CNS, ALC, ANXIOLYTICS, ANTDEPRESS! Flashcards
what is psychchotropic vs phychoactive
psychotropic- any substance that acts centrally
Psychoactive- substances that alter mood
neuromodulators
act upon postsynaptic cells without producing action pot but altering the post synaptic response
size of classic nts
small molecules ranging from 111-190 da
What are the amino acid neurotransmitters (excitatory and inhibitory)
excitatory- glutamate
inhibitory- GABA, glycine
what are neuropeptides
alpha and beta endorphins which are endogenous opiods
sodium/chloride/potassium conc loc
pot higher inside
sodium and choride higher outside
ach synthesis and degredation
choline is taken up by neurons and converted by choline acetyltransferase to ach
acetylcholine esterase hydroxyzes it to acycle coa and choline
how is serotonin formed
formed by hydroxylation and decarboxylation of aa tryptophan
How is serotonin degraded
degreded by monoamine oxidase isozymes into 5-HIAA
How is most excess serotonin delt with
reuptake into ppre synaptic nerve endings
What is the production of catacholamines
tyrosine->L dopa-> dopamine-> noradrenaline-> adrenaline
how are catecholamines removed from the synaptic cleft
catechol-o-methyl transferase and high affinity transporters that carry undegraged nts into the pre synaptic cytoplasm
what are the excitatory and inhibitory catecholamine receptors
D1= excitatory D2= inhibitory
what about alcohol makes it more intoxicating
lipophilicity increases with each carbon number and so does the degree of intoxication
How much of alcohol is oxidized by the liver
90%
what is the steps to alcohol biotransformation
- oxidation of ethanol into acetaldehyde by alcohol dehydrogenase
- acetaldehyde to acetate by acetaldhede dehydrogenase
- enzymes found in cytosol of hepatic cells
what order metabolism does alcohol go thru
zero order metabolism
What is the microsomal pathway used for in alcohol metabolism
during chronic ethanol consumption meos activity increases resulting in faster elimination of alcohol from blood
what is oxidation of alcohol inhibited by
disulfiram which inhibits acetyladehyde dehydrogenase
How does ethanol affect neurotransmission
Enhances the action of GABA at the GABA (a) receptor and inhibits the ability of glutamate to open cation channels (NMDA)
what does methaanol biotransformation result in and what is side effect of poisoning + antidote
slow formation of formaldyhyde and formic acid
-most characteristic side effect is visual disturbances and metabolic acidosis
Fomepizole used to inhibit ADH
What occurs during binding of GABA to benzo receptor
chloride channels open and cl flows into the cell resulting in neuronal hyperpolarization
what is the antidote for bentzos in a overdose sit
Flumaxenil is a specific antagonist at the GABA a receptor
what enzyme systems are used for benzo biotransformation
phase 1 (p450) then phase 2 after
oxazepan just goes through phase 2
what was the first antidepressent
mao inhibitor iproniazid
What is an SSRI and SNRI
SSRI= selective serotonin reuptake inhibitor
SNRI= selective noradrenelin reuptake inhibitor
what are the negative side effects of tricyclic antidepresents
anti cholinergic activity as related to brain + heart
All produce considerable blockage of muscarinic cholingeric receptors resulting in sedation + cardiotox
what is the benifit of SSRIs over TCAs
less cardiotoxic effect (ex venladxine has none)
What can the mixing of MAOIs with TCAs cause
Seritonin syndrome
- -muscle tone up
- -body temp up
- -tachycardia
- -hypertension
what can mixing ectasy and TCAs lead to
hyper and hypotension and hyper pyrexia
what are antipsychotics made to do
antagonists of the dopamine D2 recetor that exists pre and post synaptically
(side effect may be parkinsonism)
what is the drug of choice for the management of PD related psychotic reactions
Quetiapine
Adverse effects of antipsychotics (5)
- Akinesia
- Rigidity
- Tremor
- Akathisia (restlessness)
- dyskinesias (involuntary)
