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- is structurally and pharmacologically distinct from all other anxiolytics. It blocks certain 5HT receptors, does not possess anticonvulsant or muscle-relaxant
- properties, does not impair psychomotor function or cause sedation or physical dependence. Its onset of anxiolytic effects can be as long as 2 weeks and it is used for the treatment of generalized anxiety disorder.
- has been used for many years as a perioperative sedative and anxiolytic and is considered an effective alternative treatment for generalized anxiety
reduce the sympathetic arousal aspect of anxiety and are used to control stage fright and other specific anxiety states.
The benzodiazepines (BDZs) compared to others
- much higher therapeutic index than other sedating drugs.toxicity curve for BDZs reaches a plateau
- but the barbiturate toxicity curve does not.
- These are schedule C-IV controlled substances.
- flumazenil – the only benzodiazepine antagonist
- zolpidem – benzodiazepine like
- zaleplon - benzodiazepine like
- flurazepam, alprazolam, lorazepam, oxazepam, triazolam, diazepam
BDZ form active metabolites with long half-lives.
Diazepam, chlordiazepoxide, clorazepate and flurazepam Each drug attains peak blood levels several hours after oral administration and has a slow decline over days.
Alprazolam and lorazepam are that can cause residual drowsiness after their sedative effects have dissipated.
short - acting drugs BDZ
Oxazepam and triazolam may cause rebound anxiety when their effects terminate.
BDZ- all undergo this type of metabolism
phase II conjugation prior to urinary excretion
BDZ w/no active metabolite
oxazepam, lorazopam- used for pts with compromized liver fn- no phase I
Cl ionotropic channel, causes rapid hyperpolarization decrease neuron firing. calmer less anxious brain, closer to sleep
is cross tolerance and rxn common with BZDs?
how are BZD and barbituates acting on GABA?
- BZD alter freq of cl opening
- barb open Cl and cause then to stay open
- EtOH similar to barb
triazolam and AE
- BZM, short half life- no active metab
- drug inxns P4503A4 decrease clearance especially careful with old and fat with compromised liver fn
- anterograde amnesia and severe rebound anxiety
- increase risk with EtOH, daytime anxiety- when used for sleep
midazolem and AE
- short act for conscious sedation, anxiolysis, amnesia for sugery
- short term anterograde amnesia
- AE- resp depress in 11% IM pts, 23% IV
- reduced tidal volume . apnea and hiccups, and site rxn
alprazolam and AE
- anxiety, panic attacks, agoraphobia, very potent 10x>diazepam
- AE- significant p450a34 decrease clearance, high addiction potential
- high abuse potential with EtOHlics
flumenazil and AE
- parenteral BDZ ANTagonist, used to treat BZM overdose and reverse BZM anesthesia, DOES NOT work for barbs, opiates, TCAs
- AE- short DOA, compared to BZM,- resedation,
BZM common AE
- teratogenesis Cat X
- sleep related behaviors- sleep driving, phone calls or sleep eating.
- Paradoxical CNS stim 10% pts particularly psych pts and hyper children.- nightmares, talkative, excitement, mania, tremor, insomnia, anxiet, restless, euphoria, rage, hyperactivity
addiction and withdrawal of BZM
little as 2 weeks of use, irritable, nervous, insombia, ab cramps, confusion, depression, perceptial disturbance, sweating, NV, tach, trembling
alleviate muscle spasms such as in MS. presynaptic inhibition of Spinal cord with sedation
long acting sleep- no rebound insomnia. low hypnotic and tolerance potential. may cause daytime sedation, REDUCED REM sleep
fast sleep onsent, not used for long time because of rebound insomnia. RAPID TOLERANCE, does NOT protect REM
selective A1 subunit target. quick on and off. associated with tolerance and amnesia. intended for only a week, claims to protect REM sleep
interacts with a1 and a2 subunits has anticonvulsant, anxiolytic, hypnotic and myorelaxant properties. decreases time to sleep onset for up to 35 days w/o tolerance, minimal AE. REM protectant
General AE of sleep inducing agents
- HA, daytime drowsy, dizziness, drugged feeling
- anaphylactoid rxns- angiodema
- complex sleep related behaviors- sleep driving with amnesia