First Flashcards
What are five causes of anxiety?
respiratory endocrine cardiovascular metabolic neurologic
What are the drugs that can cause anxiety?
stimulants
sympathomimetics
anticholinergics/antihistaminergic
dopaminergics
TCA is an example of a drug that can cause ____________
anxiety
Meperidine is an __________ derivative
opioid
*anticholinergic/antihistaminic
What does baclofen do?
relaxes the muscles
Baclofen, cycloserine, hallucinogens and indomethacin can all lead to ____________
anxiety
What are narcotics?
opioids and their derivatives only
Hypnotics are drugs that enduce ___________
sleep
Small doses of hypnotics cause _______
sedation
Medium doses of hypnotics cause _________
hypnosis
High dises of hypnotics cause ____________
surgical anesthesia
What system is primarily depressed by sedatives?
respiratory
“situational stress” insomnia is best treated by ___________
hypnotics
What is the most commonly prescribed antianxiety drug?
benzodiazepines
*b/c of their large therapeutic index
MOA of benzodiazepines
enhace neuronal GABA-mediated chloride channels
*increases permeability to chloride
_______________ are positive allosteric modulators of the GABAa receptor
benzodiazepines
Once a neuron is hyperpolarized it can no longer _________________
depolarize
Chloride causes the cell to________________
hyperpolarize
Alpha1 subunit causes _______
sedation
Alpha2 subunit causes_________
anxiolysis
Alpha3 subunit causes_________
processing of sensory motor information related to a schizophrenia endophenotype
Alpha4 subunit causes _________
sedation, hypnotic and anesthetic effects
Alpha5 subunit is ______
extrasynaptic
Beta3 subunit causes ____________
sedation, hynosis and anesthesia
*pentobarbital
propofol
etomitate something
benzodiazepines are ____________
anxiolytics
_______________ is the major inhibitory neurotransmitter in the CNS
GABA
Benzodiazepines ___________ effect the ANS
do not
*does not effect blood pressure
How do benzodiazepines relieve anxiety?
through enhacement of the inhibitory activity of GABA
Blood pressure is an indication of your ____________ control
autonomic
What benzo is commonnly used to treat panic disorders?
alprazolam
What benzo is commonly used to treat muscular spasms?
diazepam (fast acting)
What benzo is commonly used to treat seizure disorders and epilepsy?
clonazepam
diazepam
What benzos are commonly used to treat conscious sedation insomnia?
flurazepam (long acting)
temazepam (intermediate)
triazolam (short)
Benzos are used as an ___________ in pt’s with schizophrenia
adjuncts
What is the gold standard for treating a sustained seizure (status epilepticus) ?
diazepam
What is the speed of onset of oxazepam?
slowest
What is the fastest acting benzodiazepine?
diazepam
What benzodiazepam has the longest half life?
diazepam
What benzodiazepam has the shortest half life?
oxazepam
What benzodiazepam has the slowest speed of onset?
oxazepam
What benzodiazepams are available in IM form?
lorazepam
midazolam
What is the onset of action of IV lorazepam?
1-5 minutes
What is the onset of action of IM lorazepam?
15-30 minutes
What are possible AE of parenteral administration of benzodiazepines?
apnea hypotension bradycardia cardiac arrest *especially in older patients
Benzodiazepines are ____________ and rapidly absorbed after oral administration
lipophyllic
Avoid co administration of lorazepam IM and ___________ d/t reports of related death
olanzapine IM
Do benzodiazepine cross the placenta?
yes
_____________ combined with benzodiazepine may cause severe hypotension, respiratory or cardiac arrest, loss of consciousness
clozapine
Smoking will __________ the effect of benzodiazepines
decreased
Alcohol will __________ the effect of benzodiazepines
increase
Antifungals will __________ the effect of benzodiazepines
increase (increased plasma concentration)
What are the AE of benzodiazepines?
