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
|
|
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
|
|
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
|
|
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
|
|
Term
| Benzodiazepines do not bind directly at the GABA site, rather they provide ___ ___ at the GABA site. |
|
Definition
|
|
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
|
|
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
|
|
Term
| BZD antagonits ___ antagonize BZD agonists. |
|
Definition
|
|
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
|
|
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
|
|
Term
|
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
|
|
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
|
|
Term
|
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
|
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
|
|
Term
|
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
|
|
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
|
|
Term
|
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
|
|
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
|
|
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
|
Definition
- impaired motor function
- slurred speech
- ataxia |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
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
|
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
|
Definition
|
|
Term
|
Definition
| - less effect from same dose |
|
|
Term
|
Definition
| - withdrawal signs/symptoms occur when you stop |
|
|
Term
| abuse potential for BZD is __ ___ |
|
Definition
|
|
Term
| abuse potential for barbituates: |
|
Definition
| - very high (except not for phenobarbital) |
|
|
Term
| abuse potential for BZD1 agents: |
|
Definition
|
|
Term
|
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
|
|
Term
| BZD antagonists drive BZD off the receptors and make withdrawal much worse. |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
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
|
|
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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|
