Term
| Name the ultra-short acting barbituates. |
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Definition
| sodium thiopental, thiamylal, methylhexital |
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Term
| Name the short-to-intermediate acting barbituates? |
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Definition
| secobarbital, pentobarbital |
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Term
| Name a long acting barbituiate. |
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Definition
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Term
| Ultra-short acting barbiturates work for 5-8 minutes but have a half life of 12 hours. How is this possible? |
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Definition
| drug is very lipophilic so it quickly crosses the BBB and is concentrated there for 5-6 minutes; then the effect of the drug ends when it is redistributed throughout the body |
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Term
| The rate of distribution of barbiturates depends on their ______. |
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Definition
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Term
| Why are intermediate acting barbiturates not used as an outpatient drug? |
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Definition
| because at high doses the barbiturates can open the GABA (A) receptors by themselves; this gives the drugs a narrow therpeutic index |
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Term
| Compare/contrast GABA (A) versus GABA (B) receptor |
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Definition
A= post synaptic, pentameric Cl- ion channel
B= presynaptic, GPCR |
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Term
| What is the MOA of benzodiazepines? |
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Definition
| positive allosteric modulators meaning they bind to an allosteric site on the GABA (A) channel that fascilitates GABA binding |
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Term
| Name the positive allosteric modulators of the GABA Cl- channel. |
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Definition
| alcohol, barbituates and benzodiazepines |
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Term
| What are teh different bindings sites on the GABA (A) channel? |
|
Definition
| ethanol, barbituate, GABA, benzodiazepine |
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Term
| Which CNS depressant enhances its own metabolism with repeated administration? |
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Definition
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Term
| What determines whether or not someone is physically dependent on a drug? |
|
Definition
| whether they have withdrawal symptoms |
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Term
| What are the withdrawal symptoms of barbiturates? |
|
Definition
| proconvulsant state, anxiety, insomnia |
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Term
| What are teh clinical uses of barbiturates? |
|
Definition
| induction of anesthesia (for ultra-short acting), and treat some forms of epilepsy (phenobarbital) |
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Term
| What are the adverse effects of barbiturates? |
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Definition
| CNS depression, respiratory depression, tolerance, dependence, abuse |
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|
Term
| What types of drug interactions occur with barbiturates? |
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Definition
| additive effects with other CNS depressants; enhance hepatic metabolism of drugs |
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Term
| What types of disorders are CNS depressants used to treat? |
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Definition
| used as anxiolytics for anxiety or as sedative/hypnotics for insomnia; also used as anticonvulsants or for conscious sedation (managed anesthesia) |
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Term
| T/F you can become dependent on benzodiazepines at therapeutic doses. |
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Definition
|
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Term
| Which is safer: benzodiazepines or barbiturates? why? |
|
Definition
| benzodiazepines because they can't open the GABA (A) channels by themselves |
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|
Term
| What are the two types of sleep disorders? |
|
Definition
| sleep onset and sleep maintenance disorder |
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|
Term
| Name the short acting benzodiazepines? |
|
Definition
|
|
Term
| What are the intermediate-acting benzodiazepines? |
|
Definition
| lorazepam, oxazepam, temazepam, alprazolam, chlordiazepoxide |
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|
Term
| What are the long-acting benzodiazepines? |
|
Definition
| flurazepam, diazepam, clonazepam |
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|
Term
| What are short acting benzodiazepines used for? |
|
Definition
| induction agents for conscious sedation; sleep onset disorder because of short t1/2 |
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|
Term
| What kind of sedative is given via a sucker to children? |
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Definition
|
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Term
| What drugs are first choice for status epilepticus? How do you administer them? |
|
Definition
| lorazepam, diazepam; IM because the patient is moving around |
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|
Term
| What is oxazepam used for? |
|
Definition
|
|
Term
| What is temezapam used for? |
|
Definition
| as a sedative hypnotic for sleep maintenence disorder |
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|
Term
| Which benzodiazepine is noted for the excessive amounts of people who abuse it? |
