Pharmacological Treatment Options for ___________Osteoarthritis_____________
Kun Cai, PharmD Candidate 2007
Therapeutic Class/Agents
Product
Availability
Tylenol (acetaminophen)
Generic (Brand)
Therapeutic Class/Agents
NSAIDs
Acetylated: Aspirin
Non-acetylated:
salsalate(Amgesic),
diflunisal(Dolobid)
Therapeutic Class/Agents
Therapeutic Class/Agents
Capsaicin
(arthriCare, Capsagel, Zostrix)
Glucosamine, Chondroitin
Induces release of substance P
from peripheral sensory
neurons, after repeated
application, capsicin depletes
the neuron of substance P and
prevents reaccumulation.
Glucosamine is an aminosugar that is naturally
produced in humans. It is the
substrate used in synthesis of
major structural components of
cartilage. Chondroitin sulfate
inhibits synovial enzymes
(elastase, hyaluroidase) which
Acetic Acids: diclofenac
(cataflam), etodolac (lodine),
sulindac (Clinoril),
nabumetone (Relafen)
Propionic Acids: fenoprofen
(Nalfon), Ketoprofen (Orudis),
naproxen (Naprosyn)
sulfonamide:
Celecoxib (celebrex)
Oxicams:
Meloxicam (Mobic),
piroxicam (Feldene)
Mechanism
of Action
inhibits the synthesis of
prostaglandins in the central
nervous system and
peripherally blocks pain
impulse generation; produces
antipyresis from inhibition of
hypothalamic heat-regulation
center
Kun Cai, PharmD Candidate 2007
University of Maryland School of Pharmacy
Inhibits prostaglandin
synthesis by decreasing the
activity of the enzyme,
cyclooxygenase, which results
in decreased formation of
prostaglandin precursors to
relieve pain and inflammation.
Pharmacotherapy Presentation – Pharmaceutical Care Rotation
Happy Harry’s Pharmacy Patient Care Center, Perryville, MD
may contribute to cartilage
destruction and loss of joint
function.
EFFICACY
(Indication/Use,
Clinical Data
Support)
SAFETY
(Major Drug
Interactions,
Pre-cautions,
Contraindications,
Adverse Effects,
Pregnancy Risk
Category)
comparable relief of mild to
moderate OA pain has been
documented for
acetaminophen at 2.6-4g/day
Warnings/Precautions: Limit
dose to <4g/day. May cause
severe hepatic toxicity on
acute overdose and chronic
daily dosing in adults has
resulted in liver damage in
some patients. Use with
caution in patients with
alcoholic liver disease;
consuming over 3 alcoholic
drinks/day may increase the
risk of liver damage. Use
caution in patients with known
G6PD deficiency.
Contraindications:
hypersensitivity to
acetaminophen or any
component of the formulation.
Kun Cai, PharmD Candidate 2007
University of Maryland School of Pharmacy
NSAIDs are often prescribed
for OA patients after treatment
with acetaminophen proves
ineffective or for patients with
inflammatory OA. All
NSAIDs and aspirin have
similar analgesic and antiinflamatory effects. However,
individual patient response
does differ among NSAIDs.
Cox-2 inhibitors demonstrate
similar analgesic benefits when
compared to traditional
NSAID.
To be effective, capsaicin must
be used regularly and it may
take up to 2 weeks to work. It
is well tolerated, except a
temporary burning sensation at
the site of application.
Capsaicin cream has been
shown in controlled studies to
provide pain relief in OA when
applied over affected joints.
Controlled clinical trials have
shown that chondroitin and
glucosamine are superior to
placebo in alleviating pain
from knee or hip OA. A metaanalysis has shown that both
agents had efficacy in reducing
pain and improving mobility.
Adverse effects:
GI: nausea, dyspepsia,
anorexia, abdominal pain,
flatulence, diarrhea, GI
bleeding. Cox-2 inhibitors
have decreased risk of GI
toxicity compared to
nonspecific NSAIDs.
Renal: acute renal
insufficiency, tubulointerstitial
nephrophathy, hyperkalemia
Cardiovascular: increased
cardiovascular risk with cox-2
inhibitors
Platelet Function and
Coagulation:
Aspirin – irreversible platelet
aggregation inhibition
Adverse effects:
dermatologic: itching, stinging
sensation, erythema
Local: transient burning on
application which usually
diminishes with repeated use
Contraindications:
hypersensitivity to capsicin or
any component of the
formulation
Drug interactions: minor
substrate of CYP2E1
Glucosamine and chondroitin
are marketed as dietary
supplements, neither the
products nor their purity is
adequately regulated by the
FDA.
Pregnancy category: C
Adverse effects:
Glucosamine: abdominal pain,
dizziness, nausea, loose stools,
elevation in blood glucose
Avoid in shellfish allergy
Chondroitin: no known
toxicities
Drug interactions: No
interactions have been
reported.
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Happy Harry’s Pharmacy Patient Care Center, Perryville, MD
Drug interactions: (minor)
substrate of CYP1A2, 2Ab,
2C9, 2D6, 2E1, 3A4; (weak)
inhibits CYP3A4
Pregnancy category: B
Most others – reversible
inhibition
Consider discontinuing
NSAID prior to elective
surgery (assess risk vs. benefit)
Little to no platelet effects:
Nonacetylated salicylates,
nabumetone, etodolac
COX-2 selective agents
Others: drug induced hepatitis,
hypersensitivity reaction,
drowsiness, dizziness,
headches, depression.
