1. NSAIDs, Acetaminophen Flashcards
2016 RxPrep p657
MOA of acetaminophen
Analgesic: thought to inhibit prostaglandin synthesis in the CNS and reduce pain impulse generation; may include the endogenous cannabinoid system and inhibit NMDA receptors
Antipyretic: mediated by inhibition of heat regulating centers in the brain
Lacks anti-inflammatory effects; does not inhibit thromboxane = no anti-platelet effects
acetaminophen (brand)
available as tablet/caplet, chewable tablet, ODT, injection, suspension, infant drops, suppository
Tylenol
Most “non-Aspirin” pain relievers
Ofirmev (IV)
FeverAll (rectal suppository)
acetaminophen dosing (for max/day, 325 mg, 500 mg, 650 mg, rectal suppository, and IV)
–Max: 4 g/day, 325 mg per Rx dosing unit in combo products
–325 mg: max 2 tab Q4-6h, NTE 10 tabs/day (3250 mg)
–500 mg: max 2 tab Q6h, NTE 6 tabs/day (3000 mg)
–650 mg ER: max 2 tab Q8h, NTE 6 tab/day (3900 mg)
–rectal supp: 650 mg Q4-6h, NTE 6 supp/day (3900)
–IV (for ≥50 kg): 650 mg Q4h (3900 mg) or 1g Q6h (4000 mg)
acetaminophen dosing (pediatrics)
–10-15 mg/kg Q4-6h; max 5 doses/day
–infant drops come in 160 mg/5 mL (like children’s suspension to avoid dosing confusion and toxicity risk)
–rectal supp: 80, 120, 325, 650 mg
acetaminophen BBW
May cause severe hepatotoxicity (potentially requiring liver transplant or resulting in death), usually associated with excessive acetaminophen intake (>4 g/day) or use of more than one acetaminophen containing product; risk of 10-fold dosing errors with injection
acetaminophen SEs
–Hepatotoxicity (possibly fatal)
–Severe skin rash (rare: SJS, TEN, AGEP - stop drug, seek immediate medical help)
–Nephrotoxicity (rare: usually with chronic overdose; generally safer than NSAIDs in renal disease)
acetaminophen is pregnancy category ___ (IV formulation)
C
often used for mild pain in pregnancy
avoid using ______ for acetaminophen on patient labels
APAP
acetaminophen safety consideration: use the _______ ____ or ______ provided with the medicine.
dosing syringe
cup
acetaminophen safety consideration: caution with IV acetaminophen. Concentration is 10 mg/mL (in 100 mL vials). Order in ___, not ____. Nurses should not be permitted to prepare doses; it should be prepared in the _____.
mg
mL
pharmacy
acetaminophen overdose:
–antidote: _________ (PO-Mucomyst, IV-Acetadote)
–MOA: restores [intra/extra]cellular ______
–administer immediately; even before the results of APAP level are obtained; within ___ hrs of ingestion
–Give ___ mg/kg PO loading dose, then ___ mg/kg PO Q4h x ___ doses (unless initial APAP level is non-toxic)
–Often causes N/V due to _____ of ______ ______
–N-acetylcysteine (NAC) (IV is more costly) –intra; glutathione –8 –140; 70; 17 –odor; rotten eggs
acetaminophen DDI: [may/may not] be used with warfarin; chronic use of >__ g/day can increase INR
may
2
acetaminophen DDI: avoid or limit _____ use due to risk of hepatotoxicity
alcohol (1 drink/day for women; 2 drinks/day for men)
acetaminophen counseling point: should see Dr. if self-treating condition worsens, persists for more than ___ days, experiencing a high fever >____ºF, rash, N/V, or blood in stool; this applies for ______ as well; _____ should be seen by a pediatrician.
2
102.5
children
infants
MOA of NSAIDs
–non-selective: block synthesis of COX-1 (binds reversibly) and COX-2
–selective: block COX-2 only (decreasing GI risk)
–salicylates (aspirin): inhibits COX-1 irreversibly
COX-1 vs COX-2
–both enzymes catalyze the conversion of arachidonic acid
–COX-1: cytoprotective prostaglandins to protect GI mucosa; thromboxane to aid platelet aggregation
–COX-2: inflammatory prostaglandins sensitize skin pain receptors, recruit inflammatory molecules, regulate hypothalamic temperature control
NSAID BBW
a MedGuide is required to address GI and CV risks
all NSAIDs, including aspirin BBW: GI risk (define)
Can occur at any time during use and without warning. _____ patients, those with a hx of GI bleed, pts taking ______ and those taking ____/____ are at greatest risk for serious GI events
GI risk: bleeding, ulceration, perforation of stomach and intestines, which can be fatal
Elderly
corticosteroids
SSRIs/SNRIs
all non-aspirin NSAIDs BBW: CV risk (define)
Can occur in first few ____ of use. Risk may be increased with ____ doses or _____ duration of use and in patients with ___ disease or ____ _____ for it.
