid underexcretion (90%): impaired renal function limiting urate excretion; drug-induced inhibition of urate excretion.

Urate overproduction (10%): excessive purine intake; tumor lysis syndrome.

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14
Q

What causes plasma [urate] to increase? (2)

A

Fractional excretion is less than normal.

GFR falls (i.e. kidney disease).

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15
Q

Treatment of Gout acutely:

Treatment of Gout if there are recurrences:

A

Acutely, anti-inflammatory drugs:

  1. NSAIDs
  2. Colchicine
  3. Glucocorticoids

If recurrences, must lower [urate]

  1. Lifestyle changes.
  2. Meds: allopurinol, febuxostat, probenecid, pegloticase, etc.
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16
Q

What is the MOA of Colchicine?

What is the indication?

Which patients are contraindicated?

What are the major adverse-effects?

A

It diffuses into cells to block tubulin and blocks formation of microtubules which leads to inhibition of WBC migration and phagocytosis.

NSAID intolerances/contraindations.

Advanced renal and hepatic impairment.

GI distress, N/V/D.

17
Q

What is the MOA of Allopurinol?

What are the indications?

What are the major adverse-effects?

A

Competitive inhibition of xanthine oxidase, which inhibits the conversion of hypoxanthine and xanthine to uric acid.

Recurrent gout, cancer/chemo-induced hyperuricemia (tumor lysis syndrome).

*SJS, skin rash, N/V, elevated LFTs.

18
Q

What is the MOA of Febuxostat?

What are the indications?

What are the major adverse-effects?

A

Inhibition of xanthine oxidase so that hypoxanthine and xanthine are excreted more easily.

Patients who can’t tolerate allopurinol.

Very few, but it is highly expensive.

19
Q

What is the MOA of Pegloticase?

What are the major adverse-effects?

A

It is a recombinant mammalian uricase and is covalently attached to methoxyy-polyethelyene glycol. It converts uric acid to allantoin (more solluble).

Infusion reactions mainly.

20
Q

What is the MOA of Rasburicase?

What is it used for?

A

Non-pegylated recombinant uricase.

Prevention of acute uric acid nephropathy due to tumor lysis syndrome in a patient with high-risk lymphoma or leukemia.

21
Q

What is the MOA of Probenecid?

What is the major indication?

What are the major adverse-effects?

A

It is an organic acid that blocks urate resorption more than urate secretion. Thus, it increases fractional excretion of urate (decreases plasma concentration).

Underexcreters with GFR > 60 ml/min and NO stones.

  • hyperuricemia
  • frequent attacks

It is a sulfa-containing drug, so sulfa reactions are possible.