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92 Cards in this Set
- Front
- Back
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Gastric ulcer
MI |
Disease related anxiety
Treat the disease Short term Rx of sedative-hypnotic |
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death of family member
surgery |
Situational anxiety
Short term Rx |
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generalized anxiety disorder
panic disorder |
Chronic anxiety
psychotherapy and Rx |
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sleep apnea
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do not use hypnotics- dec arousal response to hypoxia; exacerbate obstructive sleep apnea by reducing muscle tone
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circadian rhythm disturbances
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hypnotics can help
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disease-related insomnia (depression, anxiety, psychosis, chronic heart failure, pain)
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treat medical condition first
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Rx/substance related insomnia (alcohol, SSRIs, anti-Parkinson's, methylxanthines, diuretics)
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first alter dosing regimen or medication choices
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Transient insomnia
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Rx for 2-3 days, not more than 2-3 wks --> than taper
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chronic insomnia
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first change exercise, diet, behavior
some new hypnotics are safe(r) long term use is problematic/not recommended |
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Name six classes of sedative hypnotics
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1. barbituates
2. benzodiazepine receptor ligands 3. older sedative-hypnotics 4. serotonergic agents 5. OTC sleep aids 6. GHB/sodium oxybate |
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Where do barbituates work?
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bind barbituate site on GABA-A receptor --> allosteric enhancement of GABA --> inc duration of GABA induced Cl channel opening
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Where do barbituates work at higher doses?
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directly activate GABA-A receptors
inhibit AMPA receptor |
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What is the barbituate dose dependent continuum of CNS depression?
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sedation -> sleep -> coma -> anesthesia -> death
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Barbituates...
Do/do not induce phsyiologic sleep? High/low therapeutic index? Do/do not have drug interactions? Do/do not cause abuse and addiction? |
Do not
low significant drug interactions yes to abuse and addiction |
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Mechanism of barbituate tolerance?
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1. pharmacokinetic- induces CYP450
2. pharmacodynamic- neurons less sensitive and have cross tolerance to other CNS depressants |
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What happens with barbituate withdrawal?
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1-2 nights rebound insomnia --> life threatening CNS excitation --> seizures --> coma --> death
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When do you use long acting barbituates?
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daytime, antiseizure
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When do you use intermediate acting barbituates?
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hypnotic, preoperative sedative, emergency management of seizures
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When do you use short acting barbituates?
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induction or maintenance of anesthesia
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mephobarbital
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long acting barbituate
10-70 hrs |
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phenobarbital
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long acting barbituate
80-120 hrs also used for hypnosedative withdrawal |
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amobarbital
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intermediate acting barbituate
10-40 hrs |
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secobarbital
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intermediate acting barbituate
15-40 hrs |
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pentobarbital
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intermediate acting barbituate
15-50 hrs |
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thiopental
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short acting barbituate
8-10 hrs |
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methohexital
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short acting barbituate
3-5 hrs |
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Are barbituates used as anxiolytics?
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no
still used as hypnotics and antiseizure agents in limited settings |
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How are barbituates metabolized?
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metabolism/conjugation in liver --> renal excretion
short acting- highly lipophyllic--> terminated by redistribution from CNS into muscle and fat |
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When are older sedative-hypnotics used?
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rarely, but still in some institutionalized patients
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Which older sedative-hypnotic is similar to benzodiazepines (with greater abuse) instead of barbituates
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meprobamate
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How do they work?
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bind benzodiazepine site on GABA-A receptor --> allosteric enhancement of GABA --> inc FREQUENCY of cl channel openings
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chloral hydrate
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older sedative-hypnotic
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ethchlorvynol
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older sedative-hypnotic
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paraldehyde
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older sedative-hypnotic
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methyprylon
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older sedative-hypnotic
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ethinamate
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older sedative-hypnotic
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glutethimide
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older sedative-hypnotic
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meprobamate
(mep-ro-ba'-mate) |
older sedative-hypnotic
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Name two serotonergic agents
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buspirone (byoo-SPY-rone)- partial 5-HT1A agonist
and SSRIs |
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Name three uses of serotonergic agents?
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1. anxiety
2. depression 3. many other psych ds |
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3 advantages of serotonergic agents over benzodiazepines
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safer
less psychomotor impairement less abuse potential |
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4 disadvantages of buspirone
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weak anxiolytic
dizziness headache nausea |
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4 disadvantages of SSRIs
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slow onset
non-responders to anxiolytic effects sexual dysfunction sleep disturbances |
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Name 3 OTC sleep aids
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antihistamines
melatonin valerian |
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What's wrong with antihistamines as sleep aids
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rapid tolerance
inadequate dosages pradoxical stimulation residual daytime sedation |
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Where is melatonin made?
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pineal gland, controlled by light
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What does melatonin do?
