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Pharmacology Exam 2: Anti-anxiety
pharm exam 2 anti-anxiety
100
Anatomy
Graduate
02/16/2011

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Term
Signs of anxiety are ___ ___ and include the following:
Definition
- objectively measurable
- tremors
- cardiac palpitations
- autonomic hyperexcitability
Term
Symptoms of anxiety are ___ ___ and include the following:
Definition
- subjective phenomenon
- tension
- fear
- worry
- poor concentration
- sense of impending doom
Term
Sedatives diminish ___, cause ___, and diminish ___ ____.
Definition
- diminish awareness
- cause drowsiness
- diminish motor activity
Term
Sedatives are generally ___, but sedation is not a desirable property of an ____.
Definition
- anxiolytic
- anxiolytic
Term
A hypnotic is an agent that promotes ___ and inhibits ____.
Definition
- promotes sleep
- inhibits wakefulness
Term
Serotonin Selective Reuptake Inhibitors (SSRIs), such as ____ and ____, work through blocking serotonin reuptake. This is one method of treating anxiety.
Definition
- venlafaxine
-tricyclics
Term
Benzodiazepines can also be used to treat anxiety. They bind to ___ ___ on the ___ receptor to facillitate ___ ____.
Definition
- benzodiazepine sites
- GABA receptor
- GABA neurotransmission
Term
Benzodiazepines were used a lot from the 60s to the 80s b/c effective for treatment of :
Definition
- post traumatic stress syndrome
- generalized anxiety
Term
SSRIs (Venlafaxine and Tricyclics) are efficacious in treating ___ ___ ___, ___ ___, and ___ ___ ___ .
Definition
- obsessive compulsive disorder
- panic disorder
- generalized anxiety disorder
Term
SSRIS have a ___ onset of __ to __ weeks. They must be taken ____. They are preferred agents for treatment b/c have little potential for ___ and no poetential for ___.
Definition
- slow onset of 2 to 4 weeks
- continuously
- little potential for dependence
- no potential for abuse
Term
first like of treatment for anxiety:
Definition
SSRIs
Term
GABA agents may also be used to treat anxiety. They have a ___ onset of action and a much more dependable ___ effect. But their disadvantages are numerous.
Definition
- quicker
- positive
Term
Benzodiazepines do not bind directly at the GABA site, rather they provide ___ ___ at the GABA site.
Definition
- steric modulation
Term
The GABA-a receptor complex is critical for anxiolytic/sedative-hypnotic effects of ___, ___, and ___.
Definition
- benzodiazephines
- barbituates
- alcohol
Term
When ___ binds the GABA-a receptor complex, a channel opens allowing ___ to rush in, which ___ the cell and ___ neural firing.
Definition
- GABA
- chloride
- hyperpolarizes
- decreases neural firing
Term
Increased chloride conductance, ___ ___ ___.
Definition
- decreases neural firing
Term
___ chloride conductance excites neurons (seizures).
Definition
Decreased
Term
The GABA receptor has a GABA ___ ___ site, and then ____ and ___ sites that modulate GABA binding.
Definition
- GABA true receptor site
- benzodiazephine
- barbituate
Term
What are the 3 types of BZD drugs?
Definition
- BZD agonits
- BZD antagonits
- BZD inverse agonist
Term
BZD agonists facilitate ___ action at GABA-a receptors by ___ frequency of chloride channel openings.
Definition
- GABA
- increasing
Term
BZD antagonits ___ antagonize BZD agonists.
Definition
- competetively
Term
BZD Inverse agonists ___ chloride conductance by inhibiting ___ in a ____ way.
Definition
- decrease chloride
- inhibiting GABA in a non-competitive way
Term
BZD antagonists are ___. BZD inverse agonists are ___ ___.
Definition
- competitive
- non-competitive
Term
BZD agonists are ___, ___, ___, ___, and produce ____. As doses go up, progression of effects increase, but there is ___ ___ that prevents ____, unless the injection is too rapid.
