Medical Pharmacology

Presented by : Organized by
Haidar Muhammad Amin Macos Health
BSc, Public Health

© Business & Legal Reports, Inc. 1110

COX inhibitors
• Nonsteroidal anti-
inflammatory drugs(NSAIDS)
• Nonopioid analgesics
 Key words
 These below words are a key to understand the Pain killer
drug group.
 NSAIDS: Non steroidal anti-inflammatory drugs

 Arachidonic acid: Acid produced during inflammatory response

 COX: cyclooxygenase

 PGs: Prostaglandin

© Business & Legal Reports, Inc. 1110

Beneficial actions of NSAIDs due
to prostanoid synthesis inhibition
1. Analgesic
prevention of pain nerve ending sensitization
2. Antipyretic
connected with influence of thermoregulatory
center in the hypothalamus
3. Anti-inflammatory action

4. Antithrombotic action
in very low daily doses such as asprin
 Cyclooxygenases
• COX-1 – constitutive – prostanoids involved in
physiological processes (gastroprotective effects,
platelet activities)
• COX-2 – inducible– activity enhanced by
Proinflammatory factors and improve filtration by
kidney.
– prostanoids  inflammation, fever, pain
• COX-3 – central mechanism of analgesic and
antipyretic effect (localization: heart + CNS)
 Inflammatory stimulus
(+)
Ex
Phospholipids Phospholipase A2
In

Arachidonic acid

Cyclooxy genase (COX)

5-lipoxygenase 15-lipoxygenase Endoperoxides

Leucotrienes Lipoxins PGs TxA2

 COX inhibitors
Nonselective
NSAIDs COX-1/COX-2
inhibitors

COX-2 COX-3
inhibitors inhibitors
• Selective (coxibs) •Antipyretic
• Preferential analgesics
Shared toxicities of NSAIDs due
to prostanoid synthesis inhibition
1. Gastric mucosal damage
connected with PGE inhibition
2. Bleeding: inhibition of platelet
function (TxA2 synthesis)
3. Limitation of renal blood flow
Na+ and water retention
4. Delay / prolongation of labour
connected with PGF2α inhibition
5. Asthma and anaphylactoid reactions
connected with PGF2α inhibition
Except paracetamol,Asprin,profem,ponstan
11