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76 Cards in this Set
- Front
- Back
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Treatment of Pain and Inflammation |
Non-pharmacologic Analgesics - opioids (narcotics) - nonopioids * acetaminophen * aspirin * NSAIDs Anti-inflammatory agents - aspirin - NSAIDs - glucocorticoids |
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Opioids |
Alter pain perception Used in moderate-severe pain Indicated in: - acute pain (post surgery, trauma) - chronic pain (CA, neuropathy, etc) |
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Common Opioids |
- morphine (used for >100yrs) - codeine - hydrocodone (Vicodin) - oxycodone (OxyContin) - meperidine (Demerol) - fentanyl (Duragesic) patch - fentanyl (Actiq) lollipop - propoxyphene (Darvon) |
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2 Schedule Opioid Drugs |
- morphine - fentanyl (Duragesic) patch - fentanyl (Actiq) lollipop |
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3 Schedule Opioid Drugs |
- codeine |
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5 Schedule Opioid Drugs |
- hydrocodone - oxycodone (OxyContin) - meperidine (Demerol) - propoxyphene (Darvon) - methadone |
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Side Effects of Opioids |
- sedation - mood changes - confusion - respiratory depression (esp. if pulm system is compromised) - orthostatic hypotension (increased risk of backward falls) - nausea/vomiting - constipation - tolerance & dependence
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Non-opioid Analgesics : Tylenol |
For mild to moderate pain Tylenol - analgesic - antipyretic (fever reduction) |
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Non-opioid Analgesics : Aspirin & NSAIDs |
For mild to moderate pain Aspirin & NSAIDs - analgesic - antipyretic - anticoagulant - anti-inflammatory
Take baby aspirin for anticoagulation effect for those as risk for cardiac problems |
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Acetaminophen (APAP) Tylenol etc Relationship to NSAIDs |
Analgesic properties equal to NSAIDs No gastric irritation w/ Tylenol No anti-inflammatory effect or anticoagulant effect Tylenol overdose: liver toxicity - 15g can be hepatotoxic (kill you) - esp if liver is already compromised (alcohol) |
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Relationship of Tylenol to NSAIDs cont... |
MOA - central analgesic Dosing - 325-650mg; OA - up to 1gm QID (4x per day max) Cheap, available as OTC and relatively safe Watch out for patients with other hepatic disorders! |
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Acetaminophen + Opioids |
Hydrocodone + APAP - Vicoden, Lortab, Lorcet Oxycodone + APAP - Percocet Propoxyphene (Darvon) + APAP - Darvocet Tramadol (Ultram) + APAP - Ultracet |
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Aspirin |
Prototype for NSAIDs Aspirin = acetylsalicylic acid = ASA Used clinically for a century (bark of willow tree) Some patients disrespect Aspirin - old drug - inexpensive - readily available without prescription |
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The Truth About Aspirin |
Aspirin is a very powerful, very effective drug - drug of choice for Rheumatoid Arthritis (if tolerated) - we still haven't found a drug that can do as many things as Aspirin - if it were produced today, it would likely not pass FDA |
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NSAIDs Mechanism of Action |
Prostaglandins - lipid-like compounds - produced by every cell (except RBCs) - wide range of effects * pain, fever, coagulation, inflammation, uterine contractions, protection for stomach and kidney |
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Aspirin Mechanism of Action |
Inhibits the cyclo-oxygenase pathway - prevents the conversion of arachadonic acid to Thromboxane A2 and prostaglandin PGE2 |
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Aspirin Effects at Different Doses |
- anti platelet effect = 65-81mg (irreversible) - analgesic and antipyretic effect = 325mg - anti-inflammatory effect = high doses 1-2g QID |
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Anti-platelet Effect of Aspirin |
Aspirin binds to platelets for 7-10 days - need to stop taking Aspirin for 7-10 days prior to surgery - do not want to thin your blood, b/c need clotting for the surgery |
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Adverse Effects of Aspirin |
Overdose - Aspirin intoxication - hearing loss - tinnitus (affinity for 8th cranial nerve) - confusion - headache As little as 10g can be fatal - 10g = twice the dose for anti-inflammatory response Children w/ viral symptoms should NOT take it - Reyes Syndrome = significant neurological affects, liver effects, brain swelling, death |
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Percodan |
Aspirin + oxycodone |
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The Aspirin Triad |
AKA aspirin exacerbated respiratory disease (AERD)
Chronic rhinosinustitis (complicated by nasal polyps) - inflammation of sinuses and nasal passages Severe bronchial asthma Aspirin intolerance - can vary from 5-10% w/ mild asthma, but up to 25% in severe asthmatics
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Therapeutic Effects of NSAIDs |
- analgesic - antipyretic - anticoagulant (reversible) - anti inflammatory (higher doses) - anti-colorectal cancer effect * emerging evidence for this as a protective mechanism |
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Over the Counter NSAIDs |
- ibuprofen - naproxen - ketoprofen |
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Ibuprofen |
Motrin, Advil - analgesic at lower doses - anti-inflammatory at higher doses |
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Naproxen |
Naprosyn, Aleve
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Ketoprofen |
Orudis - becoming more used |
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ibuprofen (Motrin) |
prescription NSAID |
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naproxen (Naprosyn) |
prescription NSAID
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ketoprofen (Orudis) |
prescription NSAID |
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ketorolac (Toradol) |
prescription NSAID |
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piroxicam (Feldene) |
prescription NSAID |
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meloxicam (Mobic) |
prescription NSAID |
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indomethacin (Indocin) |
prescription NSAID |
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diclofenac (Voltaren) |
prescription NSAID |
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etodolac (Lodine) |
prescription NSAID |
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salsalate (Disalcid) |
prescription NSAID |
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nabumetone (Relafen) |
prescription NSAID |
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oxaprozin (Daypro) |
prescription NSAID |
