MSK pharmacology NSAIDS/WUHS Flashcards
week 9
What are names of prescription NSAIDS?
- salsylate (disalcid)
- indomethacin (indocin)
- meclofenamate(meclomen)
- piroxicam (feldene)
- sulindac (clinoril)
- tolmetin (tolectin)
- diclofenac (voltaren -cream)
- diflusinal (dolobid)
- etodolac (lodine)
- fenoprofen (nalfon)
- flurbiprofen (ansaid)
- ketoralc (toradol)
- mefenamic acid (ponstel)
- nabumetone (relafen)
- oxaprozin (daypro)
- phenylbutazone (cotylbutazone)
- voltaren down are also aspirin substitutes
what is diclofenac (voltaren)
NSAID cream - arthritis pain reliever
how is ketorolac (toradol) administered?
IV or intramuscular
what are the 3 over the counter NSAIDS?
- aspirin (many trade names)
- ibuprofen (advil, motrin, others)
- naproxen (aleve, naprosyn)
OTC NSAIDs are sold ?
in smaller doses
why are OTC NSAIDS sold in smaller doses?
greater patient safety
what is a normal mg tablet amount for OTC ibuprofen?
200 mg
what is the mg tablet amount for prescription motrin?
800 mg
* take 4, 200mg ibuprofen tablets for same effect
what is the benefit of trying OTC medication first?
big cost difference
aspirin is the prototype for NSAIDS - what is aspirin made of?
- acetylsalicylic acid = ASA
- used clinically for century
what are some misconceptions of ASA (aspirin)? what is the truth of ASA?
some patients discrespect ASA
- see it as “old” drug
- inexpensive
readily available without prescription
truth: ASA is very powerful, very effective drug; probably drug of choise
- as PT may need toweight placebo effect of gettinga prescription (patient expectation)
ASA vs. other NSAIDS
- other NSAIDS are attempts by drug companies to make a better aspirin
goals of making other NSAIDs:
- more effective
- fewer side effects
waht is the usual dosage of other NSAIDS (not asa)? what is the result?
325mg-650mg every 4 hours for aches, pains, fevers
result:
- most have no significant advantage
- higher costs
MOTRIN
indications:
contraindications:
Dosage:
indications:
- arthritis
- musculoskeletal pain
- inflammatin
contraindications:
- sensitivity/allergic reaction to ibuprofen, aspirin other NSAIDS
- asthma caused by aspirin or other NSAIDS
- angioedema
- as well as general contraindictions for all NSAIDS
dosage:
- OA, RA: 1200 to 3200 mg/day divided into 3-4 doses. do not exceed 3200 mg per day.
- mild to moderate pain: 400mg every 4-6 hrs
NAPROXEN
Indications:
contraindications:
Dosage:
indications:
- pain management
- bursitis
- tendonitis
contraindications:
- prior allergies to naproxen
- NSAID induced asthma, rhinitis or nasal polyps
- carefully question about asthma, urticaria, nasal polyps, hypotension assoc. with NSAIDS
- all contraindications of general NSAIDS
Dosage:
- 375 mg or 500 mg 2x daily
relative contraindications for NSAIDS
10 of them …
- history of peptic ulcer disease
- history of renal disease
- history of liver disease
- history of congestive heart failure
- hypertension
- asthma/reactive airway disease
- pregnancy, nuring mothers
- concurrent use of corticosteroids
- concurrent use of anticoagulants
- age ≤ 15 or ≥ 65
what is the contraindication for NSAIDS and acute muscle injury?
evidence shows that NSAIDs given during acute stage of muscle injury may delay muscle fiber regeneration and recovery of force generating capacity
what are the main adverse side effects of all NSAIDS?
- gastric irritation, ulcers
- hepatic and renal toxicity, particularly in patients with previous damage
what are the adverse side effects of overdose: ASA intoxication?
- hearing loss
- tinnitis
- confusion
- headache
what is the half life (h), onset (min), comments for Aspirin?
half life (h): 0.25
onset (min): 10-30
comments: prototypical NSAID
what is the half life (h), onset (min), comments for ibuprofen (motrin, etc) (propionic acid derivative)
half life (h): 2.00
onset (min): 10-30
comments: inc. GI intolerance compared to ASA
what is the half life (h), onset (min), comments for naproxen, naprosyn (propionic acid derivative)?
half life (h): 13.00
Onset (min): 60-120
comments: inc. GI tolerance compared to ASA
potential NSAID adverse effects by system
system: gastrointestinal
adverse effects:
nausea, heartbur, dyspepsia, gastric ulcers, duodenal ulcers, perforations, bleeding complications
system: Renal
Adverse Effects:
sodium retention
edema
hyperkalemia
acute failure
nephritic syndrome
papillary necrosis
system: CNS
Adverse effects:
tinnitus
sedation
dizziness
system: hematological
Adverse Effects:
hemorrage
anemia
COX-2 cardiovascular events
system: allergic reactions
adverse effects:
other NSAID - or salicylin containg foods:
apples, oranges, bananas
identification of patients at high risk and potential adverse effects
high risk population:
increasing age, female sex, age > 85 y
adverse affect:
slowed metabolism and elevated tissue levels of more lipid soluable drugs
high risk population: history of peptic ulcer
adverse effect:
repeat ulceration and GI hemorrhage
high risk population: low serum albumen
adverse effect:
elevated serum NSAID levels and possible overdosage
high risk population: concomitant use of multiple antithrombotic agents
adverse effect:
hemorrhage
high risk pop: concomitant use of other NSAIDs or steroid agents, increase nsaid dose, new nsaid user
GI injury
gastric hemorrhage
initiation of Gi hemorrhage
high risk pop: hypovolemic states, renal impairment due to age, atherosclerosis, hypertensive renal disease, otherintrinsicrenal disease
adverse effect:
renal failure, impairemnt of glomerular filtration, acute renal failure, edema, iinterstitial nephritis, papillary necrosis, chronicrenal fialure, hyperkalemia (high potassium)
what is the primary reason for NSAID use in elderly?
