Analgesics

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Analgesics

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Title: Analgesics

1
Analgesics
NAPLEX
PG 132
2
(No Transcript)
3
Treatment Algorithm for Pain
4
Treating Specific Types of Cancer Pain

Bone pain
NSAIDs, bisphosphonates, corticosteroids, opiates
Visceral pain
NSAIDs, opiates
Neuropathic pain
TCAs, gabapentin, carbamazepine, corticosteroids
Muscle spasms
Benzodiazepines, baclofen

5
Non Opioid Analgesics
Drug Dose Interval Renal Adjustment Hepatic Adjustment
Acetaminophen 500-1000 mg Max 4 g 4-6 hours GFR gt50 ml/min q4h, 10-50 ml/min q6h, lt10 ml/min q8h 1/2 life is increased, Can be given safely
Aspirin 500- 1000 mg Max 4 g 4-6 hours Avoid Avoid
Celecoxib 100-200 mg Max 800 mg 12 hours Avoid Decrease dose by 50
Rofecoxib (off market) 12.5 mg-25 mg Max 50 mg Daily Avoid Avoid
Valdecoxib (off market) 10-20 mg Max 40 mg Daily Avoid Avoid
PG 134
6
Non Opioid Analgesics cont
Drug Dose Interval Renal Adjustment Hepatic Adjustment
Ibuprofen 200-800 mg Max 3.2 g/day 4-6 hours Use with caution Contraindicated in renal failure No dose alterations, Kinetics minimally effected
Naproxen 550 mg initial, 250 subsequent Max 1.5g/day 6-8 hours Use with caution Reduce dose 50
Indomethacin 25 mg Max 200mg/day 8-12 hours Use with caution Avoid
Ketoralac 30 mg or 60 mg IM Max 5 days of combine treatment (IM PO) 6 hours Avoid Avoid
7
NSAID's
Propionic Acids
Carboxylic Acids
oxaprozin naproxen ibuprofen ketoprofen fenoprofen
flurbiprofen
Nonacetylated Salicylates
Salicylates
ASA
salsalate diflunisal choline
Oxicams
piroxicam meloxicam
Acetic Acids
Naphthylalkanone
sulindac etodolac indomethacin tolmetin diclofenac
ketorolac
nabumetone
Fenamates
GI Sparing Agents
meclofenamate mefenamic acid
diclofenac/misoprostol
8
Weak Opioid Analgesics
Drug Dose Interval Renal Adjustment Hepatic Adjustment
Codeine 15-60 mg Max 120 mg 4-6 hours CrCl 10-50 ml/min75 of dose, lt10 ml/min50 of dose A dosage adjustment decrease
Oxycodone w/ -acetaminophen -aspirin 5 mg Max 4 g 4-6 hours Be conservative, drug levels increase by 50 1/3 to 1/2 of usual dose, Elimination 1/2 life increase by 2.3 hours
Hydrocodone w/ -ibuprofen (7.5/200) -acetaminophen (5/500) -aspirin (5/500) 1-2 tabs Max 5 tabs 1-2 tabs Max 4 g 1-2 tabs Max 4 g 4-6 hours 4-6 hours 4-6 hours Use cautiously in mild to moderate renal failure, avoid in severe renal failure Avoid
Tramadol -acetaminophen (37.5/325) 50-100 mg Max 400mg 2 tabs Max 8 tabs 4-6 hours 4-6 hours CrCl lt 30 ml/min increase dosing interval to q12h with a max of 200 mg per day Cirrhosis 50 mg q12h Avoid
9
Weak Opioid Analgesics cont
Drug Dose Interval Renal Adjustment Hepatic Adjustment
Propoxyphene -acetaminophen -aspirin 1-2 tabs Max 4 g 1-2 tabs 4 hours 4 hours Dont give in severe renal failure, use cautiously in mild and moderate renal failure Avoid
10
Strong Opioid Analgesics
Drug Dose Interval Renal Adjustment Hepatic Adjustment
Meperidine - Binds opiate receptors 50 - 150 mg Metabolite accumulation (normeperidine) Anxiety, agitation, tremor /or seizures 3-4 hours GFR gt50 ml/min No adjustment 10-50 ml/min 75 of dose lt10 ml/min 50 of dose Decrease dose, 1/2 life is increased
Morphine (gold standard) -immediate release -IV, IM, SQ, continuous infusion -epidural -intrathecal -rectal 10-30 mg 2.5-20 mg 0.8 to 10 mg/hr Max 80 mg/hr 5mg bolus, redose 1 hr 1 to 2 mg Max 10 mg/24 hr 0.2 to 1 mg 10-20 mg Titrate to response 2-6 hours No repeat dose 4 hours GFR gt50 ml/min No adjustment 10-50 ml/min 75 of dose lt10 ml/min 50 of dose (morphine-6-glucuronide) accumulates in renal failure 1/2 life prolonged increase interval by 1.5 to 2 times
11
Strong Opioid Analgesics cont
Drug Dose Interval Renal Adjustment Hepatic Adjustment
Hydromorphone -PO, IM, IV, SQ -rectal 1-4 mg 3 mg 4-6 hours 6-8 hours Decrease dose
Oxycodone - percocet (APAP) - percodan (ASA) 5 mg May titrate to response no maximum dose 6 hours Be conservative, drug levels increase by 50 1/3 to 1/2 of usual dose, Elimination 1/2 life increase by 2.3 hours
Methadone -PO, IM, SQ -IV 2.5-10 mg Max1000 mg 0.1mg/kg 3-8 hours 4 hrs x 3 doses then 6-12 hours GFR gt50ml/min q6h 10-50 ml/min q8h lt10 ml/min q12h CrCl lt10 ml/min 50-75 dose No Change in dose mild to moderate disease, Avoid in severe liver disease
12
Strong Opioid Analgesics cont
Drug Dose Interval Renal Adjustment Hepatic Adjustment
Fentanyl -transdermal -transmucosal Parenteral Initial 25 mcg/hr Initial 200 mcg 72 hours 30 min CrCl 10-50 ml/min 75 of dose lt10 ml/min 50 of dose Unaffected by cirrhosis, effected by hepatic blood flow