CNS depression
disorientation, irritability
impairment of memory and recall
respiratoy depression
With what conditions should benzodiazepines be given cautiously?
liver disease
glaucoma
alcohol
CNS depression
What part of brain is involved in memory formation?
hippocampus
How do benzodiazepines cause memory impairment?
Effect hippocampus
Tolerance to benzodiazepines ________ in response to the medication side effects
Decreases
How is physical dependence to a drug defined?
when medication is stopped, withdrawal or discontinuation symptoms occur
___________ is a benzo with a high risk of withdrawal d/t the short 1/2 life
alprazolam
How can you prevent benzodiazepine withdrawal?
convert to longer acting agent to taper slowly
What is the number one benzodiazepine blocker?
flumazenil (IV)
MOA of flumazenil
binds competitively to benzodiazepine receptors
Flumazenil given with what drug may increase the risk of seizures?
TCAs and benzodiazepines
AE of flumazenil
agitation, confusion, sweating, n/v, blurred vision, seizure
Buspirone is a ___________ agonist
serotonin type 1A receptor
What is the risk of dependence to buspirone?
very low-none
Buspirone is metabolized by ______________
liver enzymes
CYP34A
Buspirone may increase __________ secretion and growth hormone
prolactin
Buspirone may cause _ thermia
hypo
What is a risk of buspirone?
Risk of serotonin syndrome when co-administered with an SSRI
How does someone with serotonin syndrome present?
restlessness, diaphoresis, tremors
abdominal cramps
MOA of zolpidem?
act on GABA, not an anticonvulsant, no w/d effect
Zolpidem is more selective for _________ subunit of benzodiazepine receptor complex
alpha- 1
Zolpidem is hepatically oxidized by ___________
CYT-P450
Zaleplon affects ____________ and ___________ functions
psychomotor
congnititve
Zaleplon is metabolized by the ___________
liver
What is the 1/2 life of zolpidem?
2.5 hours
What is hydroxyzine?
antihistamine
antiemetic
What beta blockers are commonly used to treat stage fright?
atenolol
propranolol?
What is the indication for alprazalam?
panic attack, anxiety, depression
Flurazepam has the ___________ half life of the benzos
longest
What is the effect of most hypnotics on the sleep pattern?
decrease onset latency
increase NREM duration
decrease REM duration
What is the ultra short acting barbituate?
thiopental
What are the short-intermediate acting barbituates?
pentobarbital, secobarbital, amobarbital
What is the long acting barbituate?
phenobarbital
MOA of barbituates
at high concentrations, direcly activate the GABAa receptor to enhacne chloride permeability–in addition to allosteric modulation of the GABAa receptor
What are the membrane effects of barbituates?
nonspecific neuronal depression has been reported at highly very high (toxic) doses
What barbituate is often used for sedation (anesthesia)?
thiopental (inducer)
What is an unusual use of barbituates?
neonatal hyperbilirubinemia and kernicterus
usually manifests the second day
When barbituates are excreted in the urine, they are in a ______________ form
anionic
AE of barbituates
hangovers, hyperalgesia, CNS excitation, hypersensitivity
What do barbituates do at sub-lethal dose intoxications?
ganglionic blockade
hypotension/hypothermia
What is a major contraindication to barbituates?
acute intermittenet porphyria
In a barbituate overdose, what can you give them to alkalinizate their urine?
bicarb
Why do you want to alkanilize the urine in a barbituate overdose?
excreets the drug faster
Barbituates are a _________ inducer of cytochrome P450
potent
What are the sedatives/hypnotics
benzos barbiturates antihistamines chloral hydrate ethanol
What benzdiazepine is often used for sleep maintenance?
temazepam
What benzodiazepine is often used for short term treatment?
triazolam
What do benzidiazepines do in regards to sleep?
increase total sleep time but may prevent transition from lighter stage 2 sleep into deep restorative stages (stages 3 and 4)
