Anxiolytics Flashcards

1
Q

Anxiolytic

A

A drug that reduces anxiety without causing significant sedation

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2
Q

Depressant

A

General term for any drug that slows or reduces CNS activity, drugs can belong to different pharmacologic classes

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3
Q

Sedative

A

Drug used to relax, calm, or tranquilize

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4
Q

Hypnotic

A

Drug used to induce sleep

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5
Q

Barbiturate

A

Class of prescription drugs used to sedate, reduce anxiety and general anesthesia

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6
Q

Benzodiazepine

A

Class of prescription drugs used to sedate, reduce anxiety and reduce muscle tension

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7
Q

Non-barbiturate/Non-benzodiazepine

A

Prescription drugs from different classes used to sedate, promote sleep and reduce anxiety

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8
Q

Inhalants

A

Chemicals that depress CNS function via inhalation, many are household products

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9
Q

Barbiturate

A

High potential for abuse/dependence
Often paired with anphetamines in 1940s
Low therapeutic index
Several still in use today

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10
Q

Onset and Duration Barbiturate

A

Ultra Short(Methohexital) .2 min onset, .25 hour duration
Short(pentobarbital) 15 minute onset, 2-3 hours
Medium (Aprobarbital) 30 minute onset, 5-6 hour duration
Long, (mephobarbital) 60 minute onset, 6-10 hour duration

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11
Q

Mechanism of Action

A

Potentiate the effects of neurotransmitter GABA
Enhance binding to GABA receptor
Barbiturate binding sites are near GABA binding sites
Inhibits release of excitatory neurotransmitter
Higher doses mimic the effects of GABA
Lead to profound CNS depression and reduced respiration
Paradoxical stimulation of CNS at low doses due to suppression of inhibitory brain systems

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12
Q

Barbiturate Effect on CNS

A

Low dose: euphoria, sense of well being, greater self esteem, increased feelings of confidence, increased talking and social acceptability
Moderate Dose: Sedation and sleep
Higher Dose: Surgical Anesthesia
Overdose: Coma

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13
Q

Barbiturate Pattern of Use and Abuse (General)

A

Oral administration most common route
Pentobarbital (yellow) and secobarbital(red) are preferred
Older adults
Original contact may be via prescription for insomnia or anxiety
Patterns range from infrequent sprees of gross intoxication lasting a few days to prolonged compulsive daily use
- Hover around 19% of population
- Taken by opiate dependent individuals trying to boost heroine- use frequent enough to develop tolerance to both drugs which complicates treatment
Alcoholics use it to relieve from withdrawal

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14
Q

Barbiturate Use and Abuse Types

A

Adults
Obtain prescription for anxiety or insomnia
Develop tolerance, get higher dose–> physical dependence
Get prescription from multiple physicians to hide abuse
don’t refer to themselves as abusers
Young Adults
Diverted prescription meds to get high
Typically take at large doses with ethanol
Thriving black market
Frequency of use is episodic, so dependence does not always occur
Acute toxic reactions are frequent

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15
Q

Metabolic Tolerance- Barbiturate

A

Increase liver enzymes that metabolize barbiturates, shortens duration but does not induce need for higher doses

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16
Q

Pharmacologic Tolerance- Barbiturate

A

Reduced sensitivity to direct effects on neurons resulting in lowered CNS, respiratory and toxic effects, dose must be increased to achieve original response

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17
Q

Cross Tolerance- Barbiturate

A

Tolerance to lethal effects does not occur

Cross tolerance is complete with many CNS depressants, including alcohol

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18
Q

Dependence- Barbiturate

A

Like alcohol
Onset of withdrawal depends on half-life
Tremors, hallucinations, convulsions, delirium
Withdrawal can be fatal

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19
Q

Benzodiazepine Clinical Use

A
Anxiety Disorder
GAD, acute anxiety, panic disorder, social phobia, PTSD, OCD
Anxiety Illness
cardiovascular, GI, chemotherapy
Insomnia
Convulsive, spastic, involuntary movement
Detoxification
Pre-surgical anesthetic
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20
Q

