PATIENT-SPECIFIC PAIN CONTROL
©kbaker 2011
I.
NONSTEROIDAL ANTI-INFLAMMATORY DRUGS (Non-acetylated)
A. NSAIDS APPROVED FOR ACUTE PAIN (NON-ACETYLATED)
NSAID
ROLE
in
Tp
(hr)
t 1/2
(hr)
ANALGESIC
Onset (hr) Duration (hr)
P
P
P,I
P,I
P,I
P,I
1-2
1.5
1-2
.5-2
2-4
1-2
1-2
2-3
5.7
1.8-2.
2-4
12-15
12-13
12-13
1
2
.5
1
1
1
1
4-6
6-7
4-6
6-7
up to 7
up to 7
up to 7
P,I
P,I
P
P
1-2
2-3
1-2
.5-1
1-2
1-2
7.3
3.8-6
.5
1
.5
.5
4-6
4-6
4-12
6-8
-
2-4
2-4
1
P,I
2-3
8-12
3
11
USUAL ADULT DOSE
(mg)
Therapy
*
PROPRIONIC ACIDS
fenoprofen (Nalfon,G)
flurbiprofen (Ansaid G)
ibuprofen (Motrin,G,otc)
ketoprofen (Orudis,OTC,G)
naproxen(Naprosyn,G)
naproxen Na (Anaprox,DS,G)
naproxen Na (Aleve – OTC,G)
ACETIC ACIDS
diclofenac K(Cataflam)
diclofenac Na (Voltaren,G)
etodolac (Lodine,G)
ketorolac (Toradol oral,G)
FENAMATE
mefenamic acid (Ponstel)
SALICYLATE
diflunisal (Dolobid,G)
COX-2 SELECTIVE
Celecoxib (Celebrex)
I
200-400 q4-6h
50-100 q4-6h
400-600 q4-6h
50 q6-8h
500 stat, then 250 q6-8h
550 stat, then 275 q6-8h
440 stat, then 220 q 8-12h
MAX.
DAILY
DOSE
(mg)
3200
300
3200/1200
300/75
1500
1650
660
100 stat, then 50 q6-8h
50 q6h
200-400 q6-8h
20 stat, then 10 q4-6h
200
200
1200
40
6
500 stat, then 250 q6h
1000
1
8
1000 stat, then 500 q8h
1500
2
up to 24h
100-200mg 1d-bid
400
*P=pain relief, I=inflammation reduction
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B. CLINICAL APPLICATIONS:
1.
NSAIDS VS NARCOTICS
ADVANTAGES OF PRESCRIBING NSAIDS
no sedation, constipation or respiratory depression
reduced swelling and trismus
no central nausea and vomiting side effects
no potential for abuse or habituation
2.
DISADVANTAGES OF NSAIDS
GI irritation is common
no adult liquid preps are available
patient expectations are not fufilled
no activity limitations or sedation
possible increased risk of blood clots
GENERAL PRESCRIBING GUIDELINES
a) NSAIDS can be mixed with narcotics +/or acetaminophen for additional effects, not synergistic
b) AVOID NSAID + NSAID combinations:
- take medication history, including OTC agents
- no therapeutic advantage, deleterious effects on GI tract, platelets
c) NSAID failure - try switching chemical classes
-acetic acid derivatives are structurally different so switch from one to another to improve resp.
3.
PATIENT-SPECIFIC FACTORS
ASPIRIN TRIAD
ASTHMA
ELDERLY
GASTRITIS, ALCOHOLISM
LIVER DISEASE
HIATAL HERNIA
PUD
POST-OP PAIN
RENAL DISEASE
MAJOR SURGERY
WARFARIN THERAPY
Asthma, chronic urticaria, nasal polyps = sensitivity triad.
Avoid NSAIDS if one triggers asthma, avoid COX-2s
Choose NSAID with short t ½ to avoid accumulation
Use cytoprotective agent prophylaxis, COX-2s are better
Avoid diclofenac and piroxicam (Feldene)
AVOID ASPIRIN, caution with any NSAID, COX-2s are better
Caution with any agent, may need prophylaxis, COX-2s are better
Ketorolac very effective if substance abuse history
Caution, diflunisal may be best NSAID, COX-2s NO BETTER
D/C ASA or Feldene 1 week prior, D/C other NSAIDS 24 hours prior, COX-2
Agents DO NOT increase bleeding risk and don’t have to be D/C’d.
AVOID NSAID THERAPY. COX-2’s increase bleeding due to a drug intx.
C. INDIVIDUAL AGENTS
1.
IBUPROFEN (Motrin, g)
- Many dosage forms: 100mg caplet, 50 & 100mg chewable tablets, 100mg/5ml susp, gel caps
- still the best first line agent due to good safety profile and reliable efficacy in acute pain
- 800mg q 4 hours can be given initially, no analgesic value in doses above 3200mg/day
2.
KETOROLAC (Toradol, g)



