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42 Cards in this Set

  • Front
  • Back
What are anxiolytics?
deacrease anxiety
What are sedatives?
decrease activity, alertness, intellectual performance, responsiveness; produce "calming" effects; usually non-specifically releive anxiety
What are hypnotics?
produce drowsiness, shorten sleep onset and reduce nocturnal wakening
What are anesthethics?
cause a state of charct. analgesia, LOC, absence of arousal in respone to noxious stimuli
What ia common characteristic of all sedative/hypnotics?
All "gemeral" CNS depressants, capable of producing dose-dependent CNS depression to medullary depression, coma and death. EXCEPT BDZ!!
What are the pharmaco properties of BDZ?
1. high lipid/water partition coefficeint, bind 70-90% with plasma protien
2. are redistributed and helps terminate the action of some
3.completely absorbed orally, some IM or IV
4. Metabolized by liver before excreted
What are the drugs of BDZ and relative half lifes?
Long (>1day): Flurazepam,chlordiazepoxide, clorazepate, diazepam
Interm (6-24hrs): temazepam, estazolam
Short (<6hrs): trazolam, zolpidem

Others: lorazepam, midazolam, alprazolam, clonazepam,
What is the mechanism of action of BDZ?
Positive allosteric modulators of GABA-operated Chloride channels (GABAa receptors). Site distinct from barbituate site
***4 different a units that bind BDZ
Where are the locations of the a subunits that bind the BDZ in the body?
a1-a3 bind in the CNS
a1=cortex and thalamus=sedation and amnesia
a2=limbic system and hippocampus= anxiolytic affect
a3= reticular formation, thalamus=LOC
Overall effect of BDZ?
To increase synaptic inhibitions, no effect on Chloride channel conductance in the absence of GABA
Whar are the pharm/clinic properties of BDZ?
1. All work in CNS
2. not work lower than brainstem so little cardiorespiratory sx
3.Not analgesic
4.assoc with tolerance and dependence
What are the CNS effects of BDZ?
anxiolytic effects, sedation, muscle relazation, anticonvulsant, hypnosis, retrograde amnesia, ataxia, confusion,stupor
What does the intensity of withdrawal depend on for BDZ?
2 things:
1. dose of drug daily: higher the more severe
2. the half life of the drug: the longer the less severe
What are the SE of BDZ?`
1. excessive sedation and impaired motor perfomance
2. additive effects of other CNS depressants can be lethal with alcohol
3. adversley affect breathing
4. disinhibition reactions=hypomanic or hostile behavior
What drugs are used for insomnia of the BDZ
1. BDZ
*Common drugs:
a:Flurazepam (long half-life)-little hangoer, impaired driving after
b: Temazepam (interm half), sense of refreshing sleep without hangover, but still impaired drive in AM
c: Estazolam &Triazolam (short half 2-3hrs) SE of waking early and being anzious during the day, one dose tolerance with rebound?
2. Non-BDZ:
a1 subunit selective is Zolpidem (ambien); short half 1-2hrs, zaleplon (sonata) shorter to allow reuse, eszopiclone (lunesta)
What are the BDZ used for anxiety?
1. with prominent autonomic signs use: alprazolam, clonazepam, lorazepam (other tx AD)
2. generalized or non-specific syndromes use: any BDZwith long half; (alternative buspirone
What drugs are used as pre-anesthetic meds?
Midzolam (Versed)IM or Lorazepam (ativan)Im or IV.
What are the other uses of BDZ?
1. Clonazepam=absence seizures
2. Lorazepam=emergent status epilepticus
3. also suppress dangerous symptoms from withdrawal from CNS depressants (ethanol)
4. Diazepam=muscle spasticity
5. Lorazepam=antiemetic
What us flumazenil?
A BDZ antagonist=binds the same site on the GABA receptor but produces no effect on its own;
What is the use of flumazenil quickly reverse the sedative effects of BDZ after general anesthesia or after proceduces
2. rvs toxicity due to or suspected BDZ OD
What are the Cautions with Flumazenil?
1. may precipitate withdrawal in dependent people
2.short half life (1hr) mayneed repeated for a long half life BDZ
What is Buspirone?
anxiolytic but not a sedative-hypnotic; not related to BDZ
What is the mechanism of Buspirone?
