-
Buspirone
- 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.
-
Hydroxyzine
- has been used for many years as a perioperative sedative and anxiolytic and is considered an effective alternative treatment for generalized anxiety
- disorders.
-
Propranalol
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.
-
BDZ ex
- chlordiazepoxide
- clorazepate
- 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.
-
intermediate-acting BDZ
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
-
gaba
Cl ionotropic channel, causes rapid hyperpolarization decrease neuron firing. calmer less anxious brain, closer to sleep
-
is cross tolerance and rxn common with BZDs?
yes
-
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
-
diazepam indication
alleviate muscle spasms such as in MS. presynaptic inhibition of Spinal cord with sedation
-
sleep inducers
- flurazepam
- triazolam
- zolpidem
-
flurazepam indication
long acting sleep- no rebound insomnia. low hypnotic and tolerance potential. may cause daytime sedation, REDUCED REM sleep
-
triazolam
fast sleep onsent, not used for long time because of rebound insomnia. RAPID TOLERANCE, does NOT protect REM
-
zolpidem
selective A1 subunit target. quick on and off. associated with tolerance and amnesia. intended for only a week, claims to protect REM sleep
-
zaleplon
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
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