NSAIDS
- what are the classes?
- what do you do if one class isnt working for a pt?
- what is the function of COX-1 and COX -2
Classes:
- salicylate (acetylated)
- salicylate (nonacetylated)
- proprionic acids
- acetic acids
- oxicams
- fenamates
- nonacidic
- selective cox-2 inhibitors
It is reasonable to substitute with a different class of failure of one drug. **Trial of 2 weeks at max anti-inflammatory dose before failure is considered.
COX-1: gastric cytoprotection, vascular homeostasis, platelet aggregation, kidney function)
COX-2: inhibits inflammation
NSAIDS:
- general MOA
- does IV administration of NSAIDS affect the gut?
- adverse effects?
General MOA:
-inhibits COX1 and COX 2 which impairs the tranformation of arachadonic acid to prostaglandins and thromboxanes.
Yes, I NSAIDS still have an effect on the gastric stuff, high incidence of gastritis
Adverse Effects:
- GI
- Renal
- CV
- Liver
- Pulmonary
- Hematologic
- Malignancy
- Dermatologic
- Healing of MSK injuries
Describe the effects of NSAIDS on:
- renal
- hepatic
- pulmonary
- heme
- CNS
- skin
- fx healing
Renal:
-acute renal failure, hypertension, hyperkalemia, edema, renal vasoconstriction
Hepatic:
-elevation of liver transaminases
Pulmonary:
- bronchospasm
- pulmonary infiltrates with eosinophilia
Heme:
- neutropenia
- antiplatelet effects d/t inhibition of COX-1
- -interaction with warfarin (may increase INR)
- -higher risk of bleeding with anticoagulant use.
CNS:
- aseptic meningitis
- tinnitus (usually w/ salicylates but can occur with all NSAIDS)
- psychosis & Cognitive impairment (MC with indomethacin)
Skin:
- drug rash or pseudopophyria (blister with sun exposure)
- blistering skin lesions that may be life threatening (TENS. SJS)
Fx healing:
- may cause non-union
- AVOID NSAIDS 90 post fx
NSAIDS:
-CI
CI:
- NSAID:
- -Nursing or pregnancy
- -Serious bleeding
- -Allergy/asthma/angioedema
- -impaired renal function
- -Drug (anticoagulants)
NSAID; SALICYLATE:
- drug name in this class
- special MOA features from other NSAIDS
- use
Drug name: Aspirin
MOA:
-different from other classes by irreversible platelet inhibition for the life of the platelet.
Use:
-use for CV protective effects, dont use for pain.
NSAID: Proprionic Acids:
-Drugs in this class
Drugs:
- Naproxen*
- -aleve
- -naprosyn
- Ibuprofen*
- -advil
- -motrin
Proprionic Acid: NAPROXEN
- does this have a CV risk?
- maximum daily dose?
- indications
YES, all NSAIDS have CV risk, but this one has the lowest.
Maximum daily dose: 1250mg daily dose day 1. 1000mg subsequent daily doses.
Indications:
good choice for tx of acute or chronic pain if an NSAID is indicated.
Proprionic Acid: IBUPROFEN:
- max dose
- usual analgesic dose?
Max dose: 2400mg/day with loading dose of up to 1600mg.
analgesic dose: 400mg q 4-6hrs
NSAIDS: Acetic acids:
-medications
Meds:
- IV ketorolac (toradol)
- Indomethacin (Indocin)
Acetic Acid: TORADOL
- indications
- route of admin
Indications:
- tx of moderate to severe post op pain
- not for chronic pain/inflammation
Route: NOT for oral
Acetic Acid: INDOMETHACIN:
- max dose
- indications
- SE
Max dose: 150mg/day
Indications:
-acute gout and pericarditis
SE:
-aplastic anemia
NSAID: Oxicams:
-drugs in this class
Drugs:
- meloxicam (Mobic)
- Prioxicam (Feldene)
Oxicams: MELOXICAM
-dosing
Oxicams: PIROXICAM:
- indications
- dosing
Dosing: once daily dosing.
PIROXICAM:
- indications: chronic pain that is unresponsive to other NSAIDS
- once daily dosing.
NSAIDS: Selective Cox-2 inhibitor:
- drug
- no effect on what?
Drugs:
-celecoxib (Celebrex)
No effects on platelet function
Fracture:
- tx
- who require narcotics?
Tx:
-usually treated with APAP or NSAID, occasionally narcotics
Requirements for narcotics:
- significant soft tissue swelling, echymosis suggests significant injury.
- pain at rest
- night pain
- pain uncontrolled with NSAIDS or APAP
- anyone who had surgery
Narcotics:
-drugs
Drugs:
- codeine
- hydrocodone
- oxycodone
Narcotics: CODEINE:
- strong or weak opioid?
- indications
- DEA Schedule?
- metabolism
Weak opioid
Indications: mild/moderate pain
DEA schedule III
Metabolism: metabolized to morphine
Narcotic: HYDROCODONE:
- aka
- DEA Schedule
- indications
- strong or weak opioid?
AKA:
-lorcet, lorab, norco, vicodin
DEA: Schedule III
Indications: moderate to severe pain
MODERATE opioid
Narcotic: OXYCODONE:
- aka
- DEA Schedule
- indications
- strong or weak opioid?
AKA:
-percocet, roxicet, endocet
DEA: schedule II
Indication: moderate to severe pain
Strong opioid.
Naloxone:
-indications?
Indications: reverses respiratory depression, sedation, and analgesia
Extended release and long acting opioids:
- used in acute pain?
- medications
Extended release and long acting opioid analgesics are to never be used for acute pain or in a narcotic naive patient.
Meds:
- Morphine sulfate ER: (MS contin)
- Buprenorphine Transdermal (Butrans)
- Methadone (Dolophine)
- Fentanyl Transdermal (Duragesic)
- Hydromorphone (exalgo)
Toxicities of ALL opioids
Sedation and respiratory depression
Constipation (morphine)
Decreased effectiveness of diuretics
QT prolongation
interaction with Cytochomr P450 inhibitors or inducers. (opioid levels may increase or decrease beyond expected range when given with these drugs. (buproprion, fluoxetine, duloxetine, FQ, ketoconazol,PPI, verapamil, rifampin)
Transdermal Narcotics:
- can you cut/tear a patch?
- what are the SE of excessive heat on the patch?
- application
You should never cut or tear a patch.
heat exposure can increase release and absorption of transdermal opioid analgesics.
Application:
- chest, side of waist, upper arm.
- avoid hairy areas
- rotate sites
- wash with water only
Tramadol: -MOA -DEA schedule -indications -
MOA:
-works at Mu receptors and also inhibits NE and serotonin
DEA: schedule IV
Indications: neuropathic pain (commonly used with fibromyalgia)
