Term
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Definition
| induction of a state of relaxation |
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Term
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Definition
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Term
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Definition
loss of sensation
General anesthesia: decreased consciousness with loss of sensation & decreased ability to feel pain |
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Term
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Definition
: extremely deep anesthesia or depression of brain activity
precursor to respiratory & circulatory failure |
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Term
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Definition
Benzodiazepines
Antidepressants
Barbiturates
Others
Hydroxyzine (Atarax, Visatril®)
Buspirone (Buspar®) |
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Term
| Benzodiazepines (BZDs) - MoA |
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Definition
GABA-A receptors
GABA: major inhibitory neurotransmitter of CNS
Effects: depends on type, subunits, & location of receptors
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Term
| Benzodiazepines: Actions - Anxiolytics |
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Definition
Low doses
Probably due to selective enhancement of GABA transmission in neurons having α2-subunits in the GABA-A receptors
Causes inhibition of neuronal circuits in the limbic system of the brain |
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Term
| BZD Actions - Sedation/Hypnotic |
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Definition
All BZDs have some sedative properties
Some produce hypnosis (artificial induction of sleep) at higher doses
α1-GABA-A |
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Term
| BZD Actions - Anterograde Amnesia |
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Definition
Temporary impairment of memory
α1-GABA-A |
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Term
| BZD Actions - Anticonvulsant |
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Definition
Several BZDs have anticonvulsant activity & are useful for treating seizure disorders |
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Term
| BZD Actions - Muscle Relaxant |
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Definition
High doses of some BZDs may cause relaxation of spasticity of skeletal muscle
α2-GABA-A |
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Term
| Benzodiazepines: Therapeutic Uses - Muscular Disorders |
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Definition
Diazepam (Valium®): Useful in treatment of skeletal muscle spasms
Muscle strain, spasticity associated with degenerative disorders (multiple sclerosis, cerebral palsy) |
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Term
| Flurazepam (Dalmane®) - BZD |
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Definition
Long-acting BZD: reduces sleep latency, reduces number of awakenings during the night, increases total sleep time
Causes little rebound-insomnia – when pt comes of drug
Active metabolites have a t ½ up to 85 hours
Daytime sedation, accumulation of drug
Maintains efficacy for insomnia for about 4 weeks – after that tolerance increases and drug is not as effective |
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Term
| Temazepam (Restoril®) - BZD |
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Definition
Useful in patients with frequent awakenings (or inability to stay asleep), but peak sedative effect occurs 3 hours after dose |
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Term
| Triazolam (Halcion®) - BZD |
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Definition
Short-acting BZD: useful for sleep induction (inability to go to sleep)
Tolerance develops quickly (few days), best for intermittent use (not daily to avoid tolerance & withdrawal)
Withdrawal causes rebound insomnia |
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Term
Alprazolam (Xanax®) - BZD |
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Definition
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Term
Clonazepam (Klonopin®) - BZD |
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Definition
Anxiolytic
Antiseizure activity |
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Term
Lorazepam (Ativan®) - BZD |
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Definition
Anxiolytic
Antiseizure activity |
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Term
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Definition
Anxiolytic
Muscle relaxant activity
Antiseizure activity |
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Term
Short-Acting (3-8 hours) - BZD
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Definition
Oxazepam (Serax®)
Triazolam (Halcion®) |
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Term
Intermediate-Acting (10-20 h) - BZD |
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Definition
Alprazolam (Xanax®)
Estazolam (Prosom®)
Lorazepam (Ativan®)
Temazepam (Sonata®) |
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Term
Long-Acting (1-3 days) - BZD |
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Definition
Clorazepate (Tranxene®)
Chlordiazepoxide (Librium®)
Diazepam (Valium®)
Flurazepam (Dalmane®)
Quazepam (Doral ®) |
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Term
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Definition
GABA receptor antagonist - BZD antagonist
Rapidly reverses the effects of benzodiazepines
Administered IV: rapid onset, short duration (t ½ is about 1 hour)
Multiple or frequent administrations may be required to maintain reversal of long-acting BZDs
Precipitates withdrawal in dependent patients or seizures in patient taking BZDs for seizure control
Adverse effects: dizziness, nausea/vomiting, agitation |
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Term
| Buspirone (Buspar®) - MoA |
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Definition
Anxiolytic effects: precise MoA is unknown but does NOT act on BZD receptors
are probably due to serotonin (5HT1A, 5HT2A) receptors, also show some affinity for DA2 receptors |
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Term
| Buspirone (Buspar®) - Actions |
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Definition
Lacks anticonvulsant & muscle relaxant activity
Very minimal sedation, & unlikely to result in dependence
Slow onset of action (compared to BZDs) |
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Term
Buspirone (Buspar)
Side Effects |
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Definition
Headaches, dizziness, nervousness
Decreased body temperature, prolactin, & growth hormone secretion
Low potential for cognitive or motor impairment |
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Term
Buspirone (Buspar)
Kinetics
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Definition
Liver metabolism by CYP 450 (CYP 450 Substrate—interaction with other substrates, inducers, & inhibitors) |
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