CV risk: thrombotic events, MI, stroke, HF weeks higher longer CV risk factors
non-aspirin NSAID CI
treatment of perioperative pain in the setting of CABG surgery
aspirin/acetylsalicylic acid (brand, dosing)
available as tablet/caplet, chewable tablet, suppository
Ascriptin, Bufferin, Ecotrin:
cardioprotection dosing 81-162 mg; analgesic dosing 325-650 mg Q4-6h
Durlaza (Rx): 162.5 mg daily
GI bleed s/sx
–dark, tarry stools
–stomach upset
–weakness
–coffee-ground emesis (indicates a more serious, fast GI bleed)
non-acetylated salicylates (5)
–salsalate –magnesium salicylate –choline magnesium trisalicylate –diflunisal –salicylate salts
salsalate (brand, dosing)
generic only
up to 3 g/day divided BID-TID
magnesium salicylate (brand, dosing)
Doans, Doans ES, Momentum, Keygesic
ES: 580 mg/tab - 2 tab Q6h, NTE 8 tab/day
choline magnesium trisalicylate (brand, dosing)
generic only
1 g BID-TID or 3 g QHS
diflunisal (brand, dosing)
500 mg BID-TID; max 1.5 g/day
salicylate salts (brand, dosing)
Arthropan, Asproject, Magan, Mobidin, Resolate, Tusal
*no longer commonly used
NSAID warning: avoid with ______ hypersensitivity, nasal _____, asthma
NSAID
polyps
salicylate warning: avoid in ______ and teenagers with any _____ infection due to potential risk of ______ syndrome (Sx include _______, N/V, _______, confusion.
children viral Reye's somnolence lethargy
NSAID warning: severe skin rash (rare) including ____/____.
SJS/TEN
Stop drug, seek immediate medical help
NSAID warning: upper GI events (ulcers), avoid if possible __-__ weeks before surgery due to _____ effects
1-2
antiplatelet
NSAID SEs:
dyspepsia, heartburn, bleeding, renal impairment, increased BP, CNS effects (fatigue, confusion, dizziness; caution in elderly), photosensitivity, fluid retention/edema, hyperkalemia (in renal impairment or with potassium-retaining agents), blurred vision
most NSAIDs are pregnancy category __ or __ (avoid, especially in the ___ trimester)
C or D
3rd
To decrease nausea with NSAIDs, use ___/______ product or take with _____.
EC/buffered
food
____ may be used to protect the gut with chronic NSAID use; consider risks of their chronic use (2)
PPIs
decreased bone density, increased infection risk
Do NOT use Durlaza when…
immediate effect is needed (e.g., MI)
salicylate overdose can cause _____
tinnitus
salicylates should be taken with food, water or milk to minimize ___ _____; all NSAIDs [should/can] be taken with food; salicylates usually cause [more/less] nausea
GI upset
should
more
_____ salicylate is a popular OTC topical found in Bengay, Icy Hot, Flexal, Thera-Gesic, Salonpas
methyl
ibuprofen (brand, dosing)
available as tablet/capsule, chewable tablet, suspension, injection
Motrin, Advil, Caldolor (IV)
OTC: 200-400 mg Q4-6h, max 1.2 g/day
Rx: 400-800 mg Q6-8h, max 3.2 g/day
higher doses required for inflammation
ibuprofen self-treatment should be limited to ___ days
10
ibuprofen dosing (pediatrics)
5-10 mg/kg/dose Q6-8h (as an antipyretic), max 40 mg/kg/day
Caldolor IV injection: for mild-moderate pain, can decrease ____ dose; can be used when oral routes are not available; must be ______
opioid
diluted
ibuprofen is similar to aspirin except for….
risk of Reye’s in children is not present (safe to use in pediatrics)
Neoprofen injection is indicated for….
closure of patent ductus arteriosis (PDA) in premature infants
naproxen (brand, dosing)
Aleve (OTC), Naprelan, Naprosyn, Anaprox
OTC (for pain, fever): 200 or 220 mg - 1 tab Q8-12h (may take 2 tab for 1st dose), NTE 3 tab/day
Rx: (for inflammation, mild-mod pain): 500 mg Q12h (or 250 mg Q6-8h); max 1250 mg on Day #1, then 1000 mg thereafter
naproxen is sometimes preferred by prescribers and patients for its ___ dosing
BID
naproxen base ____ mg = naproxen Na ____ mg
200
220
The PPI in _____ is used to protect the gut from damage caused by the NSAID
Vimovo
diclofenac (brand, dosing)
available as tablet/capsule, packet, gel, patch, topical solution, injection
Voltaren-XR, Dyloject (IV), Voltaren gel
PO tab: 50-75 mg BID-TID
IV: 37.5 mg Q6h
diclofenac + misoprostol (Arthrotec) BBW
not to be used in women of childbearing potential unless woman is capable of complying with effective contraceptive measures
oral diclofenac formulations are…
not bioequivalent even if mg strength is the same
diclofenac + misoprostol note: misoprostol is used to replace gut-protective _______ to decrease risk of GI damage (was more popular before PPIs); increases ______ ______ and causes cramping and ______
prostaglandin
uterine contractions - which may terminate pregnancy!