Remind patients that heat can increase fentanyl
absorption. Warn against extended exposure of the
patch to heating pads, hot tubs, sunbathing, high
fever, etc.
13
Opioid Equianalgesic Dosing
Drug Oral (mg) Parenteral (mg)
Morphine 30 10
Hydromorphone 7.5 1.5
Oxycodone 20-30 10-15
Methadone 10-20 acute? 2-4 chronic 10 acute? 2-4 chronic
Levorphanol 4 acute 1 chronic 2 acute 1 chronic
Fentanyl x 0.1-0.2
Oxymorphone x 1
Meperidine 300 75
14

Morphine Analogs---table 2-28, pg.132
General properties
CNS depression
Respiratory depression
Reduce propulsive activity of the gut
Urinary retention
Toxicity causes pinpoint pupils
No maximum dose

Meperidine Analogs---See Table 2-28, pg.132
General properties
Good analgesic (parenteral)
Less CNS depression or constipation than opiates
Spasmolytic action - may be useful for pain
related to uterus, GI, bronchi, etc.
Combination with hydroxyzine or promethazine
permits 2550 dosage reduction
Principal drugs
Meperidine (Demerol)---accumulates in renal
disease, metabolite can cause siezures
Diphenoxylate atropine (Lomotil) C-V
- antidiarrhea - subtherapeutic dose of
atropine to prevent abuse

Central Analgesics
Tramadol (Ultram) oral
- binds to u-opiate receptors in the CNS -
inhibits reuptake of NE 5HT in ascending pain
pathway - CYP 450 2D6 - renal adjusted
Clonidine (Duraclon) - epidural, PO or patch for
HTN
For neuropathic pain-----See other sections

