Pharm Section 6 Flashcards
pain is not a ____, it’s a ______
not a disease, it’s a symptom
people with what hair color are more sensitive to pain?
redheads
chronic pain is classified into what two types?
nocieptive
neuropathic
nociceptive pain
nociceptors (nerves that sense and respond to parts of body suffering from damage) detect irritation or injury and transmit pain signals via peripheral nerves and spinal cord to brain
visceral pain
subtype of nociceptive pain that involves internal organs and is usually poorly localized
neuropathic pain
results from injury or malfunction of PNS or CNS. pain is usually burning, lancinating/stabbing, or electric shock quality. also characterized by persistent allodynia (pain from non painful stimulus)
mainstays for pain treatment include
opioids
NSAIDs
acetaminophen
first-line treatment for mild to moderate acute pain
acetaminophen
first line NSAIDs for mild to moderate acute pain
ibuprofen and naproxen
second-line meds for mild to moderate pain
COX-2 selective NSAIDs
adjunctive for pain associated with nausea
promethazine (Phenergen)
adjunctive for pain associated with inflammation, edema
corticosteroids
adjunctive for pain associated with anxiety
anxiolytics and sedatives
adjunctive for pain associated with muscle spasms
muscle relaxants
adjunctive for pain associated with CNS depression
caffeine
fibromyalgia
chronic disorder mainly affecting women characterized by diffuse musculoskeletal pain, fatigue, IBS, and sleep problems. Treated with variety of meds: analgesics, muscle relaxants, anticonvulsants, antidepressants
what drugs are approved for treating fibromyalgia?
Pregabalin (Lyrica) SNRI dulozetine (Cymbalta) SNRI milnacipran (Savella)*only fibromyalgia*
PDN
painful diabetic neuropathy. pain associated with neuropathy (stabbing, burning, tingling pain). often opioid resistant pain. antidepressants and anticonvulsants commonly used to treat it, as well as gabapentin (Neurontin) and pregabalin (Lyrica)–level A. All drugs used other than pregabalin are level B.
Gabapentin (Neurontin)
Not CS, but can be abused. Used to treat PDN/PHN.
pregabalin (Lyrica)
CS V drug approved to treat PHD, PDN, partial seizures, and fibromyalgia. side effects include: dizziness, drowsiness, difficulty concentrating
chronic pain
lasts longer than 90 days
salicylates
non-narcotic analgesics. two forms: acetylated and non-acetylated
acetylsalicylic acid (Aspirin)
non-narcotic analgesic. acetylated salicylate. originally derived from the bark of the willow tree. Charles Frederick Gerhardt discovered, Felix Hoffman made famous.
diflusinil (Dolobid)
non-acetylated salicylate. non-narcotic analgesic. derivative of, but not metabolized to salicylate
salicylsalicylic acid/salsalate (Dislacid)
non-acetylated salicylate. non-narcotic analgesic.
choline magnesium trisalicylate (Trilisate)
non-acetylated salicylate. non-narcotic analgesic. liquid.
triethanolamine salicylate (Myoflex, Aspercreme)
non-acetylated salicylate. non-narcotic analgesic. topical only.
pharmacological effects of aspirin
analgesia, antipyresis, ant-iinflamatory (large doses only), anti-platelet aggregation, anti-cancer effects
adverse effects of aspirin
most common: GI upset
1st sign toxicity: tinnitus
allergic reactions
dec. excretion of uric acid (worsens gout)
dec. renal blood flow (LT nephrotoxicity)
aspirin in children
don’t use! can cause Reye’s syndrome
explain the analgesic effects of aspirin
inhibits COX 1 and 2, which inhibits production of prostaglandins, which inhibits inflammation and platelet aggregation.
how does aspirin decrease platelet aggregation?
inhibits COX1 for lifetime of platelet, which inhibits the production of thromboxane, which decreases platelet aggregation
what types of cancer has aspirin been shown to reduce the risk for?
colorectal, esophageal, stomach, pancreatic, breast, prostate, and lung. Only reduces cancer risk after 3 years of being on therapy and only reduces cancer mortality after 5.
Alka-seltzer
effervescent tablet containing aspirin
acetaminophen (Tylenol)
aka paracetamol in Eur. Equal analgesic and antipyretic effects as aspirin, but not anti-inflammatory. MOA not clear.
acetaminophen and OA/RA.
good for reducing pain with OA, but doesn’t affect inflammation so not very useful for RA
adult dose for acetaminophen
325-1000mg every 4-6 hours with max dose 4000 mg/day
pediatric dose for acetaminophen
10-15 mg/kg every 4-6 hours with max 5 doses/day
maximum single dose of acetaminophen in healthy adults
between 7500 and 10,000mg
maximum single dose of acetaminophen in healthy kids
> 150mg/kg
FDA is considering lowering the max single dose to what?
625mg/ dose and 3250mg/day
FDA limit on acetaminphen dose in combo products
limited to 325 mg/dose because so many products contain acetaminohpen
infant drops of acetaminophen are marketed as one strength, which is…?