Benzodiazepine Half Lives

A
Anxiolytics
Clorazepate- 2
Oxazepam- 8
Chlordiazepoxide-10
Alprazolam- 12
halazepam- 14

Anticonvulsant
clonazepam- 23

Hypnotic
midazolam-2 
triazolam- 3
estazolm- 10 
temazepam- 11

Preanesthetic
midazolam-3

21
Q

Benzodiazepine Mechanism of Action

A

Potentiate the effects of GABA
Binding sites near GABA binding sites
Self-limiting effect, so toxicity is low
Affect neurons at all levels, including CNS and muscles
Increases the flow of Cl- ions into the cell

22
Q

Benzo effect at different doses

A

Low- Reduces anxiety, not general depressant
Moderate- Light headedness, lassitude, increased reaction time, sedation
High- Motor incoordination, relaxed muscle tone, impaired mental function, confusion, sleep
Higher- anteretrograde, amnesia

23
Q

Benzo Use and Abuse

A

Similar to barbiturate
Only short acting alprazolam and highly lipophilic diazepam are abused
Taken with other drugs
Take the edge of the fear of trying other drugs
Animal models- Barbiturates more self administered than benzos
Most commonly mentioned in combination with another drug
Perceived as reinforcing, but generally only by experienced sedative users/abusers
naive subjects don’t like the effects
Schedule IV

24
Q

Benzo Tolerance

A

Similar to barbiturate, except benzo does not stimulate its own metabolism
Develops to all CNS effects except to memory disturbances
Tolerance to sedative effects quickly

25
Q

Benzo Dependence

A

Similar to benzo but less severe
Convulsions can occur, but are rare
Withdrawal symptoms– similar to anxiety so difficult to document
Receptor antagonist can precipitate withdrawal

26
Q

Anxiety

A

Cardinal symptom of many psychiatric disorders, but frequent component of medical/surgical procedures
Emotion that allied with fear is adaptive
Separate acute episode-dependent anxiety from non specific disease-driven anxiety, drugs better at treating the former
Treatment should be limited in duration

27
Q

Insomnia

A

Treated carelessly
Prescribing drugs without knowing what causing the insomnia puts patient at risk for abuse
Behavioral therapy, psychotherapy or nonhypnotic drugs may be superior to hypnotics when there is a specific cause
If transient in nature, use may be satisfied
- Administer no more than every third night to avoid abuse

28
Q

Other Insomnia Agents

A

Ambien, Sonata and Lunesta
Non benzo used for short term management for insomnia
Little occurrence of tolerance or rebound insomnia
Schedule IV

29
Q

Inhalants: Definition and Type

A

Breathing in chemical vapors to get high
Common Home or Workplace Products
Adhesive, Aerosols, Anesthetics, Cleaning Agents, Volatile Solvents and gases, erosol whipped cream canisters, room deodorizers

30
Q

Volatile Solvents

A

Gases or liquids that vaporize at room temperature

ex. paint thinners, nail polish removers, degreasers, felt tip markers, adhesives, glue

31
Q

Aerosols

A

Sprays that contain solvents and propellants

spray paint, hair spray deodorant spray, fabric protector spray

32
Q

Gases

A

Found in household/commercial products as well as anesthetics
ex. butane lighters, propane tanks, refrigerant gases, ether, chloroform, halothane

33
Q

Nitriles

A
Special class used primarily as sexual enhancers
ex. Vasodilators, smooth muscle relaant
Amyl nitrile packaged in ampules commonly known as "poppers" and are highly flammable
Butyl nitrite found in video head cleaner, room odorizer, leather cleaner
34
Q

Scope fo Abuse

A

Primarily abused by boys 10-15
adolescents between 12-17
Adults exposed at work place can also abuse
Abuse increasing, especially among isolated Native American and Hispanic populations
Products readily available and inexpensive
Other countries now experiencing problems
Most tried drug of abuse in 8th grade

35
Q

Inhalant Use

A

Directly from container to nose
From a soaked rag through the mouth
From a soaked bag
From inside a balloon
Inhalation continues until desired effects, few minutes
Leads to unconsciousness, relax grip on bag, and let fall away so that individual breaths again
Both solo and group sniffing bags, bags are sometimes shared

