Anxiolytics & hypnotics Flashcards

1
Q

Fear is

A

Described as short-term, stimulus-specific response.

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2
Q

Anatomical Localization of Fear

A

Basolateral, central, and medial nuclei of amygdala

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3
Q

Anatomical Localization of Anxiety

A

Basolateral amygdala projections to bed nucleus of stria terminalis

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4
Q

Anxiety is

A

Described as Sustained response influencing behavior after the stimulus is removed

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5
Q

Panic disorder is

A

a prevalent, debilitating illness associated with high utilization of multiple medical services, poor quality of life and a high incidence of suicide.

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6
Q

Panic disorder may lead

A

to anticipatory anxiety, which may induce a panic reaction or result in a related symptom of agoraphobia, here are high rates of comorbidity with other mood disorders and substance abuse.

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7
Q

Panic Disorder with or without

A

Agoraphobia

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8
Q

Needs to be addressed with pt’s with panic disorder

A
  • the patient’s catastrophic misinterpretation of panic symptoms, such as their beliefs that they may die or that the attacks produce physical harm
  • taught appropriate cognitive interventions
  • suggest and instruct in relaxation therapies; diaphragmatic breathing; positive self-talk; scheduling “worry periods,” when the patient is encouraged to focus on just one worry at a time, saving subsequent worries for another day; keeping logs, in order to look for triggering events; smoking cessation, exercise, the appropriate increase in pleasurable activities (such as spending time with others); and elimination of the use of caffeine, alcohol and illicit substances.
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9
Q

Treatment of panic disorder combines

A

cognitive-behavioral therapy, self-management techniques, and medications, including antidepressants and anxiolytic agents.

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10
Q

FDA-approved medications to treat Panic Disorder

A
  • Alprazolam (Xanax) and paroxetine (Paxil)
  • experience is showing the superiority of the selective serotonin reuptake inhibitors (SSRIs) and clomipramine (Anafranil) over benzodiazepines, monoamine oxidase inhibitors (MAOIs), and tricyclic and tetracyclic drugs in terms of effectiveness and tolerance of adverse effects
  • venlafaxine (Effexor), and buspirone (BuSpar) has been suggested as an additive medication in some cases, Venlafaxine is approved by the FDA for the treatment of generalized anxiety disorder and may be useful in panic disorder combined with depression.
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11
Q

Obsessive-compulsive disorders are set apart by an array of recurrent

A
  • obsessive ideas or compulsive actions that significantly interfere with daily functioning
  • Obsessions are persistent thoughts, images or impulses experienced as alien intrusions that must be neutralized or suppressed, e.g., obscene or blasphemous thoughts, repugnant sexual images, and unrealistic doubts about whether something has been done correctly
  • Compulsions are repetitive, purposeful behaviors performed in response to an obsession or according to certain rules.
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12
Q

abnormal brain structure and activity in patients with OCD, the abnormality apparently lies

A

mainly in a pathway that links the frontal lobes of the cerebral cortex with the basal ganglia.

MRI suggests a loss of tissue in the caudate nuclei, areas in the basal ganglia that filter messages, fails to dampen the obsessional thinking.

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13
Q

treatments for obsessive-compulsive disorder are

A

behavior therapy and medications

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14
Q

behavior therapy for OCD

A

Therapists may train the patient in “thought stopping” therapy (when the obsessive thought encroaches, the patient says “stop”) or saturation therapy (in which the client concentrates so intensely on the obsessive thought that it loses its compelling quality).

Unfortunately, patients usually relapse unless they go on taking the drug indefinitely. Compliance by patients can be a problem in that many patients with OCD are also reluctant to take drugs

patient with OCD will fare better if those surrounding them or their family do not tell them “just stop this behavior.” An expectation or statement about simply stopping the behavior usually only increases the anxiety for those with OCD.

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15
Q

medications 4 OCD

A

standard approach is to start treatment with a SSRI or clomipramine and then move to other pharmacological strategies if the serotonin-specific drugs are not effective. The serotonergic drugs have increased the percentage of patients with OCD who are likely to respond to treatment to the range of 50 to 70 percent.

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16
Q

specific drugs 4 OCD

A

fluoxetine/Prozac, fluvoxamine/Luvox, sertraline/Zoloft or paroxetine/Paxil.

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17
Q

PTSD

A

Often PTSD does not overtly present itself in patients who seek help.

Typically complaints are of a somatic nature or are comorbid with major depression or substance abuse.

In fact, PTSD is comorbid with another condition 80% of the time.

