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anxiety
A vague, uneasy feeling, the source of which is often nonspecific, or unknown to the individual
feeling of fear or dread
tremors and palpations
sweating
faintness
Symptoms of HPA axis
Defining characteristics of anxiety: [5]
De-realization
KNowing you are in a situation but it doesn’t feel like its happening to you
insomnia
Inability to sleep or remain asleep throughout the night
hypersomnia
too much sleep. Seen in teenage and young adults.
Parasomnia
Disorders associated with the sleep stages
sleep-wake schedule disorders
Normal sleep but at the wrong time
Breast cancer
females who work permanent night shifts are at increased risk for what?
the elderly. usually related to a medical condiitonthe
Most people diagnosed with insomnia are:
Benzodiazepines.
the drug of choice for anxiety and insomnia
has a large therapeutic index when used by themselves
Therapeutic range of benzodiazepines:
Diazepam (Valium)
Prototype drug for anxiety
GABA
Inhibitory neurotransmitter located throughout the CNS
Not direct agonists but amplifies the actions of endogenous GABA in limbic and cortical areas of the brain.
Benzodiazepines MOA:
Opens chloride channels
hyperpolarizes cell
slows firing in CNS to decrease anxiety
Diazepam (Valium) MOA:
Decreases neuron firing
How are benzodiazepines used for seizures?
general anesthesia
pre-op sedation
muscle spasms
panic disorders
withdrawal from alcohol
other clinical uses of benzodiazepines: [5]
Anterograde amnesia
blocked recall of events
drowsiness
lack of coordination
difficult concentrating
anterograde amnesia
paradoxical effect
respiratory depression
headache
nausea
adverse responses of benzodiazepines: [8]
orally, highly lipid soluble '
crosses the blood-brain-barrier
can be given IM or IV as well
How are benzodiazepines given (pharmacokinetics): [3]
Extensively metabolized.
half life is 2-3 hours but active metabolites is 50 hours
Metabolism of benzodiazepines:
Triazolam (Halicon): has a rapid onset
Recommended benzodiazepine for falling sleep:
Estazolam (ProSom): slower onset
Recommended benzodiazepine to avoid waking:
Lorazepam (Ativan)
Recommended benzodiazepine for anxiety with an intermediate duration:
Flumazenil
antidote for benzodiazepines. similar to naloxone:
Signs of drowsiness, lethargy, confusion.
Symptoms of benzodiazepine toxicity (rare): [3]
other CNS depressants (other benzos)
alcohol
Benzodiazepine interactions that can cause drug toxicity: [2}
use cautiously in suicidal patients
do not crush or chew sustained release
do not use alcohol or other CNS depressants
Warnings for benzodiazepines: [3]
Phenobarbital
non-selective barbiturate usually used for seizures
Acts as direct GABA agonist. MORE GABA
No limits on CNS depression, stimulates drug metabolizing enzymes
Phenobarbital MOA:
depressed mood
loss of pleasure or interest in all or nearly all past activities or pastimes
Diagnostic criteria for depression (some): [2]s
shock therapy
ECT
Somatic depression therapies: [2]
initial response in 1-3 weeks
maximal response may not be until 12 weeks
How long do depression pharmacotherapies take to work?
Selectively blocks the reuptake of serotonin
causing increased activation of post-synaptic receptors
Selective Serotonin reputake inhibitors (SSRIs) MOA:
MAOIs
SSRIs should not be used with what due to the risk of serotonin syndrome?
Serotonin syndrome
Altered mental state related to serotonin. Jitters, sweating, hallucinations, etc.
Fluoxetine (prozac)
Major depression SSRI that is widely distributed and highly bound to plasma protein
4 weeks
How long does it take for prozac to reach steady state plasma levels?
Well absorbed orallyO
how is prozac absorbed?
Citalopram (Celexa)
Paroxetine (Paxil)
Other examples of SSRIs: [2]
Causes powerful blockage of NE and serotnin reuptake
Keeps more epinephrine and serotonin in the brain (very similar to SSRIs)
Serotonin/Norepinephrine Reuptake inhibitors (SNRIs) MOA:
nausea
headache
sexual dysfunction
Adverse effects of Venlafaxine (Effexor) [3]
Venlafaxine (effexor)
SNRI prototype drug:
Blocks neuronal reuptake of norepinephrine and serotonin
among first antidepressants, not as safe as newer ones
Tricyclic antidepressant MOA:
can cause cardiac toxicity
Key danger of tricyclic antidepressants:
Amitriptyline (Elavil)
Tricyclic antidepressant prototype:
sedation
orthostatic hypotension
cardiac toxicity
Adverse effects of Amitriptyline (Elavil): [3]
bipolar syndrome
fibromyalgia
neuropathic pain
Other uses for amytryptiline (elavil) besides depression:. used as an adjunct medication [3]
biochemical effects occur within hours; therapeutic effects take several weeks
How long do the effects of amytryptiline (elavil) take to work?
