Anxiolytics Flashcards
Anxiolytic
A drug that reduces anxiety without causing significant sedation
Depressant
General term for any drug that slows or reduces CNS activity, drugs can belong to different pharmacologic classes
Sedative
Drug used to relax, calm, or tranquilize
Hypnotic
Drug used to induce sleep
Barbiturate
Class of prescription drugs used to sedate, reduce anxiety and general anesthesia
Benzodiazepine
Class of prescription drugs used to sedate, reduce anxiety and reduce muscle tension
Non-barbiturate/Non-benzodiazepine
Prescription drugs from different classes used to sedate, promote sleep and reduce anxiety
Inhalants
Chemicals that depress CNS function via inhalation, many are household products
Barbiturate
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
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
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 Insomnia Convulsive, spastic, involuntary movement Detoxification Pre-surgical anesthetic
Benzodiazepine Half Lives
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
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