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18
Q

PTSD is

A

the injury that results from a traumatic event that overwhelms a person’s coping mechanisms. This event must meet two criterion: that the person has directly experienced the potentially life-threatening event and the person must have experienced extreme distress through fear, helplessness and/or horror

patient with PTSD re-experiences the event avoids situations that may cause a re-experiencing of the event and hyperarousal or hypervigilance related to the event.

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19
Q

treatments for PTSD,

A

sertraline (Zoloft) and paroxetine (Paxil), are considered first-line treatments due to their efficacy, tolerability, and safety ratings. SSRIs reduce symptoms from all PTSD symptom clusters and are effective in improving symptoms unique to PTSD, not just symptoms similar to those of depression or other anxiety disorders

Buspirone (BuSpar) is serotonergic and may also be of use.

efficacy of imipramine (Tofranil) and amitriptyline (Elavil), two tricyclic drugs, in the treatment of PTSD is supported by a number of well-controlled clinical trials

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20
Q

PTSD Nightmares:

A

Prazosin is used in psychiatry to suppress nightmares, particularly those associated with PTSD. In patients w/ PTSD, excessive adrenaline can cause nightmares. Prazosin blocks some of the effects of adrenaline. Prazosin is recommended as a first-line for nighttime PTSD symptoms like nightmares or sleep disturbances.

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21
Q

Benzodiazepines

A
  • the name is derived from their molecular structure.
  • Share a common effect on receptors that have been termed benzodiazepine receptors, which in turn modulate GABA activity.
  • GABA binds to GABAa receptor -> Increase of influx of CL-ions (Chloride) -> Hyperpolarization of neuronal cell membrane -> Decreased excitability
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22
Q

Pharmacological Effects Benzodiazepine

A

All benzodiazepines have anxiolytic effects
Can cause paradoxical hyperexcitability
Induction of sleep
Anterograde amnesia
Anticonvulsant Effect (Clonazepam as an antiepileptic / Diazepam in acute seizures)
Reduces muscle tone by a central action on GABAa receptors primarily in the spinal cord
In pre-anesthetic doses, decreases blood pressure and increases heart rate
Tolerance occurs with all benzodiazepines
Benzodiazepines vary greatly in the duration of action
Short-acting - better hypnotics with reduced hang-over effect upon wakening
Long-acting - better anxiolytics and anticonvulsant drugs
Withdrawal symptoms typically mimic those of anxiety disorders

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23
Q

“Z” compounds e.g. Zolpidem (Ambien), Eszopiclone (Lunesta)

A

Structurally unrelated to benzodiazepines
Act as agonists on the benzodiazepine site of the GABAa receptor
Tolerance and physical dependence are not as common as seen in benzodiazepine use
Lunesta is approved for long term use

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24
Q

Barbituates e.g. Phenobarbitol

A

High abuse potential and addiction potential
Narrow therapeutic range with low therapeutic index and unfavorable side effects
Use has been significantly minimized by use of benzodiazepines and hypnotics

25
Q

Buspirone

A

Anxiolytic medicine
Similar to that of benzodiazepines in anxiolytic effect
Acts as a partial agonist for serotonin 5-HT1a receptors in the brain
No physical dependence/withdrawal/abuse potential
Less sedation and psychomotor impairment
Lack of interaction with alcohol
Slow onset of action (1 - 2 weeks)
Requires BID - TID dosing due to t 1/2

26
Q

Melatonin Congeners e.g. Ramelteon

A

Melatonin 1 and 2 receptor agonist
Binds selectively to melatonin 1 and 2 receptors as a full agonist
Primary use is for insomnia - reduces time to sleep onset, increases total sleep time and may improve quality of sleep

27
Q

Clonidine - Antihypertensive; Centrally Acting Alpha 2 Agonist Off Label

A

Anxiety disorders, including PTSD and Social Anxiety)

28
Q

Propranolol - Beta Blocker-Off Label

A

PTSD, GAD, Violence/Aggressive Behavior

29
Q

Addiction

A

The state of response to a drug whereby the drug taker feels compelled to use the drug and suffers anxiety when separated from it

30
Q

Anesthesia

A

Loss of consciousness associated with absence of response to pain

31
Q

Anxiolytic

A

A drug that reduces anxiety, a sedative

32
Q

Dependence

A

The state of response to a drug whereby removal of the drug evokes unpleasant, possibly life-threatening symptoms, often the opposite of the drug’s effects

33
Q

Hypnotic

A

A drug that produces drowsiness and facilitates the onset and maintenance of a state of sleep that resembles natural sleep

34
Q

REM sleep

A

Phase of sleep associated with rapid eye movements; most dreaming takes place during REM sleep

35
Q

Sedation

A

Reduction of anxiety

36
Q

Tolerance

A

Reduction in drug effect requiring an increase in dosage to maintain the same response