Definition
- anxiolytic, anti-convulsant, amnestic, hypnotic, produce confusion (AAAHC)
- ceiling effect
- coma
Term
Retrogad amnesia- get hit and don’t remember it and stuff before getting hit is fuzzy for a while
Definition
Term
Anterigrad amnesia- from the event going forward some period of time, memory is whiped out
Definition
Term
BZD are not lethal b/c of ___ ___.
Definition
ceiling effect
Term
Ethanol and barbituates do not have a ___ ___, so they can be lethal.
Definition
- do not have ceiling effect
Term
Benzodiazepines are ___ anxiolytics, have a __ onset, and are safe by themselves. However, if combined with sedative-hypnotics like ___ or ___, lethality is increased.
Definition
- efficacious
- fast
- ethanol or barbituates
Term
With benzodiazepines, ___ is a huge problem. The __ half lives foster drug hangover and next-day drug interactions.
Definition
- dependence
- long half lives
Term
BZD is not lethal in overdose if it is used alone. However, if it is mixed with __, ___, or ___ it can result in ___ ___ and death.
Definition
- alcohol, opiods, barbituates
- respiratory depression
Term
Pregnant women should NOT be on BZD b/c not known how it affects baby.
Definition
Term
what is the BZD prototype?
Definition
- Diazepam= Valium
Term
Diazepam:
Definition
- prototype benzodiazepine
- aka Valium
- anxiolytic
- hypnotic
- muscle relaxant
- pre-anesthetic b/c amnestic effect
- blocks convulsions in ___ or ___ withdrawal
- long half life (50+ hours) (highly lipid soluble)
Term
___ can be used to block convulsions from BZD or alcohol withdrawal.
Definition
Diazepam
Term
Diazepam given i.v. is second choice to terminate ____ ____ but it is very lipid soluble. Thus ____ is the first choice to terminate ___ ___ b/c it is more __ soluble.
Definition
- status epilepticus
- Iorezepam
- water
Term
Diazepam is not used for long term seizure control. Why?
Definition
- profound tolerance develops rapidly
Term
____ is a very popular BZD, but it has much greater abuse potential.
Definition
Alprazolam
Term
Midazolam:
Definition
- water soluble BZD
- very short acting
- used in i.v. anesthetic pre-op
- anxiolytic so good for moving patient to O.R. table
- muscle relaxant
- causes anterograde amnesia at high enough doses so not embarassed or intimated about procedure
Term
Flumazenil:
Definition
- BZD- site antagonist
- initially approved for reversing BZD component of respiratory depression in suspected drug overdose
- causes seizures in BZD dependent patients
- use is now restricted to relieving respiratory depression when BZDs may be prolonging recovery from anesthesia
- used cautiously
Term
drug used to relieve respiratory depression in surgery patients when BZD may be prolonging recovery from anesthesia:
Definition
- Flumazenil
Term
Two types of insomnia:
Definition
- trouble getting to sleep
- trouble staying asleep
Term
which type of insomina tends to be more troubling?
Definition
- trouble staying asleep
- increases with age
Term
BZD as sedative hypnotics:
Definition
- effective
- hang over effect occurs with long acting drugs like Diazepam
- rebound insomnia is problem for short acting BZD- triazolam
- early morning awakening is problem with short and intermediate acting BZDs
- tolerance/dependence/withdrawal develop (especially with Triazolam)
Term
___ causes seizures in BZD dependent patients.
Definition
Flumazenil
Term
BZD-1 Receptor-Subtype Selective drugs (sleeping drugs):
Definition
- Zolpidem (ambien)
- Zaleplon
- Eszopiclone
Term
Zolpidem is a ___ __ _receptor drug. It is ___ a ___. Though it is just as efficacious as BZD in producing sleep. What actions does it not have that a BZD does?
Definition
- BZD omega 1
- NOT a BZD
- not anxiolytic
- not muscle relaxant
- not anticonvuslant
Term
Zolpidem, a BZD-1 selective drug, has a __ half life (__ to __ hours), so it has less of a ___ effect than BZD. Abuse and dependence potential is ___ for Zolpidem than for BZDs. There is ___ rebound insomnia with Zolpidem even after 30 days of consecutive use.
