1. 10/2/2024
Department of Pharmacology/ 3rd stage
1
Self care & OTC products
Non Steroidal Anti-
inflammatory Drugs (NSAIDs)
Dr. Asmaa Abdulmajeed Ahmed
Knowledge University
College of Pharmacy
Department of Pharmacy
Lecture (4)
2. Introduction
Nonsteroidal anti-inflammatory drugs
(NSAIDs) are commonly used for mild
pain symptoms.
They possess analgesic, anti-
inflammatory, and antipyretic effects.
The use of these agents is complicated
by their GI side effects and
cardiovascular risks.
Ibuprofen and naproxen are two agents
in the class that are available OTC and
found in many common cold and
headache formulations.
3. Mechanism of Action for the Drug Class
Inhibit prostaglandin synthesis by
decreasing the activity of COX
enzymes 1 and 2 non-selectively,
resulting in decreased formation of
prostaglandin precursors
associated with inflammation and
pain.
4. Members of the Drug Class In this section
Aspirin, diclofenac, ibuprofen,
indomethacin, ketorolac,
meloxicam, naproxen, ketoprofen,
mefenamic acid, piroxicam,
sulindac.
COX-2 selective inhibitors have
fewer gastrointestinal side effects,
but promote thrombosis, and some
of these agents substantially
increase the risk of heart attack,
such as rofecoxib, celecoxib,
5. Adverse Reactions for the Drug Class
Most Common
Nausea, gastritis, diarrhea,
abdominal cramps, GI ulcers,
peripheral edema, hypertension
Rare/Severe/Important
GI perforation and bleeding, renal
toxicity, acute renal failure,
angioedema, bronchoconstriction,
asthma, rash, tinnitus, hearing loss
6. Major Drug Interactions
Drugs Affecting NSAIDs
● Corticosteroids: Increased GI
side effects
● Ethanol: Increased GI irritation
NSAIDs’ Effects on Other Drugs
● ACE inhibitors and AIIRB :
Decreased antihypertensive effect;
increased risk of renal toxicity
● Anticoagulants & Antiplatelet:
Increased bleeding risk
● Beta blockers: Decreased effect
● Digoxin: Increased level
● Diuretics: Decreased diuretic
effect; increased risk of renal
toxicity
7. Contraindications for the Drug Class
History of allergic reaction to
aspirin or other NSAIDs (asthma,
urticaria),
Perioperative pain management in
the setting of CABG surgery (a
procedure used to treat coronary
artery disease)
8. Key Points for the Drug Class
■ Contraindicated in perioperative
pain management in the setting of
CABG surgery (except aspirin)
■ Increased risk for thrombosis,
stroke, and myocardial infarction
(except aspirin)
■ Increased risk of serious GI events,
including bleeding, perforation, and
ulceration (except aspirin)
● Elderly are at increased risk for GI
effects, CNS effects, and renal
toxicities
● Use caution with a history of GI
disease (bleeding or ulcers); take it
with food or use of proton pump
inhibitors or histamine-2 antagonists
may reduce the risk of GI ulcer.
● Use with caution in patients with
fluid retention, congestive heart failure,
renal insufficiency, or hypertension
9. Acetylsalicylic acid
Brand Names
Bayer, Bufferin, Ecotrin, Excedrin,
various others
Generic Name Aspirin
Dosage Forms
Enteric-coated, buffered,
chewable, and controlled-release
tablets; caplets; extended-release
capsule; gum; suppository
10. Usage
Treatment of mild to moderate pain, inflammation, and fever;
Prevention & treatment of MI, acute ischemic stroke, and transient
ischemic episodes;
Adjunctive therapy in stent implantation;
Prevention of thromboembolism in atrial fibrillation;
Management of rheumatoid arthritis, rheumatic fever, osteoarthritis,
and gout (high dose)
11. Pregnancy Category
No formal category, but it is contraindicated except for low doses.
Aspirin crosses the placenta; adverse effects have been reported, though
fetal harm has not been shown in use of low doses for necessary
treatment of certain conditions in pregnancy
Avoiding NSAIDs in pregnant women at 20 weeks or later in
pregnancy.