37
Q

benzodiazepine metabolism

A
  • all except for 3 are converted to active metabolites in the liver (diazepine, flurazepam) and may accumulate over time and have more drug-to-drug reactions due to the cyp450 pathways
  • 3 benzos are conjugated outside the liver or by the process of glucuronidation ( lorazepam, temazepam, & oxazepam) so they have no active metabolites and they are rarely susceptible to drug-drug interactions
38
Q

Short-acting Benzodiazepines

A

Triazolam (Halcion),
Lorazepam (Ativan),
Diazepam (Valium),
Midazolam (Versed)

39
Q

Intermediate-acting Benzodiazepine

A

Alprazolam (Xanex)

40
Q

Long-acting Benzodiazepine

A

Flurazepam (Dalmane)

41
Q

Ultra-short acting Barbituates

A

Thiopental

42
Q

Short-acting Barbituates

A

Secobarbital

43
Q

Long-acting Barbituates

A

Phenobarbital (can be excreted in the urine unchanged)

44
Q

List of Benzodiazepines

A
  • Most common
    Chlordiazepoxide (Librium)
    Diazepam (Valium)
    Lorazepam (Ativan)
    Clonazepam (Klonopin)
    Alprazolam (Xanax)
    Temazepam (Restoril)
    Triazolam (Halcion)
    Midazolam (Versed)
  • not as common
    Oxazepam (Serax)
    Flurazepam (Dalmane)
    Halazepam (Paxipam)
    Clobazam (Onfi)
    Quazepam (Doral)
    Estazolam (Prosom)
    Clorazepate (Tranxene)
45
Q

List of Atypical Anxiolytics

A
  • More Common
    Buspirone (BuSpar)
    Zolpidem (Ambien)

-Less Common
Zopiclone (Imovane)
Eszopiclone
Zaleplon (Starnoc)
Chloral Hydrate
Ramelteon, tasimlteon
Suvorexart

46
Q

Atypicals have in common

A
  • Rapid metabolism by liver enzymes
  • Short duration of action
  • Used as sleep aids
47
Q

Benzo & Barbs dose-response on the CNS curve

A

From Sedation, anxiolysis -> Antiseizure activity -> Hypnosis spectrum -> Anesthesia -> Medullary depression -> Coma

48
Q

Benzo & Barbs dose-response on the CNS curve - Sedation/ Anxiolytics

A
  • At low doses both drugs can
  • Benzo used more frequent
49
Q

Benzo & Barbs dose-response on the CNS curve - Antiseizure activity

A
  • low doses of barbituates (phenobarbital)
  • high doses of benzo (lorazepamm, midalozam)
50
Q

Benzo & Barbs dose-response on the CNS curve - Hypnosis spectrum

A
  • benzo can induce sleep
  • REM is often reduced (fewer dreams)
  • Rebound effect: Hyper-REM sleep (nightmares)
  • Fewer side effects w/ newer agents
51
Q

Benzo & Barbs dose-response on the CNS curve - Anesthesia

A
  • Amnesia, suppressed reflex
  • Anterograde amnesia is common with benzos (date rape drug)
  • Anesthesia with most barbiturates (Thiopental - OR)
  • Short-term sedation w/ benzo (IV- Lorazepam or IV-Diazepam (ICU))
52
Q

Benzo & Barbs dose-response on the CNS curve - Medullary depression & Coma

A
  • Resp Depression
  • Hypotension
  • Cardiovascular Collapse
  • DEATH
53
Q

Anxiety is

A
  • normal, everyone experiences
  • Characterized by a diffuse, unpleasant, vague sense of apprehension, and often accompanied by autonomic symptoms such as headache, perspiration, palpitations, tightness in the chest, stomach discomfort, and restlessness.
  • Anxiety is also an alerting signal that warns of impending danger and enables a person to take measures to deal with a threat with a “flight or fight” reaction.
54
Q

Anxiety Symptoms (at the center or core)

A

*Excessive fear
*Excessive worry
*Anxiety

55
Q

When does anxiety become an anxiety disorder

A

The presence of anxiety is maladaptive and develops into an anxiety disorder

56
Q

Generalized Anxiety Disorder (GAD) Symptoms

A

Generalized worry
Generalized anxiety/ fear

affecting
Muscle Tension
irritability
sleep
concentration
fatigue
arousal

57
Q

Panic Disorder symptoms and affects

A

Worry about panic attacks
Anticipatory anxiety/ fear

affects
Phobic Avoidance Behavior change
Unexpected Panic Attacks

58
Q

Social Anxiety symptoms and affects

A

Worry about exposure