Pharm Review Flashcards
Most preferred NSAIDs for pts?
- Naproxen and ibuprofen
- most can be dosed w/ loading dose if needed
Diff classes of NSAIDs?
- Salicylate (acetylated)
- Salicylate (nonacetylated)
- Propionic acids
- acetic acids
- oxicams
- fenamates
- nonacidic
- selective COx 2 inhibitors
MOA of NSAIDs?
- inhibit Cox which impairs transformation of: arachadonic acid - to prostaglandins - prostacyclin and thromboxanes
- Cox 1 enzymes: regulates normal cellular processes (gastric cycytoprotection, vascular homeostasis, platelet aggregation, kidney fxn)
- Cox 2: expression of this is increased during states of inflammation, effects of Cox-2 inhibition on inflammation isn’t completely understood
Adverse effects of NSAIDs?
- GI
- Renal
- CV
- liver
- pulm
- heme
- malignancy
- derm
- healing of MSK injuries
- up to 12% of hosp admissions for adverse drug runs are NSAID related
Renal adverse rxns of NSAID use?
- renal vasoconstriction, acute renal failure, HTN, hyperkalemia, hyponatremia, edema, increased risk of Renal cell cancer
Hepatic adverse rxns of NSAIDs?
- can cause elevation of liver transaminases
- actual NSAID assoc liver injury is rare
- may be disease specific (more common in SLE and RA)
Pulm adverse rxns of NSAIDs?
- adverse events seem to be more likely to be related to nonselective COX 1/2 inhibitors and less likely w/ selective COX 2 inhibition
- bronchospasm
- pulm infiltrates w/ eosinophilia
Heme adverse rxns of NSAIDs?
- neutropenia
- antiplatelet effects due to inhibition of COX1:
for most NSAIDs - platelet fxn normalizes w/in 3 days of d/c of drug (24 hrs for ibuprofen) - but still need to continue ASA for cardioprotection if using NSAID therapy
- interaction w/ warfarin, may increase INR
- higher risk of bleeding w/ anticoag. use
CNS adverse effects of NSAIDs?
- Aseptic meningitis
- tinnitus: usually w/ salicylates but can occur w/ all NSAIDs, usually reversible upon d/c
- ## psychosis and cog impairment: more common w/ indomethacin, elderly
Skin adverse effects of NSAIDs?
- drug rash or pseudoporphyria (blistering w/ sun exposure)
- blistering skin lesions that may be potentially life threatening:
TENS
SJS
NSAIDs effects on fx healing?
- may cause non-union (approx 1%)
- may want to avoid NSAIDs for up to 90 days post fx
- data isn’t clear, more studies needed
NSAID CIs mnemonic?
- Nursing or preg
- Serious bleeding
- Allergy/asthma/angioedema
- Impaired renal fxn
- Drug (anticoag)
NSAIDs: salicylates?
- Acetylated
- ASA only one in this group
- diff from other classes by irreversible platelet inhibition for the life of the platelet
- don’t use to tx pain, just use for its CV protective effects
- other NSAIDs may dampen it’s anti-platelet effects
- usually continue chronic aspirin use if adding another NSAID for pain management
Propionic acids?
- Naproxen
- Ibuprofen
Naproxen pros, formulations and dosages?
- available OTC
- long acting
- less CV risk compared to others
- 2 formulations: naproxen base and naproxen sodium
- dose: 200 mg naproxen base = 220 mg naproxen sodium (has quicker onset of action than base)
- max daily dose: Day 1- 1250 mg naproxen base, subsequent daily doses shouldnt exceed 1000 mg naproxen base (or 1100 mg naproxen sodium)
- take q 12 hrs
- good choice for tx of acute or chronic pain if NSAID is indicated
- may give loading dose of 500 mg naproxen base or 550 mg naproxen sodium
Use of ibuprofen, dosing?
- available OTC
- short duration of effect
- alt to naproxen
- max dose: 2400 mg/day (up to 3200 mg on day 1 if loading dose used)
- may give loading dose up to 1600 mg
- usual analgesic dose is 400 mg q 4-6 hrs
Acetic acids class?
- IV ketorolac (toradol)
- Indomethacin (Indocin)
Use of Ketorolac (toradol)?
- optional loading dose: 30 mg (usually just need 15 mg)
- adjust dose based on age and wt
- tx of moderate to severe postop pain
- risk of gastropathy when used more than 5 days
- not for oral use
- don’t use for chronic pain or inflammation
- make sure pts are well hydrated and w/o sig kidney disease
Use of Indomethacin (indocin)?
- optional loading dose 75 mg
- comes in an immediate release and extended release
- max dose per day: 150 mg
- used for tx of acute gout and pericarditis mainly**
- not for chronic daily use: higher risk of GI bleed, adverse effects
- may be assoc w/ aplastic anemia
Oxicams class?