Definition
- short 3-5 hours
- less of a hangover effect
- less
- NO rebound insomnia
Term
Zaleplon is a ___ agent with a __ __ half life. It is used in ___ ___ for those with ___ ___ ___ ___.
Definition
- BZD1
- very short
- inducing sleep
- mid-cycle awakening problems
Term
Melatonin is structurally modified serotonin made by your pineal gland. It is is responsive to light/dark cycles. It can be purchased OTC to __ ___ and ___ ___ ___. ___ tolerance develops and doses are variable.
Definition
- induce sleep
- reset body's clock
- rapid tolerance
Term
ZolpiDem makes it "Dim" all night. ZalePlon makes you "Plop" back down if you wake up mid-cycle.
Definition
Term
Ramelteon binds to __ receptors (both __ and ___) but does NOT bind ___ ___. It is non-scheduled. No risk for ___, ___, ___ ___, or ____. It is basically a ___ agonist.
Definition
- melatonin (MT1 and MT2)
- does not bind GABA-a receptors
- no risk for dependence, abuse, rebound insomnia, or withdrawal
- melatonin agonist
Term
RAMELteon "RAMs" up the Melatonin
Definition
Term
Ramelteon is useful for ___ __ or ___ __, but rapid ___ develops.
Definition
- jet lag or shift work
- tolerance
Term
Ramelteon should NOT be used in combination with ____. ___ binds the _____ and inhibits Ramelteon metabolism.
Definition
- Fluvoxamine
- Fluxoxamine
- CYP1A2
Term
Depression is a contraindication to ___ and ____ use:
Definition
Melatonin
Ramelteon
Term
Barbituate drugs:
Definition
- pentobarbital
- secobarbital
- phenobarbital
Term
Barbituates have a ___ therapeutic index, thus they should NEVER be used on outpatient basis for sleep. ___ is used for seizure control.
Definition
- poor
- Phenobarbital
Term
Barbituates have same effects as BZD plus:
Definition
- CNS depression (coma)
- respiratory depression
- abuse potential
Term
___ and ___ are schedule II drugs b/c of their abuse potential.
Definition
- Secobarbital
- Pentobarbital
Term
Alcohol enhances ___ neurotransmission and blocks ___ neurotransmission.
Definition
- enhances GABA neurotransmission
- blocks glutamate neurotransmission
Term
If you drink at all, chance of problems with drug is 1 in 5, chance of being alcoholic is 1 in 20. so if over 25 and Oh intake is going up, then it is a problem.
Definition
Term
Alcohol is classified as a ___ ____.
Definition
sedative hypnotic
Term
define one alcoholic drink:
Definition
- 10 g EtOH
- 1.5 oz 80 proof whiskey
- 12 oz beer
- 4 oz of wine
Term
each drink increases BEC by :
Definition
0.025g/dL

0.08 is legally intoxicated (3 drinks)
Term
Blood Ethanol Concentration
BEC = BAC = BEL = BAL
Units: % (g/dL) or mg % (mg/dL)
Definition
Term
As blood alcohol is rising, dopamine is being released into mesolimbic system. But when blood alchool peaks and falls, dopamine relase goes down and then you see GABA neutransmission phenomenon- hypnotic.
Definition
Term
alcohol pharmacokinetics:
Definition
Small, predictable amounts excreted through the lungs
Small amounts excreted in the urine
Primarily metabolized by oxidation in the liver (>90%)
EtOH elimination follows
ZERO ORDER KINETICS
Term
With zero order metabolism of alcohol, elimination rate is ____ of concentration but dependent on ___ ___ and ___ __. An average adult metabolizes 7-10 g/hour or 0.7 drinks per hour. So one drink in per hour, 3/4 drink out per hour.
