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NURS526 Pharmacology Dr. Nolan.  Nervousness, tension, worry, feelings of dread, apprehension  Palpitations, chest pressure, dizziness  May be chronic,

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Presentation on theme: "NURS526 Pharmacology Dr. Nolan.  Nervousness, tension, worry, feelings of dread, apprehension  Palpitations, chest pressure, dizziness  May be chronic,"— Presentation transcript:

1 NURS526 Pharmacology Dr. Nolan

2  Nervousness, tension, worry, feelings of dread, apprehension  Palpitations, chest pressure, dizziness  May be chronic, related to chronic illness, home, school, work

3  May be episodic, related to acute illness, death, loss of employment, taking a test ◦ “Situational anxiety” is a natural, adaptive response – can motivate to problem solving and coping activities, prepare a person to meet a challenge ◦ Remember, “anxiety” is a normal, human response ◦ “anxiety disorder” is where we see drug therapy employed

4  When does anxiety become “disorder” and require treatment? ◦ no clear line ◦ generally, when anxiety becomes long term (months) and impairs person’s ability to successfully function in school, work, home, it’s termed “anxiety disorder” ◦ ~18% incidence in US

5  Types of anxiety disorder ◦ GAD – generalized anxiety disorder  DSM-IV – excessive worry over two or more circumstances with multiple sx for ≥ 6 mos  symptoms include motor tension, restlessness, fatigue, over-activity of ANS (dyspnea, palpitations, diaphoresis, tachycardia, xerostomia, nausea, diarrhea)  can be triggered by/exacerbated by SNS stimulating drugs:  decongestants, beta-2 agonists, nicotine, caffeine

6  Types of anxiety disorder ◦ SAD – social anxiety disorder  excessive concern in social situations regarding rejection, “saying the wrong thing”, etc.  often irrational concern they will be humiliated or embarrassed ◦ Panic disorder  sudden, acute attacks of anxiety  intense fear, terror, impending doom  symptoms include SOB, palpitations, tachycardia, nausea  usually last 1-10 minutes  dx requires ≥ 1 month of worry about another attack

7  NE – excitatory  GABA – inhibitory ◦ gamma aminobutyric acid ◦ major inhibitory neurotransmitter in CNS  when GABA receptors are stimulated, the nerve terminal is less likely to “fire”  Serotonin – role in anxiety response?  Anxiety = “imbalance” of these neurotransmitters? ◦ over-simplistic, but does relate to the way we treat the disorder

8  Sleep latency ◦ the period of drowsiness before sleep, ~ 30 min  Sleep (75% deep, 25% REM) ◦ stages I, II – early sleep ◦ stages III-IV – deep sleep  physically restorative ◦ REM – post stage 4  mentally and emotionally restorative  deprivation can lead to serious psychological problems  Insomnia – altered sleep pattern ◦ increased sleep latency, decreased deep sleep

9  Benzodiazepines ◦ Modulate GABA  non-benzodiazepines ◦ Modulate NE, serotonin, dopamine  SSRI’s (selective serotonin reuptake inhibitors) ◦ Modulate synaptic serotonin levels  TCA’s (tri-cyclic antidepressants) ◦ Modulate serotonin, NE  barbiturates

10  Uses ◦ acute anxiety ◦ generalized anxiety (second line) ◦ insomnia (short term!) ◦ pre-operative sedation/anxiety ◦ alcohol withdrawal ◦ seizures ◦ critical care sedation

11  Bind to GABA receptors and intensify the effect of GABA ◦ resulting in neuronal inhibition  Main difference between BZD’s is onset and duration of effect

12  Some SHORT acting BZD’s ◦ triazolam (Halcion) – 30m onset, 2h duration ◦ oxazepam (Serax) – 3h onset, 4+ h duration ◦ midazolam (Versed) – 30m onset, 3h duration  Some INTERMEDIATE actings BZD’s ◦ alprazolam (Xanax) – 6-12h duration ◦ lorazepam (Ativan) – 6-12h duration ◦ temazepam (Restoril) – 8-20h duration

13  Some LONG acting BZD’s ◦ clorazepate (Tranzene) ◦ chlordiazepoxide (Librium) ◦ diazepam (Valium) ◦ flurazepam (Dalmane) ◦ clonazepam (Klonopin)

14  BZD’s typically used for anxiety ◦ alprazolam ◦ chlordiazepoxide ◦ clonazepam ◦ clorazepate ◦ diazepam ◦ lorazepam ◦ oxazepam

