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RUSMpsychopharm3+4

Sedatives, hypnotics, and anxiolytics

QuestionAnswer
What part of the brain contains wake-promoting neurons Post. Hypothalamus
What part of the brain contains sleep-active neurons? Ant. Hypothalamus
NTs of wakefulness NE, 5-HT, Ach, DA, GLU, Hypocretin/orexins, Histamine
NTs of sleep Adenosine, GABA, prostaglandins, galanin
NTs of REM specifically Ach, 5-HT, NE, hypocretin. (all the waking hormones except for DA, These act to inhibit cholinergic neurons.
Transient insomnia. Rx? Triazolam. Transient insomnia = those who normally sleep well, but are having a transient problem. This drug is ideal because is has a short T1/2 and no hangover
Temazepam / Triazolam is used to treat what sleep condition Transient insomnia and initial insomnia
Initial insomnia. Rx? pt who has trouble getting to sleep, but once they are asleep, they are able to maintain. Rx drug with an early peak concentration and short T1/2. : **Triazolam, temazepam, zolpidem or zaleplon.
Pt complains of having trouble falling asleep, but it able to stay asleep if he is able to fall asleep initially. Dx? Rx? Initial insomnia. Rx: Triazolan, temazepam, zolpidem, zaleplon.
Sleep maintenance insomnia. Rx? Pt who are able to get to sleep but cannot stay asleep. Rx drug with intermediate T1/2. ** Oxazepam, larazepam**
Elderly with sleeping problems. Rx? Oxazepam.
Pt is able to get to sleep but cannot stay asleep. Dx? Rx? sleep maintenance insomnia. Rx: oxazepam or larazepam.
Oxazepam and lorazepam are drug of choice for what type of insomnia Sleep maintnance.
Oxazepam is drug of choice for what type of insomnia Elderly pt with sleep problems and sleep maintenance insomnia. Slowly absorbed.
What benzo has the longest t1/2 flurazepam. Used for frequent awakenings... but has a side effect of daytime sedation.
Alprazolam is used to treat Anxiety states
Amitriptyline role in sleep therapy Useful for treating depressed pts who complain of early morning awakening
DOC for early morning awakening in pt with depression amitryptyline
Drug sometimes used for nocturnal waking.... it is taken when pt wakes up in the middle of the night (as needed) zaleplon. This tx is not recommended.
Intermediate length sedation used to treat sleep maintenance insomnia Lorazepam
Pt complains of having trouble getting to sleep, but requires a drug that will not impair his day to day activities, as he has a job that requires full-alertness. Rx? zolpidem
Drug of choice for a post-op patient to help them sleep. diazepam. the degree of sedation will be advantageous following surgery, especially if pain is involved.
Drugs of choice for GAD. What is the rationale for using these drugs? Drug with intermediate half life so as to cover pt needs throughout the day and night, but minimum hangover over effects (ie no active intermediates) ***Diazepam, buspirone, SSRI such as venlafaxine. Trend is moving toward using SSRIs for anxiety d/o t
Stress related anxiety rx? Drug must cover 24 hour/day needs. Diazepam, oxazepam, lorazepam, alprazolam, clonazepam.
Panic disorder rx? Drug must provide rapid symptomatic relief or act in a prophylactic manner. Ie; alprazolam, clonazepam, SSRI, TCD, MAOI
Social Phobias... rx? SSRI's, MAOI'
Tremor associated with social phobia...rx? propanolol
PTSD... rx? SSRIs, MAOI, or benzos are all effective for PTSD
What benzos are useful as muscle relaxants diazepam, lorezepam, and clonazepam
Rx for status epilepticus lorazepam
What is the most potent antiepileptic agent clonazepam
rx for complex partial seizures chlorazepate dipottasium
Chlorazepate dipottasium is used to treat... complex partial seizures
lorazepam is used to treat what seizure disorder status epilepticus
What benzo is given rectally or by IV for generalized epilepsy in children diazepam
What 3 drugs have desmethyldiazepam as an active intermediate chlordiazepoxide, diazepam, flurazepam. Because of this these drugs will have prolonged effects (desmethyldiazepam t1/2=100)
Oxazepam is the common endpoint in metabolism (active metabolite) of what drugs? Diazepam and methyldiazepam
What effects do SSRIs have on diazepam SSRIs inhibit CYP3A4, thus causing increased diazepam plasma levels.
