Classes and Mechanisms of Analgesics Detailed
Classes and Mechanisms of Analgesics Detailed
Analgesics
A Comprehensive and Detailed
Overview
Introduction
• Analgesics, or painkillers, are drugs used to
relieve pain by acting on the peripheral or
central nervous system. They are essential in
managing acute and chronic pain and are
classified into different types based on their
mechanisms of action and therapeutic
indications.
Non-Opioid Analgesics
• Mechanism: Primarily inhibit cyclooxygenase (COX) enzymes,
reducing prostaglandin synthesis to alleviate pain and
inflammation.
• Examples:
• - **Paracetamol (Acetaminophen):** Acts on the central
nervous system, used for mild to moderate pain and fever.
• - **NSAIDs:** Block COX-1 and COX-2 enzymes, used for
inflammatory conditions, musculoskeletal pain, and arthritis.
• - Common NSAIDs: Ibuprofen, Aspirin, Naproxen, Diclofenac.
• - Selective COX-2 inhibitors: Celecoxib (reduced GI side
effects).
Opioid Analgesics
• Mechanism: Bind to opioid receptors (mu, kappa, delta) in the
central and peripheral nervous system, altering pain
perception.
• Examples:
• - **Weak opioids:** Codeine, Tramadol (used for moderate
pain).
• - **Strong opioids:** Morphine, Fentanyl, Oxycodone (for
severe pain).
• - **Partial agonists:** Buprenorphine (lower abuse potential).
• Applications: Post-surgical pain, cancer pain, end-of-life care.
• Side effects: Respiratory depression, constipation,
dependence.
Adjuvant Analgesics
• Mechanism: Drugs used primarily for other conditions but with pain-
relieving properties, especially in neuropathic pain.
• Examples:
• - **Antidepressants:**
• - Tricyclics (e.g., Amitriptyline): Enhance serotonin and norepinephrine
levels.
• - SNRIs (e.g., Duloxetine): Effective in diabetic neuropathy and
fibromyalgia.
• - **Anticonvulsants:**
• - Gabapentin and Pregabalin: Stabilize nerve membranes, used in
neuropathic pain.
• - **Corticosteroids:**
• - Dexamethasone: Reduces inflammation and nerve
compression pain.
Local Anesthetics
• Mechanism: Block sodium channels in nerve cells,
preventing the conduction of pain signals.
• Examples:
• - Lidocaine: Topical or injectable.
• - Bupivacaine: Long-acting for surgical anesthesia.
Other Analgesics
• - **Cannabinoids:**
• - THC and CBD act on endocannabinoid
receptors, useful in chronic pain and spasticity.
• - **Ketamine:**
• - NMDA receptor antagonist with strong
analgesic and dissociative effects, used in
severe pain and palliative care.
Mechanisms of Analgesics
• - Inhibition of prostaglandin synthesis
(Paracetamol, NSAIDs).
• - Opioid receptor activation (Opioids).
• - Modulation of neural activity
(Antidepressants, Anticonvulsants).
• - Sodium channel blockade (Local anesthetics).
• - Reduction of inflammation (NSAIDs,
Corticosteroids).
• - NMDA receptor antagonism (Ketamine).
Clinical Applications
• - **Mild Pain:** Paracetamol, NSAIDs (e.g.,
headaches, sprains).
• - **Moderate Pain:** Weak opioids ± NSAIDs (e.g.,
post-operative pain).
• - **Severe Pain:** Strong opioids ± adjuvants (e.g.,
cancer pain).
• - **Neuropathic Pain:** Antidepressants,
anticonvulsants (e.g., diabetic neuropathy).
• - **Procedural Pain:** Local anesthetics, Ketamine
(e.g., dental procedures, surgeries).
Conclusion
• Analgesics are vital in pain management, with
different classes targeting specific mechanisms
and conditions. A comprehensive
understanding ensures effective and safe pain
relief while minimizing side effects.