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 |
|
|
