Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
25 Cards in this Set
- Front
- Back
|
MOA Benzos
|
Inhibitory at postsynaptic GABAa receptors in amgdala
Non linear kinetics Cleared by hepatic metabolism Do not change hepatic drug metabolizing activity with cts. use |
|
|
Barbituates
|
Bind to multiple isoforms of GABAa receptors (different site than benzos)
Increase duration of GABA gated chloride channel openings Facilitate actions of GABA at multiple sites in CNA Less selective than benzos Depress actions of excitatory NT glutamic acid Slow metabolism (except thiobarbiturates) May increase hepative metabolism (of self and other drugs)-- Especially PB and meprobamate |
|
|
Newer Hypnotics
|
Selectively bind only a1 subunits of GABAa
Don't change hepatic drug metabolizing activity with cts. use Metabolized to inactive form Rapid onset, modest day after psychomotor depression with few amnestic effects Preferred over older drugs (chloral hydrate, secobarbital, pentobarbital) |
|
|
Alprazolam
|
Undergoes a-hydroxylation
-Creates short half life metabolite |
|
|
Chlordiazepoxide
|
Long acting and self tapering because of active metabolites; prodrug
|
|
|
Clorazepate
|
Converted to active metabolite Nordiazepam (long half life) with rapid absorption
|
|
|
Diazepam
|
More rapid absorption
Long half life |
|
|
Estazolam
|
Right to Glucuronidation
|
|
|
Flurazepam
|
Short half life
|
|
|
Lorazepam
|
Intermediate/Short half life
Right to Glucuronidation |
|
|
Midazolam
|
Short half life
|
|
|
Oxazepam
|
Intermediate/short half life
Right to Glucuronidation |
|
|
Quazepam
|
Long half life
|
|
|
Temazepam
|
Intermediate half life
|
|
|
Triazolam
|
Extremely rapid absorption
Rapid onset of CNS effects Short elimination Short half life |
|
|
Pentobarbital
|
Shorter elimination half life
|
|
|
Secobarbital
|
Shorter elimination half life
|
|
|
Flumazenil
|
Benzo antagonist
High affinity for benzo binding site on GABAa receptors (competitive antagonist) Blocks actions of benzos, zolpidem, zaleplon, eszopiclone Acts rapidly with a short half life (due to rapid hepatic clearance) Synthetic benzo derivative |
|
|
Eszopiclone
|
Absorbed rapidly into the blood
Rapid onset of CNS effects Similar to benzos Half life= 6hrs |
|
|
Zaleplon
|
Similiar to benzos
Absorbed rapidly into the blood Rapid onset of CNS effects More minimal tolerance Acts rapidly Short half life (1hr) |
|
|
Zolpidem
|
Biphasic release
Similar to benzos Absorbed rapidly into the blood Rapid onset of CNS effects Half life= 1.5-3.5hrs |
|
|
Ramelteon
|
Agonist at MT1 and MT2 (Melatonin receptors)
No direct effects on GABAergic NT in CNS Reduces latency of persistent sleep Rapidly absorbed No effects on sleeep architecture, no rebound insomnia or significant withdrawal symptoms |
|
|
Buspirone
|
Slow onset anxiolytic agent
Doesn't interact directly with GABAergic systems Partial agonist at brain 5-HT1a receptors Affinity for D2 receptors |
|
|
Meprobamate
|
Formation of gastric bezoars occurs with intoxication
Little impairment of locomotor activity Can cause widespread depression of CNS Mostly metabolized in liver |
|
|
Chloral hydrate
|
Metabolized rapidly to active compound in liver
Exhibits barbiturate like effects on GABAa receptor channels |