diarrhea
indomethacin (brand, dosing)
available as capsule, oral suspension, suppository, injection
Indocin, Tivorbex
IR: 20-50 mg BID-TID
CR: 75 mg daily-BID
Tivorbex: 20 mg TID, 40 mg BID-TID
indomethacin has a high risk for ____ SEs and ___ toxicity
CNS (avoid in psych conditions)
GI
indomethacin IR formulation is an older NSAID approved for _____; any NSAID can be used
gout
Tivorbex is _______ for faster _______
micronized
dissolution
indomethacin injection is indicated for ____ in premature infants
PDA
piroxicam (brand, dosing)
Feldene
10-20 mg day
piroxicam has a high risk for ___ toxicity and severe ____ reactions; use when other NSAIDs have ______; may need agent to protect ____
GI
skin
failed
gut (PPI, misoprostol)
ketorolac (brand, dosing)
available as tablet, injection, nasal spray, ophthalmic
Toradol, Sprix (nasal spray), Acular (opthalmic)
PO: 10-20 mg x1, then 10 mg Q4-6h PRN; max 40 mg/day
IV (≥50 kg): 30 mg x1 or 30 mg Q6h
IM (≥50 kg): 60 mg x1 or 30 mg Q6h
Sprix:
ketorolac parenteral doses should be decreased if ≥___ yo
65
ketorolac: always start __, __, or ____ _____ and continue with ____, if necessary
IV
IM
nasal spray
oral
ketorolac is not to be used in any situation with increased ______ risk
bleeding
ketorolac BBW: for short-term ____ to ____ pain only as continuation of IV or IM ketorolac; max combined duration IV/IM and PO/nasal is ___ days in adults
moderate
severe
5
ketorolac BBW: not for ______ or epidural use
intrathecal
ketorolac BBW: CI in advanced ______ impairment or risk due to _____ depletion; decrease dose if ≥65 yo,
renal
volume
ketorolac can cause severe adverse effects including GI bleeding and perforation, post-op bleeding, _____ _____ failure, ______ failure and ________ shock
acute renal
liver
anaphylactic
ketorolac is used in [post/pre]-op, never [post/pre]-op
post
pre
Sprix should be primed by spraying __ times before…
5
1st dose each day
suldinac (brand, dosing)
is sometimes used with reduced ____ function and in patients on ____ requiring an NSAID
Clinoril
150-200 mg BID
renal
lithium
COX-2 selective NSAIDs lower risk for ___ complications (but is still present), increase risk for ___/_____ (avoid with ___ risk, avoid in high doses and longer duration if use is necessary), same risk for _____ complications
GI
MI/stroke
CVD
renal
What are the COX-2 selective NSAIDs? (4)
celecoxib (most selective)
meloxicam
etodolac
nabumetone
celecoxib (brand, dosing, indications)
available as a capsule
CeleBREX
OA: 100 mg BID or 200 mg daily
RA: 100-200 mg BID
Indications: OA, RA, juvenile RA, acute pain, primary dysmenorrhea, ankylosing spondylitis
celecoxib CI
with sulfonamide allergy
celecoxib BBW
same as other NSAIDs
celecoxib is pregnancy category __ prior to ___ weeks gestation and is category __ starting after
C
30
D
meloxicam (brand, dosing)
available as tablet/capsule, oral suspension
Mobic: 7.5-15 mg daily
Vivlodex: 5-10 mg daily
(Vivlodex capsules and other meloxicam formulations are not interchangeable)
etodolac (brand, dosing)
available as tablet/capsule
Lodine
300-500 mg Q6-8h
nabumetone (brand, dosing)
available as tablet
Relafen
1000-2000 mg daily (can be divided BID)
NSAID DDI: increased bleeding risk with…
other anticoagulants, antiplatelets, some herbals, SSRIs, SNRIs, thrombolytics, steroids (GI risk)
NSAID DDI: use with other NSAIDs with one exception…
low dose aspirin for cardioprotection, but the cardioprotective effects may be blocked by ibuprofen and other NSAIDs - if aspirin needs to be taken for cardioprotection and ibuprofen for pain, take aspirin 1 hr before or 8 hrs after ibuprofen
NSAID DDI: NSAIDs can increase levels of (2)
lithium (avoid concurrent use) and methotrexate
NSAID DDI: caution with the use of aspirin and other _______ agents (aminoglycosides, IV loop diuretics, etc)
ototoxicity
NSAID counseling: –address bleeding, DDIs, GI and CV risk –do not use after \_\_\_\_\_ \_\_\_\_ surgery unless instructed by doctor or after any elective surgery –take with \_\_\_\_\_ –do not use if past allergy with NSAIDs –may raise \_\_\_\_ \_\_\_\_\_ –may cause fluid and water to accumulate, particularly in \_\_\_\_\_ –photosensitivity _do not use if \_\_\_\_\_\_\_\_
coronary heart food blood pressure ankles pregnant