PG 133
17

Drugs for Migraine
Headache Types
- Tension, Cluster, Migraine
- Migraine is unilateral, pulsating,
throbbing, with or w/o aura,
nausea, photophobia, sonophobia
Treatments Prophylactic and Abortive
Abortive
Aspirin - analgesic, antipyretic,
anti-inflammatory, anti-platelet
Acetaminophenanalgesic, antipyretic
NSAIDs - analgesic, antipyretic,
anti-inflammatory (See Table pg. 133)
Mechanism of action
Common adverse effects GI toxicity,
hypersensitivity, renal effects

PG 133
18

Contraindications to the use of Imitrex
include
which of the following
I. uncontrolled HTN
II. use of and MAOI within the past 2 weeks
III. ischemic heart disease
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III

Contraindications to the use of Imitrex
include
which of the following
I. uncontrolled HTN
II. use of and MAOI within the past 2 weeks
III. ischemic heart disease
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III

Drugs for Migraine
Abortive - (cont.)
Dihydroergotamine (Migranal) - nasal spray dose
may be repeated after 15 min MOA blocks alpha
adrenergic causing vasoconstrition
5-HT1D Receptor Agonists - avoid in patients with
cardiovascular disease
Almotriptan (Axert)
Eletriptan (Relpax) tablets newest agent on
the market another me-too
Frovatriptan (Frova) tablets longest half
life among agents
Naratriptan (Amerge) - tablets
Rizatriptan (Maxalt) - tablets also Maxalt MLT
(oral disintegrating tab)
Sumatriptan (Imitrex) - injection, tablet,
nasal spray
Zolmitriptan (Zomig) - tablets also Zomig ZMT
(oral disintegrating tab)

PG 132
21

Drugs for Migraine
Prophylactic Therapy
- Given to patients with gt2-3 HA/month, severe
HA, ineffective
treatment
Drugs of Choice
- propranolol (Inderal) use if patient also
has HTN
- amitriptyline (Elavil) concomitant
depression
- valproate (Depakote) - concomitant seizures
Other agents
- verapamil, topiramate

PG 133
22
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23
Pathophysiology
24
Complications
Source www.arava.com
25
Rheumatoid Arthritis

Corticosteroids early, acute, not long-term
- also NSAIDs / COX-2 Inhibitors
Disease Modifying Antirheumatic Drugs (DMARDs)
liver, heme
Auranofin (Ridaura)
Aurothioglucose (Solganol)
Azathioprine (Imuran)
Cyclophosphamide (Cytoxan)
Cyclosporine (Neoral, Sandimmune)
Gold sodium thiomalate (Myochrysine)
Hydroxychloroquine (Plaquenil) retinal
toxicity Q 6 months
Methotrexate (Rheumatrex)
Leflunomide (Arava)---Preg Cat X, long
half-life, hepatotoxic
Penicillamine (Cuprimine, Depen)
Sulfasalazine (Azulfindine) orange-yellow
urine

Gold
PG 134
26

Biologic Response Modifiers
Etanercept (Enbrel) avoid with live vaccine
(soluble receptor TNF inhibitor)
Anakinra (Kineret) monitor for pulmonary
problems (IL-1 receptor antagonist)
Infliximab (Remicade) monitor for infection
(monoclonal antibody for TNF)
Adalimumab (Humira) monitor for infection
(monoclonal antibody for TNF receptor)
Abatacept (Orencia) monitor for
infection (Inhibits T-Cell (T-lymphocytes
activation by binding to CD80 and CD86 on antigen
presenting cells)
Osteoarthritis (OA)
- acetaminophen NSAIDs
- surgery knee/hip replacement
- glucosamine/chondrotin NIH study (GAIT)

PG 134
27
Joint Distribution RA Compared to OA
Rheumatoid Arthritis
Osteoarthritis
28

SLE (systemic lupus erythematosus) occurs more
frequently in
a. male African Americans
b. Asians
c. post-menopausal women
d. people of Mediterranean origin
e. young women

SLE (systemic lupus erythematosus) occurs more
frequently in
a. male African Americans
b. Asians
c. post-menopausal women
d. people of Mediterranean origin
e. young women

