1- Sedative-Hypnotics and Anxiolytics Flashcards
What is the primary use of sedative-hynotic and anxiolytic drugs?
Encourage calmness and produce sleep
GABA is the major inhibitory NT. Activation of it leads to what effect on the body?
Decreased anxiety and promotion of sleep
depression of electrical activity/ CNS depressant
HA, palpitaions, tremor, perspiration, GI effects and dizziness are manifestation of what class of disorders?
Anxiety disorders
What is a maladaptive response in a person w/ an anxiety disorder?
Chronic and psychological stress, organ dysfunction, physical sxs
What is the “ideal drug” for treating an anxiety disorder?
Relieves anxiety w/o sedation/ drowsiness, no physical/ psychological dependence
What is the tx for acute anxiety disorder (short term and self limited) vs generalized anxiety disorders (chronic)?
Acute- benzodiazepines
Generalized- benzodiazepines/ buspirone
What is the tx for anxiety in children and adolescents?
Antidepressants
What is the tx for panic disorder/ agoraphobia (episodic, severe attacks)?
SSRIs
What is the tx for OCD?
SSRIs
What is the tx for PTSD?
Antidepressants
What an “ideal” drug to tx insomnia?
Sedative hypnotic → fall asleep quickly and stay asleep for as long as want, wear off in the AM, no “hangover” effect
What is the tx for transient or short-term insomnia (occurs w/ situational stress)?
Sedative hypnotics
What is the tx for long-term insomnia (related to underlying psychiatric disease or chronic alcohol/drug abuse)?
Behavioral therapy and lifestyle changes
What is the tx for hypersomnia and narcolepsy?
Stimulants
Kleine-Levin Syndrome is aka what and falls under what class of disorders?
AKA: “Sleeping beauty”, sleep disorders
What is the DOC for enureisis?
Tricyclic Antidepressants
What is the tx for sleep apnea?
CPAP and lifestyle changes
What is the MOA for barbiturates?
Bind to GABAA receptor to produce Cl influx and inhibition independent of GABA
Why are barbiturates abuses?
Causes feelings of euphoria
Do barbiturates cross the BBB?
Yes
Where are barbiturates metabolized? What do they induce?
Liver, induce CYP450s (LOTS of drug interactions)
What are the SEs for barbituates? (7)
CNS depression (toxic doses) Paradoxical excitement Severe dependence (psych + phys) Vertigo N/V/D Allergic rxn Respiratory depression
When are barbiturates C/i? (2)
Porphyria, in combo w/ alcohol (supra-additive effects)
Withdrawal from what medication will cause severe sx of restlessness, anxiety, weakness, seizure, but is not fatal?
Barbiturates
Do barbiturates have a ceiling effect? Why? What does this mean for its margin of safety?
No, b/c functions independently of GABA. LOW margin of safety
Coma, espiratory depression and hypotension are overdose sx of what medication?
Barbiturates
What is the tx for barbiturate overdose?
Supportive care, diuresis, alkalization of the urine
What drug class is Thiopental?
Barbiturates
What is the duration of action for Thiopental?
Short acting
What is Thiopental used for?
Induction of anesthesis
What drug class is Phenobarbital?
Barbiturates
What is the duration of action for Phenobarbital?
Long acting
What is Phenobarbital used for?
Used as anticonvulsant to tx partial and generalized tonic-clonic seizures
What is the MOA for benzodiazepines?
Bind to GABAA receptor, ↑ affinity of receptor to GABA prolonging its actions (effect dependent on GABA)
Do Benzodiazepines have a ceiling effect?
Yes! (limited GABA pool = effect plateaus once all GABA is used up despite an ↑ dose)
How are benzodiazepines metabolized?
CYP3A4 in liver
When are IV benzodiazepines used?
Emergencies, pre-anesthesia
What are the SEs for benzodiazepines? (3)
CNS depression (toxic doses), paradoxical excitement (dis-inhibition of suppressed behavior), sleep-related behaviors (sleep driving, eating, walking, etc)
When are benzodiazepines C/i? (4)
pregnancy, sleep apnea, elederly (can’t metabolize well), w/ alcohol use (supre-additive effects),
Tolerance to benzodiazepines is common. What effect does this have on dose and abuse potential?
Doses are not typically increased. High abuse potential
What are the effects of abrupt cessation/withdrawal of benzodizepines? (7)
Rebound ↑ anxiety and insomnia, muscle weakness, tremor, hyperalgesia, vomiting, weight loss, convulsions
What is the recommendation for stopping chronic benzodiazepine use?
Taper very slowly
What are the sx of a benzodiazepine OD?
Long deep sleep (24-48 hrs). Overall drug is relatively safe.
Possible fatality from a benzodizepine OD can occur in what populations?
People w/ respiratory difficulties, children, combine w/ alcohol
When prescribing a benzodiazepine. What is the general recommendation for dose and duration?
Lowest effect dose for shortest possible duration (to limit SE)
What is a general SE of drugs used to tx insomnia?
Minor depression of REM sleep → “hangover” effect