Tx of Bone and Joint disorders Flashcards
Acetylsalicylic Acid (Aspirin) facts ?
Aspirin was first introduced by the drug and dye firm Bayer in 1899
Classified among the nonsteroidal anti-inflammatory drugs (NSAIDs)
Inhibits prostaglandin and thromboxane synthesis
Acetylsalicylic Acid (Aspirin) what is required for effective anti-inflammatory action ?
Higher dose
Acetylsalicylic Acid (Aspirin) low doses ?
typically 75 to 81 mg/day
inhibits platelet generation resulting in an antithrombotic effect.
anti platelet effect
Acetylsalicylic Acid (Aspirin) intermediate doses ?
(650 mg to 4 g/day)
inhibit COX-1 and COX-2, blocking prostaglandin (PG) production, analgesic and antipyretic effects.
Aspirin anti platelet effect ?
Measurable prolongation of bleeding time (PTT)
Inhibitory effect on platelet aggregation lasts for up to 8 days
Significantly reduces the incidence of stroke and myocardial infarction in patients at risk
Common in patients who self-medicate ?
Watch for salicylism (salicylate poisoning) pg. 47
Salicylism ?
Mild chronic salicylate intoxication after repeated administration of high doses
Aspirin, pharmacokinetics change at ?
higer doses
Severe form requires immediate treatment (within 1 to 2 hours)
- *watch people with liver disease you can send them into an OD
- *
Salicylism sxs ?
headache,
dizziness,
tinnitus,
hearing loss,
mental disturbances,
sweating,
thirst,
hyperventilation,
nausea,
vomiting,
and sometimes diarrhea
Salicylism tx ?
Immediate treatment needed
Gastric lavage (NG tubes)
Activated charcoal to adsorb drug left in the stomach / dialysis
An association between aspirin use and induction of ___________ exists in children
Reye’s syndrome
FDA recommends NO ASA to those under the age of __ ?
16
what is Reyes syndrome ?
Reye’s syndrome is a rapidly progressive encephalopathy which usually begins shortly after recovery from an acute viral illness, especially influenza and varicella (chickenpox).
liver encephalopathy
The exact cause is unknown and, while it has been associated with aspirin consumption by children with viral illness ?
Reyes syndrome
Reye’s syndrome elevates blood _____ levels , lowers blood _____ .
ammonia
sugar
ammonia level to see if they are truly encephalopathic
hepatic encephalopathy
Reye’s syndrome results in
Fatty liver with minimal inflammation and cerebral edema
Effects many organs, especially the brain and liver
Reye’s syndrome classic features ?
rash, vomiting, and liver damage
ASA dose ?
325 mg
ASA complication and precautions ?
GI bleeding
coagulation disorder
G6PD deficiency
influenza, varicella, or febrile viral infection (pts <20 yo)
caution in pts 80 yo and older
Theenzyme ____________________ responsible for the formation of prostanoids
cyclooxygenase (COX)
Precursor to formation of three main groups ?
Prostanoids
Prostacyclins
Thromboxanes
Cyclooxygenase-1 (COX-1) is known to be present in most ______
tissues
In the gastrointestinal tract, COX-1 maintains the ______________.
normal lining of the stomach
COX-1 also involved in ?
kidney and platelet function
Cyclooxygenase-2 (COX-2) is primarily present at sites of ___________ ?
inflammation
Traditional NSAIDs are considered “nonselective” because they inhibit both ?
COX-1 and COX-2
Inhibition of COX-1 is
undesirable
inhibition of COX-2 is considered ?
desirable
What are the three categories of NSAIDs ?
Salicylates (aspirin)
Traditional NSAIDs (non-selective)
COX-2 selective NSAIDs
Non-selective NSAID’s examples ?
Indomethacin (Indocin)
Ibuprofen (Motrin)
Naproxen (Anaprox)
Ketoralac (Toradol) - GI offensive but great in IV form in ER - works well with real stones or renal colic ( great IV NSAIDs in acute care setting)
NSAIDs choice is typically determined via ?
trial and error
NSAID’s facts and choice ?
Patient choice
Typically cause GI effects
Use with H2 blockers chronic use
Acetaminophen preferred for mild to moderate pain without inflammation
**watch GI effects with non selectives , use you pepcids with with like the H2 ’s **
NSAID’s Pharmacokinetics ?
Rapidly and completely absorbed GI tract
Crosses placenta
Metabolized by Liver
watch if liver disease
Excreted in Urine
________ enters breast milk
Naproxen
- *watch special populations
- *
______ does not enter breast milk
Motrin
back pain patient in female
NSAID’s HL: Children ?
(under 8 years old)
8-17 hours
on call peds: motrin every 8 hours
NSAID’s HL: Adolescents ?
(8-14 years)
8-10 hours
NSAID’s HL: Adults ?
(over 14 years)
10-20 hours
NSAID’s common side effects ?
Coagulation disorders (Avoid with anticoagulant therapy) synergistic effect
Metabolic acidosis
Rash
Blurred vision, tinnitus, amblyopia (lazy eye)
GI bleed, N/V, abd pain
Headache, altered mental (ASA toxicity)
NSAID’s Safety ” concerned prescribing ?