MANUFACTURER PRESCRIBING GUIDELINES LIMIT USE OF ORAL TABLETS
New prescribing guidelines in response to serious adverse events
Manufacturer not liable for adverse outcomes if practitioner uses medication outside of labeling
Emphasizes the importance of proper patient selection criteria for all NSAIDS
3. ASPIRIN (ASA)
- enteric-coated products (Ecotrin, generics) are easier on the gastric mucosa
- tablets mixed with antacids have no proven benefits over adequate water intake
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D. ADVERSE EFFECTS OF NSAIDS
5) MISCELLANEOUS GI ADVERSE EFFECTS:
ADVERSE
EFFECT
(%)
Nausea (+/-V)
Vomiting
Diarrhea
Constipation
Ab distress/pain
Dyspepsia
Anorexia
DICLOFENAC
(VOLTAREN, G)
DIFLUNISAL
(DOLOBID,G)
3-9
<1
3-9
3-9
3-9
3-9
3-9
1-3
3-9
1-3
3-9
<1
ETODOLAC
(LODINE, G)
3-9
1-3
3-9
1-3
3-9
10
<1
IBUPROFEN
(MOTRIN,G)
KETOPROFEN
(ORUDIS,G)
KETOROLAC
(TORADOL, G)
NAPROXEN
(NAPROSYN,G)
3-9
>3
>1
>3
>3
>3
11.5
>1
3-12
<3
3-9
3-9
13
12
3-9
<1
<3
<3
3-9
3-9
<3
<3
<3
3-9
E. CONTRAINDICATIONS AND WARNINGS
1. ALLERGY
5% of asthmatics are allergic to aspirin/NSAIDS
Cross-reactivity between ASA allergy and NSAID allergy
Can be lethal - anaphylactic shock
2. Sulfa Sensitivity
avoid Celebrex (celcoxib)
F. NSAID DRUG INTERACTIONS: COX-2s probably interact with all of the following:
ANTICOAGULANTS - coadministration may prolong PT, consider GI mucosal effects, additive antiplatelet effects
CYCLOSPORINE - nephrotoxicity of both agents may be increased
DIGOXIN - ibuprofen and indomethacin may increase digoxin serum levels
DIURETICS - (loops & thiazides) decreased effects - best agent is diflunisal
LITHIUM - serum Li levels may be increased - watch for toxicity – best agent is sulindac
METHOTREXATE – increased MTX serum levels with possible severe toxicity, best is celecoxib
PHENYTOIN - serum PHT levels may be increased - watch for PHT toxicity
SALICYATES - decrease plasma concentrations of NSAIDS. Avoid concurrent use since it offers NO therapeutic advantage
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II. ACETAMINOPHEN (APAP)
Maximum daily dosage:

ACUTE THERAPY: Maximum of 4 grams APAP/day:

CHRONIC THERAPY +/or ELDERLY PATIENT: Maximum of 2.6 grams APAP/day
PRODUCT
DOSAGE
ACUTE
CHRONIC
Regular Strength APAP
325mg
Extra Strength APAP
500mg
Extended Relief APAP
650mg
Toxicity risk is increased by:

Fasting during acetaminophen therapy

3 or more alcoholic drinks per day
12/day
8/day
6/day
8/day
5/day
4/day
III. TRAMADOL (Ultram, G, Ultracet - Ortho/McNeil,)
A. MECHANISM OF ACTION:
-
unique complimentary dual mechanisms
tramadol is a weak opioid receptor binder as well as an inhibitor of serotonin and norepinephrine reuptake
no inhibition of prostaglandin synthesis
not a controlled substance/ FDA pregnancy category C
B. THERAPEUTIC USE: 100MG =ASA/codeine 650/60
NEW COMBINATION: Ultracet = 37.5mg tramadol/325mg acetaminophen
C. ADVERSE REACTIONS:
Dizziness
Constipation
Sedation
26%
24%
16%
Nausea 24%
Headache 18%
D. DRUG INTERACTIONS
carbamazepine   reduced tramadol effectiveness
MAOI  possible sympathomimetic potentiation (AVOID TRAMADOL)
CYP206 inhibitor  increased tramadol levels – caution with Prozac, Paxil, Zoloft
CNS depressants  increased tramadol sedation
E. DOSAGE & ADMINISTRATION


F.
50-100mg q 4-6 hours prn pain to maximum of 400mg/day ( max dose for pts > 75 years is 300mg/day)
100mg initially is more effective for severe pain
PATIENT SELECTION CRITERIA





