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27 Cards in this Set
- Front
- Back
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Where is the Benzodiazepine receptor located |
A specific binding site is on the alpha subunit of the GABAa receptor complex |
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What does benzodiazepine receptor modulate |
Modulates the binding of GABA to its site |
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What are the binding sites of the GABAa receptors |
2x GABA sore BZD site Cl- pore |
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What does BDZs enhance the ability of activates GABA receptors to open |
Increased frequency of opening No change in channel conductance No change in mean duration of opening |
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How do BDZs compare to barbiturates |
No change in frequency of opening No change in channel conductance Increased mean duration of opening |
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What is the affinity and positive efficacy of an agonist |
E=1 |
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What is the affinity and efficacy of inverse agonists |
e=-1 |
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What is the efficacy and affinity of a antagonist at BDZ receptor ligand |
e= 0 |
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What is the efficacy and affinity of partial agonists |
Affinity and low positive efficacy 0 |
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What are endozepines |
Endogenous compounds with BDZ like effects |
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What are BDZ agonists |
Positive allosteric modulators Enhance GABA-mediate inhibitory effects Anticonvulsant |
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What are some examples of BDZ agonist |
Diazepam Clonazepam |
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What are examples of Z-drugs |
Zoloiderm Zopiclone Zaleplon |
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What’s re Z drugs similar to |
BDZ |
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Where do BDZ receptor inverse agonists bind |
Negative allosteric modulators |
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What are partial BDZ agonists good for |
Anxiolytic effect |
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What do benzodiazepines cause as cns depressants in ascending dose |
Increase seizure threshold Euphoria intense feeling of pressure Anxiety relief Relaxation Sleepiness Unconsciousness Death |
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What are unwanted effect of BDZ |
Excessive CNS depression Paradoxical CNS effects Habituation Tolerance |
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What is excessive CNS depression |
Drowsiness Confusion Memory problems |
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What is paradoxical CNS effects |
Increased anxiety Aggressive behaviour More common in children and elderly More common in shorter acting drugs |
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What is habituation |
Associated with an unpleasant withdrawal syndrome |
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What is tolerance |
Loss of clinical effect in repeated use |
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What are the therapeutic uses of BDZ receptor agonists |
Treat epilepsy, muscle spasms, reduce anxiety, reduce anxiety Sedated restless parties and promote sleep Induce surgical anaesthesia |
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How do BDZ treat epilepsy |
BDZ strengthen inhibitory inputs, increasing seizure threshold |
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How does BDZ treat muscle spasm |
Inhibition action of BDZs in spinal cord |
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How do BDZs reduce anxiety |
Inhibitory action if BDZs in limbo system |
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How do BDZs induce surgical anaesthesia |
Intravenous administration of short acting compound |