Does not interact with GABA-gated Cl-channels;
Action is partial agonist activity at 5-HT1a receptor
What are the pharmacokinetics of Buspirone?
well absorbed orally,
low bioavailabitlity
Eliminated by liver metab
What are the clinica effects of Buspirone?
1. less effective than BDZ in tx of severe anxiety, but not promote sleep. Anxiolytic take 1-2 wks
2. Appears not to produce rebound anxiety upon withdrawal
What are the SE of Buspirone?
well tolerated, free of tolerance, dependence, withdrawal problems
What are the common CNS properties to all NON-BDZ sedative hypnotics?
1. Progressive, dose-related CNS depression; dec cognitive/motor-> dec. inhibition and/or frank excitement-> to sleep and LOC without analgesia->coma->severe respiratory depression and cardiovascular collapse 2 to hypoxia
What are the properties of tolarnce for all non BDZ sed-hypnotics?
*rapidly to all CNS depressant effect xlethal respiratory and cardio
*Cross-tolerance btwn members of this group
What is the tx of acute intoxication with all non-bdz sed. hypnotics?
1. support ox and cardio fucntion
2. eliminate any unabsorbed drug and accelerte clearnce
3. get rid of BDZ if a mixed toxi with flumazenil
What are the properties of Barbituates?
*half: 8-48 hrs x for ones as anticonvulsants that are longer
*short acting=thiopental used for anesthesia are very lipid solubel ad duration is 10min.
*Can cause hyperalgesia so can interfere with hypnotic effects!
**Powerful induction of microsomal enzymes (pheonobarbital good at this)
What is the mechanism of action of barbituates?
*Low dose: potentiate GABAergic transmission by prolonging duration of GABA-induced openings of receptors
*High dose: promote Cl- influx thru GABA gated channel in the absence of GABA. less pronounced with anticonvulsants
*Very high: exert non-specific depressant effects by perturnng lipid membrence lie other anesthetics
What is the mechanism of metabolims of ethanol?
alchol dehydrogenas (RLS) then by aldehyde dehydrogenase
**Acetaaldehyde depletes hepatic glutathione and causes lipid peroxidation and damage.
***Zero-order kinetcis, blood concentrationlinear with time
What are the important facts of ethanol?
1. Alcohol inc. GABAa rec/Cl-funtcion and has other neuro effects
2.disrupts normal sleep pattern, exacerbates sleep apnea
3. produces cutaneous vasodilation, but overall inc. vasoconstriction, esp in coronary and cerebral beds and can inc. BP
4. dec. release of ADH and oxytoci from Ant. pituitary
What are the hallmarks of physical dependence/withdrawal from ethanol?
1. Very severe dependece, with DT as the most serious withdrawl sndrome that can be lethal
How do you treat alchohol withdrawal?
1. Give BDZ
2. rehydrate, check electrolytes
3. anticonvulsant= carbamazepine for seizure component only
What is the pharm. tx of alcoholism?
2. Disulfiram ("aversive")
3. Naltrexone
4. Acamrpsate A
5. Anti-depresants, buspirone
6. Ondansetron
What is Disulfiram?
binds aldehyde dehydrogenase leads to dangerous SE when drinking the smallest amount
What is Naltrexone
Opiate receptor antagonist, stops pleasurable aspects of alcohol
What is AcamprosateA
reduces rate of relapse after detox by attenuating the craving
What are the beneficial uses of Alchohol?
1. Small amts to reduce cornoary areter dz by inc. HDL/LDL ratio; promoting relaxation and good nutrition
2. Tx poisening with methanol or ethylene glycol: dec. the amount of formaldehyde in body by competitively bind the alchohol dehydrogenase
What are the "other" sedative-hypnotics?
1. Antihistamines- OTC sleep aids: diphenhydramine; hydroxyzine (iM ) as preanesthetic med for sedative, antimuscarinic, and antiemetic (not anymore b/c of midazolam)
2. meprobamte, chloral hydrate, drugs still perscribed for anxitey or insomnia but should not because of dependence issues
What are the Barbituates?