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Cox inhibitors
- NSAIDs-1st & 2nd gen
- Acetaminophen
- initial drug of choice for mild-moderate pain
- pain relief-limited
- all tx fever, all but acetaminophin < inflam.
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Cox 1
- Good- stomach lining, kidney, platelets, most other tissues
- protects stomach lining, promotes renal blood flow/function, promotes platelet aggregation
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Cox 2
- Bad-injured tissue & CNS
- promotes; inflamation, painful sensation, fever
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1st gen NSAIDs
- Aspirin, Ibprofen, Naproxen, & others
- inhibits both Cox 1 & 2
- inhibit cox 2=<inflam., pain, & fever
- inhibit cox 1= GI ulcer/ bleeding, renal failure, > bleeding
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Aspirin
- prototype
- inhibits platelet aggregation irreversibly tx/prevent HA & stroke
- stop 5-7 d prior to surg
- Reyes syndrome-associated w/viral illness, do not admin to <16yo
- ADR: GI ulcer/bleed, renal fx, salicylism (od-tinnitus), reyes, preg cat D, hypersensitive reaction
- toxicity= acute emergency-resp dep, hyper therm, dehyd, acidosis
- DD= anticoagulants, steroids, alcohol, ibuprofen
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Non-aspirin NSAIDs
- ibuprofen (advil), Indomethacin (indocin), Naproxen Sodium (alieve), Ketorolac (toradol)
- torodol- <5d use, great analgesic
- Inhibit Cox 1&2 reversibly
- benefit: anti inf, anti pyretic, analgesic
- ADR:not as bad as aspirin- gastric ulceration, bleeding, renal impairment
- *take w/ food
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Second Gen NSAID
- Celecoxib (celebrex)
- inhibits Cox 2 only: <pain & inflam.
- ADRs: <1st gen nsaids, ab pain/ dyspepsia, rarely renal tox &edema, less bleeding
- caution w/ sulfonimide allergy
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Acetaminophen
- inhibits cox 1&2 but only in CNS (not peripheral tissue)
- mild-moderate pain relief not inflam reducer
- 1st choice in osteoarthritis, can admin to kids
- ADR- severe liver dmg w/ OD
- DD- alcohol, lrg dose warfarin (>inr)
- OD= >4000 mg/24hr tx=acetylcysteine (mucomist/acetadote) 17 dose liquid, rotten egg (removes toxic metabolite)
- Nomogram- helps determine how much taken but must know time of admin
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Opioids
- opioid- any drug w/ similar action to morphine
- opiate- drugs derrived from opium (poppy)
- narcotics- opioids
- opioid receptors- mu, kappa, delta
- Agonist- stimulates mu (euphoria)
- morphine, methadone
- Agonist/ Antagonist- stimulates Kappa relieves pain/ blocks mu: no euphoria/ sedation, <dependency
- butorphanol (stadol), nalbuphine (nubain)
- Antagonist-block access of agonist to mu receptor. antidote to morphine
- naloxone (narcan)
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Morphine Sulfate
- prototype: agonist @ mu- moderate-severe p
- schedule II- abuse potential
- ADR: resp distress, constipation, N/V
- DD: alcohol, barb, benz, <BP, agonist-antagonist opioids
- toxicity: coma, resp dep, pinpoint pupils
- OD: Narcan
- Monitor: RR, BP, pulse (get baseline)
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Other strong opioid agonists
- Fentanyl- patch (100x more powerful than morphine)
- Meperidine (demerol)- caution in renal impairment
- Methadone (Dolophine)- tx heroin addiction
- hydromorphine (dilaudid)- 7x more powerful than morphine
- Heroin- illegal in US (cat I)
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Moderate to strong opioid agonist
- Hydrocodone (vicodin, lortab)- sch 3 available only in combo w/ ASA, acetaminophine, ibprofen
- Oxycodone (oxycontin, percocet, percodin)- sch 2 available alone or in combo
- Codeine (robitussin AC, Tylenol #3)
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Drugs for muscle spasm (relaxants)
- mechanism-sedation (not direct relaxation of muscle)
- use-spasm, injury, <pain/ tenderness, >ROM
- ADR-sedation
- Ex)Cycobenzaprine (flexeril), Carisoprodol (Soma), Metaxalone (skelaxin), Benzodiazepines-Diazepam (valium)
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