160 mg/ 5 ml
injectable acetaminophen
OFIRMEV. 15 min infusion q6h with max single dose of 1gm and max daily dose of 4gm.
adverse effects of acetaminophen
hepatotoxic. 1/2 of all liver transplants caused by acetaminophen. Fasting and malnutrition increase toxicity. If survive liver toxicity, may also be nephrotoxic, cause severe skin reactions like SJS/TEN/AGEP.
acetaminophen and pregnancy
worries that it may increase the incidence of ADHD, but need further investigations to determine
what is a source you can use to determine what products contain acetaminophen?
knowyourdose.org
pediatric antipyretic/analgesic: ibuprofen vs. acetaminophen
equal safety, equal analgesic efficacy, ibuprofen may be superior anti-pyretic (also can be dose less frequently b/c longer duration of action.
should you alternate acetaminophen and ibuprofen?
no. try acetaminophen first. alternating can confuse the caregiver and may mix up meds
does treating kids’ fevers help them get better faster?
no, just makes them more comfortable
pediatric dose of ibuprofen
10mg/kg per dose
NSAIDs
non-steroidal anti-inflammatory drugs. most prescribed and OTC purchased drugs in the world. three classes include: non-specific/traditional, preferential, and selective
two biggest safety concerns with NSAIDs
GI toxicity
cardio-renal toxicity
others: hepatotoxicity, clotting, fatal skin reactions, and pregnancy (last 6-8 weeks)
aspirin allergy and NSAIDs
may be cross-allergic reactions between people allergic to aspirin and NSAIDs. COX2 selectives may be safer.
non-specific or traditional NSAIDs
inhibits both COX1 (GI tract, platelets) and COX2 (brain, bone, cartilage, inflammation sites)
ibuprofen (Advil, Motrin, Midol)
non-specific or traditional NSAID. OTC forms limited to 200mg or less. available as pediatric (NeoProfen) and adult (Caldolor) injections. Also available as combo with famotidine (Duexis).
naproxen (Aleve)
OTC non-specific or traditional NSAIDs. Possibility for false positive for THC on drug screen.
diclofenac
non-specific or traditional NSAID. many forms, such as Voltaren (delayed release formulation).
most effective NSAID available for improving pain and function in osteoarthritis(OA) is what? what’s the problem with it?
diclofenac 150mg/day, but also most likely to cause hepatotoxicity
sulindac (Clinoril)
non-specific or traditional NSAID.
tolmetin (Tolectin)
non-specific or traditional NSAID.
indomethacin (Indocin)
non-specific or traditional NSAID. has the most prostaglandin inhibition. used primarily for gout, secondarily for tocolysis (suppresses premature labor). Can be used for PDA in infants.
piroxicam (Feldene)
non-specific or traditional NSAID.
ketorlac (Toradol)
non-specific or traditional NSAID. oral, injectable, nasal spray, and tablets available. NSAID, but used clinically like narcotic. major role: tx for pain associated with kidney stones. inhibits platelet aggregation (like all NSAIDs), so can prolong bleeding time.
carprofen (Rimadyl)
non-specific or traditional NSAID. vet use only.
preferential COX-2 inhibitors (NSAIDs)
at normal doses, have no inhibition of COX-1. Less likely to cause GI bleed, platelet aggregation than traditional NSAIDs.
etodolac (Lodine)
preferential COX-2 inhibiting NSAID
nambumetone (Relafen)
preferential COX-2 inhibiting NSAID
meloxicam (Mobic)
preferential COX-2 inhibiting NSAID
COX-2 specific inhibitors (NSAIDs)
equally as effective as traditional NSAIDs for analgesia and anti-inflammatory effects, but less likely to cause GI complications or inhibit platelet aggregation. NO EFFECT ON PLATELETS.
celecoxib (Celebrex)
the only COX-2 specific inhibitor NSAID approved for human use in the US
Upper GI toxicity with NSAIDs
dyspepsia, ulcers, bleeding
some use PPIS, but ulceration due to systemic depletion of prostaglandins, not local effect.
risk factors for GI complications with NSAIDs
older age (>60)
history of PUD or GI bleed
high dose, multiple NSAID use
co-used with prednisone or anticoagulant
cario-renal toxicity with NSAIDs
long-term use can lead to renal papillary records, renal insufficiency, acute renal failure, and the renal injuries. Don’t use in patients with creatinine clearance <50. ALL NSAIDs INC. RISK OF HEART ATTACK AND STROKE. these effects can occur after only a week of therapy.
NSAIDs and Alzheimer’s disease
new research shows they are not beneficial for preventing dementia…actually increase risk for cognitive decline with heavy NSAID use
NSAIDs and bone regrowth
prostaglandin inhibition may lead to delayed bone healing, delayed new bone formation (delays osteoblastic formation of new bone, which require inflammation/prostaglandins for healing).
concomitant ibuprofen and aspirin use?
taking ibuprofen may interfere with anti platelet effects of low-dose aspirin
non-aspirin NSAIDs and cancer protection?
other NSAIDs match aspirin’s anti-cancer effects, especially for colorectal cancer (greatest reduction in COX2 selective inhibitors–Celebrex).