Patients who are life time smokers have the
greatest risk of leg pain associated with?
a. hypokalemia
b. rhabdomylosis
c. intermittent claudication
d. dopamine deficiency
e. myocardial infarction

Patients who are life time smokers have the
greatest risk of leg pain associated with?
a. hypokalemia (cramps)
b. rhabdomylosis (statins)
c. intermittent claudication (PVD)
d. dopamine deficiency (RLS)
e. myocardial infarction

Trigeminal neuralgia is treated by the use of
a. aspirin
b. carbamazepine
c. dipyridamole
d. methylprednisolone
e. thiamine

Trigeminal neuralgia is treated by the use of
a. aspirin
b. carbamazepine
c. dipyridamole
d. methylprednisolone
e. thiamine

When dispensing a prescription for Robitussin AC,
the pharmacist should attach label(s) indicating
I. May cause drowsiness
II. Shake well before using
III. Finish all of this medication
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III

When dispensing a prescription for Robitussin AC,
the pharmacist should attach label(s) indicating
I. May cause drowsiness
II. Shake well before using
III. Finish all of this medication
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III

Which of the following is/are appropriate
warning(s) for the use of Duragesic transdermal
system patches?
I. Do not cut patches before applying
II. Not intended for use in children under the
age of 12
III. Replace patch every day unless pain is
under control
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III

Which of the following is/are appropriate
warning(s) for the use of Duragesic transdermal
system patches?
I. Do not cut patches before applying
II. Not intended for use in children under the
age of 12
III. Replace patch every day unless pain is
under control
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III

The upper daily dosing regimen for naproxen is
NOT more than
a. 0.5 g
b. 1 g
c. 1.5 g
d. 2.5 g
e. 4 g

The upper daily dosing regimen for naproxen is
NOT more than
a. 0.5 g
b. 1 g (mefenamic)
c. 1.5 g (naproxen)
d. 2.5 g
e. 4 g (acetaminophen)
Ibuprofen (3.2g) Indomethacin (200mg)

Which of the following ingredients is are present
in Percodan but not in Percocet
I. Aspirin
II. Acetaminophen
III. Oxycodone
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III

Which of the following ingredients is are present
in Percodan but not in Percocet
I. Aspirin
II. Acetaminophen
III. Oxycodone
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III

42
Drugs for the Treatment of Asthma
NAPLEX
PG 142
43
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44
(No Transcript)
45
Classification
46
Drugs for the Treatment of Asthma
phosphodiesterase Adenyl cyclase cyclic AMP
(bronchodilation) elimination Sympathomimetics
Increase formation of cyclic AMP Nonselective
Ephedrine Epinephrine (Adrenalin,
Medihaler-Epi, Bronkaid, Primatene, etc.)
Ethylnorepinephrine (Bronkephrine)
PG 142
47

Drugs for the Treatment of Asthma
Selective Short-Acting Beta-2 Agonists. Provide
quick relief may cause tachycardia, tremor, etc.
Albuterol (Proventil, Ventolin, Airet, Volmax)
0.5hr peak, 4

hours
duration
Albuterol - oral sustained-release product
Pirbuterol (Maxair) Autoinhaler longer
duration 6 hrs (tertiary butyl

group)
Levalbuterol (Xopenex) active isomer of
albuterol, neb., less cardiac

side effects
Metaproterenol (Alupent, Metaprel) delayed
onset (1 hour)

prolonged effect (4 hour)
Terbutaline (Brethine, Bricanyl) delayed
onset 1 hour prolonged duration (6hr)
no-inhalation in U.S. (management of pretermed
labor)
isoproterenol (Isuprel, Medihaler-Iso)
beta-1 beta-2 activity

