Intro To Neuropharmacology And CNS Depressants Flashcards
What determines selectivity?
The dose
What are the biogenic amine NTs?
NE, DA, 5-HT (serotonin), histamine
What do EPSPs lead to?
APs
What is excitability?
Rate and pattern of AP gen, result of neuron’s integration over time of its many excitatory and inhibitory inputs
How can drugs depress the excitability of a neuron?
By I- a N that excites the 1st N
By exciting a N that I- the 1st N
I- directly!
How can drugs ⬆️ the excitability of a N?
By stim a N that excites the 1st N
By I- a N that i- the 1st N
Stim Directly!
What are the non selective CNS depressants?
Barbs
Non barb sed-hyps (chloral hydrate)
Ethanol
Inhalational and IV anesthetics
Long, short/int and ultra short acting barbs? Uses?
Long: phenobarbital (anticonvulsant, sed)
Short/int: pentobarbital (hyp)
Ultra short: thiopental (anesthesia)
What are most drugs that act in the CNS like?
Weak org acids or bases, good lipid solubility
The S in thiopental ⬆️ lipid solubility
Drug safety is a function of?
Slope
How’s ARAS involved?
Non selective CNS depressants reversibly I- it, ⬆️ threshold for cortical arousal
What’s disinhibition?
When drug depresses inhib N, releasing their target N from tonic inhib tone
-hyperactivity of resp reflexes
What’s the rate limiting step in Ethanol metabolism? Kinetics?
NAD regen
0 order
Drugs to treat alcohol addiction?
Disulfiram
- prevent further ethanol use
- problem if used with ethanol, acetaldehyde poisoning
Naltrexone
- long acting opioid anta
- problem if used w/ opioid ago
Func v metabolic tolerance?
Func:
Target tissue is less sensitive to the drug
Metabolic:
Less drug cuz of ⬆️ biotransformation (only w/ barbs and mixed func oxidases)