Definition
- independent of concentration
- dependent on body weight and liver weight
Term
effects of alcohol in cns b/w BEC of 0.05 and 0.1% in non-tolerant individuals:
Definition
- sedation
- subjective high
- slowed reaction times
- 2-4 quick drinks
Term
BEC of 0.1-0.2%:
Definition
- impaired motor function
- slurred speech
- ataxia
Term
BEC of 0.2-0.3%:
Definition
- emesis
- stupor
Term
BEC of 0.4-0.5%:
Definition
- coma
Term
BEC greater than 0.5%
Definition
- respiratory depression
- death

even if drink a lot and have tolerance
Term
alcohols affect on endocrine system:
Definition
- diuresis via blocking release of anti-diuretic hormone (vasopressin)
Term
Pharmocologic treatment of alcohol abuse:
Definition
- Disulfiram (antabuse)
- Naltrexone
Term
Disulfiram makes pt sick if drink alcohol with it b/c it blocks the conversion of ___ to ____. The ___ cause vasodilate and cause emesis. This is type of aversion therapy- not popular.
Definition
- aldehyde to acetate
- aldehyde
Term
Naltrexone:
Definition
use to treat alcohol abuse
- opiod antagonist
- decreases craving for alcohol
- used in some treatment programs
Term
____, ___, and ____ are characterized by producing physical dependence manifested by similar signs and symptoms upon withdrawal. This is called ___ ___ ___ ____ ____. These drugs ___ ___ ___ from one another.
Definition
- BZD, Ethanol, and Barbituates
- General Sedative Hypnotic Withdrawal Syndrome
- cross suppress withdrawal
Term
So give barbituate or benzodiazepine to alcohol withdrawal, it reinstates the dependence and ends withdrawal. IT HAS TO BE SEDETIVE HYPNOTIC.
Definition
Term
When you withdraw from sedative hypnotics, you activate the __ nervous system, ___ ___ seizures occur and death is likely.
Definition
- sympathetic
- tonic clonic
Term
withdrawal from sedative hypnotics is __ ___. withdrawal from opiods is ___ ___ ___.
Definition
- life threatening
- NOT life threatening
Term
define abuse:
Definition
"I like it"
Term
define tolerance:
Definition
- less effect from same dose
Term
define dependence:
Definition
- withdrawal signs/symptoms occur when you stop
Term
abuse potential for BZD is __ ___
Definition
. very low
Term
abuse potential for barbituates:
Definition
- very high (except not for phenobarbital)
Term
abuse potential for BZD1 agents:
Definition
very low
Term
BZD tolerance:
Definition
The higher the dose, and
The more frequently the dose is taken, and
The longer the dose is taken, then
The greater the tolerance
Term
BZD dependence will be revealed when:
Definition
- drug adminstration stops
- an antagonist is given
Term
The ___ the elimination half life, theworse the withdrawal is.
Definition
shorter
Term
BZD antagonists drive BZD off the receptors and make withdrawal much worse.
Definition
Term
withdrawal signs:
Definition
- seizures
- tremors
Term
withdrawal symptoms:
Definition
- anxiety
- insomnia
- nausea
- malaise
Term
early withdrawal can be undone with drugs, but once seizures hit hard to treat. just have to wait it out.
Definition
Term
BZD Dependence:

KNOW THIS WELL
Definition
1. Initial anxiety returns during withdrawal
2. Additional anxiety occurs because of withdrawal
Net effect = intolerable anxiety
Symptoms of withdrawal occur before signs of withdrawal, and anxiety/insomnia are the first withdrawal symptoms
Term
So what is good use for BZD: 2-3 day situational anxiety (about flying to daughter’s wedding or something like that), same thing with sleeping pills (2-3 days max)
Definition
Term
BZD withdrawal alone is not as likely to cause seizures.
Definition
Term
alcohol withdrawal more likely to experience seizures, so you taper pt down with ___ if necessary to minimize seizure risk.
Definition
BZDs
Term
how to avoid BZD dependence:
Definition
Limit the number of pills in a prescription
Counsel the patient to never use them for more than 3 successive days
For tx of anxiety, always try to use an SSRI if possible
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