BDZ
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42 terms
Terms | Definitions |
|---|---|
 5 CNS effects of BDZ | Anxiolytic, amnestic Muscle relaxant, anticonvulsant, sedation/hypnosis |
| Anxiolytic effect of BDZ | Regulate firing of raphe nuclei neurons |
| Amnestic effects of BDZ | Inhibition of hypocampal LTP |
| Muscle relaxing effects of BDZ | Enhanced presynaptic inhibition in spinal cord |
| Anticonvulsant effect of BDZ | inhibit firing in epileptic foci |
| Sedation effect of BDZ Increase? Other use? | Decrease sleep latency, increase sleep time Increase stage 2, decrease 1,3,4, REM Anesthetic: combined with other full anesthetics |
| 4 other effects of BDZ | Improve anxiety related GI disorders Decrease BP and increase HR Slight respiratory depression Worsens sleep related breathing disorders |
| All MOA of BDZ are due to | enhanced GABAa receptor activation |
| BDZ increases (2)? Require? | Increase affinity of GABA binding site for agonists, opening frequency of Cl channels Require a gamma-2, a beta, and certain alpha subunits |
| Alpha 1 | Sedative Anticonvulsant |
| Alpha 2 and 3 | anxiolytic |
| Alpha 5 | amnestic |
| What's flumazenil | BDZ competitive antagonist |
| What are picrotoxin, bicucullin? | BDZ noncompetitive antagonists |
| 7 SE of BDZ | Sedation, memory dysfunction Nightmares, uninhibited behavior, rage, suicide |
| SE's are due to | disinhibition reaction decrease REM withdrawal from short acting agents |
| Pharmacokinetics and metabolism of BDZ (5) | Orally absorbed, 70-99% protein bound Metabolized in liver by 3A4, 2D19, conjugation |
| Pharmacokinetics for specific agents is determined by | half life of parent drugs and active metabolites |
| how BDZ interact with CNs depressants | synergistic |
| BDZ's metabolism is inhibited by (3) | Cimetidine, disulfiram, OC |
| Metabolism of BDZ is increased by | Chronic ethanol, Phenytoin, isoniazid |
| 5 classes | Anxiolytic Alcohol Sleep anticonvulsant Preanesthetic |
| 8 anxiolytics | chlordiazepoxide, lorazepam, oxazepam, clonazepam, clorazepate, diazepam, alprazolam, prazepam |
| halfe life of anxiolytics? Except? | Long Except Lorazepam, alprazolam, Oxazepam: Medium |
| 3 alcohol | Diazepam Chordiazepoxide Oxazepam |
| half life of alcohol? | D: L chlordiazepoxide: L Oxazepam: M |
| 6 sleeping agents and their half lifes | Triazolam, Zolpidem: S Estazolam, Temazepam: M Flurazepam, Quazepam: L |
| 4 preanesthetics and their half life | Lorazepam: M Midazolam: S Chlordiazepoxide: L Diazepam: L |
| Diazepam could be used for? Except? Chlordiazepoxide could be used for? Except? | D: All except sleep C: all except Sleep and anticonvulsant |
| MOA of flumazenil Used for? Dosage? half life? | Nonselective antagonist Used for BDZ overdose IV: extensive first pass 1 hr |
| Bretazenil +? MOA (2) 3 effects? Less? (2) | Imidazenil Full agonist at A5, antagonist at A1 Anticonvulsant, anxiolytic, Little sedation Less tolerance, alteration of subunit composition |
| Zolpidem +? | Zalepon Eszopiclone Indiplon |
| MOA of zolpidem, eszopiclone, indiplon? Effect? Less ?(4) | Only binds to A1 subunits Very potent sedative effects less effect on REM, rebound insomnia, tolerance and dependence |
| MOA of L838417 Effect? | Agonist at A2,3, antagonist at A1 Anxiolytic with no sedation |
| Clonazepam +? 3 MOA? | Nitrazepam, nordazepam Selective anticonvulsant Partial agonsists or subtype slective |
| MOA of loreclezole? Effect? | Selective for receptors containing B2 subunit Selective anticonvulsant with no sedation Can stimulate GABAa receptor in absence of GABA |
| More tolerance to? Less to? Due to? | More tolerance to sedation, less to anticonvulsant, very little anxiolysis Due to altered GABAa receptor subunit composition |
| Tolerance to sedation requires | A5 subunit |
| Moderate withdrawal | Anxiety, insomnia, increase REM |
| Severe withdrawal Most severe if? | panic, muscle twitches, convulsant If flumazenil is given |
| Physical dependence is due to? | Altered GABAa receptor subunit composition Less A1 and Gama 2 subunits |
| 3 treatment of dependence | Switch to longer Acting BDZ Decrease dose over 10-21 days Substitute with Zolpidem. |
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