-
phenobarbital
- long acting barbituate
- MOA: binds the GABA A Cl channel on the beta subunit. increases the duration the channel is open. increases hyperpolarization
- USES: seizures, rapid ability to alleviate fear and anxiety (but no longer used)
- AE: sedation, high dependance, lethal in overdose, narrow TI
-
thiopental
- ultra short acting barbituate
- MOA: binds to GABA A of Cl channel, increases the duration the channel is open.
- USES: anesthesia, IV b/c so short acting, not good for seizures
- AE: sedation, high dependence, lethal overdose, narrow TI
- induces p450 enzymes
-
diazepam
- long acting BZ (valium)
- MOA: binds to GABA A on Cl channels. increases the frequency of the Cl channel opening
- USES: anxiety b/c of the long t1/2
- AE: anterograde amnesia, won't cause coma or death with overdose.paradoxical excitement
- don't use for more than 5 weeks
-
chlordiazepoxide
- long acting BZ
- MOA: binds to GABA A on Cl channels. increases the frequency of the Cl channel opening
- USES: anxiety b/c of the long t1/2
- AE: anterograde amnesia, won't cause coma or death with overdose.
- paradoxical excitementdon't use for more than 5 weeks
-
oxazepam
- intermediate acting BZ
- MOA: increase the freq of the Cl channel opening
- USES: anxiety b/c has a longer t1/2.
- has no toxic metabolites so can be used in the elderly
- AE: amnesia, paradoxical excitment
-
lorazepam
- intermediate acting BZ
- MOA: increases the freq of Cl channel opening
- USES: insomnia b/c shorter t1/2, can be used in emergency situations b/c can be administered IV.
- AE: amnesia
-
temazepam
- intermediate acting BZ
- MOA: increase the frequency of Cl channel opening, binds to GABA A.
- USES: insomnia
- AE: amnesia
- no toxic metabolites can be used in the elderly
-
midazolam
- ultra short acting BZ
- MOA: increase the frequency of Cl channels opening, binds GABA A
- USES: adjunct for anesthsia, used in emergencies b/c given IV
-
flumazenil
- BZ antagonist
- MOA: competative BZ receptor antagonist
- USES: used to counteract excessive effects of BZ
- doesn't block the effects of other sedative hypnotics
- doesn't produce sedation, confusion, or mental clouding
-
buspirone
- atypical sedative
- MOA: partial agonist at 5 HT. acts as an agonist where 5 HT is low and as an antagonist where 5HT is high
- USES: anxiolytic adjunct therapy for depression
- onset 1-2 weeks
- CI: MAOI's
-
zaleplon
- non-BZ, Z drug
- MOA: agonist at GABA A, increases melatonin
- USES: insomnia, rapid onset, used to fall asleep
- AE: no tolerence, or rebound insomnia
-
zolpidem
- non-BZ, Z drug, Ambien
- MOA: selective agonist at GABA A
- USES: insomnia, shortens sleep latency, prolongs total sleep time.
- AE: tolerance and dependence are rare
-
eszopiclone
- non-BZ, Z drug, lunesta
- MOA: agonist at GABA A
- USES: insomnia, falling asleep and staying asleep, increases sleep time
- effective for 6-12 months without dependence, fewer AE than BZ
- only Z drug approved for long term use
-
ramelteon
- non-BZ, Z drug, Rozerem
- MOA: melatonin agonist
- USES: insomnia, shortens sleep latency
- no tolerance or dependence
- no abuse potential
-
alprazolam
- intermediate acting, BZ
- MOA: increase the freq of Cl channel opening, alters the channel so that GABA binds more efficiently
- USES: anti-anxiety, sedation, insomnia, anticonvulsants
- AE: amnesia
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