Professional Documents
Culture Documents
Analgesics
Analgesics
Analgesics
Pain
What is pain ?
• A protective mechanism to warn of damage or the
presence of disease
• Part of the normal healing process
Morphine
• Extracted from opium
• Strong opioid analgesics
• Multiple pharmacologic effects
Therapeutic uses
• Analgesia- relief of pain [moderate- severe]
• Postoperative
• Cancer
• Labor & delivery
• Diarrhea
• Cough
Adverse effects
• Respiratory depression
• Constipation-Rx-methylnaltrexone
• Orthostatic hypotension-histamine-VD
• Urinary retention
• Cough suppression
• Biliary colic
• Emesis
• Elevation of intracranial pressure- by supp. resp.—CO2
• Euphoria/dysphoria
• Sedation
• Miosis
• Neurotoxicity
• Physical & psychological dependence
Meperidine
• A synthetic opioid structurally unrelated to morphine.
• Used for acute pain
• Not clinically useful in treatment of diarrhea or cough
Methadone
• A synthetic, orally effective opioid
• Equal in potency to morphine
• Induces less euphoria
• Longer duration of action
• Used as an analgesic & in controlled withdrawal of dependent
abusers from heroin and morphine
Fentanyl
• Chemically related to meperidine
• 100-fold the analgesic potency of morphine
• Used in anesthesia
• Highly lipophilic
• Rapid onset and short duration of action
• Causes papillary constriction
Heroin
• Produced by diacetylation of morphine
• A 3-fold increase in its potency
• No accepted medical use
Moderate to Strong Opioid Agonists
Codeine
• Prodrug of morphine
• Antitussive effects
• Much less potent analgesic than morphine
• But with a higher oral effectiveness
• Produces less abuse & euphoria than morphine
• Used in combination with aspirin or acetaminophen
Oxycodone
• A semisynthetic derivative of morphine.
• Orally active
• Formulated with aspirin or acetaminophen
• Used to treat moderate to severe pain
Propoxyphene
• A derivative of methadone
• A weaker analgesic than codeine
• Used in combination with acetaminophen
2. Agonist-Antagonist Opioids
Pentazocine
• Promotes analgesia by activating receptors in the
spinal cord
• Used to relieve moderate pain
• Administered either orally or parenterally
• Produces less euphoria compared to morphine.
Buprenorphine
Nalbuphine
Butorphanol
3. Pure analgesic antagonists
Naloxone
• Used to reverse coma and respiratory depression of opioid
overdose
• Rapidly displaces all receptor-bound opioid molecules
• Able to reverse the effect of a heroin overdose
Naltrexone
• Longer duration of action than naloxone
• Hepatotoxic
Nalmefene
• A parenteral opioid antagonist
• Similar actions to naloxone and naltrexone
• Longer duration of action
4. Nonopioid Centrally Acting Analgesics
1. Clonidine- α2 agonist
• blocks nerve traffic from periphery to brain in S. cord
2. Ziconotide- n-type CCBs [nociceptive afferent
neurons in s. cord]
3. Dexmedetomidine- α2 agonist
• Do not cause
• Respiratory depression
• Physical dependence
• Abuse
4. Tramadol
• Conventional/traditional NSAIDs
• Inhibit both COXs
• Large & widely used family of drugs
• Clinically used to:
1. Treat inflammatory disorders
2. Alleviate mild to moderate pain
3. Suppress fever
4. Relieve dysmenorrhea
Aspirin, ASA
Diclofenac
• For long-term use in the treatment of RA,
osteoarthritis, and ankylosing spondylitis
• Similar toxicities to other NSAIDs
Second-Generation NSAIDs
• COX2Is
• Coxibs
• Selectively inhibit COX-2
• Suppress pain & inflammation
• Little or no risk of gastric ulceration
• Increase risk of MI & stroke
• Celecoxib
• Rofecoxib
• Valdecoxib
Celecoxib