Anxiety and Sleep Flashcards
decreases motor activity, coordination, and mental acuity
sedative
increases tendency to sleep from which the patient is easily awakened
hypnotic
induces sleep from which the patient is not easily awakened
anesthetic
- produce anesthesia, coma and and death
- barbiturates
- ethanol
complete CNS depressants
- typically don’t produce anesthesia and will not induce coma or death alone
- benzodiazepenes
- non benzodiazepine, BZ receptor agonists
incomplete CNS depressants
Barbiturates bind that barbiturate binding site on the _______ receptor, increasing ______ ion channel flux by increasing channel open time
GABAa
chloride
effect of barbiturates on CNS? respiratory and cardiovascular?
- complete CNS depressant
- no effect on cardiovascular up to anesthetic dose
barbiturates induce what type of tolerance?
pharmacokinetic (induce CYP450, decrease plasma levels of other drugs)
- tolerance to this class of drugs develops over time (kinetic and dynamic)
- addiction common
- withdrawal - anxiety, tremor, n/v, weight loss, psychosis, seizures, hyperthermia, cardiovascular collapse can be fatal
- treatment: measured reduction over time (2-3 wks)
barbiturates
long acting barbiturate?
phenobarbital
pentobarbital and secobarbital are _______ acting barbiturates
medium
methohexital and amobarbital are ______ acting barbiturates
short, given IV
ultra short acting barbiturate given IV?
thiopental
used as sedatives, hypnotics (not 1st line), anticonvulsants, drug induced coma, preanesthetic, anesthetic, WADA test, truth serum, euthanasia
barbiturate uses
- readily diffuse across all membranes
- redistribution accounts for differences in duration of action
- cross placenta
- high bound to plasma proteins (drug interactions)
- metabolized in liver
- excreted in urine
pharmacokinetics of barbiturates
Benzodiazepines bind to BZ sites on GABAa receptor, increase _______ of GABAa receptor for GABA increasing likelihood of channel opening
affinity
what underlies the differences in effects of various benzodiazepine compounds?
heterogeneity of receptor subunits, different affinities for BZ binding sites
- incomplete CNS depressant
- decreased anxiety
- skeletal muscle relaxant
- anticonvulsant
- hypnotic
- tolerance develops to sedative, hypnotic, anticonvulsant actions
- paradoxical excitement
- no CV, resp, GI effects
effects of diazepam (benzodiazepines)
- sedation and ataxia
- amnesia
- nightmares, irritability, anxiety, seizures
- treat acute overdose with flumazenil
- withdrawal: rebound anxiety irritability, insomnia, tremor, sweating, anorexia, seizures, psychosis
- low risk of fatal OD if used alone
side effects of benzos (diazepam)
midazolam and triazolam are _______ benzodiazepines
short acting
most rapidly inactivated benzo used for anesthesia IV?
midazolam
anxiolytic/hypnotic used for panic attacks, rapid oral absorption/onset
alprazolam
chlordiazepoxide, lorazepam are _____ benzos used as anziolytics/preanesthetic
moderate acting
long acting benzo used as anticonvulsant?
clonazepam
very long acting benzo with active metabolites used as anxiolytic, anticonvulsant, muscle relaxant, antispastic, pre-anesthetic?
diazepam
flurazpeam is a _____ benzo
very long acting
fast acting, amnestic, date rape drug, no therapeutic use
flunitrazepam
used to reverse overdose of benzos and anesthesia?
flumazenil
- rapidly absorbed from GI
- admin orally, highly protein bound but few drug interactions
- cross placenta
- numerous active metabolites
- metabolized in liver, excreted in urine
benzodiazepines
- BZ1 agonists and non selective
- hypnotic, short half life, less amnestic than benzos
- produce less tolerance
- hallucinations, sleepwalking, amnesia
zolpidem, zaleplon, eszopiclone
partial agonist at 5-HT1a site, slow onset of action 1-2 wks, dysphoric at high doses
buspirone
increase synaptic availability of 5-HT, used for GAD and prophylaxis for panic attack
SSRIs
H1 blocker, pre and post op, antipruritic and antiemetic
hydroxyzine
MT1/2 melatonin receptor antagonist, indicated for insomnia with prolonged sleep onset
ramelteon
indicated for difficulties with sleep onset or maintenance, orexin antagonist
suvorexant
H1 blocker, common OTC sedative
diphenhydramine
blocks 5HT reuptake, antidepressant but also used as hypnotic
trazodone