Pharm - Analgesics and Anti-inflammatories Flashcards
Full opioid agonist exemplar
Morphine
Morphine metabolism
Absorbed from GI tract, extensively metabolized during first pass Principle metabolite (90%) is inactive Morphine-6-glucuronide (~10%) is more active than morphine
Morphine indications
severe pain from trauma, MI, cancer
Full agonists effectiveness
Fentanyl»_space; morphine > codeine
Partial opioid agonist exemplar
Tramadol
Tramadol mechanism
partial mu-opioid agonist
inhibits reuptake of 5HT and NE
analgesic effect mediated by M1 metabolite
Tramadol drawbacks
M1 metabolite mediated by CYP2D6, which is highly polymorphic
like giving morphine and SNRI in unknown ratio
Tramadol side effects
Hypoglycemia, decreased seizure threshold
interacts with antidepressants
Opioid antagonists mechanism
Bind to opioid receptors and prevent conformational change needed for activation and agonist activity
Opioid antagonists exemplar
Naloxone
Naloxone indications
Opioid OD, added to oral opioid agonists to curb using IB
Non-specific COX inhibitors exemplars
ASA, ibuprofen
ASA mechanism
irreversible inhibition if COX by covalently binding to COX, remaining is competitive inhibitor
ASA CI
Children with viral infections d/t Reye syndrome
ASA adverse effects
GI irritation/ ulcers/ bleeding
Tinnitus
High doses - hyperventilation, fever, dehydration, metabolic acidosis, impairment of hemostasis
Hypersensitivity reactions uncommon but fatal