2. Pain: its an unpleasant sensory and emotional experience
arising from actual or potential tissue damage.
Analgesic: drug that selectively relieves pain by acting in
CNS or on peripheral pain mechanism, without significantly
altering consciousness
Anti-inflammatory: drug or substance that reduces
inflammation (redness, swelling, and pain) in the body by
blocking inflammatory cytokines such as IL-1β, TNF-α, IL-6
and IL-15 and chemokines such as IL-8 and GRO-alpha
Introduction
3. 1. Non Opioid Analgesics
Nonsteroidal anti-inflammatory (NSAIDs)/Non narcotic/aspirin like
analgesics
2. Opioid Analgesics
Narcotics/Morphine like analgesics
Classification
4. • Chemically diverse but most are organic acids.
• Grouped together as these drugs have common anti-inflammatory,
analgesic (pain reducing) and antipyretic effects at higher dose.
• Do not depress CNS – no physical dependence or abuse liability.
• Weaker analgesics than Morphine- except inflammatory pain
• Primarily act on peripheral pain mechanism, and also in CNS (raise
threshold)
Introduction to NSAIDs
5. Group Mechanism of action Drugs
Cox-1 Inhibitor
• Prostaglandin (PGs)
inhibitor
• Thromboxane A2 inhibitor
Aspirin, Ketoprofen Indomethacin,
Piroxicam and Sulindac
Cox-2 inhibitor
• Prostaglandins (PGE2 &
PGI2) inhibitors, decrease
sensitivity to bradykinin,
histamine serotonin and
other pain mediators
• Pro-inflammatory factors
inhibition (IL-1, IL-2, TNF-
α and oncogenes)
Preferential Nimesulide,
Diclofenac,
Aceclofenac,
Meloxicam, Etodolac
and Nabumetone
Selective Celecoxib, Etoricoxib
and Parecoxib,
Lumiracoxib
Classification
6. • 0steoarthritis, gout and rheumatoid arthritis
• Headache, myalgia and dysmenorrhea
Anti-inflammatory and
analgesics
• Decrease PGE2 synthesis in hypothalamusAntipyretic uses
• Inhibit platelet aggregation,
• formation of thrombi
CVS
• Acne, corns, Calluses and warts
• Arthritis Cream and sports rubs
External application
Pharmacological action
7. Aspirin (acetylsalicylic acid)
• Weak organic acids
• Fast oral absorption
• After short term administration t1/2 is 3-6hr,
long term use and or toxic overdose
increase t1/2 to 15-30hr
10. Paracetamol (Acetaminophen)
• Derivative of P-aminophenol
• Inhibits COX-3 and prostaglandins biosynthesis in
CNS
• Minimal anti-inflammatory action
• Good oral absorption
• Toxicity Start at low dose (≤ 2g/day), serious hepatic
and renal toxicity seen at dose of 150mg/ kg or 10g
in adults
Antidote (overdose/toxicity)
N-acetylcysteine 150 mg/ kg
20. Fentanyl
• A potent, synthetic opioid analgesics with
a rapid onset and short duration of action.
• Strong agonist at μ receptors.
• Use in epidural anesthesia
Sufentanil, alfentanil, and
remifentanil
• Synthetic opioid agonists related to
fentanyl.
• Sufentanil is more potent than
fentanyl.
• Majorly used for there analgesic and
sedative properties.
21. Methadone
• Synthetic Opioid
• Μediated by μ receptors
• Less euphoria
• Longer duration of action
Pharmacological Actions
Equianalgesic potency compared to morphine
Control withdrawal of opioid and heroin
Anti tussive
22. Partial Agonists and Mixed Agonist-Antagonist
Buprenorphine
• Partial agonist on μ receptor
• Opioid detoxification
• Less several withdrawal
• Treatment of opioid dependence
Pentazocine
• Agonist on κ receptors, weak antagonist
on μ and δ receptors
• Relieve moderate pain
• Less euphoria compared to morphine
• in higher doses cause hallucinations,
nightmares, dysphoria, tachycardia and
dizziness
23. Nalbuphine, Butorphanol
• Mixed opioid agonist-antagonist
• Limited role in treatment of chronic pain
• Butorphanol available as nasal formulation for severe
headaches, but associated with abuse
24. Other Analgesics
Tapentadol and Tramadol
• Centrally acting analgesics, agonist to μ opioid receptor
• Manage moderate to severe pain, both acute and chronic
pain
