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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
NSAID
SAARD
DMARD
Analgesik
Antipiretik
Anti inflamasi

Anti Inflamasi Non Steroid


Non Steroidal Anti Inflammation Drug
Slow Acting Anti Rheumatic Drug
Disease Modifying Anti Rheumatic Drug
Obat utk mengurangi nyeri sedang-ringan
Obat utk menurunkan demam
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

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