12. Adverse Reactions Drug Interactions
Rare/Severe/Important
Reye’s syndrome (children) Major
Most Common
Nausea, gastritis, diarrhea,
abdominal cramps, GI ulcers,
peripheral edema, hypertension
Drugs Affecting Aspirin
● Ginkgo biloba: antiplatelet effect
● Other NSAIDs: bleeding risk
Aspirin’s Effect on Other Drugs
● ACE inhibitors: Decreased
antihypertensive effect
● Anticoagulants: Increased bleeding
risk
● Ticagrelor: Decreased efficacy
with concomitant aspirin doses of
>100–150 mg daily
13. Contraindications
Hypersensitivity to salicylates or
other NSAIDs;
Patients with asthma, rhinitis, and
nasal polyps;
Do not use in children (< 16 years
of age) for viral infections
(chickenpox or flu symptoms),
with or without fever, due to a
potential association with Reye’s
syndrome
15. Usage
Acute treatment for mild to
moderate pain, dysmenorrhea,
osteoarthritis, rheumatoid arthritis,
ankylosing spondylitis,
postoperative inflammation,
migraine
Pregnancy Category
● Topical gel 3%: Category B
● Ophthalmic, topical solution,
topical patch, injection:
Category C
● Oral, topical solution, injection
≥ 30 weeks gestation: Category D
16. Contraindications
Hypersensitivity to bovine
protein (capsule formulation only)
Postoperative patients with
moderate to severe renal
impairment who are at risk for
volume depletion (injection
formulation only)
17. SELECTIVE COX-2 INHIBITOR
Celecoxib
Brand Name Celebrex
Generic Name Celecoxib
Dosage Form Capsule
Usage
Relief of the signs and symptoms
of osteoarthritis, rheumatoid
arthritis, ankylosing spondylitis,
and juvenile idiopathic arthritis
(JIA);
management of acute pain;
treatment of primary
dysmenorrhea;
acute gout
18. Uses & Dosing
● Osteoarthritis: 200 mg/day PO as a
single dose or in divided doses twice
daily
● Rheumatoid arthritis: 100–200 mg PO
twice daily
● Acute pain or primary dysmenorrhea
● Ankylosing spondylitis:
● Renal impairment: Avoid in advanced
renal disease
● Hepatic impairment: Reduce dose by
50% in moderate impairment; not
recommended in severe impairment
Pregnancy Category
Category C < 30 weeks’
Gestation and
Category D ≥ 30 weeks’
Gestation
19. Adverse Reactions
Most Common
Nausea, diarrhea, GI ulcers,
hypertension, headache, peripheral
edema
Rare/Severe/Important
GI ulcers, bleeding, and perforation;
thrombosis, MI, and stroke; acute renal
failure; erythema multiforme, Stevens–
Johnson syndrome, and toxic
epidermal necrolysis; fulminant
hepatitis and liver failure
Contraindications
Hypersensitivity to sulfonamides,
aspirin, and other NSAIDs;
perioperative pain in the setting of
coronary artery bypass graft (CABG)
surgery
20. Major Drug Interactions
Drugs Affecting Celecoxib
● Antacids: Decreased absorption of
celecoxib
● Corticosteroids: Increased GI side
effects
● Ethanol: Increased GI irritation ●
Fluconazole: Increased
concentrations of celecoxib
Celecoxib’s Effect on Other Drugs
● ACE inhibitors and angiotensin II
receptor blockers: Decreased
antihypertensive effect; increased risk
of renal toxicity
● Anticoagulants: Increased bleeding
risk
● Aspirin: Increased bleeding risk;
decreased cardioprotective effect
● Cyclosporine: Increased cyclosporine
levels
● Diuretics: Decreased effects;
increased risk of renal toxicity
● Lithium: Increased concentrations
21. Counseling Points
● Be informed about signs and
symptoms of GI bleeding
● Take with food if GI upset
occurs
● Report any abnormal swelling or
bleeding to your healthcare
provider
● It increase cardiovascular risk
(thrombosis, stroke, and
myocardial infarction)
● Celecoxib does not inhibit
platelets or prolong bleeding time
● Not recommended for use in
patients with advanced renal
disease
● Do not use in patients who
experience bronchospasm,
asthma, rhinitis, or urticaria with
NSAID or aspirin therapy
