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What is the primary goal of sedative-hypnotic and antianxiety drugs?
Relax the patient promote normal sleep and decrease anxiety without excessive sedation
What neurotransmitter do benzodiazepines enhance? Inhibit?
Enhance: Dopamine, Serotonin, Norepinephrine
Inhibit: GABA
What is GABA?
The primary inhibitory neurotransmitter in the CNS
How do benzodiazepines reduce neuronal excitation?
By increasing chloride ion conductance through GABA-A receptors
What ion enters the neuron when GABA-A receptors are activated?
Chloride (Cl-)
What effect does increased chloride conductance have on neurons?
Hyperpolarization making action potentials harder to generate
What are sedative-hypnotics?
Drugs that cause excessive sedation and promote sleep
Name sedative-hypnotic benzodiazepines
Estazolam Quazepam Temazepam Triazolam
What are Z-drugs?
Not BZD, function similar for sedation
Zolpidem and Zaleplon
Are Z-drugs benzodiazepines?
No but they bind GABA receptors and increase chloride conductance
One advantage of Z-drugs over benzodiazepines?
Less rebound insomnia and fewer withdrawal problems
Which drug affects GABA but is not a benzodiazepine?
Eszopiclone
Which sedative-hypnotic works on melatonin receptors?
Ramelteon
What is anterograde amnesia?
Inability to remember events after taking the drug
What complex behaviors are associated with Ambien?
Sleepwalking and sleep-driving
How does alcohol interact with sedative-hypnotics?
It reinforces sedative effects
What is rebound insomnia?
Worsening sleep or anxiety after stopping the drug
Why are older adults at higher risk with sedative-hypnotics?
Falls cognitive effects and adverse reactions
Why should sedative-hypnotics be avoided in older adults?
They treat symptoms not causes and have significant adverse effects
Name non-drug strategies for anxiety and sleep
Exercise counseling relaxation reducing anxiety sources
What effect do anti-anxiety drugs have at higher doses?
Cause sedation and can act as sleeping pills
Common benzodiazepine anxiolytics
Diazepam Chlordiazepoxide Lorazepam Alprazolam
What class of drug is buspirone?
Azapirone
How does buspirone work?
Stimulates serotonin receptors in the CNS
One benefit of buspirone?
Less sedation and dependence
One drawback of buspirone?
Slow onset and moderate efficacy
Which patients benefit most from buspirone?
Older adults with mild anxiety
Why are antidepressants used for anxiety?
Anxiety often coexists with depression
Examples of antidepressants with anxiolytic effects
Paroxetine Venlafaxine
Advantage of antidepressants for anxiety?
Fewer side effects and less addiction risk
Alternative drugs used for anxiety
Quetiapine Gabapentin Antihistamines
How is depression defined clinically?
Incapacitating sadness with neurochemical changes
Current theory of depression?
Deficiency of CNS biogenic amine neurotransmitters
Which neurotransmitters are implicated in depression?
Norepinephrine dopamine serotonin
General drug strategy for treating depression?
Increase or prolong neurotransmitter effects
What does SSRI stand for?
Selective Serotonin Reuptake Inhibitor
Examples of SSRIs
Fluoxetine Paroxetine Sertraline Citalopram Escitalopram Fluvoxamine
What does SNRI stand for?
Serotonin Norepinephrine Reuptake Inhibitor
Examples of SNRIs
Desvenlafaxine Duloxetine Venlafaxine
What neurotransmitters do tricyclic antidepressants affect?
Serotonin norepinephrine epinephrine
Common naming feature of tricyclic antidepressants?
Often end in ine
Why are MAO inhibitors last resort drugs?
High risk of dangerous interactions and side effects
How do antidepressants increase neurotransmitter effects?
Inhibit reuptake or prevent breakdown
What percentage of neurotransmitters are recycled?
60 to 80 percent
What percentage are broken down by MAO?
20 to 40 percent
How do antidepressants affect BDNF?
They increase BDNF production
What is the role of BDNF?
Promotes hippocampal growth and synaptic connections
Major adverse effects of tricyclic antidepressants?
Sedation anticholinergic effects CV problems seizures fatal overdose
Major risks of MAO inhibitors?
CNS excitation hypertension stroke MI
Common SSRI and SNRI side effects?
GI problems and increased seizure risk
What causes serotonin syndrome?
Excessive stimulation of CNS serotonin receptors
Cardiovascular signs of serotonin syndrome?
Increased heart rate and blood pressure
Cognitive signs of serotonin syndrome?
Confusion hallucinations agitation
Musculoskeletal signs of serotonin syndrome?
Dystonia dyskinesia muscle pain shivering
Is serotonin syndrome reversible?
Usually but can be fatal if untreated
When do antidepressants start to work?
One to two weeks
When do antidepressants reach maximal effect?
Six to eight weeks
How does ketamine act as an antidepressant?
Blocks NMDA receptors and reduces glutamate activity
Why is ketamine not widely used?
Abuse potential and side effects
Which antidepressants are used off label for chronic pain?
Amitriptyline Amoxapine
Conditions treated with antidepressants for pain?
Fibromyalgia neuropathic pain headaches low back pain Raynauds
Classic treatment for bipolar disorder?
Lithium
How does lithium work?
Mood stabilizer that prevents manic episodes
Why is lithium dangerous?
Narrow therapeutic window and renal elimination
What lithium level is considered toxic?
Above 2 milliequivalents per liter
Other treatments for bipolar disorder?
Antiseizure drugs and antipsychotics