Musculoskeletal Drugs Flashcards
Bisphosphonates MOA
inhibit osteoclast activity, promote osteoclast apoptosis
Bisphosphonates Examples
- Alendronate (Fosamax)
- Risedronate (Actonel)
- Ibandronate (Boniva)
- Zolendronate (Reclast/Zometa)
Considerations when taking Bisphosphonates
take on empty stomach, separate from other medications, don’t lie down for 30 minutes to 1 hour after taking
Bisphosphonates Route of Administration
- Alendronate: oral daily, or oral weekly in high dose
- Risendronate: weekly
- Ibandronate: monthly
- Zolendronate - IV yearly
Bisphosphonates Indications
- treatment and prevention of osteoporosis
2. Paget’s disease
Bisphosphonates Contraindications
- Hypocalcemia
- Poor renal function
- Significant GI disease (ie esophagitis)
- Invasive dental procedures (can cause osteonecrosis of the jaw)
Bisphosphonates Side Effects
- GI - nausea, dyspepsia, reflux, cramps
- esophagitis or esophageal erosion
- osteonecrosis of the jaw
Lab Work with Bisphosphonates
- Ca and BMP (kidney function) prior to starting
2. Monitor serum calcium, phosphorous, alkaline phosphatase
Recommended daily intake of Vit D3
- 600 IU/day
2. 800 IU/day for females over age 71
Effect of Vit D
increase serum calcium concentrations (increase calcium absorption from intestine and distal renal tubules, regulate bone resorption and formation)
Vit D effect on PTH
inhibits PTH
What kind of vitamin is vitamin D?
lipophilic
Indications for Vit D
- osteoporosis
- hyperparathyroidism
- osteomalacia
- Rickets
Contraindications for Vit D
hypercalcemia
Vit D drug interactions
- Vit D analogues - calcitrol, paricaltrol, and doxercalciferol –> hypercalcemia –> headache, nausea, dizziness, vomiting, and loss of appetite
- Hydrocholorthiazide –> hypercalcemia
Side effects of Vit D
- Vit D toxicity –> GI pain, renal stones, psychiatric disturbance
How are sunlight and Vit D related?
UV -B rays convert 7-dehydrocholesterol to pre-vitamin D3 which then becomes Vit D3
sunlight recommendations
5-30 minutes of sun exposure between 10 am and 3 pm twice a week, to face, arms, legs, or back
Types of NSAIDs
- Nonselective
2. COX-2 selective
Nonselective NSAID examples
- ibuprofen (Motrin/Advil)
- naproxen (Aleve/Anaprox)
- ketorolac (Toradol)
- indomethacin (Indocin)
- etodolac
COX-2 selective NSAID example
Celecoxib/Celebrex
NSAID MOA
acts on arachidonic acid pathway and blocks COX-1 and COX-2 and causes decrease in prostaglandin formation which results in decreased inflammation, pain, and fever
Function of COX-1 pathway
production of protective lining in stomach
platelet aggregation
Function of COX-2 pathway
inflammatory response
Pharmacokinetics of NSAIDs
- well absorbed
- hepatic metabolism (most)
- short to intermediate half-lives (2-12 hr)
Indications for NSAIDs
pain, inflammation, fever
Contraindications for nonselective NSAIDs
history of peptic ulcers, GI bleeding, chronic inflammation of GI tract, history of sensitivity
Contraindications for COX-2 selective NSAIDs
history of sensitivity
history of sensitivity to sulfonamides
Side Effects of nonselective NSAIDs
GI, edema, dizziness, acute renal failure
Side Effects of COX-2 selective NSAIDs
cardiovascular, dizziness, edema
which NSAID is the strongest
Indomethacin
Aspirin - MOA and function
- irreversibly inhibits COX-1 and COX-2
2. prolonged platelet activity (prevents clotting)
Contraindications for aspirin
same as other NSAIDs anti-coagulation 3rd trimester pregnancy children!!! pre-surgery
Aspirin side effects
- Reyes syndrome
- asthma
- ototoxicity
- bledding
what medication class should you NOT use NSAIDs with
glucocorticosteroids –> increased risk of GI bleed
What is gout?
Dysfunction in uric acid metabolism –> high levels of circulating uric acid in blood –> uric acid crystals deposited in cartilage (big toe, ankle, knee, elbow) –> crystals grow and causes inflammation/pain
Gout medication examples
- Colchicine
- Probenecid
- Allopurinol
Colchicine MOA
suppresses immune function (affects PMNs ability to attract other immune modulators)
Colchicine route of administration
oral
Colchicine route of excretion
89-90% fecal
10-20% renal
Colchicine Indications
- acute gout attacks
- long term prevention of recurrent gout attacks in combo with uric acid lowering therapy
- 2nd line therapy
Colchicine Contraindications
- renal failure
- hepatic disease
- cardiac disease
Side effects of Colchicine
- DIARRHEA, GI UPSET
- bone marrow suppression
- myopathy
- neuropathy
Probenecid MOA
increase uric acid excretion
Indication for Probenecid
- prevention of gout
2. improve effectiveness of penicillin
Contraindications of Probenecid
- renal insufficiency
- urolithiasis
- peptic ulcer disease
Side effects of Probenecid
- generally well tolerated
- GI irritation (N/V/D)
- allergic reaction
Important Patient Education with Probenecid
- Adequate hydration to prevent kidney stones
2. may have precipitating acute gout attack when starting Probenecid (can take indomethacin)
Allopurinol MOA
decreases uric acid synthesis
Indications for Allopurinol
- prevention of gout
- prevention of uric acid renal stones
- complicated hyperuricemia
Allopurinol contraindications
previous hypersensitivity
Side effects of Allopurinol
- skin reactions (Steven-Johnsons Syndrome)
- liver reactions
- renal insufficiency
Considerations for taking Allopurinol AND Probenecid
- Need higher dose of allopurinol
2. makes probenecid more effective
What do you need to monitor in patients taking daily medication for gout prevention
- CMP (renal and liver function)
2. CBC (anemia or bleeding issues)
Why should you be cautious when giving colchicine?
it has a narrow therapeutic index, overdose if fatal –> not used for chronic control
what is allopurinol often taken in conjunction with ?
colchicine for acute treatment and prevention
NSAIDs and surgery?
all NSAIDs must be stopped 7-10 days prior to surgery
dose of naproxen
500 mg BID (according to pharm tutor)
useful info about Ketorolac/Toradol
can give IV, stronger than ibuprofen
What is an indication for indomethacin?
gout if lots of inflammation but more GI S/E
When would you suggest Celebrex?
if patient has lots of abdominal pain when taking nonselective NSAIDs
aspirin indications
- clot prevention
- coronary artery dx, hx of MI (baby aspirin 81 mg)
- acute MI (4 baby aspirin or 1 adult aspirin 325 mg)
- fever and pain
Reyes syndrome
altered mental status, jaundice due to liver damage, encephalopathy
benefits of aspirin
doesn’t irritate GI lining, don’t have to worry about overdose like tylenol
name of vitamin D2
ergocalciferol (plant source?)
name of vitamin D3
cholecalciferol (animal source?)
aspirin’s effect on uric acid levels
causes net retention of uric acid
first line treatment for Gout
NSAIDs - indomethacin, naproxen, sulindac