CNS Flashcards
What is glutamate
Excitatory neurotransmitter in CNS
Describe the conversion of glutamine into glutamate
Glutamine is converted to glutamate presynaptically.
GLU then packaged into a vescicle and removed via exocytosis when an action potential arrives.
Then gets converted back to glutamine after binding to astrocyte
NMDA is a receptor for which neurotransmitter
Glutamate
What effect does glycine have on NMDA receptor?
It is a positive allosteric modulator. It increases the receptor’s affinity for glutamate
Ketamine and PCP are non-competitive antagonists of which receptor?
NMDA
What effect do ketamine and PCP have on the receptor?
They bind intracellularly and block ion movement through the channel
GABA is the primary — neurotransmitter in the CNS
Inhibitory
What are the 3 monoamine neurotransmitters
Dopamine, serotonin and noradrenaline
Current theory for the cause of depression is…
Reduced activity of NA and 5-HT
Goal of depression pharmacology is… and …
Prevent neurotransmitter reputable by the neuron, and to prevent enzymatic breakdown
Compare TCAs and SNRIs
Both inhibit reuptake of 5-HT and NA, but SNRIs are more specific with less off-target binding
SSRI has 2 mechanisms of action. Describe them
- slow reuptake
- slow degradation
Monoamine oxidase inhibitors bind to which receptor?
MAO-A
List positive symptoms of schizophrenia
Hallucinations, delusions, hyperactivity
List negative symptoms of schizophrenia
Withdrawn and flat mood
How did the typical schizophrenia drugs work
D2 antagonists, focussed on positive symptoms
Main ADR of typical antipsychotics?
Extra-pyramidal symptoms.
Chlorpromazine and haloperidol were examples of ….
Typical antipsychotics
Off target antagonism of muscarinic receptors leads to….
Constipation.
Opposite of sludge-bbb
Clozapine, rispridone and aripiprazole are examples of…
Atypical antipsychotics
Describe hit and run antagonism of atypical antipsychotics
Lower affinity for the D2 receptor lessens the time the drug stays bound to the receptor. This lowers risk of EPS symptoms
Purpose of 5-ht antagonism of atypical antipsychotics?
Treatment of negative symptoms
