Week 11: Bisphosphonates Flashcards
Bisphosphonates:
Alendronate (Fosamax), Risedronate (Actonel) indications / MOA
“-dronate”
indication: osteoporosis (1st line), high fracture risk, hypercalcemia, pagets dz, metastatic bone dz
MOA: reduces osteoclasts which inhibits bone resorption
-works best 1st year, then plateaus after 2-3 yrs
how to take bisphosphonates?
“-dronate”
Alendronate, Risedronate zoledronic acid (Reclast)
EMPTY stomach, 8 oz water ONLY
sit up right 30-60 mins after due to esophagitis / gastric irritation
bisphosphonates contraindications
Alendronate (Fosamax), Risedronate (Actonel) zoledronic acid (Reclast)
NO in :
- CKD < 35 CrCl
- uncorrected hypocalcemia
- delayed esophageal emptying (stricture)
- can’t sit up/stand for 30 mins
- inc aspiration risk
- bariatric surgery (upper GI inflammed)
Alendronate (Fosamax), Risedronate (Actonel) , zoledronic acid (Reclast) adverse effects
-atypical femur fractures (don’t stay on med > 5 years)
-severe bone/joint/muscle pain
-upper GI mucosa irritation
-hypocalcemia
-jaw osteonecrosis
drug holiday after 5 yrs after bone density stable
- zoledronic acid: IV
- check CrCl before therapy -> renal toxicity risk, flush, tylenol after to reduce reaction
drug interaction with bisphosphonates
ranitidine. doubles alendronate bioavailability
What’s gout? and risk factors
Crystals only form in hyperuricemia from meds (diuretics), normal breakdown of purines from body nucleic acid or diet alcohol or meats Risk factors: -Obesity -dehydration -canned, processed foods -alcohol -seafood
Antigout agents:
Xanthine oxidase inhibitors MOA & indication
allopurinol and febuxostat
Decrease uric acid lvls by selectively inhibiting xanthine oxidase, which is the enzyme responsible for the conversion of hypoxanthine to xanthine to uric acid
Uric acid then decreases reducing risk of crystallization and gout attack
- chronic gout (allopurinol first line)
1 week for full effects
febuxostat- inc cardiac deaths, give w/ NSAID or colchicine x 6 months
xanthine oxidase inhibitors caution/contraindications
- NO with azathioprine, mercaptopurine, theophylline
- NO pregnancy
- korean, hans chinese, thai pts = test for HLA- B5801 allele = steven jonson syndrome
xanthine oxidase inhibitors SE’s
Hypersensitivity (rare) maculoapular skin rash -Arthralgia n/d Elevated transaminases Hepatotoxicity (rare)
what is used 2nd line for chronic gout or adjunct to allopurinol/colchicine ?
cautions? pregnancy?
probenecid
ONLY ONE GOOD FOR PREGNANCY AND ELDERLY!!!!
NO blood dyscrasia, cc < 30, aspirin, G6PD def, SULFA ALLERGY
what can you use for acute gout?
how long does it take for effect?
colchicine
takes 18-24 hrs to take effect, 48 for full
colchicine MOA
inhibits neutrophils to area of gout attack –> dec inflammation/pain
antiinflamm fo r pain but NOT analgesic
colchicine cautions & SE’s
NO grapefruit juice
-caution in renal,hep, elderly, preg
SE:
- GI
- agrunulocytosis
- aplastic anemia
- alopecia
- abd pain, myopathy
- if pain started more than > 36 hrs prior, colchicine no longer preferred agent. NSAID or corticosteroids!
Prednisone indications / MOA
suppress migration leukocytes so decrease inflammation
anti-inflammatory
ind: acute gout, rhematoid arthritis
prednisone c/c
no active infxns
adrenal suppression
diabetics (causes hyperglycemia)