depressants Flashcards
(18 cards)
depressants
diminishes physiological activity and cortical arousal
- act directly or indirectly on GABA
GABAA Receptor
5 subunit ionotropic receptor
- allow Cl- into neuron
- 2 binding sits for GABA
- allosteric binding sites for GABA, barbs, benzos, alcohol
barbs
synthesized from barbital synthesized from barbituric acid
- used in psychiatric hospitals
- can cause respiratory depression
- increase duration of Cl- channel opening (direct)
- dose-dependent response
types of barbs
- ultra short acting: high lipid
- short acting: medium lipid
- long acting: low lipid
benzos
librium, diazepam, PAM
- increase frequency of channel opening (indirect)
- if no GABA no effect therefore less CNS depression
- larger TI than barbs
- slower tolerance
alcohol
most used depressant (ethanol)
alcohol by volume (ABV)
grams of alcohol per 100mL of solution
proof
double ABV
issues with j-shaped curve
- health issues lead to reduced alcohol consumption
- old people drink less
- moderate drinks have healthier lifestyles
- don’t include those who have died
- poor measurement of what is heavy drinker vs. abstainer
alcohol and CNS
- GABAA: positive modulator (indirect) + direct
- glutamate antagonist
- Ca2+ channels: inhibits NT release
- increases dopamine + serotonin
- CB1
where does alcohol metabolism occur?
stomach AND liver
BAC
g of alcohol in 100mL blood
how is alcohol eliminated
zero order kinetics until all enzymes saturated, then first order
narcotics/opioids
most effective pain-relieving + most addictive
- inhalation, IV, oral
- natural (opium) + synthetic
opium wars
british trade of indian opium to china led to widespread addiction - emperor tried to ban opium
opioids mech of action
3 key receptors
- Mu, delta, kappa
- most act at Mu
- pure agonists + antagonists
- partial agonists
- mixed
addiction potential of opioids
at neural level
Mu opioid receptor binding inhibits GABA neurons which usually suppress dopamine release ∴ very rewarding
how does naloxone work
temporarily displaces opioids due to stronger receptor affinity