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16. Sedative-Hypnotics (16)
Terms in this set (73)
Signs are _____ measurable
Symptoms are _____ measurable
_____ can be useful at low levels, but may impair an individual's ability to function at high levels
This class of drug inhibits anxiety
This type of drug is generally anxiolytic, but the full effect is not a desirable property of an anxiolytic
An agent that promotes sleep and inhibits wakefulness
This class of drugs is effective in treating OCD and panic disorder
-It has no potential for abuse or dependence
-It has a slow onset (2-4 weeks) and must be taken continuously
Selective Serotonin Reuptake Inhibitors (SSRIs)
Along with SSRI's these drugs can be used for generalized anxiety disorder
What is the first-line treatment for anxiety?
The GABA A receptor has how many subunits?
-What are the subunits?
-Alpha 1, Alpha 2
-Beta 1, Beta 2
Where does GABA bind to on the GABA A receptor?
Alpha and Beta
Where do benzodiazepines bind to on the GABA A receptor?
Alpha and Gamma
Where does Flumazenil bind to on the GABA A receptor?
Alpha and Gamma
Where does Zolpidem bind to on the GABA A receptor?
Alpha and Gamma
What happens to the GABA A receptor physiologically speaking when GABA binds to it?
The channel opens to Cl- ions. The increased Cl- influx hyper polarizes the receptor and inhibits neural firing
These agents facilitate GABA action at GABA A receptors by increasing the frequency of Cl- channel openings
These agents competitively antagonize benzodiazepine agonists
These agents decrease Cl- conductance; inhibit GABA in a non-competitive fashion
Benzodiazepine Inverse Agonists
_____ when used alone have a ceiling effect, they tend not to cause a massive amount of respiratory depression
Though they are generally safe drugs when used alone, benzodiazepines are potentially lethal (respiratory depression) when combined with what class of drugs?
Alcohol or barbiturates
This class of drugs has long half-lives and dependence is a serious problem
This drug is the prototype benzodiazepine, it has a half life of around 50 hours
What is the dose dependent effect of diazepam?
Low dose anxiolytic, high dose hypnotic
These two benzodiazepines are approved to treat status epilepticus
Diazepam and Lorazepam
-Used for anxiolytic and hypnotic effect
-Some potential for early morning awakening
-Tolerance/dependence if over-used
-Said to be less sedative than other BZDs (use as hypnotic may be based on anxiolytic effect)
What is the current benzodiazepine of choice for panic disorder and generalized anxiety?
These two benzodiazepines have no metabolites, they are directly conjugated by the liver after injection.
-This leads to a relatively short half life and serves a benefit in older patients.
Oxazepam and Lorazepam
What is the difference between anterograde amnesia and retrograde amnesia?
-Anterograde: causes amnesia immediately after administration
-Retrograde: causes amnesia a few minutes after administration
This benzodiazepine is water soluble and has a short duration of action
-It causes anterograde amnesia
What is the benzodiazepine receptor antagonist?
What should you administer in the case of a benzodiazepine overdose when dependence is involved?
Nothing, flumazenil will precipitate withdrawal
There is a significant potential for _____ with the administration of flumazenil.
These type of drugs increase the CNS depressant effect when administered with benzodiazepines
_____ inhibits liver mixed-function oxidase. Prolongs the action of most benzodiazepines.
-What benzodiazepines should you use with this drug if you have to?
-Oxazepam or lorazepam
There is a differential tolerance to the _____ vs. _____ effects of benzodiazepines.
-Which effect is less affected by tolerance?
-Sedative vs. anxiolytic
What things can lead to benzodiazepine tolerance?
-Higher dose, more frequent dosing, the longer the dose is taken
What can cause withdrawal if a patient has benzodiazepine dependence?
-Drug administration stops
-An antagonist (flumazenil) is administered
With benzodiazepines, the greater the physical dependence, the worse the _____
Signs of benzodiazepine withdrawal
Symptoms of benzodiazepine withdrawal
-Anxiety (First symptom)
Which occurs first in benzodiazepine withdrawal, signs or symptoms?
What is the first symptom in benzodiazepine withdrawal?
What is "dependence of the sedative-hypnotic type," or "dependence of the benzodiazepine type"
Benzodiazepine can have cross-dependence with other sedative-hypnotics such as ETOH and barbiturates
What can to help minimize the chance for benzodiazepine dependence?
-Limit the number of pills in a prescription
-Counsel the patient to never use them for more than 3 successive days
What is the difference between benzodiazepine withdrawal related to long half-lives and short half-lives?
