CNS Depressants
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- Created by: LailaFrancis
- Created on: 10-02-23 14:56
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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MIXEDGABA-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?
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
Decreasing availability GABA for synaptic transmission and therefore neuronal inhibition
what drug blocks this function
Vigabtrin
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Other cards in this set
Card 2
Front
how can a synapse be modulated (4)
Back
transmitter-gated ion channels, GPCRs, reuptake transporters, degradative enzymes
Card 3
Front
what is GABA
Back
Card 4
Front
function of GABA in brain
Back
Card 5
Front
GABA hyperpolarises neuron's which decreases what
Back
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