|
Definition
|
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Term
| What is alprazolam FDA approved to treat? |
|
Definition
| depression, panic disorder, etc. etc. |
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|
Term
| Name the first benzodiazepine. |
|
Definition
|
|
Term
| Whyis flurazepam not routinely used? |
|
Definition
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Term
| If considering alzhiemer's in an elderly patient, you should first make sure they are not on which drug? why? |
|
Definition
| benzodiazepines because a side effect of those drugs is anterograde amnesia |
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|
Term
| What drug was infamous as the first date rape drug? |
|
Definition
| flunitrazepam ("rohypnol"), now formulated to turn drinks blue/cloudy |
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|
Term
| Why is lorazepam preferable over diazepam for treating status epilepticus? |
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Definition
| because lorazepam is woter soluble; when you give diazepam IM it can cause thrombophlebitis because not water soluble |
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|
Term
| What is the antagonist or "antidote" for benzodiazepines? |
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Definition
| flumazenil= a competitive and neutral modulator at the benzodiazepine binding site on the GABA(A) receptor complex; half life= around 60 minutes |
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|
Term
| What drug is used to control aggression in psych/combative patients? |
|
Definition
|
|
Term
| Which benzodiazepine is an active compounds (i.e. doesn't need to be metabolized to an active compound)? |
|
Definition
|
|
Term
| Name a benzodiazepine that is subject to both phase I (oxegenase) and phase (transferase) II reactions by the liver? |
|
Definition
|
|
Term
| What are the drugs of choice for alcohol withdrawal? |
|
Definition
|
|
Term
| What is the MOA of benzodiazepines? |
|
Definition
| binds to a specific site on the GABA (A) receptor to facilitate the actions of GABA; DO NOT activate the GABA(A) receptor directly |
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|
Term
| As you increase the dose of barbituates, what effects are sequentially seen? |
|
Definition
| sedation, hypnosis, anesthesia, coma, death |
|
|
Term
| What are the clinical uses of benzodiazepines? |
|
Definition
| anxiolytics, sedative, muscle relaxant, anticonvulsant, induction of anesthesia |
|
|
Term
| What are the adverse effects of benzodiazepines? |
|
Definition
| CNS depression, anterograde amnesia, respiratory depression, tolerance dependence, abuse potential |
|
|
Term
| What are the drug interactions associated of benzodiazepines? |
|
Definition
| additive effects with other CNS depressants |
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|
Term
| T/F Withdrawal from benzodiazepines can be life-threatening. |
|
Definition
|
|
Term
| Which CNS depressants can be excreted into milk? |
|
Definition
|
|
Term
| What types of drugs are used in the treatment of anxiety disorders? |
|
Definition
| benzodiazepines, buspirone, antidepressants, beta blockers |
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|
Term
| What drugs are used to prevent performance anxiety? |
|
Definition
|
|
Term
| What drugs are first choice in treating panic disorder? |
|
Definition
| antidepressants like SSRIs, TCAs, and MAOIs |
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|
Term
| What is the MOA of buspirone? |
|
Definition
| serotonin type 1A (5-HT1A) agonist |
|
|
Term
| What anxiety disorder is buspirone not effective in treating? |
|
Definition
|
|
Term
| What are the adverse effects of buspirone? |
|
Definition
| headache, dizziness, and nausea |
|
|
Term
| What are the pros and cons of using buspirone to treat anxiety? |
|
Definition
| supposed to be not as sedative, but has a long latency to obtain anxiolytic effects |
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|
Term
| Which benzodiazepines are used to treat insomnia? |
|
Definition
| triazolam, flurazepam, temazepan |
|
|
Term
| What types of drugs are used to treat insomnia? |
|
Definition
| benzodiazepines, non benzodiazepines that bind to the BZ1 site, antidepressants, antihistamines, melatonin, meprobamate, carisoprodol |
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|
Term
| Name some non-benzodiazepines that bind to the BZ1 site. |
|
Definition
| zolpidem, zaleplon, eszopiclone |
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|
Term
| Which antidepressants are used to treat insomnia? |
|
Definition
|
|
Term
| Which antihistamines are used to treat insomnia? |
|
Definition
| hydroxyzine, diphenhydramine |
|
|
Term
| What is the MOA of melatonin? |
|
Definition
| binds to MT receptors; relatively long MOA |
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|
Term
|
Definition
| approved as an antianxiety agent in 1955, but became popular as a sedative hypnotic |
|
|
Term
| What is the active metabolite of carisoprodol? |
|
Definition
|
|
Term
|
Definition
| a skeletal muscle relaxant also used for insomnia that has abuse potential and has become a popular street drug ("soma") |
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|
Term
|
Definition
| active ingredient is EtOH (which is metabolized via 0 order kinetics); very uneven kinetics that depends on many factors including whether it is taken on a full stomach, etc; DO NOT USE FOR INSOMNIA |
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|
Term
| Most OTC sleep aids contain which active ingredient? |
|
Definition
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|
Term
| Hydroxyzine is often used in combination for _____. |
|
Definition
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|
Term
| If you want to treat both depression and insomnia, a drug that would do both would be ______. |
|
Definition
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