Wawaimuli Arozal

Pharmacologic classes and agents

Opioid receptor agonists
NSAIDs
Tricyclic antidepressants
Anticonvulsants (Sodium channels blockers)
NMDA receptor antagonists
5HT1 receptor agonists (for acute treatment of
migraine)
Opioid receptor agonists
Primary drug class used in the acute management of
moderate to severe pain
Produce both analgesia by acting on -opioid
receptors
Sites of analgesic action: brain, brainstem, spinal cord
and primary afferent peripheral terminals
Receptors in the medullary respiratory control center,
medullary chemoreceptor zone and the
gastrointestinal tracts respiratory depression,
nausea and vomiting, and constipation
Also sedation, confusion, dizziness and euphoria
Associated with the development of tolerance
repeated use of a constant dose of a drug results in a
decreased therapeutic effect
Physical dependence abrupt cessation of treatment
withdrawal syndrome
Addiction substance abuse or drug-seeking
behaviour
Morphine, Codeine and Derivatives
Morphine is typically considered the reference opioid
Intravenous or subcutaneous administration
Treating cancer pain, severe acute pain of trauma,
burn, acute MCI
Codeine: less effective for analgesic antitussive
Higher oral bioavailability than morphine
Synthetic agonists
2 classes of synthetic -opioid receptor agonists :
phenylheptylamines (methadone) and
phenylpiperidines (fentanyl, meperidine)
Methadone: long duration of action long lasting
relief in chronic pain, prevention of signs and
symptoms of withdrawal after chronic uses of opiate
like heroin
Fentanyl: short acting, for anelgesia intra/post
operative
Meperidine: analgesic effect morphine; produced
dysphoria
Partial and mixed agonists
and agonists
Butorphanol and buprenorphine morphine-like
analgesia, less euphoric symptoms
Nalbuprine ( agonists and antagonists activity),
psychological dysphoria

Opioid receptor antagonists
Use for reverse life-threatening side effect of opioid
administration (respiratory depression)
Naloxone (parenteral), naltrexone (oral; outpatient
setting)
Nonsteroidal anti-inflammatory
drugs and nonopioid analgesics
Inhibit the activity of cyclooxigenase enzymes (COX-1
and COX-2)
Acetylsalicylic acid (aspirin)
Ibuprofene, naproxene
Diclofenac and ketorolac
Acetaminopheneb (paracetamol)
Antidepressants
Adjuvant therapy in pain management
Tricyclic antidepressants: produce analgesia by
blocking sodium channels and by increasing activity of
anti-nociceptive noradrenergic and serotonergic
projections from the brain to the spinal cord
Amitriptyline, imipramine
Dual NE and 5-HT reuptake inhibitor: venlafaxine and
duloxetine neuropathic pain and fibromyalgia
Anticonvusants
To manage symptoms of chronic pain condition on
the basis of their ability to reduce neuronal excitability
Gabapentin, pregabaline
Diabetic neuropathy, trigeminal neuralgia
Migraine Therapy
Selective 5-HT1B and 5-HT1D receptors
Reduce both sensory activation in the periphery and
nociceptive transmission in the brainstem trigeminal
nucleus diminish central sensitization
Also cause vasoconstriction
Sumatriptan