PG 143
48
Drugs for the Treatment of Asthma (cont.)
Long-Acting Beta-2 Agonists. For long-term
symptom control frequently used with
inhalational corticosteroids may cause
tachycardia, tremor, etc. for prophylaxis
only. Formoterol (Foradil) DPI -
capsule Salmeterol (Serevent) DPI
Diskus NOT SUITABLE AS A RESCUE
INHALER!!!!!!!!!!!!!!
PG 142
49

Drugs for the Treatment of Asthma
Xanthines
Phosphodiesterase inhibitors generally for
prophylaxis adverse effects similar to caffeine
Theophylline (Slo-Phyllin, Theolair,
Theo-Dur)----Think drug interactions, serum
levels 10-20, arryhthimogenic at high levels
Dyphylline (Lufyllin).theophylline derivative
Aminophylline (Somophyllin-CRT).anhydrous
contains 86
- 300mg theo (PO) 380mg Amino (IV)
theophylline, dihydrate 79
Oxtriphylline (Choledyl).contains 64
theophylline
Leukotriene receptor drugs
For prophylaxis may reduce need for beta-2
agonist
Zafirlukast (Accolate).leukotriene receptor
antagonist
Montelukast Sodium (Singulair).leukotriene
receptor antagonist
Zileuton (Zyflo).inhibits leukotriene
formation (5-lipoxygenase inhibitor)
monitor hepatic function, think
DIs---potent inhibitor

PG 142
50

Zyflo CR will be given BID instead of QID.
But patients will still need liver function
tests every month for the first 3 months...then
every 2 to 3 months for the rest of the first
year. 2007
Omalizumab. Save the monoclonal antibody, Xolair,
for patients with severe asthma and
allergies...who are not responding adequately to
high-dose inhaled steroids and long-acting
beta-agonists.
New NIH guidelines will improve asthma
treatment. You'll see renewed emphasis on
controlling symptoms...patient education...and
avoiding allergens.

Drugs for the Treatment of Asthma
Corticosteroids
Inhalational reduce inflammation and bronchial
reactivity may cause oral candidiasis, cough,
and other steroid effects (with prolonged use).
Prophylaxis only.
Beclomethasone dipropionate (Beclovent,
Vanceril)
Triamcinolone acetonide (Azmacort)
Flunisolide (Aerobid)
Fluticasone propionate (Flovent)
Mometasone (Asmanex Twisthaler)
Budesonide (Pulmicort) (Pulmicort Respules
only neb ICS)
Anticholinergics
Ipratropium bromide (Atrovent) bronchodilator.
Reduces secretions alternative to beta-2
agonists anticholinergic adverse effects
- combivent albuterol and ipratropium
Tiotropium (Spiriva)----long acting, dry powder
capsule for inhalation

PG 142
52

Drugs for the Treatment of Asthma
Mast cell stabilizers
Anti-inflammatory very safe for prophylaxis
only
Cromolyn sodium (Intal, Nasalcrom)
Nedocromil sodium (Tilade)
Combination products
Ipratropium bromide/albuterol sulfate (Combivent)
Salmeterol xinafoate/fluticasone propionate
(Advair Diskus)
Symbicort contains the corticosteroid budesonide
(Pulmicort)...plus the long-acting beta-agonist
formoterol (Foradil). - 2007 - 2 puffs BID

PG 143
53

Side effects of oral corticosteroids include
all of the following except
a. hyperglycemia
b. nervousness
c. fluid retention
d. HPA axis suppression
e. thrombocytopenia

Side effects of oral corticosteroids include
all of the following except
a. hyperglycemia
b. nervousness
c. fluid retention
d. HPA axis suppression
e. thrombocytopenia

Patients exhibiting Cushing syndrome should avoid
products containing
a. corticosteriods
b. iodine
c. sulfas
d. penicillins
e. salicylates

Patients exhibiting Cushing syndrome should avoid
products containing
a. corticosteriods
b. iodine
c. sulfas
d. penicillins
e. salicylates

Which of the following drugs is/are
administered by dry powder inhalation?
I. Ipratropium (atrovent of combivent)
II. Pirbuterol (MaxAir Turboinhaler)
III. Salmeterol (Diskus)
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III

