CNS Depressants

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what's a synapse
connection allowing one neuron to talk to another neuron
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how can a synapse be modulated (4)
transmitter-gated ion channels, GPCRs, reuptake transporters, degradative enzymes
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what is GABA
amino acid
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function of GABA in brain
main inhibitory neurotransmitter
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GABA hyperpolarises neuron's which decreases what
probability of it firing an action potential
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GABA-A is
ion channel selectively permeable to Cl- ions
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GABA-B
metabotropic  2nd messenger cascade results in the opening of potassium channels  hyperpolarisation
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what do subunit combos determine
ANATOMICAL LOCATION, PHYSIOLOGY and PHARMACOLOGY of the receptor subtype.
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Where do benxodiazepines bimd?
between alpha and GABA2
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where does GABA bind
between alpha and beta
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do BZDs have agonist activity
no
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BZDs have affinity to what
GABA-A receptors
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Why are BZDs called allosteric modulators PAM)(positive negative allosteric modulator)
they can enhance or change effect when added to something but not by themselves
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BZDS cause increase in frequency of what
of channel-opening events when GABA is bound to the receptor.
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which subunits are insensitive to BZDs
a4 and a6
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Most BZDs are
short term treatment
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which BZD treats: muscle spasm, convulsions, anxiety, acute alcohol withdrawal
Diazepam
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which BZD treats: anxiety, anaesthesia premedication, convulsions
Lorazepam
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which BZD treats: convulsions, sedation and antipsychotic for confusion and restlessness in palliative care
Midazolam
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which BZD treats: short term use in anxiety
Alprazolam
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name 3 short term side effects of BZDs
memory, interact w other drugs to depress rest and cardiovascular centres in brainstem, violence
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name 3 long term side effects of BZDs
apathy, dependence, aggravate depressive, sudden withdrawal= epileptic seizures
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what's a BZD antagonist (reverse side effects of BZDs including overdose)
flumazenil
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Non-benzodiazepines allosteric modulators of GABA-A receptors are AKA
Z drugs
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Name 2 Z drugs
zolpidem and zopiclone
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Z drugs have high affinity for what subunit
a1
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Pool effect?
strong sedation, weak anxiolytic
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clinical use of Z drugs
insomnia
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MIXED GABA-A receptor Allosteric modulation AND Agonism AKA?
Barbituates
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name 2 commonly used barbiturates
thiopental and phenobarbital
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at normal conc barbiturates are what
allosteric modulators (enhance gaba)
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at high conc barbiturates are what
direct agonists on their own
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BZDs increase frequency of channel openings, but what do barbiturates increase?
duration of GABA gated chloride channel openings
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Barbituates used to induce what?
Anesthesia
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Binding site is on γ, α, β subunits of the GABA-A receptor
Also inhibits sodium ion channels
acts as a positive allosteric modulators by enhancing the effects of endogenous GABA
very potent anaesthetic drug?
Propofol
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GABA-B receptor agonist
Baclofen
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Baclofen (anti muscle spasmodic) acts on what
presynaptic terminals
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GAT (GABA transporter) decreases GABAergic synaptic transmission and therefore neuronal inhibition, what drug blocks the functioning of this transporter
Tiagabine
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The enzyme GABA Transaminase (GABA-T) degrades GABA not packed into synaptic vesicles
Decreasing availability GABA for synaptic transmission and therefore neuronal inhibition
what drug blocks this function
Vigabtrin
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Card 2

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how can a synapse be modulated (4)

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transmitter-gated ion channels, GPCRs, reuptake transporters, degradative enzymes

Card 3

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what is GABA

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Card 4

Front

function of GABA in brain

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Card 5

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GABA hyperpolarises neuron's which decreases what

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