15  BZD’s typically used for sleep ◦ 3-4x per week for a few weeks only! ◦ estazolam (Prosom) ◦ flurazepam (Dalmane) ◦ temazepam (Restoril) ◦ triazolam (Halcion)  BZD’s typically used for muscle relaxing effects ◦ Diazepam (the only FDA approved benzo for skeletal muscle spasms )  BZD’s typically used for procedure related sedation ◦ Midazolam ◦ Diazepam ◦ Lorazepam

16  BZD’s indicated for seizure disorder ◦ Onfi (clobazam) ◦ Diazepam ◦ Clonazepam ◦ Clorazepate ◦ Lorazepam (for status epilepticus)

17  Adverse effects ◦ tolerance  considerably less risk of tolerance/dependence than barbiturates  can develop after weeks of therapy, usually much more prominent re: sedative effects than anxiolytic effects  WEAN dose slowly when D/C’ing to avoid rebound insomnia  Withdrawal symptoms seen if D/C’d too quickly

18  Adverse effects ◦ sedation  often cause daytime sleepiness, but effects diminish after a week or two of therapy  can cause sleep related behaviors that pt does not remember  sleepwalking, eating, driving ◦ no respiratory depression at therapeutic doses ◦ overdose: unlikely to cause death except at extreme doses  symptoms: respiratory depression, coma

19  Adverse effects ◦ withdrawal  usually occurs 1-2 days after the last dose of short acting, 5-10 days after last dose of long acting  resembles withdrawal of other CNS depressants  severe withdrawal can occur after abrupt D/C of high doses after 4 months of therapy  prevention: taper by 10% per week ◦ pregnancy/lactation  contraindicated! ◦ geriatrics  caution! (BEERS list drug)  risk of sedation and falls

20  Reversal ◦ flumazenil (Romazicon)  given rapid IV injection (usually into IV line in large vein)  compete with BZD’s for GABA receptor  reverses sedation within minutes  but NOT respiratory depression  very short duration, repeat doses may be needed every 45 seconds  Caution! pt may awaken suddenly with agitation and even seizures

21  buspirone (Buspar) ◦ Not chemically or pharmacologically related to BZD or barbiturates ◦ No anticonvulsant or muscle relaxant effect ◦ No prominent sedative effect ◦ 5-HT 1a agonist (serotonin agonist) ◦ Moderate affinity for D 2 receptors (antagonizes) ◦ Increases adrenergic neuron firing ◦ No affinity for BZD receptor and no effect on GABA ◦ Indicated for short term tx of anxiety only

22  buspirone (Buspar) ◦ takes weeks for optimal effect ◦ does not potentiate the effects of opioids/EtOH ◦ does not cause dependence ◦ not a controlled substance ◦ usually USELESS if follows BZD therapy

23  SSRI’s / SNRI’s ◦ Most have been shown to be effective in GAD and/or SAD  TCA’s ◦ Effective as other antidepressants, but more adverse effects  Anticholinergic adverse effects

24  zolpidem (Ambien® & Ambien CR)  zaleplon (Sonata®)  eszopiclone (Lunesta®)  ramelteon (Rozerem®)  trazodone  “PM” OTC drugs contain…. ◦ ?

25  zolpidem (Ambien® & Ambien CR) ◦ interacts with BZD/GABA receptor complex ◦ approved only for the short term treatment of insomnia  7-10 days  very often used beyond that time frame ◦ decreases sleep latency (how long it takes to fall asleep) ◦ decreases nighttime awakenings ◦ some dependence risk (CIV)  UPDATE: the FDA has just announced it is requiring zolpidem manufacturers to recommend half the currently used dose ◦ studies show many patients (especially women) have serum concentrations of zolpidem in the AM high enough to impair driving  39 million Rx’s for zolpidem in 2011

26  zaleplon (Sonata®) ◦ similar to zolpidem, shorter onset and duration  eszopiclone (Lunesta®) ◦ similar to zolpidem, FDA approved for longer term treatment of insomnia ◦ T 1/2 longer than zolpidem  ramelteon (Rozerem) ◦ metatonin receptor agonist ◦ does not work as well as zolpidem etc. especially re: sleep maintenance ◦ appears safe for long term use, no dependence risk

27  trazodone ◦ this and other antidepressants with anticholinergic side effects are used for insomnia, but most cause next day sleepiness and xerotomia ◦ no dependence risk


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