Which of the following drug(s) is/are
administered by dry powder inhalation?
I. Ipratropium (atrovent of combivent)
II. Pirbuterol (MaxAir Turboinhaler)
III. Salmeterol (Diskus)
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III

All of the following drugs are available as
aerosol units EXCEPT
a. Spiriva
b. Azmacort
c. Rhinocort
d. Beconase
e. Combivent

All of the following drugs are available as
aerosol units EXCEPT
a. Spiriva
b. Azmacort
c. Rhinocort
d. Beconase
e. Combivent

61
Drugs Used to Treat Glaucoma
NAPLEX
62
Causes of Glaucoma Wide or open angle most
common, malfunction of trabecular meshwork
Narrow angle or closed angle obstruction of the
outflow of aqueous humor through the trabecular
meshwork.
PG 136
63

An instrument used to measure intraocular
pressure is a(n)
a. gonioscope
b. otoscope
c. ophthalmoscope
d. tonometer
e. barometer

An instrument used to measure intraocular
pressure is a(n)
a. gonioscope (lens to study angle of eye)
b. otoscope (instrument to examine the drum
membrane of the ear)
c. ophthalmoscope (device to study interior of
eye)
d. tonometer (device to measure intraocular
pressure)
e. barometer (device to measure the atmospheric
pressure)

Drugs for Glaucoma Treatment
Goal of Therapy reduced intraocular pressure
(IOP)
- measured by a tonometer (10-20mmhg)
- decrease rate of aqueous humor production
- increase rate of outflow (drainage) of aqueous
humor
Sympathomimetics increase outflow and decrease
production of aqueous humor
- epinephrine (Epifrin, Glaucon) discard if
color change occurs
- dipiverfrin (Propine) epinephrine prodrug
less side effects
- apraclonidine (Iopidine) alpha-2 agonist
watch for ocular allergy
- brimonidine (Alphagan) - alpha-2 agonist, more
selective

PG 136
66

Drugs for Glaucoma Treatment
Miotics (direct acting)have direct cholinergic
action causing miosis increases outflow, may
cause eye pain, burning, blurred vision less
with gel and Ocusert formulations
- acetylcholine (Miochol)
- carbachol (Isoptocarbachol)
- Pilocarpine (Isoptocarpine, Pilocar, Pilostat,
Pilopine HS, Ocusert Pilo)
Miotics (cholinesterase inhibitors)increase
cholinergic action by inhibiting cholinesterase
similar adverse effects as direct-acting miotics
- physostigmine (Eserine) may cause cataracts
- Demecarium (Humersol)
- Echothiophate (phospholine iodide)

mydriasis
PG 136
67

Drugs for Glaucoma Treatment
Beta-adrenergic blocking agents reduce
production of aqueous humor watch for possible
breathing difficulty, bradycardia, hypotension,
and CNS depression
- betaxolol (Betopic, Betoptic S) beta 1
selective
- levobetaxolol (Betaxon) beta 1 selective
- carteolol (Ocupress), levobunolol (Betagan,
AKBeta)
- metipranolol (Optipranolol),
- timolol (Timoptic, Timoptic XE) B1 B2
Prostaglandin analogs increase outflow of
aqueous humor may darken iris color and cause
thickened lashes
- latanoprost (Xalatan)
- bimatoprost (Lumigan)
- travoprost (Travatan)
- Unoprostone (Rescula) Not available in U.S.

PG 136
68

Drugs for Glaucoma Treatment
Carbonic anhydrase inhibitors suppress
production of aqueous humor watch for urinary
frequency and nephrolithiasis
- dichlorphenarnide (Daranide)
- acetazolamide (Diamox)----oral capsules, IV
Also used for mountain sickness
- methazolamide (Neptazane)
- dorzolamide (Trusopt)
- brinzolamide (Azopt)
Osmotic diuretics----given orally or IV
- glycerin (Osmoglyn) , mannitol (Osmitrol)
- urea (Ureaphil), isosorbide (Isomotic)

PG 136
69