DENT 601 Sedatives and Anxiolytics
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KTay1127 Plus on May 14, 2012
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Terms | Definitions |
|---|---|
 Drugs to treat anxiety or produce sedation | Benzodiazepines "Non-benzodiazepine," non-barbiturate sedatives Barbiturates |
| non-benzodiazepines to treat anxiety | Buspirone (BuSpar)- 5HT1A partial agonists (+ other mechanisms); no or little sedation, muscle relaxant, or anticonvulsant effects; no abuse potential; anxiolytic effects are slow onset (~1-2 wks) Chronic antidepressants (not acute) - TCAs, SSRIs, MAOIs Antihistamines - mainly sedation, anticholinergic b-blockers - treats autonomic components of anxiety, used for stage fright. Not effective chronically. Mainly propranolol (Inderal) |
| GABA(a) Receptor | Agonist - bind to the GABA site, increase Cl- conductance Antagonist - bind to the GABA site, block agonist binding but no effect on own Positive allosteric modulator - binds to allosteric site, increases efficiency of GABA overall increases Cl- conductance Negative allosteric modulator - binds to allosteric site, decreases efficiency overall decrease Cl- conductance GABA agonist and a Positive allosteric modulator relieve anxiety and produce sedation |
| ... | BDZ site - interface of a and g subunits Different combinations of a and g subunits = different effects a1 associated = sedative, amnestic, and some anticonvulsant activity a2, a3, a5 associated = anxiolytic and anticonvulsant |
| Effects of GABA(a) Receptor Stimulation | Sleep/Sedative hypnotic Anxiety - all types Seizures Amnesia Muscle Relaxation |
| Allosteric Modulator Sites | 1. Barbituates - sedative, hypnotic, antiseizure (CII,III, IV) -Range of actions, ultrashort-acting -Respiratory depression -Suicide/Lethal injections -High abuse potential -Significant tolerance and dependence -Induce hepatic drug-metabolizing enzymes -used in specific cases (IV sedation, seizures) 2. Benzodiazepines (not subtype selective) (CIV) 3. "Nonbenzodiazepine", nonbarbiturate CNS depressant (CIV) "Z-drugs" -Treat insomnia, not anxiety -bind to BDZ site -preferential binding to one subtype (a1 containing) |
| Benzodiazepines | Bind to benzodiazepine site on GABA receptor; greater therapeutic index than barbiturates Agonists - almost all end in "-pam" or "-lam" Neutral antagonists - block effects of agonist (or inv. agonist) No activity of own Do not alter constitutive activity Flumazenil (Romazicon) |
| Benzodiazepines Nomenclature | Imidazobenzodiazepines Triazolobenzodiazepines Imidazo ring - 2 nitrogens Triazolo ring - 3 nitrogens Prevent creation of long-acting metabolites (metabolize quickly); most end in "-lam" |
| Benzodiazepines: Metabolism | Bind to plasma proteins! Aspirins, Warfarin (blood thinner) all bind to the plasma proteins Pregnant women should never take these Does not induce P450, the metabolisng protein in the liver, this is why they are better than barbituates |
| Benzodiazepines: Pharmacology | Tolerance - with repeated administration, use higher doses to get same effects; alcohol and barb users = insensitive Physical dependence - after repeated administration, withdrawal syndrome occurs upon rapid discontinuation (withdrawal syndrome - opposite to therapeutic effects) How might this be prevented??? Withdrawal from therapeutic doses - not life threatening Withdrawal from high doses - life threatening!!! WHY??? |
| Non-benzodiazepine, non-barbiturate CNS depressant | Z-drugs: zolpidem (Ambien), zaleplon (Sonata), eszopiclone (Lunesta) Treat insomnia short-term, not anxiety or seizures |
| Flumanezil | Reverses the affect of benzodiazepines |
| Benzodiazepines: age-related effects | -> 65 yr - particularly sensitive to CNS depressant effects -Elderly and children can have paradoxical effects -CNS excitation instead of CNS depression -hyperactivity, insomnia, irritability, rage + hostility if do sleep, often have nightmares may be due to disinhibition (sensitive GABA system) |
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