Contraindication:
hypersensitivity reaction, 3rd
trimester preganacy
Drug interactions:
Serious interactions include the
use of NSAIDs with lithium,
warfarin, oral hypoglyemics,
high-dose methotrexate,
antihypertensives, ACE
inhibitors, beta-blockers, and
diuretics.
Pregnancy Category: B
Pregnancy Category: C/D
(third trimester)
Therapeutic Class/Agents
Dosage &
Adults: 650-1000 mg q 6 hrs
Administration prn
(Include renal
and/or hepatic
adjustments)
Max: 4 gm/day
For chronic use: 2 gm/day
PRN dosing preferred, chronic
dosing for more severe cases
Kun Cai, PharmD Candidate 2007
University of Maryland School of Pharmacy
Therapeutic Class/Agents
Ibuprofen:
Analgesia: 200-400 mg q4-6
h, max 1200 mg
Anti-inflammatory: 400-800
mg q6-8h, max 3200 mg
Aspirin:
Analgesic/antipyretic dosing:
Therapeutic Class/Agents
Therapeutic Class/Agents
Topical: apply to affected area
at least 3-4times/day. It may
take up to 2 weeks to work.
Glucosamine 1500 mg/day PO
Chondroitin 1200 mg/day PO
Discontinue use in 3 month if
no efficacy, can take up to 4
weeks to demonstrate effect
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Happy Harry’s Pharmacy Patient Care Center, Perryville, MD
Dosage interval in renal
impairment:
CLcr 10-50 ml/min: administer
every 6 hours
CLcr< 10ml/min: administer
every 8 hours
325 to 650 mg q4h, max dose
4 gm/24 hours
Anti-inflammatory: starting
dose 2.6 to 4.5 gm/day divided
into 4-8 hour intervals
Dosing adjustment in hepatic
impairment: avoid chronic use
in hepatic impairment.
Limited, low-dose therapy is
usually well tolerated in
hepatic disease.
Monitoring
(Efficacy and
Toxicity
Parameters)
Efficacy: Reduction in pain
(VAS, 1 to 10 scale)
Range of motion for affected
joints
Improvement in QOL (SF-36)
Toxicity: liver function
Patient
Education
Take exactly as directed. Most
adverse effects are related to
excessive use. Take with food
or milk. While using this
medication, avoid or limit
alcohol to <3 drinks/day.
Maintain adequate hydration
(2-3 L/day of fluids).
Kun Cai, PharmD Candidate 2007
University of Maryland School of Pharmacy
Efficacy: pain, range of
Efficacy: : pain, range of
motion, grip strength, mobility, motion, grip strength, mobility,
ADL function
ADL function
Toxicity: skin rash, redness,
Toxicity: CBC; occult blood
itching, stinging sensation.
loss and periodic liver function
tests, inflammation, weight
gain, edema, renal function(
urine output, serum BUN and
creatinine), bruising, GI effects
(abdominal pain, bleeding,
dyspepsia), mental confusion,
disorientation
Efficacy: :pain, range of
motion, grip strength, mobility,
ADL function
Toxicity: abdominal pain,
dizziness, nausea, loose stools,
hypersensitivity reaction
While use this medication, do
not use alcohol, excessive
amounts of vitamin C or other
medication containing aspirin
or salicylate or other NSAIDs
without consulting prescriber.
Maintain adequate hydration
(2-3L/day of fluids). You may
experience nausea, vomiting,
Use with caution when you are
allergic to shell fish.
Discontinue it if there is no
improvement for 3 month.
For external use only. Wear
gloves to apply and wash
hands immediately after
application. Discontinue use if
severe burning or itching
occurs. If symptoms persit
longer than 14-28 days, contact
physician.
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Happy Harry’s Pharmacy Patient Care Center, Perryville, MD
and gastric discomfort. Stop
taking medication when you
experience bleeding (mouth,
urine, stool), skin rash, unusual
swelling of extremities, chest
pain or palpitations.
Cost
(1-month)
References
(Guidelines,
Drug Info
Sources)
(www.drugstore,com)
Tablets (Tylenol)
300mg (30): $ 7.99
500mg (30): $ 7.99
(www.drugstore,com)
Ibuprofen:
400mg (30): $ 7.99
800mg (30): $8.99
Cream (xostrix-HP): 0.075%:
$16.71
Glucosamine, Chondroitin
(500mg,400mg)
Tablet (120): $16.99
American College of Rheumatology:
Recommendations for the Medical
Management of Osteoarthritis of the
Hip and Knee
American College of Rheumatology:
Recommendations for the Medical
Management of Osteoarthritis of the
Hip and Knee
American College of Rheumatology:
Recommendations for the Medical
Management of Osteoarthritis of the
Hip and Knee
American College of Rheumatology:
Recommendations for the Medical
Management of Osteoarthritis of the
Hip and Knee
Lexi-comp
Lexi-comp
Lexi-comp
Lexi-comp
Kun Cai, PharmD Candidate 2007
University of Maryland School of Pharmacy
Pharmacotherapy Presentation – Pharmaceutical Care Rotation
Happy Harry’s Pharmacy Patient Care Center, Perryville, MD