Pharmacology Flashcards
After nerve injury, gaba and glycine receptor activation become paradoxically excitatory
True
Opioid activate post synaptic —- channels
K+
This allows K to leave and hyperpolarize the neuron
Opioids block these presynaptic channels
Ca2+
This reduces presynaptic release of activating neurotransmitters such as substance P
Opioids and PAG
Opioids inhibit GABA activity
Inhibition of these inhibitory neurons increases output from PAG (leading to more serotonin and NE outflow to the limbic forebrain
Opioid receptor for chemical visceral pain
Kappa
Mechanical and inflammatory opioid receptor
Delta
2D6 opioids (3)
Codeine
Oxycodone
Hydrocodone
3A4 converts these two opioids to inactive forms
Fentanyl
Methadone
Erythromycin
Azithromycin
Clarithromycin
Inhibit P450
Baclofen mechanism
GABA B
Decreased NK cell activity
Opioid receptor
Mu
Do opioids reduce testosterone and estrogen?
Yes both
Low estrogen in women can cause depressions, dysmenorrhea, osteoporosis
Quinidine
Paroxetine
Fluoxetine
Buproprion
Inhibit p450 and prevent codeine -> morphine conversion
M3G vs M6G
M6G is analgesic and acts like any other opioid
M3G produces opposite effects(hyperalgesia, myoclonus, seizures, alloys is)
Active metabolite of oxycodone
Oxymorphone
Normeperidine
Seizures in renal insufficiency
Hydromorphone can cause seizures?
Yes hydromorphone 3 glucuronide
Methadone pharmacology
NMDA antagonist
Opioid agonist
SSRI
Methadone active metabolite
None
Methadone alpha elimination
8-12 hrs and this explains the 6-8 he analgesic effect
Methadone beta elimination
30-60 hrs
Does renal insufficiency affect methadone
No
TCA + methadone dangers
Both are serotonergic
Both prolong QT
Oxymorphone potency
2-5x higher than morphine