What drugs are conjugated without any phase 1 metabolism? What effect does this have? Oxazepam, lorazepam, and temazepam. These drugs do not have active intermediates so they will not accumulate with chronic dosing. Useful for pt with liver disease and old people
What drugs are useful for pts with liver disease and old people? Why? Oxazepam, lorazepam, and temazepam. No active intermediates... will not accumulate with chronic dosing.
DOC for anxiety in an elderly pt oxazepam
What naturally occurring chemical in the brain acts as an inverse agonist against GABA-A receptors? Beta carbolines. reduces GABA affinity for the GABA-A receptor. Decreasing GABA activity
What are the three types of benzodiazepine receptors? Omega-1, omega-2, omega 3. Hypnotic fx, anxiolytic effects, and myelorelaxant effects, respectively.
What effects do BZs have on GABA activity BZs increase GABAs activity at the GABA-A receptor. Thus inducing sedative effects due to increase GABA
What three types of drugs should be avoided when taking BZs alcohols, opiates, and barbiturates.
"date rape" drugs aka "roofies" are what drug? flunitrazepam
Non BZ rx for GAD buspirone
What is buspirone? (use, features, etc) Non-BZ/non-Barb drug used for treated me GAD. DOES NOT cause sedation and has minimal effects on psychomotor performance. Delayed onset (not useful in acute anxiety attacks)
MOA of buspirone? Partial 5-HT1A agonist. (Gi/Go)
Zolpidem: uses AKA ambien. Short term treatment of insomnia (ie initial insomnia). May cause rebound insomnia with discontinued use.
Zolpidem: MOA AKA ambien. Structurally different than BZs, but acts at the ****OMEGA 1 receptors** BZ1 (explains its hypnotic effects.
Zaleplon: use AKA sonata. Faster onset than zolpidem (30M to 1hr) with a shorter duration of action. Also acts on Omega 1. (similar drug to zolpidem, but with shorter action and faster onest0
The "Z" drugs include: Zolpidem (ambien) and zaleplon (sonata).
Adverse effects associated with zolpidem and zaleplon? Hypersensitivity (anaphylaxis) and dangerous sleep related activities such as sleep driving, sleep-eating, and telephone calling .
Chloral hydrate Really bad tasting drug used to sedate children and elderly. Rarely used due to GI A/E and potential carcinogenic action.
What intermediate is chloral hydrate converted to? trichloroethanol
Why is diazepam not used for sleep disorders (in most cases)? Because of its long half-life and the formation of an active metabolite with an even longer half-life, it will result in day-time sedation. Exception: post-op pt who is in pain... in this context a degree of sedation is advantageous
Venlafaxen: Uses SSRI that blocks 5-HT and NE reuptake. Approved for treatment of GAD
What SSRI is approved in tx of GAD venlafaxen XR
What specific BZ receptors are acted on by benzodiazepines BZ1-BZ3 (omega-1, omega-2, omega-3)
What is flumazenil used for? Treating coma due to BZ O/D (note: a coma cannot be induced by BZs alone... BZ o/d is invariably due to BZ alongside opiates and/or EtOH
Major adverse effects of BZs Paradoxical aggression and reduction in sensitivity of medullary center to CO2.
Good drug to use for sedating a pt during a bronchoscopy so as to relieve situational anxiety and provide anterograde amnesia of the procedure Triazolam
What respiratory disorder are BZs C/I in sleep apnea due to decreased sensitivity to hypercapnea
hyponotic drugs have what effect on CNS ion conductance (what ion does it act on and in what way) Increase Cl- conductance due to GABAergic activity -- hyperpolarization
Created by: rkirchoff
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