8 times the therapeutic dose. Overdose can be life threatening.
lethal dose of amytryptiline (elavil)
Should not be combined with other drugs that cause CNS depression because this one causes CNS depression
amytryptiline (elavil) drug interactions:
Monoamine oxidase
enzyme that breaks down serotonin
inhibits the enzyme that breaks down serotonin
MAOI MOA:
Isocarboxazid (Marplan)
MAOI prototype:
they can cause hypertensive crisis, triggered by eating foods rich in tyramine
MAOIs are more dangerous antidepressants becuase:
mirtazepine (Remeron)
Buproprion (Zyban)
Atypical antidepressants [2]
Weight gain, the drug increases appetite
Mirtazepine (Remeron) side effect:
acute dystonia
parkinsonism
akathisia
tardive dyskinesia
First generation antipsychotics adverse effects:
Dystonia
Spasms of the back and neck
Parkinsonism
Parkinson-like sympoms including shuffling gat
Akathisia
uncontrolled need to be in movement
Chlorpromazine
Low potency first generation antipsychotic:
Haloperidol (Haldol)ot
high potency first generation antipsychotic:
neuroleptic malignant syndrome
orthostatic hypotension
anticholinergic effects
sedation
neuroendocrine effects
seizures
sexual dysfunction
agranulocytosis
severe dysrhythmias
other adverse effects of first generation antipsychotics: [9]
Blocks neurotransmitters (dopamine, NE, serotonin etc.)
First generation antipsychotic MOA:
increases risk of sedation
risk of CNS depressants and first gen antipsychotics interacting:
levodopa increases dopamine and cancels out antipsychotic
levodopa and first gen antipsychotic interaction:
Blocks receptors for dopamine and serotonin
Second generation antipsychotic MOA:
Clozapine (clozaril)
prototype second gen antipsychotic
agranulocytosis (can be fatal)
metabolic: weight gain, exaccerbates diabetes, dyslipidemia
seizures
EPS
Myocarditis
orthostatic hypotension
second generation antipsychotic adverse effects: [6]
pure manic episode (euphoric mania)
hypomanic episode (hypomania)
major depressive episode (depression)
mixed episode
types of bipolar episodes: [4]
mood stabilizers
antipsychotics
antidepressants
drug therapies for bipolar: [3]
lithium
divalproex sodium (Valproate)
Carbamazepine (Tegretol)
Mood stabilizers: [3]
Altered distribution of cerain ions (magnesium, sodium, calcium)
altered synthesis and release of NE, serotonin and dopamine
effects on second messengers (e.g. Cyclic AMP)
Lithium MOA:
Very narrow, requires lots of monitoring
Litium therapeutic range:
well absorbed orally
even distribution
short half life
excreted by kidneys
Litium pharmacokinetics: [4]Adverse efe
mild:
1. ine hand tremor
GI upset
Thirst
muscle weakness
adverse effects of lithium at toxic levels[4]
tremor
polyuria
renal toxicityt
goiter and hypothyroidism
teratogenesisLiti
Adverse effects of lithium at therapeutic range:
diuretics promote sodium loss and increase the risk of lithium toxicity
lithium and diuretic drug interaction
NSAIDs can increase lithium levels by increasing renal reabsorption
lithium and NSAID drug interaction
Anticholinergic drugs can cause urinary hesitancy (lithium is salt based. can be uncomfortable)
lithium and anticholinergic drug interactions:
Alcohol use disorder
chronic, relapsing disorder with impaired control over drinking. Has preoccupation with alcohol consumption and distortions of thinking (denial of a problem)
Helps with delirium tremins. When withdrawing from anything, you get jittery. Benzos help.
Benzodiazepines for alcohol withdrawal:
prevents delirium tremins
How does tegretol treat alcohol withdrawal:
helps with the cardiovascular symptoms of withdrawal (vasoconstriction, increased HR, etc.)
Atenolol and propanolol (Beta blockers) for alcohol withdrawal:
carbamazepine (Tegretol)
Clonidine
Atenolol and propanololdrugs used to maintain abstinence from alcohol
Drugs used to facilitate alcohol withdrawal [3]
disulfiram (makes you sick)
naltrexone
acamprosate
drugs used to maintain abstinence from alcohol: [3]
changes receptors, don’t get same pleasure from drinking alcohol
how do maltrexone and acamprosate maintain abstinence from alcohol?
Nicotine Chewing Gum
Nicotine Lozenges
Nicotine Transdermal Systems (Patches)
Nicotine Inhaler
Nicotine Nasal Spraya-typical antidepres
Pharmacologic Aids to Stop Smoking [5]
Buproprion (Zyban)
atypical antidepressant that changes receptors and decreases the urge to smoke:
Verenicline (Chantix, Champix)
Partial agonist at nicotine receptors. Take te drug and smoke for two weeks, eventually it takes the pleasure away from smoking
Methadone (Methadose)
drug creates tolerance so that opioid drugs have little effect:
Opioid agonist
Methadone (Methadose) MOA:
Buprenorphine (Suboxone)
Drug that alleviates cravings/suppresses cravings for opioids
Opoid agonist-antagonist (agonist at some opioid receptors and antagonist at others)
Buprenorphine (Suboxone) MOA: