Pharmacology of Pain Flashcards
Opioids
Diversity of opioid peptides- Enkephalins, dynorphins, beta-endorphin
Peptides derived from large molecular weight precursors
–> enkephalins from proenkephalin
Peptides are targets for peptidases
Endogenous opioid systems
Proopiomelanocortin-derived
Proenkephalin-derived
Prodynorphin-derived
Opioid receptors
Mu- 1,2,3 Delta- 1,2 Kappa- 1,2,3 Nociceptin/orphanin Opioid receptors are widespread
Morphine MOA
Attaches to receptor in cell
Activation of potassium conductance and decreased calcium conductance
Ca2+ entry blocked
–> decreased excitability + decreased release of neurotransmitters
Effects mediated by main opioid receptors
Analgesia Resp. depression Pupillary constriction Reduced GI motility Sedation Euphoria Dysphoria Dependence
Types of opioid
Codeine Methadone Morphine Oxycodone Tramadol
Effects of opioids- CNS
Analgesia Resp. depression Drowsiness Euphoria Miosis Nausea + vomiting
Effects of opioids- CV system
Hypotension
Effects of opioids- GI
Delayed gastric emptying
Decreased biliary and pancreatic secretions
Other Effects of opioids
Urinary urgency
Itching
Morphine
M6G active metabolite
Heroin
High solubility compared to morphine
Dextromoramide
Active sublingually
Meptazinol
Less resp. depression
Mu 1 receptor agonist
Warnings of opioid use
Resp. depression
Toxicity
Accumulation of methadone
Accumulation of M6G if renal function impaired
Opioid tolerance
Depends on genetic background + ethnicity
Can switch opioids when patients become tolerant to particular opioid drug