Opiates Flashcards
Dynorphin
protein made in cell body and then packaged into vesicles to move to axon terminals
binds to opiate receptors
Opiate Receptors
activation leads to inhibition of adenyl cyclase which decreases cAMP concentration
Mu/Delta: opens K channels + hyperpolarization (decreases AP generation)
Kappa: decreases Ca influx in presynaptic terminal
can counter the excitatory input and decrease signal (less pain / physiological analgesia)
Opioid Agonists
relieve pain of any source, treats dyspnea, anti-tussive, antidiarrheal, opiate addiction tx and adjunct anesthesia
Heroin, Hydromorphone, Levorphanol, Oxymorphine
Morphine
gold standard of pain management
sedative + respiratory depressant
HIGHLY addictive
oxycodone
oral + addictive (similar to morphine)
Methadone
used for opiate dependence tx because it has a less severe but longer withdrawal than morphine
less constipation/emesis
Loperimide
Antidiarrheal – selectively targets GI receptors
Merperidine
no miotic effect and weak antitussive/antidiarrheal with less withdrawal
used for dyspnea tx
Fentanyl
HIGHLY ADDICTIVE + POTENT and significant withdrawal
pain control and anesthesia
withdrawal symptoms
pupil dilation, irritable, insomnia, N/V/D, chills, flush, muscle cramps
Anxiety + cravings - 8 hours
anxiety, insomnia, GI, mydriasis, rhinorrhea, sweating - 8-24 hours
Tachycardia, Fever, Chills, Seizure, Muscle spasms, Tremor - uo to 3 days
contraindications for opioid agonists
shock, pregnancy, asthma, head injuries (ICP)
Codeine + Dextromethorphan
antitussive tx (cough meds)
Hydrocodone
partial opioid agonists that is similar to morphine
Mixed Mechanism
Tramadol: binds to opiate receptor and inhibits reuptake of 5HT and NE
used for moderate to severe pain
caution with MAOI, TCA, SSRI
Mixed Agonist + Antagonists
Depends on patient’s naive to opiates
can either be a pain medication or induce withdrawal
Nalbuphine, Butorphanol, Pentazocine
Buprenophine: not recommended if not trained with pain management