- meloxicam (mobic)
- prioxicam (feldene)
Use of Meloxicam?
- long duration of effect (qday dosing): 7.5-15 mg qday
- slow onset of action
- max daily dose: 15 mg
- relatively COX2 selective at lower total dose of 7.5 mg
Use of Piroxicam (feldene)?
- an option for tx of chronic pain and inflammation poorly responsive to other NSAIDs
- daily dose of more than 20 mg increase risk of serious GI complications
- usual daily dose is 10-20 mg once daily
Use of celecoxib (celebrex)?
- selective COX-2 inhibitor
- optional loading dose of 400 mg
- max daily: 400 mg
- usual dose is 100 mg BID or 200 mg daily
- no effect on platelet fxn
- decreased GI toxicity
- dose related renal and CV effects
- sulfa allergy - CI to celebrex use
How do you judge who needs narcotics?
- sig soft tissue swelling or ecchymosis suggests sig injury
- pain at rest
- night pain
- pain uncontrolled by NSAIDs or APAP
- anyone who has had surgery
- sometimes may just need narcotics at night
Narcotic pain relief used in ortho pain?
- codeine
- hydrocodone
- oxycodone
Use of Codeine?
- considered weak opioid
- for mild-moderate pain
- schedule III
- met. to morphine: if not properly metabolized it isn’t effective
- if metabolized too quickly = initial overdose, shorter duration of action, more SEs
- 5-10% of pts have genetic variation fo metabolism and may have only limited or no benefit from codeine
Use of hydrocodone?
- lorcet, lortab, norco, vicodin
- Schedule III
- for moderate to severe pain
- onset of action: 10-20 min
- duration: 4-8 hrs
- in combo w/ acetaminophen
Use of oxycodone?
- percocet, roxicet, endocet
- schedule II
- moderate to moderately severe pain
- onset of action: 10-30 min
- in combo w/ APAP
- avoid long acting combos for acute pain (MS contin)
Use of Naloxone?
- reverses resp depression, sedation and analgesia
- 0.04mg-0.08 mg IV push q 1 min x 2
- may need to repeat dosing as half life is short
Extended release and long acting opioid analgesics - when should these never be used?
- NEVER for acute pain
- NEVER in narcotic naive pt
Toxicities of all opioids in general?
- sedation and resp depression: drugs that act on CNS potentiate effects, EToH, sedative-hypnotics, TCAs, BZDs, MAOIs
- constipation: worse w/ sustained release morphine compared to fentanyl patch, stool softners alone are not enough (need laxative)
- decreased effectiveness of diuretics: induce release of ADH and counteracts effect of diuretics
- QT prolong
When may opioid drug levels decrease or increase?
- if used concomitantly w/ cytochrome P450 inhibitors or inducers
- inhibitors: buproprion, fluoxetine, paroxetine, cimetidine, acyclovir, duloxetine, fluoroquinolones, ketoconazole, PPIs, verapamil, diltiazem, grapefruit juice
- inducers: carbamazepine, isoniazid, tobacco, rifampin, St. John’s wort
Extended relief and long acting opioid analgesics?
- morphine sulfate ER: MS contin, kadian, Embeda, Avinza
- buprenorphine transdermal: butrans
- methadone: dolophine
- fentanyl transdermal: duragesic
- hydromorphone: Exalgo
Rules for transdermal admin?
- never cut or tear patch
- heat exposure can increase release and absorption of transdermal opioid analgesics
- application: chest, side of waist, upper arm, avoid hairy areas but if not clip the hair, rotate sites, wash site w/ water only
Use of Tramadol? MOA? Metabolism? Caution?
- not a controlled substance (schedule IV), but has high potential for physical and psych dependence
- works at mu receptors and also inhibits NE and serotonin
- effective for relief of neuropathic pain
- improved fxnl outcomes in pts w/ fibromyalgia
- may be no more effective than NSAIDs or nortryptyline for chronic pain
- extensively metabolized in the liver
- use w/ caution in elderly and w/ renal insufficiency
Skeletal muscle relaxants used?
- cylcobenzaprine (flexeril)
- tizanadine (zanaflex)
- metaxalone (skelaxin)
- diazepam (Valium)
Use of muscle relaxants?
- short course of therapy only
- most benefit is w/in 1st 1-2 wks of therapy
- very sedating w/ anticholinergic SEs
- not generally for long term use unless neuromuscular problems that cause spasticity
Risk of abuse of muscle relaxants?
- diazepam (valium) and carisoprodol (soma) should be used only briefly (few days)
- high potential for abuse
Use of muscle relaxants and NSAIDs?
- may have synergistic effect for tx of acute low back pain
- pts more likely to improve when used in combo
What offers the best pain relief?
- NSAIDs or APAP in combo w/ narcotics
How do you avoid bowel obstruction if tx w/ narcotics?
- tx w/ stool softeners and gentle stimulant laxatives prn