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diflunisal (Dolobid) |
prescription NSAID |
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fenoprofen (Nalfon) |
prescription NSAID |
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flurbiprofen (Ansaid) |
prescription NSAID
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mefenamic acid (Ponstel) |
prescription NSAID |
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meclofenamate (Meclomen) |
prescription NSAID |
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sulindac (Clinoril) |
prescription NSAID |
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tolmetin (Tolectin) |
prescription NSAID |
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Pyrolizine Carboxcylic Acids |
ketorolac (Toradol) |
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ketorolac (Toradol) Facts |
- used intramuscularly (glut or quad) for extremely severe pain - dispensed in the ER (acute LBP and MSK) - used short term therapy for moderate to severe pain = 5 days max - analgesic potency up to 25x greater than naproxen (good pain med) |
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Oxicams |
piroxicam (Feldene) meloxicam (Mobic) |
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piroxicam (Feldene) Facts |
- highest COX 1 specificity - highest incidence of GI disturbance - long half-life
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meloxicam (Mobic) Facts |
- COX-2 selective at lower doses |
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Indole Acetic Acids |
indomethacin (Indocin) etodolac (Lodine) sulindac (Clinoril) |
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indomethacin (Indocin) Facts |
- high incidence of side-effects - use short-term |
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etodolac (Lodine) Facts |
- COX-2 preferential |
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sulindac (Clinoril) Facts |
structurally similar to indomethacin |
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Phenylacetic Acids |
diclofenac sodium (Voltaren) salsalate (Disalcid) |
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diclofenac sodium (Voltaren) Facts |
- similar pain relief to ibuprofen - takes several days for best effect - increases liver function tests in 15% of pts * monitor liver function |
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salsalate (Disalcid) Facts |
when compared with Aspirin - less GI irritation - less platelet activity |
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Primary Problem w/ NSAIDs? |
They cause GI irritation through indirect and direct damage - esp. in the elderly |
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Cyclo-oxygenase Subtypes |
COX-1 & COX-2 - two isoforms (isoenzymes) of cycle-oxygenase |
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COX-1 |
- normally present, protect cells (particularly in stomach, kidneys & platelets) - NSAIDs that go after COX 1 cells destroy protective cells which causes GI side effects |
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COX-2 |
- produced when cells are injured - NSAIDs that target COX 2 cells are going after the cells produced in injury, sparing the COX 1 protective cells |
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COX-2 Selective Drugs Examples |
celecoxib (Celebrex) rofecoxib (Vioxx) - no longer on the market valdecoxib (Bextra) |
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COX-2 Selective Drugs |
- thought to be specific for inhibition of COX-2 - spare the protective COX-1 cells - may decrease pain and inflammation w/ less gastric irritation, less renal toxicity - more expensive |
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Side Effects of COX-2 Drugs |
- lower GI tract cramping - diarrhea |
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Why were Vioxx & Bextra Removed from the Market? |
- serious cardiovascular events (MI/stroke) - increased risk by 3.9 (esp. if taken long-term) - 12 months or more of therapy - higher risk in patients w/ established heart disease & heart failure - black box warning for heart issues but it was still given to the wrong people for too long |
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Mechanism for Vioxx and Bextra |
- balance between prostaglandins (inflammation) and thromboxane favors thrombosis |
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Preferential COX-2 Drugs |
Have more of an affinity towards them - etodolac (Lodine) - meloxicam (Mobic) - nabumetone (Relafen) Cost is between non-selective and selective agents - selective are most expensive |
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How important is known about COX 2 Drugs? |
- 0.7% 1.3% of OA and RA patients will have a serious GI complication - 103,000 hospitlizations/year - 16,500 NSAID related deaths/year - $2 billion for hospitalizations - target the high risk patient |
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Who is high risk? |
- age >60 - history of ulcers or lack of normal stomach lining - history of other ulcer-promoting meds (steroids, anticoagulants, etc) - serious concomitant diseases (CAD) AKA comorbitidies
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Relative Contraindications |
- negotiable - if they are on the mild end of the spectrum they may be able to use the drug for a short time
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Absolute Contraindications |
- non negotiable - cannot take the drug no matter what |
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Relative Contraindications for NSAIDs |
- history of peptic ulcer disease - history of renal disease - history of liver disease - history of CHF - HTN - asthma/reactive airway disease - pregnancy, nursing mothers - concurrent use of corticosteroids - concurrent use of anticoagulants - age <15 or >65 |
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Patient Education About Dosing NSAIDs |
- the analgesic doses for NSAIDs are usually less than anti-inflammatory doses - patients who don't like to take meds will break a pill in half so they will only get the analgesic effect when they really need the inflammatory effect - analgesic effects (20-30mins) are realized sooner than anti-inflammatory effects (10-21days) - patients are impatient |
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Patient Education About NSAIDs |
- NSAIDs should not be taken on an empty stomach to protect the GI tract - most patients will have to be convinced to comply w/ anti-inflammatory regimen - Tyenol is NOT the same as an NSAID |
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Aspirin VS. Other NSAIDs Summary |
Other NSAIDs are attempts by drug companies to make a better aspirin - attempt to be more efficacious - fewer side effects - better dosing schedule |
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Aspirin VS. Other NSAIDs Results |
Most are really no better, but are far more expensive - may provide better effects in some patients - probably more tolerable and better compliance - great degree of trial and error (error = non-responsive) |
