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18 Cards in this Set
- Front
- Back
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What are the 2 types of Benzodiazepines?
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1. GABA agonist
2. GABA antagonist |
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What is the mechanism of GABA agonists?
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1. They bind to/activate benzodiazepine receptor on GABA-a
2. Increases opening of chloride ion channels which leads to hyperpolarization of postsynaptic neuron 3. Decreasing neuronal transmission |
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What is the mechanism of GABA antagonists?
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1. They competitively antagonize action of benzodiazepines on BZ receptor site on GABAa
2. Prevents hyperpolarization of postsynaptic neuron 3. Increasing neuronal transmission |
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What benzodiazepine(s) are GABA agonists?
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* Diazepam
* Midazolam * Lorazepam |
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What benzodiazepine(s) are GABA antagonists?
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Flumazenil
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What are the Benzodiazepines discussed in class?
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* Diazepam
* Lorazepam * Flumazenil * Midazolam |
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What is the MOA of Benzodiazepines?
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They bind to a GABA receptor which increases GABA binding and action (synergistic effect) which leads to increased Cl- influx and thus hyperpolarization of postsynaptic neuron and then decreased neuronal transmission
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How are Benzodiazepines metabolized and eliminated?
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biotransformation in liver, renal excretion into urine
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What is Diazepam used for?
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Used for status epilepticus, not for chronic management
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What is the MOA of Diazepam?
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Increases seizure thresh-hold and decreases electrical activity
Potentiates GABA; Increases Cl conductance |
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What are the adverse effects of Diazepam?
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tachyphylaxis, tolerance, hepatic necrosis (cats)
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What is Midazolam used for?
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sedative-hypnotic
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What is the MOA of Midazolam?
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Potentiates GABA; Increases Cl conductance
(2x more potent than Diazepam) |
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What is Lorazepam used for?
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sedative-hypnotic, status epilepticus
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What is the MOA of Lorazepam?
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Potentiates GABA; Increases Cl conductance
(10x more potent than Diazepam) |
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What drug is used to reverse benzodiazepines?
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Flumazenil (Benzodiazepine competitive antagonist)
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What is the MOA of Flumazenil?
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Antagonizes by binding to the GABAA receptor and preventing hyperpolarization of the post-synaptic membrane
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What are adverse effects of Flumazenil?
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seizures in patients chronically using benzodiazepines
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