anxiolytics and hypnotics Flashcards
what is anxiety and what about it?
Anxiety is an unpleasant state of tension, apprehension, or uneasiness (of unknown source)
Anxiety Is good for you Is a negative reinforcer Keeps us out of danger Motivates escape and avoidance Crucial for learning and memory Hard wired neural circuitry Innate, species specific, releasing stimuli
Anxiety has an inverted U-shaped effect on performance
Nucleus accumbens
Amygdala
what are the functions of emotions and their dysfunction in affective disorders?
- Emotion reflects the survival significance of incoming sensory data, directs memory formation and reinforces survival directed behavior
- Affective disorders are characterized by pathological inappropriate emotions and behavior, loss of contact with reality, inoperative reinforcement contingencies and the irrelevance of survival
what if the anxiety is inescapable or unavoidable?
What if the anxiety is inescapable or unavoidable?
“Escape” from anxiety by suppressing neural activity in the anxiety pathways
ethanol 35,000 years opium 5,000 years cannabinoids 3,000 years barbiturates 120 years benzodiazepines 60 years atypical 20 years What about people with physiological abnormalities in the anxiety pathways in their brains?
“Anti-depressant” drugs 5 years
anxiety disorders include?
Anxiety disorders include: Generalized anxiety disorder Panic disorder Obsessive-compulsive disorder Post-traumatic stress disorder Social phobia Social anxiety disorder Specific phobias
what is the DSM-IV criteria for GAD(greater than or equal to 3)? (watch for question on this)
DSM-IV criteria for GAD (≥3):
BE SKIM
Blank mind
Easily fatigued
Sleep disturbance Keyed up Irritability Muscle tension Toronto Notes 2012
what is the DSM-IV criteria for panic attack (≥4)?
DSM-IV criteria for panic attack (≥4):
STUDENTS FEAR the 3 C’s Sweating Trembling or shaking Unsteadiness, dizziness, light-headed Derealization or depersonalization Excessive heart rate, palpitations Nausea or abdominal distress Tingling (numbness ) Shortness of breath
Fear of dying, losing control, going crazy
3 C’s: Chest pain, chills or choking
Toronto Notes 2012
what is the anxiolytic, benzodiazepines like?
ANXIOLYTICS BENZODIAZEPINES Pharmacological effects Anxiolytic Hypnotic Anticonvulsant muscle relaxant Neurochemical effects increase GABA inhibition down-regulate benzodiazepine receptors up-regulate downstream receptors for NA, 5-HT, etc., increasing GABA reduces the release of NA, 5HT, etc., which up-regulates the receptors for NA, 5HT, etc. overdose of benzodiazepines is not lethal but benzodiazepines do potentiate the lethal actions of other compounds like alcohol and narcotics
You enhance the effects of GABA activity when you use benzodiazepines.
what do Beta-carbolines do?
β-carbolines also interact with the GABAA receptor at the benzodiazepine allosteric binding site
Decrease affinity of GABA for its binding site (inverse agonist)
No therapeutic use, but are found in nature (psychedelic plants)
what are the properties of some benzodiazepines? (look at this slide in the powerpoint)
complicated
what is tolerance and addiction (rebound vs. withdrawl)?
Tolerance and Addiction (rebound vs withdrawal)
altered receptor density produces tolerance, i.e., the neural system returns to its pre-drug level of functioning
effects of drug withdrawal after tolerance has developed is the exact opposite of the direct drug effects
withdrawal lasts until enough receptors have returned to their pre-drug state to maintain normal nerve impulse traffic
the withdrawal syndrome is more severe with short half-life drugs because all active drug molecules are eliminated before any receptors can return to pre-drug densities
what is benzodiazepine withdrawl?
Benzodiazepine withdrawal
is severe with short half-life drugs such as triazolam (T1/2 = 2 to 3 hours)
is the opposite of the direct drug effect i.e., anxiety, agitation, insomnia, convulsions, muscle tension and aches and pains
withdrawal is usually not a problem with long half-life drugs such as diazepam (T1/2 > 100 hours)
to discontinue a short half-life drug, switch patient to a comparable dose of a long half-life drug, and reduce the amount of drug given by 10% a week
what is an atypical anxiolytic?
ATYPICAL ANXIOLYTICS
Buspirone:
is not a benzodiazepine
acts as a partial agonist at serotonin 5HT1A inhibitory presynaptic autoreceptors
seems to be a selective anti-anxiety drug
lacks hypnotic, anti-convulsant or muscle relaxant effects
does not potentiate the respiratory depressant actions of alcohol, narcotics, etc.
little or no withdrawal syndrome
BUT: it takes 2 to 3 weeks for buspirone to have its antianxiety effects, most patients won’t wait that long
What is proranolol like?
Propranolol:
Β-adrenergic receptor antagonist
Treat performance anxiety
Suppress sympathetically-mediated somatic and autonomic symptoms
what is the definition of sleep disorders and the types?
Definition
Difficulty initiating or maintaining sleep, or waking up earlier than desired (leading to sleep that is chronically non-restorative/poor quality) despite adequate opportunity and circumstances for sleep
Impaired sleep produces deficits in daytime function
Types
Poor sleep hygeine – irregular sleep schedule, disruptive environment
Psychophysiologic insomnia –hyerarousal and escalating anxiety
Paradoxical insomnia – normal sleep demonstrated despite complaints of poor sleep
pure insomnia is rare
sleep is disrupted by environmental events, medical conditions, psychological stresses, etc.
sleep deficit is usually made up in a couple of nights
characteristic sleep anomalies in psychiatric disorders
- sleep apnea - periodic limb movement disorder
sleep is an active process of the brain
sleep stages - several EEG patterns
- slow wave sleep - fast wave sleep = REM
chemically induced sleep is not normal sleep
many drugs suppress REM sleep
during withdrawal, get REM rebound
hypnotic drugs are rarely needed but help in:
jet lag shift work bereavement
use only for 2 to 3 nights
what are some hypnotic agents?
Benzodiazepines triazolam, T1/2 = 2 to 3 hours temazepam, T1/2 = 8 to 10 hours Benzodiazepines triazolam, T1/2 = 2 to 3 hours temazepam, T1/2 = 8 to 10 hours
Atypical
zopiclone (Imovane), T1/2 = 5 hours
zolpidem (Ambien), T1/2 = 2 hours
Ramelteon – look-up
both are reported to have less effects on sleep EEG than the benzodiazepines, but still do not produce ‘normal’ sleep
(LOOK AT THE HYPNOTICS TABLE ON THIS SLIDE)
LOOK UP REMELTEON TO SEE MORE ABOUT THIS.
