Term
What is the drug that is the only sleep aid with no evidence of abuse??
what is it metabolized by? |
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Definition
Ramelteon
and metabolized by CYP1A2,3A4 and 2C |
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Term
| What drug is a melatonin receptor agonist at M1 and M2 R and should not be used in a patient with renal impairment, not be taken with alcohol and appears to decrease testosterone and increase prolactin levels? |
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Definition
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Term
| What is the active metabolite of ramelteon? |
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Definition
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Term
| T/F: Ramelteon helps you fall asleep and maintain sleep |
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Definition
| NOOOOOO, false. does NOT maintain sleep |
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Term
| Name the normal stages of sleep |
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Definition
Stage 1: drowsiness
Stage 2: light sleep
Stage 3+4: deep "slow wave" sleep
REM : dream sleep
sleep consists of repetitive cycles lasting 90 minutes, advancing through non-REM stages to REM |
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Term
| Barbituates and BZDs give you what stage of sleep and Decrease/knock out what stage of sleep? |
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Definition
Stage 2
BZDs that are on the market decrease stage 3 and 4
REM and Stage 3 and 4 are knocked out by Barbituates |
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Term
| during what stage of sleep does one experience night terrors (not dreams) and bed wetting? |
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Definition
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Term
| T/F: REM is predominant earlier in night, Stage 3 and 4 laters in night and the length of 3 and 4 increase as the night progresses |
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Definition
FALSE!
REM = later in night
3,4 = earlier in night
as night progresses length of 3 and 4 decrease |
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Term
| This area in your brain is important for the control of sleep. Neurons here promote sleep; lesions here cause total insomnia; and this area sends inhibitory GABA projections to locus coeuleus (NE), Raphe nucleus (5HT) ad tuberomamillary nucleus (histamine) |
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Definition
| VLPA - ventrolateral preoptic area |
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Term
| ___ = important for the control of REM sleep |
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Definition
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Term
| What will the effect of an increased Ach release from neurons in the peribranchial pons by on sleep? |
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Definition
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Term
| Where do pontine ACH neurons project? |
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Definition
1. thalamus (control cortical arousal)
2. basal forebrain (arousal and desynchrony)
3. tectum (rapid eye movements) |
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Term
| how to pontine cells induce REM motor paralysis or atonia |
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Definition
| they project via magnocellular cells within medulla to the spinal chord and release glycine to inhibit alpha-motor neurons. |
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Term
| what NT is essential for sleep? |
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Definition
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Term
| a decrease of something in the nucleus of mynert causes |
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Definition
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Term
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Definition
REM payalysis occurs and the persn is still conscious.
sleep paraylysis is when rem payalysis occurs just before or just after sleep. |
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Term
_______ have reduced CSF level of neuropeptide orexin OR altered activity of orexin-B receptor
Orexin causes the release of what NT |
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Definition
narcolepsy
Orexin - is released from the lateral nucleus of the hypothalamus and it stimulates ACH to release in the forebrain which increases wakefulness and arousal |
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Term
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Definition
1. approved for treatment of narcolepsy
2. excessive somnolence
3. obstructive sleep- apnea |
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Term
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Definition
alpha-agonist (prazosin antagonizes some effects)
facilitates Glu-transmission
reduces GABA - transmission
modafinil activates orexin producing neurons |
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Term
| This R-enantiomer is used to treat narcolepsy, obstructive sleep apnea, hypopnea syndrome and shift work sleep disorder |
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Definition
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Term
| This drug is prescribed for narcolepsy but also causes increased vigilence, mood brightening, enhances the willingness to work and enhances memory. compared to amphetamines it causes less jitteriness, anxiety, agitation, no hypersomnolescent rebound effect and less peripheral effects |
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Definition
modafinil
* think i need some! |
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Term
| what NT must you accumulate in the brain to inhibit the basal forebrain cells responsible for arousal. Caffeine blocks its receptors |
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Definition
| adenosine (another NT that normally allows you to sleep) |
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Term
| when you have been craming for an exam and suddenly decide to get a full nights sleep included REM. You will see a high density of what on your EEG? |
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Definition
| high density PGO waves (distinctive pattern of REM sleep) |
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Term
| Patient is experiencing somatosized tension and therefore suffers from what you think is psycophysiologic insomnia. what treatment do you recommend? |
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Definition
| sleep hygiene, short term hypnotic and behavioral techniques |
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Term