osteoarthritis
NSAID users are how many times more likely to be hospitalized?
new nsaid users?
4x more likely
5x-6x more likely
what % of elderly (≥65yrs) are on prescription NSAIDS?
15%
how many death yearly occur from NSAID prescriptions?
7,600
how many hospitalizations per year occur due to NSAIDS?
76,000
elderly _____ are ___ as likely to have GI problems from NSAIDS than _____
women are 2x, than men
what % of NSAID prescriptions were unnecessarily written?
42%
what are the alternatives to NSAIDS used for osteoarthritis?
- physical therapy (evidence based, active treatment programs)
- behavior modification
- joint protection
- exercise
- weight loss
- acetaminophen (not NSAID - affects brain differently)
should people be choosing the drug with a longer or shorter 1/2 life first?
avoid first choice use of longer half-life agents (naproxen at 13 hrs vs ibuprofen at 2 hrs)
where NSAIDS found to be more helpful than other drugs when it comes to LBP?
no - NSAIDS are not more effective than other drugs (including tylenol, mms relaxants, opiates) for acute LBP, lacking evidence for chornic LBP
acetaminophen (tylenol)
indications:
difference from NSAID:
adult dosage:
indications: analgesic, antipyretics
difference: equivalent analgestic benefit to low dose NSAID, no anticoagulant or anit inflammatory effect
adult dosage:
325 mg tabelts take 2 every 4-6 hrs, do not exceed 12 tablets in 24 hrs
500 mg tablets take 2 gelcaps, 4-6 hrs no more than 8 gelcaps in 24 hrs
generally up to 1000 mg TID is sufficient
acetaminophen (tylenol) adverse effects
- less gastric irritaion with tylenol
- tylenol drug of choice for pregnant women and children w fever
metabolzied and excreted by liver (liver toxicity) - do not take if liver or kidney problems
- tylenol overdose - liver toxicity (potentially fatal!!)
what is the toxic dose for acetaminophen?
varies, depends on many factors including hydration level (hydrated cells more robust)
the mechanism is unknown
selection of NSAID or acetaminophen - how to pick?
inflammation or pain & inflammation –> assess risk factors for GI or renal toxicity —> if no risk factors nonselective NSAID (ibuprofen, naproxen aspirin)
if risk factor is present –> refer NSAID prescription choise to PC. will require non selective NSAID + GI protective agent
pain only:
acetaminophen
drugs for muscle spasms
polysynapticinhibitors
- methocarbal (robaxin)
- cyclobenzaprine (flexeril)
diazepam (calium)
polysynaptic inhibitors (muscle spasms)
Flexeril (cyclobenzaprine)
indications:
action:
dosage:
duration of therapy:
considerations for use:
indications: relief muscle spasms assoc. with acute, painful MSK considitons
action: relieves msucles spasm oflocal origin
dosage: 10 mg TID, not to exceed 60 mg/day
duration: 2-3 weeks
considerations of use:
- take 1-2 hrs before bed if using at night only
- may cut in half, if siginificant drowsiness in morning
- no driving/heavy equipemnet operation
muscle spasms
contraindications for flexeril (cyclobenzaprine)
- hypersensitivity to drug
cardiac disease, CHF, arrhythmias, heart block or conduction disturbances
-hyperthyroidism
-concamitant use of MAO inhibitors, or within 12 days of discontinuation - concomitant use of tricyclinc antidepressants
what are some drug intractions/precautions for flexeril (cyclobenzaprine)?
- may enhance effects of alcohol, barbiturates, CNS depressants
- may impair mental/physical abilities requires for performance of hazardous tasks (ddriving, operating machinery)
muscle spasms
Robaxin (methocarbamol) 1
indications
dosage
indications: relief of discomfort associated with acute painful MSK conditions
dosage: initial 1500 mg QID
maintenance: 1000 mg QID or 1500 TID
robaxin (methocarbamol) 2
contraindications:
adverse reactions:
contraindications:
- hypersensitivity to any of the ingredients
- kidney or liver disease
- porphyria
- epilepsy
adverse reactions:
light headedness, dizziness, drowsiness, nausea, blurred vision, headache, fever, rash
what are the main take aways fro muscle relaxants?
3 of them
- indicated for acute msucle spasm associated with pain
- treatment efficacy greatest in 1st 4 days
- outcomes better when NSAIDS and MS relaxants combined then NSAIDS alone