Patients on NSAIDs, Coumadin or oral hypoglycemics
Patients with history of histamine release with opiates or on hemodialysis
Diagnosis of neuropathic pain or history of gastrointestinal viceration
Patients with an opiate dependence hx. Should not take Ultram
Patients with severe allergic rx to CODEINE OR OTHER OPIATES should NOT take tramadol
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©kbaker, analgesia 03/09/16
IV. OPIOID ANALGESICS
A. OPIOIDS COMMONLY USED ORALLY FOR MILD TO MODERATE PAIN
OPIOID AVAILABLE
EQUIANANALG.
DOSE (MG)
PEAK
(HR)
DURATION
(HR)
COMMENTS
PRECAUTIONS
Codeine (avoid in pts. On
2D6 inhibitors* - Prozac,
Paxil, Cymbalta)
Hydrocodone
(Vicodin-ES,HP,
Lortab,Zydone,G)
Meperidine
(Demerol,G)
40-60
1.5-2
4-6
5
2
4-6
10% transformed to
morphine, not useful after
60mg q 3 hr
not useful after 10mg q 3
hr
50
1-1.5
4-5
Oxycodone
(Percodan, Percocet,
Roxicet, Tylox,G)
2.5
1
3-4
Impaired ventilation,
asthma, high intracranial
pressure
Most addictive Schedule 3
Health care providers are
at risk of abuse
Normeperidine can
accumulate with repeated
dosing – causing seizures,
avoid in pts. on MAOIs
always a C II substance as
it causes euphoria
Biotransformed to
normeperidine, a toxic
metabolite, max dose
200mg/24 hours orally
not useful after 10mg q 3
hr
*Amiodarone, Cimetidine, Desipramine, Duloxetine,Fluoxetine, Paroxetine, Propafenone, Quinidine, Ritonavir
B. CLINICAL USE OF NARCOTIC ANALGESICS
1. POTENCY ESCALATION
PATIENT CAUTIONS/INSTRUCTIONS
Rx: Codeine 30mg w/APAP 300mg (Tylenol #3, G)
Disp: #15
Sig: 1-2 tabs q 3-4 hrs prn pain. Take with food/milk
Maximum: 14/24 hours
Rx: Hydrocodone 5mg w/APAP 500mg (Vicodin, G)
Disp: #15 (10mg of Hy = 80mg of Codeine)
Sig: 1-2 tabs q 4-6 hrs prn pain. Take with food/milk
- if vestibular or GI problems, try 1/2 dose with
1/2 dosing interval
- combine with NSAID (Motrin 800mg q6-8h prn)
to provide SYNERGISTIC pain relief & for sleep
- consider APAP content of RX when
recommending supplemental APAP
-Zydone is 400mg APAP with 5,7.5,or10mg HC
Rx: Oxycodone 5mg w/APAP 500mg (Tylox, G)
- may take with additional APAP
Disp: #15 (10mg of Ox = 160mg of Codeine)
- take with food/milk
Sig: 1 cap q 4-6 hrs prn pain. Take with food/milk
- drowsiness, EtOH intensifies effect
Maximum: 8/24 hours
- avoid activity requiring concentration or movement
NOTE: Percocet now comes in SIX combinations (2.5/325, 5/325,7.5/325,7.5/500,10/325,10/650)
C. OPIOID COMBINATIONS WITH IBUPROFEN – NOT RECOMMENDED!!
1. OXYCODONE 5MG/IBUPROFEN 400MG (COMBUNOX)
2. HYDROCODONE 7.5mg/IBUPROFEN 200mg (VICOPROFEN)
D.ALLERGIC REACTION: If allergic to one chemical category, switch to an alternative category:
[Morphinams – butorphanol]
Phenanthrenes
Morphine,codeine,oxycodone,
hydrocodone,nalbuphine,
hydromorphone
[Benzomorphans – pentazocine]
Phenylpiperidines
Meperidine, fentanyl, alfentanil,
sufentanil, remifentanil
Phenylheptylamines
Methadone
E. PSEUDO-ALLERGY
1. Symptoms
2. Less Potent Agents
3. Management
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©kbaker, analgesia 03/09/16
PEDIATRIC
DOSE
(mg/day)
AVAILABLE
PEDIATRIC
PREPARATIONS
3-7
10mg/kg q 4-6 hrs
(max 65mg/kg/day)
3
1
4-6
4-6
2-4mg/kg/day
(max 200mg/day)
Oral Solution: 48-325mg/5ml
Chewable tabs: 80 + 160mg
Rectal supp: 120,125,325,650mg
Diclofenac EC tab 25, 50, 75mg
Cataflam tab 50mg
60
2-3
4-7
10mg/kg q 8 hrs
(max 1500mg/day)
Ibuprofen (Advil, Children’s
Motrin, Medipren, Nuprin, g)
20-30
1-2
4-6
5-10mg/kg q4-6 hrs
(max 40mg/kg/day)
Ketoprofen (Orudis, Oruvail, g)
OTC-Actron, Orudis KT
30
1-2
4-6
0.5-1mg/kg q6-8 hrs
(max 300mg/day)
Naproxen (Naprosyn, g)
60
1-2
4-7
10mg/kg/day
(max 1500mg/day)
Naproxen Na (Anaprox, DS, g)
60
1-2
4-7
11mg/kg/day
(max 1650mg/day)
Narcotics
Codeine (sulfate or phosphate)
15-30
0.5-1
3-6
0.5mg/kg q4 hr
(max120mg/day)
DRUG
ONSET
(min)
PEAK
(hrs)
Non-Narcotics
Acetaminophen (Tylenol,
Tempra, Panadol, g.)
20-30
0.5-2
Diclofenac (Voltaren -Na+salt)
(Cataflam- K+salt)
120
30
Diflunisal (Dolobid, g)
DURATION
(hrs)
Tablets:250, 500mg
Hydocodone (Hydrocet, Lorcet,
Vicodin, Zydone, g)
Meperidine (Demerol, g)
15-30
15-45
0.5-1
1
4-8
0.1-0.2mg/kg q4-6h
(max= 90mg/day)
4-5
1-3mg/kg q 3-4h
(max 20mg/kg/day)
Oral Susp: 100mg/5ml
Chew tabs: 50, 100mg
Caplet:100 ,200mg
Tablets: 200,400,600,800mg
Capsules: 25,50,75mg
Ext.Release (Oruvail) 200mg
Oral Susp: 125mg/5ml
Tablets: 250,375,500mg
Tablets: 220,275, 500mg
Caplets: 220mg
Codeine PO4/promethazine
oral syrup: 10mg +6.25mg/5ml
Codeine/APAP
elixir: 12mg/120mg per 5ml
susp: 12mg/120mg/5ml
Lortab Elixir: 2.5 HC + 167
APAP/5ml
Tabs: 5/500 (Vicodin, Lorcet,g)
2.5/500 (Lortab)
7.5/500 (Lortab 7.5)
7.5/650 (Lorcet Plus)
7.5/750 (Vicodin ES,)
Tabs: 50,100mg
Oral Soln: 50mg/5ml
Mepergan Fortis: 50mg MPD/
25mg promethazine
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©kbaker, analgesia 03/09/16