-Shorter half-life drugs have nastier signs and symptoms of withdrawal
-Longer half-life drugs have less severe signs and symptoms of withdrawal, but last for a longer time
What do you do if benzodiazepine withdrawal is threatening to become intolerable or if seizures are likely?
Consider administering a longer-acting benzodiazepine
How do 5-HT 1A agonist work physiologically?
Increase K+ conductance via same channels as GABA B receptors
This 5-HT 1A partial agonist causes no sedation or motor impairment
-It is used to treat anxiety; has no efficacy in sleep disorders
What might you consider if SSRIs are ineffective at controlling anxiety?
Switch from SSRI to buspirone or add buspirone to the SSRI
-10% of patients cannot tolerate this drug because it increases their anxiety
-High doses cause anxiety
-Slow onset -- 1 week onset; 2-4 weeks maximal effect
-Poor patient acceptance
-Dizziness, nausea, vomiting
-No dependence or tolerance
-No cross-tolerance with BZDs
-Does not alleviate BZD or EtOH withdrawal
What type of drugs does buspirone interact with?
-MAOI leads to hypertension
What is the treatment for OCD?
Buspirone + SSRI
This drug can be used to prevent jitters associated with excess stimulation of B2 receptors
-It is used as the treatment for "performance anxiety"
Insomnia involves getting to sleep and staying asleep, which one is usually more troubling?
-Incidence increases with _____
Characteristics of the ideal hypnotic
-Produces sleep rapidly
-Does not alter sleep pattern
-No early morning awakening
-No rebound insomnia
-No tolerance or dependence
-Has a high TI (Therapeutic Index)
Problems with using benzodiazepines as sedative-hypnotics
-"Hangover" is a problem for long-acting benzodiazepines
-Rebound insomnia is a problem for short-acting benzodiazepines
-Early morning awakening is a problem
short and intermediate-acting benzodiazepines
This benzodiazepine has a short elimination half-life and causes no hangover
This benzodiazepine has shown rebound insomnia and other withdrawal signs with continued use
-However, some individuals show mild aspects of this phenomenon with a single dose.
These drugs are not benzodiazepines, they are benzodiazepine receptor-subtype selective drugs
-Zolpidem, Zaleplon, Eszopiclone
How do benzodiazepine receptor-subtype selective drugs work physiologically?
These drugs bind relatively selectively to GABA receptors containing the alpha 1 subunit (benzodiazepine subtype of the GABA receptor)
This benzodiazepine receptor-subtype selective drug is nearly as efficacious in producing sleep and benzodiazepines
-However, it has much less anxiolytic, anticonvulsant, and muscle relaxant effects
-Short half-life (3-5 hrs)
-Less hangover than with long-acting BZDs
-Abuse/dependence potential is lower than with BZDs
-No rebound insomnia even after 30 consecutive days use
-Like zolpidem, binds benzodiazepine (alpha1) receptors and has same profile of effects
-Shorter half-life than zolpidem (approx 1hr)
Marketed for PRN use
-Take either before bedtime or upon awaking in the middle of the night (if more than 4 hr remain in sleep cycle)
-A treatment for those who awake mid-sleep cycle
Is abuse more or less common with zolipidem than benzodiazepines?
This benzodiazepine receptor-subtype selective drug has the same profile of effects as zolpidem
This is a pineal gland hormone that regulates sleep/wake cycle
-It is particularly useful for sleep problems related to "jet-lag" or changing day/night hours
Melatonin is contraindicated in patients with _____
This sleep medication is OTC and has no problems with dependence
Barbiturates include what drugs
Effects of benzodiazepines plus barbiturates
-Effects of BZDs plus barbiturates
-Profound CNS depression is possible, including anesthesia and coma
What is the difference between benzodiazepines and barbiturates physiologically speaking?
-Benzodiazepines facilitate the effects of GABA, increasing Cl- influx, they do not activate the GABA receptor
-Barbiturates facilitate the effects of GABA, increasing Cl- influx, they do not activate the GABA receptor at low doses.
-Barbiturates directly activate the receptor at high doses
Effects of alcohol on ion channels
-Alcohol facilitates the influx of chloride on the GABA receptor, using GABA as the neurotransmitter
-Alcohol inhibits the influx of calcium on NMDA receptors, using Glutamate as the neurotransmitter
-Of little interest as a medicinal hypnotic
-Slipped into a drink to produce rapid intoxication/unconsciousness
-Today-GHB or flunitrazepam (Rohypnol, BZD)
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