ANALGESIC AND NSAIDS

Dr. Budhi Setiawan, M.Kes

Pharmacology
 OBJECTIVES
List the major effects of prostaglandin and
leucotriene
List important sites of synthesis and the effects of
thromboxane and prostacyclin in the vascular
system
List the currently available antagonists of
leucotrienes and prostaglandins and their targets
Explain the different effects of aspirin on
prostaglandin synthesis and on leucotriene
synthesis
 OBJECTIVES

Contrast the functions of COX-1 & COX-2

Describe the effects of Aspirin on prostaglandin
synthesis
Contrast the action and toxicity of Aspirin, the
older non selective NSAIDs & COX-2 selective
drugs
List the toxic effect of Aspirin
Describe the effects and the major toxicity of
Acetaminophen
 TERMINOLOGY
AINS Anti Inflamasi Non Steroid
NSAID Non Steroidal Anti Inflammation Drug
SAARD Slow Acting Anti Rheumatic Drug
DMARD Disease Modifying Anti Rheumatic Drug
Analgesik Obat utk mengurangi nyeri sedang-ringan
Antipiretik Obat utk menurunkan demam
Anti inflamasi Obat utk menghambat keradangan
 Pain
An unpleasant sensory and emotional
experience associated with actual or
potential tissue damage, or described in
terms of such damage.
 Eicosanoid
Klasifikasi : Prostaglandin, Prostasiklin,
Tromboksan, Leukotrien
Mekanisme Kerja : Aktifasi reseptor :
protein G Adenylyl Cyclase (c AMP) /
Phosphatidylinositol cascade ( IP3 & DAG)
 Penggunaan Klinis
Obgyn : PGE2 (Dinoprostone), PGF2,
mematangkan Cervix, PGE1 (Misoprostol)
Kontraksi uterus
Pediatry : PGE1 Patent Duktus Arteriosus
Dialysis : PGI2 (Epoprostenol) Hipertensi
Pulmoner
Ulkus Peptikum AINS : Misoprostol
Urology : PGE1 (Alprostadil) Impotensi
Ophthalmology : PGE2 (Latanoprost)
Glaucoma, Unoprostone Meningkatkan out
flow Humor Aqueous
 Antagonis Eicosanoid
Kortiko steroid
AINS
Antagonis Leukotrien : Zileuton
Lypoxygenase inhibitor, Leukotrien
receptor antagonist Zafirlukast,
Montelukast
 Steps in Pain Control
1. NSAID or acetaminophen
(Ibuprofen, Naprosyn, Tylenol)
2. Add adjuvant analgesic
(TCA, Anticonvulsant, Tramadol)
3. Add opioid analgesic to above
(codeine, hydrocodone, oxycodone)
4. Increase potency of opioid
(morphine, Fentanyl, hydromorphone)
 Medications used for chronic
pain management
Acetaminophen
NSAIDs
Adjunct medications
Tricyclic antidepressants
Anitconvulsants
Serotonin reuptake inhibitors
Muscle relaxants
 Psychotropic Drugs
Tricyclic Antidepressants
Amitryptiline, Nortryptiline
Serotonin Reuptake Inhibitors
Prozac, Zoloft
Anticonvulsant
Tegretol, Dilantin, Gabapentin

Effective for chronic nerve-related pain

Ibuprofen - Advil
Naproxen - Anaprox, Naprosyn
Diclofenac - Voltaren
Indomethacin Indocin
Piroxicam - Feldene
Metamizole - Novalgin
Mefenamic Acid - Ponstan
Ketorolac Tromethamine Toradol
Ketoprofen - Profenid
 AINS Selective COX-2
Celecoxib
Rofecoxib
Nimesulide
Meloxicam
 TOKSISITAS
Gastritis
Tinnitus
Prolonged Bleeding Time
Allergy
Reyes syndrome Aspirin
 Analgesik Lainnya :
Acetaminophen
Sejak 1893 Paracetamol
Dipakai sebagai analgesik &
antipiretik
Tidak mempunyai efek anti inflamasi
Menghambat PG di sentral
Tidak mengiritasi lambung
Dosis besar hepatotoksik
 DRUGS USED IN GOUT
Anti Inflammatory
Uricosuric Agent
Allopurinol
 DRUGS USED IN GOUT
Subclass Prototype Other Significant
Agents

Anti Inflammatory Colchicine NSAIDs :

Drugs Indomethacine,
Glucocorticoid
Uricosuric Agent Probenecid Sulfinpyrazone

Xanthine Oxidase Allopurinol

Inhibitor
 Anti Inflammatory Drugs Used for Gout
Mechanism : NSAIDs reduce prostaglandin formation,
Colchicine reduce leukocyte migration through
microtubules inhibition
Clinical use : treatment of acute gouty arthritis
Toxicity : Indomethasin renal damage & bone narrow
depression, Glucocorticoid behavioral & blood
glucose, Colchicine liver & kidney damage
 Uricosuric Agent
Mechanism : compete with uric acid
reabsorbtion in S2 segment of proximal
tubule
Clinical Use : treatment of chronic gout
(after 1-2 week)
Toxicity : attack precipitation, allergenicity
 Xanthine Oxidase Inhibitor
Mechanism : inhibit enzyme XO that
converts hypoxanthine to xanthine and uric
acid
Clinical Use : treatment of chronic gout
(after 1-2 week)
Toxicity : attack precipitation, GIT, neuritis
and vasculitis (rare)