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46 Cards in this Set
- Front
- Back
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What is the definition of a sedative?
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induce calm without sleepiness
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What is the definition of hypnotic?
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induce normal sleep
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What is the definition of a anxiolytic?
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reduce anxiety
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WHat percent of the US population has an anxiety disorder?
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18%
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What percent of the US population has a sleeping disorder
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10%
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What are the benzodiazepines?
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The "lams and pams"
Chloridiazepoxide Diazepam flurazepam alprazolam trazolam midazolam temazepam flunitrepam |
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What are the properties of benzodiazepines in low doses?
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decrease aggression and anxiety
also a muscle relaxant, and may have anti-convulsive effects |
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What are the properties of benzodiazepines in high doses
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cause sedation, hynosis and loss of memory
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What is the mechanism of action of the benzodiazepines?
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bind to benzodiazepine receptors which are associated with GABA receptors. They then enhance the response of GABA receptors to GABA
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How are the benzodiazepines administered?
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orally or by IV
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What will happen is a patient is take a bezodiazepine for a long period of time and then suddenly withdrawal?
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may suffer from seizures
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What is the therapeutic index of benzodiazepines?
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very high, but may have interactions (fatal) if taken in combination with others
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What are the SE of benzodiazepines?
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drowsiness, ataxia, confusion
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What are the visual disturbances that may occur with benzodiazepines?
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diplopia and nystagmus due to muscle relaxation
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What is the mechanism of action of flumazenil
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Benzodiazepine receptor blocker
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What are the non-benzodiazepine hypnotics?
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zolpidem
Zalplon eszopiclone ramelteon meprobamate buspirone |
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What is the mechanism of zolpidem (Ambien)
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Used as a sleep aid by acting at the same site as bezodiazepine but cause less tolerance and dependence than BZ
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What is the mechanism of zaleplon (Sonata)?
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Used as a sleep aid by acting at the same site as bezodiazepine but cause less tolerance and dependence than BZ
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What is the mechanism of eszopiclone (Lunesta)
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Used as a sleep aid by acting at the same site as bezodiazepine but cause less tolerance and dependence than BZ
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What is the half life of zolpidem?
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2 hours
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What is the half life of zalplon?
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1 hour
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What is the half life of eszopiclone
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5 hours
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What is the mechanism of ramelteon (Rozerem)
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Melatonin receptor agonist to help maintain normal circadian rhythms
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What are the SE of ramelteon
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no rebound insomnia, can cause sedation, fatigue and dizziness and is not to be taken with alcohol
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What are the SE of meprobamate?
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Easy to become addicted
withdrawal will cause seizures Low therapeutic index Toxic when taken with ethanol |
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What is the mechanism of Buspirone
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5HT (serotonin) receptor agonist
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What are the SE at high doses of Buspirone?
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Causes pupil constriction
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What are the barbituates?
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phenobarbital
thiopental amobarbital pentobarbital |
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What is the mechanism of action of barbituates?
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direct activation of GABA receptors or greatly increase the response of receptors to GABA
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What are the sites of action of barbituates?
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CNS
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What is the mechanism of action of phenobarbital?
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direct activation of GABA receptors or greatly increase the response of receptors to GABA
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What is the mechanism of action of thipental?
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direct activation of GABA receptors or greatly increase the response of receptors to GABA
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What is the mechanism of action of amobarbital
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direct activation of GABA receptors or greatly increase the response of receptors to GABA
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What is the mechanism of action of pentobarbital?
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direct activation of GABA receptors or greatly increase the response of receptors to GABA
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What are the properties of barbituates?
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Inhibition of the reticular activating system which will cause sleep
Inhibition of the sensory cortex which will cause one to lose conciousness Acts on the medullary respiratory system and will suppress breathing at high doses HAVE NO EFFECT ON PAIN |
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What is the usual cause of death wtih an overdose of barbituates?
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medullary overdose and breathing will stop
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What effects to barbituates have on the metabolism of other drugs?
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In the love they will strongly induce the P459 system and they are likely to affect other drugs metabolized by the P450 system
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What is the solubility of barbituates?
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they are lipid soluble and will be stored in fatty tissue and continue to be released even have a patient stops taking the drug
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What are the contraindications of barbituates?
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1. Don't want to give a patient with respiratory problems a barbituate because they will have a harder time breathing than they already do
2. Do not want to give a patient with kidney problems a barbituate because it will increase barbituate activity 3. Barbituates can cross through the placenta |
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What is the therapeutic index of barbituates
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10
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Can one become tolerant to barbituates?
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yes, a steady user will need more to get the same affect
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What are some other sleep inducers?
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chloral hydrate, paraldehyde, methaqualone, piperodinediones
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What are the piperidinediones?
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Glutethimide and Thalidomide
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What are the side effects of Thalidomide?
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Cause abnormal development of extremities in fetuses
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What is Thalidomide now used for?
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mulitple myeloma
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What over the counter drugs are used as sleep inducers?
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antihistamies
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