ANALGESICS

REAGAN KABUKA
Bpharm, MPH
ANALGESIC
Analgesics are drugs used to relieve pain due
to multiple causes.
Classification of Analgesics;
•Non-Opioid analgesics; Used in mild to
moderate pain. E.g. Non-Steroidal Anti-
inflammatory drugs(NSAIDs) Paracetamol
•Opioid analgesics; Used in moderate to
severe pain. E.g. Morphine, Synthetic Opioids
NSAIDs and Paracetamol
NSAIDs share in common the capacity to
induce Anti-inflammatory, Analgesic and
Antipyretic effects.
Paracetamol is an Analgesic-Antipyretic with
No Anti-inflammatory action
PARACETAMOL
• Paracetamol inhibits PG synthesis in CNS resulting in
Analgesic and Antipyretic effects
• It has No Anti-inflammatory effect.
• Analgesic-Antipyretic with No Anti-inflammatory
action.
• It is given orally (500-1000mg 3 times daily) and is
metabolized in the liver.
MoA-NSAIDs
Cyclo-oxygenase(COX) enzymes:
COX enzymes produce Prostaglandin (PG) and
Thromboxane-A2 from arachidonic acid.
• COX-1 is constitutive (present normally in tissues
regulating its physiological functions). It is
responsible for forming protective PGs in GIT and
Kidney, as well as preventing premature closure of
dactus arteriosus
• COX-2 is inducible (formed during inflammation).
MoA cont..
• Acetyl Salicylic acid (Aspirin), induces irreversible
inhibition of both COX-1 and COX-2 enzymes.
• Celecoxib and Rofecoxib are selective COX-2
inhibitors.
INDICATIONS OF NSAIDS
•Rheumatic fever,
•Rheumatoid arthritis,
•Fever
•Dental pain
•Headache
•Dysmenorrhea and Postpartum pain.
•Antiplatelet (Aspirin)
Low dose Aspirin-use
•Prophylaxis against Transient Ischemic
Attacks, Myocardial infarction and
•Unstable Angina.
•Cerebrovascular accident
Aspirin Doses
• Anti-platelet effect: - 75 – 150mg/day.
• Analgesic and Antipyretic: - 300 mg, 1-2 tablets
when necessary.
OTHER NSAIDS
Ibuprofen
• Effective and better tolerated (decreases incidence
of side effects)
• First choice in inflammatory joint disease.
Naprofen
• It is related to Ibuprofen, more potent with
moderate risk of side effects. It is longer acting
(given twice daily).
Other NSAIDs cont…

Piroxicam
• Potent and long acting, given once daily.
• Dose 20mg Once a day
• No accumulation in the elderly or in patients with
renal impairment.
Other NSAIDs
Diclofenac
• It is very potent and used in:
Long-term treatment of chronic inflammatory
musculoskeletal disorders e.g. Rheumatoid arthritis,
Osteoarthritis.
• An ophthalmic solution is used for post-operative
inflammation.
Other NSAIDs cont…

Indomethacin
•Potent, but due to its serious adverse effects,
has limited use
•CNS: Dizziness, confusion, ataxia, severe
headache (cerebral vasodilatation).
•Salt and water retention and hyperkalemia.
•Aplastic anemia.
 SIDE EFFECTS OF NSAIDS
Common particularly in the elderly;
• Dyspepsia,
• Nausea,
• Vomiting,
• Gastritis,
• Ulceration with risk of hemorrhage (due to direct
irritant effect on the mucosa and decreased protective
PGs).
S.Es cont…
•Renal damage (Analgesic nephropathy):
due to decreased renal vasodilator PGs.
•Hypersensitivity reactions: Skin rash,
Rhinitis, excercebates asthmatic attacks
in asthmatics patients.
•Interefers with uric acid for excretion
(Aspirin).
S.Es cont…
•Reye’s syndrome (Aspirin)
•Increased bleeding tendency: Anti-platelet
effect.
DRUG INTERERACTIONS
•Anti coagulants with Aspirin increases the
risk of GI bleeding. Binds to albumin and
displaces other bound drugs, thereby
potentiates Warfarin anticoagulant effect.
•Reduces the effect of anti hypertensive drugs
SELECTIVE COX-2 INHIBITORS

•Celecoxib and Rofecoxib are selective COX-2

inhibitors that spare COX-1
•They do not inhibit synthesis of protective
PGs in the GIT. Hence they have less GIT side
effects.
•Celecoxib is structurally related to
Sulphonamides. Therefore its use might be
associated with development of skin rash.
QUESTIONS???