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Flashcards in Anxiolytics Deck (49):


A drug that reduces anxiety without causing significant sedation



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



Drug used to relax, calm, or tranquilize



Drug used to induce sleep



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



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



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



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



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


Onset and Duration Barbiturate

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


Mechanism of Action

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


Barbiturate Effect on CNS

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


Barbiturate Pattern of Use and Abuse (General)

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


Barbiturate Use and Abuse Types

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


Metabolic Tolerance- Barbiturate

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


Pharmacologic Tolerance- Barbiturate

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


Cross Tolerance- Barbiturate

Tolerance to lethal effects does not occur
Cross tolerance is complete with many CNS depressants, including alcohol


Dependence- Barbiturate

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


Benzodiazepine Clinical Use

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


Benzodiazepine Half Lives

Clorazepate- 2
Oxazepam- 8
Alprazolam- 12
halazepam- 14

clonazepam- 23

triazolam- 3
estazolm- 10
temazepam- 11



Benzodiazepine Mechanism of Action

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


Benzo effect at different doses

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


Benzo Use and Abuse

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


Benzo Tolerance

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


Benzo Dependence

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



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



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


Other Insomnia Agents

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


Inhalants: Definition and Type

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


Volatile Solvents

Gases or liquids that vaporize at room temperature
ex. paint thinners, nail polish removers, degreasers, felt tip markers, adhesives, glue



Sprays that contain solvents and propellants
spray paint, hair spray deodorant spray, fabric protector spray



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



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


Scope fo Abuse

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


Inhalant Use

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


Pattern of Abuse- Inhalant

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


Access of Inhalant

- 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


Inhalant Pharmacology

General CNS depressant, but can stimulate at low doses
Onset of action and duration of action typically short


Effects- Inhalant

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


Tolerance- Inhalant

Many anecdotal reports exist
Unknown if cross tolerance exists


Dependence Inhalant

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


Treatment for Abuse

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


Nitrous Oxide

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


Nitrous Oxide- Mechanism of Action

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


Nitrous Oxide Time Course

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


Nitrous Oxide Methods

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


Nitrous Oxide- Long Term Toxicity

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


Inhalant Effects on Brain

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


Sudden Sniffing Death Syndrome

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