| patient has been experiencing insomnia for 3days to 3 weeks caused by problems at work. is this a long term or short term or transient type of insomnia? |
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Definition
short term
long term- more than 3 weeks
and transient = less than 3 days |
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Term
1. patient on SSRI, with insomnia thats not going away - give them _____
2. schizophrenic patient on dopamine blocking agent and still agitates and insomnia continues give them ______ |
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Definition
1. trazadone
2. anxiety disorder etc - with those symptoms - give benzodiazepines |
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Term
| what drugs are contraindicated in patients with sleep apnea?? |
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Definition
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Term
| side effects of hypnotic agents used to treat insomnia |
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Definition
1. decreased effectiveness over time
2. rebound insomnia on discontinuation
2. changes in sleep architecture - barbituates decrease REM sleep; benzodiazepines reduce slow wave non-REM sleep (Stage 3 and 4)
3. Benzodiazepines produce cognitive changes - next day confusion, increase rate of falls in old, rebound anxiety and amnesia, worse sleep apnea
4. short acting agents - rapid sleep but wake up 3-4 hours later and cant go back to sleep |
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Term
| patients taking hypnotic drugs for more than 2 weeks should be slowly tapered without abrupt discontinuation (t/F?) |
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Definition
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Term
| Compare BZDs with short half life versus one with a longer half-life? |
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Definition
short half life: patients with sleep onset insomnia and no daytime anxiety
long half life - give to patients who have day time anxiety |
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Term
| why are benzodiazepines prefered in the elderly when treating insomnia |
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Definition
1. less risk of falls and respiratory depression
Note: at higher doses - early morning wakening, rebound daytime anxiety and amnesic episodes |
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Term
| what drugs do you want to avoid bcause of potential for abuse and easy overdose |
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Definition
1. barbituates
2. glutethimide
3. meprobamate |
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Term
| what are the indication for short acting barbituate sedative hypnotics such as pentobarbital sodium or secobarbitoal sodium? |
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Definition
| short term (less than 2 weeks) treatment of insomnia (use as a sedative preoperatively as a preanesthesia agent) and onset of action is 10-15 minutes and duration is 3-4 hours. |
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Term
| what NT does barbituates work on andd what isoform of the receptor does it bind to (A,B,C??)?? |
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Definition
| GABA receptors and specifically GABA A Receptors (binds at a different site than that of BZDs and is not blocked by flumazenil) |
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Term
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Definition
1. increases GABA effect (increased duration of opening)
2. directly activates GABA a channels at high concentrations
3. blocks glutamate NT effects
4. blocks NA channels |
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Term
| these drugs have a similar effect to alcohol and they dress the sympathetic nervous system actiivty. they are used to induce sleep and reduce anxiety and have a higher toxicity than BZDs also has the steepest dose response curve for the hypnotics |
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Definition
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Term
| T/F: barbituates have tranquilizing effect, hypnotic effect, at larger doses a anticonvulsant and anesthetic effect and relieve pain |
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Definition
| FALSEE: DO NOT relieve pain! |
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Term
| This drug is a non-benzo sedative that will make you fall asleep in a half an hour and in the middle of the night you might get up and eat but will not remember doing so in the morning. |
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Definition
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Term
| what drug will make you fall asleep quicker than zolpidem but will not keep you asleep anddd is recomended for 7-10 days only. |
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Definition
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Term
| ______ and alcohol compete for metabolism by the same enzyme. when mixed with alcohol = micky finn and is rapidly absorbed and acts quickly. you have a prolonged action when mixed and often misused by the elderly as a sleep aid |
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Definition
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Term
| what is the active metabolite of chloral hydrate? |
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Definition
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Term
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Definition
| binds to GABA A receptor with alpha and beta subunits and enhance the effect of GABA on Cl- current. exerts no effect in the absence of GABAA |
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Term
| what type of amnesia does bzds produce? |
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Definition
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Term
| names of benzodiazepines used to treat insomnia; Side effect = daytime sedation and REM sleep reduced and rebound with bizzare dreams. |
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Definition
estazolam
flurazepam
triozalam |
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Term
| characteritics of zolpidem, eszopiclone, and zalepion is |
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Definition
less daytime sedation
no effect of REM sleep
- these are not BZDs but work at BZD side on GABA receptor. they may preferentially bind to receptors that contain the a1 subunit. |
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Term
| which bzd is most likely to develop memory impairment? |
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Definition
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