GI increased risk bleeding
Renal impairment, HTN, heart failure
Contraindicated in Third Trimester – premature closure of ductus arteriosus
(pulmonary artery to the heart)
Elderly and alcohol users
Acetaminophen (Tylenol) has what properties ?
Analgesic and Antipyretic properties
NSAIDs dont
Acetaminophen (Tylenol) class ?
analgesic / antipyretic
Acetaminophen (Tylenol) is Ineffective as an____________________
anti-inflammatory agent
Acetaminophen (Tylenol) is different than NSAIDs in that ?
Tylenol has no…
Has no COX-1 or COX-2 effects
No GI effects generally
Mediator for inhibiting prostaglandin synthesis in the CNS, brain and spinal cord (Cox-3)
you get the effect through the COX 3 pathway
Tylenol doses up to _ grams four times a day
1
Tylenol High dose greater than 2 grams daily increase risk of ?
Increased risk bleeding with Coumadin
Increased risk liver toxicity (liver disease, alcoholics)
Tylenol adults dosage ?
325mg, 650mg, 1000mg
Extra Strength 500mg tabs
Tylenol meds dosage ?
15
Why is tylenol better than NSAIDs ?
Analgesic action
Antipyretic action
Significantly reduced gastric irritation
When prescribing patients tylenol be sure to watch for ?
acetaminophen poisoning
what happens in acetaminophen poisoning ?
Potentially fatal hepatic necrosis over 7 to 8 days
acetaminophen poisoning
Day 1-2 sxs. ?
day 1: nausea, vomiting, diaphoresis
both: liver enzymes, ALT, bilirubin, and PT rise
acetaminophen poisoning Day 3-4 sxs ?
peak hepatotoxicity
acetaminophen poisoning Day 7-8 sxs ?
death or recovery
unless aggressively treated
acetaminophen poisoning tx ?
Treatment must be immediate
Acetaminophen Overdose tx ?
Presentation similar hepatic encephalopathy
Treatment with N -acetylcysteine (NAC)
NAC is nearly 100% hepatoprotective when it is given within 8 hours after an acute acetaminophen ingestion
Activated charcoal
Nomogram ?
based on time, dosage and serum levels
tracking OD
Acetaminophen Overdose facts ?
More 3 glasses wine may produce hepatotoxicity – discuss alcohol use
Discuss doses with parents due to different concentrations
15mg/kg oral remember this dose!
Cytoprotective agents ?
Misoprostol
Misoprostol trade ?
(Arthrotec/Cytotec)
Cytoprotective agents MOA ?
Increases production of mucous lining the stomach
Inhibits gastric acid secretion
Misoprostol (Cytotec)
is a what combination ?
Dicloenac Sodium (NSAID) combination
Misoprostol (Cytotec)
indications ?
Indicated NSAID induced ulcer or protection
Misoprostol (Cytotec)
is used with ?
Used with NSAID’s / ASA
Misoprostol (Cytotec)
o used in ?
Used in early pregnancy termination
Misoprostol (Cytotec) BBW ?
Black Box warning with pregnancy / miscarriage
**cytotec is actually a abortion medicine - so that is BBW
Arthrotec reduces incidence of ulcers by __% compared to Diclofenac
60%
arhtrotec combos are alot better as far as producing ulcers
Ibuprofen trade ?
Advil, Motrin, Nuprin
Ibuprofen is in a sub-class of ?
propionic acid derivative that inhibits COX
Ibuprofen primary used because ?
used for its anti-inflammatory properties
Ibuprofen is effective a relieving ?
mild to moderate pain
Ibuprofen is NOT used for what ? But is does have what action ?
anti platelet activity
Anti-pyretic action
Ibuprofen pharmacokinetics and HL ?
Metabolized by Liver
Excreted by Kidneys
Half-life 2-4 hours for the standard does but it can go up if people taking it chronically
Ibuprofen adverse reactions ?
Prolonged bleeding times, Thrombocytopenia (avoid bleeding conditions)
Rash Arrhythmias Edema Headache, psychosis May inhibit antiplatelet activity of ASA Chewable contain aspartame (caution phenylketonuria)
COX-2 Inhibitors own notes ?
more specific ones used more as a target
for RA and chronic inflammatory states
COX-2 Inhibitors are more specific to ?
inflammation
COX-2 Inhibitors are free of ?
GI side effects
COX-2 Inhibitors may produce what ?
NSAID induced nephrotoxicity (COX-2 produced in the kidney)
COX-2 Inhibitors example ?
Celecoxib
Celecoxib trade ?
Celebrex
What two previous COX2-Inhibitors were removed from the market ?
Vioxx
Bextra
When COX-2 Inhibitors reach therapeutic levels, there is little or no effect on ?
COX-1
Celecoxib (Celebrex)
adverse reactions ?
edema
HTN
increased risk of MI
Rash
Renal toxicity
Fatigue, headaches, flu-like symptoms
once starting it they can get this serum sickness when they first start it : flue achy, N/V