Term
|
Definition
|
|
Term
|
Definition
| personality/mental retardation |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| reduces anxiety w/o effecting motor/mental fxn |
|
|
Term
|
Definition
| produces drowsiness and encourages onset and maint of sleep |
|
|
Term
| general fxn of sedative-hypnotics |
|
Definition
| facilitate GABA transmission at GABAaR |
|
|
Term
|
Definition
|
|
Term
| prototypical GABAaR agonist |
|
Definition
|
|
Term
| prototypical GABAaR antagonist |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| 1. presyn terminals controlling release of NTs via dec in Ca conductance 2. postsyn allowing K conductance |
|
|
Term
|
Definition
|
|
Term
| GABA receptor affected by benzos/barbs |
|
Definition
|
|
Term
|
Definition
|
|
Term
| how many TM domains in each GABAaR subunit? |
|
Definition
|
|
Term
| where are the amino/carboxy termini of each subunit of the GABAaR? |
|
Definition
|
|
Term
| most common form of GABAaR? |
|
Definition
|
|
Term
| what subunits does benzo binding on the GABAaR depend mostly on? |
|
Definition
| type of alpha unit coupled to the g2 |
|
|
Term
| on what subunits does GABA bind to the GABAaR? |
|
Definition
|
|
Term
| where do benzos bind to the GABAaR? |
|
Definition
|
|
Term
| do benzos compete w/ GABA on the GABAaR? |
|
Definition
|
|
Term
| where do imidazopyridines bind to the GABAaR? |
|
Definition
|
|
Term
| what are the imidazopyridines? |
|
Definition
|
|
Term
| action of zolpidem, zaleplon? |
|
Definition
|
|
Term
| classic BZ GABAaR antagonist? |
|
Definition
|
|
Term
| what two classes of drugs does flumazenil antagonize? |
|
Definition
|
|
Term
| what three classes of drugs does flumazenil not antagonize? |
|
Definition
|
|
Term
| half like of flumazenil IV? |
|
Definition
|
|
Term
| clearance of flumazenial? |
|
Definition
|
|
Term
| inverse agonists of the GABAaR? |
|
Definition
|
|
Term
| do barbs bind to the BZ on the GABAaR? |
|
Definition
|
|
Term
|
Definition
| increase duration of Cl channel opening in presence of GABA |
|
|
Term
|
Definition
| direct opening of Cl channel |
|
|
Term
| what neurosteroid can potentiate GABA by acting on GABAaR? |
|
Definition
|
|
Term
|
Definition
| neurosteroid, potentiates GABA by acting on GABAaR |
|
|
Term
| effect of EtOH on GABAaR? |
|
Definition
| appears to act somewhat like a benzo |
|
|
Term
|
Definition
|
|
Term
| bioavailability of benzos? |
|
Definition
|
|
Term
| protein binding of benzos? |
|
Definition
|
|
Term
| what does benzo binding to GABAaR do? |
|
Definition
| inc affinity of GABAa for its binding site, inc freq of opening of Cl channels |
|
|
Term
| use of benzos in pregnancy? |
|
Definition
| cross placenta, may be teratogenic |
|
|
Term
|
Definition
|
|
Term
| benzos that undergo both I and II metabolism |
|
Definition
| diaz, fluraz, clonaz, flunitraz, midazo, apraz, triaz |
|
|
Term
| which two benzos have active metabolites w/ a long HL? |
|
Definition
|
|
Term
| what happens when midazo, alprazo, and triazo are oxidized? |
|
Definition
| they are rapdily eliminated |
|
|
Term
| benzos that undergo only II metabolism |
|
Definition
|
|
Term
| do oxaz, loraz, temaz have an active metabolite? |
|
Definition
|
|
Term
|
Definition
| drowsiness, ataxia, amnesia |
|
|
Term
| what symptoms are possible when pts over the age of 50 are given high doses of triazolam? |
|
Definition
| confusion, excitement, rage |
|
|
Term
|
Definition
| bind to GABAaR distinct from BZ sites, inc duration of Cl opening, depress action of excitatory NTs |
|
|
Term
| are barbs specific to the GABAaR? |
|
Definition
|
|
Term
| why do barbs not have a "ceiling effect" on their potential for CNS depression? |
|
Definition
| they can be GABAmimetic at hi-dose |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| intermediate acting barbs? |
|
Definition
| amobarbital, secobarbital, pentobarbital |
|
|
Term
|
Definition
|
|
Term
| adverse effects of barbs... |
|
Definition
| low TI, dependence, stimulate of CYP450 and microsomal oxidases, tolerance, anesthesia |
|
|
Term
| clinical uses of phenobarbital |
|
Definition
|
|
Term
| clinical uses of thiopental and methohexital |
|
Definition
|
|
Term
|
Definition
|
|
Term
| action of chloral hydrate |
|
Definition
| metabolized to trichloroethanol, 6-10hr hl |
|
|
