Study sets, textbooks, questions
Upgrade to remove ads
Intro to CNS (Pharm)
Terms in this set (55)
What 2 physical properties make it more likely for drugs to enter the CNS?
1. lipid solubility
What is the only type of movement that occurs at the BBB?
Give a rationale as to why low dose inhibition of neurons can lead to paradoxical excitation
inhibitory neurons are more sensitive to the inhibition and get blocked first at low concentrations
What is an example of CNS pharmacological antagonism?
opioids + naloxone
What are 2 conditions where a drug that affect voltage-gated sodium channels would be useful?
What happens when GABA binds to its receptor in the CNS?
receptor (chloride channel) opens and chloride enters the cell
-- result is hyper-polarization (an inhibitory response)
What are 2 examples of molecules that act at TRP channels?
TRP = transient receptor potential channels
Which class of CNS receptor is fast? Slow?
Inhibitory ionotropic channels are associated with what signaling molecule?
(BS only) What part of the brain is involved in the production of acetylcholine?
nucleus basalis of Meynert
What are 2 diseases that exhibit a loss of cholinergic CNS neurons?
What CNS disease has an overstimulation of M1 receptors? What happens as a result?
Parkinson's; loss of DA neurons = loss of ACH inhibition
-- excess M1 activity causes tremors/rigidity
List the excitatory and inhibitory metabotropic acetylcholine receptors. What ionotropic receptors are stimulated by ACH?
M1, M3 = excitatory
M2, M4 = inhibitory
nicotinic = excitatory ionotropic
List the order of substrates of catecholamine synthesis
Tyrosine -- Dopa -- DA -- NE -- Epi
What are 3 ways to terminate catecholamine activity?
2. COMT breakdown
3. MAO breakdown
What are 4 substrates for COMT?
- Levodopa (used to Tx Parkinson's)
In addition to neurons, where else will COMT be found?
-- breaks down circulating catecholamines
What is an example of a dietary amine broken down by MAO?
What can happen if a patient's MAO is not breakdown down tyramine and it is allowed to build up in the body?
-- tyramine found in beer, wine, cheese, meat
-- consider in a Pt on a MAO inhibitor
What MAO isoform is found in the liver and brain? What are its substrates?
-- catecholamines, tyramine and 5-HT
What MAO isoform is found in the brain and platelets? What are its substrates?
-- tyramine and DA
Which DA pathway is involved in control of posture and voluntary movement?
-- lost in Parkinson's disease
What DA pathway, when blocked, is associated with galactorrhea?
-- DA blocks prolactin release
Excess activity of the mesolimbic tract is associated with:
schizophrenia (positive symptoms)
Stimulation of the mesolimbic tract is associated with: (2)
Insufficient activity of the mesolimbic tract is associated with: (2)
Where are D1 receptors located on neurons? What is their overall effect?
post-synaptic; excitatory (+ adenylate cyclase)
Where are 3 locations where D2 receptors are found on neurons? What do they do at each location?
1. post-synaptic -- inhibit adenylate cyclase
2. somatodendritic -- inhibit spontaneous action potentials
3. axon terminal -- inhibit DA synthesis and release
Where are noradrenergic cell bodies located in the CNS?
What are 3 disorders characterized by dysfunction in NE neurons?
Which adrenoceptor subtype is inhibitory?
Most serotonin neurons project from what location in the CNS?
dorsal raphe nucleus
Dysfunction of serotonin signaling has been implicated in which 3 psychiatric conditions?
What is a common side effect of SSRIs? Explain why this is the case.
sexual dysfunction; serotonin in the spinal cord inhibits physiological sex responses
What is a therapeutic usage of 5-HT receptor blockers?
reduction of nausea and vomiting
Which serotonin receptor is an somatodendritic autoreceptor?
-- inhibit AP firing
Which serotonin receptor is an axon terminal autoreceptor?
-- inhibit 5-HT release
Which serotonin receptor shows excess activity in schizophrenia?
-- post-synaptic, excitatory
Which serotonin receptor is involved with nausea/vomiting at the CTZ?
What is the effect of H1 receptor stimulation in the CNS?
-- this is why First Gen anti-histamines cause drowsiness
The major inhibitory NT of the CNS
Deficit of GABA receptors have been implicated in what disorder?
What neurons release glycine? Where are these mainly found?
interneurons in the spinal cord and brainstem
Strychnine, a convulsant, is an antagonist of what receptors?
Principle fast excitatory NT in the CNS
What are 2 ionotropic glutamate receptors in the CNS?
What occurs with prolonged stimulation of AMPA or NMDA channels?
Glu excitotoxicity due to excess Ca entry
What are the 4 endogenous opioids?
Note: ALL are inhibitory
What 2 opioid receptors are drug targets?
Mu and Kappa
Contrast Mu with Kappa opioid receptors with respect to mood
Contrast Mu with Kappa opioid receptors with respect to wakefulness
Contrast Mu with Kappa opioid receptors with respect to respiratory depression
Kappa: less significant
What is the triad of opioid overdose?
- respiratory depression
What is an example of an endogenous cannabinoids?
What receptor is responsible for the effects of marijuana?
Recommended textbook explanations
Physical Science Concepts In Action
Frank, Wysession, Yancopoulos
Matta, Staley, Waterman, Wilbraham
Chemistry Matter and Change
Buthelezi, Dingrando, Hainen, Wistrom
Glencoe Physical Science
McLaughlin, Thompson, Zike
Sets found in the same folder
Drugs of Abuse
Sets with similar terms
What are the classes of Neurotransmitters?
Exam 4 Practice
Psychopharmacology Exam 2
Other sets by this creator
BRS Peds Chapter 1