36
Q

Pattern of Abuse- Inhalant

A

Typically episodic in nature following fads
“Huffing”- through mouth
“Sniffing” through nose
Semiliquid products placed in bags and held over mouth and nose,
Heating increases the concentration
Gas sprayed onto cloths , propellants separated from particulates

37
Q

Access of Inhalant

A
  • Products are widely available, accessible, inexpensive to use and legal
    Warning labels alert individuals to potentially new sources
    Isolated pockets of abuse can grow quickly if overreact in the media
38
Q

Inhalant Pharmacology

A

General CNS depressant, but can stimulate at low doses

Onset of action and duration of action typically short

39
Q

Effects- Inhalant

A

Immediate effects are euphoria, giddiness,, ataxia, slurred speech, perceptual distortions
Effects last 15-45 minutes after sniffing ends
Drowsiness and stupor last for 1-2 hrs

40
Q

Tolerance- Inhalant

A

Many anecdotal reports exist

Unknown if cross tolerance exists

41
Q

Dependence Inhalant

A

No evidence for physical dependence,
unlikely because short duration of action
- If exists, similar to barbiturates and ethanol

42
Q

Treatment for Abuse

A

No accepted treatment plan
Many centers refuse to treat because believe that abusers are resistant to treatment
Complex psychosocial, economic and biophysical issue, longer time periods are needed for treatment
- No support from insurance for treatment

43
Q

Nitrous Oxide

A

Lauging gas
Colorless, non-flammable gas with slight sweet odor
Currently used in surgical procedures as well as minor dental procedures
Thought of as a minor anesthetic
reports of use on a small scale since 1971
Most used by inhaling from balloons or plastic bags
Generally pleasant effects, but short lived
Cognitive deficiencies were noted during high

44
Q

Nitrous Oxide- Mechanism of Action

A

Not completely understood
Most likely modulates ion channels
Blocks NMDA and acetylcholine regulated channels
May inhibit GABAc and 5-HT receptors
May slightly potentiate GABAa and glycine receptors
Anxiolytic effect- GABA a
Analgesic Effect- endogenous opioids and noradrenergic
Euphoria- mesolimbic pathway via antagonizing NMDA receptors that hten increase dopamine release in ventral tegmentum and nucleus accumbens

45
Q

Nitrous Oxide Time Course

A
Effects perceived at 10% concentration
Deprives brain of oxygen
At 100%, experience sense of well-being, "high"
Difficultly maintaining balance
Slow to answer questions
Low response to pain, noise and speech
Lapse into unconsciousness
Breathing reflex is surppressed for a few seconds
Can be fatal very quickly
46
Q

Nitrous Oxide Methods

A

Crackers: 2’ metal or plastic cannisters filled with pure N2O
Whip Its: Small cartridges used for dispensing whipped cream, discharged into a balloon and then inhaled
Tanks; Either medical grade or autoracing grade tanks, 20 pounds
Charging Bottles: similar to seltzer bottles

47
Q

Nitrous Oxide- Long Term Toxicity

A
Nitrous oxide binds with oxygen in body
Results in vitamin B12 deficiency
RBC count is lowered anemia
Nerve degeneration can occur, results in
pain in arms and legs, unsteady gait, irritable, cognitive deterioration
Severe headaches
Rashes in nose and mouth
Weight loss
Red eyes, glassy eyes
Menstrual disorders
Night sweats
48
Q

Inhalant Effects on Brain

A

Atrophy of cerebral, cerebellar and brainstem white matter, resulting in dementia
Chronic use can lead to neuropsych deficits, such as impairments in processing speed, attention, memory retrieval, language and executive function
Consisten with white matter pathology

49
Q

Sudden Sniffing Death Syndrome

A

Most common form of acute death
Can occur after only 1 use
Precipitated when startled- causes a burst of epinephrine that can cause fatal cardiac arrythmia

Death by aspiration, accidental trauma while under the influence, or suffocation