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lightens skin pigment
suppresses ovarian function sold to reduce jet lag/promote sleep |
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What exactly is valerian
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dietary supplement from valerian plant- used forever to treat sleep disorders but no convincing clinical data
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doxylamine
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antihistamine
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diphenhydramine
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antihistamine
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pyrilamine
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antihistamine
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Mechanism of action of GHB/sodium oxybate
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metabolite of GABA --> CNS depressants
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Why is GHB a schedule I controlled substance?
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addictive, abused for euphoric/hallucinogenic properties, now more popular than rohypnol as a date rape drug
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When is sodium oxybate a schedule III controlled substance?
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when it is used as prescribed for tx of cataplexy in patients with narcolepsy
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Adverse effects of GHB/sodium oxybate when abused?
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amnesia
vomiting respiratory and cardiovascular depression LOC seizures death |
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Adverse effects of GHB/sodium oxybate when used as prescribed?
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confusion
headacthe nausea vomiting dizziness urinary incontinence |
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When are spasmolytics used?
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tx sk mm spasms from MS, ALS, spinal cord transection, CP, stroke or local muscle trauma
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Which two benzodiazepines are spasmolytic?
What is their adverse effect? |
diazepam
clonazepam sedation |
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Baclofen
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spasmolytic
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baclofen mechanism of action
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GABA-B agonist
- inc K perm, dec Ca influx --> dec transmitter release |
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tizanidine
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spasmolytic
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tizanidine mechanism of action
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central alpha-2 adrenergic agonist
inc pre and post-synaptic inhibition of motor neurons |
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dantrolene
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spasmolytic
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dantrolene mechanism of action
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direct action of sk mm --> dec Ca release from sarcoplasmic reticulum --> inhibits excitation/contraction coupling
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other uses for dantrolene
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malignant hyperthermia
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Name four reasons why benzodiazepines positive modulators have replaced barbituates and older agents as sedative hypnotics?
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1. higher Therapeutic index
2. lower toxicity w/ overdose 3. fewer sleep pattern alterations 4. dec. tolerance and abuse |
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Do benzodiazepine positive modulators work in the absence of GABA?
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no
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Are benzodiazepine positive modulators general CNS depressants?
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no
continuum is sedation --> sleep |
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Why should patients on benzodiazepine modulators not take alcohol>
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even though respiratory and CV function depression is rare with overdose, depressant actions are additive with other CNS depressants
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alprazolam
(xanax) |
benzodiazepine for anxiety (short acting)
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chlordiazepoxide
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benzodiazepine for anxiety, alcohol withdrawal, preanesthetic
(short acting) |
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clonazepam
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benzodiazepine for seizures, mania, movement disorders
(intermediate) |
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clorazepate
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benzodiazepine for anxiety and seizures
(very short) PRODRUG |
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diazepam
(valium) |
benzodiazepine for anxiety, status epilepticus, muscle relaxant, preanesthetic
(long) |
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estazolam
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benzodiazepine for insomnia
(short) |
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flurazepam
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benzodiazepine for insomnia
(very long) |
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lorazepam
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benzodiazepine for anxiety, status epilepticus, preanesthetic
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midazolam
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benzodiazepine for preanesthetic and intraoperative medication
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oxazepam
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benzodiazepine for anxiety
(short) |
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quazepam
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benzodiazepine for insomnia
(long) |
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temazapam
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benzodiazepine for insomnia
(short) |
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triazolam
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benzodiazepine for insomnia
(short) |
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Common benzodiazepine drug interaction?
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Cyp450 3A4 inhibitors
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What is the metabolism of benzodiazepines
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first go to high perfusion areas (bain) than to lower areas (mm, fat)
--> metabolized in liver to other active metabolites |
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adverse effects of benzodiazepines
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1. alters sleep patterns
2. impaired mental/motor function, ataxia, daytime sedation, anterograde amnesia, additive with other CNS depressants 3. Abrupt withrdawal can cause anxiety, nausea, seizures 4. Abuse- flunitrazepam as date rape drug |
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advantages of non-benzodiazepine modulators?
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no anxiolytic, mm relaxant, antiseizure properties, no rebound insomnia or other withdrawal sx
(Blind to BZ) |
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zolpidem
(ambien) |
non-benzodiazepine modulator
for use as hypnotic, maintain nl sleep patterns |
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zaleplon
(sonata) |
non-benzodiazepine modulator
for use as hypnotic, maintain nl sleep patterns |
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adverse effects of non-benzodiazepine modulators?
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abuse potential like benzodiazepines
morning sedation w/ late night use of zolpidem |
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flumazenil
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competitive benzodiazepine site antagonist for decreasede recovery time from benzodiazepine modulators
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flumazenil fast or slow acting? fast or slow metabolism?
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rapid onset, short half life
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Adverse effects of flumazenil
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agitation, confusion, dizziness, nausea
inc risk of seizures/other withdrawal sx in patients with benzodiazepine tolerance or barbituate, tricyclic antidepressant overdose |
